Controlled release powder and process for its preparation
AssigneeElan Corporation, plc
InventorsRandall T. Sparks, Edward J. Geoghegan
Life of this patent
Estimating the term…
Abstract
A controlled release powder containing discrete micro-particles for use in edible, pharmaceutical and other controlled release compositions is disclosed. The micro-particles have an average size in the range of from 0.1 to 125 .mu.m. Each of the micro-particles is in the form of a micromatrix of an active ingredient uniformly distributed in at least one non-toxic polymer. The micro-particles have a predetermined release of active ingedient when the dissolution rate thereof is measured according to the Paddle Method of U.S. Pharmacopoeia XX at 37.degree. C. and 75 r.p.m.
Claims52
A controlled release taste masked powder containing discrete micro-particles for use in edible pharmaceutical and other controlled release compositions, said powder comprising particles containing an active ingredient in intimate admixture with at least one non-toxic insoluble, permeable, impermeable, or biodegradable controlled release polymer, or mixtures thereof, in an amount effective to provide a predetermined and controlled release of said active ingredient, each of said particles being in the form of a micromatrix with the active ingredient uniformly distributed throughout the matrix, but not entirely coated by the polymer, said particles having an average size of from 0.1 to 125 .mu.m, being unlikely to be significantly degraded or ground by any chewing action, and having a predetermined release of said active ingredient.
A controlled release powder containing discrete micro-particles for use in edible, pharmaceutical and other controlled release compositions, said powder comprising particles containing an active ingredient in intimate admixture with at least one non-toxic polymer, wherein said polymer substantially but not entirely coats the active ingredient, each of said particles being in the form of a micromatrix with the active ingredient uniformly distributed throughout the matrix, said particles having an average size of from 0.1 to 125 .mu.m, and a dissolution rate of active ingredient from said particles which is substantially proportional to the square root of time, said active ingredient selected from the group consisting of:
- metoclopramide bromide, propantheline bromide, aluminium trisilicate, aluminum hydroxide, cimetidine, phenylbutazone, indomethacin, naproxen, ibuprofen, flurbiprofen, diclofenac, dexamethasone, prednisone, glyceryl trinitrate, isosorbide dinitrate, pentaerythritol tetranitrate, soloctidilum, vincamine, naftidrofuryl oxalate, co-dergocrine mesylate, cyclandelate, papaverine, nictoninic acid, erythromycin stearate, cephalexin, nalidixic acid, tetracycline hydrochloride, ampicillin, flucloxacillin sodium, hexamine mandelate, hexamine hippurate, flurazepam, diazepan, 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, nifedipine, 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, disbenase glucagon, insulin, triiodothyronine, thyroxine and propylthiouracil, furosemide, chlorthalidone, hydrochlorthiazide, spironolactone, triamterene, ritodrine, appetite fenfluramine hydrochloride, phentermine and diethylproprion hydrochloride, aminophylline, theophylline, salbutamol, orciprenaline sulphate, terbutaline sulphate, guaiphenesin, dextromethorphan, noscapine, carbocisteine, cetylpyridinium chloride, tyrothricin, chlorhexidine, phenylpropanolamine, pseudoephedrine, dichloralphenazone, nitrazepam, promethazine theoclate, ferrous sulfate, folic acid and calcium gluconate, sulphinpyrazone, allopurinol and probenecid.
Dependencies are inferred from the claim text.