(12) United States Patent (10) Patent No.: US 7,122,198 B1 Singh Et Al

Home , Azanidazole, Cyclofenil, DDT, Diisopropyl paraoxon, Dixanthogen, Fencamine

US007122198B1

(12) United States Patent (10) Patent No.: US 7,122,198 B1 Singh et al. (45) Date of Patent: Oct. 17, 2006

(54) FAST DISSOLVING COMPOSITION WITH (52) U.S. Cl...... 424/401; 424/464; 424/465; PROLONGED SWEET TASTE 424/479: 424/484 (58) Field of Classification Search ...... 424/400, (75) Inventors: Amarjit Singh, New Delhi (IN); 424/441, 497, 430, 427, 401, 464, 465, 479, Rajesh Jain, New Delhi (IN) 424/484: 514/819, 785 See application file for complete search history. (73) Assignee: Panacea Biotec Limited, New Delhi (IN) (56) References Cited (*) Notice: Subject to any disclaimer, the term of this U.S. PATENT DOCUMENTS patent is extended or adjusted under 35 5,939,091 A * 8/1999 Eoga et al...... 424/441 U.S.C. 154(b) by 1 day. 6,048,541. A * 4/2000 Misra et al. ... 424/401 6,248,363 B1* 6/2001 Patel et al...... 424/497 (21) Appl. No.: 10/148,651 FOREIGN PATENT DOCUMENTS EP O229000 7, 1987 (22) PCT Filed: Nov. 24, 2000 EP 0452268 10, 1991 (86). PCT No.: PCT/INOO/OO113 FR 2766089 1, 1999 * cited by examiner S 371 (c)(1), Primary Examiner Johann Richter (2), (4) Date: Aug. 19, 2002 Assistant Examiner Mina Haghighatian (87) PCT Pub. No.: WO01/39749 (74) Attorney, Agent, or Firm—Ladas and Parry LLP PCT Pub. Date: Jun. 7, 2001 (57) ABSTRACT A novel fast dissolving pharmaceutical composition in Solid (30) Foreign Application Priority Data dosage form with prolonged Sweet taste which comprises (a) Nov. 30, 1999 (IN) ...... 1514/DEL/99 At least one pharmaceutically active agent, (b) At least one water soluble Sugar, (c) At least one non-sugar Sweetner in (51) Int. Cl. normal fast release form and (d) At least one non-Sugar A6 IK 9/00 (2006.01) Sweetner in a mucoadhesive slow release form. A6 IK 9/20 (2006.01) A6 IK 9/22 (2006.01) 7 Claims, No Drawings US 7,122,198 B1 1. 2 FAST DISSOLVING COMPOSITION WITH material Susceptible to variability and microbial contamina PROLONGED SWEET TASTE tion. The composition described in U.S. Pat. No. 5,720,974 requires a special "Compression-Molding process to pro INTRODUCTION duce fast dissolving tablet. U.S. Pat. No. 5,837.285 discloses 5 fast soluble tablets which are produced by a novel process The present invention is related to a novel composition of which involves the compression shaping of a wet kneaded a Fast dissolving pharmaceutical preparation in Solid dosage mass of drug and Sugar alcohol. The wettablets produced are form with prolonged Sweet taste and a process for the thereafter dried. manufacture thereof. Another U.S. Pat. No. 5,869,098 discloses fast dissolving 10 compressed tablets manufactured by using partially hygro BACKGROUND OF THE INVENTION scopic shearform matrices. Such matrices are prepared from Sugar carriers using a flash-heat process. Further U.S. Pat. Generally, Solid pharmaceutical preparation Such as tab No. 5,112,616 discloses the use of solid selected from lets/capsules are designed so that after oral administration, polyethylene glycols and glycerides, wherein glycerides they disintegrate or dissolve in the digestive organs and the 15 melt in the range of 25° C. to 45° C. surfactants selected active ingredients are absorbed. Such compositions are not from the groups consisting of nonionic Poly (oxypropylene) meant to disintegrate or dissolve in the oral cavity. Poly (oxyethylene) copolymers, polyoxyethylene polysor However, in certain conditions there is a requirement of bate derivatives and sodium lauryl sulfate to prepare fast fast disintegrating or dissolving tablets which can be admin dissolving buccal tablets. istered even without water. Such fast dissolving tablets PCT Application Number WO 93/23017 defines a fast disperse readily to form a suspension or Solution of the drug dissolving matrix consisting of gelatin, pectin and/or soy after mixing with the saliva, which is easily swallowed by the patients. These are particularly suitable for children or fiber protein and one or more amino acids having from 2 to aged patients who have difficulty in chewing and/or Swal 12 carbon atoms. lowing an intact tablet/capsule. 25 All the compositions disclosed in the prior art suffer from Fast mouth dissolving tablets are also suitable for those the drawback of a bitter taste in the mouth after consumption patients:— and also do not provide for a prolonged Sweet taste in oral a) Who are Suffering from nausea or vomiting; cavity after consumption of Such fast dissolving composi b) Who have an upper gastrointestinal tract disease e.g., tions. injury in food pipe; 30 It is the object of the present invention to provide a c) Who have undergone upper GI Surgery; pharmaceutical preparation in Solid dosage form, preferably d) Who are prostrate; in the form of a compressed tablet which when orally e) Who are elderly and have frequent urination problems administered dissolves or disperses in the mouth within one at night. minute requiring very little amount of body fluids like saliva f) Who are incapacitated elderly patients e.g. Suffering 35 to produce a smooth solution or Suspension of the drug with from Parkinson's disease; a prolonged Sweet taste. g) Who are children: Accordingly the present invention relates to a novel fast h) Who are in a situation where water is not available. dissolving pharmaceutical composition in Solid dosage form All the above conditions necessitate that solid dosage with a prolonged Sweet taste which comprises: form like tablets and capsules should be modified to accom 40 a) at least one pharmaceutically active agent in an amount modate above conditions. Formulating conventional tablets of from 0.1 to 99 weight % of the total dosage form: and liquid dosage forms does not solve all the problems b) at least one water soluble Sugar in an amount of from stated above. Dispersible tablets still require water and lead 5 to 95 weight % of the total dosage form; to gritty Suspensions. Such reconstituted dosage forms as c) at least one non-Sugar Sweetener in a fast release form well as ready-made Suspensions still cannot be given in all 45 in an amount of from 0 to 10 weight % of the total above conditions and additionally they pose problems of dosage form; and uniformity of doses and stability of the drug. d) at least one non-Sugar Sweetener in a mucoadhesive In the past, techniques have been reported for producing slow release form in an amount of from 0.5 to 20 Such fast dissolving tablets, but most of them require the use weight % of the total dosage form. of highly specialized manufacturing processes or specialized 50 packaging. The Zydis technology from R. P. Scherer, The present invention also relates to a process for the England for instance, utilizes freeze drying of active ingre preparation of a fast dissolving pharmaceutical composition dient with polymer, Sugar and other ingredients to form a in Solid dosage form with a prolonged Sweet taste which fast dissolving dosage form. (Manuf. Chemist. February, consists essentially of mixing the following ingredients: 1990). European Patent Application No. EP0839 526 A2 55 a) at least one pharmaceutically active agent in an amount describes the use of a high cost excipient i.e. erythritol in of from 0.1 to 99 weight % of the total dosage form: combination with an active ingredient, crystalline Cellulose b) at least one water soluble Sugar, in an amount of from and disintegrants to prepare fast disintegrating buccal tab 40 to 95 weight % of the total dosage form: lets. U.S. Pat. No. 5,073.374 discloses a fast dissolving c) at least one non-Sugar Sweetener in a fast release form buccal tablet containing an active ingredient, a water soluble 60 in an amount of from 0 to 10 weight % of the total sugar such as sorbitol and a lubricant. U.S. Pat. No. 5,085, dosage form; 876 discloses a Surprisingly fast dissolving Sweetening agent d) at least one non-Sugar Sweetener in a mucoadhesive in combination with caramel. slow release form in an amount of from 0.5 to 20 U.S. Pat. No. 5,466,464 discloses a solid preparation weight '% of total dosage form; soluble in buccal cavity containing agar in combination with 65 Sugars like lactose and/or mannitol and an active ingredient. and compressing the resulting mixture obtained into tablets The drawback in this preparation is that agar is a natural or any other solid dosage form. US 7,122,198 B1 3 4 The water soluble sugars which can be used in the process cine, Methadone, Metopon, Morphine, Morphine Deriva according to the present invention are Mannitol, Sorbitol, tives, Myrophine, Nalbuphine, Narceline, Nicomorphine, Xylitol and/or the like. Norlevorphanol, Normethadone, Normorphine, Norpi The non-Sugar Sweeteners which can be used in the panone, Opium, Oxycodone, Oxymorphone, Papaveretum, process according to the present invention are Aspartame, Pentazocine, Phenadoxone, Phenazocine, Phenoperidine, Acesulfame potassium, Saccharin Sodium, Cyclamates, Gly Piminodine, Piritramide, Proheptazine, Promedol, Properi cirrhizin and/or the like. dine, Propiram, Propoxyphene, Sufentanil, Tilidine. The non-Sugar Sweetener in a mucoadhesive slow release ANALGESIC (NON-NARCOTIC) such as Acetami form is obtained by mixing, coating, granulating, encapsu nophen, Acetaminosalol, Acetanilide, Acetylsalicylates, lation, matrix formulation or complexation of a non-Sugar 10 Acetylsalicylic Acid, Aceclofenac, Alminoprofen, Alox Sweetener with a mucoadhesive agent as stated herein. iprin, Aluminum Bis (acetylsalicylate), Aminochlorthenox The drugs, pharmaceutically active agents or their salts to azin, 2-Amino-4-picoline, Aminopropylon, Aminopyrine, be employed for the fast dissolving buccal tablet in accor Antipyrine, AntipyrinP Salicylate, Antrafenine, ApaZone, dance with the present invention can be selected from the Aspirin, Benorylate, Benoxaprofen, BenZpiperylon, Benzy following group of drugs 15 damine, p-Bromoacetanilide, 5-Bromosalicylic Acid C-ADRENERGICAGONIST such as Adrafinil, Adrena Acetate, Bufexamac, Bucetin, Bumadizon, Butacetin, Car lone, Amidephrine, Apraclonidine, Budralazine, Clonidine, bamazepine, Carbetidine, Carbiphene, Carsalam, Chloralan Cyclopentamine, Detomidine, Dimetofrine, Dipivefrin, tipyrine, Chlorthenoxazin(e), Cholin salicylate, Cin Ephedrine, Epinephrine, Fenoxazofine, GuanabenZ, Guan chophen, Ciramadol, Clometacin, Cropropamide, facine, Hydroxyamphetamine, Ibopamine, indanazoline, Crotethamide, Dexoxadrol, Difenamizole. Diflunisal, Dipy tsometheptene, Mephentermine, Metaraminol, Methoxam rocetyl, Dipyrone, EmorfaZone, Enfenamic Acid, Epirizole, ine, Methylhexaneamine, Metizoline, Midodrine, Naphazo Etersalate, Ethenzamide, Ethoxazene, Etodolac, Felbinac, line, Norepinephrine, Norfenefrine, Octodrine, Octopamine, Fenoprofen, Floctafenine, Flufenamic Acid, Fluoresone, Oxymetazoline, Phenylephrine, Phenyfpropanolamine, Phe Flupirtine, FluproduaZone, Flurbiprofen, Fosfosal, Gentisic nylpropylmethylamine, Pholedrine, Propylhexedrine, Pseu 25 Acid, Glafenine, Ibufenac, Imidazole Salicylate, Indometha doephedrine, Rilmenidene, Synephrine, Tetrahydrozo(ine, cin, Indoprofen, IsofeZolac, Isoladol, Isonixin, Ketoprofen, Tiamenidine, TramaZoline, Tuaminoheptane, Tymazoline, Ketorolac, p-Lactophenetide, Lefetamine, Loxoprofen, Tyramine, Xylometazoline. Lysine Acetylsalicylate, Methotrimeprazine, Metofoline, |B-ADRENERGICAGONIST such as Formoterol, Meth Miroprofen, Morazone, Morpholine Salicylate, Naproxen, oxyphenamine, Ritodrine, Terbuterol. 30 Nefopam, Nifenazone, 5' Nitro-2'Propoxyacetanilide, C-ADRENERGICBLOCKER such as Dapiprazole, Dox Parsalmide, Perisoxal, Phenacetin, Phenazopyridine, Pheno aZosin, Ergoloid, Mesylates, Fenspiride, Prazosin, Tera coll, Phenopyrazone, PhenylAcetylsalicylate, Phenyl sali Zosin, Tolazoline, Yohimbine cylate, Phenyramidol, Pipebuzone, Piperylone, Prodilidine, C-ADRENERGICBLOCKER such as Acebutolol, Amo Propacetamol, Propyphenazone, Proxazole, Quinine Salicy Sulalof, Arotinolol, Atenolol. Befunolol, Betaxolol, Bevan 35 late, RamifenaZone, tolol, Bisoprolol, Bopindofol, Bucumofol, Bufetolol. Rimazolium metisulfate, Salacetamide, Salicin, Salicyla Buforalol, Bunitrolol, Bupranolol, Butofilolol, Carazolol, mide O-acetic acid, Salicylic Acid, Salicylates and deriva Carteolol, Carvedilol, Celiprolo(, Cetamolol, Cloranolol, tives, Salicylsulfuric Acid, Salsalate, Salverine, Simetride, Dilevalol, Epanolol, Esmolol, Indenolol, Labetalol, Sulfamipyrine, Suprofen, Talniflumate, Tenoxicam, Terofe Levobunolol, Mepindolol, Metipranolol, Metoprolol, 40 namate, Tetrandrine, Tinoridine, Tolfenamic Acid, Tolpro Moprolol, Nadolol, Nadoxolol, Nifenalol, Nipradillol, nine, Tramadol, Viminol, Xenbucin, Zomepirac Oxprenolol, Penbutolol, Pindolol, Practolol, Propranolol, ANDROGEN such as Boldenone, Fluoxymesterone, Sotalol, Sulfinalol, Tafinolol, Tertatolol, Timolol, Toliprolol, Mestanolone, Mesterolone, Methandrostenolone, 17-Meth Xibenolol. yltestosterone, 17a-Methyl-testosterone 3-cyclopenty1 Enol ALCOHOL DETERRENT such as calcium cyanamide 45 Ether, Norethandrolone, Normethandrone, Oxandrolone, citrated, Disulfiram, Nitrefazofe ALDOSE REDUCTASE Oxymetholone, Prasterone, Stanolone, Stanozolol, Test INHIBITOR such as Epairestat, Ponalrestat, Sorbinil, Tolr osterone, Testosterone 17-Chloral Hemiacetal, Testosterone estat ANABOLIC such as Androisoxazole, Androstenediol, 17.-Cypionate, Testosterone Enanthate, Testosterone nicoti Bolandiol, Bolasterone, Clostebol, Ethylestrenol. Formyl nate, Testosterone Phenylacetate, Testosterone Propionate, dienolone, 4-Hydroxy-19-nortestosterone, Methandriol, 50 Tiomesterone, Methenolone, Methyltrienolone, Nandrolone decanoate, ANESTHETIC such as Acetamidoeugenol, Alfadolone Nandrolone P-Hexyloxyphenyl-propionate, Nandrolone acetate, Alfaxalone; Ambucaine. Amolanone, Amylocalne, Phenpropionate, Norbolethone, Oxymesterone, Quinbolone, BenoXinate, Betoxycaine, Biphenamine, Bupivacaine, Bure Stenbolone, Trenbolone, ANALGESIC (DENTAL) such as thamine. Butacaine, Butamben, Butanilicaine, Buthalital, Chlorobutanol, Clove, Eugenol, Potassium Nitrate, Potas 55 Butoxycaine, Carticaine, 2-Chloroprocaine, Cocaethylene, sium Oxalate. Cocaine, Cyclomethycaine, Cocaethylene, Dibucaine, ANALGESIC (NARCOTIC) such as Alfentanil, Allyl Dimethisoquin, Dimethocaine, Diperodon, Dyclonine, prodine, Alphaprodine, Anileridine, Benzylmorphine, Bez Ecgonidine, Ecgonine, Ethyl Aminobenzoate, Ethyl Chlo itramide, Buprenorphine. Butorphanol, ClonitaZene, ride, Etidocaine, Etoxadrol, P-Eucaine, Euprocin, Fenal Codeine, Desomorphine, Dextromoramide, Dezocine, 60 comine, Fomocaine, Hexobarbital, Hexylcaine. Hydroxydi Diampromide, Dihydrocodeine, Dihydrocodeinone Enol one, Hydroxyprocaine. Hydroxytetracaine, isobutyl Acetate, Dihydromorphine, Dimenoxadol, Dimepheptanol, p-Aminobenzoate, Ketamine, Leucinocaine Mesylate, Dimethylthiambutene, Dioxaphetyl butyrate, Dipipanone, Levoxadrol, Lidocaine, Mepivacaine, Meprylcaine, Eptazocine, Ethoheptazine, Ethylmethylthiambutene, Ethyl Metabutoxycaine, Methohexital, Methyl Chloride, Mida morphine, EtonitaZene, Fentanyl, Hydrocodone, Hydromor 65 Zolam, Myrtecaine, Naepaine, Octacaine, Orthocaine, Oxet phone, Hydroxypethidine, Isomethadone, Ketobemidone, hazaine, Parethoxycaine, Phenacaine, Phencylidine. Phenol, Levorphanol, Lofentanil, Meperidine, Meptazinol, Metazo Piperocaine, Piridocaine, Polidocanol, Pramoxine, Prilo US 7,122,198 B1 5 6 calne, Procaine, Propanidid, Propanocaine, Proparacaine, mide, Azathioprine, Di-tert-Butyl-phenols, Calcium 3-Au Propipocaine, Propofol, Propoxycaine, Pseudococaine. Pyr rothio-2-propanol-1-sulfonate, ClobuZarit, Cuproxoline, rocaine, Risocaine, Salicyl Alcohol, Tetracaine. Thialbar Diacerein, Glucosamine, Gold Sodium Thiosulfate, bital. Thiamylal. Thiobutabarbital. Thiopental, Tolycaine, Hydroxychloroquine, KebuZone, Lobenzarit, Melittin, Myo Trimecaine, Zolamine. ral, Penicillamine ANOREXIC such as Aminorex, Amphecloral, BenZphet amine, Chlorphentermine, Clobenzorax, Cloforex, Antibacterial (Antibiotic) Cyclexedrine, Di phemethoxidine, Fenbutrazate, Fenflu Aminoglycosides such as Amikacin, Apramycin, Arbeka ramine, Fenproporex, Furfurylmethylamphetamine, cin, Bambermycins, Butirosin. Dibekacin, Dihydrostrepto Levophacetoperane, Mefenorex, Metamfepramone, Norps 10 mycin, Fortimicin(s), Fradiomycin, Gentamicin, Isepamicin. eudoephedrine, Phenpentermine, Picilorex ANTHELM kanamycin, Micronomicin, Neomycin, Neomycin Unde INTIC. cylenate, Netilmicin. Paromomycin, Ribostamycin, Sisomi (CESTODES) such as Arecoline, Aspidine, Aspidinol, cin, Spectinomycin, Streptomycin, Streptonicozid, Tobra Dichlorophen(e), Embelin, Kosin, Naphthalene, Niclosa mycin mide, Pelletierine, Pelletierine tannate, Quinacrine. 15 Amphenicols such as AZidamfenicol, Chloramphenicol, Anthelmintic (NEMATODES) such as Alantolactone, Chloramphenicol Palmitate, Chloramphenicol Pantothenate, Amoscanate, Ascaridole, Bephenium, Bitoscanate, Carbon Florfenicol. Thiamphenicol, Tetrachloride, Carvacrol, Cyclobendazole, Diethylcarbam Ansamycins such as Rifamide, Rifampin, Rifamycin, azine, Diphenane, Dithiazanine Iodide, Dymanthine, Gen Rifaximin, Rifapentene tian Violet, 4Hexylresorcinol, Kainic Acid, Mebendazole, B-Lactams 2-Naphthol, Oxantel, piperazines, Pyrantel, Pyrvinium Carbapenems such as Imipenem Pamoate, a-Santonin, Stilbazium Iodide, Tetrachloroethyl Cephalosporins, such as 1-Carbadethia)Cephalosporin, ene. Thiabendazole, Thymol, Thymyl N-Isoamylcarbamate, Cefaclor, Cefadroxil, Cephalosporins, Cefatrizine, Cefaze Triclofenol piperazine, Urea Stibamine. done, Cefazolin, Cefixime, Cefinenoxime, Cefodizime, ANTHELMINTIC (ONCHOCERCA) such as Ivermectin 25 Cefonicid, CefoperaZone, Ceforamide, Cefotaxime, Cefo ANTHELMINTIC (SCHISTOSOMA) such as Ampho tiam, Ce?pimizole, Ce?piramide, Cefpodoxime Proxetil, tallide, Antimony(s) and Derivatives, Becanthone. Hycan Cefroxadine, Cefsulodin, Ceftazidime, Cefteram, Ceftezole, thone, Lucanthone, Niridazole, Oxamniquine, Praziquantel, Ceftibuten, Ceftizoxime, Ceftriaxone, Cefuroxime, Cefu Stibocaptate, Stibophen. Zonam, Cephacetrile, Sodium, Cephalexin, Cephaloglycin, ANTHELMINTIC (TREMATODES) such as Anthi 30 Cephaloridine, Cephalosporin C, Cephalothin, Cephapirin olimine Sodium, Cephradine, Piveefalexin Cephamycins such as ANTIACNE such as Algestone acetophenide, AZelaic Cefbuperazone, Cefinetazole, Cefninox, Cefotetan, Cefox Acid, Benzoyi Peroxide, Dichloroacetic acid, Motretinide, itin Retinoic Acid, Tetroquinone. Manobactams such as Aztreonam, carumonam, Tige ANTIALLERGIC such as Amlexanox, Astemizole, 35 Oa AZelastine, Cromolyn, Fenpiprane. Histamine, Ketotifen, Oxacephems such as Flomoxef, Moxolactam Nedocromil, Oxatomide, Pentigetide, Poison Ivy Extract, Penicillins such as Amidinocillin, Amdinocillin pivoxil, Poison Oak Extract, Poison Sumac Extract, Repirinast, Amoxicillin, Ampicillin, Apalcillin, Aspoxicillin, AZidocil Tiaramide, Tranilast, Traxanox, Urushiol, Cetirizine, Fex lin, AZiocillin, Bacampicillin, Benzylpenicillinic Acid, Ben ofenadine. 40 Zylpenicillin, Carbenicillin, Carfecillin, Carindacillin, ANTIAMEBIC such as Arsthinol, Bialamicol, Carbar Clometocillin, Cloxacillin, Cyclacillin, Dicloxacillin, sone, Cephaeline, Chlorbetamide, Chlorphenoxamide, Diphenicillin, Epicillin, Fenbenicillin, Floxicillin, Hetacil Dehydroemetine, Dibromopropamidine, Diloxamide, lin, Lenampicillin, Metampicillin, Methicillin, Meziocillin, Diphetarsone, Emetine, Fumagillin, Glaucarubin, Glycobi Nafcillin, Oxacillin, Penamecillin, Penethamate Hydriodide, arsol, 8-Hydroxy-7-iodo-5-quinoline sulfonic acid, Iodoch 45 Penicillin G Benethamine, Penicillin G BenZathine, Peni lorhydroxyquin, Iodoquinol, Paromomycin, Phanquinone, cillin G Benzhydrylamine, Penicillin G Calcium, Penicillin Phenarsone, Sulfoxylate, Polybenzarsol, Propamidine, G Hydrabamine, Penicillin G Potassium, Penicillin G Quinfamide, Secnidazole, Sulfarside. Teclozan, Thiocarbar Procaine. Penicillin N, Penicillin O, Penicillin V, Penicillin Sone. Thiocarbasone, Timidazole. V Benzathine, Penicillin V Hydrabamine, Penimepicycline, ANTIANDROGEN such as Bifluranol, Cyoctol, Cypro 50 Phenethicillin, Piperacillin, Pivampicillin, Propicillin, terone, Oxendolone Quinacillin, Sulbenicillin, Talampicillin, Temocillin, Ticar ANTIANGINAL such as Amlodipine, Amyl Nitrate, cillin Lincosamides such as clindamycin, Lincomycin Cinepazet Maleate, Imolamine, Isosorbide Dinitrate, Macrollides such as Azithromycin, Carbomycin, Limaprost, Molsidomine, Nitroxyalklamide Derivatives Clarithromycin, Erythromycin(s) and Derivatives, Josamy ANTIARRHYTHMIC such as Acecainide, Adenosine, 55 Ajmaline, Alprenolol, S-Aminoalkyl-S-Arylsulfoximines, cin, Leucomycins, Midecamycins, Miokamycin, Oleando Amoproxan, Aprindine, Bretylium Tosylate, Bucumolol. mycin, Primycin, Rosaramicin, Roxithromycin, Spiramycin, Bunaftine, Butidrine. Butobendine, Capobenic Acid, Cifen Troleandomycin, line, Disopyramide, Encainide, Flecainide, Hydroquinidine, Polypeptides Such as Amphomycin, Bacitracin, Capreo Indecainide, pratopium, Lorajmine, Lorcainide, Meoben 60 mycin, Colistin, Enduracidin, Enviomycin, Fusafungine, tine, Mexiletine, Moricizine, Pirmenol, Prajmaline, Gramicidin(s), Gramicidin S. Mikamycin, Polymyxin, Poly Procainamide, Pronethalol, Propafenone, Pyrinoline, Quini myxin B-Methane sulfonic acid, Pristinamycin, Ristocetin, dine, Quinidine Sulfate, Tocainide, Viduidil. Teicoplanin, Thiostrepton ANTIARTERIOSCLEROTIC such as Pyridinol Carbam Tuberactinomycin, Tyrocidine, Tyrothricin, Vancomycin, ate 65 Viomycin(s), Virginiamycin, Zinc Bacitracin ANTIARTHRITIC/ANTIRHEUMATIC Such as Allocu Tetracyclines such as Apicycline, Chlortetracycline, Clo preide Sodium, Auranofin, Aurothioglucose, Aurothioglyca mocycline, Demeclocycline, Guamecycline, Lymecycline, US 7,122,198 B1 7 8 Meclocycline, Methacycline, Minocycline, Oxytetracycline, Oxyphencyclimine, Oxyphenonium, Pentapiperide, Penimepicycline, Pipacycline, Rolitetracycline, Sancycline, Penthienate, Phencarbamide, Phenglutarimide, Pipenzolate, Senociclin, Tetracycline Piperidolate, Piperilate, Poldine methylsulfate, Pridinol, Pri Others Such as Cycloserine, Mupirocin, Tuberin finium, Propyromazine, Scopolamine N-Oxide, Stilonium, Stra Antibacterial (Synthetic) monium, Sultroponium, Thihexinol, Thiphenamil, Tiemo 2,4-Diaminopyrimidines Such as Brodimoprim, TetroX nium, Timepidium, Tiquizium, Tridihexethyl Iodide, Trihex oprim, Trimethoprim yphenidyl hydrochloride, Tropacine, Tropenzile, Nitrofurans such as Furaltadone, Furazolium, Nifuradene, Nifuratel, Nifurfoline, Nifurpirinol, Nifurprazine, Nifurtoi Tropicamide, Trospium, Valethamate, Xeny tropium 10 ANTICONVULSANT such as Acetylpheneturide, Albu nol, Nitrofurantoin Quinolones and Analogs such as Ami toin, Aloxidone, Aminoglutethimide, 4-Amino-3-hydroxy floxacin, Cinoxacin, Ciprofloxacin, Difloxacin, Enoxacin, butyric Acid, Atrolactamide, Beclamide, Buramate, Car Fleroxacin, Flumequine, Lomefloxacin, Miloxacin, Nalid bamazepine, Cinromide, Clonazepam, Decimemide, ixic Acid, Norfloxacin, Ofloxacin, Oxolinic acid, Pfloxacin, Diethadione, Dimethadione, Doxenitoin, Eterobarb, Ethadi Pipemidic Acid, Piromidic Acid, Rosoxacin, Temafloxacin 15 one, Ethosuximide, Ethotoin, Fluresone. Sulfonamides Such as Acetyl Sulfamethoxypyrazine, 5-Hydroxytryptophan, Lamotrigine, Magnesium Sulfate, Acetyl Sulfisoxazoie, AZosulfamide, Benzylsulfamide, Mephenyloin, Metharbital, Methetoin, MethSuximide, Chloramine-B, Chloramine-T, DichloramineT, Formosul 5-Methyl-5-(3-phenanthryl)-hydantoin, 3-Methyl-5Phenyl fathiazole, N2-Formyl-Sulfisomidine, N 4-O-D-Glucosyl hydantoin, Narcobarbital, Nimetazepam, Nitrazepam, sulfanilamide, Mafenide, 4'-(Methyl-sulfamoyl) sulfa Paramethadione, Phenacemide, Pheneturide, Phensuximide, nilanilide, p-Nitrosulfathiazole, Noprylsulfamide, Phenyloin, Phethenylate Sodium, Primidone, Progabide, Phthalylsulfacetamide, Phthalylsulfathiazole, Salazosulfadi Solanum, Strontium, Suclofenide, Sulthiame, Tetrantoin, midine. Succinylsulfathiazole, Sulfabenzamide, Sulfaceta Trimethadione, Valproic Acid, Valpromide, Vigabatrin, mide. Sulfachlorpyridazine, Sulfachrysoidine, Sulfacytine, Zonisamide. Sulfadiazine, Sulfadicramide, Sulfadimethoxine, Sulfadox ine, Sulfaethidole, Sulfaguanidine, /Sulfaguanol, Sulfalene, 25 Antidepressant Sulfaloxic acid, Sulfamerazine, Sulfameter, Sulfamethazine, Bicyclics such as Binedaline, CaroXaZone, Citalopram, Sulfamethizole, Sulfamethomidine, Sulfamethoxazole, Sul Dimethazan, Indalpine, fencamine, Indeloxazine, Nefopam, famethoxypyridazine, Sulfametrole, Sulfamidochrysoidine, Nomifensine, Oxitriptan, Oxypertine, Paroxetine, Sertraline, Sulfamoxole, Sulfanilamide, Sulfanilamidomethane ThiaZesim, Trazodone, Zometapine, sulfonic acid, Triethanolamine Salt, 4-Sulfanilamidosaly 30 Hydrazides/Hydrazines such as Benmoxine, Iproclozide, cylic acid, N-Sulfanilylsulfanilamide, Sulfanilylurea, Iproniazid, Isocarboxazid, Nialamide, Octamoxine, Phe N-Sulfanilyl-3,4 xylamide, Sulfanitran, Sulfaperine, Sul neizine. faphenazole, Sulfaproxyline, Sulfapyrazine, Pyrrolidones such as Cotinine, Rolicyprine, Rolipram. Sulfapiridine, Sulfasomizole, Sulfasymazine, Sulfathio 35 Tetracyclics such as Maprotiline, Metralindole, Zole, Sulfathiourea, Sulfatolamide, Sulfisomidine, Sulfisox Mianserin, Oxaprotiline. Tricyclics Such as Adinazolam, azole Amitriptyline, Amitriptylinoxide, Amoxapine, Butriptyline, Sulfones such as Acedapsone, Acediasulfone, Acetosul Clomipramine, Demexiptiline. Desipramine, Dibenzepin, fone, Dapsone, Diathimosulfone, Glocosulfone, Solasul Dimetacrine, Dothiepin, Doxepin, Fluacizine, Imipramine, fone, Succisulfone, Sulfanilic Acid, p-sulfanilylbenzy Imipramine N-Oxide, Iprindole, Lofepramine, Melitracen, lamine, p.p-Sulfonyldianiline, —N,N'digalactoside, 40 Metapramine, Nortriptyline, Noxiptilin, Opipramol, Sulfoxone, Thiazolesulfone Propizepine, Protriptyline, Quinupramine, Tianeptine, Others such as Clofoctol, Hexedine, Magainis, Meth Trimipramine enamine Anhydromethylenecitrate, Methenamine Hippu Others such as Benactyzine, Bupropion, Butacetin, rate, Methenamine Mandelate, Methenamine Sulfosalicy 45 Deanol, Deanol Aceglumate, Deanol Acetamidobenzoate, late, Nitroxoline, Squalamine, Xibornol Dioxadrol, etoperidone, Febarbamate. Femoxetine, Fenpen ANTICHOLINERGIC Such as Adiphenine, Alverine, tadiol, Fluoxetine, Fluvoxamine, Hematoporphyrin, Hyperi Ambutonium, Aminopentamide, Amixetrine, Amprotropine cin, Levophacetoperane, Lithium Medifoxamine, phosphate, Anisotropine methylbromide, Apoatropine, Atro Minaprine, Moclobemide, Oxaflozane, Piberaline, Polycy pine, Atropine N-Oxide, Benactyzine, Benapryzine, Ben 50 clic Imides, Prolintane, Pyrisuccideanol, Rubidium, Zetimide, Benzilonium, Benztropine mesylate, Bevonium Sulpiride, Sultopride, Teniloxazine, Thozalinone, Tofenacin, Methyl Sulfate; Biperiden, Butropium Toloxatone, Tranylcypromine, L-Tryptophan, Viloxazine, N-Butyiscopolammonium Bromide, Buzepide, Camy Zimeldine. lofine, Caramiphen, Chlorbenzoxamine, Chlorphenoxam Antidiabetic ine, Cimetropium, Clidinium, Cyclodrine, Cyclonium, 55 Biguanides such as Buformine, Metformin, Phenformin. Cyclopentolate, Cycrimine, Deptropine, Dexetimide, Dibu Sulfonylurea Derivatives such as Acetohexamide, 1-Bu toline Sulfate, Dicyclomine, Diethazine. Difemerine, Dihex tyl-3-metanily lurea, Carbutamide. Chlorpropamide, Glib yverine, Diphemanil methylsulfate, N-(1.2Diphenylethyl) ornuride, Gliclazide, Glipizide, Gliquidone, Glisoxepid, nicotinamide, Dipiproverine, Diponium, Emepronium, Glyburide, Glybuthiazol(e), Glybuzole, Glyhexamide, Gly Endobenzyline, Ethopropazine, Ethybenztropine, 60 midine, Giypinamide, Phenbutamide, Tolazamide, Tolbuta Ethylbenzhydramine, Etomidoline, Eucatropine, Fenpiv mide, Tolcyclamide erinium, Fentonium, Flutropium, Glycopyrrolate, Hetero Others such as Acarbose, Benzylthiazoldone-2,4-dione, nium, Hexocyclium Methyl Sulfate, Calcium Mesoxalate, Miglitol. Homatropine, Homatropine Methyl Bromide, Hyos ANTIDIARRHEAL such as Acetyltannic Acid, albumin cyamine, pratropium, Isopropamide, Levomepate, Meclox 65 Tannate, Alkofanone, Aluminium Salicylates, Catechin, amine, Mepenzolate, Metcaraphen, Methantheline, Methix Difenoxin, diphenoxylate, Lidamidine, Loperamide, ene, MethScopoiamine, Octamylamine, Oxybutynin, Mebiquine, Trillium, Uzarin. US 7,122,198 B1 9 10 ANTIDIURETIC such as Desmopressin, felypressin, HMG CoA Reductases Inhibitors such as Lovastatin, Lypressin, Ornipressin, Oxycinchophen, Terlipressin, Vaso Pravastatin, Simvastatin Nicotinic Acid derivatives Alumi pressin. num Nicotinate, Acipimox, Niceritol, Nicoclonate, Nico ANTIESTROGEN such as Delmadione Acetate, mol. Oxiniacic Acid Ethamoxytriphetol, Tamoxifen, Toremifene Thyroid Hormones/Analogs such as EtiroXate, thyro Antifungal (Antibiotics) propic Acid Polyenes such as Amphotericin-B, Candicidin, Dermosta Others such as Acifran, AZacosterol, Benfluorex, P-Ben tin, Filipin, Fungichromin, Zalbutyramide, Benzodioxole. Carnitine, Chondroitin Sul Hachimycin, Hamycin, Lucensomycin, Mepartricin, fate, Clomestone, Detaxtran, Dextran Sulfate Sodium, 5.8, 10 11.14.17-Eicosapentaenoic Acid, Eritadenine, Farnesylated Natamycin, Nystatin, Pecilocin, Perimycin. tetrahydronaphthalenols, Furazabol, Meglutoi, Melinamide, Others such as AZaserine, Griseofulvin, Oligomycins, Mytatrienediol, Naphthyltetrahydronaphtyl-diphospho Pyrrolnitrin, Siccanin, Tubercidin, Viridin. nates, Ornithine, y-Oryzanol, Pentethine, Penataerythritol, Antifungal (Synthetic) Tetraacetate.-Phenylbutyramide, Phylate Acids And Salts, Allylamines such as Naftifine, Tebinafine. 15 Pirozadil, Probucol, a-Sitosterol, Sultosilic Acid, Tiadenol, Imidazoles such as Bifonazole, Butoconazole, Chlordan Triparanol toin, Chlormidazole, Cloconazole, Clotrimazole, Econazole, Antihypertensive Enilconazole, Fenticonazole, Isoconazoie, Ketoconazole, Benzothiadiazine Derivatives sich as Althiazide, Bendrof Miconazole, Omoconazole, Oxiconazole nitrate, Sulcona lumethiazide, Benzthiazide, Benzylhydrochlorothiazide, Zole, Tioconazole Buthiazide, Chlorothiazide, Chlorthalidone, Cyclopenthiaz Triazoles Such as Fluconazole, Itraconazole, Terconazole. ide, Cyclothiazide, Diazoxide, Epithiazide, Ethiazide, Fen Others such as Acrisorcin, Amorolfine, Biphenamine, quizone, Hydrochlorothiazide, Hydroflumethiazide, Methy Bromosalicylchloranilide, Buclosamide, Chlorphenesin, clothiazide, Meticrane, Metolazone, Paraflutizide, Ciclopirox, Cloxyquin, Coparafinate. Diamthazole dihydro 25 Polythiazide, Tetrachlormethiazide, Trichlormethiazide chloride. Exalamide, Flucytosine, Halethazole, Hexetidine, N-Carboxyalkyl (peptide/lactam) Derivatives such as Loflucarban, Nifuratel, Potassium Iodide, Propionates, Pro Alacepril, Captopril, Cilazapril, Enalapril, Enalaprilat, Fosi pionic Acid. Pyrithione, Salicyianilide, Sulbentine, Tenoni nopril, Lisinopril, Moveltipril, Perindopril, Quinapril, Rami trozole, Tolciclate.-Tolindate, Tolnaftate, Triacetin, pril Ujothion, Undecylenic Acid 30 ANTIGLAUCOMA such as Dapiprazoke. Dichlorphena Guanidine Derivatives Bethanidine, Debrisoquin, Guana mide, Dipivefrin, Pilocarpine. cline, Guanadrel, GuanaZodine, Guanethidine, Guanochlor, ANTIGONADOTROPIN such as Danazol, Gestrinone, GuanoXabenz, Guanoxan Paroxypropione Hydrazines/Phthalazines such as Cadralazine, Dihydrala zine, Endralazine. Hydracarbazine, Hydralazine, Phenipra ANTIGOUT such as Colchicine, Probenecid, Sulfinpyra 35 ZO Zine, Pildralazine, Todralazine Antihistamic Alkylamine Derivatives Such as Acrivas Imidazole Derivatives such as Lofexidine, Phentolamine, tine, Bamipine, Brompheniramine, Chlorpheniramine, Tolonidine Dimethindeda, Tolpropamine, Triprolidine Quaternary Ammonium Compounds AZamethonium Aminoalkyl Ethers such as Bietabanautine, Bromo 40 Chlorisondamine. Hexamethonium, Pentacynium bis(meth diphenhydramine, Carbinoxamine, Clemastine, Diphe ylsulfate), Pentamethonium, Pentolinium Tartate, Phenac nylpyraline, Doxylamine, Embrammine, Medrylamine, tropinium, Trimethidinium Methosulfate Mephenhydramine, p-Methyldiphenhydramine, Quinazoline Derivatives Such as AlfuZosin, BunaZosin Orphenadrine, Phenyltoloxamine, Piprinhydrinate, Setastine Reserpine Derivatives such as Bietaserpine, Deserpidine, Ethylenediamine Derivates Such as Alloclamide, p-Bro 45 Rescinnamine, Reserpine, Syrosingopine mtripelennamine, Chloropyramine, Chlorothen, Histapyrro Sulfanoamide Derivatives such as Ambuside, Clopamide, dine, Methafurylene, Methaphenilene, Methapyrilene, Furosemide, Indapamide, QuinethaZone, Tripamide, Xipa Phenbenzamine, Pyrilamine, Talastine. Thenyldiamine, mide Thonzylamine, Tripelennamine, Zolamine Others such as Ajmaline, g-Aminobutyric Acid, Bufe Piperazines such as Cetirizine, Chlorcyclizine, Clociniz 50 niode, Chlorthalidone, Cicletainine, Ciclosidomine, Crypte ine, Hydroxyzine Tricyclies Phenothiazines such as Ahistan, namine Tannates, Floseduinan, Indoramin, Ketanserin, Met Etymemazine, Fenethazine, N-Hydroxyethyl promethazine, butamate, Mecamylamine, Methyldopa, Methyl 4-Pyridyl Isopromethazine, Mequitazine, Promethazine, Pyrathiazine, Ketone Thiosemicarbazone, Metolazone, Minoxidil. Thiazinamium Methyl Sulfate Muzolimine, Pargyline Glycine Aminopropargyl Diols, Pro Others such as AZatadine, Clobenzepam, Cyproheptadine, 55 toveratrines, Raubasine, Rescimetol, Saralasin, Sodium Deptropine, Isothipendyl, Loratadine, Prothipendyl Nitroprusside, Ticrynafen, Trimethaphan camsylate, Tyrosi Others such as Antazoline, Cetoxime, Clemizole, Cloben nase, Urapidil Ztropine, Diphenazoline, Diphenhydramine, Mebhydroline, ANTIHYPERTHYROID Such as 2-Amino-4-methylthi Phenindamine, Terfenadine, Tritoqualine 60 azole, 2-Aminothiazole, Carbimazole, 3,5-Dibromo-L-ty Antihyperlipoproteinemic rosine, 3,5-Diiodotyrosine, Hinderin, Iodine, lothiouracil, Aryloxyalkanoic Acid Derivatives such as Bazafibrate, Methimazole, Methylthiouracil, Propylthiouracil, Sodium Binifibrate, Ciprofibrate, Clinofibrate, Clofibrate, Clofibric Perchlorate. Thibenzazoline. Thiobarbital, 2-Thiouracil Acid, Etofibrate, Fenofibrate. Gemfibrozil, Nicofibrate. Piri ANTIHYPOTENSIVE such as Amezinium Methyl Sul fibrate, Ronifibrate, Simfibrate, Theofibrate 65 fate, Angiotensin Amide, Etifelmin, Etilefrin, Gepefrine Bile Acid Sequesterants such as Cholestyramine Resin, ANTIHYPOTHYROID such as Levothyroxine, Liothy Colestipol, Polidexide ronine, Thyroid, Thyroidin, Thyroxine, Tiratricol US 7,122,198 B1 11 12 Anti-Inflammatory (Nonsteroidal) Nitrogen Mustards such as Chlorambucil, Chlornaphaz Aminoarylcarboxylic Acid Derivatives such as Etofe ine, Cyclophosphamide, Estramustine, Ifosfamide, Mechlo namate, Meclofenamic Acid, Mefanamic Acid, Niflumic rethamine, Mechlorethamine Oxide Hydrochloride, Mel Acid phalan, Novembichin, Phenesterine, Prednimustine, Arylacetic Acid Derivatives such as Acemetacin, Trofosfamide, Uracil Mustard Amfenac, Cinmetacin, Clopirac, Diclofenac, Fenclofenac, Nitrosoureas Carmustine, Chlorozotocin, Fotemustine, Fenclorac, Fenclozic Acid, Fentiazac, Glucametacin, ISOX Lomustine, Nimustine, Ranimustine epac, Lonazolac, Metiazinic Acid, Oxametacine, Proglu Others such as Dacrabazine, Mannomustine, Mitobroni metacin, Sulindac, Tiaramide, Tolimetin tol, Mitolactol, Pipobroman Arylbutyric Acid Derivatives such as Butibufen, Fen 10 Antibiotics such as Aclacinomycins, Actinomycin F1, bufen Anthramycin, AZaserine, Bleomycins, Cactinomycin, Caru Arylcarboxylic Acids such as Clidanac, Ketorolac, Tino bicin, Carzinophilin, Chromomycins, Dactinomycin, radine Daunorubicin, Carzinophilin, Chromomycins, Dactinomy Arylpropionic Acid Derivatives such as Bucloxic Acid, cin, Daunorubicin, 6-Diazo-5oxo-L-norleucine, Doxorubi Carprofen, Fenoprofen, Flunoxaprofen, Ibuprofen, Ibu 15 cin, Epirubicin, Mitomycins, Mycophenolic Acid, Nogala proxam, Oxaprozin, Piketoprofen, Pirprofen, Pranoprofen, mycin, Olivomycins, Peplomycin, Plicamycin, Protizinic Acid, Tiaprofenic Acid Profiromycin, Puromycin, Streptonigrin, Streptozocin, Pyrazoles such as Epirizole Tubercidin, Ubenimex, Zinostatin, Zorubicin Pyrazoles such as Mepirizole Antimetabolites Pyrazolones such as ClofeZone, Feprazone, Mofebuta Folic Acid Analogs such as Denepterin, Methotrexate, Zone, Oxyphenbutazone, Phenylbutazone, Phenyl Pyrazoli Pteropterin, Trimetrexate Purine Analogs such as Fludara dininones, Suxibuzone. Thiazolinobutazone bine, 6-Mercaptopurine. Thiamiprine. Thiguanaine Salicylic Acid Derivatives such as Bromosaligenin, Fen Pyrimidine Analogs such as Ancitabine, AZacitidine, 6-AZauridine, Carmofur, Cytarabine, Dibexyuridines, Doxi dosal, Glycol Salicylate, Mesalamine, 1-Naphthyl Salicy 25 late, Olsalazine, Sulfasalazine fluridine, Enocitabine, floxuridine, Fluorouracil, Tegafur Thiazinecarboxamides such as Droxicam, Isoxicam, Enzymes such as L-Asparaginase, Pulmozyme Piroxicam Others such as Aceglatone, Aldophosphamide Glycoside, Aminolevulinic Acid, Amsacrine, Bestrabucil, Bisantrene, Others such as e-Acetamidocaproic Acid, S-Adenosylme Carboplatin, Deformide, Demecolcine, Diaziquone, thionine, 3-Amino-4-hydroxybutyric Acid, Amixetrine, 30 Elformithine, Elliptinium Acetate, Etoglucid, Etoposide, Bendazac, Bucolome, Carbazones. Difenpiramide, Ditazoi, Gallium Nitrate, Hydroxyurea, Interferon-a, Interferon-0. GuaiaZulene, Heterocyclic Aminoalkyl Esters of Mycophe Interferon-y, Interleukin-2, Lentinan, Lonidamine, Mitogua nolic Acid And Derivatives, Nabumetone, Nimesulide, Zone, Mitoxantrone, Mopidamol, Nitracrine, Pentostatin. Orgotein, Oxaceprol, Oxazole Derivatives Paranyline, Phenamet, Pirarubicin. Podophyllinic Acid, 2-Ethylhy Pifoxime, 2-subsitituted-4,6-di-tertiary-butyl-s-hydroxy-1, 35 3-pyromidines, ProquaZone, Sialyl Lewis Dimers, Tenidap drazide, Procarbazine, PSKR), Razoxane, Sizofiran, Spirog ANTIMALARIAL such as Acedapsone, Alphamino ermanium, Taxol. Teniposide, TenuaZonic Acid, Triazi quinolines, 40 Aminoquinolines. Amodiaquin, Arteether, quone, 2.2.2"Trichlorotriethylamine, Urethan, Vinblastine, Artemether, Artemisinin, Artesunate, Bebeerine, Chirata, Vincristine, Vindesine Chlorguamide, Chloroquine, Chlorproguanil, Chinchona, 40 Antineoplastic(Hormonal) Cinchonidine, Cinchonine, Cycloguanil, Eudinine. Gen Androgens Such as Calusterone, Dromostanolone Propi tiopicrin, Halofantrine, Mefloquine Hydrochloride, 3-Me onate, Epitiostanol, Mepitiostane, Testolactone Antiadrenals thylarsacetin, Pamaquine, Plasmocid, Primaquine, Such as Aminoglutethimide, Mitotane, TriloStane Pyrimethamine, Quinacrine, Quinine, (Acids, Salts and Antiandrogens such as Flutamide, Nilutamide Derivatives), Quinine Formate, Quinine Gluconate, Quinine 45 Antiestrogens such as Aromatase Inhibiting 4(5)-Imida Tannate, Quinine Urea Hydrochloride, Quinocide, Quino Zoles form, Quinoline, Sodium Arsenate, Diabasic ANTIMIGRAINE such as Alpiropride, Dihydroergota Antineoplastic Adjunct mine, Ergocornine, Ergocorninine, Ergocryptine, Ergot, Folic Acid Replenisher such as Frolinic Acid Ergotamine, Flumedroxone FlumedroXone acetate, Fona 50 ANTIPARKINSONIAN such as Amantadine, Benser zine, Methysergid(e), Oxetorone, Pizotyline, Sumatriptan azide, Bietanautine, Biperiden. Budipine, Carbidopa, Depre ANTINAUSEANT such as Acetylleucine Monoethano nyl, Dexetimide, Diethazine, Droxidopa, Ethopropazine, lamine, Bietanautine, Bromopride, Buclizine, Clebopride, Ethylbenzhydramine, Levodopa, Piroheptine, Pridinol, Cyclizine, Dimenhydrinate, Diphenidol, Domperidone, Gra Prodipine, Terguride, Tiapride, Tigloidine nisetron, Meclizine, Methallatal, Metoclopramide, Metopi 55 ANTIPHEOCHROMOCYTOMA such as Metyrosine, mazine, Nabilone, Phenoxybenzamine Ondansetron, Oxypendyl, Pipamazine, Piprinhydrinate, ANTIPNEUMOCYSTIS Such as Eflornithine Scopolamine, Tetrahydrocannabinols. Thiethylperazine, Tri ANTIPROSTATIC HYPERTROPHY Such as ProScar(R) methobenzamide ANTIPROTOZOAL (LEISHMANIA) such as Ethyl 60 stibamine, Hydroxystilbamidine, N-Methylglucamine, Pen Antineoplastic tamidine, Stilbamidine Alkyl agents: Alkyl Sulfonates Such as BuSulfan, Impro ANTIPROTOZOAL (TRICHOMONAS) such as Acetar sulfan, Piposulfan, Aziridines such as Benzodepa, Carbo Sone, Aminitrozole, Anisomycin, AZanidazole, forminitra quone, Meturedepa, Uredepa Zole, furazolidone, AZanidazole, Lauroguadine, Metronida Ethylenimines and Methylmelamines such as Altre 65 Zole, Nifuratel, Nimorazole, Silver Picrate, Tenonitrozole tamine, Triethylenemelamine, Triethylenephosphoramide, ANTIPROTOZOAL(TRYPANOSOMA) such as Ben Triethylenethiophosphoramide, Trimethylolmelamine Znidazole, Eflornithine, L. Melarsoprol, Nifurtrimox, US 7,122,198 B1 13 14 Oxophenarsine, Puromycin, Quinapyramine, Suramin Codeine Methyl Bromide, Codeine N-Oxide, Codeine Phos Sodium, Trypan Red, Tryparsamide phate, Codeine Sulfate, Cyclexanone, Dextromethorphan, ANTIPRURITIC such as Camphor, Cyproheptadine, Dibunate Sodium, Dihydrocodeine, Dihydrocodeinone Eno Dichlorisone, Glycine, Halometasone, 3-Hydroxycamphor, Acetate, Dimemorfan, Dimethoxanate a, a-Diphenyl-2-pi Menthol, Mesulphen, Methdilazine, Phenol, Spirit Of Cam 5 peridinepropanol, Dropropizine, Drotebanol, EpraZinone, phor, Trimeprazine Ethyl Dibunate, Ethylmorphine, Fominoben, Guaiapate, ANTIPSORIATIC such as Acitretin, Anthralin, 6-AZau Hydrocodone, Isoaminile, Levopropoxyphene, Morclofone, ridine, Bergrapten(e), Chrysarobin, Etretinate, Pyrogallol Narceline, Normethadone Noscapine, Oxeladin, Oxolamine, Antipsychotic Pholcodine, Picoperine, Pipazethate, Piperidione, Prenoxdi Butyrophenones such as Benperidol, Bromperidol, Dro 10 azine, Racemethorphan, TaZiprinon hydrochloride, Tipepi peridol, Fluanisone, Haloperidol, Melperone, Moperone, dine, Zipeprol Pipamperone, Spiperone, Timiperone, Trifulperidol ANTITULCERATIVE such as Aceglutamide Aluminum Phenothiazines Such as Acetophenazine. Butaperazine, complex, F-Acctamidocaproic Acid Zinc Salt, Acetoxolone, Carphenazine, Chlorproethiazine, Chlorpromazine, Clospi Arbaprostil, Benexate Hydrochloride, Bismuth Subcitrate razine, Mepazine, Mesoridazine, Methoxypromazine, 15 Sol(Dried), Carbenoxolone, Cetraxate, Cimetidine, Enpros Metofenazate, Oxflumazine, Perazine, Pericyazine, Perimet tii, Esaprazole, Famotidine, Ftaxilide, Gefarnate, GuaiaZu hazine, Prochlorperazine, Promazine, Sulforidazine. Thio lene, Irsogladine, Nizatidine, Omeprazole, Ornoprostil, propazate. Thioridazine, Trifluoperazine, Triflupromazine YOryzanol, Pifamine, Pirenzepine, Plaunotol, Ranitidine, Thioxanthenes such as Chlorprothixene, Clopenthixol, Rioprostil, Rosaprostol, Rotraxate, Roxatidine Acetate, Flupentixol. Thiothixene Sofalcone, Spizofurone. Sucralfate, Teprenone, Trimopros Other Such as Alizapride, Amisulpride, 4-Arylpipera til, Trithiozine, Troxipide, Zolimidine. Zines, 4-Arypiperdines, Buramate, Fluspirilene, Molindone, ANTIUROLITHIC such as Acetohydroxamic Acid, Penfluridol, Pimozide, Spirilene, Sulpiride Allopurinol, Potassium citrate. Succinimide. ANTIPYRETIC such as Aconine, Aconite, Aconitine, ANTIVENIN such as Lyovacr(R), Antivenin. Phenicarbazide 25 Antiviral ANTIRICKETTSIAL such as p-Aminobenzoic Acid Purines/Pyrimidines such as 2-Acetyl-pyridine 5-((2-py ANTISEBORRHEIC such as 3-O-Lauroylpyridoxol ridylamino) thiocarbonyl). ThiocarbonohydraZone, Acyclo Diacetate, Piroctone, Resorcinol, Selenium Sulfides, Tiox Vir, Dideoxyadenosine, Dideoxycytidine, Dideoxyinosine, olone 30 Edoxudine, Floxuridine, Ganciclovir, Idoxuridine, MADU, Antiseptic Pyridinon, Trifluridine, Vidarabine, Zidovudine. Others such as Acetylleucine, Monoethanolamine, Acridi Guanidines Such as Alexidine, Ambazone, Chlorhexi anamine, Alkylisoxazoles, Amantadine, Amidinomycin, dine, Picloxydine Halogens/Halogen compounds such as Cuminaldehyde. ThiosemicarbZone, Foscarnet Sodium, Bronyl Chloride, Calcium Iodate, Iodine Monochloride, Kethoxal, Lysozyme, Methisazone, Moroxydine, Podophyl Iodine Trichloride, Iodoform, Povidone-Iodine, Sodium 35 Hyopchlorite, Sodium Iodate, Symclosene, Thymol Iodide, lotoxin, Ribavirin, Rimantadine, stallimycin, statolon, Thy Triclocarban, Triclosan, Troclosene Potassium mosins, Tromantadine, Xenazoic Acid. Nitrofurans such as Furazolidone, 2-(Meth oxymethyl)- Anxiolytic 5-Nitrofuran, Nidroxy Zone, Nifuroxime, Nifurzide, Nitro Arylpiperazines such as Buspirone, Gepirone, Ipsapirone. furaZone 40 Benzodiazepine Derivatives Alprazolam, Bromazepam, Phenols such as Acetomeroctol, Chloroxylenol, Camazepam, Chlordiazepoxide, Clobazam, CloraZepate, Hexachlorophene, 1-Naphthyl Salicylate, 2,4,6-Tribromo Clotiazepam, Cloxazolam, Diazepam, Ethyl Loflazepate, m-cresol. 3'4',5-Trichlorosalicylanilide Etizolam, Fluidazepam, Flutazolam, Flutoprazepam, Quinolines Such as Aminoquinuride, Chloroxine, Chlo Halazepam, Ketazolam, Lorazepam, Loxapine, rquinadol, Cloxyquin, Ethylhydrocupreine, Halquinol, 45 Medazepam, Metaclazepam, Mexazolam, Nordazepam, Hydrastine, 8-Hydroxquinoline Sulfate Oxazepam, Oxazolam, Pinazepam, Prazepam, Tofisopam. Others such as Boric Acid, Chloroazodin, m-Cresyl Carbamates Such as Cyclarbamate, Emylcamate, Hydrox Acetate, Cuperic Sulfate, Ichthammol yphenamate, Meprobamate, Phenoprobamate, Tybamate. ANTISPASMODIC such as Alibendol, Ambucetamide, Others Alpidem, Benzoctamine, Captodiamine, Chlorme Aminopromazine, Bietamiverine. Butaverine, Butropium, 50 Zanone, Etifoxine, Fluoresone, Glutamic Acid, Hydrox Caroverine, Cimetropium, Cinnamedrine, Clebopride, Coni yZine, Mecloralurea, Mephenoxalone, Oxanamide, Phenag ine hydrobromide, Coniine, Difemerine, Diisopromine, lycodol, Suriclone. Dioxaphetyl Butyrate, Drofenine, Ethaverine, Feclemine, BENZODIAZEPINE ANTAGONIST Such as Flumaze Fenalamide, Fenoverine, Fenpiprane, Flavoxate, Flopropi nil. one. Gluconic Acid, Guaiactamine, Hydramitrazine, Hyme 55 cromone, Leiopyrrole, Mebeverine, Moxaverine, Nafiver Bronchodilator ine, Octaverine, Phenamacide, Phloroglucinol, Pinaverium, Ephedrine Derivatives such as Albuterol, Bambuterol, Piperilate, Pipoxolan hydrochloride, Pramiverin, Properi Bitolterol, Carbuterol, Clenbuterol, Clorprenaline, Diox dine, Propivane, ethedrine, Eprozinol, Etafedrine, Ethylnorepinephrine, ANTITHROMBOTIC such as Anagrelide, Argatroban, 60 Fenoterol, Hexoprenaline, Isoetharine, Isoproterenol, Cilostazol, Daltroban, Defibrotide, Enoxaparin, Fraxipari Mabuterol, Metaproterenol, N-Methylephedrine, Pirbuterol, ner R, Indobufen, Lamoparan, OZagrel, Picotamide, Procaterol, Protokylol, Reproterol, Rimiterol, Soterenol, Plafibride, Tedelparin, Ticlopidine, Triflusal. Terbutaline, Tulobuterol. ANTITUSSIVE such as Allocamide, Amicibone, Benpro Quaternary Ammonium Compounds such as Flutropium perine, BenZonatate, Bibenzonium, Bromoform, 65 Bromide, Oxitropium Bromide. Butamirate. Butethamate, Caramiphen Ethanedisulfonate, Xanthine Derivatives such as Acefylline piperazine, Ace Carbetapentane, Chlophedianol, Clobutinol, Cloperastine, fylline Ambuphylline, Aminophylline, Bamifylline, Choline US 7,122,198 B1 15 16 Theophyllinate, Doxofylline, Dyphylline, Enprofylline, Pentylenetetrazole, Phenidimetrazine, Phenmetrazine, Etamiphyllin, Eto?ylline, Guaithylline, Proxyphylline, Phentermine, Picrotoxin, Pipradrol, Prolintane, Pyrovale Theobromine, 1-Theobromineaceatic Acid, Theophylline. rone, Terahydrobenzothienpphyridines. Others such as Methoxyphenanime, Tretoquinol. DECONGESTANT such as Cafaminol, nordefrin DENTAL CARRIES PROPHYLACTIC Such as Sodium Calcium Channel Blocker fluoride. Arylalkylamines such as Bepridil, Diltiazem, Fendiline, DEPIGMENTOR such as Hydroquinine, Hydroquinone, Gallopamil, Terodiline, Verapamil. Monobenzone Dihydropyridine derivates such as Felodipine, Isradipine, Nicardipine, Nifedipine, Nilvadipine, Nimodipine, Nisol Diuretic dipine, Nitrendipine 10 Organomercurials such as Chlormerodrin, Meralluride, Piperazine Derivatives Such as Flunarizine Mercamphamide, Mercaptomerin Sodium, Mercumallylic Others Such as Perhexiline. Acid, Mercumatillin Sodium, Mercurous Chloride, Mersa CALCIUM REGULATOR such as Calcifediol, Calcito lyl. nin, Calcitriol, Clodronic Acid, Dihydrotachysterol, Elcato 15 Pteridines such as Furterene, Triamterene. nin, Etidronic Acid, Ipriflavone, Pamidronic Acid, Parathy Purines such as 7-Morpholinomethyltheophylline, Pam roid Hormone, Teriparatide Acetate. abrom, Protheobromine, Theobromine CARDIOTONIC such as Acetyldigitoxins, 2-Amino Steroids such as Canrenone, Oleandrin, Spironolactone 4-Picoline, Amrinone, Buclasdesine, Cerberoside, Cam Sulfonamide Derivatives such as Acetazolamide, photamide, Convallatoxin, Cymarin, Denopamine, Deslano AZosemide, Bumetanide, Butazolamide, Chloraminophena side, Digitalin, Digitalis, Digitoxin, Digoxin, Dobutamine, mide, Clofenamide, Clorexolone, Diphenylmethane-4,4'- Dopamine, Dopexamine, Enoximone, Erythrophleine, Disulfonamide, Disulfamide, EthoXZolamide, Flumethiaz Fenalcomine, Gitalin, Gitoxin, Glycocyamine, Heptaminol, ide, Mefruside, Methazolamide, Piretamide Torasemide. Hydrastinine, Lanatosides, Metamivam, Uracils such as Aminometradine, Amisometradine Substituted Methoxyphenyl-4,5-dihydro-3(2H)-pridazi 25 Others such as Amanozinde, Amiloride, Arbutin, Chlora nones, Milrionone, Neriifolin, Oleandrin, Ouabain, Oxy Zanit, Ethacrynic Acid, Etozolin, Isosorbide, Mannitol, fedrine, Prenalterol, Proscillaridin, Resilbufogenin, Scil Metochalcone, Perhexiline, Urea. laren, Scillarenin, Strophanthin, Sulmazole. Theobromine, DOPAMINE RECEPTORAGONIST such as Bromocrip Xamoteroi. tine, Fenoldopam, Lisuride, Naxagolide, Pergolide. ECTOPARASITICIDE such as Amitraz, Benzyl Ben CHELATING AGENT such as Deferoxamine, Edetate 30 Zoate, Carbaryl, Crotamiton, DDT. Dixanthogen, Isobornyl Calcium Disodium, Edetate Disodium, Edeate Sodium, Ede Thiocyanoacetate (Technical), Lime Sulfurated Solution tate Trisodium, Pentetate Calcium Trisodium, Pentectic Lindane, Malathion, Mercuric Oleate, Sulphur (Pharmaceu Acid, Succimer, Trientine. tical). Cholecystokinin Antagonist (Proglumide) 35 Enzyme CHOLELITHOLYTIC AGENT such as Chenodiol, Digestive such as Amylase(Swine Pancreas), Lipase, Methyl tert-Butyl Ether, Monooctanoin, Ursodiol. Pancrelipase, Pepsin, Renin CHOLERETIC such as Alibendol, Anethole Trithion, AZintamide, Cholic Acid, Cicrotoic Acid, Clanobutin, Penicillin Inactivating such as Penicillinase Cyclobutyrol, Cyclovalone, Cynarin(e) Dehydrocholic Proteolybc Such as Collagenase, Chymopapain, Chymot Acid, Deoxycholic Acid, Dimecrotic Acid, d-Ethylbenzyl 40 rypsins, Papain, Trypsin Alcohol, Exiproben, Feguprol, Fencibutirol, Fenipentol, ENZYME INDUCER (HEPATIC) such as Flumecinol. Florantyrone, Hymecromone, Menbutone, 3-(OMethox Estrogen yphenyl)-2-Phenylacrylic Acid, Metochalcone, Moquizone, Nonsteroidal such as Benzestrol, Broparoestrol, Chloro Osalmid, Ox Bile Extract, 4,4'-Oxydi-2-Butanol, Piprozolin, 45 trianisene, Dienestrol, Diethylstilbestrol, Diethylstilbestrol Prozapine, 4-Salicyloylmorpholine, Sincalide, Taurocholic Diproprionate, Dimestrol, Fosfestrol, Hexestrol, Methallen Acid, Timonacic, Tocamphyl, Trepibutone, Vanitiolide. stril, Methestrol. CHOLINERGIC such as Aceclidine, Acetylcholine bro Steroidal such as Colpormon, Conjugated Estrogenic mide, Acetylcholide, Aclatonium napadisilate, BenZpy Hormones, equilenin, Equilin, Esterified Estrogens Estropi rinium bromide, Bethanechol, Carbachol, Carpronium, 50 pate, 17 B-Estradiol, Estradiol, estradiol Benzoate, Estradiol Demecarium, Dexpanthenol. Diisopropyl Paraoxon, 17b-Cypionate, Estrone, Ethinyl Estradiol, Mestranol, Mox Echothiophate, Edrophonium, Eseridine, Furtrethonium, estrol, Mytatrienediol, Polyestradiol Phosphate, Quinestra Isoflurophate, Methacholine chloride, Muscarine Neostig diol, Quinestrol. mine, Oxapropanium, Physostigmine, Pyridostigmine. GASTRIC SECRECTION INHIBITOR Such as entero CHOLINESTERASE INHIBITOR such as Ambenonium, 55 gastrone, Octreotide. Distigmine, Galanthamine. GLUCOCORTICOID such as 21-Acetoxypregnenolone, CHOLINESTERASE REACTIVATOR Such as Obi Alclometasone, Algestone, Amcinonide, Beclomethasone, doxime, Pralidoxime CNS STIMULANT/AGENT Such as Betamethasone, Betamethasone dipropionate, Budesonide, Amineptine, Amphetamine, Amphetaminil, Bemegride, Chloroprednisone, Clobetasol, Clobetasone, Clocortolone, Benzphetamine, Brucine, Caffeine, Chlorphentemine, 60 Cloprednol, Corticosterone, Cortisone, Cortivazol, Deflaza Clofenciclan, Cloratermine, cort, DeSonide, DeSoximetasone, Dexamethasone, Diflo Coca, Demanyl Phosphate, Dexoxadrol, Dextroamphet rasone, Diflucortolone. Difluprednate amine Sulfate, Diethylpropion, N-Ethylamphetamine, Enoxolone, Fluazacort, Flucloronide, Flumethasone, Ethamivan, Fencamfamine, Fenethylline, Fenozolone, Flunisolide, Fluocinolone acetonide, Fluocinonide, Fluocor Flurothyl, Hexacyclonate Sodium, homocamfin, Mazindol, 65 tin butyl, Fluocortolone, Fluorometholone, Fluperolone Mefexamide, Methamphetamine, Methylphenidate, Nico acetate, Fluprednidene acetate, Fluprednisolone, Flurandre tine, Nicotinic agonist, Nikethamide, Pemoline, nolide. Formocortal, Halcinonide, Halometasone, Halopre US 7,122,198 B1 17 18 done Acetate, Hydrocotramate, Hydrocortisone, Hydrocor razepam, Thiocolchicoside, Tizanidine, Tolperisone, tisone Acetate, Hydrocortisone phosphate, Hydrocortisone Tubocurarine, Vecuronium, Zoxazolamine. 21-Sodium Succinate, Hydrocortisone Tebutate, NARCOTIC ANTAGONIST such as Amiphenazole, Mazipredone, Medrysone, Meprednisone, Methylpredniso Cyclazocine, Levallorphan, Nadide, Nalmafene, Nalor lone, Mometasone furoate, Paramethasone, phine, Nalorphine Dinicotinate, Naloxone, Naltrexone. Prednicarbate, Prednisolone, Prednisolone 21-Diethy NEUROPROTECTIVE such as Dizocilpine laminoacetate, Prednisolone Sodium Succinate, Predniso NOOTROPIC such as Aceglutamide, Acetylcarnitine, lone Sodium Phosphate, Prednisolone Sodium 21-mSul Aniracetam, Bifemelane. Exifone, Fipexide, Idebenone, fobenzoate, Prednisolone 21-Stearoylglycolate, Indeloxazine, Nizofenone, Oxiracetam, Piracetam, Pro Prednisolone Tebutate 10 pentofylline, Propentofylline Pyritinol Prednisolone 21-Trimethylacatate, Prednisone, Prednival, OPHTHALMICAGENT such as 15-ketoprostaglandins. Prednylidene, Prednylidene 21-Diethylaminoacetate, Tixo cortal, Triamcinolone, Triamcinolone acetonide, Triamcino Ovarian Hormone such as Relaxin lone benetonide, Triamcinolone hexacetonide, GONAD OXYTOCIC such as Carboprost, Cargutocin, Deami STIMULATING PRINCIPLE such as Clomiphene, 15 nooxytocin, Ergonovine, Gemeprost, Methylergonovine, Cyclofenil, Epimestrol, FSH, HCG, LH-RH. Oxytocin, Pituitary (Posterior), Prostaglandin E2. Prosta GONADOTROPIC HORMONE such as LH, PMSG gandin F2a, Sparteine. GROWTH HORMONE INHIBITOR Such as Somatostatin PEPSIN INIBITOR such as Sodium Amylosulfate GROWTH HORMONE RELEASING FACTOR Such as PERISTALTICSTIMULANT such as Cisapride Sermorelin PROGESTOGEN such as Allylestrenol, Anagestone, GROWTH STIMULANT such as Somatotropin Chlormadinone Acetate, delmadinone Acetate, Demege HEMOLYTIC such as Phenylhydrazine stone, Desogestrel, Dimethisterone, Dydrogesterone, Ethi HEPARIN ANTAGONIST Such as Hexadimethrine nylestrenol, Ethisterone, Ethynodiol, Ethynodiol Diacetate, Protamines. Flurogestone Acetate, Gestodene, Gestonorone Caproate, HEAPATOPROTECTANT such as Betaine, Citiolone, 25 Haloprogesterone, 17-Hydroxy-16-methylene-progester Malotilate, Orazamide, Phosphorylcholine, Protoporphyrin one, 17-Hydroxyprogesterone, 17a-Hydroxygesterone IX. Silymarin-Group. Thioctic Acid, Caproate, Lynestrenol, Medrogestone, Medroxyprogester IMMUNOMODULATOR such as Amiprilose, Bucil one, Megestrol acetate, Melengestrol, Norethindrone, Nore lamine, Ditiocarb Sodium, Inosine Pranobex, Muroctasin, thindrone Acetate, Norethynodrel, Norgesterone, Norgesti Platonin, Procodazole, Tetramisole, 6-Aryl-1-5-6-Digy 30 mate, Norgestrel, Norgestrienone, 19-Norprogesterone, droimidazol-(2,1-B) Thiazole Derivatives, Thymomodulin, Norvinisterone, Pentagestrone, Progesterone, Promege Thymopentin. Stone, Quingestrone, Trengestone IMMUNOSUPPRESSANT such as Cyclophilin, PROLACTIN INHIBITOR such as Metegoline Cyclosporins, FK-506, Mizoribine, Rapamycin, Rapamycin PROSTAGLANDINAPROSTAGLANDIN ANALOG Sulfamates 35 such as Beraprost, Prostacyclin, Prostaglandin E1, Suipro IONEXCHANGE RESIN such as Carbacrylic Resins, StOne Resodec, Sodium Polystyrene Sulfonate PROTEASE INHIBITOR such as Aprotinin, Camostat, LACTATION STIMULATING HORMONE Such as Pro Gabexate, Nafamo.stat lactin RESPIRATORY STIMULANT such as Almitrine, Dime 40 fline, Dimorpholamine, Doxapram, Lobeline, Mepixanox, LH-RHAGONIST such as Buserelin, Goserelin, Leupro Pimeclone, Sodium Succinate, Tacrine lide, Nafarelin, Triptorelin. SCLEROSING AGENT such as Ethanolamine, Ethy LIPOTROPIC such as N-Acetylmethionine, Choline lamine, 2-Hexyldecanoic Acid, Sodium Ricinoleate, Sodium Chloride, Choline Dehydrocholate, Choline Dihydrogen Tetradecyl Sulfate, Tribenoside Citrate, Inositol, Lecithin, Methionine 45 LUPUS ERYTHEMATOSUS SUPPRESSANT Such as Sedative/Hypnotic Bismuth Sodium Triglycollamate, Bismuth Subsalicylate. Acyclic Ureides such as Acecarbromal, Apronalide, Bro MINERALOCORTICOID such as Aldosterone, Deoxy misovalum, Capuride, Carbromal, Ectylurea, Alcohols such corticosterone, Fludrocortisone. as Chlorhexadol, Ethchlorvynol, 4-Methyl-5-thiazoleetha 50 nol, Tert-Pentyl Alcohol, 2.2.2.-Trichloroethanol MIOTIC such as Pilocarpus Amides such as Butoctamide, Diethylboromoacetamide, MONOAMINE OXIDASE INHIBITOR Such as Phenox Ibrotamide, Isovaleryl Diethylamide, Niaprazine, Triceta ypropazine, Pivyalylbenzhydrazine mide, Trimetozine, Zolpidem, Zopiclone, Barbituric Acid MUCOLYTIC such as Acetylcysteine, Bromhexine, Car Derivatives Such as Allobarbital, Amobarbital, Aprobar bocysteine, Domiodol, Letosteine, Mecysteine, Mesna, 55 bital, Barbital, Bralobarbital, Butabarbital sodium, Butal Sobrerol, Stepronin, Tiopronin, Tyloxapol bital, Butallylonal, Butethal, Carbubarb, Cyclobarbital, MUSCLE RELAXANT (SKELETAL) such as Afloqua Cyclopentobarbital, Enallylpropymal, 5-Ethyl-5-(1-Pip lone, Alcuronium, Atracurium Besylate, Baclofen, Benzo eridyl) Barbituric Acid, 5-Furfuryl-5-isopropylbarbituric quinonium, C-Calebassine, Carisoprodol, Chlorphenesin Acid, Heptabarbital, Hexethal sodium, Hexobarbital, Carbamate, ChlorZoxaZone, Curare, Cyclobenzaprine, dan 60 Mephobarbital, Methitural, Narcobarbital, Nealbarbital, trolene, Decamethonium, Eperisone, Fazadinium, Flumetra Pentobarbital Sodium, Phenallymal, Phenobarbital, Phe mide, Gallamine triethiodide, Hexacarbacholine, Hexafluo nobarbital Sodium, Phenylmethylbarbituric Acid, Probar renium, Idrocilamide, Laudexium Methyl Sulfate, bital, Propallylonal, Proxibarbal, Reposal, Secobarbital Leptodactyline, Memantine, Mephenesin, Metaxalone, Sodium, Talbutal, Tetrabarbital, Vinbarbital Sodium, Vinyl Methocarbamol, Metocurine Iodide, Pancuronium, Pipecu 65 bital rium, Promoxolane, Quinine Sulfate, Styramate. Succinyl Benzodiazepine Derivatives such as Brotizolam, Dox choline. Succinylcholine Suxethonium Bromide, Tet efazepam, Estazolam, Flunitrazepam, Flurozepam, Helox US 7,122,198 B1 19 20 aZolam, Loprazolam, Lorimetazppam, Nitrazepam, The compressed tablets have sufficient mechanical Quazepam, Temazepam, Triazolam strength which allows them to be packed in normal push Bromides such as Ammonium Bromide, Calcium Bro through type blister packages and does not require special mide, Calcium Bromolactobionate, Lithium Bromide, Mag packaging like peel-off blisters. nesium Bromide, Potassium Bromide, Sodium Bromide Carbamates such as Amyl Carbamate(Tertiary), Ethi The manufacturing process is exemplified below: namate, Hexapropymate, Meparfynol carbamate, Novonal, Trichlorourethan EXAMPLE 1. Chloral Derivatives such as Carbocloral, Chloral Betaine, Chloral Formamide, Chloral Hydrate, Chloralantipyrine, 10 Dichloralphenazone, Pentaerythritol Chloral, Triclofos Step 1: Preparation of Non-Sugar Sweetener in Mucoadhe Piperidinediones such as Glutethimide, Methyprylon, sive Form. Piperdione, Pyrithyldione, Taglutimide, Thalidomide Quinazolone Derivatives such as Etaqualone, Mecloqua lone, Methaqualone Others such as Acetal, Acetophenone, 15 Aldol, Ammonium Valerate, Amphenidone, d-Bornyl a-Bro Aspartame 20.00 g moisovalerate, d-Bornyl Isovalerate, Bromoform, Calcium PVM/MA Copolymer (Gantrez AN 169) 0.40 g 2-Ethylbutanoate, Carfinate, C.-Chloralose, Clomethiazole, Cypripedium, doxylamine, Etodroxizine, Etomidate, Fena Acetone 20.00 ml diazole, Homofenazine, Hydrobromic Acid, Mecloxamine, Menthyl Valerate, Opium, Paraldehyde, Perlapine, Propiom azine, Rilmazafone, Sodium Oxybate, Sulfonethylmethane, Dissolve Gantrez, AN 169 in 20 ml Acetone. Granulate Sulfonmethane Aspartame with this solution and dry at 40° C. Sift through THROMBOLYTIC such as APSAC, Plasmin, Pro-Uroki 60 mesh sieve. nase, Streptokinase, Tissue Plasminogen Activator, Uroki 25 aSC Step 2: Tablet Formulation THYROTROPIC HORMONE such as TRH, TSH MISCELLANEOUS. Viatamins, Mineral as well as other Nutrients, Vit B1, B2, B6, B12 and other water soluble NimeSulide (Pharmaceutically active agent) 100.0 mg vitamins, Vitamin C, Vitamin A.D.E and other oil soluble 30 Mannitol 204.5 mg Vitamins, Iron, Zinc and other Miconutrinets and their Aspartame of step 1 in mucoadhesive form 7.0 mg combinations with Vitamins, Antiosidants i.e. Betavarotene Flavour 1.5 mg and combination thereof with Vitamins, Ginseng and other Sodium Starch Glycolate 3.0 mg rejuvenants and Suitable combinations of drugs disclosed Magnesium Stearate 4.0 mg above. 35 The Suitable mucoadhesive agents include cellulose derivatives like methyl cellulose, hydroxypropylmethyl cel Sift all the ingredients through 40 mesh sieve and blend. lulose, hydroxypropyl cellulose, cellulose acetate phthalate, Compress into tablets at a hardness of 1 to 5 Kg. cellulose acetate, cellulose acetate butyrate, cellulose acetate propionate, cellulose acetate trimelliate, cellulose car 40 EXAMPLE 2 boxymethyl ethers and their salts, hydroxypropylmethyl cellulose phthalate, hydroxypropylmethyl cellulose acetate Succinate, polyethylene, polyvinyl acetate (homopolymer), Step 1: Preparation of Non-Sugar Sweetener in Mucoadhe polyvinyl acetate phthalate, propylene glycolalginate, sive Form: PVMI/MA copolymer, PVP/dirnethiconylacrylate/polycar 45 bamyl/polyglycolester, PVP/dimethylaminoethylmethacry late/polycarbamyl polyglycol ester, PVP/polycarbamyl Aspartame 20.00 g polyglycol ester, PVPNA copolymer, gelatin and Gelatin Carbomer (Carbopol 934P) 0.40 g derivatives. Water 20.00 ml Alginates, Carbomers, Polycarbophils. 50 Methacrylic acid copolymers. Carrageenans, pentins, chitosans, cyclodextrins, lecitins. Disperse Carbopol 934P in 20 ml Water. Granulate Aspar Natural gums containing galactomannans like Xanthan tame with it and dry at 40° C. Sift through 60 mesh sieve. gum, Acacia, tragacanth, agar, guar gum and the like. The fast soluble part of the sweetener gives a rapid burst 55 Step 2: Tablet Formulation of the Sweetness whereas the mucoadhesive form binds to the oral mucosa and gives a prolonged Sweet taste thereby effectively masking the bitter or bad after-taste of the NimeSulide (Pharmaceutically active agent) 100.0 mg pharmaceutically active agents. Mannitol 204.5 mg The conventional therapeutically acceptable additives like 60 Aspartame 3.0 mg binding agents, lubricants, disintegrants, flavouring agents, Aspartame of step 1 in mucoadhesive form 4.0 mg Flavour 1.5 mg colouring agents, pH modifiers and wetting agents may be Sodium Starch Glycolate 3.0 mg added to the pharmaceutical composition prepared. Magnesium Stearate 4.0 mg If desired, the active pharmaceutical agent may be first Subjected to the conventional taste neutralization treatment 65 like forming matrix microspheres, microencapsulation, Sift all the ingredients through 40 mesh sieve and blend. complexation and the like. Compress into tablets at a hardness of 1 to 5 Kg. US 7,122,198 B1 21 22 EXAMPLE 3 -continued

Step 1: Taste Neutralization of Drug Substance. % Wiw Povidone O.25 Ibuprofen (Pharmaceutically active agent) 95.95 g Aspartame in mucoadhesive form 6.25 Tribehenin 4.00 g (from step 1 of example 1) Polysorbate 80 0.05 g Magnesium Stearate OSO Water 40.00 ml Aerosil 0.75 Sodium Starch Glycolate 3.75 10 Sodium Chloride 3.00 Heat water to about 50° C.–60° C. Add polysorbate 80 Citric Acid 2.OO and mix. Under stirring add Tribehenin followed by Ibupro Flavour 2.75 fen. A Wet dough will be formed. Cool it to 35° C. Size it through 20 mesh sieve. Dry at about 45° C. till moisture Dissolve Cetirizine dihydrochloride in 20 times of its content is 1 to 3%. Sift through 60 mesh sieve. 15 weight of water. Add Crosslinked Poiyacrylic Acid in small Step 2: Tablet Formulation increments with constant stirring. Adjust pH to 3 with hydrochloric acid. Keep aside for 1 to 6 hours and then Ibuprofen from step 1 200.0 mg decant the water. Wash the sediment with water at least Equivalent to Ibuprofen twice. Dry the sediment at 40 to 50° C. Pass through sieve Xylitol 204.5 mg Aspartame in mucoadhesive form 7.00 mg of mesh no 60 (BSS). Mix with pre-sifted (through mesh no. (from step 1 of example 2) 30BBS) blend of Mannitoi, Croscarmeilose Sodium, Povi Flavour 1.5 mg done, Aspartame (in mucoadhesive form), Magnesium Sodium Starch Glycolate 3.0 mg Megnesium Stearate 4.0 mg Stearate, Aerosil, Sodium Starch Glycolate, Sodium Chlo 25 ride, Citric Acid and Flavour. Compress into tablets using conventional tabletting machine at a hardness of 1-3 kg. Sift all the ingredients through 40 mesh sieve and blend. Compress into tablets at a hardness of 1 to 5 Kg. EXAMPLE 6 EXAMPLE 4 30 Step 1. Preparation of Non-Sugar Sweetener in Mucoadhe sive Form: % ww Cisapride (Pharmaceutically active agent) 2.50 Liquid Paraffin O.25 Saccharin Sodium 100.00 g Sorbitol 84.75 35 Polycarbophil (Noveon AA-1) 4.00 g Sodium Starch Glycolate S.OO Water 10.00 g Croscarmellose Sodium 1.25 Magnesium Stearate 1.25 Aspartame in mucoadhesive form 3.00 Disperse Polycarbophil in Water. Granulate Saccharin (from step 1 of example 1) Sodium with this dispersion. Dry at 50° C. and sift through Colloidal Silicon Dioxide 1.25 40 Flavour 0.75 mesh no. 40 (BSS). Step 2. Pass the drug through mesh no. 60 (BSS) sieve. Granulate the drug with a solution of Liquid Paraffin in Dichlo % Wiw romethane and pass through mesh no. 40(BSS) sieve. Dry at 45 a temperature of 45–50° C. Sift Sorbitol through mesh no. Chloroquine Phosphate (Pharmaceutically active agent) 1O.O Crosslinked Polyacrylic Acid, Potassium salt 2O.O 60(BSS) sieve and mix with drug containing Liquid Paraffin. (Ion-exchange resin) This blend is then granulated with water and then dried at a Hydrochloric Acid q.S. to adjust pH temperature of 50–60° C. The dried granules are sifted Mannitol 51.50 through mesh no. 22(BSS) sieve. 50 Crosscarmellose sodium 3.SO Povidone 1.OO Sift Sodium Starch Glycollate, Magnesium Stearate, Col Saccharin Sodium in mucoadhesive form 2.OO loidal Silicon Dioxide, Crosscarmellose Sodium, Aspartame (from step 1 of example 6) (in mucoadhesive form) and Flavours through mesh no. 30 Magnesium Stearate O.SO (BSS) sieve and mix with the above said bulk. Compress Sodium Starch Glycolate 3.75 55 Sodium Chloride 3.00 into tablets using conventional tabletting machine at a Citric Acid 2.OO hardness of 1–3 Kg. Flavour 2.75 EXAMPLE 5 Dissolve Chloroquine Phosphate in 20 times of its weight 60 of water. Add Crosslinked Polyacrylic Acid in small incre % Wiw ments with constant stirring. Adjust pH to 6 with hydro Cetirizine Dihydrochloride (Pharmaceutically active agent) 2.5 chloric acid. Keep aside for 1 to 6 hours and then decant the Crosslinked Polyacrylic Acid (Ion-exchange resin) 1O.O Hydrochloric Acid q.S. to adjust water. Wash the sediment with water at least twice. Dry the pH sediment at 400 to 50° C. Pass through sieve of mesh no 60 Mannitol 64.5 65 (BSS). Mix with pre-sifted (through mesh no.30 BSS) blend Croscarmellose Sodium 3.75 of Mannitol, Povidone, Saccharin Sodium (in mucoadhesive form), magnesium Stearate, Sodium US 7,122,198 B1 23 24 EXAMPLE 7 The advantages of the present invention are: a. The pharmaceutical tablets prepared according to the Step 1: Taste Neutralization of Drug Substance. present invention dissolve/disperse in the mouth within one minute requiring very little amount of body fluids Ascorbic Acid 96.00 g like saliva to produce a solution or Suspension of the Gelatin 4.00 g drug for oral administration. Water 30.00 ml b. The tablet leaves a prolonged sweet taste in the mouth. c. The unpleasant or bitter taste of the drug is masked Heat water to about 60° C. 70° C. Add Gelatin and without significantly interfering with the dissolution dissolve. Coat the Ascorbic Acid by spraying the gelatin 10 and ultimate bioavailability of the drug present in the solution using fluidized bed coater. Size the coated drug tablet. powder through 40 mesh sieve. d. The process of this invention has low manufacturing cost avoiding the special and costly techniques like Step 2: Mucoadhesive Sweetener. Lyophilization, Spray-drying and the like. 15 Since many apparently different embodiments of the Ammonium Glycirrhizinate 20.00 g present invention could be made without departing from the PVM/MA Copolymer 0.40 g (Gantrez AN 169) spirit and scope thereof, it is intended that the description of Acetone 20.00 ml the invention herein be interpreted as being illustrative only and not limiting in any manner whatsoever. Dissolve Gantrez, AN 169 in 20 ml Acetone. Granulate We claim: Ammonium Glycirrhizinate with this solution and dry at 40° 1. A fast dissolving pharmaceutical composition in Solid C. Sift through 60 mesh sieve. dosage form with a prolonged Sweet taste which consists essentially of: Step 3: Tablet Formulation a) at least one pharmaceutically active agent in an amount 25 of from 0.1 to 99 weight % of the total dosage form: Ascorbic Acid from step 1 b) at least one water soluble Sugar in an amount of from 40 to 95 weight % of the total dosage form: Equivalent to Ascorbic Acid 100.0 mg c) at least one non-Sugar Sweetener in a fast release form Sorbitol 204.5 mg in an amount of from greater than 0 to 10 weight% of Ammonium Glycirrhizinate in Mucoadhesive form 7.00 mg 30 (from step 2) the total dosage form; and Flavour 1.5 mg d) at least one non-Sugar Sweetener in a mucoadhesive Sodium Starch Glycolate 3.0 mg slow release form in an amount of from 0.5 to 20 Magnesium Stearate 4.0 mg weight % of the total dosage form. 2. The composition according to claim 1, wherein the Sift all the ingredients through 40 mesh sieve and blend. 35 water soluble Sugar is selected from the group consisting of Compress into tablets at a hardness of 1 to 5 Kg. mannitol, sorbitol and xylitol. 3. The composition as claimed in claim 1, wherein the EXAMPLE 8 non-Sugar Sweetner is selected from the group consisting of Tablet Formulation isomalt, aspartame, acesulfame potassium, saccharine 40 Sodium, cyclamates, neohesperidine and glycirrhizin. Interferon (Alpha) equivalent to 18 Million I.U. 4. A process for the preparation of a fast dissolving Mannitol 204.5 mg pharmaceutical composition according to claim 1, which Aspartame in mucoadhesive form 7.0 mg consists essentially of mixing the following ingredients: (from step 1 of example 1) Flavour 1.5 mg 45 a) at least one pharmaceutically active agent in an amount Sodium Starch Glycolate 3.0 mg of from 0.1 to 99 weight % of the total dosage form: Magnesium Stearate 4.0 mg b) at least one water soluble Sugar in an amount of from 40 to 95 weight % of the total dosage form: Sift all the ingredients through 40 mesh sieve and blend. c) at least one non-Sugar Sweetener in a fast release form 50 in an amount of from greater than 0 to 10 weight% of Compress into tablets at a hardness of 1 to 3 Kg. the total dosage form; and EXAMPLE 9 d) at least one non-Sugar Sweetener in a mucoadhesive slow release form in an amount of from 0.5 to 20 Alprazolam 1 mg weight % of the total dosage form; Isomalt 98.9 mg 55 and compressing the resulting mixture into the a solid Aspartame 0.03 mg dosage form. Acesulfame potassium 0.03 mg Neohesperidine in 0.04 mg 5. The process according to claim 4 wherein the solid Mucoadhesive form dosage form is a tablet. 6. The process according to claim 4, wherein the water 60 soluble Sugar is selected from the group consisting of Procedure mannitol, sorbitol and xylitol. Prepare the non-Sugar Sweetener neohesperidine in 7. The process as claimed in claim 4, wherein the non mucoadhesive form similar to as mentioned in the process Sugar Sweetner is selected from the group consisting of for preparation of the non-Sugar Sweetener aspartame in said isomalt, aspartame, acesulfame potassium, saccharine form (from step 1 of example 1). Sift all the ingredients 65 Sodium, cyclamates, neohesperidine and glycirrhizin. through 30 mesh sieve and blend. Compress into tablets at a hardness of 1 to 3 Kg.