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    • 48. 发明专利
    • Extrusion process for making compositions with poorly compressible therapeutic compounds e.g. metformin hydrochloride
    • NZ585116A
    • 2011-12-22
    • NZ58511606
    • 2006-05-08
    • NOVARTIS AG
    • VASANTHAVADA MADHAVLAKSHMAN JAYTONG WEI-QINSERAJUDDIN ABU T MJOSHI YATINDRAKOWALSKI JAMES
    • A61K31/155A61K9/16A61K9/20
    • A process for making an oral dosage form of a pharmaceutical composition comprising the steps of: (a) combining a therapeutic compound selected from the group consisting of metoclopramide and propantheline bromide; aluminum trisilicate, aluminium hydroxide, cimetidine, phenylbutazone, indomethacin, naproxen, ibuprofen, flurbiprofen, diclofenac, dexamethasone, prednisone, prednisolone, glyceryl trinitrate, isosorbide dinitrate, pentaerythritol tetranitrate , soloctiditum, vincamine, naftidrofuryl oxalate, co-dergocrine mesylate, cyclandelate, papaverine, nicotinic acid, erythromycin stearate, cephalexin, nalidixic acid, tetracycline hydrochloride, ampicillin, flucolaxacillin sodium, hexamine mandelate, hexamine hippurate, fluazepam, diazepam, temazepam, amitryptyline, doxepin, lithium carbonate, lithium sulfate, chlorpromazine, thioridazine, trifluperazine, fluphenazine, piperothiazine, haloperidol, maprotiline hydrochloride, imipramine, desmethylimipramine, methylphenidate, ephedrine, epinephrine, isoproterenol, amphetamine sulfate, amphetamine hydrochloride, diphenhydramine, diphenylpyraline, chlorpheniramine, brompheniramine, bisacodyl, magnesium hydroxide, dioctyl sodium sulfosuccinate, ascorbic acid, alpha tocopherol, thiamine, pyridoxine, dicyclomine, diphenoxylate, verapamil, nifedepine, diltiazem, procainamide, disopyramide, bretylium tosylate, quinidine sulfate, quinidine gluconate, propranolol hydrochloride, guanethidine monosulphate, methyldopa, oxprenolol hydrochloride, captopril, hydralazine, ergotamine, epsilon aminocaproic acid, protamine sulfate, acetylsalicylic acid, acetaminophen, codeine phosphate, codeine sulfate, oxycodone, dihydrocodeine tartrate, oxycodeinone, morphine, heroin, nalbuphine, butorphanol tartrate, pentazocine hydrochloride, cyclazacine, pethidine, buprenorphine, scopolamine, mefenamic acid, phenytoin sodium, sodium valproate, dantrolene sodium, tolbutamide, diabenase glucagon, insulin, triiodothyronine, thyroxine, propylthiouracil, furosemide, chlorthalidone, hydrochlorthiazide, spironolactone, triampterene, ritodrine, fenfluramine hydrochloride, phentermine, diethylproprion hydrochloride, aminophylline, theophylline, salbutamol, orciprenaline sulphate, terbutaline sulphate, guaniphenesin, dextromethorphan, noscapine, carbocisteine, cetylpyridinium chloride, tyrothricin, chiorhexidine, phenylpropanolamine, pseudoephedrine, dichtoraiphenazone, nitrazepam, promethazine theoclate, ferrous sulphate, folic acid, calcium gluconate, sulphinpyrazone, allopurinol, and probenecid with at least one granulating component to form a mixture, wherein said granulating component is a polymer (which may be selected from the group consisting of water-soluble polymers, water-swellable polymers, and water-insoluble polymers) having a Tg less than the melting point of said therapeutic compound; (b) kneading said mixture in an extruder while heating said mixture to a heating temperature less than a melting point of said therapeutic compound and greater than or equal to the Tg of said polymer; (c) extruding said mixture to form granules; and, (d) compressing or molding said granules.