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US 20050181041A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0181041 A1 Goldman (43) Pub. Date: Aug. 18, 2005

(54) METHOD OF PREPARATION OF MIXED Related US. Application Data PHASE CO-CRYSTALS WITH ACTIVE AGENTS (60) Provisional application No. 60/528,232, ?led on Dec. 9, 2003. Provisional application No. 60/559,862, ?led (75) Inventor: David Goldman, Portland, CT (US) on Apr. 6, 2004. Correspondence Address: Publication Classi?cation LEYDIG VOIT & MAYER, LTD (51) Int. Cl.7 ...... A61K 31/56; A61K 38/00; TWO PRUDENTIAL PLAZA, SUITE 4900 A61K 9/64 180 NORTH STETSON AVENUE (52) US. Cl...... 424/456; 514/179; 514/2; CHICAGO, IL 60601-6780 (US) 514/221 (73) Assignee: MedCrystalForms, LLC, Hunt Valley, (57) ABSTRACT MD This invention pertains to a method of preparing mixed phase co-crystals of active agents With one or more materials (21) Appl. No.: 11/008,034 that alloWs the modi?cation of the active agent to a neW physical/crystal form With unique properties useful for the delivery of the active agent, as Well as compositions com (22) Filed: Dec. 9, 2004 prising the mixed phase co-crystals. Patent Application Publication Aug. 18, 2005 Sheet 1 0f 8 US 2005/0181041 A1 FIG. 1a

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METHOD OF PREPARATION OF MIXED PHASE active agent, lack the high concentrations that the mixed CO-CRYSTALS WITH ACTIVE AGENTS phase co-crystals enable, and lack the multi-functional aspects that mixed phase co-crystals offer With respect to CROSS-REFERENCE TO RELATED PATENT improved drug delivery. APPLICATIONS [0006] Co-crystalliZation of chemically related materials [0001] This patent application claims the bene?t of US. is illustrated by the preparation of co-crystalliZed sugars Provisional Patent Application No. 60/559,862, ?led Apr. 6, (US. Pat. Nos. 4,101,680 and 4,338,339), of acetylenic 2004 and US. Provisional Patent Application No. 60/528, compounds (US. Pat. No. 4,384,980), and sugar alcohols 232, ?led Dec. 9, 2003, Which are incorporated by reference (US. Pat. Nos. 5,679,398; 5,958,471 and 6,083,438). The herein. simple co-crystals therein described do not have the broad utility that mixed phase co-crystals have for the enhance FIELD OF THE INVENTION ment of properties of Widely different structures and physico-chemical properties. [0002] This invention pertains to methods of preparing an active agent as mixed phase co-crystals that have unique [0007] Incorporation of minor components by a process physical properties that differ from the active agent in pure described as ‘co-crystallization’ that yields a product of form, as Well as compositions comprising mixed phase indeterminate crystalline structure is illustrated by US. Pat. co-crystals. The formulated mixed phase co-crystals are Nos. 6,376,481, and 6,267,963 (sterol esters); US. Pat. No. heterogenous and contain crystalline regions Within the 6,214,402 (dilution of sWeetener); US. Pat. No. 4,751,294 particles/granules produced. Mixed phase co-crystals are (stabiliZation by a base); US. Pat. No. 5,910,523 (nanocom useful for systemic delivery of the active agent as human and posites); US. Pat. No. 5,876,506 (mesomorphic sugar), US. animal pharmaceuticals, dietary supplements, and agro Pat. No. 5,075,291 (uniform dispersion of drug in sugar chemicals. Furthermore, mixed phase co-crystals have util ); and US. Pat. No. 5,451,416. These materials of ity in imparting desirable physical and stability properties indeterminate structure lack the ability of mixed phase otherWise not achievable for the pure active agent or in co-crystals to maintain primary crystalline characteristics of combination as a simple formulation With the materials the active agent While imparting amorphous-like properties incorporated With the active agent. along With designed functionalities to enhance solubility, dissolution, and absorption. BACKGROUND OF THE INVENTION [0008] Complex mixtures of crystalline materials formed [0003] Co-crystals occur in nature and form spontane by melt/congealing process are described in US. Pat. Nos. ously With closely related chemical structures, such as 6,267,963 (sterol-emulsion complexes); US. Pat. Nos. chemical isomers (racemates, diasteriomers, and the like). 4,855,326 and 5,853,762 (rapidly dissolving dosage unit); Co-crystals are also found for materials that complex and US. Pat. No. 5,075,291. The process for preparing together in solution such as protein-ligands, chelates, inclu co-crystals by evaporation or cooling from a solvent system sion complexes as With cyclodextrins, and ligands. In US. is described in US. Pat. No. 4,145,214 (photoconductors); Pat. Nos. 4,971,797; 6,312,723 and 6,312,712, complexes of US. Pat. Nos. 4,751,294; 4,971,797; and 6,214,402. Appli cyclodextrin and active agents are described as being co cations for Which no active agent is incorporated are crystalliZed together from solution. These complexes lack described in US. Pat. Nos. 4,145,214 and 4,384,980. These the ?exibility to incorporate materials With broadly different materials of indeterminate structure lack the ability of mixed chemical structures and lack the multi-functional properties phase co-crystals to maintain primary crystalline character that mixed co-crystals can impart. istics of the active agent While imparting amorphous-like properties along With designed functionalities to enhance [0004] In certain cases, macromolecules (both polymers solubility, dissolution, and absorption. and biopolymers) are capable of forming co-crystals With other macromolecules. These co-crystalliZed products have [0009] In the ?eld of active agent delivery, inherent prob been used to isolate macromolecules such as proteins for lems associated With the active agent exist, such as particle structural characteriZation. An example of this is found in siZe, stability, solubility, poWder physical properties and the paper by Murphy et al. (Acta CrystallogrD Biol Crys release rates. NeW and improved methods to solve the tallogr; 55(Pt 9), 1594-1597 (1999)). These simple co problems associated With active agent delivery are needed. crystals are not useful to enhance solubility, dissolution or The invention provides such a method, as Well as mixed absorption of poorly absorbed active agents. phase co-crystal compositions comprising an active agent. These and other advantages of the invention, as Well as [0005] Minor amounts of materials can be incorporated in additional inventive features, Will be apparent from the a particle sub-structure. These components co-exist With description of the invention provided herein. crystalline phases of the particle and produce co-crystalline regions Within the particle. The resulting co-crystalliZed BRIEF SUMMARY OF THE INVENTION material has a high level of crystallinity and lacks signi?cant amounts of amorphous phase. Examples of these applica [0010] The invention is directed to a method of preparing tions can be found in patents describing the dilution of mixed phase co-crystals comprising: (a) forming a ?rst sWeetening agents in sugar carriers as in US. Pat. Nos. solution of a ?rst active agent and at least one crystal lattice 6,214,402 and 6,365,216. Incorporation of small amounts of modi?er dissolved in a solvent; (b) mixing an anti-solvent single constituents differs from mixed phase co-crystals With the ?rst solution to form a second solution; and (c) since the particles produced do not have a signi?cant amount forming a mixed phase crystalline material, Wherein the of amorphous phase as indicated by melting properties and active agent and crystal lattice modi?er are contained Within solubility. In addition, these materials do not contain an the mixed phase crystalline material. US 2005/0181041 A1 Aug. 18, 2005

[0011] The invention also is directed to a mixed phase monotropic co-crystal materials. The enhanced properties of co-crystal composition comprising a mixed phase co-crystal the mixed phase co-crystal materials are obtained even When of an active agent and at least one crystal lattice modi?er, the thermodynamically favored polymorph of the active Wherein the content of the active agent ranges from about agent is present as a component of the mixed phase co 5% to 95% by Weight of the total Weight of the material, and crystal structure. Mixed phase co-crystal materials enable Wherein the crystal lattice modi?er ranges from about 2% to formation of conglomerates of the active agent With modi 95% by Weight for each individual modi?er of the total ?ers that facilitate drug absorption process through perme Weight of the material. ability modi?cation, inhibitors of gut Wall metabolism, and stabiliZation of supersaturated solutions. Since these mate BRIEF DESCRIPTION OF THE DRAWINGS rials are linked through the conglomerated mixed phase co-crystal structure, they act in concert With the dissolution [0012] FIG. 1A is a graph shoWing heat How to tempera of the active agent and are resistant to premature dissolution ture of a pure form of active agent Wherein the active agent of the modi?er in the absence of the active agent. By this is acetate. mechanism the modi?er imparts a full effect. [0013] FIG. 1B is a graph shoWing heat How to tempera [0024] The process herein described for the mixed phase ture of a mixed phase co-crystal Wherein the active agent is co-crystals is Well suited for the direct formation and incor hydrocortisone acetate. poration of mixed phase co-crystals as part of the dosage [0014] FIG. 2A is a graph of an x-ray diffraction (XRD) form manufacturing process Without the need to isolate or pattern of pure stearic acid. purify the mixed phase co-crystal material. [0015] FIG. 2B is a graph of an XRD pattern of a mixed [0025] Accordingly, the present invention is directed to phase co-crystal of a crystal lattice modi?er (stearic acid) mixed phase co-crystal compositions and methods of mak and active agent (hydrocortisone). ing mixed phase co-crystal compositions. The inventive method of preparing mixed phase co-crystals comprises: (a) [0016] FIG. is a graph of an XRD pattern of pure forming a ?rst solution of an active agent and at least one active agent (hydrocortisone). crystal lattice modi?er dissolved in a solvent; (b) mixing an [0017] FIG. 3A is a graph of an XRD pattern of a mixed anti-solvent With the ?rst solution to form a second solution; phase co-crystal of hydrocortisone (HC) acetate, Methocel and (c) forming the mixed phase co-crystal composition, E4M (hydroxypropyl methylcellulose), and cetosteryl Wherein the active agent and crystal lattice modi?er are alchohol. contained Within the mixed phase co-crystal composition. The inventive method can further comprise evaporating the [0018] FIG. 3B is a graph of an XRD pattern of pure HC solvent(s), isolating the mixed phase co-crystal composition, acetate. Washing the mixed phase co-crystal composition, and/or [0019] FIG. 4 is a graph comparing dissolution pro?les drying the mixed phase co-crystal composition. (mcg/mL over time) of mixed phase co-crystals of [0026] A mixed phase co-crystal is a particle or granule cyclosporin prepared using the method described in composed of tWo or more crystalline or non-crystalline Example 4. phases that are distributed randomly throughout the particle [0020] FIG. 5 is a graph shoWing the intrinsic dissolution structure. One or more of the mixed phase co-crystal com rate of mixed phase co-crystals in a 3% sodium ponents must be solids at room temperature. lauryl sulfate 20% isopropanol:0.1 N HCl (1:1) media. [0027] An active agent that is co-crystalliZed With one or [0021] FIG. 6 is a graph shoWing comparing the in vitro more materials (additives) forms a mixed phase co-crystal dissolution rate for four lots of mixed phase co-crystal line form of the active agent and additive(s) that behaves as formulations (F833-023c, -024A, -025A, and -025B) con conglomerated particles or granules that have unique physi taining the active ingredient as compared to cal properties that are distinguishable from the pure active commercial Prometrium 200 mg capsules from tWo batches. agent or pure additive(s). These formulated mixed phase co-crystals have crystalline, co-crystalline, and amorphous DETAILED DESCRIPTION OF THE regions Within the particle matrix. The active agent’s crys INVENTION talline form is usually maintained except that the additive(s) are co-crystalliZed as part of active agent’s crystal lattice [0022] The mixed phase co-crystal materials produced by structure, thus forming co-crystalline regions or amorphous this invention have unique and unexpected properties such regions or semi-crystalline regions With crystal defects. This as increased apparent solubility, increased dissolution rate, results in a characteristic reduction in melting point and reduced melting point of the active agent, and decrease in crystallinity of the thermodynamically favored crystalline crystallinity of the active agent. In addition, the mixed phase form of the active agent. co-crystal materials produce supersaturated concentrations [0028] Although not Wishing to be bound by any particular of active agent for prolonged periods of time When sus pended in Water, Which facilitates absorption in vivo. These theory, it is believed that the additive(s) are co-crystalliZed as minor non-stoichiometric components in the active changes in properties of the active agent are particularly agent’s crystalline matrix. This co-crystalline phase has advantageous for the delivery of the active agent, e.g., in an oral dosage form. semi-crystalline nature and contains a high incidence of crystal defects. Any excess additive that is not co-crystal [0023] Furthermore, combinations of more than one crys liZed With the active agent forms a separate phase (Additive tal lattice modi?er With the active agent can result in additive Phase) apart from the active agent, Which results in the and super-additive effects that cannot be obtained With mixed phase co-crystal composition. The Additive Phase US 2005/0181041 A1 Aug. 18, 2005

and the active agent crystals containing co-crystalliZed addi [0033] 1. ot- agonists such as Adra?nil, Adre tive can be tightly agglomerated forming a mixed phase nolone, , , BudralaZine, Cloni co-crystal particle. The unique physical properties obtained dine, , , , Dipiv by this process of preparation can include changes in appar efrin, , Epinephrine, , , ent solubility, crystallinity, Water Wetability, dissolution , Hydroxyamphetamine, , IndanaZo rates, physical poWder properties (e.g., bulk density, abso line, , , , Meth lute density, refractive index, x-ray diffraction, spectral, oxamine Hydrochloride, Methylhexaneamine, MetiZolene, ?oWability, hygroscopicity, adsorption, and compaction), , , , , bioavailability, apparent permeability, apparent taste, and/or , , , stability. For example, the inventive method of preparation Hydrochloride, Hydrochloride, Phe of the composition provides (a) an increase in Water solu nylpropylmethylamine, , , Pseu bility, (b) a decrease in melting point, (c) decrease in melting doephedrine, , , TetrahydroZoline, enthalpy, (d) an increase in dissolution rate, (e) a reduction , , , , in crystallinity, or a combination of tWo or more of (a)-(e) , and . as compared to the active agent itself. [0034] 2. [3-Adrenergic agonists such as Albuterol, Bam [0029] The mixed phase co-crystal that forms from the buterol, , , , Clorprenaline, active agent and additive(s) is not a pure form stiochiometric , Dioxethedrine, , Ephedrine, Epi eutectic. The mixed phase co-crystal composition produced nephrine, , Ethylnorepinephrine, , For according to the invention are thermodynamically favored. moterol, , Ibopamine, Isoetharine, Isoproter That is, the crystals exist at a loWer energy, stable state. enal, , Metaproterenol, , , , , , , [0030] In another aspect of the invention, after step (b) a , , , Soterenol, Terbuterol, and kinetically favored crystalline phase is formed in the second . solution. The kinetically favored crystalline phase is also characteriZed as kinetically derived, meta-stable and ther [0035] 3. ot-Adrenergic blockers such as , Aro modynamically disfavored. The meta-stable (i.e., kinetically tinolol, , , Mesylates, Fen favored) crystalline phase is typically formed as a precipiate spiride, , , , , Tera in the second solution. The meta-stable crystalline phase is Zosin, , and . then subsequently transformed (i.e., converted) to the ther [0036] 4. [3-Adrenergic blockers such as , modynamically favored mixed-phase co-crystal comopsi , Amosulalol, , , , tion. The mixed phase co-crystalline material of the inven , , , , , tion are kinetically favored and form upon standing and/or Befetolol, , , , mixing of the initial meta-stable crystalline phase. Hydrochloride, Buto?lolol, , , [0031] The amount of time required to achieve transfor , , , , Dilevalol, mation (i.e., conversion) from a kinetically favored crystal , Esmolol, , Labetalol, , line phase to the mixed phase co-crystal composition , Metipranalol, , , Nadox depends on the particular active agent and other additives olol, , , , , Pin present in the second solution. The second solution contain dolol, , , , , Sul? ing the initial meta-stable crystalline phase is generally nalol, , , , , and . mixed or alloWed to stand for a sufficient period of time to permit complete conversion to the mixed phase co-crystal [0037] 5. Alcohol deterrents such as Calcium Cyanamide line material. This transformation step may take occur for Citrated, Disul?ram, Nadide, and NitrefaZole. any suitable amount of time (e.g., about 10 seconds, about [0038] 6. Aldose reductase inhibitors such as Epalrestat, 30 seconds, about 1 minute, about 5 minutes, about 10 minutes, about 30 minutes, about 1 hour, about 2 hours, Ponalrestat, Sorbinil, and Tolrestat. about 10 hours, about 20 hours, about 30 hours, about 40 [0039] 7. Anabolics such as AndroisoxaZole, Androstene hours, about 50 hours, or more). One of ordinary skill in the diol, Bolandiol, Bolasterone, Clostebol, Ethylestrenol. art Will recogniZe the amount of time required for conver Formyldienolone, 4-Hydroxy-19-nortestosterone, Meth sion of the kinetically favored crystalline material to the andriol, Methenolone, Methyltrienolone, Nandrolone, Nan thermodynamically favored mixed phase co-crystal compo drolone Decanoate, Nandrolone p-Hexyloxyphenylpropi sition. Incomplete conversion Will result in problems ?lter onate, Nandrolone Phenpropionate, Norbolethone, ing the crystalline material, and therefore, more incubation Oxymesterone, PiZotyline, Quinbolone, Stenbolone, and time is required. Trenbolone. [0032] The active agent for use in the composition and [0040] 8. () such as , Allyl method of the invention include any suitable active agent. prodine, Alphaprodine, , , BeZ The active agent is preferably a small chemical entity that is itramide, , , , approximately less than 10,000 daltons (e. g., less than about , Codeine Methyl Bromide, Codeine Phosphate, 9,000 daltons, less than about 8,000 daltons, less than about Codeine Sulfate, , , DeZo 7,000 daltons, less than about 6,000 daltons, less than about cine, , , Dihydrocodeinone 5,000 daltons), such as a pharmacologically active substance Enol Acetate, , , Dimephep (drug), vitamin, insecticide, fungicide, antibacterial agent, tanol, , , Dipi antiviral agent, antiparasitic agent or hormone. Exemplary panone, , , Ethylmethlythiam of active agents include, but are not limited to the folloWing: butene, , , , US 2005/0181041 A1 Aug. 18, 2005

Hydrocodone, , , Diperadon Hydrochloride, Dyclonine, Ecgonidine, Ecgo , , , , nine, Ethyl AminobenZoate, Ethyl Chloride, Etidocaine, Meperidine, , , Hydro EtoXadrol, [3-Eucaine, Euprocin, Fenalcomine, Fomocaine, chloride, , , Morphine Derivatives, Myro HeXobarbital, HeXylcaine Hydrochloride, HydroXydione phine, , Narceine, , Norlevorpha Sodium, HydroXyprocaine, HydroXytetracaine, Isobutyl nol, , , , , p-AminobenZoate, Kentamine, Leucinocaine Mesylate, , , , , LevoXadrol, Lidocaine, Mepivacaine, Hydro , , Pheoperidine, , Pir chloride, MetabutoXycaine Hydrochloride, MethoheXital itramide, , Promedol, , , Sodium, Methyl Chloride, MidaZolam, Myrtecaine, Nae PropoXyphene, , and . paine, Octacaine, Orthocaine, OXethaZaine, ParethoXycaine, Phenacaine Hydrochloride, , Phenol, Piper [0041] 9. Analgesics (non-narcotic) such as Acetami ocaine, Piridocaine, Polidocanol, PramoXine, Prilocaine, nophen, Acetaminosalol, Acetanilide, Acetylsalicylsalicylic Procaine, Propanidid, Propanocaine, Proparacaine, Propi Acid, Alclofenac, Alminoprofen, AloXiprin, Aluminum pocaine, Propofol, PropoXycaine Hydrochloride, Pseudoco Bis(acetylsalicylate), AminochlorthenoXaZin, 2-Amino-4 picoline, Aminopropylon, Aminopyrine, Ammonium Sali caine, Pyrrocaine, Quinine Urea Hydochloride, Risocaine, cylate, Antipyrine, Antipyrine Salicylate, , Apa Salicyl Alcohol, Tetracaine Hydrochloride, Thialbarbital, Zone, , Benorylate, BenoXaprofen, BenZpiperylon, Thimylal, Thiobutabarbital, Thiopental Sodium, Tolycaine, , p-Bromoacetanilide, S-Bromosalicylic Acid Trimecaine, and . Acetate, Bucetin, BufeXamac, BumadiZon, Butacetin, Cal [0044] 12. Anorectics such as , Amphecloral, cium Acetylsalicylate, CarbamaZepine, Carbetidine, Carbi , BenZaphetamine, , phene, Carsalam, Chloralantipyrine, ChlorthenoXaZin(e), , , , CycleXedrine, Destro Salicylate, Cinchophen, , Clometacin, amphetamine Sulfate, Diethylpropion, DiphemethoXidine, Cropropamide, Crotethamide, DeXoXadrol, , N-Ethylamphetamine, , Fen?uramine, Fenpro Di?unisal, DihydroXyaluminum Acetylsalicylate, Dipyro poreX, Furfuirylmethylamphetamine, Levophacetoperate, cetyl, Dipyrone, EmorfaZone, Enfenamic Acid, EpiriZole, , , Metamfeproamone, Methamphet Etersalate, EthenZamide, EthoXaZene, , Felbinac, , Norpseudoephedrine, , Phenmetra Fenoprofen, Floctafenine, Flufenamic Acid, Fluoresone, Zine, Phenpentermine, Phenylpropanolamine Hydrochlo , FluproquaZone, , Fosfosal, Gentisic ride, and . Acid, , Ibufenac, Salicylate, Indometha cin, Indoprofen, IsofeZolac, Isoladol, IsoniXin, , [0045] 13. Anthelmintics (Cestodes) such as , , p-Lactophenetide, , LoXoprofen, Aspidin, Aspidinol, Dichlorophen(e), Embelin, Kosin, Lysine Acetylsalicylate, Magnesium Acetylsalicylate, Meth Napthalene, Niclosamide, Pellertierine, Pellertierine Tan otrimepraZine, , Miroprofen, , Mor nate, and Quinacrine. pholine Salicylate, , , NifenaZone, 5‘ [0046] 14. Anthelmintics (Nematodes) such as Alantolac Nitro-2‘ propoXyacetanilide, Parsalmide, PerisoXal, Phen tone, Amoscanate, Ascaridole, Bephenium, Bitoscanate, acetin, PhenaZopyridine Hydrochloride, Phenocoll, Phe Carbon Tetrachloride, Carvacrol, CyclobendaZole, Diethyl nopyraZone, Phenyl Acetylsalicylate, Phenyl Salicylate, carbamaZine, Diphenane, DithiaZanine Iodide, Dymanthine, Phenyramidol, PipebuZone, , , Propac Gentian Violet, 4-HeXylresorcinol, Kainic Acid, Mebenda etamol, , , Quinine Salicylate, Zole, 2-Napthol, OXantel, Papain, , PiperaZine RamifenaZone, Metilsulfate, Salacetamide, Adipate, PiperaZine Citrate, PiperaZine Edetate Calcium, , , Salicylamide O-Acetic Acid, Salicyl PiperaZine Tartrate, Pyrantel, Pyrvinium Pamoate, ot-Santo sulfuric Acid, Salsalte, Salverine, Simetride, Sodium Sali nin, StilbaZium Iodide, Tetrachloroethylene, Tetramisole, cylate, Sulfamipyrine, Suprofen, Talni?umate, TenoXicam, thiabendaZole, Thymol, Thymyl N-Isoamylcarbamate, Tri Terofenamate, Tetradrine, Tinoridine, Tolfenamic Acid, Tol clofenol PiperaZine, and Urea Stibamine. pronine, , , Xenbucin, and Zomepirac. [0047] 15. Anthelmintics (Onchocerca) such as Ivermectin [0042] 10. Androgens such as Boldenone, FluoXymester and Suramin Sodium. one, Mestanolone, Mesterolone, Methandrostenolone, 17-Methyltestosterone, Methyltestosterone, 17ot-Methyltes [0048] 16. Anthelmintics (Schistosoma) such as Amoscan tosterone 3-Cyclopentyl Enol Ether, Norethandrolone, ate, Amphotalide, Antimony Potassium Tartrate, Antimony Normethandrone, OXandrolone, OXymesterone, Sodium Gluconate, Antimony Sodium Tartrate, Antimony OXymetholone, Prasterone, Stanlolone, StanoZolol, Test Sodium Thioglycollate, Antimony Thioglycollamide, osterone, Testosterone 17-Chloral Hemiacetal, Testosterone Becanthone, Hycanthone, Lucanthone Hydrochloride, Niri 17[3-Cypionate, Testosterone Enanthate, Testosterone Nico daZole, OXamniquine, PraZiquantel, Stibocaptate, Sti tinate, Testosterone Pheynylacetate, Testosterone Propi bophen, and Urea Stibamine. onate, and Tiomesterone. [0049] 17. Anthelmintic (Trematodes) such as Anthi [0043] 11. Anesthetics (intravenous) such as Acetami olimine and Tetrachloroethylene. doeugenol, Alfadolone Acetate, AlfaXalone, Amucaine, [0050] 18. Antiacne drugs such as Algestone Amolanone, Amylocaine Hydrochloride, BenoXinate, Acetophenide, AZelaic Acid, BenZoyl Peroxide, Cyoctol, BetoXycaine, Biphenamine, Bupivacaine, Butacaine, Buta , Motretinide, Resorcinol, Retinoic Acid, and ben, Butanilicaine, Burethamine, Buthalital Sodium, ButoX Tetroquinone. ycaine, Carticaine, 2-Chloroprocaine Hydrochloride, ethylene, , Cyclomethycaine, [0051] 19. Antiallergics such as AmleXanoX, , DibucaineHydrochloride, Dimethisoquin, , , Cromolyn, , Histamine, Ibudilast, US 2005/0181041 A1 Aug. 18, 2005

Nedocromil, Oxatomide, Pentigetide, Poison Ivy Extract, rfenicol, and ; Ansamycins such as Rifamide, Poison Oak Extract, Poison Sumac Extract, Repirinast, Rifampin, Rifamycin, and ; [3-Lactams, including: Tranilast, Traxanox, and Urushiol. Carbapenems such as Imipenem; Cephalosporins such as [0052] 20. Antiamebics such as Arsthinol, Bialamnicol, Cefactor, Cefadroxil, Cefamandole, CefatriZine, CefaZe Carbarsone, Cephaeline, Chlorbetamide, Chloroquine, done, CefaZolin, Ce?xime, Ce?nenoxime, CefodiZime, Chlorphenoxamide, Chlortetracycline, Dehydroemetine, Cefonicid, CefoperaZone, Ceforanide, Cefotaxime, Cefo Dibromopropamidine, Diloxanide, Dephetarsone, Emetine, tiam, CefpimiZole, Cefpirimide, Cefpodoxime Proxetil, Fumagillin, Glaucarubin, Glycobiarsol, 8-Hydroxy-7-iodo Cefroxadine, Cefsulodin, CeftaZidime, Cefteram, CefteZole, S-quinolinesulfonic Acid, Iodochlorhydroxyquin, Ceftibuten, CeftiZoxime, Ceftriaxone, Cefuroxime, Cefu Iodoquinol, , Phanquinone, Phearsone Sul Zonam, Cephacetrile Sodium, Cephalexin, Cephaloglycin, foxylate, PolybenZarsol, Propamidine, Quinfamide, Sec Cephaloridie, Cephalosporin, Cephalothin, Cephapirin Sodium, Cephradine and Pivcefalexin; Cephamycins such as nidaZole, Sulfarside, TecloZan, Tetracycline, Thiocarbam CefbuperaZone, CefmetaZole, Cefminox, Cefetan and iZine, Thiocarbarsone, and TinidaZole. Cefoxitin; Monobactams such as AZtreonam, Carumonam [0053] 21. Antiandrogens such as Bi?uranol, Cyoctol, and Tigemonam; Oxacephems such as Flomoxef and Mox Cyproterone, , Flutimide, Nilutamide, olactam; Penicillins such as Amidinocillin, Amdinocillin and Oxendolone. Pivoxil, , Ampicillan, Apalcillin, Aspoxicillin, [0054] 22. such as Acebutolol, Alprenolol, AZidocillan, AZlocillan, Bacampicillin, BenZylpenicillinic Amiodarone, Amlodipine, Arotinolol, Atenolol, Bepridil, Acid, BenZylpenicillin Sodium, Carbenicillin, Carfecillin Bevantolol, Bucumolol, , Bufuralol, Bunitrolol, Sodium, Carindacillin, Clometocillin, Cloxacillin, Cyclacil Bupranolol, CaroZolol, Carteolol, Carvedilol, Celiprolol, lin, Dicloxacillin, Diphenicillin Sodium, Epicillin, Fenbeni CinepaZet Maleate, DiltiaZem, Epanolol, Felodipine, Gallo cillin, Floxicillin, Hetacillin, Lenampicillin, Metampicillin, pamil, Imolamine, Indenolol, Isosorbide Dinitrate, Israd Methicillin Sodium, MeZlocillin, Nafcillin Sodium, Oxacil ipine, Limaprost, Mepindolol, Metoprolol, Molsidomine, lin, Penamecillin, Penethamate Hydriodide, Penicillin G , Nicardipine, Nifedipine, Nifenalol, Nilvadipine, Benethamine, Penicillin G BenZathine, Penicillin G Ben Nipradilol, Nisoldipine, Nitroglycerin, Oxprenolol, Oxy Zhydrylamine, Penicillin G Calcium, Penicillin G Hydrab amine, Penicillin G Potassium, Penicillin G Procaine, Peni fedrine, OZagrel, Penbutolol, Pentaerythritol Tetranitrate, cillen N, Penicillin O, Penicillin V, Penicillin V BenZathine, , Pronethalol, Propranolol, Sotaiol, , Penicillin V Hydrabamine, Penimepicycline, Phenethicillin Timolol, Toliprolol, and . Potassium, Piperacillin, Pivapicillin, Propicillin, Quinacil [0055] 23. Antiarrhythmics such as Acebutol, Acecaine, lin, Sulbenicillin, Talampicillin, Temocillin and Ticarcillin; Adenosine, Ajmaline, Alprenolol, Amiodarone, Amoproxan, Lincosamides such as Clindamycin and Lincomycin; Mac Aprindine, Arotinolol, Atenolol, Bevantolol, rolides such as AZithromycin, Carbomycin, Clarithromycin, Tosylate, Bubumolol, Bufetolol, Bunaftine, Bunitrolol, Erythromycin, Erythromycin Acistrate, Erythromycin Esto Bupranolol, Butidrine Hydrochloride, Butobendine, late, Erythromycin Glucoheptonate, Erythromycin Lacto Capobenic Acid, CaraZolol, Carteolol, Cifenline, Clo bionate, Erythromycin Propionate, Erythromycin Stearate, ranolol, Disopyramide, Encainide, Esmolol, Flecainide, Josamycin, Leucomycins, Midecamycins, Miokamycin, Gallopamil, Hydroquinidine, Indecainide, Indenolol, Iprat Oleandomycin, Primycin, Rokitamycin, Rosaramicin, ropium Bromide, Lidocaine, Lorajmine, Lorcainide, Roxithromycin, Spiramycin and Troleandomycin; Polypep Meobentine, , , MoriciZine, Nadox tides such as Amphomycin, Bacitracin, Capreomycin, Colis olol, Nifenalol, Oxprenolol, Penbutolol, Pindolol, Pirmenol, tin, Enduracidin, Enviomycin, Fusafumgine, Gramicidin(s), Practolol, Prajmaline, Procainamide Hydrochloride, Prone Gramicidin S, Mikamycin, Polymyxin, -Meth thalol, , Propranolol, Pyrinoline, Sul anesulfonic Acid, Pristinamycin, Ristocetin, Teicoplanin, fate, Quinidine, Sotalol, Talinolol, Timolol, Tocainide, Vera Thiostrepton, Tuberactinomycin, Tyrocidine, Tyrothricin, pamil, Viquidil, and Xibenolol. , Viomycin, Viomycin Pantothenate, Virginia mycin and Zinc Bacitracin; Tetracyclines such as Apicy [0056] 24. Antiarteriosclerotics such as Pyridinol Carbam cline, Chlortetracycline, Clomocycline, Demeclocycline, ate. Doxycycline, Guamecycline, Lymecycline, Meclocycline, [0057] 25 . Antiarthritic/Antirheumatics such as Allocupre Methacycline, Minocycline, Oxytetracycline, Penimepicy ide Sodium, Aurano?n, Aurothioglucose, Aurothiogly cline, Pipacycline, Rolitetracycline, Sancycline, Senociclin canide, AZathioprine, Calcium 3-Aurothio-2-propanol-1 and Tetracycline; and other such as Cycloserine, sulfonate, Chloroquine, ClobuZarit, Cuproxoline, Diacerein, and Tuberin. Glucosamine, Gold Sodium Thiomalate, Gold Sodium Thio sulfate, Hydroxychloroquine, KebuZone, LobenZarit, Melit [0059] 27. Antibacterial drugs (synthetic), including: 2,4 tin, Methotrexate, Myoral, and Penicillamine. Diaminopyrimidines such as Brodimoprim, Tetroxoprim and Trimethoprim; such as Furaltadone, Fura [0058] 26. Antibacterial () drugs including Ami Zolium Chloride, Nifuradene, Nifuratel, Nifurfoline, noglycosides such as Amikacin, Apramycln, Arbekacin, Nifurpirinol, NifurpraZine, Nifurtoinol and Nitrofurantoin; Bambermycins, Butirosin, Dibekacin, Dihdrostreptomycin, Quinolones and Analogs such as Ami?oxacin, Cinoxacin, Fortimicin(s), Gentamicin, Ispamicin, Kanamycin, Micro Cipro?oxacin, Di?oxacin, Enoxacin, Fleroxacin, Flume nomicin, , Neomycin Undecylenate, Netilmicin, quine, nome?oxacin, Miloxacin, Nalidixic Acid, Nor?oxa Paromomycin, Ribostamycin, Sisomicin, Spectinomycin, cin, O?oxacin, Oxolinic Acid, Pe?oxacin, Pipemidic Acid, , StreptonicoZid, and Tobramycin; Ampheni Piromidic Acid, Rosoxacin, Tema?oxacin and Tosu?oxacin; cols such as AZidamfenicol, Chloramphenicol, Chloram Sulfonamides such as Acetyl SulfamethoxypyraZine, Acetyl phenicol Palmitate, Chloramphenicol Pantothenate, Flo Sul?soxaZole, AZosulfamide, BenZylsulfamide, Chloram US 2005/0181041 A1 Aug. 18, 2005

ine-B, Chloramine-T, Dichloramine T, FormosulfathiaZole, droXybutyric Acid, Atrolactamide, Beclamide, Buramate, N.sup.2 Formylsul?somidine, N.sup.2-[3-D-Glucosylsulfa Calcium Bromide, CarbamaZepine, Cinromide, Clomethia nilamide, Mafenide, 4‘-(Methylsulfamoyl) sulfanilanilide, Zole, ClonaZepam, Decimemide, Diethadione, Dimethadi p-NitrosulfathiaZole, Noprylsulfamide, Phthalylsulfaceta one, DoXenitoin, Eterobarb, Ethadione, EthosuXimide, Etho mide, , SalaZosulfadimidine, Succinyl toin, Fluoresone, S-Hydroxytryptophan, Lamotrigine, sulfathiaZole, SulfabenZamide, Sulfacetamide, Sulfachlo Magnesium Bromide, Magnesium Sulfate, Mephenytoin, rpyridaZine, Sulfachrysoidine, Sulfacytine, SulfadiaZine, Mephobarbital, Metharbital, Methetoin, MethsuXimide, Sulfadicramide, SulfadimethoXine, SulfadoXine, Sulfaethi 5-Methyl-5-(3-phenanthryl)hydantoin, 3-Methyl-5-phenyl dole, , Sulfaguanol, Sulfalene, SulfaloXic hydantoin, Narcobarbital, NimetaZepam, NitraZepam, Acid, SulfameraZine, Sulfameter, SulfamethaZine, Sulfame Paramethadione, Phenacemide, Phenetharbital, Pheneturide, thiZole, Sulfamethomidine, SulfamethoXaZole, Sul Phenobarbital, Phenobarbital Sodium, PhensuXimide, Phe famethoXypyridaZine, Sulfametrole, Sulfamidochrysoidine. nylmethylbarbituric Acid, Phenytoin, Phethenylate Sodium, SulfamoXole, Sulfanilamide, Sulfanilamidomethanesulfonic Potassium Bromide, Primidone, Progabide, Sodium Bro Acid Triethanolamine Salt, 4-Sulfanilamidosalicylic Acid, mide, Solanum, Strontium Bromide, Suclofenide, Sulthi N.sup.4-Sulfanilylsulfanilamide, Sulfanilylurea, N-Sulfa ame, Tetrantoin, Trimethadione, Valproic Acid, Valpromide, nilyl-3,4-Xylamide, Sulfanitran, Sulfaperine, Sul Vigabatrin and Zonisamide. faphenaZole. SulfaproXyline, SulfapyraZine, Sulfapyridine, [0062] 30. , including: Bicyclics such as SulfasomiZole, SulfasymaZine, SulfathiaZole, Sulfathiourea, Binedaline, CaroXaZone, Citalopram, , Indal Sulfatolamide, Sul?somidine and Sul?soXaZole; Sulfones pine, , Hydrochcloride, Nefopam, such as Acedapsone, Acediasulfone, Acetosulfone Sodium, , OXitriptan, OXypertine, , Sertraline, , Diathymosulfone, Glucosulfone Sodium, Solasul ThiaZesim, and Zometapine; HydraZides/Hydra fone, Succisulfone, Sulfanilic Acid, p-SulfanilylbenZy Zines such as BenmoXine, IprocloZide, IproniaZid, Isocar lamine, p,p‘-Sulfonyldianiline-N.N‘ digalactoside, SulfoX boXaZid, Nialamide, OctamoXin and PhenelZine; Pyrroli one Sodium and ThiaZolsulfone; and others such as dones such as , Rolicyprine and Rolipram; Clofoctol, HeXedine, Methenamine, Methenamine Anhy Tetracyclics such as , Metralindole, dromethylene-citrate, Methenamine Hippurate, Meth and . Tricyclics such as AdinaZolam, Amitrip enamine Mandelate, Methenamine Sulfosalicylate, NitroXo tyline, , , , Clomi line and Xibomol. pramine, , , , Dime [0060] 28. such as Adiphenine Hydro tracrine, Dothiepin, , , , chloride, , Ambutonomium Bromide, Aminopenta Imipramine N-OXide, Iprindole, , , mide, AmiXetrine, Amprotropine Phosphate, Anisotropine , , NoXiptilin, , PiZoty Methylbromide, Apoatropine, , Atropine N-OXide, line, , , , , BenapryZine, BenZetimide, BenZilonium Bro and ; and others such as Adra?nil, Benac mide, BenZtropine Mesylate, Methyl Sulfate, tyZine. , Butacetin, Deanol, Deanol Aceglumate, , Butropium Bromide, N-Butylscopolammonium Deanol AcetamidobenZoate, DioXadrol, , Febar Bromide, BuZepide, Camylo?ne, Hydrochlo bamate, , , FluoXetine, FluvoXam ride, , , Cimetropium ine, Hematoporphyrin, Hypercinin, , Bromide, , Cyclodrine, Cyclonium , Minaprine, Moclobemide, OXa?oZane, Pib Iodide, Cycrimine Hydrochloride, , , eraline, , Pyrisuccideanol, , Dibutoline Sulfate, Dicyclomine Hydrochloride, DiethaZ Sulpiride, Sultopride, TeniloXaZine, , , ine, , , Diphemanil Methylsulfate, ToloXatone, , L-Tryptophan, N-(1,2-Diphenylethyl) nicotinamide, Dipiproverine, Dipo and Zimeldine. nium Bromide, , EndobenZyline Bro [0063] 31. Antidiabetics, including: Biguanides such as mide, EthopropaZine, EthybenZtropine, EthylbenZhy Buformin, Metformin and Phenformin; Hormones such as dramine, Etomidoline, Eucatropine, Glucagon, Insulin, Insulin Injection, Insulin Zinc Suspen Bromide, , Flutropium Bromide, Gly sion, Isophane Insulin Suspension, Protamine Zinc Insulin copyrrolate, Heteronium Bromide, Methyl Suspension and Zinc Insulin Crystals; Sulfonylurea deriva Sulfate, , , , tives such as AcetoheXamide, 1-Butyl-3-metanilylurea, , Levomepate, MecloXamine, Carbutamide, Chlorpropamide, Glibornuride, GliclaZide, Bromide, Metcaraphen, Bromide, MethiX GlipiZide, Gliquidone, GlisoXepid, Glyburide, GlybuthiaZ ene, Methscopolamine Bromide, Octamylamine, OXybuty ol(e), GlybuZole, GlyheXamide, Glymidine, Glypinamide, nin Chloride, , , Phenbutamide, TolaZamide, Tolbutamide and Tolcyclamide; Pentapiperide, Bromide, Phencarbamide, Phen and others such as Acarbose, Calcium MesoXalate and glutarimide, , , Piperilate, Miglitol. Methysulfate, , Pri?nium Bromide, Procy clidine, Propanthel ine Bromide, PropenZolate, Propyro [0064] 32. Antidiarrheal drugs such as Acetyltannic Acid, maZine, , Scopolamine N-OXide, Stilonium Albumin Tannate, Alkofanone, Aluminum Salicylates-Ba Iodide, Stramonium, Sultroponium, ThiheXinol, Thiphe sic, , , , Lidamidine, Lop namil, , , TiquiZium eramide, Mebiquine, Trillium and UZarin. Bromide, Iodide, Hydrochlo [0065] 33. Antidiuretics such as Desmopressin, Fely ride, Tropacine, TropenZile, , Trospium Chlo pressin, Lypressin, Ornipressin, OXycinchophen, Pituitary ride, Valethamate Bromide and Xenytropium Bromide. Posterior, Terlipressin and Vasopressin. [0061] 29. Anticonvulsants such as Acetylpheneturide, [0066] 34. Antiestrogens such as Delmadinone Acetate, Albutoin, AloXidone, , 4-Amino-3-hy EthamoXytriphetol, Tamoxifen and Toremifene. US 2005/0181041 A1 Aug. 18, 2005

[0067] 35. drugs (antibiotics), including: Poly Nico?brate, Piri?brate, Roni?brate, Sim?brate and Theo? enes such as Amphotericin-B, Candicidin, Dermostatin, brate; Bile acid sequesterants such as Cholestyramine Resin, Filipin, Fungichromin, Hachimycin, , Lucensomy Colestipol and PolideXide; HMG CoA reductase inhibitors cin, Mepartricin, , , Pecilocin and Peri such as Lovastatin, Pravastatin Sodium and Simvastatin; mycin; and others such as AZaserine, , Oligo Nicotinic acid derivatives Aluminum Nicotinate, AcipimoX, mycins, Neomycin Undecylenate, Pyrrolnitrin, Siccanin, Niceritrol, Nicoclonate, Nicomol and OXiniacic Acid; Thy Tubercidin and Viridin. roid hormones and analogs such as EtiroXate, Thyropropic Acid and ThyroXine; and others such as Acifran, AZacos [0068] 36. Antifungal drugs (synthetic), including: Ally terol, Ben?uoreX, [3-BenZalbutyramide, Camitine, Chon lamines such as Nafti?ne and Terbina?ne; such droitin Sulfate, Clomestone, DetaXtran, DeXtran Sulfate as , , Chlordantoin, ChlormidaZole, Sodium, 5,8,11,14,17-Eicosapentaenoic Acid, Eritadenine, CloconaZole, , , EnilconaZole, Fen FuraZbol, Meglutol, Melinamide, Mytatrienediol, Omithine, ticonaZole, , , , Omo y-OryZanol, Pantethine, Penataerythritol Tetraacetate, conaZole, , Nitrate, and Tiocona ot-Phenylbutyramide, PiroZadil, Probucol, ot-Sitosterol, Sul Zole; such as , ItraconaZole and tosilic Acid, PiperaZine Salt, Tiadenol, Triparanol and Xen ; and others such as Acrisorcin, Amorol?ne, bucin. Biphenamine, Bromosalicylchloranilide, Buclosamide, Cal cium Propionate, Chlophenesin, , CloXyquin, [0074] 42. Antihypertensive drugs, including: Arylethano Coparaf?nate, DiamthaZole, Dihydrochloride, EXalamide, lamine derivatives such as Amosulalol, Bufuralol, Dilevalol, , HalethaZole, HeXetidine, Lo?ucarban, Nifura Labetalol, Pronethalol, Sotalol and Sul?nalol; AryloXypro tel, , Propionic Acid, Pyrithione, Salicyla panolamine derivatives such as Acebutolol, Alprenolol, Aro nilide, Sodium Propionate, , TenonitroZole, Tol tinolol, Atenolol, BetaXolol, Bevantolol, Bisoprolol, Bopin ciclate, Tolindate, , Tricetin, Ujothion, dolol, Bunitrolol, Bupranolol, Buto?lolol, CaraZolol, and Zinc Propionate. CarteZolol, Carvedilol, Celiprolol, Cetamolol, Epanolol, Indenolol, Mepindolol, Metipranolol, Metoprolol, [0069] 37. Antiglaucoma drugs such as AcetaZolamide, Moprolol, Nadolol, Nipradilol, OXprenolol, Penbutolol, Pin Be?nolol, BetaXolol, Bupranolol, Carteolol, DapipraZoke, dolol, Propranolol, Talinolol, Tetraolol, Timolol and Tolip Dichlorphenamide, Dipivefrin, Epinephrine, Levobunolol, rolol; BenZothiadiaZine derivatives such as AlthiaZide, Ben MethaZolamide, Metipranolol, , Pindolol and dro?umethiaZide, BenZthiaZide, Timolol. BenZylhydrochlorothiaZide, ButhiaZide, ChlorothiaZide, Chlorthalidone, CyclopenthiaZide, CyclothiaZide, DiaZoX [0070] 38. Antigonadotropins such as , Gestrinone ide, EpithiaZide, EthiaZide, FenquiZone, HydrochlorothiaZ and ParoXypropione. ide, Hydro?umethiaZide, MethyclothiaZide, Meticrane, [0071] 39. Antigout drugs such as Allopurinol, Carprofen, MetolaZone, Para?utiZide, PolythiaZide, TetrachlormethiaZ Colchicine, Probenecid and Sul?npyraZone. ide and TrichlormethiaZide; N-Carboxyalkyl (petide/lactam) derivatives such as Alacepril, Captopril, CilaZapril, Delapril, [0072] 40. , including: Alkylamine deriva Enalapril, Enalaprilat, Fosinopril, Lisinopril, Moveltipril, tives such as Acrivastine, , , Perindopril, Quinapril and Ramipril; Dihydropyridine Chlorpheniramine, Dimethindene, Metton S., , derivatives such as Amlodipine, Felodipine, Isradipine, , Thenaldine, and ; Nicardipine, Nifedipine, Nilvadipine, Nisoldipine and Aminoalkyl ethers such as Bietanautine, Bromodiphenhy Nitrendipine; dramine, , , Diphenlypyraline, , Embrammine, , Mephenphy [0075] 43. derivatives such as , dramine, p-Methyldiphenhydramine, , Phenyl Debrisoquin, GuanabenZ, Guanacline, , GuanaZo toloXamine, Piprinhydrinate and Setasine; Ethylenediamine dine, , Guanfacine, Guanochlor, derivatives such as , p-Bromtripelennamine, and ; HydraZines and phthalaZines such as , , , Methafu BudralaZine, CadralaZine, DihydralaZine, EndralaZine, Hyd rylene, , , , racarbaZine, HydralaZine, PhenipraZine, PildralaZine and Pyrilamine, Talastine, , TodralaZine; ImidaZole derivatives such as , Hydrochloride, Tripelennamine and Zolamine; , , Tiamenidine and ; such as CetiriZine, , , ClociniZine Quaternary ammonium compounds AZamethonium Bro and ; Tricyclics, including: mide, Chlorisondamine Chloride, HeXamethonium, Penta such as Ahistan, ,HydroXyaZine, N-HydroXy cynium Bis(methyl sulfate), Pentamethonium Bromide, ethylpromethaZine Chloride, , , Pentolinium Tartate, Phenactopinium Chloride and Trime , PyrathiaZine and ThiaZinamium Methyl Sul thidiunumMethosulfate; QuinaZoline derivatives such as fate; and others such as , , Cypro , , DoXaZosin, Prasosin, and heptadine, Deptropine, Isothipendyl, Loratadine and Pro TrimaZosin; Reserpine derivatives such as Bietaserpine, thipendyl; and other antihistamines such as , Deserpidine, Rescinnamine, Reserpine and Syrosingopine; AstemiZole, AZelastine, CetoXime, , ClobenZ derivatives such as Ambuside, Clopamide, tropine, DiphenaZoline, , Mebhydroline, Furosemide, Indapamide, QuinethaZone, Tripamide and , Terfenadine and Tritoqualine. Xipamide; and others such as Ajmaline, y-AminobutYric Acid, Bufeniode, Chlorthalidone, Cicletaine, Ciclosidom [0073] 41. Antihyperlipoproteinemics, including: Ary ine, Cryptenamine Tannates, Fenoldopam, Flosequinan, loXyalkanoic acid derivatives such as Beclorbrate, BaZa? Indoramin, , Metbutamate, Mecamylamine, brate, Bini?brate, Cipro?brate, Clino?brate, Clo?brate, , Methyl 4-Pyridyl Ketone ThiosemicarbarZone, Clo?bric Acid, Eton?brate, Feno?brate, Gem?broZil, MetolaZone, MinoXidil, MuZolimine, Pargyline, Pempidine, US 2005/0181041 A1 Aug. 18, 2005

Pinacidil, , Prirnaperone, Protoveratrines, crine, Quinine, Quinine Bisulfate, Quinine Carbonate, Raubasine, Rescirnetol, Rilrnenidene, Saralasin, Sodium Quinine Dihydrobrornide, Quinine Dihydrochloride, Qui Nitroprusside, Ticrynafen, Trirnethaphan Carnsylate, Tyro nine Ethylcarbonate, Quinine Forrnate, Quinine Gluconate, sinase and . Quinine Hydriodide, Quinine Hydrochloride, Quinine Sali [0076] 44. Antihyperthyroids such as 2-Arnino-4-rneth cylate, Quinine Sulfate, Quinine Tannate, Quinine Urea ylthiaZole, 2-ArninothiaZole, CarbirnaZole, 3,5-Dibrorno-L Hydrochloride, Quinocide, Quinoline and Sodiurn Arsenate , 3,5-Diiodotyrosine, Hinderin, Iodine, Iothiouracil, Diabasic. MethirnaZole, Methylthiouracil, propylthiouracil, Sodium [0081] 49. Antirnigraine drugs such as Alpiropride, Dihy Perchlorate, ThibenZaZoline, Thiobarbital and 2-Thiouracil. droergotarnine, Ergocornine, Ergocorninine, Ergocryptine, [0077] 45. Antihypotensive drugs such as ArneZiniurn Ergot, Ergotarnine, FlurnedroXone acetate, FonaZine, Methyl Sulfate, Angiotensin Amide, Dirnetofrine, Dopam , Methysergid(e), , PiZotyline and ine, Etifelrnin, Etilefrin, , Metararninol, Mido Surnatriptan. drine, Norepinephrine, Pholedrinead and Synephrine. [0082] 50. Antinauseant drugs such as Acetylleucine [0078] 46. Antihypothyroid drugs such as LevothyroXine Monoethanolarnine, , BenZquinarnide, Bietanau Sodium, Liothyronine, Thyroid, Thyroidin, ThyroXine, tine, Brornopride, , ChlorprornaZine, , Tiratricol and TSH. , Dirnenhydrinate, Dipheniodol, Dornperidone, [0079] 47. Anti-In?ammatory (non-steroidal) drugs, Granisetron, , Methalltal, Metocloprarnide, including: ArninoarylcarboXylic acid derivatives such as MetopirnaZine, Nabilone, Ondansteron, OXypendyl, Piparn Enfenarnic Acid, Etofenarnate, Flufenarnic Acid, IsoniXin, aZine, Piprinhydrinate, , Scopolarnine, Tet Meclofenarnic Acid, Mefanarnic Acid, Ni?urnic Acid, Talni rahydrocannabinols, ThiethylperaZine, ThioproperZaine and ?urnate, Terofenarnate and Tolfenarnic Acid; Arylacetic acid TrirnethobenZarnide. derivatives such as Acernetacin, Alclofenac, Arnfenac, [0083] 51. Antineoplastic drugs, including: Alkylating BufeXarnac, Cinrnetacin, Clopirac, Sodiurn, agents, including: Alkyl sulfonates such as Busulfan, Impro Etodolac, Felbinac, Fenclofenac, Fenclorac, FencloZic Acid, sulfan and Piposulfan; AZiridines such as BenZodepa, Car FentiaZac, Glucarnetacin, Ibufenac, Indornethacin, Isof eZolac, IsoXepac, LonaZolac, MetiaZinic Acid, OXarnetacine, boquone, Meturedepa and Uredepa; Ethylenirnines and Proglurnetacin, Sulindac, Tiararnide, Tolrnetin and Zornepi rnethylrnelarnines such as Altretarnine, Triethylen rac; Arylbutyric acid derivatives such as BurnadiZon, Buti emelamine, Triethylenephosphoramide, Triethylenethio bufen, Fenbufen and Xenbucin; ArylcarboXylic acids such phosphorarnide and Trirnethylolornelarnine; Nitrogen rnus as Clidanac, Ketorolac and Tinoridine; Arylpropionic acid tards such as Chlorarnbucil, ChlornaphaZine, derivatives such as Alrninoprofen, BenoXaprofen, BucloXic Chclophospharnide, Estrarnustine, Ifosfarnide, Mechlore Acid, Carprofen, Fenoprofen, FlunoXaprofen, Flurbiprofen, tharnine, Mechloretharnine Oxide Hydrochloride, Mel , IbuproXarn, Indoprofen, Ketoprofen, LoXopro phalan, Novernbichin, Phenesterine, Prednirnustine, Trofos fen, Miroprofen, NaproXen, OXaproZin, Piketoprofen, Pir farnide and Uracil Mustard; Nitrosoureas such as profen, Pranoprofen, ProtiZinic Acid, Suprofen and Tiapro Carrnustine, ChloroZotocin, Forernustine, Lornustine, fenic Acid; PyraZoles such as DifenarniZole and EpiriZole; Nirnustine and Ranirnustine; and others such as Dacarba PyraZolones such as ApaZone, BenZpiperylon, FepraZone, Zine, Mannornustine, Mitobronitol, Mitolactol and Pipobro MofebutaZone, MoraZone, OXyphenbutaZone, Phenybuta rnan; Antibiotics such as Aclacinornycins, Actinornycin Fl, Zone, PipebuZone, PropyphenaZone, RarnifenaZone, SuXi Anthrarnycin, AZaserine, Bleornycins, Cactinornycin, Caru buZone and ThiaZolinobutaZone; derivatives bicin, CarZinophilin, Chrornornycins, Dactinornycin, such as Acetarninosalol, Aspirin, Benorylate, Brornosalige Daunorubicin, 6-DiaZo-5-oXo-L-norleucine, DoXorubicin, nin, Calciurn Acetylsalicylate, Di?unisal, Etersalate, Fen Epirubicin, Mitornycins, Mycophenolic Acid, Nogalarnycin, dosal, Gentisic Acid, Glycol Salicylate, IrnidaZole Salicy Olivornycins, Peplornycin, Plicarnycin, Por?rornycin, Puro late, Lysine Acetylsalicylate, Mesalarnine, Morpholine rnycin, Streptonigrin, StreptoZocin, Tubercidin, UbenirneX, Salicylate, I -Naphthyl Salicylate, , Parsalrnide, Zinostatin and Zorubicin; Antirnetabolites, including: Folic Phenyl Acetylsalicylate, Phenyl Salicylate, Salacetarnide, acid analogs such as Denopterin, MethotreXate, Pteropterin Salicylarnine O-Acetic Acid, Salicylsulfuric Acid, Salsalate and TrirnetreXate; Purine analogs such as Fludarabine, 6-Mercaptopurine, Thiarniprine and Thioguanaine; and and ; ThiaZinecarboXarnides such as DroXicarn, IsoXicarn, PiroXicarn and TenoXicarn; and others such as Pyrirnidine analogs such as Ancitabine, AZacitidine, epsilon.-Acetarnidocaproic Acid, S-Adenosylrnethionine, 6-AZauridine, Carrnofur, Cytarabine, DoXi?uridine, Enocit 3-Arnino-4-hydroXybutyric Acid, ArniXetrine, BendaZac, abine, FloXuridine, Fluroouracil and Tegafur; EnZyrnes such BenZydarnine, Bucolorne, Difenpirarnide, DitaZol, Ernorfa as L-Asparaginase; and others such as Aceglatone, Arnsa Zone, GuaiaZulene, Naburnetone, Nirnesulide, Orgotein, crine, Bestrabucil, Bisantrene, Carboplatin, Cisplatin, Defo OXaceprol, Paranyline, PerisoXal, PifoXirne, ProquaZone, farnide, Dernecolcine, DiaZiquone, Elfornithine, Elliptiniurn ProXaZole and Tenidap. Acetate, Etoglucid, Etoposide, Galliurn Nitrate, Hydrox yurea, Interferon-0t, Interferon-[3, Interferon-y, Interleukine [0080] 48. Antirnalarial drugs such as Acedapsone, Arno 2, Lentinan, Lonidarnine, MitoguaZone, MitoXantrone, diaquin, Arteether, Arternether, Arternisinin, Artesunate, Mopidarnol, Nitracrine, Pentostatin, Phenarnet, Pirarubicin, Bebeerine, Berberine, Chirata, Chlorguanide, Chloroquine, Podophyllinicc Acid, 2-EthythydraZide, ProcarbaZine, Chlorproguanil, Cinchona, Cinchonidine, Cinchonine, PSK®, RaZoXane, SiZo?ran, Spirogerrnaniurn, TaXol, Teni Cycloguanil, Gentiopicrin, Halofantrine, HydroXychloro poside, TenuaZonic Acid, TriaZiquone, 2,2‘,2“Trichlorotri quine, Me?oquine Hydrochloride, 3-Methylarsacetin, Pam ethylarnine, Urethan, Vinblastine, Vincristine and Vin aquine, Plasrnocid, Prirnaquine, Pyrirnetharnine, Quina desine; US 2005/0181041 A1 Aug. 18, 2005

[0084] 52. Antineoplastic (hormonal) drugs, including: , Clomacran, Clothiapine, , Androgens such as Calusterone, Dromostanolone Propi Opipramol, Prothipendyl, TetrabenaZine, and ; and onate, Epitiostanol, Mepitiostane and Testolactone; Antia others such as AliZapride, Amisulpride, Buramate, Fluspir drenals such as Aminoglutethimide, and Trilos ilene, Molindone, Pen?uridol, PimoZide, Spirilene and tane; Antiandrogens such as Flutamide and Nilutamide; and Sulpiride. Antiestrogens such as Tamoxifen and Toremifene. [0096] 64. Antipyretics such as Acetaminophen, Acetami [0085] 53. Antineoplastic adjuncts including folic acid nosalol, Acetanilide, Aconine, Aconite, Aconitine, replenishers such as Frolinic Acid. Alclofenac, Aluminum Bis(acetylsalicylate), Aminochlorth [0086] 54. Antiparkinsonian drugs such as , enoXaZin, Aminopyrine, Aspirin, Benorylate, BenZydamine, BenseraZide, Bietanautine, Biperiden, , Berberine, p-Bromoacetanilide, BufeXamac, BumadiZon, Budipine, Carbidopa, Deprenyl, DeXetimide, DiethaZine, Calcium Acetysalicylate, ChlorthenoXaZin(e), Choline Sali , EthopropaZine, EthylbenZhydramine, cylate, Clidanac, DihydroXyaluminum Acetylsalicylate, Levodopa, NaXagolide, , , Pridinol, Dipyrocetyl, Dipyrone, EpiriZole, Etersalate, ImidaZole Prodipine, , Tigloidine and TriheXyphenidyl Salicylate, Indomethacin, IsofeZolac, p-Lactophenetide, Hydrochloride. Lysine Acetylsalicylate, Magnesium Acetylsalicylate, Meclofenamic Acid, MoraZone, Morpholine Salicylate, [0087] 55. Antipheochromocytoma drugs such as Mety NaproXen, NifenaZone, 5‘-Nitro-2‘propoXyacetanilide, pro rosine, and Phentolamine. poXyacetanilide, , PhenicarbaZide, Phenocoll, [0088] 56. Antipneumocystis drugs such as Effomithine, PhenopyraZone, Phenyl Acetylsalicylate, Phenyl Salicylate, and SulfamethoXaZole. PipebuZone, , PropyphenaZone, Ramifena Zone, Salacetamide, Salicylamide O-Acetic Acid, Sodium [0089] 57. Antiprostatic hypertrophy drugs such as Gesto Salicylate, Sulfamipyrine, Tetrandrine and Tinoridine. norone Caproate, Mepartricin, OXendolone and Finasteride (ProscarO). [0097] 65. Antirickettsial drugs such as p-AminobenZoic Acid, Chloramphenicol, Chloramphenicol Palmitate, [0090] 58. AntiprotoZoal drugs (Leshmania) such as Anti Chloramphenicol Pantothenate and Tetracycline. mony Sodium Gluconate, Ethylstibamine, HydroXystilbami dine, N-Methylglucamine, Pentamidine, Stilbamidine and [0098] 66. Antiseborrheic drugs such as ChloroXine, 3-O Urea Stibamine. LauroylpyridoXol Diacetate, Piroctone, Pyrithione, Resorci nol, Selenium Sul?des and TioXolone. [0091] 59. AntiprotoZoal drugs (Trichomonas) such as Acetarsone, AminitroZole, Anisomycin, AZanidaZole, Form [0099] 67. Antiseptics, including: such as initraZole, FuraZolidone, Hachimycin, Lauroguadine, AleXidine, AmbaZone, ChlorheXidine and PicloXydine; Mepartricin, MetronidaZole, Nifuratel, NifuroXime, Halogens and halogen compounds such as Bismuth Iodide NimoraZole, SecnidaZole, Silver Picrate, TenonitroZole and Oxide, Bismuth Iodosubgallate, Bismuth Tribromophenate, TinidaZole. Bomyl Chloride, Calcium Iodate, Chlorinated Lime, Clof [0092] 60. AntiprotoZoal drugs (Trypanosma) such as lucarban, Flurosalan, Iodic Acid, Iodine, Iodine Monochlo BenZnidaZole, E?omithine, Melarsoprol, NifurtimoX, ride, Iodine Trichloride, Iodoform, Methenamine Tetraiod OXophenarsine, Hydrochloride, Pentamidine, Propamidine, ine, OXychlorosene, Povidone-lodine, Sodium Puromycin, Quinapyramine, Stilbamidine, Suramin Hypochlorite, Sodium Iodate, Symclosene, Thymol Iodide, Sodium, Trypan Red and Tryparasmide. Triclocarban, Triclosan and Troclosene Potassium; Mercu rial compounds such as Hydragaphen, Meralein Sodium, [0093] 61. Antipuritics such as Camphor, , Merbromin, Mercuric Chloride, Mercuric Chloride, Ammo , Glycine, , 3-HydroXycamphor, niated, Mercuric Sodium p-Phenolsulfonate, Mercuric Suc , Mesulphen, , Phenol, Polidocanol, cinimide, Mercuric Sul?de, Red, Mercurophen, Mercurous Risocaine, Spirit of Camphor, Thenaldine, Tolpropamine Acetate, Mercurous Chloride, Mercurous Iodide, Nitromer and TrimepraZine. sol, Potassium Tetraiodomercurate(II), Potassium Tri [0094] 62. Antipsoriatic drugs such as Acitretin, Ammo iodomercurate(II) Solution, Thimerfonate Sodium and nium Salicylate, Anthralin, 6-AZauridine, Bergapten(e), Thimerosal; Nitrofurans such as FuraZolidone, 2-(Meth Chrysarobin, Etretinate and Pyrogallol. oXymethyl)-5-, NidroXyZone, NifuroXime, NifurZ ide and NitrofuraZone; Phenols such as Acetomeroctol, [0095] 63. Antipsychotic drugs, including: Butyrophe Bithionol, Cadmium Salicylate, Carvacrol, ChloroXylenol, nones such as Benperidol, Bromperidol, , Flu Clorophene, Cresote, Cresol(s), p-Cresol, Fenticlom, anisone, , , Moperone, , HeXachlorophene, l-Napthyl Salicylate, 2-Napthyl Salicy Sniperone, Timiperone and Tri?uperidol; PhenothiaZines late, 2,4,6-Tribromo-m-cresol, and 3‘,4‘,5-Trichlorosalicyla such as , , CarphenaZine, Chlo nilide; Quinolines such as Aminoquinuride, BenZoXiquine, rproethaZine, , ClospiraZine, , , ChloroXine, Chlorquinaldol, CloXyquin, DiXyraZine, , ImiclopaZine, MepaZine, Ethylhydrocupreine, Euprocin, Halquinol, Hydrastine, , MethoXypromaZine, MetofenaZate, OXa?u 8-HydroXquinoline, 8-HydroXquinoline Sulfate and Iodoch maZine, , PericyaZine, PerimethaZine, Perphena lorhydroXyquin; and others such as Aluminum Acetate Solu Zine, PiperacetaZine, , ProchlorperaZine, Pro tion, Aluminum Subacetate Solution, Aluminum Sulfate, maZine, , , , 3-Amino-4-hydroXybutyric Acid, Boric Acid, ChlorheXi Tri?uoperaZine and Tri?upromaZine; such as dine, ChloroaZodin, m-Cresyl Acetate, Cupric Sulfate, , , and ThiothiX Dibromopropamidine, Ichthammol, Negatolg, NoXytiolin, ene; other tricyclics such as BenZquinamide, , OmidaZole, [3-Propiolactone, ot-Terpineol. US 2005/0181041 A1 Aug. 18, 2005

[0100] 68. Antispasmodic drugs such as Alibendol, Ambu LysoZyme, MethisaZone, MoroXydine, PodophyllotoXin, cetamide, AminopromaZine, Apoatropine, Bevonium Ribavirin, , Stallimycin, Statolon, Tromanta Methyl Sulfate, Bietamiverine, Butaverine, Butropium Bro dine and XenaZoic Acid. mide, N-Butylscopolammonium Bromide, , [0106] 74. AnXiolytic drugs, including: ArylpiperaZ ines , , Clebopride, Coniine such as , and ; BenZodiaZ Hydrobromide, Coniine Hydrochloride, Cyclonium Iodide, epine derivatives such as AlpraZolam, BromaZepaam, Difemerine, , DioXaphetyl Butyrate, Dipo CamaZepam, ChlordiaZepoXide, ClobaZam, CloraZepate, nium Bromide, , Emepronium Bromide, Ethaver ChotiaZepam, CloXaZolam, DiaZepam, Ethyl Lo?aZepate, ine, Feclemine, Fenalamide, , Fenpiprane, Fen EtiZolam, FluidaZepam, FlutaZolam, FlutopraZepam, piverinium Bromide, Fentonium Bromide, , HalaZepam, KetaZolam, LoraZepam, , Flopropione, Gluconic Acid, Guaiactamine, Hydramitra MedaZepam, MetaclaZepam, MeXaZolam, NordaZepam, Zine, Hymecromone, Leiopyrrole, , , OXaZepam, OXaZolam, PinaZepam, PraZepam and To?so Na?verine, Octamylamine, Octaverine, Pentapiperide, Phe pam; Carbamates such as Cyclarbamate, Emylcamate, namacide Hydrochloride, , Pinaverium Bro HydroXyphenamate, Meprobamate, Phenprobamate and mide, Piperilate, PipoXolanHydrochloride, Pramiverin, Pri Tybamate; and others such as Alpidem, , ?nium Bromide, Properidine, Propivane, PropyromaZine, Captodiamine, ChlormeZanone, EtifoXine, Fluoresone, ProZapine, Racefemine, , Spasmolytol, Stilonium Glutamic Acid, HydroXyZine, Mecloralurea, MephenoXa Iodide, Sultroponium, Tiemonium Iodide, TiquiZium Bro lone, OXanamide, Phenaglycodol, Suriclone. mide, , , Tricromyl, Trifolium, Tri mebutine, N,N-1Trimethyl-3,3-diphenyl-propylamine, Tro [0107] 75. BenZodiaZepine antagonists such as FlumaZe penZile, and Xenytropium Bromide. nil. [0101] 69. Antithrombotic drugs such as Anagrelide, [0108] 76. , including: Ephedrine deriva Argatroban, CilostaZol, Daltroban, De?brotide, EnoXaparin, tives such as Albuterol, , Bitolterol, Carbuterol, FraXiparine®, Indobufen, Lamoparan, OZagrel, Picotamide, Clenbuterol, Clorprenaline, DioXethedrine, Ephedrine, Pla?bride, Tedelparin, Ticlopidine and Tri?usal. Epiniphrine, EproZinol,Etafedrine, Ethylnorepinephrine, Fenoterol, HeXoprenaline, Isoetharine, Isoproterenol, [0102] 70. Antitussive drugs such as Allocamide, Amici Mabuterol, Metaproterenol, N-Methylephedrine, Pirbuterol, bone, , , , Procaterol, Protokylol, Reproterol, Rimiterol, Soterenol, Bromoform, , Butethamate, Caramiphen and ; Quaternary ammonium com Ethanedisulfonate, Carbetapentane, Chlophedianol, Clobu pounds such as Bevonium Methyl Sulfate, Clutropium Bro tinol, , Codeine, Codeine Methyl Bromide, mide, Ipratropium Bromide and ; Xan Codeine N-OXide, Codeine Phosphate, Codeine Sulfate, thine derivatives such as Acefylline, Acefylline PiperaZine, CycleXanone, , Sodium, Dihy Ambuphylline, , Bamifylline, choline Theo drocodeine, Dihydrocodeinone Enol Acetate, , phyllinate, DoXofylline, Dyphylline, Enprofylline, Etami , ot,ot-Diphenyl-2-piperidinepropanol, Dro phyllin, Etofylline, Guaithylline, ProXyphylline, Theobro propiZine, , , Ethyl Dibunate, Ethyl mine, l-Theobromineacetic Acid and ; and morphine, , Guiaiapate, , Isoami others such as , MedibaZine, MethoXyphenanime nile, , , Narceine, and . Normethadone, , , OXolamine, Pholcod ine, Picoperine, PipaZethate, , [0109] 77. Calcium channel blockers, including: Arylalky Hydrochloride, Racemethorphan, TaZiprinone Hydrochlo lamines such as Bepridil, DitiaZem, Fendiline, Gallopanil, ride, and . , Terodiline and Verapamil; Dihydropyridine derivatives such as Felodipine, Isradipine, Nicardipine, [0103] 71. Antiulcerative drugs such as Nifedipine, Nilvadipine, Nimodipine, Nisoldipine and Aluminum Complex, epsilon.-Acetamidocaproic Acid Zinc Nitrendipine; PiperaZine derivatives such as CinnariZine, Salt, AcetoXolone, Arbaprostil, BeneXateHydrochloride, Flunarisine and Lido?aZine; and others such as Bencyclane, Sol (Dried), , , Etafenone and PerheXiline. , , EsapraZole, , FtaXilide, [0110] 78. Calcium regulators such as Calcifediol, Calci , GuaiaZulene, Irsogladine, , NiZati tonin, Calcitriol, Clodronic Acid, Dihydrotachysterol, Elca dine, , Ornoprostil, y-OryZanol, Pifarnine, tonin, Etidronic Acid, Ipri?avone, Pamidronic Acid, Par , Plaunotol, , Rioprostil, Rosaprostol, athyroid Hormone and Teriparatide Acetate. RotraXate, , Sofaicone, SpiZofurone, , , Trimoprostil, ThrithioZine, [0111] 79. Cardiotonics such as Acefylline, Acetyldigiti and . toxins, 2-Amino-4-picoline, Amrinone, Benfurodil Hemisuccinate, Buclasdesine, Cerberoside, Camphotamide, [0104] 72. Antiurolithic drugs such as AcetohydroXamic ConvallatoXin, Cymarin, Denopamine, Deslanoside, Ditalin, Acid, Allopurinol, Potassium Citrate and Succinimide. Digitalis, DigitoXin, , DigoXin, , , [0105] 73. Antiviral drugs, including: Purines and pyrimi DopeXamine, EnoXimone, Erythrophleine, Fenalcomine, dinones such as Acyclovir, Cytarabine, DideoXyadenosine, Gitalin, GitoXin, Glycocyamine, , Hydrastinine, DideoXycytidine, DideoXyinosine, EdoXudine, FloXuridine, Ibopamine, Lanotodises, Metamivam, Milrinone, Neriifolin, Ganciclovir, IdoXuridine, Inosine PranobeX, MADU, Tri?u Oleandrin, Ouabain, OXyfedrine, Prenalterol, Proscillaridin, ridine, Vidrarbine and Zidovudiine; and others such as Resibufogenin, Scillaren, Scillarenin, Strophanthin, Sulma Acetylleucine Monoethanolamine, Amantadine, Amidino Zole, and Xamoterol. mycin, Cuminaldehyde ThiosemicarbZone, Foscarnet [0112] 80. Chelating agents such as DeferoZmine, Ditio Sodium, Interferon-0t, Interferon-[3, Interferon-y, KethoXal, carb Sodium, Edetate Calcium Disodium, Edetate Diso US 2005/0181041 A1 Aug. 18, 2005

dium, Edeate Sodium, Edetate Trisodium, Penicillamine, and Theobromine; Steroids such as , Oleandrin Pentetate Calcium Trisodium, Pentectic Acid, Succimer and and ; Sulfonamide derivatives such as Aceta Trientine. Zolmide, Ambuside, AZosemide, Bumetanide, ButaZola mide, Chloraminophenamide, Clofenamide, Clopamide, [0113] 81. Cholecystokinin antagonists such as Proglu CloreXolene, Diphenylmethane-4.4‘-disulfonamide, Disulfa mide. mide, EthoXZolamide, Furosemide, Indapamide, Mefruside, [0114] 82. Cholelitholytic agents such as Chenodiol, MethaZolamide, Piretanide, QuinethaZone, Torasemide, Tri Methyl tert-Butyl Ether, Monooctanoin and Ursodiol pamide and Xipamide; Uracils such as Aminometradine and [0115] 83. Choleretics such as Alibendol, Anethole Amisometradine; others such as AmanoZine, Amiloride, Trithion, AZintamide, Cholic Acid, Cicrotoic Acid, Clanobu Arbutin, ChloraZanil, Ethacrynic Acid, EtoZolin, Hydracar tin, Cyclobutyrol, Cyclovalone, Cynarin(e), Dehydrocholic baZine, Isosorbide, , Metochalcone, MuZolimine, Acid, DeoXycholic Acid, Dimecrotic Acid, ot-EthylbenZyl PerheXiline, Ticrynafen and Urea. Alcohol, EXiproben, Feguprol, Fencibutirol, Fenipentol, [0124] 92. Dopamine receptor agonists such as Bro Florantyrone, Hymecromone, Menbutone, 3-(o-MethoX mocriptine, DopeXamine, Fenoldopam, Ibopamine, yphenyl)-2-phenylacrylic Acid, Metochalcone, MoquiZone, Lisuride, NaXagolide and Pergolide. Osalmid, OX Bile Extract, 4.4‘-OXydi-2-butanol, PiproZolin, [0125] 93. Ectoparasiticides such as , BenZyl Ben ProZapine, 4-Salicyloylmorpholine, Sincalide, Taurocholic Zoate, Carbaryl, Crotamiton, DDT, DiXanthogen, isobomyl Acid, Timonacic, Tocamphyl, Trepibutone and Vanitiolide. Thiocyanoacetate-Technical, Lime Sulfurated Solution, LIn [0116] 84. agents such as , Acetyl dane, Malathion, Mercuric Oleate, Mesulphen and Sul choline Bromide, Acetylcholide Chloride, Aclatonium phur—Pharmaceutical; and Mucolytic enZymes such as Napadisilate, BenZpyrinium Bromide, chlo LysoZyme. ride, , Carpronium chloride, Demecarium Bro mide, DeXpanthenol, Diisopropyl ParaoXon, Echothiophate [0126] 94. EnZyme inducers (hepatic) such as Flumecinol. Iodide, Edrophomium chloride, Eseridine, Furtrethonium, [0127] 95. Estrogens, including: Nonsteroidal estrogens Iso?urophate, chloride, , Neostig such as BenZestrol, Broparoestrol, Chlorotrianisene, Dienes mine, OXapropanium Iodide, Physostigmine and Pyridostig trol, Diethylstilbestrol, Diethylstilbestrol Diproprionate, mine Bromide. Dimestrol, Fosfestrol, HeXestrol, Methallenestril and Meth estrol; and Steroidal estrogens such as Colpormon, Conju [0117] 85. inhibitors such as Ambenonium Chloride, Distigmine Bromide and Galanthamine. gated Estrogenic Hormones, Equilenin, Equilin, Estradiol, Estradiol BenZoate, Estradiol 17[3-Cypionate, Estriol, [0118] 86. Cholinesterase reactivators such as ObidoX Estrone, Ethinyl Estradiol, Mestranol, MoXestrol, imine Chloride and PralidoXime Chloride. Mytatrienediol, Quinestradiol and Quinestrol. [0119] 87. Central nervous system and agents [0128] 96. Gastric secretion inhibitors such as Enterogas such as , Amphetimine, Amphetaminil, Beme trone and . gride, , Brucine, , Chlorphenter mine, , Clortermine, Coca, Demanyl Phos [0129] 97. such as 21-AcetoX phate, DeXoXadrol, Sulfate, yprefnenolone, Aalclometasone, Algestone, Amicinonide, Diethlpropion, N-Ethytlamphetamine, Ethamivan, Etife Beclomethasone, , , Chloropred lmin, Etryptamine, Fencamfamine, , Fenoso nisone, , Blovetasone, , , lone, , Sodium, Homocam?n, , , , De?aZacort, Des MaZindol, MegeXamide, , Methylpheni onide, , , Di?orasone, date, , , PentylenetetraZole, Pheni Di?ucortolone, Di?uprednate, , , Flu dimetraZine, , Phenternine, , cloronide, Flumehtasone, , , Prolintane and . Acetonide, , Butyl, , , Acetate, [0120] 88. such as Amidephrine, Cafami Acetate, , Flurandrenolide, , nol, Cyclopentamine, Ephedrine, Epinephrine, FenoXaZo , Halometasone, Acetate, Hydro line, IndanaZoline, , NaphaZoline, Nordefrin cortamate, Hydrocortisone, Hydrocortisone Acetate, ydro Hydrochloride, Octodrine, OXymetaZoline, Phenylephrine cortisone Phosphate, Hydrocortisone 21-Sodium Succinate, Hydrochloride, Phenylpropanolamine Hydrochloride, .Phe Hydrocortisone Tebutate, , , Mepre nylpropylmethylamine, PropylheXedrine, , dnisone, Methyolprednisolone, Furoate, TetrahydroZoline, TymaZoline and XylometaZoline. , , , Prednisolone [0121] 89. Dental carries prophylactics such as Sodium 21-Diethylaminoacetate, Sodium Phosphate, Fluoride. Prednisolone Sodium Succinate, Prednisolone Sodium 21-m-SulfobenZoate, Prednisolone 21-Stearoylglycolate, [0122] 90. Depigmentors such as Hydroquinine, Hydro Prednisolone Tebutate, Prednisolone 21-Trimethylacetate, quinone and MonobenZone. Prednisone, Prednival, , Prednylidene 21-Di ethylaminoacetate, TiXocortal, , Triamcino [0123] 92. Diuretics, including: Organomercurials such as lone Acetonide, Triamcinolone Benetonide and Triamcino Chlormerodrin, Meralluride, Mercamphamide, Mercaptom lone HeXacetonide. erin Sodium, Mercumallylic Acid, Mercumatilin Sodium, Mercurous Chloride and Mersalyl; Pteridines such as Fur [0130] 98. Gonad-Stimulating principles such as Buser terene and Triamterene; Purines such as Acefylline, 7-Mor elin, Clomiphene, Cyclofenil, Epimestrol, FSH, HCG and pholinomethyltheophylline, Pamabrom, Protheobromine LH-RH.