Title of Invention

"FAST DISSOLVING PHARMACEUTICAL COMPOSITIONS IN SOLID FORM WITH PROLONGED SWEET TASTE AND A PROCESS FOR THE MANUFACTURE THEREOF "

Abstract A novel fast dissolving pharmaceutical composition in solid dosage form with a prolonged sweet taste is provided which comprises at least one pharmaceutical active agent in an amount of from 0.1 to 99 weight % of the total dosage form; at least one water soluble sugar in an amount of from 5 to 95 weight % of the total dosage form; at least one non-sugar sweetener in a fast release form in an amount of from greater than 0 to 10 weight % of the total dosage form; and at least one non-sugar sweetener in a mucoadhesive slow release form in an amount of from 0.5 to 20 weight % of the total dosage form. Also provided is the process of manufacture of such novel compositions.
Full Text The present invention relates to a novel composition of a Fast dissolving pharmaceutical preparation in solid dosage form with prolonged sweet taste and a process for the manufacture thereof.
Background of the Invention:
Generally, solid pharmaceutical preparation such as tablets/capsules are designed so that after oral administration, they disintegrate or dissolve in the digestive organs and the active ingredients are absorbed. Such compositions are not meant to disintegrate or dissolve in the oral cavity.
However, in certain conditions there is a requirement of fast disintegrating or dissolving tablets which can be administered even without water. Such fast dissolving tablets disperse readily to form a suspension or solution of the drug after mixing with the saliva, which is easily swallowed by the patients. These are particularly suitable for children or aged patients who have difficulty in chewing and/or swallowing an intact tablet/capsule. Fast mouth dissolving tablets are also suitable for those patients:-
a) Who are suffering from nausea or vomiting;
b) Who have an upper gastrointestinal tract disease e.g., injury in food pipe;
c) Who have undergone upper Gl surgery;
d) Who are prostrate;
e) Who are elderly and have frequent urination problems at night.
f) Who are incapacitated elderly patients e.g. suffering from Parkinson's disease;
g) Who are children;
h) Who are in a situation where water is not available.
All the above conditions necessitate that solid dosage form like tablets and capsules should be modified to accommodate above conditions. Formulating conventional tablets and liquid dosage forms does not solve all the problems stated above. Dispersible tablets still require water and lead to gritty suspensions. Such reconstituted dosage forms as well as ready-made suspensions still cannot be given in all above conditions and additionally they pose problems of uniformity of doses and stability of the drug.
In the past, techniques have been reported for producing such fast dissolving tablets, but most of them require the use of highly specialized manufacturing processes or specialized packaging. The Zydis technology from R.P. Scherer, England or instance, utilizes freeze-drying of active ingredient with polymer, sugar and other ingredients to form a fast dissolving dosage form. (Manuf. Chemist. Feb., 1990). European Patent Application No. EP 0 839 526 A2 describes the use of a high cost excipient i.e. erythritol in combination with an active ingredient, crystalline Cellulose and disintegrants to prepare fast disintegrating buccal tablets. U.S. Patent No. 5,073,374 discloses a fast dissolving buccal tablet containing an active ingredient, a water soluble sugar such as sorbitol and a lubricant. U.S.Patent No.5,085,876 discloses a surprisingly fast dissolving sweetening agent in combination with caramel.
US Patent No. 5,466,464 discloses a solid preparation soluble in buccal cavity containing agar in combination with sugars like lactose and/or mannitol and an active ingredient. The drawback in this preparation is that agar is a natural material susceptible to variability and microbial contamination.
The composition described in U.S. Patent No. 5,720,974 requires a special "Compression-Molding" process to produce fast dissolving tablet. U.S. Patent No. 5,837,285 discloses fast soluble tablets which are produced by a novel process which involves the compression shaping of a wet kneaded mass of drug and sugar alcohol. The wet tablets produced are thereafter dried.
Another US Patent No. 5,869,098 discloses fast dissolving compressed tablets manufacturing by using partially hygroscopic shearform matrices. Such matrices are prepared from sugar carriers using a flash-heat process. Further U.S. Patent No. 5,112,616 discloses the use of solid selected from polyethylene glycols and glycerides, wherein glycerides melt in the range of 25°C to 45°C surfactants selected from the groups consisting of nonionic Poly (oxypropylene) Poly (oxethylene) copolymers, polyoxyethylene polysorbate derivatives and sodium lauryl sulfate to prepare fast dissolving buccal tablets.
PCT Application Number WO 93/23017 defines a fast dissolving matrix consisting of gelatin, pectin and/or soy fiber protein and one or more amino acids having from 2 to 12 carbon atoms.
All the compositions disclosed in the prior art suffer from the drawback of a bitter taste in the mouth after consumption and also do not provide for a prolonged sweet taste in oral cavity after consumption of such fast dissolving compositions.
It is the object of the present invention to provide a pharmaceutical preparation in solid dosage form, preferably in the form of a compressed tablet which when orally administered dissolves or disperses in the mouth within one minute requiring very little amount of body fluids like saliva to produce a smooth solution or suspension of the drug with a prolonged sweet taste.
Accordingly the present invention relates to a novel fast dissolving pharmaceutical composition in solid dosage form with a prolonged sweet taste which comprises:
a) At least one pharmaceutical active agent from 0.1 to 99 weight %
b) At least one water soluble sugar, such as herein described, in an amount of from
5 to 95 weight % of the total dosage form;
c) At least one non-sugar sweetener, such as herein described, in their normal fast
release form in an amount of from 0 to 10 weight % of the total dosage form; and
d) At least one non-sugar sweetener, such as herein described, in a mucoadhesive
slow release form obtained as herein described in an amount of from 0.5 to 20
weight % of the total dosage form.
The present invention also relates to a process for the preparation of a novel fast dissolving pharmaceutical composition is solid dosage form with prolonged sweet taste which comprises mixing the following ingredients:
a) At least one pharmaceutically active agent from 0.1 to 99 weight %
b) At least one water soluble sugar, such as herein described, in an amount of form 5
to 95 weight % of the total dosage form;
c) At least one non-sugar sweetener, such as herein described, in their normal fast
release form in an amount of from 0 to 10 weight % of the total dosage form; and
d) At least one non-sugar sweetener, such as herein described, in a mucoadhesive
slow release form obtained as herein described in an amount of from 0.5 to 20
weight % of total dosage form;
and compressing the resulting mixture obtained into tablets or any other solid dosage form.
The water soluble sugars which can be used in the process according to the present invention are Mannitol, Sorbitol, Xylitol and the like.
The non-sugar sweeteners which can be used in the process according to the present invention are Aspartame, Acesulfame potassium, Saccharin sodium, Cyclamates, Glycirrhizin and the like.
The non-sugar sweetener in a mucoadhesive slow release form is obtained by mixing, coating, granulating, encapsulation, matrix formulation or complexation of a non-sugar sweetener with a mucoadhesive agent as stated herein.
The drugs/pharmaceutical agents or their salts to be employed for the fast dissolving buccal tablet in accordance with the present invention can be selected from the following group of drugs-
a- ADRENERGIC AGONIST such as Adrafinil, Adrenolone, Amidephrine, Apraclonidine, Budralazine, Clonidine, Cyclopentamine, Detomidine,
Dimetofrine, Dipivefrin, Ephedrine, Epinephrine, Fenoxazoline.Guanbenz, Guanafacine, Hydroxyamphetamine, Ibopamine, Indanazoline, Isomethepten, Mephentermine, Metaraminol, Methoxamine, Methylhexaneamine, Metizolene, Midodrine, Naphazoline, Norepinephrine, Norfenefrine, Octodrine, Octopamine, Oxymetazoline, Phenylephrine, Phenylpropanolamine, Phenylpropymethylamine, Pholedrine, Propylhexedrine, Pseudoephredrine, Rilmenedine, Synephrine, Tetrahydrozoline, Tiamenidine, Tramazoline, Tuaminoheptane, Tymazoline, Tyramine, Xylometazoline.
ß-ADRENERGIC AGONIST such as Formoterol, Methoxyphenamine, Ritodrine, Terbuterol.
α-ARENERGIC BLOKER such as Dapiprazole, Doxazosin, Ergoloid, Mesylates, Fenspiride, Parazosin, Tarazosin, Tolazoline, Yohimbine
α-ADRENERGIC BLOCKER such as Acebutolol, Amosulalol, Arotinolol, Atenolol, Befunolol, Betaxolol, Bevantolol, Bisoprolol, Bopindolol, Bucumolol, Bufetolol, Buforalol, Bunitrolol, Bupranolol, Butofilolol, Carazolol, Carteolol, Carvedilol, Celiprolol, Cetamolol, Cloranolol, Dilevalol, Epanolol, Esmolol, Indenolol, Labetalol, Levobunolol, Mepindolol, Metipranolo, Metoprolol, Moprolol, Nadolol, Nadoxolol, Nifenalol, Nipradilol, Oxprenolol, Penbutolol, Pindolol, Practolol, Propranolol, Sotalol, Sulfinalol, Talinolol, Tertatolol, Timolol, Toliprolol, Xibenolol
ALCOHOL DETERRENT such as calcium cyanamide citrated, Disulfiram, Nitrefazole
ALDOSE REDUCTASE INHIBITOR such as Epalrestat, Ponalrestat, Sorbinil, Tolrestat
ANABOLIC such as Androisoxazole, Androstenediol, Bolandiol, Bolasterone, Clostebol, Ethylestrenol, Formyldienolone, 4-Hydroxy-19-nortestosterone, Methandriol, Methenolone, Methyltrienolone, Nandrolone Decanoate, Nandrolone-Hexyloxyphenyl-propionate, Nandrolone Phenpropionate, Norbolethone, Oxymesterone, Quinbolone, Stenbolone, Trenbolone, ANALGESIC (DENTAL) such as Chlorobutanol, Clove, Eugenol, Potassium Nitrate, Potassium Oxalate
ANALGESIC (NARCOTIC) such as Alfentanil, Allylprodine, Alphaprodine, Anileridine, Benzylmorphine, Bezitramide, Buprenorphine, Butorphanol, Clonitazene, Codeines, Desomorphine, Dextromoramide, Dezocine, Diampromide, Dihydrocodeine, Dihydrocodeineone Enol Acetate, Dihydromorphine, Dimenoxadole, Dimepheptanol, Dimethylthiambutene, Dioxaphetyl Butyrate, Dipipanone, Eptazocine, Ethoheptazine, Ethylmethlythiambutene, Ethylmorphine, Etonitazine, Fentanyl, Hydrocodone, Hydromorphone, Hydroxypethidine, Isomethadone, Ketobemidone, Levorphanol, Lofentanil, Meperidine, Meptazinol, Metazocine, Methadone, Metopon, Morphine, Morphine Derivatives, Myrophine, Nalbuphine, Narceine, Nicomorphine, Norlevorphanol, Normethadone, Normorphine, Norpipanone, Opium,Oxycodone Oxymorphone, Papaveretum, Pentazocine, Phenadoxone, Phenazocine, Pheoperidine, Piminodine, Piritramide, Proheptazine, Promedol, Properidine, Propiram, Propoxyphene, Sufentanil, Tilidine.
ANALGESIC (NON-NARCOTIC) such as Acetaminophene, Acetaminosalol, Acetanilide, Acetylsalicylates, Acetylsalicylsalicylic Acid, Alclofenac,
Alminoprofen, Aloxiprin, Aluminium Bis(acetylsalicylate), Aminochlorthenoxazine, 2-Amino-4-picoline, Aminopropylon, Aminopyrin, Antipyrine, Antipyrine Salicylate, Antrafenine, Apazone, Aspirin, Benorylate, Benoxaprofen, Benzpiperylon, Benzydamine, p-Bromoacetanilide, 5-Bromosalicylic Acid Acetate, Bufexamac, Bucetin, Bumadizone, Butacetin, Carbamazepine, Carbetidine, Carbiphene, Carsalam, Chloralantipyrine, Chlorthenoxazin(e), Cholin
Salicylate, Cinchophene, Ciramadol, Clometacin, Cropropamide, Crotethamide, Dexoxadrol, Difenamizole, Diflunisal, Dipyrocetyl, Dipyrone, Emorfazone, Enfenamic Acid, Epirizole, Etersalate, Ethenzamide, Ethoxazene, Etodolac, Felbinac, Fenoprofen, Floctafenine, Flufenamic Acid, Fluoresone, Flupirtine, Fluproquazone, Flurbiprofen, Fosfosal, Gentisic Acid, Glafenine, Ibufenac, Imidazole Salicylate, Indomethacin, Indoprofen, Isofezolac, Isoladole, Isonixine, Ketoprofen, Ketorolac, p-Lactophenetide, Lefetamine, Loxoprofen, Lysine Acetylsalicylate, Methotrimeprazine, Metofoline, Miroprofen, Moraone, Morpholine Salicylate, Naproxen, Nefopam, Nifenazone, 5' Nitro-2' Propoxyacetanilide, Parsalmide, Perisoxal, Phenacetin, Phenazopyridine, Phenocoll, Phenopyrazone, Phenyl Acetylsalicylate, Phenyl salicylate, Phenyramidol, Pipebuzone, Piperylone, Prodilidine, Propacetamol, propyphenazone, Proxazole, Quinine Salicylate, Ramifenazone, Rimazolium, Metilsulfate, Salacetamide, salicin, Salicylamide, O-Acetic Acid, Salicylic Acid, Salicylates and derivatives, Salicylsulfuric Acid, Salsalte, Salverine, Simetride, Sulfamipyrine, Suprofen, Talniflumate, Tenoxicam, Terofenamate, Tetradrine, Tinoridine, Tolfenamic Acid, Tolpronine, Tramadol, Viminol, Xenbucin, Zomepirac
ANDROZEN such as Boldenone, Fluoxymesterone, Mestanolone, Mesterolone, Methandrostenolone, 17-Methyitestoserone, 17α -Methyl-testosterone 3-cyclopentyl Enol Ether, Norethandrolone, Normethandrone, Oxandrolone, Oxymetholone, Prasterone, Stanlolone, Stanozolol, Testosterone, Testosterone 17- Chloral Hemiacetal, Testosterone 17-pcypionate, Testosterone Enanthate,
Testosterone Nicotinate, Testosterone Phenylnylacetate, Testosterone Propionate, Tiomesterone,
ANESTHETIC such as Acetamidoeugenol, Alfadolone Acetate, Alfaxalone, Amucaine, Amolanone, Amylocaine, Benoxinate, Betoxycaine, Biphenamine, Bupivacaine, Burethamine, Butacaine, Butaben, Butanilicaine, Buthalital, Butoxycaine, Carticaine, 2-Chloroprocaine, Cocaethylene, Cocaine, Cyclomethycaine, Cocaethylene, Dibucaine, Dimethisoquin, Dimethocaine, Diperadone, Dyclonine, Ecgonidine, Ecgonine, Ethyl Aminobenzoate, Ethyl Chloride, Etidocaine, Etoxadrol, ß-Eucaine, Euprocin, Fenalcomine, Femocaine, Hexobarbital, Hexylcaine, Hydroxydione, Hydroxyprocaine, Hydroxytetracaine, Isobutyl p- Aminobenzoate, Kentamine, Leucinocaine Mesylate, Levoxadrol, Lidocaine, Mepivacaine, Meprylcaine, Metabutoxycaine, Methohexital, Methyl Chloride, Midazolam, Myrtecaine, Naepaine, Octacaine, Orthocaine, Oxethazaine, Parethoxycaine, Phenacaine, Phencylidine, Phenol, Piperocaine, Piridocaine, Polidocanol, Pramoxine, Prilocaine, Procaine, Propanidid, Propanocaine, Proparacaine, Propipocaine, Propofol, Propoxycaine, Psedococaine, Pyrocaine, Risocaine, Salicyl Alcohol, Tetracaine, Thialbarbital, Thimylal, Thiobutabarbital, Thiopental, Tolycaine, Trimecaine, Zolamine.
ANOREXIC such as Aminorex, Amphecloral, Benzaphetamine, Chlorphentermine, Clobenzorax, Chloforex, Cyclexedrine, Diphemethoxidine, Fenbutrazate, Fenfluramine, Fenproporex, Furfurylmethylamphetamine, Levophacetoperate, Mefenorex, Metamfeproamone, Norpseudoephedrine, Phenpetermine, Picilorex ANTHELMINTIC (CESTODES) such as Arecoline, Aspidine, Aspidinol, Dichlorophen(e), Embelin, Kosin, Napthalene, Niclosamide, Pellertierine, Pellertierine Tannate, Quinacrine.
ANTHELMINTIC (NEMATODES) such as Alantolactone, Amoscanate, Ascaridole, Bephenium, Bitoscanate, Carbon Tetrachloride, Carvacrol, Cyclobendazole, Diethylcarbamazine, Diphenane, Dithiazanine Iodide,
Dymanthine, Gentian Violet, 4-Hexylresorcinol, Kainic Acid, Mebendazole, 2-Napthol, Oxantel, Piperazines, Pyrantel, Pyrvinium Pamoate, a -Santonin, Stilbazium Iodide, Tetrachloroethylene, Thiabendazole, Thymol, Thymyl Nsoamylcarbamate,Trichlofenol Piperazine, Urea Stibamine,
ANTHELMINTIC (ONCHOCERCA) such as Ivermectin
ANTHELMINTIC (SCHISTOSOMA) such as Amphotalide, Antimony(s) and Derivatives, Becanthone, Hycanthone, Lucanthone, Niridazole, Oxamniquine, Praziquantel, Stibocaptate, Stibophen
ANTHELMINTIC (TREMATODES) such as Anthiolimine
ANTIACNE such as Algestone, Acetophenide, Azelaic Acid, Benzoyl Peroxide, Dichloroacetic acid, Motretinide, Retinoic Acid, Tetroquinone
ANTIALLERGIC such as Amlexanox, Astimizole, Azelastine, Cromolyn, Fenpiprane, Histamines, Ketotifen, Nedocromil, Oxatomide, Pentigetide, Poison Ivy Extract, Poison Oak Extract, Poison Sumac Extract, Repirinast, Tiaramide, Tranilast, Traxanox, Urushiol, Cetirizine, Fexophenadine.
ANTIAMEBIC such as Arsthinol, Bialamicol, Carbarsone, Cephaeline, Chlorbetamide, Chlorphenoxamide, Dehydroemetine, Dibromopropamidine, Diloxanide, Dephetarsone, Emetine, Fumagillin, Glaucarubin, Glycobiarsol, 8-Hydroxy-7-iodo-5-quinolinesulfonic Acid, lodochlorhydroxyquin, lodoquinol, Paromomycin, Phanquinone, Phearsone Sulfoxylate, Polybenzarsol, Propamidine, Quinfamide, Secnidazole, Sulfarside, Techlozan, Thiocarbamizine, Thiocarbasone, Tinidazole
ANTIANDROGEN such as Bifluranol, Cyoctol, Cyproterone, Oxendolone
ANTIANGINAL such as Amlodipine, Amyl Nitrate, Cinepazet Maleate, Imolamine, Isosorbide Dinitrate, Limaprost, Molsidomine, Nitroxyalklamide Derivatives
ANTIARRHYTHMIC such as Acecaine, Adenosine, Ajmaline, Alprenolol, s-Aminoalkyl-s-Arylsulfoximines, Amoproxan, Aprindine, Bretylium Tosylate, Bubumolol, Bunaftine, Butidrine, Butobendine, Capobenic Acid, Cifenline, Disopyramide, Encainide, Flecainide, Hydroquinidine, Indecainide, Ipratopium, Lorajmine, Lorcainide, Meobentine, Mexiletine, Moricizine, Pirmenol, Prajmaline, Procainamide, Pronethalol, Propafenone, Pyrinoline, Quinidine, Quinidine Sulfate, Quinidine, Tocainide, Viquidil.
ANTIARTERIOSCLEROTIC such as Pyridinol Carbamate
ANTIARTHRITIC/ANTIRHEUMATIC such as Allocupreide Sodium, Auranofin, Aurothioglucose, Aurothioglycanide, Azathioprine, Di-tert-Butyl-phenols, Calcium 3-Aurothio-2-propanol-1-sulfonate, Clobuzarit, Cuproxoline, Diacerein, Glucosamine, Gold Sodium TThiosulfate, Hydroxychloroquine, Kebuzone, Lobenzarit, Melittin, Myoral, Penicillamine
ANTIBACTERIAL (ANTIBIOTIC)
Aminoglycosides such as Amikacin, Apramycin, Arbekacin, Bambermycins, Butirosin, Dibekacin, Dihdrostreptomycin, Fortimicin(s), Fradiomycin, Gentamicin, Ispamicin, Kanamycin, Micronomicin, Neomycin, Neomycin Undecylenate, Netilmicin, Paromomycin, Ribostamycin, Sisomycin, Spectinomycin, Streptomycin, Streptonicozid, Tobramycin
Amphenicols such as Azidamfenicol, Chloramphenicol, Chloramphenicol Palmirate, Chloramphenicol Pantothenate, Florfenicol, Thiamphenicol,
Ansamycins such as Rifamide, Rifampin, Rifamycin, Rifaximin, Rifapentene
ß-Lactams
Carbapenems such as Imipenem
Cephalosporins, such as l-Carba(dethia) Cephalosporin, Cefactor, Cefadroxil, Cephalosporins, Cefatrizine, Cefazedone, Cefazolin, Cefexime, Cefmenoxime, Cefodizime, Cefonicid, Cefoperazone, Ceforanide, Cefotaxime, Cefotiam, Cefmizole, Cefpirimide, Cefpodoxime Proxetil, Cefroxadine, Cefsulodin, Ceftazidime, Cefteram, Ceftezole, Ceftibuten, Ceftizoxime, Ceftriaxone, Cefuroxime, Cefuzonam, Cephacetrile, Sodium, Cephalexin, Cephaloglycin, Cephaloridine, Cephalosporin, Cephalothin, Cephapirin Sodium, Cephradine, Pivcefalexine Cephamycin such as Cefbuperazone, Cefmetazole, Cefminox, Cefetan, Cefoxitin
Manobactams such as Aztreonam, carumonam, Tigemonam Oxacephems such as Flomoxef, Moxolactam
Penicillins such as Amidinocillin, Amdinocillin, Pivoxil, Amoxicillin, Ampicillan, Apalcillin, Aspoxicillin, Azidocillan, Azlocillan, Bacampicillin, Benzylpenicillinic Acid, Benzylpenicillin, Carbenicillin, Carfecillin, Carindacillin, Clometocillin, Cloxacillin, Cyclacillin, Dicloxacillin, Diphenicillin, Epicillin, Fenbenicillin, Floxicillin, Hetacillin, Lenampicillin, Metampicillin, Methicillin, Mezlocillin, Nafcillin, Oxacillin, Penamecillin, Penethamate Hydriodide, Penicillin G Benethamine, Penicillin G Benzathine, Penicillin G Benzhydrylamine, Penicillin G Calcium, Penicillin G Hydrabamine, Penicillin G Potassium, Penicillin G Procaine, Penicillin N, Penicillin O, Penicillin v, Penicillin V Benzathine, Penicillin V Hydrabamine, Penimepicycline, Phenethicillin , Piperacillin , Pivapicillin , Propicillin , Quinacillin, Sulbenicillin, Talampicillin, Temocillin, Ticarcillin Lincosamides such as clindamycin, Lincomycin
Macrolides such as Azithromycin, Carbomycin, Clarithromycin, Erythromycin(s) and Derivatives, Josamycin, Leucomycins, Midecamycins, Miokamycin,
Oleandomycin, Primycin, Rosaramicin, Roxithromycin, Spiramycin, Troleandomycin,
Polypeptides such as Amphomycin, Bacitracin, Capreomycin, Colistin, Enduracidin, Enviomycin, Fusafungine, Gramicidin(s), Gramicidin S, Mikamycin, Polymyxin, Polymyxin B-Methanesulfonic, Acid, Pritinamycin, Ristocetin, Teicoplanin, Thiostrepton, Tuberactinomycin, Tyrocidine, Tyrothricin, Vancomycin, Vimomycin(s), Virginiamycin, Zinc Bacitracin
Tetracyclines such as Apicycline, Chlortetracycline, Clomocycline, Demeclocycline, Guamecycline, Lymecycline, Meclocycline, Methacycline, Minocycline, Oxytetracycline, Penimepicycline, Pipacycline, Rolitetracycline, Sancycline, Senociclin, Tetracycline
Others Such as Cycloserine, Mupirocin, Tuberin
ANTIBACTERIAL (SYNTHETIC)
2,4-Diaminopyrimidines such as Brodimoprim, Tetroxoprim, Trimethoprim
Nitrofurans such as Furaltadone, Furazolium, Nifuradene, Nifuratel, Nifurfoline, Nifurpirinol, Nifurprazine, Nifurtoinol, Nitrofurantoin
Quinolones and Analogs such as Amifloxacin, Cinoxacin, Ciprofloxacin, Difloxacin, Enoxacin, Fleroxacin, Flumequine, Lomefloxacin, Miloxacin, Nalidixic Acid, Norfloxacin, Ofloxacin, Oxolinic Acid, Pefloxacin, Pipemidic Acid, Piromidic Acid, Rosoxacin, Temafloxacin
Sulfonamides such as Acetyl Sulfamethoxypyrazine, Acetyl Sulfisoxazole,
Azosulfamide, Benzylsulfamide, Chloramine-B, Chloramine-T, DichloramineT,
Formosulfathiazole, N2-Formyl-Sulfisomidine, N4-ß-D-Glucosysulfanilamide,
Mafenide, 4'-(Methyl-sulfamoyl) sulfanilanilide, p-Nitrosulfathiazole,
Noprysulfamide, Phthalysulfacetamide, Phthalysulfathiazole,
Salazosufadimidine, Succinylsulfathiazole, Sulfabenzamide, Sulfacetamide,
Sulfachlorpyridazine, Sulfachrysoidine, Sulfacytine, Sulfadiazine, Sulfadicramide,
Sulfadimethoxine, Sulfadoxine, Sulfaethidole, Sulfaguanidine, Sulfaguanol,
sulfalene, Sulfaloxic Acid, Sulfamerazine, Sulfameter,
Sulfamethazine.Sulfamethizole, Sulfamethomidine, Sulfamethoxazole, Sulfamethoxypyridazine, Sulfametrole, Sulfamidochrysoidine, Sulfamoxole, Sulfanilamide, Sulfanilamidomethanesulfonic Acid, Triethnolamine Salt, 4-Sulfanilamidosalycylic Acid, N4-SulfanilySulfanilamide, Sulfanilyurea, N-Sulfanilyl-3,4-xylamide, Sulfanitran, Sulfaperine, Sulfaphenazole, Sulfaproxyline, Sulfapyrazine, Sulfapiridine, Sulfasomizole, Sulfasymazine, Sulfathiozole, Sulfathiourea, Sulfatolamide, Sulfisomidine, Sulfisoxazole
Sulfones such as Acedapsone, Acediasulfone, Acetosulfone, Dapsone, Diathimosulfone, Glocosulfone, Solasulfone, Succisulfone, Sulfanilic Acid, p-sulfanilylbenzyllamine, p,p'-sulfonyldianiline,-N,N'digalactoside, Sulfoxone, Thiazolesulfone
Others such as Clofoctol, Hexedine, Magainis, Methenamine Anhydromethylene-citrate, Methenamine Hippurate, Methenamine Mandelate, Methenamine Sulfosalicylate, Nitroxoline, Squalamine, Xibornol
ANTICHOLINERGIC such as Adiphenine, Alverine, Ambutonomium, Aminopentamide, Amixetrine, Amprotropine Phosphate, Anisotropine, Methylbromide, Apoatropine, Atropine, Atropine N-Oxide, Benactyzine, Benapryzine, Benzetimide, Benzelonium, Benztropine, Mesylate, Bevonium
Methyl Sulfate, Biperiden, Butropium
N-Butylscopolammonium Bromide, Buzepide, Camylofine, Caramiphen,
Chlorbenzoxamine, Chlorphenoxamine, Cimetropium, Clidinium, Cyclodrine,
Cyclonium, Cyclopentolate, Cycrimine, Deptropine, Dexitimide, Dibutoline
sulfate, Dicyclomine, Diethazine, Difemerine, Dihexyverine, Diphemanil,
Methylsulfate, N-(1,2-Dipheylethyl)nicotinamide, Dipiprovrine, Diponium,
Emepronium, Endobenzyline, Ethopropazine, Ethybenztropine,
Ethylbenzhydramine, Etomidoline, Eucatropine, Fenpiverinium, Fentonium, Flutropium, Glycopyrrolate, Heteronium, Hexocyclium Methyl Sulfate,
Homatropine, Homatropine Methyl Bromide, Hyoscyamine, Ipratropium, Isopropamide, Levomepate, Mecloxamine, Mepenzolate, Metcaraphen, Methantheline, Methixene, Methscopolamine, Octamylamine, Oxybutynin, Oxyphencyclimine, Oxyphenonium, Pentapiperide, Penthienate, Phencarbamide, Phenglutarimide, Pipenzolate, Piperidolate, Piperilate, Poldine Methysulfate, Pridinol, Prifinium, Propyromazine, Scopolamine N-Oxide, Stilonium, Stramonium, Sultroponium, Thihexinol, Thiphenamil, Tiemonium, Timepidium, Tiquizium, Tridihexethyl Iodide, Trihexyphenidyl, Hydrochloride, Tropacine, Tropenzile, Tropicamide, Trospium, Valethamate, Xenytropium
ANTICONVULSANT such as Acetylpheneturide, Albutoin, Aloxidone, Aminoglutethimide, 4-Amino-3-hydroxybutyric Acid, Atrolactamide, Beclamide, Buramate, Carbamazepine, Cinromide, Clonazepam, Decimemide, Diethadione, Dimethadione, Doxenitoin, Eterobarb, Ethadione, Ethosuximide, Ethotoin, Fluresone.
5-Hydroxytryptophan, Lamotrigine, Magnesium Sulfate, Mephenytoin, Metharbital, Methetoin, Methsuximide, 5-Methyl-5-(3-phenanthryl)-hydantoin, 3-Methyl-5-phenylhydantoin, Narcobarbital, Nimetazepam, Nitrazepam, Paramethadione, Phenacemide, Pheneturide, Phensuximide, Phenytoin, Phethenylate Sodium, Primidone, Progabide, Solanum, Strontium, Suclofenide, Sulthiame, Tetrantoin, Trimethadione, Valproic Acide, Valpromide, Vigabatrine, Zonisamide.
ANTIDEPRESSANT
Bicyclics such as Binedaline, Caroxazone, Citalopram, Dimethazan, Indalpine, fencamine, Indeloxazine, Nefopam, Nomifensine, Oxitriptan, Oxypertine, Paroxetine, Sertraline, Thiazesim, Trazodone, Zometapine,
Hydrazides/Hydrazines such as Benmoxine, Iproclozide, Iproniazid, Isocarboxazid, Nialamide, Ictamoxine, Phenelzine.
Pyrrolidones such as Continine, Rolicyprine, Rolipram.
Tetracyclics such as Maprotiline, Metralindole, Mianserine, Oxaprotiline.
Tricyclics such as Adinazolam, Amitriptyline, Amitriptylinoxide, Amoxapine, Butriptyline, Clomiparamine, Demexiptiline, desiparamine, Dibenzepin, Dimetracrine, Dothiepin, Doxepin, Fluacizine, Imipramine, Imipramine N-Oxide, Iprindole, Lofepramine, Melitracen, Metapramine, Nortriptyline, Noxiptilin, Opipramol, Propizepine, Protriptyline, Quinupramine, Tianeptine, trimiparamine.
Others such as Benactyzine, Bupropin, Butacetin, Deanol, Deanol Aceglumate, Deanol Acetamidebenzoate, Dioxadrol, etoperidone, Febarbamate, Femoxetine, Fenpentadiol, Fluoxetine, Fluvoxamine, Hematopotphyrin, Hypercinin, Levophacetoperane, Lithium, Medifoxamine, Minaprine, Moclobemide, Oxaflozane, Piberaline, Polycyclic Imides, Prolintane, Pyrisuccideanol, Rubidium, Sulpiride, Sultopride, Teniloxazine, Thozalinone, Tofenacin, Toloxatone, Tranylcypromine, L-Tryptophan, Viloxazine, Zimeldine.
ANTIDIABETIC
Biguanides such as Buformine, Metformin, Phenformin.
Sulfontlurea Derivatives such as Acetohexamide, 1-Butyl-3-metanilylurea, Carbutamide, Chlorpropamide, Glibornuride, Gliclazide, Glipizide, Gliquidone,
Glisoxepid, Glyburide, Glybuthiazol(e), Glybuzole, Glyhexamide, Glymidine, Glypinamide, Phenbutamide, Tolazamide, Tolbutamide, Tolcyclamide.
Others such as Acarbose, Benzylthiazolldone-2,4-dione, Calcium Mesoxalate, Miglitol.
ANTIDIARRHEAL such as Acetyltannic Acid, albumin Tannate, Alkofanone, Aluminium
Salicylates, Catechin, Difenoxin, diphenoxylate, Lidamidine, Loperamide, Mebiquine, Trillium, Uzarin.
ANTIDIURETIC such as Desmopressin, felypressin, Lypressin, Ornipressin, Oxcinchophen, Terlipressin, Vasopressin.
ANTIESTROGEN such as Delmadione Acetate, Ethamoxytriphetol, Tamoxifen, Toremifene.
ATRIFUNGAL (ANTIBIOTICS)
Polyenes such as Amphotericin-B, Canadicidin, Dermostatin, Filpin, Fungichromin, Hachimycin, Hamycin, Lucensomycin, Mepartricin, Natamycin, Nystatin, Pecilocin, Perimycin.
Others such as Azaserine, Griseofulvin, Oligomycins, Pyrrolnitrin, Siccanin, Tubercidin, Viridin.
ANTIFUNGAL (SYNTHETIC) Allylamines such as Naftifine, Tebinafine.
Imidazoles such as Bifonazole, Butoconazole, Chlordantoin, Chlormidazole, Cloconazole, Clotrimazole, Econazole, Enilconazole, Fenticonazole, Isoconazole, Ketoconazole, Miconazole, Omoconazole, Oxiconazole, Nitrate, Sulconazole, Tioconazole.
Triazoles such as Fluconazole, Itraconazole, Terconazole.
Others such as Acrisorcin, Amorolfine, Biphenamine, Bromosalicylchloranilide, Buclosamide, Chlophenesin, Ciclopirox, Cloxyquin, Coparaffinate, Diamthazole, Dihydrochloride, Exalamide, Flucytosine , Halethazole, Hexetidine, Loflucarbon, Nifuratel, Potassium Iodide, Propionates, Propionic Acid, Pyrithione, Salicylanilide, Sulbentine, Tenonitrozole, Tolciclate, Tolindate, Tolnaftate.Tricetin, Ujothion, Undecylenic Acid
ANTIGLAUCOMA such as Dapiprazoke, Dichlorphenamide, Dipivefrin, Pilocarpine
ANTIGONADOTROPIN such as Danazol, Gestrinone, Paroxypropione ANTIGOUT such as Colchicine, Probenecid, Sulfinpylrazone
Antihistamic Alkylamine Derivatives such as Acrivastine, Bamipine, Brompheniramine, Chlorpheniramine, Dimethindede, Tolpropamine, Triprolidine
Aminoalkyl Ethers such as Bietabautine, Bromodiphenhydramine, Carbinoxamine, Clemastine, Diphenlypyraline, Doxylamine, Embrammine, Medrylamine, Mephenphydramine, p-Methyldiphenhydramine, Orphenadrine, Phenyltoloxamine, Piprinhydrinate, Setasine
Ethylenediamine Derivatives such as Alloclamide, p-Bromtripelennamine, Chloropyramine, Chlorothen, Histapyrrodine, Methafurylene, Methaphenilene, Methapyrilene, Phenbenzamine, Pyrilamine, Talastine, Thenyldiamine, Thozylamine, Tripelennamine, Zolamine
Piperazines such as Cetirizine, Chlorcyclizine, Clocinizine, Hydroxyzine Tricyclies
Phenothiazines such as Ahistan, Etymemazine, Fenethazine, N-Hydroxyethylpromethazine, Isopromethazine, Mequitaz inc, Promethazine, Pyrathiazine, Thiazinamium Methyl Sulfate
Others such as Azatadine, Clobenzepam, Cyproheptadine, Deptropine, Isothipendyl, Loratadine, Prothipendyl
Others such as Antazoline, Cetoxime, Clemizole, Clobenztropine, Diphenazoline, Diphenhydramine, Mebhydroline, Phenindamine, Terfenadine, Tritoqualine
Antihyperlipoproteinemic
Aryloxyalkanoic Acid Derivatives such as Bazafibrate, Binifibrate, Ciprofibrate, Clinofibrate, Clofibrate, Clofibric Acid, Etonfibrate, Fenofibrate, Gemfibrozil, Nicofibrate, Pirifibrate, Ronifibrate, Simfibrate, Theofibrate
Bile Acid Sequesterants such as Cholestyramine Resin, Colestipol, Polidexide HMG CoA Reductass Inhibitors such as Lovastatin, Pravastatin, Simvastatin
Nicotinic Acid Derivatives Aluminium Nicotinate, Acipimox, Niceritol, Nicoclonate, Nicomol, Oxiniacic Acid
Thyroid Hormones/Analogs such as Etiroxate, thyropropic Acid
Others such as Acifran, Azacosterol, Benfluorec, (3-Benzalbutyramide, Benzodioxole, Carnitine, Chondroitin Sulfate, Clomestone, Detaxtran, Dextran Sulfate Sodium, 5,8,11,14,17-Eicosapentaenoic Acid, Eritadenine, Farnesylated tetrahydro-naphthalenols, Furazbol, Meglutol, Melinamide, Mytatrienediol, Naphtyl- tetrahydronaphtyl - diphosphonates, Ornithine, y-Oryzanol, Pentethine,
Penataerythritol, Tetraacetate, a-Phenylbutyramide, Phylate Acids and Salts, Pirozadil, Probucol, a-Siosterol, Sultosilic Acid, Tiadenol, Triparanol
ANTIHYPERTENSIVE
Benzothiadiazine Derivatives sich as Althiazide, Bendroflumethiazide, Benzthiazide, Benzylhydrochlorothiazide, Buthiazide, Chlorothiazide, Chlorthalidone, Cyclopenthiazide, Cyclothiazide, Diazoxide, Epithiazide, Ethiazide, Fenquizone, Hydrochlorothiazide, Hydroflumethiazide, Methyclothiazide, Meticrane, Metolazone, Paraflutizide, Polythiazide, Tetrachlormethiazide, Trichlormethiazide
N-Carboxyalkyl (peptide/lactam) Derivatives such as Alacepril, Captopril, Cilazapril, Enalapril, Enalaprilat, Fosinopril, Lisinopril, Moveltipril, Perindopril, Quinapril, Ramipril
Guanidine Derivatives Bethanidine, Debrisoquin, Gyanacline, Guanadrel, Guanazodine, Guancthidine, Guanochlor, Guanoxabenz, Guanoxan
Hydrazines/Ohthalazines such as Cadralazine, Dihydralazine, Endralazine, Hydracarbazine, Hydralazine, Pheniprazine, Pildralazine, Todralazine
Imuidazole Derivatives such as Lofexidine, Phentolamine, Tolonidine
Quanternary Ammonium Compounds Azamethonium Chlorisondamine, Hexamethonium, Pentacynium, Bis(methylsulfate), Pentamethonium, Pentolinium Tartate, Phenactopinium, Trimethidiunum Methosulfate
Quinazoline Derivatives such as Alfuzosin, Bunazosin
Reserpine Derivatives such as Bietaserpine, Deserpidine, Rescinnamine, Reserpine, Syrosingopine
Sulfanoamide Derivatives such as Ambuside, Clopamide, Furosemide, Indapamide, Quinethazone, Tripamide, Xipamide
Others such as Aimaline, g-Aminobutyric Acid, Bufeniode, Chlorthalidone, Cicletaine, Ciclosidomine, Cryptenamine Tannates, Flosequinan, Indoramin, Ketanserin, Metbutamate, Mecamylamine, Methyldopa, Methyl 4-Pyridyl Ketone Thiosemicarbarzone, Metolazone, Minoxidil, Muzolimine, Pargyline Glycine Aminopropargyl Diols, Protoveratrines, Raubasine, Rescumetol, Saralasin, Sodium Nitroprusside, Ticrynafen, Trimethaphan Camsylate, Tyrosinase, Urapidil
ANTIHYPERTHYROID such as 2-Amino-4-methyl-thiazole, 2-Aminothiazole, Carbimazole, 3,5-Dibromo-L-tyrosine, 3,5-Diiodotyrosine, Hinderin, Iodine, lothiouracil, Methimazole, Methylthiouracil, Propylthiouracil, Sodium Perchlorate, Thibenzazoline, Thiobarbital, 2-Thiouracil
ANTIHYPOTENSIVE such as Amezinium Methyl Sulfate, Angiotensin Amide, Etifelmin, Etilefrin, Gepefrine
ANTIHYPOTHYROID such as Levothyroxine, Liothyronine, Thyroid, Thyroidin, Thyroxine, Tiratricol
ANTI-INFLAMMATORY (NONSTEROIDAL)
Aminoarylcarboxylic Acid Derivatives such as Etofenamate, Meclofenamic Acid, MefanamicAcid, NiflumicAcid
Arylacetic Acid Derivatives such as Acemetacin, Amfenac, Cinmetacin, Clopirac, Diclofenac, Fenclofenac, Fenclorac, Fenclozic Acid, Fentiazac, Glucametacin,
Isoxepac, Lonazolac, Metiazinic Acid, Oxametacine, Proglumetacin, Sulindac, Tiaramide, Tolmetin
Arylbutyric Acid Derivatives such as Butibufen, Fenbufen Arylcarboxylic Acids such as Clidanac, Ketorolac, Tinoradine
Arylpropionic Acid Derivatives such as Bucloxic Acid, Carprofen, Fenoprofen, Flunosaprofen, Ibuprofen, Ibuproxam, Oxaprozin, Piketoprofen, Pirprofen, Pranoprofen, Protizinic Acid, Tiaprofenic Acid
Pyrazoles such as Mepirizole
Pyrazolones such as Clofezone, Feprazone, Mofebutazone, Oxyphenbutazone, Phenylbutazone, Phenyl Pyrazolidininones, Suxibuzone, Thiazolinobutazone
Salicylic Acid Derivatives such as Bromosaligenin, Fendosal, Glycol Salicylate, Mesalamine, 1-Naphthyl Salicylate, Olsalazine, Sulfasalazine
Thiazinecarboxamides such as Droxicam, Isoxicam, Piroxicam
Others such as e-Acetanidocaproic Acid, S-Adenosylmethionine, 3-Amino-4-hydroxybutyric Acid, Amixetrine, Bendazac, Bucolome, Carbazones, Difenpiramide, Ditazol, Guaiazulene, Heterocyclic Aminoalkyl Esters of Mycophenolic Acid and Derivatives, Nabumetone, Nimesulide, Orgotein, Oxaceprol, Oxazole Derivatives Paranyline, Pifoxime, 2-substituted-4, 6-di-tertiary-butyl-s-hydroxy-1,3-pyromidines, Proquazone, Sialyl Lewisx Dimers, Tenidap
ANTI MALARIAL such as Acedapsone, Alphaaminoquinolines, 40Aminoquinolines, Amodiaquin, Arteether.Artmether, Artemisinin, Artesunate,
Bebeerine, Chirata, Chlorguanide, Chloroquine, Chloproguanil, Cinchone, Cinchonidine, Cinchonine, Cycloguanil, Euquinine, Gentiopicrin, Halofantrine,
Mefloquine Hydrochloride, 3-Methylarsacetin, Pamaquine, Plasmocid, Primaquine, Pyrimethamine, Quinacrine, Quinine, (Acids, Salts and Derivatives), Quinine Formate, Quinine Gluconate, Quinine Tannate, Quinine Urea Hydrochloride, Quinocide, Quinoform, Quinoline, Sodium Arsenate, Diabasic
ANTIMIGRAINE such as Akpiropride, Dihydrergotamine, Ergocornine, Ergocorninine, Ergocryptine, Ergot, Ergotamine, Flumedroxone Flumedroxone, Acetae, Fonazine, Methysergid(e), Oxetorone, Pizotyline, Sumatriptan
ANTINAUSEANT such as Acetylleucine Monoethanolamine, Bietanautine, Bromopride, Buclizine, Clebopride, Cyclizine, Dimenhydrinate, Diphenidol, Domperidone, Gransetron, Meclizine, Methaltal, Metoclopramide, Metopimazine, Nabilone, Ondansteron, Oxypendyl, Pipamizine, Piprinhydrinate, Scopolamine, Tetrahydrocannabinols, Thiethylperazine, Trimethobenzamide
ANTIMEOPLASTIC
Alkyl agents : Alkyl Sulfonates such as Busylfan, Improsulfan, Piposulfan Aziridines such as Benzodepa, Carboquone, Meturedepa, Uredepa
Ethylenimines and Methylmelamines such as Altretamine, Triethylenemelamine,
Triethylenephosphoramide, Triethylenethiophosphoramide,
Trimethylolomelamine
Nitrogen Mustards such as Chlorambucil, Chlornaphazine, Chclophosphamide, Chclophosphamide, Estramustine, Ifosfamide, Mechlorethamine, Mechlorethamine Oxide Hydrochloride, Melphalan, Novembichin, Phenesterine, Prednimustine, Trofosfamide, Uracil Mustard
Nitrosoureas Carmustine, Chlorozotocin, Fotemustine, Lomustine, Nimustine, Ranimustine
Others such as Dacrabazine, Mannomustine, Mitobronitol, Mitolactol, Pipobroman
Antibiotics such as Aclacinomycins, Actinomycin F1, Anthramycin, Azaserine, Bleomycins, Cactinomycin, Carubicin, Carzinophilin, Chromomycins, Dactinomycin, Daunorubicin. 6-Diazo-5-oxo-L-naroleucine, Doxorubicin, Epirubicin, Mitomycins, Mycophenolic Acid, Nogalamycin, Olivomycins, Peplomycin, Plicamycin, Porfiromycin, Puromycin, Streptonigrin, Streptozocin, Tubercidin, Ubenimex, Zinostatin, Zorubicin
Antimetabolites
Folic Acid Analogs such as Denepterin, Methotrexate, Pteropterin, Trimetrexate Purine Analogs such as Fludarabine, 6-Mercaptopurine, Thiamiprine, Thiguanaine
Pyrimidine Analogs such as Ancitabine, Azacitidine, 6-Azauridine, Carmofur, Cytarabine, Didexyuridines, Doxifluridine, Enocitabine, floxuridine, Fluororacil, Tegafur
Enzymes such as L-Asparaginase, Pulmozyme
Others such as Aceglatone, Aldophophamide Glycoside, Aminolevulinic Acid, Amsacrine, Bestabucil, Bisantrene, Carnoplarin, Deformide, Demecolcine, Diaziquone, Elfornithine, Elliptinium Acetate, Etoglucid, Etoposide, Gallium Nitrate, Hydroxyurea, Interferon-a, Interferon-p, Interferon-y, lnterleukine-2, Lentinan, Lonidamine, Mitoguazone, Mitoxantrone, Mopidamol, Nitracrine, Pentostatin, Phenamet, Pirarubicin, Podophyllinicc Acid, 2-Ethythydrazide, Procarazine, PSK®, Razoxane, Sizofiran, Spirogermanium, Taxol, Teniposide, Tenuazonic Acid, Triaziquone, 2,2',2"-Trichlorotriethylamine, Urethan, Vinblastine, Vincristine, Vindesine
ANTINEOPLASTIC(HORMONAL)
Androgens such as Calusterone, dromistanolone Propionate, Epitiostanol, Mepitiostane, Testolactone Antiadrenals such as Aminoglutethimide, Mitotane, Trilostane
Antiandrogens such as Flutamide, Nilutamide Antiestrogens such as Aromatase Inhibiting 4(5)-lmidazoles ANTINEOPLASTIC ADJUNCT Folic Acid Replenisher such as Frolinic Acid
ANTIPARKINSONIAN such as Amantadine, Benserazide, Bictanaurine, Biperiden, Budipine, Carbidopa, deprenyl, Dexetimide, Diethazine, Droxidopa, Ethopropazine, Ethylbenzhydtamine, Levodopa, Piroheptine, Pridinol, Prodipine, Terguride, Tiapride, Tigloidine
ANTIPHEOCHROMOCYTOMA such as Metyrosine, Phenoxybenzamine ANTIPNEUMOCYSTIS such as Efformithine ANTIPROSTATIC HYPERTROPHY such as Proscar®
ANTIPROTOSOAL(LEISHMANIA) such as Ethylstinamine, Hydroxystibamidine, N- Methylglucamine, Pentamidine, Stilbamidine
ANTIPROTOZOAL(TRICHOMONAS) such as Acearsone, Aminitrozole, Anisomycin, Azanidazole, forminitrazole, Furazolidone, Hzanidazole, Lauroguadine, Metronidazole, Nifuratel, Nimorazole, Silver Picrate, Tenonitrozole
ANTIPROTOZOAL (TRYPANOSOMA) such as Benznidazole, Eflomithine, Melarsoprol, Mifutrimox, Oxophenarsine, Puromycin, Quinapyramine, Suiramin Sodium, Trypan Red, Tryparasmide
ANTIPRURITIC such as Camphor, Cyproheptadine, Dichlorisone, Glycine, Halometasone, 3-Hydroxycamphor, Menthol, Mesulphen, Methdilazine, Phenol, Spirit of camphor, Trimeprazine
ANTIPSORLATIC such as Acitretin, Anthralin, 6-Azauridine, Bergapten(e), Chrysarobin, Eoretinate, Pyrogallol
ANTIPSYCHOTIC
Butyrophenones such as Benperidol, Bromperidol, Droperidol, Fluanisone, Haloperidol, Melperone, Moperone, Pipamperone, Sniperone, Timiperone, Trifulperidol
Phenothiazines such as Acetophenazine, Bhutaperazine, Carphenazine, Chlorproethiazine, Chlorpromazine, Clospirazine, Mepazine, Mesoridazine, Methoxypromazine, Metofenazate, Oxaflumazine, Perazine, Pericyazine, Perimethazine, Perchloperazine, Promazine, Sulforidazine, Thiopropazate, thioridaziane, Trifluoperazine, Triflupromazine
Thioxanthenes such as Chlorprothixene, Clopenthixol, Flupentixol, Thiothixene
Other such as Alizapride, Amisulpride, 4-Arylpiperazines, 4-Arypiperdines, Buramate, Fluspirilene, Moledone, Penfluridol, Pimozide, Spirilene, Sulpiride
ANTIPYRETIC such as Aconine, Aconite, Aconitine, Phenicarbazide ANTIRICKETTSIAL such as p-Aminobenzoic Acid
ANTISEBORRHEIC such as 3-O-Lauroylpyridoxol Diacetate, Piroctone, Resorcinol, Selenium Sulfides, Tioxolone
ANTISEPTIC
Guanidines such as Alexidine, Ambazone, Chlorhexidine, Picloxydine
Halogens/Halogen Compounds such as Bronyl Chloride, Calcium lodate, Iodine Monochloride, Iodine Trichloride, lodoform, Povidone-lodine, Sodium Hyopchlorite, Sodium lodate, Symclosene, Thymol Iodide, Triclocarban, Triclosan, Troclosene Potasium
Nitrofurnase such as Flrazolidone, 2-(Methoxymethyl)-5-Nitrofuran, Nidroxyzone, Nifuroxime, Nifurzide, Nitrofurazone
Phenols such as Acetomeroctol, Chloroxylenol, Hexachlorophene, 1-Napthyl Salicylate, 2,4,6-Tribromo-m-cresol, 3',4',5-Trichlorosalicylanilide
Quinolines such as Aminoquinuride, Chloroxine, Chlorquinadol, Cloxyquin, Ethylhydrocupreine, Halquinol, Hydrastine, 8-Hydroxquinoline Sulfate
Others such as Boric Acid, Chloroazodin, m-Cresyl Acetate, Cuperic Sulfate, Ichthammol
ANTISPASMODIC such as Alibendol, Ambucetamide, Aminopromazine, Bietamiverine, Butaverine, Butropium, Carverine, Cimetropium, Cinnamedrine, Clebopride, Confine Hydrobromide, Coniine, Difemerine, Diisopromine, Dioxaphetyl Butyrate, Drofenine, Ethaverine, Feclemine, Fenalamide, Fenoverine, Fenpiprane, Flavoxate, Flopropione, Gluconic Acid, Guaiactamine, Hydramitrazine, Hymecromone, Leiopyrrole, Mebeverine, Moxaverine, Nafiverine, Octaverine, Phenamacide, Phloroglucinol, Pinaverium, Piperilate, Pipoxolan Hydrochloride, Pramiverin, Properidine, Propivane, Propyromazine, Prozapine Racefemine, Rociverine, Spasmolytol, Stilonium, Tiropramide,
Trepibutone, Tricromyl, Trifolium, Trimebutine, N, N-1 Trimethyl-3, 3-diphenylpropylamine.
ANTITHROMBOTIC such as Anagrelide, Argatroban, Cilostazol, Daltroban, Defibrotide, Enoxaparin, Fraxipariner®, Indobufen, Lamoparan, Ozagrel, Picotamide, Plafibride, Tedelparin, Ticlopidine, Triflusal.
ANTITUSSIVE such as Allocamide, Amicibone, Benproperine, Benzonatate, Bibenzonium, Bromoform, Butamirate, Butethamate, Caramiphen Ethanedisulfonate, Carbetapentane, Chlophedianol, Clobutinol, Cloperastine, Codeine Methyl Bromide, Codeine N-Oxide, Codeine Phosphate, Codeine Sulfate, Cyclexanone, Dextromethorphan, Dibunate Sodium, Dihydrocodeine, Dihydrocodeinone Enol Acetate, Dimemorfan, Dimethoxanate, α, α-Diphenyl-2-piperidinepropanol, Dropropizine, Drotebanol, Eprazinone, Ethyl Dibunate, Ethylmorphine, Fominoben, Guiaiapate, Hydrocodone, Isoaminile, Levopropoxyphene, Morclofone, Narceine, Normethadonem Noscapine, Oxeladin, Oxolamine, Pholcodine, Picoperine, Pipazethate, Piperidione, Prenoxdiazine, Racemethorphan, Taziprinon Hydrochloride, Tipepidine, Zipeprol.
ANTITULCERATIVE such as Aceglutamide Aluminum, Complex, ε-Acctamidocaproio Acid Zinc Salt, Acetoxolone, Arbaprostil, Benexate Hydrochloride, Bismuth Subcitrate Sol (Dried), Carbenoxolone, Cetraxate, Cimetidinc, Enprostil, Esaprazole, Famotidine, Raxilide, Gefarnate, Guaiazulene, Irsogladine, Nizatidine, Omeprazole, Ornoprostil, γ-Oryzanol, Pifarnine, Pirenzepine, Plaunotol, Ranitidine, Rioprostil, Rosaprostol, Rotraxate, Roxatidine Acetate, Sofaicone, Spizofurone, Sucralfate, Teprenone, Trimoprostil, Thrithiozine, Troxipide, Zolimidine.
ANTIUROLITHIC such as Acetohydroxamic Acid, Allopurinol, Potassium Citrate, Succinimide.
ANTIVENIN such as Lyovacr®, Antivenin.
ANTIVIRAL
Purines/Pyrimidinones such as 2-Acetyl-pyridine 5-((2-pyridylamino) thiocarbonyl), Thiocarbonohydrazone, Acyclovir, Dideoxyadenosine, Dideoxycytidine, Dideoxyinosine, Edoxudine, Floxuridine, Ganciclovir, Idoxuridine, MADU, Pyridinon, Trifluridine, Vidrarbine, Zidovudine.
Others such as Acetylleucine Monoethanolamine, Acridianamine,
Alkylisooxazoles, Amantadine, Amidinomycin, Cuminaldehyde
Thiosemicarbzone, Foscarnet Sodium, Kethoxal, Lysozyme, Methisazone, Moroxydine, Podophyllotoxin, Ribavirin, Rimantadine, stallimycin, statolon, Thymosins, Tromantadine, Xenazoic Acid.
ANXIOLYTIC
Arylpiperazines such as Buspirone, Gepirone, Ipsapirone.
Benzodiazepine Derivatives Alprazolam, Bromazepam, Camazepam, Chlordiazepoxide, Clobazam, Clorazepate, Chotiazepam, Cloxazolam, Diazepam, Ethyl Loflazepate, Etizolam, Fluidazepam, Flutazolam, Flutoprazepam, Halazepam, Ketazolam, Lorazepam, Loxapine, Medazepam, Metaclazepam, Mexazolam, Nordazepam, Oxazepam, Oxazolam, Pinazepam, Prazepam, Tofisopam.
Carbamates such as Cyclabarmate, Emylcamate, Hydroxyphenamate, Meprobamate, Phenoprobamate, Tybamate.
Others Alpidem, Benzoctamine, Captodiamine, Chlormezanone, Etifoxine, Fluoresone, Glutamic Acid, Hydroxyzine, Mecloralurea, Mephenoxalone, Oxanamide, Phenaglycodol, Suriclone.
BENZODIAZEPINE ANTAGONIST such as Flumazenil.
BRONCHODILATOR
Ephedrine Derivatives such as Albuterol, Bambuterol, Bitolterol, Carbuterol, Clenbuterol, Clorprenaline, Dioxethedrine, Eprozinol, Etafedrine, Ethylnorepinephrine, Fenoterol, Hexoprenaline, Isoetharine, Isoproterenol, Mabuterol, Metaproterenol, N-Methylephedrine, Pirbuterol, Procaterol, Protokylol, Reproterol, Rimiterol, Soterenol, Terbutaline, Tulobuterol.
Quaternary Ammonium Compounds such as Clutropium Bromide, Oxitropium Bromide.
Xanthine Derivatives such as Acefylline, Acefylline Ambuphylline, Aminophylline, Bamifylline, Choline Theophyllinate, Doxofylline, Dyphylline, Enprofylline, Etamiphylline, Etofylline, Guaithylline, Proxyphylline, Theobromine, 1-Theobromineaceatic Acid, Theophylline.
Others such as Methoxyphenanime, Tretoquinol.
CALCIUM CHANNEL BLOCKER
Arylalkylamines such as Bepridil, Ditiazem, Fendiline, Gallopamil, Terodiline, Verapamil.
Dihydropyridine Derivatives such as Felodipine, Isradipine, Nicardipine, Nifedipine, Nilvadipine, Nimodipine, Nisoldine, Nitrendipine.
Piperazine Derivatives such as Flunarisine. Others such as Perhexiline.
CALCIUM REGULATOR such as Calcifediol, Calcitonin, Calcitriol, Clodronic Acid, Dihydrotachysterol, Elcatonin, Etidronic Acid, Ipriflavone, Pamidronic Acid, Parathyroid Hormone, Teriparatide Acetate.
CARDIOTONIC such as Acetyldigititoxins, 2-Amino 4-picoline, Amrinone, Buclasdesine, cerberoside, Camphotamide, Convallatoxin, Cymarin, Denopamine, Deslanoside, Ditalin, Digitalis, Digitoxin, Digoxin, Dobutamine, Dopamine, Dopexamine, Enoximone, Erythrophleine, Fenalcomine, Gitalin, Gitoxin, Glycocyamine, Heptaminol, Hydrastinine, Lanotodises, Metamivam,
Substituted Methoxyphenyl-4, 5-dihydro-3(2H)-pridazinones, Milrionone, Neriifolin, Oleandxin, Ouabain, Oxyfedrine, Prenalterol, Proscillaridin, Resibufogenin, Scillaren, Scillarenin, Strophanthin, Sulmazole, Theobromine, Xamoterol.
CHELATING AGENT such as Deferozmine, Edetate Calcium Disodium, Edetate Disodium, Edeate Sodium, Edetate Trisodium, Pentetate Calcium Trisodium, Pentectic Acid, Succimer, Trientine.
CHOLECYSTOKININ ANTAGONIST (CCK Antagonist)
CHOLELITHOLYTIC AGENT such as Chenodiol, Methyl tert-Butyl Ether, Monooctanoin, Ursodiol.
CHOLERETIC such as Alibendol, Anethole Trithion, Azintamide, Cholic Acid, Cicrotoic Acid, Clanobutin, Cyclobutyrol, Cyclovalone, Cynarin(e), Dehydrocholic Acid, Deoxycholic Acid, Dimecrotic Acid, ?-Ethylbenzyl Alcohol, Exiproben, Feguprol, Fencibutirol, Fenipentol, Florantyrone, hymecromone, Menbutone, 3-(O-Methoxyphenyl)-2-phenylacrylic Acid, Metochalcone, Moquizone, Osalmid, Ox Bile Extract, 4, 4'-Oxydi-2-butanol, Piprozolin, Prozapine, 4-Salicyloylmorpholine, Sincalide, Taurocholic Acid, Timonacic, Tocamphyl, Trepibutone, Vanitiolide.
CHOLINERGIC such as Aceclidine, Acetylcholine, Acetylcholide, Aclatonium Napadisilate, Benzpyrinium Bromide, Bethanechol, Carbachol, Carpronium, Demecarium, Dexpanthenol, Diisopropyl Paraoxon, Echothiophate,
Edrophomium, Eseridine, Furtrethonium, Isoflurophate, Methacholine Chloride, Muscarine Neostigmine, Oxapropanium, Physostigmine, Pyridostigmine.
CHOLINESTERASE INHIBITOR such as Ambenonium, Distigmine, Galanthamine.
CHOLINESTERASE REACTIVATOR such as Obidoximine, Pralidoxime CNS STIMULANT/AGENT such as Amineptine, Amphetimine, Amphetaminil, Bemegride, Benzphetamine, Brucine, Caffeine, Chlorphentermine, Cloferciclan, Cloratermine, Coca, Demanyl Phosphate, Dexoxadrol, Dextroamphetamine Sulfate, Diethlpropion, N-Ethylamphetamine, Ethamivan, Etifelim, Etryptamine, Fencamfamine, Fenethylline, Fenosolone, Flurothyl, Hexacyclonate Sodium, homocamfin, Mazindol, Megexamide, Methamphetamine, Methylphenidate, Nicotine, Nicorinic Agonist, Nikethamide, Pemoline, Pentylenetetrazole, Phenidimetrazine, Phenmetrazine, Phentermine, Picrotoxin, Pipradrol, Prolintane, Pyrovalerone, Terahydrobenzothienpphyridines.
DECONGESTANT such as Cafaminol, Nordefrin
DENTAL CATTIES PROPHYLACTIC such as Sodium Fluoride.
DEPIGMENTOR such as Hydroquinine, Hydroquinone, Monobenzone.
DIURETIC
Organomercurials such as Chlormerodrin, Meralluride, Mercamphamide, Mercaptomerin Sodium, Mercumallyic Acid, Mercumatilin Sodium, Mercurous Chloride, Mersalyl.
Pteridines such as Furterence, Triamterene.
Purines such as 7-Morpholinomethyltheophylline, Pamabrom, Protheobromine, Theobromine
Steroids such as Canrenone, Oleandrin, Spironolactone
Sulfonamide Derivatives such as Acetazolmide, Azosemidem, Bumetanide, Butazolamide, Chloraminophenamide, Clofenamide, Clorexolene, Diphenylmethane-4, 4'-disulfonamide, Disulfamide, Ethoxzolamide, Flumethiazide, Mefruside, Methazolamide, Piretanide Torasemide.
Uracils such as Aminometradine, Amisometradine
Others such as Amanozine, Amiloride, Arbutin, Chlorazanil, Ethacrynic Acid, Etozolin, Isosorbide, Mannitol, Metochalone, Pethexiline, Urea.
DOPAMINE RECEPTOR AGONIST such as Bromocriptine, Fenoldopam, Lisuride, Naxagolide, Pergolide.
ECTOPARASITICIDE such as Amitraz, Brenzyl Benzoate, Carbaryl, Crotamiron, DDT, Dixanthogen, Isobornyl Thiocyanoacetate (Technical), Lime Sulfurated Solution Lindane, Malathion, Mercuric Oleate, Sulphur(Pharmaceutical)
ENZYME
Digestive such as a-Amylase(Swine Pancreas), Lipase, Pancrelipase, Pepsin, Rennim
Penicillin Inactivating such as Penicillinase
Proteolytic such as Collagenase, Chymopapain, Chymotrypsins, Papain, Trypsin.
ENZYME INDUCER (HEPATIC) such as Flumecinol.
ESTROGEN
Nonsteroidal such as Benzestrol, Broparoestrol, Chlorotrianisene, Dienestrol, Diethyistilbestrol, Diethyistilbestrol Diproprionate, Dimestrol, fosfestrol, Hexestrol, Methallenstril, Methestrol.
Steroidal such as Colpormon, Conugated Estrogenic Hormones, equilenin, Equilin, Esterified Estrogens Esteropipate, 17b-Estradiol, estradiol, Estradiol Benzoate, Estradiol 17b-Cypionate, Estrone, Ethibyl Estradiol, Mestranol, Moxestrol, Mytatrienediol, Polyestradiol Phosphate, Quinestradiol, Quinestrol.
GASTRIC SECRECTION INHIBITOR such as enterogastrone, Octreotide.
GLUCOCORTICOID such as 21-Acetoxyprefnenolone, Aalclometasone, Algestone, Amicinonide, Beclomethasone, Betamethasone, Betamethasone Dipropionate, Budesonide, Chloroprednisone, Clobetasol.Blovetasone, Clocortolone, Cloprednol, Corticosterone, Cortisone, Cortisone, Cortivazol, Deflazacort, Desonide, Desoximetasone, Dexamethasone, Diflorasone, Diflucortolone, Difluprednate, Enoxolone, Fluazacort, Flucloronide, Flumehtasone, Flunisolide, Fluocinolone Acetonide, Fluocinonide, Fluocortin Butyl, Fluocortolone, Fluorometholone, Fluperolone Acetate, Fluprednidene Acetate, Fluprednisolone, Flurandrenolide, Formocortal, Halcinonide, Halometasone, Halopredone Acetate, Hydrocotramate, Hydrocortisone, Hydrocortisone Acetate, Hydrocortisone Phosphate, Hydrocortisone 21-Sodium Succinate, Hydrocortisone Tebutate, Mazipredone, Medrysone, Meprednisone, Methyolprednisolone, Mometasone Furcate, Paramethasone, Prednicarbate, Prednisolone, Prednisolone 21-Diethylaminoacerate, Prednisone Sodium Phosphate, Prednisolone Sodium Succinate, Prednisolone Sodium 21 -m-Sulfobenzoate, Prednisolone 21-Stearoylglycolate, Prednisolone Tebutatem Orednisolone 21-Trimethylacatate, Prednisone, Prednival, Prednylidene, Prednylident 21-Diethlaminoacatate, Tixocoratal, Triamcinolone, Triamcinolone Acetonide, Triamcinolone Benetonide, Triamcinolone Hexacetonide GONAD-STIMULATING PRINCIPLE such as Clomiphene , Cyclofenil, Epimestrol, FSH, HCG, LH-RH.
GONADOTROPIC HORMONE such as LH, PMSG GROWTH HORMONE INHIBITOR such as Somatostatin
GROWTH HORMONE RELEASING FACTOR such as Semorelin GROWTH STIMULANT such as Somatotropin HEMOLYTIC such as Phenylhydrazine
HEPARIN ANTAGONIST such as Hexadimethrine Protamines.
HEAPATOPROTECTANT such as Betaine, cltolone, Malotilate, Orazamide, Phosphorylcholine, Protoporphyrin IX, silymarin-Group, Thiotic Acid
IMMUNOMODULATOR such as Amiprilose, Bucillamine, Ditiocarb Sodium, Inosine Pranobex, Muroctasin, Platonin, Procodazole, Tetramisole, 6-ary 1-5-6-dihydroimidazol-(2,1-B) Thiazole Dirivatives, Thymomodulin, Thymopentin.
IMMUNOSUPPRESSANT such as Cyclophilin, Cyclosporins, FK-506, Mizoribine, Rapamycin, Rapamycin Sulfamates
IONEXCHANGE RESIN such as Caracrylic Resins, Resodec, Sodium Polystyren Sulfonate
LACTATION STIMULATING HORMONE such as Prolactin
LH-RH AGONIST such as Buserelin, Goserelin, Leuprolide, Nafarelin, Triptorelin.
LIPOTROPIC such as N-Acetylmethionine, Choline Chloride, Choline Dehydrocholate, Choline Dihydrogen Citrate, Insitol, Lecithin, Methionine
LUPUS ERYTHEMATOSUS SUPPRESSANT such as Bismuth Sodium Triglycollamate, Bismuth Subsalicylate.
MINERALOCORTICOID such as Aldosterone, Deoxycorticosterone, Fludrocortisone.
MIOTIC such as Pilocarpus
MONOAMINE OXIDASE INHIBITOR such as Phenoxypropazine, Pivalylbenzhydrazine
MUCOLYTIC such as Acetylcysteine, Bromhexine, Carbocysteine, Domiodol, Letosteine, Mecysteine, Mesna, Sobrerol, Stepronin, Tiopronin, Tyloxapol
MUSCLE RELAXANT (SKELETAL) such as Afloqualone, Alcuronium, Atracurium Besylate, Baclofen, Benzoquinonium, C-Calebassine, Carisoprodol, Chlorphenesin Carbamate, Chlozoxazone, Curare, Cyclobenzaprine, dantrolene, Decamethonium, Eperisone, Fazadinium, Flumetramide, Gallamine, Triethiodide, Hexacarbacholine, Hexafluorenium, Idrocilamide, Lauexium Methyl Sulfate, Leptodactyline, Memantine, Mephenesin, Metaxalone, Methocarbamol, Metocurine Iodide, Pancuronium, Pipecuriym, Promoxilane, Quinine Sulfate, Styramate, Succinylcholine, Succinylcholine Suxethonium Bromide, Tetrazepam, Thiocolchicoside, Tizanidine, Tolperisone, Tubocurarine, Vecuronium, Zoxolamine.
NARCOTIC ANTAGONIST such as Amiphenazole, Cyclazocine, Levallorphan, Nadide, Nalmagene, Nalorphine, Nalorphine Dinicotinate, Naloxone, Naltrexone.
NEUROPROTECTIVE such as Dizocilpine
NOOTROPIC such as Aceglutamide, Acetylcarnitine, Aniracetam, Bifematlane, Exifone, Fipexide, Idebenone, Indeloxazune, Nizofenone, Oxiracetam, Piracetam, Propentofylline, Propentofylline Pyritinol.
OPHTHALMIC AGENT such as 15-ketoprostaglandins.
OVARIAN HORMONE such as Relaxin
OXYTOCIC such as Carboprost, Cargutocin, deaminoxytocin, Erogonovine, Gemeprost, Methylergonovine, Oxytocin, Pituitary (Posterior), Prostaglandin E2, Prostagandin F2a, Sparteine.
PEPSIN INIBITOR such as Sodium Amylosulfate PERISTALTIC STIMULANT such as Cisapride
PROGESTOGEN such as Allylestrenol, Anagestone, Chlormadinone Acetate, delmadinone Acetate, Demegestone, Desogestrel, Dimethisterone, Dydrogesterone, Ethinylestrenol, Ethjsterone, Ethynodiol, ethynodiol Diacetate, Flurogestone Acetate, Gestodene, Gestonorone Caproate, Haloprogesterone, 17-Hydroxy-16-methylene-progesterone, 17-Hydroxyprogesterone, 17a-Hydroxygesterone Caproate, Lynestenol, Medtogestone, Medroxyprogesterone, Megestrol Acetate, Melengestrol, Norethindrone, Norethindrone Acetate, Norethynodrel, Norgesterone, Norgestimate, Norgestrel, Norgestrienone, 19-Norprogesterone, Norvinisterone, Pentagestrone, Progesterone, Promegestone, Quingestrone, Trengestone
PROLACTIN INHIBITOR such as Metegoline
PROSTAGLANDIN/PROSTAGLANDIN ANALOG such as Bmeprost, Prostacyclin, Prostaglandin E1, Sulprostone
PROTEASE INHIBITOR such as Aprotinin, Camostat, Ganexate, Nagamostat
RESPIRATORY STIMULANT such as Almitrine, dimefine, Dimorpholamine, Doxapram, Lobeline, Mepixanox, Pimecione, Sodium Succinate, Tacrine
SCLEROSING AGENT such as Ethanolamine, Ethylamine, 2-Hexyldecanoic Acid, Sodium Ricinoleate, Sodium Tetradecyl Sulgate, Tribenoside
SEDATIVE/HYPNOTIC
Acyclic Ureides such as Acecarnromal, Apronalide, Bomisovalum, Capuride, Carbromal, ectylurea Alcohols such as Chlorhexadol, Ethchlorvynol, 4-Methyl-5-thiazolecthanol, tert-Pentyl Alcohol, 2,2,2-Trichloroethanol
Amides Such as Butoctamide, Diethylboromoacetamide, Ibrotamide, Isovaleryl Diethylamide, Niaprazine, Tricetamide, Trimerozine, Zolpidem, Zopiclone Barbituric Acid Derivatives such as Allobarbital, Amobarbital, Aprobarbital, Barbital, Brailabarbital, Butabarbital Sodium, Butalbital, Burallylonal, Butethal, Carbubarb, Cyclobarbital, Cyclopentobarbital, Enallylpropymal, 5-Ethyl-5-(piperidyl) barbituric Acid, 5-Furfuryl-5-isopropylbarbituric Acid, Heptabarbital, Hexethal Sodium, Hexobarbital, Mephobarbital, Methitural, Narocobarbital, Nealbarbital, Prntobarbital Sodium, Phenallymal, Phenobarbital, Phenobarbital Sodium, Phenylmethylbarbituric Acid, Probarbital, Propallylonal, Proxibarbal, Reposal, secobarbital Sodium, Talbutal, Tetrabarbital, vinbarbital Sodium, Vinylbiral
Benzodiazopine Derivatives such as Brotizolam, Doxefazopam, Estazolam, Flunitrazopam, Flurazopam, Haloxazolam, Loprazolam, Lormetazepam, Nitrazepam, Quazepam, Temasepam, Triazolam
Bromides such as Ammonium Bromide, Calcium Bromide, calcium Bromilactobionate, Lithium Bromide, Magnesium Bromide, Potassium Bromide, Sodium Bromide
Carbamates such as Amyl Carbamate(Tertiary), Ethinamate, Hexaprpymate, Meparfynol Carbamate, Novonal, Tricholorourethan
Chloral Derivatives such as Carbocloral, Chloral Betaine, Chloral Formamide, Chlotal Hydrate, Chloralantipyrine, Dichloralphenazone, Pentaerythritol Chloral, Triclofos
Piperidinediones such as Glutehimide, Methyprylon, Piperione, Pyrithyldione, Taglutimide, Thalidomide
Quinazolone Derivatives such as Etaqualone, Mecloqualone, Methaqualone
Others such as Acetal, Acetophenone, Aldol, Ammonium Valerate, Amphenidone, d-Bornyl a-Bromoisovalerate, d-Bornyl Isovaletate, Bromoform, Calcium 2-Ethylbutanoate, Carfinate, a-Chlorolose, Clomethiazole, Cypripedium, doxylamine, Etodroxizine, Etomidate, Feradiazole, Homofenazine, Hydrobromic Acid, Mecloxamine, Menthyl Valerate, Opium, Paraldehyde, Perlapine, Propiomazine, Rilmazafone, Sodium Oxybate, Sulfonethylmethane, Sulfonmethane
THROMBOLYTIC such as APSAC, Plasmin, Pro-Urokinase, Streptokinass, Tissue Plasminogen Activator, Urokinass
THYROTROPIC HORMONE such as TRH, TSH
MISCELLANEOUS - Vitamins, Mineral as well as other Nutrients, Vit B1, B2, B6, B12 and other water soluble vitamins, Vitamin C, Vitamin A, D, E and other oil soluble Vitamins, Iron, Zinc and other Miconutrinets and their combinations with Vitamins, Antiosidants i.e. Betavarotene and combination thereof with Vitamins, Gensing and other rejuvenants and suitable combinations of drugs disclosed above. The suitable mucoadhesive agents include cellulose derivatives like methyl cellulose,
hydroxypropylmethyl cellulose, hydroxypropyl cellulose, cellulose acetate phthalate, cellulose acetate, cellulose acetate butyrate, cellulose acetate propionate, cellulose acetate trimellitae, cellulose carboxymethyl ethers and their salts, hydroxyproplmethyl cellulose phthalate, hydropropylmethyl cellulose acetate succinate, polyethylene, polyvinyl acetate (homopolymer), polyvinyl acetate phthalate, propylene glycolalginate,
Polyvinylmethacrylate/maleic anhydride (PVM/MA) copolymer, Polyvinylpyrollidone
(PVP) /dimethiconlacrylate /polycarbamyl /polyglycolester, PVP/
dimethylaminoethylmethacrylate / polycarbamyl polyglycol ester, PVP/ polycarbamyl polyglycol ester, Polyvinylpyrollidone/vinyl acetate (PVP/VA) copolymer, gelatin and Gelatin derivatives.
Alginates, Carbomers, Polycarbophils.
Methacrylic acid copolymers.
Carrageenans, pectins, chitosans, cyclodextrins, lecitins.
Natural gums containg galactomannans like xanthan gum, Acacia, tragacanth, agar, guar gum and the like.
The fast soluble part of the sweetener gives a rapid burst of the sweetness whereas the mucoadhesive form binds to the oral mucosa and gives a prolonged sweet taste thereby effectively masking the bitttter or bad after-taste of the pharmaceutically active agents.
The conventional therapeutically acceptable additives like binding agents, lubricants, disintegrants, flavouring agents, colouring agents, pH modifiers and wetting agents may be added to the pharmaceutical composition prepared.
If desired, the active pharmaceutical agent may be first subjected to the conventional taste neutralization treatment like forming matrix microspheres, microencapsulation, complexation and the like.
The compressed tablets have sufficient mechanical strength which allows them to be packed in normal push-through type blister packages and does not require special packaging like peel-off blisters.
The manufacturing process is exemplified below:
Example 1.
Step 1 : Preparation of non-sugar sweetener in mucoadhesive form.
Aspartame 20.00 g
PVM/MA Copolymer 0.40 g
(GantrezAN169)
Acetone 20.00 ml
Dissolve Gantrez AN 169 in 20 ml Acetone. Granulate Aspartame with this solution and dry at 40°C. Sift through 60 mesh sieve.
Step 2: Tablet Formulation
Nimesulide (Drug/Pharmaceutical agent) 100.0 mg
Mannitol 204.5 mg
Aspartame of step 1 in mucoadhesive form 7.0 mg
Flavour 1.5 mg
Sodium Starch Glycolate 3.0 mg
Magnesium Stearate 4.0 mg
Sift all the ingredients through 40 mesh sieve and blend. Compress into tablets at a hardness of 1 to 5 Kg.
Example 2.
Step 1: Preparation of non-sugar Sweetener in Mucoadhesive form:
Aspartame 20.00 g
Carbomer (Carbopol 934P) 0.40 g
Water 20.00 ml
Disperse Carbopol 934P in 20 ml Water. Granulate Aspartame with it and dry at 40°C. Sift through 60 mesh sieve.
Step 2: Tablet Formulation
Nimesulide (Drug/Pharmaceutical agent) 100.0 mg
Mannitol 204.5 mg
Aspartame 3.0 mg
Aspartame of step 1 in mucoadhesive form 4.0 mg
Flavour 1.5 mg
Sodium Starch Glycolate 3.0 mg
Magnesium Stearate 4.0 mg
Sift all the ingredients through 40 mesh sieve and blend. Compress into tablets at a
hardness of 1 to 5 Kg.
Example 3:
Step 1: Taste neutralization of drug substance.
Ibuprofen (Drug/Pharmaceutical agent) 95.95 g
Tribehenin 4.00 g
Polysorbate 80 0.05 g
Water 40.00 ml
Heat water to about 50°C - 60°C. Add polysorbate 80 and mix. Under stirring add Tribehenin followed by Ibuprofen. A wet dough will be formed. Cool it to 35°C. Size it through 20 mesh sieve. Dry at about 45°C till moisture content is 1 to 3%. Sift through 60 mesh sieve.
Step 2: Tablet Formulation
Ibuprofen from step 1 200.0 mg
Equivalent to Ibuprofen
Xylitol 204.5 mg
Aspartame in mucoadhesive form 7.00 mg
(from step 1 of example 2)
Flavour 1.5 mg
Sodium Starch Glycolate 3.0 mg
Megnesium Stearate 4.0 mg
Sift all the ingredients through 40 mesh sieve and blend. Compress into tablets at a hardness of 1 to 5 Kg.
Example 4: % w/w
Cisapride (Drug/Pharmaceutical agent) 2.50
Liquid Paraffin 0.25
Sorbitol 84.75
Sodium Starch Glycollate 5.00
Croscarmellose Sodium 1.25
Magnesium Stearate 1.25
Aspartame in mucoadhesive form 3.00
(from step 1 of example 1)
Colloidal Silicon Dioxide 1.25
Flavour 0.75
Pass the drug through mesh no. 60 (BSS) sieve. Granulate the drug with a solution of Liquid Paraffin in Dichloromethane and pass through mesh no. 40(BSS) sieve. Dry at a temperature of 45-50°C. Sift Sorbitol through mesh no. 60(BSS) sieve and mix with drug containing Liquid Paraffin. This blend is then granulated with water and then dried at a temperature of 50-60°C. The dried granules are sifted through mesh no.22 (BSS) sieve.
Sift Sodium Starch Glycollate, Magnesium Stearate, Colloidal Silicon Dioxide, Croscarmellose Sodium, Aspartame (in mucoadhesive form) and Flavours through mesh no. 30 (BSS) sieve and mix with the above said bulk. Compress into tablets using conventional tabletting machine at a hardness of 1 - 3 Kg.
Example 5: % w/w
Cetirizine Dihydrochloride (Drug/Pharmaceutical agent) 2.5
Crosslinked Polyacrylic Acid (Ion-exchange resin) 10.0
Hydrochloric Acid q.s. to adjust pH
Mannitol 64.5
Croscarmellose Sodium 3.75
Povidone 0.25
Aspartame in mucoadhesive form 6.25
(from step 1 of example 1)
Magnesium Stearate 0.50
Aerosil 0.75
Sodium Starch Glycollate 3.75
Sodium Chloride 3.00
Citric Acid 2.00
Flavour 2.75
Dissolve Cetirizine dihydrochloride in 20 times of its weight of water. Add Crosslinked Polyacrylic Acid in small increments with constant stirring. Adjust pH to 3 with hydrochloric acid. Keep aside for 1 to 6 hours and then decant the water. Wash the sediment with water atleast twice. Dry the sediment at 40° to 50°C. Pass through sieve of mesh no 60 (BSS). Mix with pre-sifted (through mesh no. 30 BSS) blend of Mannitol, Croscarmellose Sodium, Povidone, Aspartame (in mucoadhesive form), Magnesium Stearate, Aerosil, Sodium Starch Glycollate, Sodium Chloride, Citric Acid and Flavour. Compress into tablets using conventional tabletting machine at a hardness of 1 - 3 Kg.
Example 6:
Step 1. Preparation of non-sugar sweetener in Mucoadhesive form:
Saccharin Sodium 100.00 g
Polycarbophil (Noveon AA-1) 4.00 g
Water 10.00g
Disperse Polycarbophil in Water. Granulate Saccharin Sodium with this dispersion. Dry at 50°C and sift through mesh no. 40 (BSS).
Step 2. % w/w
Chloroquine Phosphate (Drug/Pharmaceutical agent) 10.0
Crosslinked Polyacrylic Acid, Potassium salt 20.0
(Ion-exchange resin)
Hydrochloric Acid q.s. to adjust pH
Mannitol 51.50
Crosscarmellose sodium 0.25
Povidone 0.25
Saccharin sodium in mucoadhesive form 6.25
(from step 1 of example 6)
Magnesium Stearate 0.50
Sodium Starch Glycollate 3.75
Sodium Chloride 3.00
Citric Acid 2.00
Flavour 2.75
Dissolve Chloroquine Phosphate in 20 times of its weight of water. Add Crosslinked Polyacrylic Acid in small increments with constant stirring. Adjust pH to 6 with hydrochloric acid. Keep aside for 1 to 6 hours and then decant the water. Wash the sediment with water atleast twice. Dry the sediment at 40° to 50°C. Pass through sieve of mesh no 60 (BSS). Mix with pre-sifted (through mesh no. 30 BSS) blend of Mannitol, Povidone, Saccharin Sodium (in mucoadhesive form), Magnesium Stearate, Sodium Starch Glycollate, Sodium Chloride, Citric Acid and Flavour. Compress into tablets using conventional tabletting machine at a hardness of 1 - 3 Kg.
Example 7:
Step 1: Taste neutralization of drug substance.
Ascorbic Acid 96.00 g
Gelatin 4.00 g
Water 30.00 ml
Heat water to about 60°C - 70°C. Add Gelatin and dissolve. Coat the Ascorbic Acid by spraying the gelatin solution using fluidized bed coater. Size the coated drug powder through 40 mesh sieve.
Step 2: Mucoadhesive Sweetener.
Ammonium Glycirrhizinate 20.00 g
PVM/MA Copolymer 0.40 g
(GantrezAN 169)
Acetone 20.00 ml
Dissolve Gantrez AN 169 in 20 ml Acetone. Granulate Ammonium Glycirrhizinate with this solution and dry at 40°C. Sift through 60 mesh sieve.
Step 3:Tablet Formulation
Ascorbic Acid from step 1
Equivalent to Ascorbic Acid 100.0 mg
Sorbitol 204.5 mg
Ammonium Glycirrhizinate in Mucoadhesive form 7.00 mg
(from step 2)
Flavour 1.5mg
Sodium Starch Glycolate 3.0 mg
Megnesium Stearate 4.0 mg
Sift all the ingredients through 40 mesh sieve and blend. Compress into tablets at a hardness of 1 to 5 Kg.
Example 8.:
Tablet Formulation
Interferon (Alpha) equivalent to 18 Million I.U.
Mannitol 204.5 mg
Aspartame in mucoadhesive form 7.0 mg
(from step 1 of example 1)
Flavour 1.5mg
Sodium Starch Glycolate 3.0 mg
Magnesium Stearate 4.0 mg
Sift all the ingredients through 40 mesh sieve and blend. Compress into tablets at a hardness of 1 to 3 Kg.
Example 9:
Alprazolam 1 mg
Isomalt 98.9 mg
Aspartame 0.03 mg
Acesulfam 0.03 mg
Neophesperidine DC in mucoadhesive form 0.04 mg
Sift all the ingredients through 30 mesh sieve and blend. Compress into tablets at a hardness of 1 to 3 Kg.
The advantages of the present invention are:
a. The pharmaceutical tablets prepared according to the present invention dissolve
/ disperse in the mouth within one minute requiring very little amount of body
fluids like saliva to produce a solution or suspension of the drug for oral
administration.
b. The tablet leaves a prolonged sweet taste in the mouth.
c. The unpleasant of bitter taste of the drug is masked without significantly
interfering with the dissolution and ultimate bioavailability of the drug present of the
tablet.
d. The process of this invention has low manufacturing cost avoiding the special
and costly techniques like Lyophilization, Spray-drying and the like.
Since many apparently different embodiments of the present invention could be made without departing from the spirit and scope thereof, it is intended that the description of the invention herein be interpreted as being illustrative only and not limiting in any manner whatsoever.






We claim:
1. A novel fast dissolving pharmaceutical composition in solid dosage form with
prolonged sweet taste which comprises:
(a) at least one pharmaceutical active agent in an amount of from 0.1 to 99
weight % of the total dosage form;
(b) at least one water soluble sugar in an amount of from 5 to 95 weight % of
the total dosage form,
(c) at least one non-sugar sweetener in a fast release form in an amount of
from greater than 0 to 10 weight % of the total dosage form; and
(d) at least one non-sugar sweetener in a mucoadhesive slow release form in
an amount of from 0.5 to 20 weight % of the total dosage form.

2. A composition as claimed in claim 1, wherein the water soluble sugar is mannitol,
sorbitol and/or xylitol.
3. A composition as claimed in claim 1, wherein the non-sugar sweetner is isomalt;
aspartame, acesulfame potassium, saccharine sodium, cyclamates,
neohesperidine and/or glycirrhizin.
4. A process for the preparation of a fast dissolving pharmaceutical composition in
solid dosage form with prolonged sweet taste as claimed in claim 1, which
comprises mixing the following ingredients:-
a. at least one drug/pharmaceutically active agent in an amount of from 0.1
to 99 weight % of the total dosage form;
b. at least one water soluble sugar in an amount of from 5 to 95 weight % of
the total dosage form;
c. at least one non-sugar sweetener in fast release form in an amount of
from greater than 0 to 10 weight % of the total dosage form; and
d. at least one non-sugar sweetener in a mucoadhesive slow release form in
an amount of from 0.5 to 20 weight % of the total dosage form;
and compressing the resulting mixture into a solid dosage form.
5. A process as claimed in claim 4, wherein the water soluble sugar is mannitol,
sorbitol and/or xylitol.
6. A process as claimed in claim 4, wherein the non-sugar sweetner is isomalt,
aspartame, acesulfame potassium, saccharine sodium, cyclamates,
neohesperidine and/or glycirrhizin.
7. A novel fast dissolving pharmaceutical composition in solid dosage form with
prolonged sweet taste substantially as here described in refere to the foregoing
description and examples.
8. A process for the preparation of a fast dissolving pharmaceutical composition in
solid dosage form with prolonged sweet taste substantially as here described in
refere to the foregoing description and examples.

Documents:

1514-del-1999-abstract.pdf

1514-del-1999-claim.pdf

1514-del-1999-correspondence-others.pdf

1514-del-1999-correspondence-po.pdf

1514-del-1999-description (complete).pdf

1514-del-1999-form-1.pdf

1514-del-1999-form-13.pdf

1514-del-1999-form-19.pdf

1514-del-1999-form-2.pdf

1514-del-1999-form-3.pdf

1514-del-1999-gpa.pdf

1514-del-1999-petition-137.pdf

1514-del-1999-petition-138.pdf


Patent Number 255203
Indian Patent Application Number 1514/DEL/1999
PG Journal Number 06/2013
Publication Date 08-Feb-2013
Grant Date 02-Feb-2013
Date of Filing 30-Nov-1999
Name of Patentee PANACEA BIOTEC LIMITED
Applicant Address B-1 EXTN./A-27 MOHAN CO-OPERATIVE INDUSTRIAL ESTATE, MATHURA ROAD, NEW DELHI 10044-INDIA
Inventors:
# Inventor's Name Inventor's Address
1 AMARJIT SINGH B-1 EXTN./A-27 MOHAN CO-OPERATIVE INDUSTRIAL ESTATE, MATHURA ROAD, NEW DELHI 10044-INDIA
2 RAJESH JAIN B-1 EXTN./A-27 MOHAN CO-OPERATIVE INDUSTRIAL ESTATE, MATHURA ROAD, NEW DELHI 10044-INDIA
PCT International Classification Number A61K 9/28
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA