US 201100284.60A1 (19) United States (2) Patent Application Publication (10) Pub. No.: US 2011/0028460 A1 Kisak et al. (43) Pub. Date: Feb. 3, 2011

(54) TOPICAL FORMULATION Publication Classification (75) Inventors: Edward T. Kisak, San Diego, CA (51) Int. Cl. (US); John M. Newsam, La Jolla, A61 K 31/19 (2006.01) CA (US); Dominic King-Smith, A61R 31/195 (2006.01) San Diego, CA (US); Pankaj A61 K 31/40 (2006.01) Karande, Troy, NY (US); Samir A61 K 31/.444 (2006.01) Mitragotri, Goleta, CA (US) A61 K 3.1/541.5 (2006.01) A6IP 29/00 (2006.01) Correspondence Address: FOLEY AND LARDNER LLP (52) U.S. Cl...... 514/226.5: 514/557, 514/567; SUITE 500 514/420; 514/334 3000 K STREET NW WASHINGTON, DC 20007 (US) (57) ABSTRACT (73) Assignee: faubed, Inc. It has been discovered that certain combinations compounds (21) Appl. No.: 12/848,792 are excellent penetration enhancers and, as such, can be incor porated in a topical formulation to facilitate administration of (22) Filed: Aug. 2, 2010 active agents. The increased penetration enhancement can also lead to a reduction in the total concentration of skin Related U.S. Application Data irritants in the formulation. There is described herein a topical formulation comprising (i) at least one active agent; (ii) a first (63) Continuation-in-part of application No. 12/281,561, compound, and (iii) a second compound, wherein the first filed on Jan. 12, 2009, now Pat. No. 7,795,309, filed as compound and second compound are different, and each is application No. PCT/IB2007/001983 on Mar. 6, 2007. selected from the group consisting of N-lauroyl sarcosine, (60) Provisional application No. 60/778,847, filed on Mar. sodium octyl sulfate, methyl laurate, isopropyl myristate, 6, 2006. oleic acid, glyceryl oleate and sodium lauryl sulfoacetate. US 2011/0028460 A1 Feb. 3, 2011

TOPICAL FORMULATION assisted techniques such as iontophoresis or ultrasound, and bypassing the stratum corneum through microneedle arrays CROSS-REFERENCE TO RELATED or ablation. APPLICATIONS [0008] Molecular or chemical penetration enhancers pro vide an effective and inexpensive means of temporarily [0001] This application is a continuation in part of co reducing skin resistance to the passage of actives and other pending U.S. application Ser. No. 12/281,561, filed on Jan. molecules. Molecular penetration enhancers or ‘MPETM’s’ 12, 2009, which is a national stage of PCT/IB20071001983, can enhance the diffusion of molecules across the skin by, for filed on Mar. 6, 2007, which claims priority to U.S. Provi example, disrupting the lipid bilayers of the stratum corneum. sional Application No. 60/778,847, filed on Mar. 6, 2006, the [0009] Over 300 substances have been identified as entire contents and disclosures of each of which are hereby MPETMs but surprisingly few have been successfully devel incorporated by reference. oped into commercial formulations. Many potent MPETMs are irritating to the cells of the epidermis which can limit both FIELD OF THE INVENTION the choice and concentration of MPETMs suitable for topical formulations. [0002] The present invention relates to a topical formula [0010] Discovery of new MPETM’s to increase skin perme tion of multiplexed molecular penetration enhancers. In a ability is highly desirable and has been an area of high activity particularly preferred embodiment, the present invention over the last 30 years. However, the number of substances relates to a topical formulation of multiplexed molecular pen identified to be penetration enhancers is still small relative to etration enhancers for topical or transdermal administration the more than 25,000,000 substances identified in the CAS of one or more active ingredients such as a pharmaceutical registry (Chemical Abstracts Service, Columbus, Ohio, agent. www.cas.orq). [0011] The number of candidate drugs suitable for topical DESCRIPTION OF THE PRIOR ART and transdermal administration could be significantly increased with improved penetration enhancers. [0003] Topical formulations for application to the skin can [0012] One example of a commercialized formulation for be useful in cosmetic applications, for treating conditions of use intransdermal administration is described in U.S. Pat. No. the upper skin layers and for transdermal administration of 4,575,515 [Sandborn]. Sandborn teaches a formulation that active agents to the local tissue underlying the skin orinto the includes a medicine and dimethyl sulfoxide (DMSO), and blood for systemic distribution. Use of a topical formulation that purportedly allows for rapid and deep penetration of the of for instance, a pharmaceutical agent is advantageous in medicine into the underlying tissue. that it avoids firstpass metabolism, circumvents gastrointes [0013] While the topical formulation taught by Sandborn tinal (“GI”) absorption, can allow delivery of an active ingre represents an advance in the art, there is room for improve dient with a relatively short biological half-life and/or a nar ment. For instance the formulation taught by Sandborn con row therapeutic window and facilitates uniform plasma tains a relatively high concentration of DMSO, which is dosing of the active ingredient, and/or can improve user com known to cause skin irritation. In particular there is a need for pliance. a topical formulation having improved flux of the active [0004] In spite of the advantages, transdermal administra ingredient through the skin as compared to the topical formu tion is usually limited to about a dozen small lipophilic drugs, lation taught by Sandborn. available in transdermal patch format (including scopola mine, fentanyl, estradiol, nitroglycerine, nicotine and test SUMMARY OF THE INVENTION osterone). [0014] It is an object of the present invention to provide a [0005] Skin has evolved to impede the flux of exogenous novel topical formulation. molecules so as to provide a strong barrier to molecular [0015] It is another object of the present invention to pro delivery, particularly agents such as pharmaceutical agents. vide a novel topical formulation for topical or transdermal Transdermal drug administration is difficult since skin is an administration of an active agent. excellent diffusion barrier. [0016] It is another object of the present invention to pro [0006] Structurally, the skin consists of two principle parts: vide a topical formulation capable of providing improved (i) a relatively thin outermost layer (the ‘epidermis’), and (ii) fluxes of therapeutically active agents and other molecules a thicker inner region (the ‘dermis’). The outermost layer of through the skin as compared to the topical formulation the epidermis (the ‘stratum corneum’) consists of flattened taught by Sandborn. dead cells which are filled with keratin. The region between [0017] Accordingly, in one of its aspects, the present inven the flattened dead cells of the stratum corneum is filled with tion provides a topical formulation comprising: (i) at least one lipids which form lamellar phases. The highly impermeable active agent, (ii) a first compound, and (iii) a second com nature of skin is due primarily to the stratum corneum. The pound, wherein the first compound and second compound are viable epidermis underlying the stratum corneum is akin to different, and each is selected from the group of MPETMs other living tissue. The dermis provides the skin’s structural consisting of N-lauroyl sarcosine, sodium octyl sulfate, strength as well as the nerve and vascular networks that sup methyl laurate, isopropyl myristate, oleic acid, glyceryl ole port the epidermis. ate and sodium lauryl sulfoacetate. [0007] Delivering an active agent into orthrough the skin in [0018] In another of its aspects, the present invention pro sufficient concentrations often requires some means for vides a topical formulation for use in topical or transdermal reducing the stratum corneum’s hindrance of penetration. A administration of a substance comprising: (i) at least one number of methods for lowering the stratum corneum’s bar active agent, (ii) a first compound, (iii) a second compound, rier properties have been developed, including electrically and (iv) a therapeutically acceptable carrier that is different US 2011/0028460 A1 Feb. 3, 2011 from the first compound and the second compound, wherein enhancercomprising two or more substances wherein each of the first compound and second compound are different, and the two or more substances is also penetration enhancer. each is selected from the group of MPETM's consisting of [0026] The present inventors have surprisingly and unex N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, pectedly discovered that certain combination of compounds isopropyl myristate, oleic acid, glyceryl oleate and sodium are excellent penetration enhancers and, as such, can be incor lauryl sulfoacetate. porated in a topical formulation to facilitate administration of [0019. In yet another of its aspects, the present invention one or more active ingredients. The increased penetration provides a topical formulation comprising a therapeutically enhancement can also lead to a reduction in the total concen active agent, a therapeutically acceptable carrier and a skin tration of skin irritants in a formulation. penetration enhancer, wherein the skin penetration enhancer [0027] The compounds acting as excellent penetration consists essentially of a mixture of N-lauroyl sarcosine and enhancers are used in combination—i.e., two (or more) com oleic acid. pounds are selected from wherein the first compound and second compound are different, and each is selected from the DETAILED DESCRIPTION OF THE PREFERRED group consisting essentially of N-lauroyl sarcosine, sodium EMBODIMENTS octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, [0020) The present invention provides a topical formula glyceryl oleate and sodium lauryl sulfoacetate. tion that may be used for the topical or transdermal adminis [0028] The preferred combinations of compounds that act tration of at least one active agent. As used throughout this as improved penetration enhancers include the following: specification, the term “transdermal” means in the broadest [0029] the first compound comprises N-lauroyl sar sense through the skin. Further the terms “transdermal’ and cosine and the second compound comprises isopropyl ‘percutaneous’ are used interchangeably throughout this myristate; specification. [0030) the first compound comprises N-lauroyl sar [0021] As used herein the term “topical formulation’ refers cosine and the second compound comprises oleic acid; to a formulation that may be applied to skin or a mucosa. [0031] the first compound comprises sodium octyl sul Topical formulations may, for example, be used to confer fate and the second compound comprises oleic acid; therapeutic benefit to a patient or cosmetic benefits to a con [0032] the first compound comprises glyceryl oleate and sumer. Topical formulations can be used for both topical and the second compound comprises sodium octyl sulfate; transdermal administration of substances. [0033] the first compound comprises glyceryl oleate and [0022] The term “topical administration’ is used in its con the second compound comprises methyl laurate; ventional sense to mean delivery of a substance, such as a [0034] the first compound comprises sodium lauryl sul therapeutically active agent, to the skin or a localized region foacetate and the second compound comprises methyl of the body. Topical administration of a drug may often be laurate; and advantageously applied in, for example, the treatment of vari [0035) the first compound comprises sodium lauryl sul ous skin disorders. foacetate and the second compound comprises isopropyl [0023] The term “transdermal administration’ is used to myristate. mean administration through the skin. Transdermal adminis [0036] Preferably, the weight ratio of the first compound to tration is often applied where systemic delivery of an active is the second compound is in the range of from about 1:9 to desired, although it may also be useful for delivering an active about 9:1. More preferably, the weight ratio of the first com to tissues underlying the skin with minimal systemic absorp pound to the second compound is in the range of from about tion. 1:4 to about 4:1. Even more preferably, the weight ratio of the [0024] The term ‘penetration enhancer’ is used herein to first compound to the second compound is in the range of refer to an agent that improves the transport of molecules such from about 1:3 to about 3:1. Even more preferably, the weight as an active agent (e.g., a medicine) into or through the skin. ratio of the first compound to the second compound is in the Various conditions may occur at different sites in the body range of from about 1:2 to about 2:1. Most preferably, the either in the skin or below creating a need to target delivery of weight ratio of the first compound to the second compound is compounds. For example, in products designed to produce about 1:1. artificial tans, delivery of dye substances into the stratum [0037] Preferably, the total concentration of the first com corneum may be advantageous. A psoriasis treatment on the pound and the second compound is up to about 50 wt.% per other hand may require delivery of therapeutic drug levels in unit volume of the formulation. More preferably, the total deeper epidermal tissue. In a treatment for osteoarthritis, concentration of the first compound and the second com delivery of the active agent into deeper underlying joint tissue pound is up to about 40 wt.% per unit volume of the formu may be necessary to achieve therapeutic benefit. In yet other lation. Even more preferably, the total concentration of the applications, for example in hormone replacement therapy, first compound and the second compound is in the range of delivery of drug to the systemic circulation may be an objec from about 1 to about to about 35 wt.% per unit volume of the tive. Thus, a ‘penetration enhancer' may be used to assist in formulation. Even more preferably, the total concentration of the delivery of an active agent directly to the skin or under the first compound and the second compound is in the range lying tissue or indirectly to the site of the disease through offrom about 1 to about to about 30 wt.% per unit volume of systemic distribution. A penetration enhancer may be a pure the formulation. Even more preferably, the total concentra substance or may comprise a mixture of different chemical tion of the first compound and the second compound is in the entities. In this specification the terms ºpenetration enhancer’, range of from about 1 to about to about 25 wt.% per unit ‘chemical penetration enhancer’, ‘molecular penetration volume of the formulation. Even more preferably, the total enhancer’ and ‘MPETM’ are used interchangeably. concentration of the first compound and the second com [0025] As used herein the term ‘multiplexed molecular pound is in the range of from about 1 to about to about 20 wt. penetration enhancers” (“MMPETM”) means a penetration % per unit volume of the formulation. Even more preferably, US 2011/0028460 A1 Feb. 3, 2011

the total concentration of the first compound and the second histamine and/or antipsychotic, specific examples of which compound is in the range offrom about 1 to about to about 15 are listed below. As is known to a person skilled in the art, wt.% per unit volume of the formulation. Even more prefer phenethylamines are chemical compounds having the general ably, the total concentration of the first compound and the core structure of Formula II: second compound is in the range of from about 1 to about to about 10 wt.% per unit volume of the formulation. Even more preferably, the total concentration of the first compound and II the second compound is in the range offrom about 1 to about to about 7.5 wt.% per unit volume of the formulation. Even more preferably, the total concentration of the first compound and the second compound is in the range of from about 1 to about to about 5 wt.% per unit volume of the formulation. [0038] Most preferably, the total concentration of the first wherein the phenyl ring, ethylene chain and nitrogen can be compound and the second compound is in the range of from substituted. The phenethylamine may be a psychoactive about 2 to about to about 5 wt.% per unit volume of the agent that exerts its effect through a monoamine neurotrans formulation. Within this most preferred embodiment, it can, mitter system, for example dopamine, serotonin and/or more in some cases, be preferable to have the total concentration of pinephrine receptors. Examples of phenethylamines, include, the first compound and the second compound in the range of for example, bupropion, amphetamine, hydroxyamphet from about 2 to about to about 4 wt.% per unit volume of the amine, dextroamphetamine, methamphetamine, ephedrine, formulation. epinephrine, pseudoephedrine, dopamine, epinephryl borate, [0039] In one aspect of the present invention, the at least etafedrine, norepinephrine and oxidopamine, and pharma one active agent is an aryl alkanoic acid, such as an O-aryl ceutically acceptable salts and solvates thereof, and mixtures alkanoic acid. As is known to a person skilled in the art, C-aryl thereof. Preferably the phenethylamine is bupropion, or a alkanoic acids are chemical compounds having the general pharmaceutically acceptable salt or solvate thereof, such as structure of Formula I; bupropion hydrochloride. The structure of bupropion, known to a person skilled in the art, is:

Ar O

R! OH wherein Ar is an aryl group and R' is H or an alkyl group, wherein aryl includes aromatic and heteroaromatic groups and alkyl includes acyclic and cyclic alkyl groups. The O-aryl alkanoic acid may be an anti-inflammatory drug such as a non-steroidal anti-inflammatory drug (NSAID) or an analge [0041] In another aspect of the present invention, the at sic, specific examples of which are listed below. Preferably, least one active agent is a steroid, for example, steroids that the C-aryl alkanoic acids is selected from the group consisting are hormones, glucosteroids, androgens, adrenocortical ste of bromfenac, diclofenac, fenoprofen, flurbiprofen, ibupro roids, anabolics, estrogens and/or progestin, specific fen, indomethacin, ketoprofen, ketorolac, naproxen, sulindac examples of which are listed below. As known to a person and tolmetin, and pharmaceutically acceptable salts and sol skilled in the art, steroids are a class of compounds having as vates thereof and mixtures thereof. Structures for these O-aryl a core structure, 4 rings joined as shown in Formula III: alkanoic acids, along with some common trade names, known to a person skilled in the art, are shown in Table 1. More preferably the C-aryl alkanoic acid is selected from the group III consisting of diclofenac, ibuprofen and ketoprofen, and phar maceutically acceptable salts and solvates thereof, and mix tures thereof. Other NSAIDs, that are not cº-aryl alkanoic acids, as well as other compounds having antipyretic and analgesic actions are also included in the scope of the present invention. Examples of such compounds include, acetami nophen (paracetamol), aspirin, celecoxib, diflunisal, etod olac, etoricoxib, meclofenamic acid, mefenamic acid, wherein the carbon atoms are optionally substituted. Prefer meloxicam, nabumetone, oxaprozin, piroxicam, salsalate, ably the steroid is testosterone, or a pharmaceutically accept and rofecoxib. Structures for these compounds along with able salt or solvate thereof. some common trade names, known to a person skilled in the [0042] Other suitable active agents include those in the art, are shown in Table 2. class of COX-2 inhibitors such as celecoxib, rofecoxib, val [0040] In another aspect of the present invention, the at decoxib, lumiracoxib, etoricoxib; Antifungals such as tolnaf least one active agent is a phenethylamine, for example, a tate, econazole, ciclopirox, Antibiotics such as clindamycin; phenethylamine that is an antidepressant, anti-anxiety agent, Musculoskeletal agents such as dantrolene; Retinoids such as anticholinergic agent, cholinergic, dopaminergic, stimulant, isotretinoin; Antivirals such as acyclovir, Vasodilating agents serotonin antiagonist, serotonin inhibitor, anti-emetic, anti such as nitroglycerine, papaverine; Hormones and synthetic US 2011/0028460 A1 Feb. 3, 2011 substitutes such as androgens, estrogens, insulin; Opiate ago [0046] Adrenocortical steroid: Ciprocinonide; Desoxycor nist such as fentanyl, oxycodone, hydromorphone; Local ticosterone Acetate; Desoxycorticosterone Pivalate; Dexam Anaesthetics such as lidocaine, tocainide and mexiletine and ethasone Acetate: Fludrocortisone Acetate: Flumoxonide; butyl-para-aminobenzoate; Anti-inflammatories such as cor Hydrocortisone Hemisuccinate; Methylprednisolone ticosteroids; NMDA receptor antagonists such as ketamine, Hemisuccinate; Naflocort; Procinonide; Timobesone dextromethorphan and amantadine. Acetate; and Tipredane. [0043] Examples of other therapeutically active agents that [0047] Adrenocortical suppressant: Aminoglutethimide; may be used include the following: adrenergic agent; adreno and Trilostane. [0048] Alcohol deterrent: Disulfiram. cortical steroid; adrenocortical suppressant; aldosterone [0049) Aldosterone antagonist: Canrenoate Potassium; antagonist; amino acid; anabolic; analeptic; analgesic; anes Canrenone; Dicirenone; Mexrenoate Potassium; Prorenoate thetic; anorectic; anti-acne agent; anti-adrenergic; anti-aller Potassium; and Spironolactone. gic; anti-amebic; anti-anemic; anti-anginal; anti-arthritic; [0050] Amino acid: Alanine; Arginine; Aspartic Acid; Car anti-asthmatic; anti-atherosclerotic; antibacterial; anticholin mitine; Cysteine Hydrochloride; Cystine; Glycine; Histidine; ergic; anticoagulant; anticonvulsant; antidepressant; antidia Isoleucine; Leucine; Lysine; Lysine Acetate; Lysine Hydro betic; antidiarrheal; antidiuretic; anti-emetic; anti-epileptic; chloride; Methionine; Phenylalanine; Proline; Serine; Threo antifibrinolytic; antifungal; antihemorrhagic; antihistamine; nine; Tryptophan; Tyrosine; and Valine. antihyperlipidemia; antihypertensive; antihypotensive; anti [0051] Ammonia detoxicant: Arginine Glutamate; and infective; anti-inflammatory; antimicrobial; antimigraine; Arginine Hydrochloride. antimitotic; antimycotic, antinauseant, antineoplastic, [0052] Amyotrophic lateral sclerosis agents: Riluzole antineutropenic, antiparasitic; antiproliferative; antipsy [0053] Anabolic: Bolandiol Dipropionate; Bolasterone; chotic; antirheumatic; antiseborrheic; antisecretory; antis Boldenone Undecylenate; Bolenol; Bolmantalate; Ethyl pasmodic; antithrombotic; antiulcerative; antiviral; appetite estrenol; Methenolone Acetate; Methenolone Enanthate: suppressant; blood glucose regulator, bone resorption inhibi Mibolerone; Nandrolone Cyclotate; Norbolethone; Pizoty tor; bronchodilator; cardiovascular agent; cholinergic; line; Quinbolone; Stenbolone Acetate; Tibolone; and Zera depressant; diagnostic aid; diuretic; dopaminergic agent; mol. estrogen receptoragonist; fibrinolytic; fluorescent agent; free [0054] Analeptic: Modafinil. oxygen radical scavenger; gastric acid suppressant; gas [0055] Analgesic: Acetaminophen; Alfentanil Hydrochlo trointestinal motility effector; glucocorticoid; hair growth ride; Aminobenzoate Potassium; Aminobenzoate Sodium; stimulant; hemostatic; histamine H2 receptor antagonists; Anidoxime; Anileridine; Anileridine Hydrochloride; Anilo hormone; hypocholesterolemic; hypoglycemic, hypolipi pam Hydrochloride; Anirolac, Antipyrine; Aspirin; Benox demic; hypotensive; imaging agent; immunizing agent; aprofen; Benzydamine Hydrochloride; Bicifadine Hydro immunomodulator; immunoregulator; immunostimulant; chloride; Brifentanil Hydrochloride; Bromadoline Maleate; immunosuppressant, keratolytic; LHRH agonist; mood regu Bromfenac Sodium; Buprenorphine Hydrochloride; Butace lator; mucolytic; mydriatic; nasal decongestant; neuromus tin; Butixirate; Butorphanol; Butorphanol Tartrate; Carbam cular blocking agent; neuroprotective; NMDA antagonist; azepine; Carbaspirin Calcium; Carbiphene Hydrochloride; non-hormonal sterol derivative; plasminogen activator; plate Carfentanil Citrate; Ciprefadol Succinate; Ciramadol; Cira let activating factorantagonist; platelet aggregation inhibitor; madol Hydrochloride; Clonixeril; Clonixin; Codeine; psychotropic; radioactive agent; scabicide; sclerosing agent; Codeine Phosphate; Codeine Sulfate; Conorphone Hydro sedative; sedative-hypnotic; selective adenosine Al antago chloride; Cyclazocine; Dexoxadrol Hydrochloride; Dex nist; serotonin antagonist; serotonin inhibitor; serotonin pemedolac, Dezocine; Diflunisal; Dihydrocodeine Bitartrate; receptor antagonist; steroid; thyroid hormone; thyroid inhibi Dimefadane; Dipyrone; Doxpicomine Hydrochloride; Drin tor; thyromimetic, tranquilizer; amyotrophic lateral sclerosis idene; Enadoline Hydrochloride: Epirizole; Ergotamine Tar agent; cerebral ischemia agent; Paget’s disease agent; trate; Ethoxazene Hydrochloride; Etofenamate; Eugenol; unstable angina agent; vasoconstrictor; vasodilator; wound Fenoprofen; Fenoprofen Calcium; Fentanyl Citrate; Floc healing agent; xanthine oxidase inhibitor; and the like. tafenine; Flufenisal; Flumixin; Flumixin Meglumine; Flupir [0044) Specific examples of pharmaceutical agents that time Maleate; Fluproduazone; Fluradoline Hydrochloride; may be included within the present topical formulation, both Flurbiprofen; Hydromorphone Hydrochloride; Ibufenac; alone or in combination, include but are not limited to: Indoprofen; Ketazocine; Ketorfanol: Ketorolac [0045] Adrenergic: Adrenalone; Amidephrine Mesylate; Tromethamine; Letimide Hydrochloride; Levomethadyl Apraclonidine Hydrochloride; Brimonidine Tartrate; Acetate; Levomethadyl Acetate Hydrochloride; Levonantra Dapiprazole Hydrochloride; Deterenol Hydrochloride; dol Hydrochloride; Levorphanol Tartrate; Lofemizole Dipivefrin; Dopamine Hydrochloride; Ephedrine Sulfate; Hydrochloride; Lofentanil Oxalate; Lorcinadol; Lornoxi Epinephrine; Epinephrine Bitartrate; Epinephryl Borate; cam; Magnesium Salicylate; Mefenamic Acid; Menabitan Esproduin Hydrochloride; Etafedrine Hydrochloride; Hydrochloride; Meperidine Hydrochloride; Meptazinol Hydroxyamphetamine Hydrobromide; Levonordefrin; Hydrochloride; Methadone Hydrochloride; Methadyl Mephentermine Sulfate; Metaraminol Bitartrate; Metizoline Acetate; Methopholine; Methotrimeprazine; Metkephamid Hydrochloride; Naphazoline Hydrochloride; Norepinephrine Acetate; Mimbane Hydrochloride; Mirfentanil Hydrochlo Bitartrate; Oxidopamine; Oxymetazoline Hydrochloride; ride; Molinazone; Morphine Sulfate; Moxazocine; Nabitan Phenylephrine Hydrochloride; Phenylpropanolamine Hydro Hydrochloride; Nalbuphine Hydrochloride; Nalmexone chloride; Phenylpropanolamine Polistirex, Prenalterol Hydrochloride; Namoxyrate; Nantradol Hydrochloride; Hydrochloride; Propylhexedrine; Pseudoephedrine Hydro Naproxen; Naproxen Sodium; Naproxol; Nefopam Hydro chloride; Tetrahydrozoline Hydrochloride; Tramazoline chloride; Nexeridine Hydrochloride; Noracymethadol Hydrochloride; and Xylometazoline Hydrochloride. Hydrochloride; Oc?entanil Hydrochloride; Octazamide; US 2011/0028460 A1 Feb. 3, 2011

Olvanil; Oxetorone Fumarate; Oxycodone; Oxycodone Oxmetidine Mesylate; Quadazocine Mesylate; Ranitidine; Hydrochloride; Oxycodone Terephthalate; Oxymorphone Ranitidine Bismuth Citrate; Ranitidine Hydrochloride; Sufo Hydrochloride; Pemedolac, Pentamorphone; Pentazocine; tidine; Teludipine Hydrochloride; Tiapamil Hydrochloride; Pentazocine Hydrochloride; Pentazocine Lactate; Tiotidine; Vapiprost Hydrochloride; and Zaltidine Hydro Phenazopyridine Hydrochloride; Phenyramidol Hydrochlo chloride. ride; Picenadol Hydrochloride; Pinadoline; Pirfenidone; [0062] Anterior pituitary activator: Epimestrol. Piroxicam Olamine; Pravadoline Maleate; Prodilidine [0063] Anterior pituitary suppressant: Danazol. Hydrochloride; Profadol Hydrochloride; Propiram Fuma [0064] Anthelmintic: Albendazole; Anthelmycin; Bromox rate; Propoxyphene Hydrochloride; Propoxyphene Napsy anide; Bunamidine Hydrochloride; Butonate; Cambenda late; Proxazole; Proxazole Citrate; Proxorphan Tartrate; Pyr zole; Carbantel Lauryl Sulfate; Clioxanide; Closantel; roliphene Hydrochloride; Remifentanil Hydrochloride; Cyclobendazole; Dichlorvos; Diethylcarbamazine Citrate; Salcolex, Salicylamide; Salicylate Meglumine; Salsalate; Dribendazole; Dymanthine Hydrochloride; Etibendazole; Sodium Salicylate; Spiradoline Mesylate; Sufentanil; Sufen Fenbendazole; Furodazole, Hexylresorcinol; Mebendazole; tanil Citrate; Talmetacin; Talniflumate; Talosalate: Tazad Morantel Tartrate; Niclosamide; Nitramisole Hydrochloride; olene Succinate; Tebufelone; Tetrydamine; Tifurac Sodium; Nitrodan: Oxantel Pamoate; Oxfendazole; Oxibendazole; Tilidine Hydrochloride; Tiopinac; Tonazocine Mesylate; Tra Parbendazole; Piperamide Maleate; Piperazine; Piperazine madol Hydrochloride; Trefer?tanil Hydrochloride; Trola Citrate; Piperazine Edetate Calcium; Proclonol; Pyrantel mine; Veradoline Hydrochloride; Verilopam Hydrochloride; Pamoate; Pyrantel Tartrate; Pyrvinium Pamoate; Rafoxanide; Volazocine; Xorphanol Mesylate; Xylazine Hydrochloride; Stilbazium Iodide; Tetramisole Hydrochloride; Thiabenda Zomepirac Sodium; and Zucapsaicin. zole; Ticarbodine; Tioxidazole; Triclofenol Piperazine; Vin [0056] Androgen: Fluoxymesterone; Mesterolone; Meth cofos; and Zilantel. yltestosterone; Nandrolone Decanoate; Nandrolone Phen [0065] Anti-acne: Adapalene; Erythromycin, Salmacedin; propionate; Nisterime Acetate; Oxandrolone; and Inocoterone Acetate. Oxymetholone; Silandrone; Stanozolol; Testosterone; Test [0066] Anti-adrenergic: Acebutolol; Alprenolol Hydro osterone Cypionate; Testosterone Enanthate; Testosterone chloride; Atenolol; Bretylium Tosylate; Bunolol Hydrochlo Ketolaurate; Testosterone Phenylacetate; Testosterone Propi ride; Carteolol Hydrochloride; Celiprolol Hydrochloride; onate; Trestolone Acetate. Cetamolol Hydrochloride: Cicloprolol Hydrochloride; Dex [0057] Anesthesia (adjunct to): Sodium Oxybate. propranolol Hydrochloride; Diacetolol Hydrochloride; Dihy [0058] Anesthetic: Aliflurane; Benoximate Hydrochloride; droergotamine Mesylate; Dilevalol Hydrochloride; Esmolol Benzocaine; Biphenamine Hydrochloride; Bupivacaine Hydrochloride; Exaprolol Hydrochloride; Fenspiride Hydro Hydrochloride; Butamben; Butamben Picrate; Chlorop chloride; Flestolol Sulfate; Labetalol Hydrochloride; Levo rocaine Hydrochloride; Cocaine; Cocaine Hydrochloride; betaxolol Hydrochloride; Levobunolol Hydrochloride; Met Cyclopropane; Desflurane; Dexivacaine; Diamocaine Cycla alol Hydrochloride; Metoprolol; Metoprolol Tartrate; mate; Dibucaine; Dibucaine Hydrochloride; Dyclonine Nadolol; Pamatolol Sulfate; Penbutolol Sulfate; Phentola Hydrochloride; Enflurane; Ether; Ethyl Chloride; Etidocaine; mine Mesylate; Practolol; Propranolol Hydrochloride; Etoxadrol Hydrochloride; Euprocin Hydrochloride; Flurox Proroxan Hydrochloride; Solypertine Tartrate; Sotalol ene; Halothane; Isobutamben; Isoflurane; Ketamine Hydro Hydrochloride; Timolol; Timolol Maleate; Tiprenolol chloride; Levoxadrol Hydrochloride; Lidocaine; Lidocaine Hydrochloride; Tolamolol; and Zolertine Hydrochloride. Hydrochloride; Mepivacaine Hydrochloride; Methohexital [0067] Anti-allergic: Amlexanox; Astemizole; Azelastine Sodium; Methoxyflurane; Midazolam Hydrochloride; Mida Hydrochloride; Eclazolast; Minocromil Nedocromil zolam Maleate; Minaxolone; Norflurane; Octodrine; Oxet Nedocromil Calcium; Nedocromil Sodium; Nivinmedone hazaine; Phencyclidine Hydrochloride; Pramoxine Hydro Sodium; Pemirolast Potassium Pentigetide; Pirquinozol; Poi chloride; Prilocaine Hydrochloride; Procaine Hydrochloride; sonoak Extract; Probicromil Calcium; Proxicromil: Repiri Propanidid; Proparacaine Hydrochloride; Propofol; Pro nast; Tetrazolast Meglumine; Thiazinamium Chloride; Tiac poxycaine Hydrochloride; Pyrrocaine; Risocaine; rilast; Tiacrilast Sodium; Tiprinast Meglumine; and Tixanox. Rodocaine; Roflurane; Salicyl Alcohol; Sevoflurane; Teflu [0068] Anti-amebic: Berythromycin; Bialamicol Hydro rane; Tetracaine; Tetracaine Hydrochloride; Thiamylal; Thia chloride; Chloroquine; Chloroquine Hydrochloride; Chloro mylal Sodium; Thiopental Sodium; Tiletamine Hydrochlo quine Phosphate; Clamoxyquin Hydrochloride; Clioquinol; ride; and Zolamine Hydrochloride. Emetime Hydrochloride; Iodoquinol; Paromomycin Sulfate; [0059] Anorectic compound: Dexfenfluramine. Quinfamide; Symetime Hydrochloride; Teclozan; Tetracy [0060] Anorexic agents: Aminorex: Amphecloral; Chlor cline; and Tetracycline Hydrochloride. phentermine Hydrochloride; Clominorex; Clortermine [0069] Anti-androgen: Benorterone; Cioteronel; Cyproter Hydrochloride; Diethylpropion Hydrochloride; Fenflu one Acetate; Delmadinone Acetate; Oxendolone; Topterone; ramine Hydrochloride; Fenisorex, Fludorex, Fluminorex, and Zanoterone. Levamfetamine Succinate; Mazindol; Mefenorex Hydro [0070] Anti-anemic: Epoetin Alfa; Epoetin Beta; Ferrous chloride; Phemnetrazine Hydrochloride; Phentermine; and Sulfate, Dried; and Leucovorin Calcium. Sibutramine Hydrochloride. [0071] Anti-anginal: Amlodipine Besylate; Amlodipine [0061] Antagonist: Atipamezole; Atosiban; Bosentan; Maleate; Betaxolol Hydrochloride; Bevantolol Hydrochlo Cimetidine, Cimetidine Hydrochloride; Clentiazem Maleate; ride; Butoprozine Hydrochloride; Carvedilol; Cinepazet Detirelix Acetate; Devazepide; Donetidine; Etintidine Maleate; Metoprolol Succinate; Molsidomine; Monatepil Hydrochloride; Famotidine; Fenmetozole Hydrochloride; Maleate; Primidolol; Ranolazine Hydrochloride; Tosifen; Flumazenil; Icatibant Acetate; Icotidine; Isradipine; Metia and Verapamil Hydrochloride. mide; Nadide; Nalmefene; Naloxone Hydrochloride; Naltr [0072] Anti-anxiety agent: Adatanserin Hydrochloride; exone; Nilvadipine; Oxilorphan: Oxmetidine Hydrochloride; Alpidem; Binospirone Mesylate; Bretazenil; Glemanserin; US 2011/0028460 A1 Feb. 3, 2011

Ipsapirone Hydrochloride; Mirisetron Maleate; Ocinaplon; Hydrochloride; Erythromycin; Erythromycin Acistrate; Ondansetron Hydrochloride; Panadiplon; Pancopride; Pazi Erythromycin Estolate; Erythromycin Ethylsuccinate; Eryth naclone; Serazapine Hydrochloride; Tandospirone Citrate; romycin Gluceptate; Erythromycin Lactobionate; Erythro and Zalospirone Hydrochloride. mycin Propionate; Erythromycin Stearate; Ethambutol [0073] Anti-arthritic: Lodelaben. Hydrochloride; Ethionamide; Fleroxacin; Floxacillin; Flu [0074] Anti-asthmatic: Ablukast, Ablukast Sodium; dalanine; Flumequine; F osfomycin; F osfomycin Bunaprolast; Cinalukast, Cromitrile Sodium; Cromolyn Tromethamine; Fumoxicillin; Furazolium Chloride; Furazo Sodium; Enofelast; Isamoxole; Ketotifen Fumarate; Levcro lium Tartrate; Fusidate Sodium; Fusidic Acid; Gentamicin makalim; Lodoxamide Ethyl; Lodoxamide Tromethamine; Sulfate; Gloximonam; Gramicidin; Haloprogin; Hetacillin; Montelukast Sodium; Ontazolast: Oxarbazole; Oxatomide: Hetacillin Potassium; Hexedine; Ibafloxacin; Imipenem; Piriprost; Piriprost Potassium; Pirolate; Pobilukast Edamine; Isepamicin; Isoconazole; Isoniazid; Josamycin; Kanamycin Quazolast; Ritolukast; Sulukast, Tiaramide Hydrochloride; Sulfate; Kitasamycin; Levofuraltadone; Levopropylcillin Tibenelast Sodium; Tomelukast; Tranilast; Verlukast; and Potassium; Lexithromycin; Lincomycin; Lincomycin Verofylline Zarirlukast. Hydrochloride; Lomefloxacin; Lomefloxacin Hydrochlo [0075] Anti-atherosclerotic: Mifobate; and Timefuronc. ride; Lomefloxacin Mesylate; Loracarbef: Mafenide; Meclo [0076] Antibacterial: Acedapsone; Acetosulfone Sodium; cycline; Meclocycline Sulfosalicylate; Megalomicin Potas Alamecin; Alexidine, Amdinocillin; Amdinocillin Pivoxil; sium Phosphate; Mequidox; Meropenem; Methacycline; Amicycline; Amifioxacin; Amifloxacin Mesylate; Amikacin; Methacycline Hydrochloride; Methenamine; Methenamine Amikacin Sulfate; Aminosalicylate sodium; Aminosalicylic Hippurate; Methenamine Mandelate; Methicillin Sodium; acid; Amoxicillin; Amphomycin; Ampicillin; Ampicillin Metioprim; Metronidazole Hydrochloride; Metronidazole Sodium; Apalcillin Sodium; Apramycin; Aspartocin; Astro Phosphate; Mezlocillin; Mezlocillin Sodium; Minocycline; micin Sulfate; A vilamycin; A voparcin; Azithromycin; Minocycline Hydrochloride; Mirincamycin Hydrochloride; Azlocillin; Azlocillin Sodium; Bacampicillin Hydrochloride; Monensin; Monensin Sodium; Na?cillin Sodium; Nalidixate Bacitracin; Bacitracin Methylene Disalicylate; Bacitracin Sodium; Nalidixic Acid; Natamycin; Nebramycin; Neomy Zinc, Bambermycins; Benzoylpas Calcium; Betamicin Sul cin Palmitate; Neomycin Sulfate; Neomycin Undecylenate; fate; Biapenem; Biniramycin; Bispyrithione Magsulfex, Netilmicin Sulfate; Neutramycin; Nifarthiazole; Nifuradene; Butikacin; Butirosin Sulfate; Capreomycin Sulfate; Carba Nifuraldezone; Nifuratel; Nifuratrone; Nifurdazil; Nifurim dox; Carbenicillin Disodium; Carbenicillin Indanyl Sodium; ide; Nifurpirinol; Nifurduinazol; Nitrocycline; Nitrofuran Carbenicillin Phenyl Sodium; Carbenicillin Potassium; toin: Nitromide: Norfloxacin; Novobiocin Sodium: Ofloxa Carumonam Sodium; Cefaclor; Cefadroxil; Cefamandole; cin; Onnetoprim; Oxacillin Sodium; Oximonam; Oximonam Cefamandole Nafate; Cefamandole Sodium; Cefaparole; Sodium; Oxolinic Acid: Oxytetracycline; Oxytetracycline Cefatrizine; Cefazaflur Sodium; Cefazolin; Cefazolin Calcium; Oxytetracycline Hydrochloride; Paldimycin; Sodium; Cefbuperazone; Cefdinir, Cefepime; Cefepime Parachlorophenol; Paulomycin; Pefloxacin; Pefloxacin Hydrochloride; Cefetecol; Cefixime; Cefnmenoxime Hydro Mesylate; Penamecillin; Penicillin G Benzathine; Penicillin chloride; Cefnmetazole; Cefnmetazole Sodium; Cefonicid G. Potassium; Penicillin G Procaine; Penicillin G Sodium; Monosodium; Cefonicid Sodium; Cefoperazone Sodium; Penicillin V; Penicillin V Benzathine; Penicillin V Hydrab Ceforamide: Cefotaxime Sodium; Cefotetan: Cefotetan Diso amine; Penicillin V Potassium; Pentizidone Sodium; Phenyl dium; Cefotiam Hydrochloride; Cefoxitin; Cefoxitin Aminosalicylate; Piperacillin Sodium; Pirbenicillin Sodium; Sodium; Ce?pimizole; Ce?pimizole Sodium; Ce?piramide; Piridicillin Sodium; Pirlimycin Hydrochloride; Pivampicillin Cefniramide Sodium; Ce?pirome Sulfate; Ce?podoxime Hydrochloride; Pivampicillin Pamoate; Pivampicillin Proxetil: Ce?prozil; Cefroxadine; Cefsulodin Sodium; Probenate; Polymyxin B Sulfate; Porfiromycin; Propikacin; Ceftazidime; Ceftibuten; Ceftiroxime Pivoxetil: Ceftizoxime Pyrazinamide; Pyrithione Zinc, Quindecamine Acetate; Sodium; Ceftriaxone Sodium; Cefuroxime; Cefuroxime Quinupristin; Racephenicol; Ramoplanin; Ranimycin; Relo Axetil: Cefuroxime Sodium; Cephacetrile Sodium; Cephal mycin; Repromicin; Rifabutin; Rifametane; Rifamexil; Rifa exin; Cephalexin Hydrochloride; Cephaloglycin; Cephalori mide; Rifampin; Rifapentine; Rifaximin; Rolitetracycline; dine; Cephalothin Sodium; Cephapirin Sodium; Cephradine; Rolitetracycline Nitrate; Rosaramicin; Rosaramicin Cetocycline Hydrochloride; Cetophenicol; Chlorampheni Butyrate; Rosaramicin Propionate; Rosaramicin Sodium col; Chloramphenicol Palmitate; Chloramphenicol Pantoth Phosphate; Rosaramicin Stearate; Rosoxacin; Roxarsone; enate Complex; Chloramphenicol Sodium Succinate; Chlo Roxithromycin; Sancycline; Sanfetrinem Sodium; Sarmox rhexidine Phosphanilate; Chloroxylenol; Chlortetracycline icillin; Sarpicillin; Scopafungin; Sisomicin; Sisomicin Sul Bisulfate; Chlortetracycline Hydrochloride; Cinoxacin; fate; Sparfloxacin; Spectinomycin Hydrochloride; Spiramy Ciprofloxacin; Ciprofloxacin Hydrochloride; Cirolemycin; cin; Stallimycin Hydrochloride; Steffimycin; Streptomycin Clarithromycin; Clinafloxacin Hydrochloride; Clindamycin; Sulfate; Streptonicozid; Sulfabenz, Sulfabenzamide; Sulfac Clindamycin Hydrochloride; Clindamycin Palmitate Hydro etamide; Sulfacetamide Sodium; Sulfacytine; Sulfadiazine; chloride; Clindamycin Phosphate; Clofazimine; Cloxacillin Sulfadiazine Sodium; Sulfadoxine, Sulfalene; Sulfamera Benzathine; Cloxacillin Sodium; Cloxyquin; Colistimethate zine; Sulfameter; Sulfamethazine; Sulfamethizole; Sul Sodium; Colistin Sulfate; Coumermycin; Coumermycin famethoxazole; Sulfamonomethoxine; Sulfamoxole, Sulfa Sodium; Cyclacillin; Cycloserine; Dalfopristin; Dapsone; nilate Zinc, Sulfanitran; Sulfasalazine; Sulfasomizole; Daptomycin; Demeclocycline; Demeclocycline Hydrochlo Sulfathiazole; Sulfazamet; Sulfisoxazole; Sulfisoxazole ride; Demecycline; Denofungin; Diaveridine; Dicloxacillin; Acetyl; Sulfisoxazole Diolamine; Sulfomyxin; Sulopenem; Dicloxacillin Sodium; Dihydrostreptomycin Sulfate; Dipy Sultamicillin; Suncillin Sodium; Talampicillin Hydrochlo rithione; Dirithromycin; Doxycycline; Doxycycline Cal ride; Teicoplanin; Temafloxacin Hydrochloride; Temocillin; cium; Doxycycline Fos?atex; Doxycycline Hyclate; Droxa Tetracycline Phosphate Complex; Tetroxoprim; Thiampheni cin Sodium; Enoxacin; Epicillin; Epitetracycline col; Thiphencillin Potassium; Ticarcillin Cresyl Sodium; US 2011/0028460 A1 Feb. 3, 2011

Ticarcillin Disodium; Ticarcillin Monosodium; Ticlatone; Hydrochloride; Bipenamol Hydrochloride; Bupropion Tiodonium Chloride; Tobramycin; Tobramycin Sulfate; Hydrochloride; Butriptyline Hydrochloride; Caroxazone; Tosufloxacin; Trimethoprim; Trimethoprim Sulfate; Trisul Cartazolate: Ciclazindol; Cidoxepin Hydrochloride; Cilo fapyrimidines; Troleandomycin; Trospectomycin Sulfate; bamine Mesylate; Clodazon Hydrochloride; Clomipramine Tyrothricin; Vancomycin; Vancomycin Hydrochloride; Vir Hydrochloride; Cotinine Fumarate; Cyclindole; Cypenamine giniamycin; and Zorbamycin. Hydrochloride; Cyprolidol Hydrochloride; Cyproximide; [0077] Anti-cancer supplementary potentiating agents: Daledalin Tosylate; Dapoxetine Hydrochloride; Dazadrol Amitryptyline; Amoxapine; Amphotericin B; Antiarrhythmic Maleate; Dazepinil Hydrochloride; Desipramine Hydrochlo drugs (e.g., Quinidine); Antihypertensive drugs (e.g., Reser ride; Dexamisole; Deximafen; Dibenzepin Hydrochloride; pine); Ca++ antagonists (e.g., Verapamil; Calmodulin inhibi Dioxadrol Hydrochloride; Dothiepin Hydrochloride; Dox tors (e.g., Prenylamine; Caroverine); Citalopram); Clomi epin Hydrochloride; Duloxetine Hydrochloride; Eclanamine pramine; Clomipramine); Desipramine; Doxepin; Maleate; Encyprate; Etoperidone Hydrochloride; Fantridone Maprotiline); Nifedipine; Nitrendipine; Non-tricyclic anti Hydrochloride; Femmetramide; Fezolamine Fumarate; Flu depressant drugs (e.g., Sertraline; Nortriptyline; Protrip otracen Hydrochloride; Fluoxetine; Fluoxetine Hydrochlo tyline; Sulfoximine) and Multiple Drug Resistance reducing ride; Fluparoxan Hydrochloride; Gamfexine; Guanoxyfen agents such as Cremaphor EL; Thiol depleters (e.g., Buthion Sulfate; Imafen Hydrochloride; Imiloxan Hydrochloride; ine; Trazodone; Tricyclic anti-depressant drugs (e.g., Imi Imipramine Hydrochloride; Indeloxazine Hydrochloride; pramine; Trifluoroperazine; Trimipramine; and Triparanol Intriptyline Hydrochloride; Iprindole; Isocarboxazid: analogues (e.g., Tamoxifen). Ketipramine Fumarate; Lofepramine Hydrochloride; Lorta [0078] Anticholelithic: Monoctanoin. lamine; Maprotiline; Maprotiline Hydrochloride; Melitracen [0079| Anticholelithogenic: Chenodiol; Ursodiol. Hydrochloride; Minaprine Hydrochloride; Mirtazapine; [0080] Anticholinergic: Alverinc Citrate; Anisotropine Moclobemide; Modaline Sulfate; Napactadine Hydrochlo Methylbromide; Atropine; Atropine Oxide Hydrochloride; ride; Napamezole Hydrochloride; Nefazodone Hydrochlo Atropine Sulfate; Belladonna; Benapryzine Hydrochloride; ride; Nisoxetine; Nitrafudam Hydrochloride; Nomifensine Benzetimide Hydrochloride; Benzilonium Bromide; Maleate; Nortriptyline Hydrochloride; Octriptyline Phos Biperiden; Biperiden Hydrochloride; Biperiden Lactate; Cli phate; Opipramol Hydrochloride; Oxaprotiline Hydrochlo dinium Bromide; Cyclopentolate Hydrochloride; Dexetim ride; Oxypertine; Paroxetine; Phenelzine Sulfate; Piran ide; Dicyclomine Hydrochloride; Dihexyverine Hydrochlo damine Hydrochloride; Pride fine Hydrochloride; Prolintane ride; Domazoline Fumarate; Elantrine; Elucaine; Hydrochloride; Protriptyline Hydrochloride; Quipazine Ethybenztropine; Eucatropine Hydrochloride; Glycopyrro Maleate; Rolicyprine; Seproxetine Hydrochloride; Sertraline late: Heteronium Bromide; Homatropine Hydrobromide; Hydrochloride; Sulpiride; Suritozole; Tametraline Hydro Homatropine Methylbromide; Hyoscyamine; Hyoscyamine chloride; Tampramine Fumarate; Tandamine Hydrochloride; Hydrobromide; Hyoscyamine Sulfate; Isopropamide Iodide; Thiazesim Hydrochloride; Thozalinone; Tomoxetine Hydro Mepenzolate Bromide; Methylatropine Nitrate; Meto chloride; Trazodone Hydrochloride; Trebenzomine Hydro quizine; Oxybutynin Chloride; Parapenzolate Bromide; Pen chloride; Trimipramine Maleate; Venlafaxine Hydrochloride; tapiperium Methylsulfate; Phencarbamide; Poldine Methyl Viloxazine Hydrochloride; Zimeldine Hydrochloride; and sulfate; Proglumide; Propantheline Bromide; Propenzolate Zometapine. Hydrochloride; Scopolamine Hydrobromide; Tematropium [0085| Antidiabetic: Acetohexamide; Buformin; Butoxam Methylsulfate; Tiquinamide Hydrochloride; Tofenacin ine Hydrochloride; Camighbose; Chlorpropamide; Ciglita Hydrochloride; Toquizine; Triampyzine Sulfate; Trihex zone; Englitazone Sodium; Etoformin Hydrochloride; Glia yphenidyl Hydrochloride; and Tropicamide. milide; Glibornuride; Glicetanile Sodium; Gliflumide: [0081] Anticoagulant: Ancrod; Ardeparin Sodium; Biva Glipizide, Glucagon; Glyburide; Glyhexamide; Glymidine lirudin; Bromindione; Dalteparin Sodium Desirudin; Dicu Sodium; Glyoctamide; Glyparamide; Insulin; Insulin marol; Lyapolate Sodium; Nafamostat Mesylate; Phenproc Human; Insulin Human Zinc, Insulin Human Zinc, Extended; oumon; Tinzaparin Sodium; and Warfarin Sodium. Insulin Human, Isophane; Insulin Lispro; Insulin Zinc, Insu [0082] Anticoccidal: Maduramicin. lin Zinc, Extended; Insulin Zinc, Prompt; Insulin, Dalanated; [0083] Anticonvulsant: Albutoin: Ameltolide; Atolide; Insulin, Isophane; Insulin, Neutral; Linogliride; Linogliride Buramate; Cinromide; Citenamide; Clonazepam; Cyhepta Fumarate; Metformin; Methyl Palmoxirate; Palmoxirate mide; Dezinamide; Dimethadione; Divalproex Sodium; Eter Sodium; Pioglitazone Hydrochloride; Pirogliride Tartrate; obarb; Ethosuximide; Ethotoin: Flurazepam Hydrochloride; Proinsulin Human; Seglitide Acetate; Tolazamide; Tolbuta Fluzinamide; Fosphenytoin Sodium; Gabapentin; Ilepcim mide; Tolpyrramide; Troglitazone; and Zopolrestat. ide; Lamotrigine; Magnesium Sulfate; Mephenytoin: [0086] Antidiarrheal: Diphenoxylate Hydrochloride; Mephobarbital; Methetoin; Methsuximide; Milacemide Methylprednisolone; Metronidazole; and Rolgamidine. Hydrochloride; Nabazenil; Nafimidone Hydrochloride; [0087] Antidiuretic: Argipressin Tannate; Desmopressin Nitrazepam; Phenacemide; Phenobarbital; Phenobarbital Acetate; and Lypressin. Sodium; Phensuximide; Phenytoin; Phenytoin Sodium; [0088] Antidote: Dimercaprol; Edrophonium Chloride; Primidone; Progabide; Ralitoline; Remacemide Hydrochlo Fomepizole; Levoleucovorin Calcium; Methylene Blue; and ride; Ropizine; Sabeluzole; Stiripentol; Sulthiame; Topira Protamine Sulfate. mate; Trimethadione; Valproate Sodium; Valproic Acid; [0089] Antidyskinetic: Selegiline Hydrochloride. Vigabatrin; Zoniclezole Hydrochloride; and Zonisamide. [0090] Anti-emetic: Alosetron Hydrochloride; Batano [0084] Antidepressant: Adinazolam; Adinazolam Mesy pride Hydrochloride; Bemesetron; Benzquinamide; Chlor late; Alaproclate; Aletamine Hydrochloride; Amedalin promazine; Chlorpromazine Hydrochloride; Clebopride; Hydrochloride; Amitriptyline Hydrochloride; Aptazapine Cyclizine Hydrochloride; Dimenhydrinate; Diphenidol; Maleate; Azaloxan Fumarate; Azepindole; Azipramine Diphenidol Hydrochloride; Diphenidol Pamoate; Dolasetron US 2011/0028460 A1 Feb. 3, 2011

Mesylate; Domperidone; Dronabinol; Flumeridone; [0100] Antihyperlipoproteinemic: Acifran; Beloxamide; Galdansetron Hydrochloride; Granisetron; Granisetron Bezafibrate; Boxidine; Cetaben Sodium; Ciprofibrate; Gem Hydrochloride; Lurosetron Mesylate; Meclizine Hydrochlo cadiol; Halofenate; Lifibrate; Meglutol; Nafenopin; Pimetime ride; Metoclopramide Hydrochloride; Metopimazine; Hydrochloride; Theofibrate; Tibric Acid; and Treloxinate. Prochlorperazine; Prochlorperazine Edisylate; Prochlorpera [0101] Antihypertensive: Alfuzosin Hydrochloride; Alipa zine Maleate; Promethazine Hydrochloride; Thiethylpera mide; Althiazide; Amiquinsin Hydrochloride; Anaritide zine; Thiethylperazine Malate; Thiethylperazine Maleate; Acetate; Atiprosin Maleate; Belfosdil; Bemitradine; Benda Trimethobenzamide Hydrochloride; and Zacopride Hydro calol Mesylate; Bendroflumethiazide; Benzthiazide; chloride. Bethanidine Sulfate; Biclodil Hydrochloride; Bisoprolol; [0091] Anti-epileptic: Felbamate; Iamotrigine; Lore Bisoprolol Fumarate; Bucindolol Hydrochloride; Bupico clezole; and Tolgabide. mide; Buthiazide; Candoxat rilat; Candoxatril; Captopril; [0092] Anti-estrogen: Clometherone; Nafoxidine Hydro Ceronapril; Chlorothiazide Sodium; Cicletanine; Cilazapril; chloride; Nitromi?ene Citrate; Raloxifene Hydrochloride; Clonidine; Clonidine Hydrochloride; Clopamide; Cyclo Tamoxifen Citrate; Toremifene Citrate; and Trioxifene Mesy penthiazide, Cyclothiazide; Darodipine; Debrisoquin Sul late. fate; Delapril Hydrochloride; Diapamide; Diazoxide; Dilt [0093] Antifibrinolytic; Na?amostat Mesylate. iazem Hydrochloride; Diltiazem Malate; Ditekiren; [0094] Antifungal: Acrisorcin; Ambruticin; Azaconazole; Doxazosin Mesylate; Ecadotril; Enalapril Maleate; Enalap Azaserine; Basifungin; Bifonazole; Butoconazole Nitrate; rilat; Emalkiren; Endralazine Mesylate: Epithiazide; Eprosa Calcium Undecylenate; Candicidin; Carbol-Fuchsin; Chlor rtan; Eprosartan Mesylate; Fenoldopam Mesylate: Flavodilol dantoin: Ciclopirox, Ciclopirox Olamine; Cilofungin; Maleate; Flordipine; Flosequinan; Fosinopril Sodium; Fosi Cisconazole; Clotrimazole; Cuprimyxin; Doconazole; noprilat; Guanabenz, Guanabenz Acetate; Guanacline Sul Econazole; Econazole Nitrate; Enilconazole; Ethonam fate; Guanadrel Sulfate; Guancvdine; Guanethidine Mono Nitrate; Fenticonazole Nitrate; Filipin; Fluconazole; Flucy sulfate; Guanethidine Sulfate; Guanfacine Hydrochloride; tosine; Fungimycin; Griseofulvin; Hamycin; Itraconazole; Guanisoquin Sulfate; Guanoclor Sulfate; Guanoctine Hydro Kalafungin; Ketoconazole; Lomoftmgin; Lydimycin; Mepar chloride; Guanoxabenz: Guanoxan Sulfate; Guanoxv?en Sul tricin; Miconazole; Miconazole Nitrate; Monensin; Mon fate; Hydralazine Hydrochloride; Hydralazine Polistirex, ensin Sodium; Naftifine Hydrochloride; Nifuratel Nifur Hydroflumethiazide; Indacrinone Indapamide; Indolapril merone; Nitralamine Hydrochloride; Nystatin; Octanoic Hydrochloride; Indoramin; Indoramin Hydrochloride; Acid, Orconazole Nitrate; Oxiconazole Nitrate; Oxifungin Indorenate Hydrochloride; Lacidipine; Leniquinsin; Lisino Hydrochloride; Parconazole Hydrochloride; Partricin; Potas pril; Lofexidine Hydrochloride; Losartan Potassium; Losula sium Iodide, Pyrrolnitrin; Rutamycin; Sanguinarium Chlo zine Hydrochloride; Mebutamate; Mecamylamine Hydro chloride; Medroxalol; Medroxalol Hydrochloride; ride; Saperconazole; Selenium Sulfide; Sinefungin; Sulcona Methalthiazide Methyclothiazide Methyldopa; Methyldo zole Nitrate; Terbinafine; Terconazole; Thiram; Tioconazole; pate Hydrochloride; Metipranolol; Metolazone Metoprolol Tolciclate; Tolindate; Tolna?tate; Triacetin; Triafungin; Fumarate; Metyrosine; Minoxidil; Muzolimine; Nebivolol; Undecylenic Acid, Viridofulvin; Zinc Undecylenate; and Nifidipine; Ofornine; Pargyline Hydrochloride; Pazoxide; Zinoconazole Hydrochloride. Pelanserin Hydrochloride; Perindopril Erbumine; Phenoxy [0095] Antiglaucoma agent: Alprenoxime Hydrochloride; benzamine Hydrochloride; Pinacidil; Pivopril; Polythiazide; Colforsin; Dipivefrin Hydrochloride; Naboctate Hydrochlo Prazosin Hydrochloride; Prizidilol Hydrochloride; Quinapril ride; Pilocarpine; and Pirnabine. Hydrochloride; Quinaprilat; Quinazosin Hydrochloride; [0096] Antihemorrhagic: Poliglusam. Quinelorane Hydrochloride; Quimpirole Hydrochloride; Qui [0097] Antihemorrheologic: Phentoxifylline. nuclium Bromide; Ramipril; Rauwolfia Serpentina; Reser [0098] Antihistaminic: Acrivastine; Antazoline Phosphate; pine; Saprisartan Potassium; Saralasin Acetate; Sodium Azatadine Maleate; Barmastine; Bromodiphenhydramine Nitroprusside; Sulfinalol Hydrochloride; Tasosartan; Hydrochloride; Brompheniramine Maleate; Carbinoxamine Temocapril Hydrochloride; Terazosin Hydrochloride; Terla Maleate; Cetirizine Hydrochloride; Chlorpheniramine Male kiren; Tiamenidine; Tiamenidine Hydrochloride; Ticrynafen; ate; Chlorpheniramine Polistirex; Cirmarizine; Clemastine; Tinabinol; Tiodazosin; Tipentosin Hydrochloride; Trichlo Clemastine Fumarate; Closiramine Aceturate; Cycliramine rmethiazide; Trimazosin Hydrochloride; Trimethaphan Cam Maleate; Cyclizine; Cyproheptadine Hydrochloride; Dex sylate; Trimoxamine Hydrochloride; Tripamide; Xipamide; brompheniramine Maleate; Dexchlorpheniramine Maleate; Zankiren Hydrochloride; and Zofenoprilat Arginine. Dimethindene Maleate; Diphenhydramine Citrate; Diphen [0102] Antihypotensive: Ciclafrine Hydrochloride; and hydramine Hydrochloride; Dorastine Hydrochloride; Doxy Midodrine Hydrochloride. lamine Succinate; Ebastine; Fexofenadine HCl; Levocabas [0103] Anti-infective: Acyclovir; Difloxacin Hydrochlo tine Hydrochloride; Loratadine; Mianserin Hydrochloride; ride; Integrase Inhibitors of HIV and other retroviruses; Lau Noberastine; Orphenadrine Citrate; Pyrabrom, Pyrilamine ryl Isoquinolinium Bromide; Moxalactam Disodium; Maleate; Pyroxamine Maleate; Rocastine Hydrochloride; Ornidazole; Pentisomicin; Protease inhibitors of HIV and Rotoxamine; Tazifylline Hydrochloride; Temelastine; Ter other retroviruses; and Sarafloxacin Hydrochloride. fenadine; Tripelennamine Citrate; Tripelennamine Hydro [0104] Anti-infective (topical): Alcohol; Aminacrine chloride; and Triprolidine Hydrochloride. Hydrochloride; Benzethonium Chloride; Bithionolate [0099] Antihyperlipidemic: Cholestyramine Resin; Clofi Sodium; Bromchlorenone; Carbamide Peroxide; Cetalko brate; Colestipol Hydrochloride; Crilvastatin; Dalvastatin; nium Chloride; Cetylpyridinium Chloride; Chlorhexidine Dextrothyroxine Sodium; Fluvastatin Sodium; Gemfibrozil; Hydrochloride; Domiphen Bromide; Fenticlor, Fludazonium Lecimibide: Lovastatin; Niacin; Pravastatin Sodium; Probu Chloride; Fuchsin, Basic; Furazolidone; Gentian Violet; col; Simvastatin; Tiqueside; and Xenbucin. Halquinols; Hexachlorophene; Hydrogen Peroxide; Ich US 2011/0028460 A1 Feb. 3, 2011

thammol; Imidecyl Iodine; Iodine; Isopropyl Alcohol; [0113] Antineoplastic: Acivicin; Aclarubicin; Acodazole Mafenide Acetate; Meralein Sodium; Mercufenol Chloride; Hydrochloride; Acronine; Adozelesin; Aldesleukin; Altre Mercury, Ammoniated; Methylbenzethonium Chloride; tamine; Ambomycin; Ametantrone Acetate; Amsacrine; Nitrofarazone; Nitromersol; Octenidine Hydrochloride; Anastrozole; Anthramycin; Asparaginase; Asperlin; Azaciti Oxychlorosene; Oxychlorosene Sodium; Parachlorophenol, dine; Azetepa, Azotomycin; Batimastat; Benzodepa; Camphorated; Potassium Permanganate; Povidone-Iodine; Bicalutamide; Bisantrene Hydrochloride; Bisnafide Dimesy Sepazonium Chloride; Silver Nitrate; Sulfadiazine, Silver; late; Bizelesin; Bleomycin Sulfate; Brequinar Sodium; Symclosene; Thimer?onate Sodium; Thimerosal; and Tro Bropirimine; Busulfan; Cactinomycin; Calusterone; Carace closene Potassium. mide; Carbetimer; Carboplatin; Carmustine; Carubicin [0105] Anti-inflammatory: Alclofenac; Alclometasone Hydrochloride; Carzelesin; Cedefingol; Chlorambucil; Cis Dipropionate; Algestone Acetonide; Alpha Amylase; platin; Cladribine; Crisnatol Mesylate; Cyclophosphamide; Amcinafal; Amcinafide; Amfenac Sodium; Amiprilose Cytarabine; Dacarbazine; Dactinomycin; Daunorubicin Hydrochloride; Anakinra; Anitrazafen; Apazone; Balsalazide Hydrochloride; Decitabine; Dexorinaplatin; Dezaguanine; Disodium; Bendazac, Bromelains; Broperamole; Budes Dezaguanine Mesylate; Diaziquone; Docetaxel; Doxorubi onide; Carprofen; Cicloprofen; Cintazone; Cliprofen; Clobe cin; Doxorubicin Hydrochloride; Droloxifene; Droloxifene tasol Propionate; Clobetasome Butyrate; Clopirac; Clotica Citrate; Dromostanolone Propionate; Duazomycin; Edatrex some Propionate; Cormethasone Acetate; Cortodoxone; ate; Eflornithine Hydrochloride; Elsamitrucin; Enloplatin; Deflazacort: Desonide; Desoximetasone; Dexamethasone Empromate; Epipropidine: Epirubicin Hydrochloride; Erbu Dipropionate; Diclofenac Potassium; Diclofenac Sodium; lozole; Esorubicin Hydrochloride; Estramustine; Estramus Diflorasone Diacetate; Diflumidone Sodium; Difluprednate; tine Phosphate Sodium; Etanidazole; Ethiodized Oil I 131; Diftalone; Dimethyl Sulfoxide; Drocinonide; Endrysone; Etoposide; Etoposide Phosphate; Etoprine; Fadrozole Enlimomab, Enolicam Sodium; Etodolac; Felbinac; Fen Hydrochloride; Fazarabine; Fenretinide; Floxuridine; Flu amole; Fenbufen, Fenclofenac; Fenclorac, Fendosal: Fempi darabine Phosphate; Fluorouracil; Flurocitabine; Fosqui palone; Fentiazac, Flazalone; Fluazacort; Flufenamic Acid; done; Fostriecin Sodium; Gemcitabine; Gemcitabine Hydro Flumizole; Flunisolide Acetate; Fluocortin Butyl; Fluo chloride; Gold Au 198; Hydroxyurea; Idarubicin, rometholone Acetate; Fluquazone; Fluretofen; Fluticasome Hydrochloride; Ifosfamide; Ilmofosine; Interferon Alfa-2a: Propionate; Furaprofen; Furobufen; Halcinonide; Halobeta Interferon Alfa-2b: Interferon Alfan 3; Interferon Alfa-n?; sol Propionate; Halopredone Acetate; Ibuprofen; Ibuprofen Interferon Beta-I a? Interferon Gamma-Ib, Iproplatin; Irino Aluminum; Ibuprofen Piconol; Ilonidap; Indomethacin tecan Hydrochloride; Isotretinoin; LanreotideAcetate; Letro Sodium; Indomethacin; Indoprofen Indoxole; Intrazole; Isof zole; Leuprolide Acetate; Liarozole Hydrochloride; Lometr lupredone Acetate; Isoxepac; Isoxicam; Ketoprofen; exol Sodium; Lomustine; Losoxantrone Hydrochloride; Lomoxicam; Loteprednol Etabonate; Meclofenamate Masoprocol; Maytansine; Mechlorethamine Hydrochloride; Sodium; Meclofenamic Acid; Meclorisonc Dibutyrate; Megestrol Acetate; Melengestrol Acetate; Melphalan; Mesalamine; Meseclazone; Methylprednisolone Suleptan Menogaril; Mercaptopurine; Methotrexate; Methotrexate ate; Morniflumate; Nabumetone; Nimazone; Olsalazine Sodium; Metoprine; Meturedepa; Mitindomide; Mitocarcin; Sodium; Orgotein; Orpanoxin; Oxaprozin, Oxyphenbuta Mitocromin; Mitogillin; Mitomalcin; Mitomycin; Mitosper; zone; Paranyline Hydrochloride; Pentosan Polysulfate Mitotane; Mitoxantrone Hydrochloride; Mycophenolic Acid; Sodium; Phenbutazone Sodium Glycerate; Piroxicam; Nocodazole; Nogalamvcin; Ormaplatin; Oxisuran; Pacli Piroxicam Cinnamate; Pirprofen; Prednazate; Prednisolone taxel; Pegaspargase; Peliomycin; Pentamustine; Peplomycin Sodium Phosphate; Prifelone; Prodolic Acid; Proquazone; Sulfate; Perfosfamide; Pipobroman; Piposulfan; Pirox Rimexolone; Romazarit; Salmacedin; Seclazone: Sermetacin; antrone Hydrochloride; Plicamycin; Plomestane; Porfimer Sudoxicam; Sulindac; Suprofen; Talniflumate; Tenidap; Sodium; Prednimustine; Procarbazine Hydrochloride; Puro Tenidap Sodium; Tenoxicam; Tesicam, Tesimide; Tixocortol mycin; Puromycin Hydrochloride; Pyrazofurin; Riboprine; Pivalate: Tolmetin: Tolmetin Sodium; Triclonide; Triflumi Rogletimide; Safingol Safingol Hydrochloride; Semustine; date; and Zidometacin. Simtrazene, Sparfosate Sodium; Sparsomycin; Spiro germa [0106] Antikeratinizinq agent: Doretinel; Linarotene; and nium Hydrochloride; Spiromustine; Spiroplatin; Streptoni Pelretin. grin: Streptozocin; Strontium Chloride Sr89; Sulofenur; Tali [0107] Antimalarial: Amodiaquine Hydrochloride; somycin; Taxane; Taxoid; Tecogalan Sodium; Tegafur, Amguinate; Artefiene; Chloroquine; Chloroquine Hydro Teloxantrone Hydrochloride; Temopor?in; Teniposide; chloride; Cycloguanil Pamoate; Empiroline Phosphate; Halo Teroxirone; Testolactone; Thiamiprine; Thioguanine; fantrine Hydrochloride; Hydroxychloroquine Sulfate; Thiotepa; Tiazofarin; Tirapazamine; Topotecan Hydrochlo Mefloquine Hydrochloride; Menoctone; Primaquine Phos ride; Triciribine Phosphate; Trimetrexate; Trimetrexate Glu phate; Pyrimethamine; Quinine Sulfate; and Tebuquine. curonate; Triptorelin; Tubulozole Hydrochloride; Uracil [0108] Antimicrobial: Aztreonam; Chlorhexidine Glucon Mustard; Uredepa; Vapreotide; Vertepor?in; Vinblastine Sul ate, Imidurea; Lycetamine; Nibroxane: Pirazmonam Sodium; fate; Vincristine Sulfate; Vindesine; Vindesine Sulfate; Vine Propionic Acid; Pyrithione Sodium; and Tigemonam Dicho pidine Sulfate; Vinglycinate Sulfate; Vinleurosine Sulfate; line. Vinorelbine Tartrate; Vinrosidine Sulfate; Vinzolidine Sul [0109] Antimigraine: Naratriptan Hydrochloride; Sergo fate; Vorozole; Zeniplatin: Zinostatin; and Zorubicin Hydro lexole Maleate; Sumatriptan Succinate; and Zatosetron Male chloride. ate. [0114] Anti-neoplastic compounds (additional): 20-epi-1, [0110] Antimitotic: Podofilox. 25 Dihydroxyvitamin D3; 5-Ethynyluracil; Abiraterone; [0111] Antimycotic: Amorolfine. Acylfulvene; Adecypenol; ALL-TKAntagonists; Ambamus [0112] Antinauseant: Buclizine Hydrochloride; and time; Amidox; Amifostine; Aminolevulinic Acid; Amrubicin; Cyclizine Lactate. Anagrelide; Andrographolide; Angiogenesis Inhibitors; US 2011/0028460 A1 Feb. 3, 2011

Antagonist D: Antagonist G.; Antarelix; Antiandrogen, Pros Nartograstim; Nedaplatin; Nemorubicin; Neridronic Acid; tatic Carcinoma; Anti-Dorsalizing Morphogenetic Protein-I; Neutral Endopeptidase; Nilutamide; Nisamycin; Nitric Antiestrogen; Antineoplaston; Antisense Oligonucleotides; Oxide Modulators; Nitroxide Antioxidant; Nitrullyn; N-Sub Aphidicolin Glycinate; Apoptosis Gene Modulators: Apop stituted Benzamides; 06-Benzylguanine; Okicenone; Oligo tosis Regulators; Apurinic Acid; Ara-CDP-DL-PTBA; Argi nucleotides; Onapristone; Ondansetron; Oracin; Oral Cytok nine Deaminase; Asulacrine; Atamestane; Atrimustine; Axi ine Inducer, Osaterone; Oxaliplatin: Oxaunomycin; nastatin 1: Axinastatin 2: Axinastatin 3; Azasetron; Azatoxin; Paclitaxel Analogues; Paclitaxel Derivatives; Palauamine; Azatyrosine; Baccatin III Derivatives; Balanol; BCR/ABL Palmitoylrhizoxin; Pamidronic Acid: Panaxytriol; Antagonists; Benzochlorins; Benzoylstaurosporine; Beta Panomi?ene; Parabactin; Pazelliptine; Peldesine; Pentostatin; Pentrozole; Perflubron; Perillyl Alcohol; Phenazinomycin; Lactam Derivatives; Beta-Alethine; Betaclamycin B; Betu Phenylacetate; Phosphatase Inhibitors; Picibanil; Pilocarpine linic Acid; br'GF Inhibitor; Bisantrene; Bisaziridinylsper Hydrochloride; Pirarubicin; Piritrexim; Placetin A; Placetin mine; Bisnafide; Bistratene A; Breflate; Budotitane; Buthion B; Plasminogen Activator Inhibitor; Platinum Complex; ine Sulfoximine; Calcipotriol; Calphostin C; Camptothecin Platinum Compounds; Platinum-Triamine Complex; Propyl Derivatives; Canarypox IL-2; Capecitabine; Carboxamide Bis-Acridone; Prostaglandin J2; Proteasome Inhibitors; Pro Amino-Triazole; Carboxyamidotriazole; CaRest MI; CARN tein A-Based Immune Modulator; Protein Kinase CInhibitor; 700, Cartilage Derived Inhibitor; Casein Kinase Inhibitors Protein Kinase C Inhibitors, Microalgal; Protein Tyrosine (1COS); Castanospermine; Cecropin B; Cetrorelix; Chlorins; Phosphatase Inhibitors; Purine Nucleoside Phosphorylase Chloroquinoxaline Sulfonamide: Cicaprost; Cis-Porphyrin; Inhibitors; Purpurins; Pyrazoloacridine, Pyridoxylated Clomi?ene analogues; Collismycin A; Collismycin B; Com Hemoglobin Polyoxyethylene Conjugate; Raf Antagonists; bretastatin A4; Combretastatin Analogue; Conagenin; Raltitrexed; Ramosetron; Ras Famesyl Protein Transferase Crambescidin 816; Crismatol; Cryptophycin 8; Cryptophycin Inhibitors; Ras Inhibitors; Ras-GAP Inhibitor; Retelliptine A Derivatives; Curacin A; Cyclopentanthraquinones; Cyclo Demethylated; Rhenium, Re 186 Etidronate; Rhizoxin; platam; Cypermycin; Cytarabine Ocfosfate; Cytolytic Factor; Ribozymes; RII Retinamide; Rohitukine; Romurtide; Roqui Cytostatin; Dacliximab: Dehydrodidenmin B; Dexifosfa nimex, Rubiginone B 1: Ruboxyl; Safingol; Saintopin; mide; Dexverapamil: Didemnin B; Didox; Diethylnorspen SarCNU; Sarcophytol A; Sdi 1 Mimetics; Senescence nine; Dihydro Azacytidine; Dihydrotaxol, 9-; Dioxamycin; Derived Inhibitor 1; Sense Oligonucleotides; Signal Trans Diphenyl Spiromustine; Docosanol; Dolasetron; Doxifluri duction Inhibitors; Signal Transduction Modulators; Single dine; Duocarmycin SA; Ebselen; Ecomustine; Edelfosine; Chain Antigen Binding Protein; Sizofiran; Sobuzoxane: Edrecolomab, Eflormithine; Elemene; Emitefur; Epirubicin; Sodium Borocaptate; Sodium Phenylacetate; Solverol; Estramustine Analogue; Estrogen Agonists; Estrogen Somatomedin Binding Protein; Sonermin; Sparfosic Acid; Antagonists; Exemestane; Fadrozole; Fiezelastine; Fla Spicamycin D: Splenopentin; Spongistatin 1; Squalamine; vopiridol; Fluasterone; Fludarabine; Fluorodaunorunicin Stem Cell Inhibitor; Stem-Cell Division Inhibitors; Stipi Hydrochloride; Forfenimex: Formestane; Fostriecin; Fote amide; Stromelysin Inhibitors; Sulfinosine; Superactive mustine; Gadolinium Texaphyrin; Gallium Nitrate; Galocit Vasoactive Intestinal Peptide Antagonist; Suradista; abine; Ganirelix; Gelatinase Inhibitors: Glutathione Inhibi Suramin; Swainsonine; Synthetic Glycosaminoglycans; Tal tors; Hepsulfam; Heregulin; Hexamethylene Bisacetamide; limustine; Tamoxifen Methiodide; Tauromustine; Tellurapy Hypericin; Ibandronic acid; Idarubicin; Idoxifene; Idraman rylium; Telomerase Inhibitors; Temozolomide; Tetrachloro tone; Ilomastat; Imidazoacridones; Immunostimulant Pep decaoxide; Tetrazomine; Thaliblastine; Thalidomide: tides; Insulin-Like Growth Factor-I Receptor Inhibitor; Inter Thiocoraline; Thrombopoietin; Thrombopoietin Mimetic; feron Agonists; Interferons; Interleukins; Iobenguane; Thymalfasin; Thymopoietin Receptor Agonist; Thymotri Iododoxorubicin; Ipomeanol, 4-; Irinotecan; Iroplact; man; Thyroid Stimulating Hormone; Tin Ethyl Etiopurpurin; Irsogladine; Isobengazole; Isohomohalicondrin B; Itasetron; Titanocene Dichloride; Topotecan; Topsentin; Toremifene; Jasplakinolide; Kahalalide F; Lamellarin-N Triacetate; Lan reotide; Leinamycin; Lentinan Sulfate; Leptolstatin; Leuke Totipotent Stem Cell Factor; Translation Inhibitors; Triacety mia Inhibiting Factor; Leukocyte Alpha Interferon; Leupro luridine; Triciribine; Tropisetron; Turosteride; Tyrosine lide+Estrogen-Progesterone; Leuprorelin; Levamisole; Kinase Inhibitors; Tyrphostins; UBC Inhibitors; Ubenimex, Liarozole; Linear Polyamine Analogue; Lipophilic Disac Urogenital Sinus-Derived Growth Inhibitory Factor, Uroki charide Peptide; Lipophilic Platinum Compounds; Lissocli nase Receptor Antagonists; Variolin B; Vector system, Eryth namide 7: Lobaplatin; Lombricine; Lometrexol; rocyte Gene Therapy; Velaresol; Veramine; Verdins; Vinorel Lonidamine; Losoxantrone; Lurtotecan; Lutetium Texaphy bine; Vinxaltine; Vitaxin: Zilascorb; and Zinostatin rin; Lysofylline; Lytic Peptides; Maitansine; Mannostatin A; Stimalamer. Marimastat; Maspin; Matrilysin Inhibitors; Matrix Metallo [0115] Antineutropenic. Filgrastim; Lenograstim; Molgra proteinase Inhibitors; Merbarone; Meterelin; Methioninase; mostim; Regramostim; and Sargramostim. Metoclopramide; MIF Inhibitor; Mifepristone; Miltefosine; [0116] Antiobsessional agent: Fluvoxamine Maleate. Mirimostim; Mismatched Double Stranded RNA; Mitogua [0117] Antiparasitic: Abamectin; Clorsulon; and Ivermec zone; Mitolactol; Mitomycin analogues; Mitonafide; Mito tin. toxin Fibroblast Growth Factor-Saporin; Mitoxantrone; [0118] Antiparkinsonian: Benztropine Mesylate; Mofarotene; Monoclonal Antibody, Human Chorionic Gona Biperiden; Biperiden Hydrochloride; Biperiden Lactate; Car dotrophin; Monophosphoryl Lipid A+Myobacterium Cell bidopa-Levodopa; Carmantadine, Ciladopa Hydrochloride; Wall Sk; Mopidamol; Multiple Drug Resistance Gene Inhibi Dopamantine; Ethopropazine Hydrochloride; Lazabemide; tor; Multiple Tumor Suppressor I-Based Therapy; Mustard Levodopa; Lometraline Hydrochloride; Mofegiline Hydro Anticancer Agent; Mycaperoxide B; Mycobacterial Cell Wall chloride; Naxagolide Hydrochloride; Pareptide Sulfate; Pro Extract; Myriaporone; N-Acetyldinaline; Nafarelin; cyclidine Hydrochloride; Ropinirole Hydrochloride; and Tol Nagrestip; Naloxone--Pentazocine; Napavin; Naphterpin; capone. US 2011/0028460 A1 Feb. 3, 2011

[0119) Antiperistaltic: Difenoximide Hydrochloride; ride; Efegatran Sulfate; Enoxaparin Sodium; Ifetroban; Difenoxin; Fluperamide; Lidamidine Hydrochloride; Lop Ifetroban Sodium; and Trifenagrel. eramide Hydrochloride; Malethamer; Nufenoxole; Parego [0133] Antitussive: Benzonatate; Butamirate Citrate; Chlo ric. phedianol Hydrochloride; Codeine Polistirex, Codoxime; [0120] Antipneumocystic: Atovaquone. Dextromethorphan; Dextromethorphan Hydrobromide; Dex [012.1] Antiproliferative agent: Piritrexim Isethionate. tromethorphan Polistirex, Ethyl Dibunate; Guaiapate; [0122) Antiprostatic hypertrophy: Sitogluside. Hydrocodone Bitartrate; Hydrocodone Polistirex; Levopro [0123] Antiprotozoal: Amodiaquine; Azanidazole; Banmi poxyphene Napsylate; Noscapine; Pemerid Nitrate; dazole; Camidazole; Chlortetracycline Bisulfate Chlortetra cycline Hydrochloride; Flubendazole; Flunidazole; Pipazethate; and Suxemerid Sulfate. Halofuginone Hydrobromide: Imidocarb Hydrochloride; [0134] Anti-ulcerative: Aceglutamide Aluminum; Cadex Ipronidazole; Misonidazole; Moxmidazole; Nitarsone; omer Iodine; Cetraxate Hydrochloride; Enisoprost; Iso Ronidazole; Sulnidazole; and Tinidazole. tiquimide; Lansoprazole; Lavoltidine Succinate; Misopros [012.4] Antipruritic: Methqilazine; Methqilazine Hydro tol; Nizatidine; Nolinium Bromide; Pantoprazole; Pi?armine; chloride; and Trimeprazine Tartrate. Pirenzepine Hydrochloride; Rabeprazole Sodium; Remi [0125] Antipsoriatic: Acitretin; Anthralin; Azaribine; Cal prostol; Roxatidine Acetate Hydrochloride; Sucralfate; cipotriene; Cycloheximide; Enazadrem Phosphate; Etreti Sucrosofate Potassium; and Tolimidone. nate; Liarozole Fumarate; Lonapalene; and Tepoxalin. [0135] Anti-urolithic: Cysteamine; Cysteamine Hydro [0126] Antipsychotic: Acetophenazine Maleate; Alente chloride; and Tricitrates. mol Hydrobromide; Alpertine; Azaperone; Batelapine Male [0136] Antiviral: Acemannan; Acv.clovir; Acyclovir ate; Benperidol; Benzindopyrine Hydrochloride; Brofoxine; Sodium; Adefovir; Alovudine; Alvircept Sudotox; Amanta Bromperidol; Bromperidol Decanoate; Butaclamol Hydro dine Hydrochloride; Aranotin; Arildone; Atevirdine Mesy chloride; Butaperazine; Butaperazine Maleate; Carphenazine late; Avridine, Cidofovir, Cipamfylline; Cytarabine Hydro Maleate; Carvotroline Hydrochloride; Chlorprothixene; Cin chloride; Delavirdine Mesylate; Desciclovir; Didanosine; perene; Cintriamide; Clomacran Phosphate; Clopenthixol; Disoxaril: Edoxudine; Enviradene; Enviroxime; Famciclo Clopimozide; Clopipazan Mesylate; Cloroperone Hydro vir; Famotine Hydrochloride; Fiacitabine; Fialuridine; Fosa chloride; Clothiapine; Clothixamide Maleate; Clozapine; rilate; Foscarnet Sodium; Fosfonet Sodium; Ganciclovir; Cyclophenazine Hydrochloride; Droperidol; Etazolate Ganciclovir Sodium; Idoxuridine; Kethoxal; Lamivudine: Hydrochloride; Fenimide; Flucindole; Flumezapine; Lobucavir; Memotine Hydrochloride; Methisazone; Nevi Fluphenazine Decanoate: Fluphenazine Enanthate: rapine; Penciclovir, Pirodavir; Ribavirin; Rimantadine Fluphenazine Hydrochloride; Fluspiperone; Fluspirilene; Hydrochloride; Saquinavir Mesylate; Somantadine Hydro Flutroline; Gevotroline Hydrochloride; Halopemide; Halo chloride; Sorivudine; Statolon; Stavudine; Tilorone Hydro peridol; Haloperidol Decanoate; Iloperidone; Imidoline chloride; Trifluridine; Valacyclovir Hydrochloride; Vidara Hydrochloride; Lemperone; Mazapertine Succinate; bine; Vidarabine Phosphate; Vidarabine Sodium Phosphate; Mesoridazine; Mesoridazine Besylate; Metiapine; Milenper one; Milipertine; Molindone Hydrochloride; Naranol Hydro Viroxime; Zalcitabine; Zidovudine; and Zinviroxime. chloride; Neflumozide Hydrochloride; Ocaperidone; Olanza [0137] Appetite suppressant: Dexfenfluramine Hydrochlo pine; Oxiperomide; Penfluridol; Pentiapine Maleate; ride; Phendimetrazine Tartrate; and Phentermine Hydrochlo Perphenazine; Pimozide; Pinoxepin Hydrochloride; Pipam ride. perone; Piperacetazine; Pipotiazine Palmitate; Piquindone [0138] Benign prostatic hyperplasia therapy agent: Tamsu Hydrochloride; Promazine Hydrochloride; Remoxipride; losin Hydrochloride. Remoxipride Hydrochloride; Rimcazole Hydrochloride; [0139] Blood glucose regulators: Acetohexamide and Glip Seperidol Hydrochloride; Sertindole; Setoperone; Spiper izide; Chloropropamide; and Human insulin. one; Thioridazine; Thioridazine Hydrochloride; Thiothixene; [0140] Bone resorption inhibitor: Alendronate Sodium; Thiothixene Hydrochloride; Tioperidone Hydrochloride; Etidronate Disodium; and Pamidronate Disodium. Tiospirone Hydrochloride; Trifluoperazine Hydrochloride; [0141] Bronchodilator: Albuterol; Albuterol Sulfate; Aza Trifluperidol; Triflupromazine; Triflupromazine Hydrochlo nator Maleate; Bamifylline Hydrochloride; Bitolterol Mesy ride; and Ziprasidone Hydrochloride. late; Butaprost; Carbuterol Hydrochloride; Clorprenaline [0127] Antirheumatic: Auranofin; Aurothioglucose; Bin Hydrochloride; Colterol Mesylate; Doxaprost; Doxofylline; darit; Lobenzarit Sodium; Phenylbutazone; Pirazolac, Prino Dyphylline; Enprofylline; Ephedrine; Ephedrine Hydrochlo mide Tromethamine; and Seprilose. ride; Fenoterol; Fenprinast Hydrochloride; Guaithylline; [0128] Antischistosomal: Becanthone Hydrochloride; Hexoprenaline Sulfate; Hoquizil Hydrochloride; Ipratropium Hycanthone; Lucanthone Hydrochloride; Niridazole; Oxam Bromide; Isoetharine; Isoetharine Hydrochloride; Isoet niquine; Pararosaniline Pamoate; and Teroxalene Hydrochlo harine Mesylate; Isoproterenol Hydrochloride; Isoproterenol ride. Sulfate; Metaproterenol Polistirex, Metaproterenol Sulfate; [0129] Antiseborrheic: Chloroxime; Piroctone; Piroctone Nisbuterol Mesylate; Oxtriphylline; Picumeterol Fumarate; Olamine; and Resorcinol Monoacetate. Piquizil Hydrochloride; Pirbuterol Acetate; Pirbuterol [0130] Antisecretory:Arbaprostil; Deprostil; Fenoctimine Hydrochloride; Procaterol Hydrochloride; Pseudoephedrine Sulfate; Octreotide; Octreotide Acetate; Omeprazole Sulfate; Quazodine; Quinterenol Sulfate; Racepinephrine; Sodium; Rioprostil; Trimoprostil. Racepinephrine Hydrochloride; Reproterol Hydrochloride; [0131] Antispasmodic: Stilonium Iodide; Tizanidine Rimiterol Hydrobromide; Salmeterol; Salmeterol Xinafoate; Hydrochloride. Soterenol Hydrochloride; Sulfonterol Hydrochloride; Sulox [0132) Antithrombotic: Anagrelide Hydrochloride; Dalte ifen Oxalate; Terbutaline Sulfate; Theophylline; Xanoxate parin Sodium; Danaparoid Sodium; Dazoxiben Hydrochlo Sodium; Zindotrine; and Zinterol Hydrochloride. US 2011/0028460 A1 Feb. 3, 2011

[0142] Carbonic anhydrase inhibitor: Acetazolamide; Polylysine; Butedronate Tetrasodium; Butilfenin; Coccidioi Acetazolamide Sodium; Dichlorophenamide; Dorzolamide din; Corticorelin Ovine Triflutate; Corticotropin Zinc Hydrochloride; Methazolamide; and Sezolamide Hydrochlo Hydroxide; Corticotropin, Repository; Diatrizoate Meglu ride. mine; Diatrizoic Acid; Diphtheria Toxin for Schick Test; Dis [0143] Cardiac depressant: Acecainide Hydrochloride; ofenin; Ethiodized Oil: Etifenin; Exametazime, Ferristenc; Acetylcholine Chloride; Actisomide; Adenosine; Amio Ferumoxides; Ferumoxsil; Fluorescein; Fluorescein Sodium; darone; Aprindine; Aprindine Hydrochloride; Artilide Fuma Gadobenate Dimeglumine; Gadodiamide; Gadopentetate rate; Azimilide Dihydrochloride; Bidisomide; Bucainide Dimegiumine; Gadoteridol; Gadoversetamide; Histoplas Maleate; Bucromarone; Capobenate Sodium; Capobenic min; Impromidine Hydrochloride; Indigotindisulfonate Acid; Cifenline; Cifenline Succinate; Clofilium Phosphate; Sodium; Indocyanine Green; Iobenguane Sulfate I 123; Disobutamide; Disopyramide; Disopyramide Phosphate: Iobenzamic Acid; Iocarmate Meglumine; Iocarmic Acid; Ioc Dofetilide; Drobuline; Edifolone Acetate; Emilium Tosylate; etamic Acid; Iodamide; Iodamide Megiumine; Iodipamide Encainide Hydrochloride; Flecainide Acetate; Ibutilide Meglumine; Iodixanol; Iodoxamate Meglumine; Iodoxamic Fumarate; Indecainide Hydrochloride; Ipazilide Fumarate; Acid; Ioglicic Acid; Ioglucol; Ioglucomide; Ioglycamic Acid; Lorajmine Hydrochloride; Lorcainide Hydrochloride; Iogulamide: Iohexol; Iomeprol; Iopamidol; Iopentol; Meobentine Sulfate; Mexiletine Hydrochloride; Modecain Iophendylate; Ioprocemic Acid, Iopronic Acid; Iopydol; ide; Moricizine; Oxiramide; Pirmenol Hydrochloride; Piro Iopydone; Iosefamic Acid; Ioseric Acid; Iosulamide Meglu lazamide; Pranolium Chloride; Procainamide Hydrochlo mine; Iosumetic Acid; Iotasul; Iotetric Acid; Iothalamate ride; Propafenone Hydrochloride; Pyrinoline; Quindonium Meglumine; Iothalamate Sodium; Iothalamic Acid; Iotrolan; Bromide; Quinidine Gluconate; Quinidine Sulfate; Iotroxic Acid; Ioversol; Ioxagiate Sodium; Ioxaglate Meglu Recainam Hydrochloride; Recainam Tosylate; Risotilide mine; Ioxaglic Acid; Ioxilan; Ioxotrizoic Acid; Ipodate Hydrochloride; Ropitoin Hydrochloride; Sematilide Hydro Sodium; Iprofenin; Isosulfan Blue; LeukocyteTyping Serum; chloride; Suricainide Maleate; Tocainide; Tocainide Hydro Lidofenin; Mebrofenin; Meglumine; Metrizamide; Metri chloride; and Transcainide. zoate Sodium; Metyrapone Tartrate; Mumps Skin Test Anti [0144] Cardioprotectant: Dexrazoxane; and Draflazine. gen; Pentetic Acid; Propyliodone; Quinaldine Blue; Schick [0145] Cardiotonic agent: Actodigin; Amrinone; Bemo Test Control; Sermorelin Acetate; Sodium Iodide I 123; radan; Butopamine; Carbazeran; Carsatrin Succinate; Desl Sprodiamide; Stannous Pyrophosphate; Stannous Sulfur Col anoside; Digitalis; Digitoxin; Digoxin; Dobutamine; Dob loid; Succimer; Teriparatide Acetate; Tetrofosmin, Tolbuta utamine Hydrochloride; Dobutamine Lactobionate; mide Sodium; Tuberculin; and Xylose. Dobutamine Tartrate; Enoximone: Imazodan Hydrochloride; [0157] Diuretic: Ambuphylline; Ambuside; Amiloride Indolidan; Isomazole Hydrochloride; Levdobutamine Lacto Hydrochloride; Azolimine; Azosemide; Brocrinat; Bumet biomate; Lixazinone Sulfate; Medorinone; Milrinone; Pel anide; Chlorothiazide; Chlorthalidone; Clazolimine; Clorex rinone Hydrochloride; Pimobendan; Piroximone; Prinox olone; Ethacrynate Sodium; Ethacrynic Acid; Etozolin; Fen odan; Proscillaridin; Quazinone; Tazolol Hydrochloride; and quizone; Furosemide; Hydrochlorothiazide; Isosorbide; Vesnarinone. Mannitol Mefruside; Ozolinone; Piretanide; Spiroxasone; [0146] Cardiovascular agent: Dopexamine; and Dopexam Torsemide; Triamterene; Triflocin; and Urea. ine Hydrochloride. [0158] Dopaminergic agent: Ibopamine. [0147] Cerebral ischemia agent: Dextrorphan Hydrochlo [0159) Ectoparasiticide: Nifluridide, Permethrin. ride. [0160] Emetic: Apomorphine Hydrochloride. [0148] Choleretic: Dehydrocholic Acid, Fencibutirol; [0161] Enzyme inhibitor: 30 Polignate Sodium; Acetohy Hymecromone; Piprozolin; Sincalide; Tocamphyl. droxamic Acid, Alrestatin Sodium; Aprotinin; Benazepril [0149] Cholinergic: Aceclidine; Bethanechol Chloride; Hydrochloride; Benazeprilat; Benurestat; Bromocriptine; Carbachol; Demecarium Bromide; Dexpanthenol; Bromocriptine Mesylate: Cilastatin Sodium; Fluro?amide; Echothiophate Iodide; Isoflurophate; Methacholine Chlo Lergotrile; Lergotrile Mesylate; Levcycloserine; Libenza ride; Neostiamine Methylsulfate; Neostigmine Bromide; pril; Pentopril; Pepstatin; Perindopril; Sodium Amylosulfate; Physostigmine; Physostigmine Salicylate; Physostigmine Sorbinil; Spirapril Hydrochloride; Spiraprilat; Taleranol; Sulfate; Pilocarpine Nitrate; and Pyridostigmine Bromide. Teprotide; Tolfamide; and Zofenopril Calcium. [0150] Cholinergic agonist. Xanomeline; and Xanomeline [0162] Estrogen: Chlorotrianiseme; Dienestrol; Diethylstil Tartrate. bestrol; Diethylstilbestrol Diphosphate; Equilin; Estradiol; [0151] Cholinesterase Deactivator: Obidoxime Chloride; Estradiol Cypionate; Estradiol Enanthate; Estradiol Undecy Pralidoxime Chloride; Pralidoxime Iodide; and Pralidoxime late; Estradiol Valerate; Estrazinol Hydrobromide; Estriol; Mesylate. Estrofurate; Estrogens, Conjugated; Estrogens, Esterified; [0152] Coccidiostat: Arprinocid; Narasin; Semduramicin; Estrone; Estropipate; Ethinyl Estradiol; Fenestrel; Mestra and Semduramicin Sodium. nol; Nylestriol; and Quinestrol. [0153] Cognition adjuvant: Ergoloid Mesylates; Pirac [0163] Fibrinolytic: Anistreplase; Bisobrin Lactate; and etam; Pramiracetam Hydrochloride; Pramiracetam Sulfate; Brinolase. and Tacrine Hydrochloride. [0164] Free oxygen radical scavenger: Pegorgotein. [0154] Cognition enhancer: Besipirdine Hydrochloride; [0165] Gastric Acid Suppressant: Lansoprazole, Pantopra Linopirdine; and Sibopirdine. zole and Omeprazole. [0155] Contrast Media: Barium Sulfate; Diatrizoate [0166] Gastrointestinal Motility agents: Cisapride. Sodium; Erythrosine Sodium; Iopanoic Acid; Ipodate Cal [0167] Glucocorticoid: Amcinonide; Beclomethasone cium; Metyrapone; and Tyropanoate Sodium. Dipropionate; Betamethasone; Betamethasone Acetate; [0156] Diagnostic aid: Aminohippurate Sodium; Ana Betamethasone Benzoate; Betamethasone Dipropionate; zolene Sodium; Arclofenin; Bentiromide; Benzylpenicilloyl Betamethasone Sodium Phosphate; Betamethasone Valerate; US 2011/0028460 A1 Feb. 3, 2011

Carbenoxolone Sodium; Clocortolone Acetate; Clocortolone [0175] Immunomodulator: Dimepranol Acedoben; Imiqui Pivalate; Cloprednol; Corticotropin; Cortisone Acetate; Cor mod; Interferon Beta-Ib, Lisofylline; Mycophenolate tivazol; Descinolone Acetonide; Dexamethasone; Dexam Mofetil; and Prczatide Copper Acetate. ethasone Sodium Phosphate; Diflucortolone; Diflucortolone [0176] Immunoredulator: Azarole; Fanetizole Mesylate; Pivalate: Flucloronide; Flumethasone: Flumethasone Piv Frentizole; Oxamisole Hydrochloride; Ristianol Phosphate: alate: Flunisolide; Fluocinolone Acetonide; Fluocinonide; Thymopentin; and Tilomisole. Fluocortolone; Fluocortolone Caproate; Fluorometholone; [0177] Immunostimulant: Loxoribine; and Teceleukin. Fluperolone Acetate; Fluprednisolone; Fluprednisolone Val [0178] Immunosuppressant: Azathioprine; Azathioprine erate; Flurandrenolide; Formocortal; Hydrocortisone; Sodium; Cyclosporine; Daltroban; Gusperimus Trihydro Hydrocortisone Acetate; Hydrocortisone Buteprate; Hydro chloride; Sirolimus; Tacrolimus. cortisone Butyrate; Hydrocortisone Sodium Phosphate: [0179] Impotence therapy adjunct: Delequamine Hydro Hydrocortisone Sodium Succinate; Hydrocortisone Valerate; chloride. Medrysone; Methylprednisolone Acetate; Methylpredniso [0180] Inhibitor: Acarbose; Atorvastatin Calcium; Benser lone Sodium Phosphate; Methylprednisolone Sodium Succi azide; Brocresine; Carbidopa; Clavulanate Potassium; nate; Nivazol; Paramethasone Acetate; Prednicarbate; Pred Dazmegrel; Docebenone; Epoprostenol; Epoprostenol nisolone; Prednisolone Acetate; Prednisolone Sodium; Epristeride; Finasteride; Flurbiprofen Sodium; Hemisuccinate; Prednisolone Sodium Succinate; Predniso Furegrelate Sodium; Lufironil; Miglitol; Orlistat; Pimage lone Tebutate; Prednisone; Prednival; Ticabesone Propi dine Hydrochloride; Pirmagrel; Ponalrestat; Ridogrel; Sul onate; Tralonide; Triamcinolone; Triamcinolone Acetonide; bactam Benzathine; Sulbactam Pivoxil; Sulbactam Sodium; Triamcinolone Acetonide Sodium; Triamcinolone Diacetate; Suronacrine Maleate; Tazobactam; Tazobactam Sodium; and Triamcinolone Hexacetonide. Ticlopidine Hydrochloride; Tirilazad Mesylate; Tolrestat; [0168] Gonad-stimulating principle: Buserelin Acetate; Velnacrine Maleate; Zifrosilone; and Zileuton. Clomiphene Citrate; Ganirelix Acetate; Gonadorelin Acetate; [0181] Keratolytic: Alcloxa; Aldioxa; Dibenzothiophene; Gonadorelin Hydrochloride; Gonadotropin, Chorionic; and Etarotene; Motretinide-I Picotrin Diolamine; Salicylic Acid; Menotropins. Sumarotene; Tazarotene; Tetroquinone; and Tretinoin. [0169] Hormone: 17 Alpha Dihydroedullenin; 17 Alpha [0182] LHRH agonist: Deslorelin; Goserelin; Histrelin; Dihydroequilin; 17 Alpha Estradiol; 17 Beta Estradiol; 17 Lutrelin Acetate; and Nafarelin Acetate. Hydroxy Progesterone; Androstenedione; Clomiphene; [0183| Liver disorder treatment: Malotilate. Cosyntropin; Dehydroepiandrosterone; Dihydroestosterone; [0184] Luteolysin: Femprostalene. Equilenin; Ethyndiol; Follicle Regulatory Protein; Follicle [0185] Memory adjuvant: Dimoxamine Hydrochloride; Stimulating Hormone; Folliculostatin; Gonadoctrinins; and Ribaminol. Gonadorelin; Gonadotropins; Han Memopausal Gonadotro [0186] Mental performance enhancer: Aniracetam. pins; Human Chorionic Gonadotropin; Insulin Growth Fac [0187] Mood regulator. Fengabine. tor; Leuprolide; Levonorgestrel; Luteinizing hormone; [0188] Mucolytic: Acetylcysteine; Carbocysteine; and Luteinizing Hormone Releasing Hormone and Analogs; Domiodol Medroxyprogesterone; Megestrol; Metogest, Norethindrone; [0189] Mucosal Protective agents: Misoprostol (Cytotec). Norethynodrel; Norgestrel; Oocyte Maturation Inhibitor; [0190] Mydriatic: Berefrine. Oxytocin; Pituitary, Posterior; Progesterone; Relaxin; Serac [0191) Nasal decongestant: Nemazoline Hydrochloride; tide Acetate; Somalapor, Somatrem: Somatropin; Some Pseudoephedrine Polistirex. nopor: Somidobove; Tamoxifen; Urofollitropin; and Vaso [0192] Neuroleptic: Duoperone Fumarate; and Risperi pressin. done. [0170] Hypocholesterolemic: Lifibrol. [0193] Neuromuscular blocking agent: Atracurium Besy [0171] Hypoglycemic: Darglitazone Sodium; and Glime late; Cisatracurium Besylate; Doxacurium Chloride; Gal piride. lamine Triethiodide; Metocurine Iodide; Mivacurium Chlo [0172] Hypolipidemic: Azalanstat Dihydrochloride; ride; Pancuronium Bromide; Pipecuronium Bromide; Colestolone; Surformer; and Xenalipin. Rocuronium Bromide; Succinylcholine Chloride; Tub [0173] Hypotensive: Viprostol. ocurarine Chloride; and Vecuronium Bromide. [0174] Immunizing agent: Antirabies Serum; Antivenin; [0194] Neuroprotective: Dizocilpine Maleate. Antivenin (Crotalidae) Polyvalent; BCG Vaccine; Botulism (0195] NMDA antagonist: Selfotel. Antitoxin; Cholera Vaccine; Diphtheria Antitoxin; Diphthe [0196) Non-hormonal sterol derivative: Pregnenolone Suc ria Toxoid; Diphtheria Toxoid Adsorbed; Globulin, Immune; cinate. Hepatitis B Immune Globulin; Hepatitis B Virus Vaccine [0197] Oxytocic: Carboprost; Carboprost Methyl; Carbo Inactivated; Influenza Virus Vaccine; Measles Virus Vaccine prost Tromethamine; Dinoprost; Dinoprost Tromethamine; Live; Meningococcal Polysaccharide Vaccine Group A; Men Dinoprostone; Ergonovine Maleate; Meteneprost; Methyler ingococcal Polysaccharide Vaccine Group C; Mumps Virus gonovine Maleate; and Sparteine Sulfate. Vaccine Live: Pertussis Immune Globulin; Pertussis Vaccine; [0198] Paget’s disease agents: Tiludronate Disodium. Pertussis Vaccine Adsorbed; Plague Vaccine; Poliovirus Vac [0199] Progestin: Algestone Acetophenide; Amadinone cine Inactivated: Poliovirus Vaccine Live Oral; Rabies Acetate; Anagestone Acetate; Chlormadinone Acetate; Immune Globulin; Rabies Vaccine; Rho(D) Immune Globu Cingestol; Clogestone Acetate; Clomegestone Acetate; lin; Rubella Virus Vaccine Live; Smallpox Vaccine; Tetanus Desogestrel; Dimethisterone; Dydrogesterone; Ethynerone; Antitoxin; Tetanus Immune Globulin; Tetanus Toxoid: Teta Ethynodiol Diacetate; Etonogestrel; Flurogestone Acetate; nus Toxoid Adsorbed; Typhoid Vaccine; Vaccinia Immune Gestaclone; Gestodene; Gestonorone Caproate; Gestrinone; Globulin; Varicellazoster Immune Globulin; and Yellow Haloprogesterone; Hydroxyprogesterone Caproate; Fever vaccine. Lynestrenol; Medrogestone; Med roxyprogesterone Acetate; US 2011/0028460 A1 Feb. 3, 2011

Methynodiol Diacetate; Norethindrone Acetate; Norgesti Etomidate; Fenobam; Flumitrazepam; Fosazepam; Glute mate; Norgestomet; Oxogestone Phenpropionate; thimide; Halazepam; Lon-metazepam; Mecloqualone; Mep Quingestanol Acetate; Quingestrone; and Tigestol. robamate; Methaqualone; Midaflur; Paraldehyde; Pentobar [0200) Prostaglandin: Cloprostenol Sodium; Fluprostenol bital; Pentobarbital Sodium; Perlapine; Prazepam, Sodium; Gemeprost; Prostalene; and Sulprostone. Quazepam; Reclazepam; Roletamide; Secobarbital; Seco [0201] Prostate growth inhibitor: Pentomone. barbital Sodium; Suproclone; Tracazolate; Trepipam Male [0202) Prothyrotropin: Protirelin. ate; Triazolam; Tricetamide; Triclofos Sodium; Trimetozine; [0203] Psychotropic: Minaprine. Uldazepam; Zaleplon; Zolazepam Hydrochloride; and Zolpi [0204] Radioactive agent: Fibrinogen I 125; Fludeoxyglu dem Tartrate. cose F 18; Fluorodopa F 18; Insulin I 125; Insulin I 131; [0212] Selective adenosine Al antagonist. Apaxifylline. Iobenguane I 123; Iodipamide Sodium I 131; Iodoantipyrine [0213] Serotonin antagonist. Altanserin Tartrate; Ameser I 131; Iodocholesterol I 131; Iodohippurate Sodium I 123; gide; Ketanserin; and Ritanserin. Iodohippurate Sodium I 125; Iodohippurate Sodium I 131; [0214] Serotonin inhibitor: Cinanserin Hydrochloride; Iodopyracet I 125; Iodopyracet I 131; Iofetamine Hydrochlo Fenclonine; Fonazine Mesylate; and Xylamidine Tosylate. ride I 123: Iomethin I 125; Iomethin I 131; Iothalamate [0215] Serotonin receptor antagonist: Tropanserin Hydro Sodium I 125; Iothalamate Sodium I 131; Iotyrosine I 131; chloride. Liothyronine I 125; Liothyronine I 131; Merisoprol Acetate [0216) Steroid: Dexamethasone Acefurate; and Mometa Hg 197; Merisoprol Acetate Hg 203; Merisoprol Hg 197; sone Furoate. Selenomethionine Se 75; Technetium Tc 99m Antimony [0217| Stimulant: Amfonelic Acid; Amphetamine Sulfate; Trisulfide Colloid; Technetium Tc 99m Bicisate; Technetium Ampyzine Sulfate; Arbutamine Hydrochloride; Azabon; Caf Tc 99m Disofenin; Technetium Tc 99m Etidronate; Techne feine; Ceruletide; Ceruletide Diethylamine; Dazopride tium Tc 99m Exametazime; Technetium Tc 99m Furifosmin; Fumarate; Dextroamphetamine; Dextroamphetamine Sul Technetium Tc 99m Gluceptate; Technetium Tc 99m Lidofe fate; Difluanine Hydrochloride; Dimefline Hydrochloride; nin; Technetium Tc 99m Mebrofenin; Technetium Tc 99m Doxapram Hydrochloride; Ethamivan; Etryptamine Acetate; Medronate; Technetium Tc 99m Medronate Disodium; Tech Fenethylline Hydrochloride; Flubanilate Hydrochloride; netium Tc 99m Mertiatide; Technetium Tc 99m Oxidronate; Flurothyl; Histamine Phosphate; Indriline Hydrochloride; Technetium Tc 99m Pentetate; Technetium Tc 99m Pentetate Mefexamide; Methamphetamine Hydrochloride; Meth Calcium Trisodium; Technetium Tc 99m Sestamibi; Techne ylphenidate Hydrochloride; Pemoline; Pyrovalerone Hydro tium Tc 99m Siboroxime; Technetium Tc 99m Succimer; chloride: Xamoterol; and Xamoterol Fumarate. Technetium Tc 99m Sulfur Colloid; Technetium Tc 99m [0218] Suppressant: Amflutizole; Colchicine; Tazofelone. Teboroxime; Technetium Tc 99m Tetrofosmin; Technetium [0219) Symptomatic multiple sclerosis: Fampridine. Tc 99m Tiatide; Thyroxine I 125; Thyroxine 1131; Tolpovi [0220) Synergist Proadifen Hydrochloride. done 1131; Triolein 1125; and Triolein 1131. [0221) Thyroid hormone: Levothyroxine Sodium; Liothy [0205] Regulator: Calcifediol; Calcitonin; Calcitriol; Clo ronine Sodium; and Liotrix. dronic Acid; Dihydrotachysterol: Etidronic Acid; Oxidronic [0222] Thyroid inhibitor: Methimazole; and Propylthiou Acid: Piridronate Sodium; Risedronate Sodium; and Secal racil. ciferol. [0223] Thyromimetic: Thyromedan Hydrochloride. [0206] Relaxant: Adiphenine Hydrochloride; Alcuronium [0224] Tranquilizer: Bromazepam; Buspirone Hydrochlo Chloride; Aminophylline; Azumolene Sodium; Baclofen; ride; Chlordiazepoxide; Clazolam; Clobazam; Clorazepate Benzoctamine Hydrochloride; Carisoprodol; Chlorphenesin Dipotassium; Clorazepate Monopotassium; Demoxepam; Carbamate; Chlorzoxazone; Cinflumide: Cinnamedrine; Dexmedetomidine; Enciprazine Hydrochloride; Gepirone Clodanolene; Cyclobenzaprine Hydrochloride; Dantrolene; Hydrochloride; Hydroxyphenamate; Hydroxyzine Hydro Dantrolene Sodium; Femalamide; Fenyripol Hydrochloride; chloride; Hydroxyzine Pamoate; Ketazolam; Lorazepam; Fetoxylate Hydrochloride; Flavoxate Hydrochloride; Fle Lorzafone; Loxapine; Loxapine Succinate; Medazepam tazepam; Flumetramide; Hexafluorenium Bromide; Isomy Hydrochloride; Nabilone; Nisobamate; Oxazepam; Pent lamine Hydrochloride; Lorbamate; Mebeverine Hydrochlo abamate; Piremperone; Ripazepam; Rolipram; Sulazepam; ride; Mesuprine Hydrochloride; Metaxalone; Methixene Taciamine Hydrochloride; Temazepam; Triflubazam; Hydrochloride; Methocarbamol; Nafomine Malate; Neleza Tybamate; and Valnoctamide. prine Maleate; Papaverine Hydrochloride; Pipoxolan Hydro [0225] Unstable angina agents: Tirofiban Hydrochloride. chloride; Quinctolate; Ritodrine; Ritodrine Hydrochloride; [0226] Uricosuric: Benzbromarone; Irtemazole; Rolodine; Theophylline Sodium Glycinate; Thiphenamil Probenecid; Sulfinpyrazone. Hydrochloride; and Xilobam. [0227] Vasoconstrictor: Angiotensin Amide; Felypressin; [0207] Repartitioning agent: Cimaterol. Methysergide; and Methysergide Maleate. [0208] Scabicide: Amitraz, Crotamiton. [0228] Vasodilator: Alprostadil; Azaclorzine Hydrochlo [0209] Sclerosing agent: Ethanolamine Oleate; Morrhuate ride; Bamethan Sulfate; Bepridil Hydrochloride; Buterizine; Sodium; Tribenoside. Cetiedil Citrate; Chromonar Hydrochloride; Clonitrate; [0210] Sedative: Propiomazine. Dipyridamole; Droprenilamine; Erythrityl Tetranitrate; Felo [0211] Sedative-hypnotic: Allobarbital; Alonimid; Alpra dipine; Flunarizine Hydrochloride; Fostedil; Hexobendine; zolam; Amobarbital Sodium; Bentazepam; Brotizolam; But Inositol Niacinate; Iproxamine Hydrochloride; Isosorbide abarbital; Butabarbital Sodium; Butalbital; Capuride; Car Dinitrate; Isosorbide Mononitrate; Isoxsuprine Hydrochlo bocloral; Chloral Betaine; Chloral Hydrate; ride; Lidoflazine; Mefenidil; Mefenidil Fumarate; Mibefradil Chlordiazepoxide Hydrochloride; Cloperidone Hydrochlo Dihydrochloride; Mioflazine Hydrochloride; Mixidine; ride; Clorethate; Cyprazepam; Dexclamol Hydrochloride; Nafronyl Oxalate; Nicardipine Hydrochloride; Nicergoline; Diazepam; Dichloralphenazone; Estazolam Ethchlorvynol; Nicorandil; Nicotinyl Alcohol; Nimodipine; Nisoldipine; US 2011/0028460 A1 Feb. 3, 2011

Oxfenicine; Oxprenolol Hydrochloride; Pentaerythritol Tet feine Citrate; Calanolide A: Calcitonin Human; Calcitonin, ranitrate; Pentoxifylline; Pentrinitrol; Perhexiline Maleate; Salmon; Calcium; Calcium Acetate; Calcium Gluceptate; Pindolol; Pirsidomine; Prenylamine; Propatyl Nitrate; Suloc Calcium Metrizoate; Calfactant; Camonagrel; Candesartan; tidil; Terodiline Hydrochloride; Tipropidil Hydrochloride; Candesartan Cilexetil: Candoxatrilat; Capromab; Capsaicin; Tolazoline Hydrochloride; and Xanthinol Niacinate. Carbarnazepine; Carbazomycin C; Carbetocin; Carbidopa/ [0229] Wound healing agent: Ersofermin. Levodopa; Carbovir; Carboxymethylated Beta-I,3-Glucan: [0230] Xanthine oxidase inhibitor: Allopurinol; and Oxy Carperitide; Carteolol; Carumonam; Carvotroline; Caspo purinol. fungin Acetate; Cebaracetam; CefadroxillCefadroxil Hemi [0231] Other active agents include: 16-Alpha Fluoroestra hydrate; Cefcapene Pivoxil; Cefdaloxime Pentexil Tosilate; diol; 16Alpha-Gitoxin; 16-Eplestriol; 17 Alpha Estradiol; Cefditoren Pivoxil; Cefepime Hydrochloride (Arginine For 17Beta Estradiol; IAlpha-Hydroxyvitamin D2; 1-Decpyrro mulation); Cefetamet; Cefetamet Pivoxil, Cefffietazole; Cef lidinone; 1-Dodecpyrrolidinone; 22-Oxacalcitriol; 2CVV, luprenam; Cefnminox; Cefodizime; Cefoselis; Cefotiam; 2'-Nor-cGMP; 3-Isobutyl GABA; 6-FUDCA; 7-Methoxyta Cefotiam Hexetil: Cefozopran; Ce?pirome; Ce?sulodin; crine; Abacavir Sulfate; Abanoquil; Abecarnil; Acadesine; Ceftazidime (Arginine Formulation); Ceftazidime Sodium; Acamprosate; Acebutolol Hydrochloride; Aceclofenac; Cefteram; Ceftibuten Dihydrate; Ceftriaxone; Celastrol; Acetomepregenol; Acetrizoate Sodium; Acetylcysteine, Celecoxib; Celikalim; Celiprolol; Cellulose Sodium Phos N–; Acetyldigitoxin; Acetyl-L-carnitine; Acetylmethadol; phate; Cepacidine A; Cericlamine; Cerivastatin; Cerivastatin Acipimox; Acitemate; Aclatonium; Aconiazide; Acrivastinet; Sodium; Certoparin Sodium; Cetiedil; Cetirizine; Cetyl Adafenoxate; Adatanserin; Adefovir Dipivoxil; Adelmidrol; Alcohol; Cevimeline Hydrochloride; Chlormerodrin, Ademetionine; Adiposin; Adrafinil; Alacepril; Aladapcin; Hg-197; Chlormezanone; Chloroorienticin A; Chloroorienti Alaptide; Alatrofloxacin Mesylate; Albolabrin; Albumin cin B; Cholecalciferol; Cholestyramine; Choriogonadotropin Chromated Cr-51 Serum; Albumin Human; Albumin Iodi Alfa; Chromic Phosphate, P-32; Chymopapain; Chymot nated I-125 Serum; Albumin Iodinated 1-131 Serum; Alde rypsin; Cibenzoline: Ciclesonide; Cicloprolol; Cilansetron; calmycin; Alendronic Acid; Alentemol; Alfacalcidol; Alfu Cilmidipine; Cilobradine, Cilostazol; Cimetropiurn Bromide; zosin; Alglucerase; Alinastine; Alitretinoin; Alkavervir, Cinitapride; Cinolazepam, Ciprostene; Cisapride Monohy Allopurinol Sodium; Almotriptan Malate; Alosetron; Alpha drate; Cisatracurium, Besilate; Cistinexine; Citalopram; Cit Idosone; Alpha-Tocopherol; Alpha-Tocopherol Acetate; alopram Hydrobromide; Citicoline; Citreamicin Alpha; Alseroxylon; Altromycin B; Amantadine-HCl, Ambenonium Clausenamide: Clidinium Bromide: Clinafloxacin; Clom Chloride: Amelometasone: Amezinium Metilsulfate:Amfeb ethiazole; Clopidogrel; Clopidogrel Bisulfate; Cobalt Chlo utamone; Amifloxacin; Aminolevulinic Acid Hydrochloride; ride, Co-57; Cobalt Chloride, Co-60; Colesevelam Hydro Aminosalicylic Acid Resin Complex; Amiodarone Hydro chloride; Colestimide; Colfosceril Palmitate; Complestatin; chloride; Amisulpride; Amlodipine; Ammonium Lactate; Contignasterol; Contortrostatin; Corticotropinzinc Hydrox Amphetamine Adipate; Amphetamine Aspartate; Amphet ide; Cosalane; Costatolide; Cotinine; Cournermycin AI; amine Resin Complex; Ampiroxicam; Amprenavir; Amylin; Cryptenamine Acetates; Cryptenamine Tannates: Cucumari Amythiamicin; Ananain; Anaritide; Anileridine Phosphate; osid; Curdlan Sulfate; Curiosin; Cyanocobalamin; Cyanoco Anisindione; Anordrin; Apadoline; Apafant; Apraclonidine; balamin, Co-57; Cyanocobalamin, Co-58; Cyanocobalamin, Aprepitant; Aprosulate Sodium; Aprotinin Bovine; Apti Co-60; Cyclazosin; Cyclic HPMPC; Cyclobenzaprine; ganel; Aranidipine; Arbekacin; Arbidol; Arbutamine; Arecat Cyclobut A: Cyclobut G; Cyclocapron; Cyclosin; Cyclothia annin B 1: Argatroban; Aripiprazol; Aripiprazole; Arotinolol; lidine; Cyclothiazomycin; Cycrimine Hydrochloride; Cypro Articaine Hydrochloride; Ascorbic Acid, Asimadoline; terone; Cysteamine Bitartrate; Cytochalasin B; Dactimicin; Aspalatone; Asperfuran; Aspoxicillin; Atazanavir Sulfate; Daidzein; Daidzin; Danaparoid; Daphnodorin A; Dapipra Atenolol, S-3 Atevirdine; Atomoxetine Hydrochloride; zole; Dapitant; Darifenacin; Darlucin A; Darsidomine; Atpenin B; Atrinositol; Aureobasidin A; Avobenzone; Aza Daunorubicin Citrate; DdCTP; Decamethonium Bromide: dirachtine; Azelaic Acid; Azelastine; Azelnidipine; Azimil Deferiprone; Deferoxamine Mesylate; Dehydrodidemnin B; ide; Azithromycin Dihydrate; Aztreonwn; Baccatin III; Baco Delapril; Delequarnine; Delfaprazine; Delmopinol; Del side A: Bacoside B: Bactobolamine; Balazipone; phinidin; Deoxypyridinoline; Deprodone; Depsidomycin Balhimycin; Balofloxacin; Balsalazide; Bambuterol; Bao deramciclane; Dermatan Sulfate; Deserpidine; Desirudin; huoside 1; Barnidipine; Batebulast; Beauvericin; Becapler Desloratadine; Desmopressin: Desoxoamiodarone; Desox min; Becliconazole; Beclomethasone Dipropionate Monohy yribonuclease; Detajrniurn Bitartrate; Dexketoprofen; Dex drate; Befloxatone; Bellenamine; Benflumetol; Benidipine; loxiglumide; Dexmethylphenidate Hydrochloride; Dexra Bentoquatam; Benzisoxazole; Benzoidazoxan; Benzoyl Per zoxane Hydrochloride; Dexsotalol; Dextrin 2-Sulphate: oxide; Benzphetamine Hydrochloride; Benzquinamide Dextroamphetamine Adipate; Dextroamphetamine Resin Hydrochloride; Benztropine; Benzyl Benzoate; Benzyl Peni Complex; Dextroamphetamine Saccharate; Dextrose; cilloyl-Polylysine; Bepridil; Beractant; Beraprost; Ber Diclofenac Digolil; Dicranin; Dienogest; Diethylhomospen lafenone; Bertosamil: Besipirdine; Beta-Carotene; Betaine, nine; Diethylnorspermine; Difenoxin Hydrochloride; Dihy Anhydrous; Betamipron; Betaxolol; Betazole Hydrochlo drexidine; Diltiazeim; Dimethyl Prostaglandin Al; Dimeth ride; Bevantolol; Bexarotene; Bifemelane; Bimakalim; ylhomospermine; Dimiracetarn; Dimyristoyl Lecithin; Bimatoprost; Bimithil; Binospirone; Biotin; Bioxalomycin Diphemanil Methylsulfate; Diphencyprone; Diphenylpyra Alpha2; Biriperone; Bisaramil; Bisaziridinylspermine; Bis line Hydrochloride; Diprafenone; Dipropylnorspermine; Benzimidazole A; Bis-Benzimidazole B: Bismuth Subsalicy Discodermolide; Divalproex; Docarparnine; Docosanol, 1-, late; Bistramide D; Bistramide K; Boldine; Bopindolol; Bort Dolasetron Mesylate Monohydrate; Domitroban; Donepezil ezomib; Brefeldin; Brimonidine; Brinzolamide: Bromfenac: Hydrochloride; Dorzolamide; Dosmalfate; Dotarizine; Dox Bucindolol; Budipine; Bunazosin; Butenafine; Butenafine azosin; Doxercalciferol; Draculin; Drosperidone; Dro Hydrochloride; Butixocort Propionate; Cabergoline; Caf spirenone; Drotaverine Acephyllinate; Droxicam, Dutast US 2011/0028460 A1 Feb. 3, 2011

eride; Ebiratide; Ebrotidine; Ecabapide; Ecabet; Ecdisteron; Interleukin-8, Interleukin? Alpha; Intrinsic Factor; Inulin; Echicetin; Echistatin; Ecteinascidin 722; Ecteinascidin 729; Invert Sugar, Iobenguane Sulfate I 131; Iobitridol; Iodamide Ecteinascidin 743; Edaravone; Edetate Calcium Disodium; Meglumine; Iodipamide Sodium; Iodoamiloride; Iodohippu Edetate Disodium; Edobacomab; Edrecolornab; Efavirenz; rate Sodium, 1-123; Iodohippurate Sodium, 1-131; Iofe Efegatran; Efonidipine; Egualen; Elcatonin; Eletriptan; Elet tamine Hydrochloride 1-123; Iofratol; Iopromide; Iopyrol; riptan Hydrobromide; Elgodipine; Eliprodil; Eltenac; Iorneprol; Iothalamate Sodium, 1-125; Iotriside; Ioxaglate Emakalim; Emedastine; Emedastine Difumarate; Emiglitate; Sodium; Ipazilide; Ipenoxazone; Ipidacrine; Ipomeanol, 4; Emoctakin; Emtricitabine; Enalapril; Enazadrem; Enfu Ipriflavone; Ipsapirone; Irbesartan; Irloxacin; Iron Dextran; virtide; Englitazone; Entacapone; Enterostatin; Eplerenone; Iron Sucrose; Irternazole; Isalsteine; Isbogrel; Iseparnicin; Epoxymexrenone; Eptastigmine; Eptifibatide; Erdosteine; Isofloxythepin; Isopropyl Unoprostone; Itameline; Itopride; Ergocalciferol; Ersentilide; Ertapenem Sodium; Erythritol; Ketoprofen, R=; Ketoprofen, S-; Ketorolac, Lactitol; Lac Escitalopram Oxalate; Esomeprazole Magnesium; Esta tivicin; Lactulose; Laennec; Lafutidine; Lanoconazole; Lan zolam; Estradiol Acetate; Esuprone; Etanterol; Ethacizin; perisone; Larnifiban; Larnotrigine; Latanoprost; Lateritin; Ethchlorvynol; Ethinamate; Ethinylestradiol; Ethoxzola Laurocaprarn, Leflunomide; Lemefloxacin; Leminoprazole; mide; Etidocaine Hydrochloride; Etizolam; Etrabamine; Lenercept; Lepirudin; Leptin; Lercanidipine; Lerisetron; Eveninomicin; Examorelin; Ezetimibe; Faerie?tmgin; Lernildipine; Lesopitron; Letrazuril; Leucomyzin; Leval Fantofarone; Famciclovir, Faropenem; Fasidotril; Fasudil; buterol Hydrochloride; Levallorphan Tartrate; Levamisole Fedotozine; Felbarnate; Fenofibrate; Fenoldopam; Fen Hydrochloride; Levetiracetam; Levobetaxolol; Levobunolol; spiride; Fentanyl; Fenticonazole; Fepradinol; Ferpifosate Levobupivacaine; Levobupivacaine Hydrochloride; Levo Sodium; Ferristene; Ferrixan; Ferrous Citrate, Fe-59; Fex cabastine; Levocarnitine; Levodropropizine; Levofloxacin; ofenadine Hydrochloride; Fibrinogen, 1-125; Fibrinolysin; Levopropoxyphene Napsylate, Anhydrous; Levormelox Flecainide; Flerobuterol; Flesinoxan; Flezelastine; Flobufen; ifene; Levornoprolol; Levosimendan; Levosulpiride; Lin Flomoxef, Florfenicol; Florifemine; Flornastat; Flosatidil; dane; Linezolid; Linotroban; Linsidormine; Lintitript; Linto Fludeoxyglucose, F-18; Flumecinol; Flunarizine; Fluocal pride; Lipase; Lirexapride; Lithium Carbonate; Lithium citriol; Fluoxetine, R=; Fluoxetine, S-; Fluparoxan; Flu Citrate; Lodoxamide; Lomerizine; Lonazolac, Lopinavir, pirtine; Flurbiprofen Axetil: Flurithromycin; Flutamide; Lorglumide; Losartan; Losigamone; Loteprednol; Loviride; Flutrimazole; Fluvastatin: Fluvoxamine; Folic Acid; Fol Loxapine Hydrochloride; LpdR; Lubeluzole; Lutetium; Luz litropin Alfa; Follitropin Alfa/Beta; Fomivirsen Sodium; indole; Lydicamycin; Lysostaphin; Magainin 2 Armide; Mag Fondaparinux Sodium; Forasartan; Formoterol; Formoterol nesium Acetate; Magnesium Acetate Tetrahydrate; Mag Fumarate; Formoterol, R,R, Fosinopril; Fosphenytoin: Fro nolol; Malathion; Mallotochromene; Mallotojaponin; vatriptan Succinate; Fulvestrant; Furosernide; Gadobenic Mangafodipir; Mangafodipir Trisodium; Manidipine; Mani Acid, Gadobutrol; Gadodiamide-EOB-DTPA; Gadopen wamycin A; Mannitol; Manurnycin E: Manurnycin F; Mapi tetate Dimeglumine; Gadoteric Acid; Galantamine; Galan nastine; Martek 8708; Martek 92211; Massetolide; Meglu tamine Hydrobromide; Galdansetron; Gallopamil: Gamo mine Metrizoate; Meloxicam, Melphalan Hydrochloride; lenic Acid; Gatifloxacin; Gefitinib; Gemifloxacin Mesylate; Menadiol Sodium Diphosphate; Menadione; Meprednisone; Gemtuzumab Ozogamicin; Gepirone; Girisopam; Glaspi Mequinol; Mersalyl Sodium; Mesna; Metformin Hydrochlo mod: Glatiramer Acetate; Glaucocalyxin A; Glucagon ride; Methantheline Bromide; Metharbital; Methoxamine Hydrochloride; Glucagon Hydrochloride Recombinant; Glu Hydrochloride; Methoxatone; Methoxsalem; Methscopola cagon Recombinant; Gluconolactone; Glutapyrone; Glu mine Bromide; Methyclothiazide; Methyldopa; Methylhista tathione Disulfide; Glycopine; Glycopril; Goserelin Acetate; mine, R-alpha; Methylinosine Monophosphate; Methylpred Grepafloxacin; Grepafloxacin Hydrochloride; Guaifenesin; nisolone Aceponate; Methyprylon; Metiparnide; Guanidine Hydrochloride; Halichondrin B; Halofantrine; Metipranolol Hydrochloride; Metolazone; Metoprolol Halomon; Haloperidol Lactate; Halopredone; Hatomarubi Fumarate; Metoprolol, S-; Metoprotol Tartrate; Metri gin C; Hatornambigin D; Hatornamicin; Hatornarubigin A; fonate; Metrizoate Magnesium; Metrizoic Acid; Mezlocillin Hatornarubigin B; Heparin Calcium; Heparin Sodium; Hexo Sodium Monohydrate; Michellarmine B; Microcolin A; cyclium Methylsulfate; Hexylcaine Hydrochloride; Histrelin Midodrine; Miglustat; Milacernide; Milarneline; Mildronate; Acetate; Hyaluronidase; Hydrocortamate Hydrochloride; Milnacipran; Milrinone Lactate; Miokarnycin; Mipragoside; Hydrocortisone Cypionate; Hydrocortisone Probutate; Mirfentanil; Mivazerol; Mixanpril; Mizolastine; Mizoribine; Hydro quinone; Hydroxocobalamin; Hydroxypropyl Cellu Moexipril; Moexipril Hydrochloride; Mofezolac, Mometa lose; Hydroxystilbamidine Isethionate; Ibandronate Sodium; sone; Mometasome Furoate Monohydrate; Monobenzone; Ibogaine; Ibudilast; Ibuprofen Potassium; Icodextrin; Illi Montinelin; Moracizine; Moricizine Hydrochloride; maquinone; Iloprost; Imatinib Mesylate: Imidapril; Imidaze Mosapramine; Mosapride; Motilide; Moxifloxacin Hydro nil; Imiglucerase; Imipramine Pamoate; Inamrinone Lactate; chloride; Moxiraprine; Moxonidine; Mupirocin; Mupirocin Indapamide; Indinavir, Indinavir Sulfate; Indium In-III Calcium; Mycophenolate Mofetil Hydrochloride; Nadifloxa Oxyquinoline; Indium In-III Pentetate Disodium; Indium In cin; Nadroparin Calcium; Nafadotride; Na?amostat; Naftopi III Pentetreotide Kit; Indometacin; Indometacin Farnesil; dil; Naglivan; Nalmefene Hydrochloride; Naltrexone Hydro Indomethacin Sodium; Inocoterone; Inogatran; Inolimomab; chloride; Napadisilate; Napsagatran; Naratriptan; Insulin Aspart; Insulin Aspart Protamine; Insulin Glargine; Nasaruplase; Nateglinide; Nateplasel; Nelfinavir Mesylate; Insulin Lispro Protamine; Interferon Alfa, Interferon Alfa Nesiritide; Niacinamide; Nicotine; Nicotine Polacrilex; NI; Interferon Beta; Interferon Beta-Ial; Interferon Gamma-I Niperotidine; Niravoline; Nisin; Nitazoxanide; Nitecapone; A: Interferon Gamma-I B; Interferon Omega; Interferon, Nitisinone; Nitrendipine, S-; Nitrofurantoin Monohydrate; Consensus; Interleukin-3; Interleukin-1; Interleukin-I Beta; Nitrofurantoin Sodium; Nitrofurantoin, Macrocrystalline; Interleukin-10; Interleukin-II; Interleukin-12; Interleukin Nitrofurazone; Nitroglycerin; Nonoxynol-9; Norel 15: Interleukin-2: Interleukin-4; Interleukin-5; Interleukin-7; gestromin; Octyl Methoxycinnamate; Olmesartan Medox US 2011/0028460 A1 Feb. 3, 2011 omil; Olopatadine; Olopatadine Hydrochloride; Olprinone; natomedin B; Somatrem: Somatropin; Sotalol; Staurospo Olsalazine; Omeprazole Magnesium; Ondansetron, R=; rine; Stepronin; Stobadine; Strontium Chloride, Sr-89; Suc Oral Hypoglyceremics; Orphenadrine Hydrochloride; Osel cibun; Sulfanilamide; Sulfaphenazole; Sulfapyridine; tamivir Phosphate; Otenzepad: Oxamisole; Oxaprozin Potas Sulfoxamine; Sulfoxone Sodium; Sulfur, Sultamicillin; Sul sium; Oxcarbazepine; Oxiconazole; Oxiracetam; Oxodipine; topride; Sumatriptan; Sutilains; Symakalim; Talbutal; Tan Oxybenzone; Oxybutynin, Oxyphencyclimine Hydrochlo dospirone; Tannic Acid; Tapgen; Taprostene; Tartaric Acid; ride; Oxyphenonium Bromide: Ozagrel; Palauarnine; Pali Tazanolast, Tegaserod Maleate; Telenzepine; Telmesteine; navir; Palomosetron Hydrochloride; Pamaparin Sodium; Pan Telmisartan; Temocapril; Tenofovir Disoproxil Fumarate; amesine; Pancrelipase; Panipenem; Panipenum; Pannorin; Tenosal; Tepirindole; Terazosin; Terbinafine Hydrochloride; Panornifene; Pantethine; Pantoprazole Sodium; Pantothenic Terflavoxate; Terguride; Terlipressin; Terodiline; Tertatolol; Acid; Paramethadione; Paricalcitol; Parnaqueside; Par Testosterone Buciclate: Thallous Chloride, TI-201: Thia nicogrel; Paroxetine Hydrochloride; Paroxetine Mesylate; mine; Thiamine Hydrochloride; Thiofedrine; Thiomarinol; Parthenolide; Pazufloxacin; Pegademase Bovine; Pegviso Thioperamide; Thiosemicarbazone; Thonzonium Bromide; mant; Pemirolast; Pemirolast Potassium; Penciclovir Thyroglobulin; Thyrotropin; Thyrotropin Alfa, Tiagabine; Sodium; Penicillamine; Pentafuside; Pentagastrin; Pentami Tiagabine Hydrochloride; Tianeptine; Tiapa?ant; Ticlopi dine; Pentamidine Isethionate; Pentetate Calcium Trisodium dine; Tienoxolol; Tilisolol; Tilnoprofen Arbamel; Tiludronic Yb-169; Pentigetide; Pentolinium Tartrate; Pentosan; Per Acid; Tiopronin; Tiotropium Bromide; Tirandalydigin; Tir flexane; Perfluoropolymethylisopropyl Ether; Perflutren; ilazad; Tirofiban; Tiropramide; Tocopherol Acetate; Toltero Pergolide; Pergolide Mesylate; Perindoprilat; Pernedolac, dine Tartrate; Torasemide; Trafennin; Trandolapril; Tranyl Perospirone; Phenaridine; Phenindione; Pheniramine Male cypromine Sulfate; Travoprost; Traxanox; Trazodone-HCl; ate; Phenmetrazine Hydrochloride; Phenotoxifyline; Treprostinil Sodium; Tretinoin Tocoferil; Triarntevene; Tri Phenserine; Phensuccinal; Phentermine Resin Complex; caprilin; Trichohyalin; Trichosanthin, Alpha; Triclosan; Phentolamine Mesilate; Phenylalanyl Ketoconazole; Phe Tridihexethyl Chloride; Trientine; Trientine Hydrochloride; nylephrine Bitartrate; Phenytoin Sodium, Extended; Pheny Triflavin; Trimegestone; Trimethoprim Hydrochloride; Tri toin Sodium, Prompt; Phosphoric Acid; Phytonadione; oxsalen; Triptorelin Pamoate; Trolamine Polypeptide Oleate Picenadol; Picroliv, Picumeterol; Pidotimod: Pilsicainide; Condensate; Trombodipine; Trometarnol; Tromethamine; Pimagedine; Pimecrolimus; Pimilprost; Pinocebrin; Pioglita Tropine Ester; Trospectomycin; Trovafloxacin; Trovafloxa zone; Piperonyl Butoxide; Pirlindole; Pirmenol; Pirodornast; cin Mesylate; Trovirdine; Tucaresol; Tulobuterol; Tylogenin: Polyestradiol Phosphate; Polyethylene Glycol 3350; Polytet Tyloxapol; Undecoylium Chloride; Undecoylium Chloride rafluoroethylene; Poractant Alfa; Potassium Chloride; Prami Iodine Complex: Unoprostone Isopropyl; Urapidil; Urea, pexole Dihydrochloride; Praziquantel; Prazosin; Prilocaine; C-13; Urea, C-14; Uridine Triphosphate; Valaciclovir; Valde Procaine Merethoxylline; Proguanil Hydrochloride; coxib; Valganciclovir Hydrochloride; Valproate Magnesium; Propagermanium; Propentofylline; Propiolactone; Propiom Valproate Semisodium; Valrubicin; Valsartan; Vamicamide; azine Hydrochloride; Propionylcamitine, L-; Propiram; Vanadeine; Vaninolol; Vasopressin Tannate; Venlafaxine; Propiram-Paracetarnol; Propiverine; Prostratin; Protegrin: Verapamil, (S); Veratrum Viride; Veroxan; Vexibinol; Vinbur Protein Hydrolysate; Protokylol Hydrochloride; Protosu nine Citrate; Vinburnine Resinate; Vinconate; Vinpocetine; floxacin; Prulifloxacin; Pyrethrins; Pyridoxine; Pyridoxine Vinpocetine Citrate; Vintoperol; Viomycin Sulfate; Vitamin Hydrochloride; Quazeparn; Quetiapine; Quetiapine Fuma A; VitaminA Palmitate; Vitamin E: Vitamin K; Voriconazole; rate; Quiflapon; Quinagolide; Quinapril; Quinethazone; Qui Voxergolide; Warfarin Potassium; Xemilofiban; Ximopro nidine Polygalacturonate; Raloxifene; Ramatroban; Ranelic fen; Yangarnbin, Zabicipril; Zacopride; Zacopride, R=; Acid; Ranolazine; Rapacuronium Bromide; Recainarn; Zafirlukast; Zalospirone; Zaltoprofen; Zanamivir; Zanar Regavirumab; Repaglinide; Rescinnamine; Resinferatoxin; nivir; Zankiren; Zatebradine; Zatosetron: Zenarestat; Reticulon; Reviparin Sodium; Revizinone; Riboflavin; Ribo Zinostatin Stimalarner, Ziprasidone; Ziprasidone Mesylate; flavin Phosphate Sodium; Ricasetron; Rilopirox, Rimanta Zoledronic Acid; Zolmitriptan; Zolpidern; Zopiclone; Zopi dine; Rimexolone; Rimoprogin; Riodipine; Ripisartan; clone, S-; Zopolrestat; and Zotepine. Risedronic Acid; Rispenzepine; Ritipenem Acoxil; Ritipen [0232) Still other examples of therapeutically active agents ern; Ritonavir; Rivastigmine Tartrate; Rizatriptan Benzoate; are listed in 2000 MedAdNews 19:56-60 and The Physicians Rnibefradil; Rnivacurium Chloride; Rofecoxib; Rokitamy Desk Reference, 53rd. Edition, pages 792-796, Medical Eco cin; Ropinirole; Ropivacaine; Ropivacaine Hydrochloride nomics Company (1999). Monohydrate; Roquinirnex; Rose Bengal Sodium, 1131; [0233] The topical formulations of the present invention Rosiglitazone Maleate; Roxatidine; Roxindole; Rubidium may include one or more skin care actives. “Skin care actives” Chloride Rb-82; Rufloxacin; Rupatidine, Ruzadolane; Sacro means all compounds or substances now known or later dem sidase; Safflower Oil: Safironil; Salbutamol, R=; Salnace onstrated to provide benefit when applied to skin and all din, R=; Samarium Sm 153 Lexidronam Pentasodium; San compounds now claimed or in the future claimed to provide fetrinem; Saprisartan; Sapropterin; Saquinavir; Sarcophytol benefit when applied to skin. Skin care actives may provide A Sargramostim; Sarneridine, Sarnpatrilat; Sarpogrelate; benefits, or claimed benefits, in areas such as one or more of Saruplase; Saterinone; Satigrel; Satumomab Pendetide; Sco wrinkle removal or wrinkle reduction, firming of skin, exfo polamine; Secretin: Selenomethionine, Se-75; Sematilide; liation of skin, skin lightening, treatment of dandruff, treat Sermorelin; Sermotiadil; Sertaconazole; Sertraline; Sertra ment of acne, skin conditioning, development of tans and line-HCl, Setiptiline; Sevelamer Hydrochloride; Sevirurnab; artificial tans, improvement of skin moisture content, Sezolamide; Sildenafil Citrate; Silipide; Silteplase; Silver improvement of skin barrier properties, control of sweat, Sulfadiazine; Simendan; Simethicone; Simethicone-Cellu anti-aging, reduction or avoidance of irritation and reduction lose; Sinitrodil; Sinnabidol; Sipatrigine; Sirnvastatin; or avoidance of inflammation. Examples of skin care actives Somatomedin C; Somatropin Recombinant; Sorbitol; Sor include molecules such as peptides, proteins, oligonucle US 2011/0028460 A1 Feb. 3, 2011

otides, fullerenes as well as small molecules. Skin care [0239] The topical formulation described above may also actives may be protease and/or enzyme inhibitors, anti-coen include propylene glycol. The propylene glycol may be zymes, chelating agents, antibodies, antimicrobials, humec present in the formulation between about 1% to about 25% tants, vitamins, skin protectants, antioxidants and/or skin w/w. Additionally the topical formulation may also include soothing agents, plant extracts and the like. Examples of skin ethanol and/or polyethylene glycol 300. The ethanol may be care actives include but are not limited to vitamin C, vitamin present in the formulation between about 1% to about 25% E (alpha tocopherol), retinoids, soy derivatives (e.g. isofla w/w. The polyethylene glycol 300 may be present in the range vones), green tea polyphenols, alpha hydroxy acids (e.g. gly of between about 1% to about 80% w/w. In addition the colic and lactic acids), betahydroxy acids (e.g. salicylic acid), topical formulation may include at least one moisturizer/ poly hydroxy acids, alpha lipoic acid, hemp oil (glycerides), humectant. [0240] The present invention provides an improved topical niacinamide, dimethyl amino ethanol, coenzyme Q10, kine formulation for preferably facilitating topical or transdermal tin (plant growth hormone), dimethyl sulfone and botulinum administration of at least one therapeutically active agent. toxin. Other examples of skin care actives may be found in This enhanced effect is discussed further below and illus The Perricone Prescription by Nicholas Perricone, Harper trated in preferred embodiments of the invention described in Collins Publishers Inc., New York, 2002. the Examples. In another preferred embodiment the topical [0234] The topical formulations described herein may also formulation of the present invention provides a means for include one or more cosmetically orpharmaceutically accept targeting atherapeutically active agent to local tissue eitherin able carriers/excipients. Suitable carriers/excipients that may the skin or the underlying tissue. This latter preferred embodi be used in the topical formulations discussed herein are ment may be particularly beneficially applied for treatment of known in the art and include, but are not limited to, solubi conditions such as osteoarthritis and dermatological condi lizers such as C2 to Cs straight and branched chain alcohols, tions. The topical formulations may be applied either occlu diols and triols, moisturizers and humectants such as glycer sively or nonocclusively to the skin. In another preferred ine, amino acids and amino acid derivatives, polyaminoacids embodiment of the invention, in applications where the objec and derivatives, pyrrolidone carboxylic acids and their salts tive is transdermal administration of a therapeutically active and derivatives, surfactants such as sodium laureth sulfate, agent to the systemic circulation, the topical formulation is sorbitan monolaurate, emulsifiers such as cetyl alcohol, applied to the skin under occlusion in a transdermal patch. stearyl alcohol, thickeners such as methyl cellulose, ethyl [0241] The present topical formulation may be applied to cellulose, hydroxymethylcellulose, hydroxypropylcellulose, the skin by any means known in the art including, but not polyvinylpyrrolidone, polyvinyl alcohol and acrylic poly limited to, by an aerosol, spray, pump-pack, brush, swab, or mers. Other examples of suitable excipients, such as binders other applicator. Preferably, the applicator provides either a and fillers are listed in Remington’s Pharmaceutical Sciences, fixed or variable metered dose application such as a metered 18th Edition, Ed. Alfonso Gennaro, Mack Publishing Co. dose aerosol, a stored-energy metered dose pump or a manual Easton, Pa., 1995 and Handbook of Pharmaceutical Excipi metered dose pump. Preferably the drug delivery system is ents, 3rd Edition, Ed. Arthur H. Kibbe, American Pharmaceu applied to the skin of the human or animal covering a delivery tical Association, Washington, D.C. 2000. surface area between about 10 and 800 cm3, more preferably [0235] The topical formulations of the present invention between about 10 and 400 cmº, and most preferably about 10 may also be formulated to include other chemical penetration and 200 cm3. The application is most preferably performed enhancers which have significant ability to enhance transport by means of a topical metered dose spray combined with an of actives. Such substances may have the character of surfac actuator nozzle shroud which together accurately control the tants, a zone-like compounds, solvents, alcohols, fatty acids, amount and/or uniformity of the dose applied. One function fatty esters, aliphatic thiols and the like. Examples of chemi of the shroud is to keep the nozzle at a pre-determined height cal penetration enhancers are reported in the paper of Santus above, and perpendicular to, the skin to which the drug deliv et al. (Santus, C. G. and Baker, R. W., Transdermal enhancer ery system is being applied. This function may also be patent literature. Journal of Controlled Release 1993.25:1 achieved by means of a spacer-bar or the like. Another func 20.) tion of the shroud is to enclose the area above the skin in order [0236] The topical formulation of the present invention to prevent or limit bounce-back and/or loss of the drug deliv may be formulated by those skilled in the art as liquids, ery system to the surrounding environment. Preferably the solutions, emulsions, creams, lotions, suspensions, triturates, area of application defined by the shroud is substantially gels, jellies, foams, pastes, ointments, shampoos, adhesives circular in shape. and the like. [0242] The drug delivery system may be a unit volume [0237] The penetration enhancing effect may be measured dispenser with or without a roll-on or other type of applicator. using techniques known in the art. An example of one mea It may also be necessary to apply a number of dosages on surement method is described in the Examples below. untreated skin to obtain the desired result. [0238] Preferably, the topical formulation includes at least [0243] Embodiments of the invention will be described one active agent such as a therapeutically effective agent or a with reference to the following Examples which are provided skin care active. Examples of suitable active agents are for illustrative purposes only and should not be used to limit described above. Preferably, the at least one active agent the scope of or construe the invention. comprises a non-steroidal antiinflammatory drug (NSAID). Examples of suitable NSAIDs that may be used in the present Examples topical formulation are described above. For example the Materials and Methods for Examples 1-7 formulation described above may include diclofenac, and particularly diclofenac sodium, as the at least one active [0244] A number of formulations (described in Examples agent. 1-7 below) containing diclofenac sodium (a non-steroidal US 2011/0028460 A1 Feb. 3, 2011 anti-inflammatory drug or NSAID) were tested for perme pylene glycol and propylene glycol 300 in a volume ratio of ation through porcine skin using the Franz diffusion cells [as 2:2:1:1. The base formulation further comprised diclofenac generally described in Franz T. J. Percutaneous absorption. sodium in a concentration of 1.5 wt.% per unit volume of the On the relevance of in vitro data. J. Invest Dermatol 1975; base composition. In the Examples below, various combina 64:190-195]. tions of the MPETMs detailed below were added to the base [0245) More specifically, Franz cells with a 5 ml receptor composition. well volume were used in conjunction with full-thickness porcine skin harvested at Perry Scientific (San Diego, Calif.). Example 1 The porcine skin was shaved free of hair, washed with water and subcutaneous fat was removed. The donor well had an [0259] In this Example, N-lauroyl sarcosine (NLS) and area of ~0.5 cm^*Receptor wells were filled with isotonic isopropyl myristate (IM) were added to the base formulation. phosphate buffered saline (PBS) doped with 0.01% sodium The details of each formulation and the results of the Franz azide. The flanges of the Franz cell were coated with vacuum diffusion cell experiments are set out in Table 3. grease to ensure a complete seal and were clamped together [0260] With reference to Table 3, it can be seen that For with uniform pressure using a pinch clamp (SS #18 VWR mulation 2 (containing a mixture of NLS and IM each at a 80073-350). concentration 2.5% wt/vol.) was more effective at enhancing [0246] After the Franz cells were assembled, the porcine diclofenac sodium flux rates through the skin when compared skin was allowed to pre-hydrate for 45 minutes with isotonic to either of Formulation 3 (containing 5% wt./vol NLS and no PBS. Isotonic PBS was then removed and 200 ml of the IM) or Formulation 4 (containing 5% wt./vol IM and no formulation was applied to the donor well. Receptor wells of NLS). the Franz cells were maintained at 37°C. (temperature on the [0261) Further and surprisingly, Formulation 1 (containing surface of the skin is ~30°C.) in a stirring block with con a mixture of NLS and IM each at a concentration of 1.5% tinual agitation via a stir bar. wt./vol) was approximately seven times more effective at [0247] The flux rates were calculated by assuming a radius enhancing the flux rate of the diclofenac sodium when com of 0.4 cm in the donor well (i.e., an area of 0.503 cm^). The pared to Formulation 2. HPLC calibration curve for diclofenac was determined to have a slope of 115.6 AUC/(ug diclofenac/ml). Example 2 [0248] Samples were drawn from the receptor wells at t=24 [0262] In this Example, N-lauroyl sarcosine (NLS) and hours and t=46 hours for all formulations. Franz diffusion cell oleic acid (OA) were added to the base formulation. The measurements were made in five-fold replicates for each details of each formulation and the results of the Franz diffu formulation. sion cell experiments are set out in Table 4. [0249] The concentration of diclofenac in the samples was [0263] With reference to Table 4, it can be seen that For measured using HPLC analysis. Specifically, HPLC was car mulation 5 (containing a mixture of NLS and OA each at a ried out with C18 column and using acetonitrile and water as concentration 1.5% wt/vol.) was more effective at enhancing the mobile phase. Flux rates were calculated using standard diclofenac sodium flux rate through the skin when compared equations based on the total transference of diclofenac across to either of Formulation 6 (containing 5% wt./vol NLS and no the skin after 46 hours. Thus, flux rates, F, were computed OA) or Formulation 7 (containing 5% wt./vol OA and no according to NLS). [0264] It is notable that the flux rate of the NSAID in Formulation 5 was higher than that achieved by either of Formulation 6 or Formulation 7 in spite of the fact that the total concentration of the molecular penetration enhancers in Formulation 5 was lower that that in Formulation 6 and For wherein; D is the concentration of the drug in the receptor mulation 7. well after incubation time t, V is the volume of the receptor well and A is the surface are of skin. Example 3 [0250] Individual penetration enhancers in the Examples discussed below were obtained from the following sources: [0265] In this Example, sodium octyl sulfate (SOS) and [0251] glyceryl oleate (glycerol monooleate) from TCI oleic acid (OA) were added to the base formulation. The (VWR), product code TCG0082 details of each formulation and the results of the Franz diffu [0252) isopropyl myristate from Sigma product code sion cell experiments are set out in Table 5. MO757 [0266] With reference to Table 5, it can be seen that For [0253) methyl laurate from Chem Service product code mulation 8 (containing a mixture of SOS and OA each at a CSO426 concentration 1.5% wt/vol and 3.5% wt/vol, respectively) [0254] N-lauroyl sarcosine from Sigma product code was more effective at enhancing diclofenac sodium flux rate L5000 through the skin when compared to either of Formulation 9 [0255] oleic acid (octadecenoic acid) from Mallinckroft (containing 5% wt./vol OA and no SOS) or Formulation 10 (VWR) product code MK274404 (containing 5% wt./vol SOS and no OA). [0256] sodium laurylsulfoacetate from Stepan (65-72%) Example 4 product code Lathanol LAL [0257) sodium octyl sulfate from Alfa Aesar (VWR) [0267] In this Example, glyceryl oleate (GO) and sodium product code AA43750-06 octyl sulfate (SOS) were added to the base formulation. The [0258] The base composition used for each formulation of details of each formulation and the results of the Franz diffu a carrier composition comprising isotonic PBS, ethanol, pro sion cell experiments are set out in Table 6. US 2011/0028460 A1 Feb. 3, 2011 20

[0268] With reference to Table 6, it can be seen that For vacuum grease to ensure a proper seal) and a receptor well. mulation 11 (containing a mixture of GO and SOS each at a The wells were clamped together and held in place using a concentration 1.5% wt/vol.) was approximately as effective spring clamp. at enhancing diclofenac sodium flux rate through the skin as [0278] The receptor wells had a volume of 3.3m.1 and the Formulation 12 (containing 5% wt./vol GO and no SOS) and clamped skin had an available surface area of ~0.55 cm for was substantially improved over that of Formulation 13 (con the diffusion study. Once the cell was assembled, the receptor taining 5% wt./vol SOS and no GO). well was filled with PBS containing 0.01 wt % NaNs (to help Example 5 prevent skin degradation). Care was taken to ensure all bubbles are removed from the receptor solution. The skin was [0269] In this Example, glyceryl oleate (GO) and methyl allowed to pre-hydrate for 20 minutes before the formulations laurate (ML) were added to the base formulation. The details were applied to the skin. of each formulation and the results of the Franz diffusion cell experiments are set out in Table 7. [0279| Diffusion cell testing: After the skin was prehy [0270] With reference to Table 7, it can be seen that For drated, 40 pil of the test formulation was applied to the skin mulation 14 (containing a mixture of GO and ML each at a with a positive displacement pipettor and the applied dose concentration 2.5% wt/vol.) was more effective at enhancing then rubbed gently across the skin with a glass stir rod. Once diclofenac sodium flux rate through the skin when compared the formulation was applied, a stir bar was added to the to either of Formulation 15 (containing 5% wt./vol GO and no receptor well. The receptor well was maintained at 32°C. and ML) or Formulation 16 (containing 5% wt./vol ML and no continuously agitated throughout the experiment. Sample ali GO). quots were drawn from the receptor well at varying time points and replaced with fresh PBS buffer. Sample aliquots Example 6 were filtered and analyzed for concentration of the active [0271] In this Example, sodium laurylsulfoacetate (SLSA) using HPLC analysis. Measurements for each formulation and methyl laurate (ML) were added to the base formulation. were carried out in six-fold replicates. The details of each formulation and the results of the Franz [0280] The individual penetration enhancers used in diffusion cell experiments are set out in Table 8. Example 8 are provided in the following table along with their [0272] With reference to Table 8, it can be seen that For abbreviation (Abbr) and Chemical Abstract Service (CAS) mulation 17 (containing a mixture of SLSA and ML each at a registry number: concentration 2.5% wt/vol.) was more effective at enhancing diclofenac sodium flux rate through the skin when compared to either of Formulation 18 (containing 5% wt./vol SLSA and no ML) or Formulation 19 (containing 5% wt./vol ML and no Abbr Chemical CAS SLSA). IM Isopropyl Myristate 110-27-0 SLSA Sodium Lauryl Sulfoacetate 1847–58–1 Example 7 OA Oleic Acid 112–801–1 ML Methyl Laurate 111–82–0 [0273] In this Example, sodium laurylsulfoacetate (SLSA) GO Glyceryl Monooleate 3.1566–31–1 and isopropyl myristate (IM) were added to the base formu NLS N-lauroyl Sarcosine 97–78-9 lation. The details of each formulation and the results of the Franz diffusion cell experiments are set out in Table 9. [0281) Numerous formulations were prepared with the [0274] With reference to Table 9, it can be seen that For MMPETMs used in conjunction with varying active agents. mulation 20 (containing a mixture of SLSA and IM each at a MMPETMs tested were SLSA/IM, SLSA/ML, IM/NLS, concentration 2.5% wt/vol.) was more effective at enhancing GO/ML, and NLS/OA in a hydroalcoholic solution. These diclofenac sodium flux rate through the skin when compared MMPETMs were tested with the active agents ibuprofen, to either of Formulation 21 (containing 5% wt./vol SLSA and buproprion HCl, ketoprofen and testosterone. Tables 10-19 no IM) or Formulation 22 (containing 5% wt./vol IM and no list the MMPETMs that showed a significant increase in flux SLSA). when compared to flux from the analogous formulations con Materials and Methods for Example 8 taining only one of the MPETMs. [0282] While this invention has been described with refer [0275] Using methodology similar to that described in ence to illustrative embodiments and examples, the descrip Examples 1-7, a number of formulations containing other tion is not intended to be construed in a limiting sense. Thus, active agents (as described in greater detail below) were various modifications of the illustrative embodiments, as well tested for permeation through porcine skin using Franz dif as other embodiments of the invention, will be apparent to fusion cells. persons skilled in the art upon reference to this description. It is therefore contemplated that the appended claims will cover Franz Cell Guidelines: any such modifications or embodiments. Further, all of the [0276] Skin preparation: Porcine skin was sourced from claims are hereby incorporated by reference into the descrip Lampire Biological Laboratories (Pipersville, Pa.). The skin tion of the preferred embodiments. was then dermatomed in house to a set thickness. [0283] All publications, patents and patent applications (0277| Diffusion cell assembly: Diffusion cells were referred to herein are incorporated by reference in their assembled using dermatomed porcine skin as the substrate. entirety to the same extent as if each individual publication, Cell assembly was carried out by clamping the skin between patent or patent application was specifically and individually a donor well (the flange was coated with a thin coating of indicated to be incorporated by reference in its entirety. US 2011/0028460 A1 Feb. 3, 2011 21

TABLE 1

NSAID TRADE NAME STRUCTURE

Diclofenac Voltaren, Pennsaid Cl

NH

C| OH

O

Indomethacin Indocin H3CO

Sulindac Clinoril F

OH º O

s-CH3 O

Tolmetin Tolectin

Naproxen Naprosyn, Aleve = º 2s OH O H3CO

Ibuprofen Advil, Brufen, Motrin OH

O US 2011/0028460 A1 Feb. 3, 2011

TABLE 1-continued

NSAID TRADE NAME STRUCTURE

Flurbiprofen Ansaid, Flurwood, Froben OH

O

F

Ketoprofen Orudis O

OH

O

Ketorolac Acular, Toradol O

N | OH

O

Fenoprofen Nalfon O

O OH

Bromfenac Xibrom O NH2

OH

Br C C O

TABLE 2

COMPOUND TRADE NAME STRUCTURE Acetaminophen Tylenol {

HO C? O

Aspirin CO2H US 2011/0028460 A1 Feb. 3, 2011

TABLE 2-continued

COMPOUND TRADE NAME STRUCTURE

Celecoxib Celebrex

~ ! /TººCF

Diflunisal Dolobid CO2H

Etoricoxib Arcoxia

Piroxicam Feldane, Roxam 2. | O OH S. N NH 2. | N 2." ~ S /\ O O Rofecoxib Vioxx \ O=S | O O

Salsalate Disalcid, Monogesic, Salflex, OH O OH Salcitab

O

O US 2011/0028460 A1 Feb. 3, 2011

TABLE 2-continued

COMPOUND TRADE NAME STRUCTURE Meloxicam Mobic _{j*sº N O OH H _^ N >s /\ O O

Etodolac Lodine OH H N | || 0

Oxaprozin Daypro O

Nabumetone Relafen O

Mefenamic acid Ponstel

Q- O OH H3C CH3

Meclofenamic Acid Meclofen, Meclomen O OH C| H N

Cl

TABLE 3 TABLE 4

NLS+ IM] - - Flux , [NLS + O.A. Flux Formulation (wt.%/vol.) Weight Ratio of NLS:IM (Ig/hr/cm^) Formulation (wt.%/vol.) Weight Ratio of NLS:OA (ug/hr/cm3) 1 3.0 1:1 3.80 - 2 5.0 1:1 0.53 5 3.0 1:1 3.29 3 5.0 1:0 0.26 6 5.0 1:0 0.26 4 5.0 0:1 0.02 7 5.0 0:1 2.70

US 2011/0028460 A1 Feb. 3, 2011 26

15. The topical formulation of claim 1, wherein the weight TABLE 1.9 ratio of the first compound to the second compound is in the range of from about 1:3 to about 3:1. Formu- TestosterOne SLSA IM Flux 16. The topical formulation of claim 1, wherein the weight lation (wt %/wt %). (wt %/wt %). (wt %/wt %). (ug/hr/cm3) ratio of the first compound to the second compound is in the 50 5 3 14.3 range of from about 1:2 to about 2:1. 51 5 3 9.1 17. The topical formulation of claim 1, wherein the weight 52 5 1.5 1.5 18.8 ratio of the first compound to the second compound is about 1:1. 18. The topical formulation of claim 1, wherein the at least What is claimed is: one active agent is an O-aryl alkanoic acid. 1. A topical formulation comprising: (i) at least one active 19. The topical formulation of claim 18, wherein the O-aryl agent, (ii) a first compound, and (iii) a second compound, alkanoic acid is an anti-inflammatory drug, such as a non wherein the first compound and second compound are differ steroidal anti-inflammatory drug (NSAID), or an analgesic. ent, and each is selected from the group consisting of N-lau 20. The topical formulation of claim 18, wherein the O-aryl roylsarcosine, sodium octylsulfate, methyl laurate, isopropyl alkanoic acid is selected from the group consisting of bro myristate, oleic acid, glyceryl oleate and sodium lauryl sul mfenac, diclofenac, fenoprofen, flurbiprofen, ibuprofen, foacetate. indomethacin, ketoprofen, ketorolac, naproxen, sulindac and 2. The topical formulation of claim 1, wherein the first tolmetin, and pharmaceutically acceptable salts and solvates compound comprises sodium lauryl sulfoacetate and the sec thereof and mixtures thereof. ond compound comprises isopropyl myristate. 21. The topical formulation of claim 20, wherein the O-aryl 3. The topical formulation of claim 1, wherein the first alkanoic acid is selected from the group consisting of compound comprises sodium lauryl sulfoacetate and the sec diclofenac, ibuprofen and ketoprofen, and pharmaceutically ond compound comprises methyl laurate. acceptable salts and solvates thereof, and mixtures thereof. 4. The topical formulation of claim 1, wherein the first 22. The topical formulation of claim 1, wherein the at least compound comprises isopropyl myristate and the second one active agent is acetaminophen or an NSAID selected compound comprises N-lauryl sarcosine. from the group consisting of aspirin, celecoxib, diflunisal, 5. The topical formulation of claim 1, wherein the first etodolac, etoricoxib, meclofenamic acid, mefenamic acid, compound comprises glyceryl monooleate and the second meloxicam, nabumetone, oxaprozin, piroxicam, salsalate, compound comprises methyl laurate. and rofecoxib, and pharmaceutically acceptable salts and sol 6. The topical formulation of claim 1, wherein the first vates thereof, and mixtures thereof. compound comprises N-lauroyl sarcosine and the second 23. The topical formulation of claim 1, wherein the at least compound comprises oleic acid. one active agent is a phenethylamine. 7. The topical formulation of claim 1, wherein the first 24. The topical formulation of claim 23, wherein the phen compound comprises sodium octyl sulfate and the second ethylamine is selected from the group consisting of antide compound comprises oleic acid pressants, anti-anxiety agents, anticholinergic agents, cholin 8. The topical formulation of claim 1, wherein the first ergics, dopaminergics, stimulants, serotonin antaogonists, compound comprises glyceryl oleate and the second com serotonin inhibitors, anti-emetics, antihistamines and/or pound comprises sodium octyl sulfate. antipsychotics. 9. The topical formulation of claim 1, further comprising a 25. The topical formulation of claim 24, wherein the phen biologically acceptable excipient. ethylamine is selected from the group consisting of bupro 10. The topical formulation of claim 1, wherein the total pion, amphetamine, hydroxyamphetamine, dextroamphet concentration of the first compound and the second com amine, methamphetamine, ephedrine, epinephrine, pound is up to about 50 wt.%, 40 wt.%, 35 wt.%, 30 wt.%, pseudoephedrine, dopamine, epinephryl borate, etafedrine, 25 wt %, 20 wt.%, 15 wt.%, 10 wt.%, 7.5 wt.% or 5 wt.%. norepinephrine and oxidopamine, and pharmaceutically per unit volume of the formulation. acceptable salts and solvates thereof, and mixtures thereof. 11. The topical formulation of claim 1, wherein the total 26. The topical formulation of claim 25, wherein the phen concentration of the first compound and the second com ethylamine is bupropion or a pharmaceutically acceptable pound is in the range of from about 2 wt.% to about 5 wt %, salt or solvate thereof. per unit volume of the formulation. 27. The topical formulation of claim 1, wherein the at least 12. The topical formulation of claim 1, wherein the total one active agent is a steroid. concentration of the first compound and the second com 28. The topical formulation of claim 27, wherein the ste pound is in the range of from about 2 wt.% to about 4 wt %, roid is selected from the group consisting of hormones, glu per unit volume of the formulation. costeroids, androgens, adrenocortical steroids, anabolics, 13. The topical formulation of claim 1, wherein the weight estrogens and/or progestin. ratio of the first compound to the second compound is in the 29. The topical formulation of claim 27, wherein the ste range of from about 1:9 to about 9:1. roid is testosterone or a pharmaceutically acceptable salt or 14. The topical formulation of claim 1, wherein the weight solvate thereof. ratio of the first compound to the second compound is in the range of from about 1:4 to about 4:1.