Storage-stable drug form

Details Storage-stable drug form Storage-stable drug form

1997-09-16

1999-08-31

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424465, 424488, A61K 914

Patent

active

059451270

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to solid drug forms obtainable by extrusion of a solvent-free melt comprising, besides one or more active substances, a mixture of or copolymers of N-vinylpyrrolidone, substances,
The production of solid drug forms by extrusion of a melt comprising, besides the active substance, polymers based on N-vinylpyrrolidone, with subsequent shaping, is disclosed, for example, in EP-B 240 904.
WO 93/10758 describes slow-release drug forms based on an amorphous carbohydrate glass matrix which contain polyvinylpyrrolidone or maltodextrins as agents for recrystallization. To produce the matrix, aqueous solutions of the matrix components are heated until viscous mixtures are obtained, and the active substance is incorporated therein by kneading, after which the active substance-containing mixture can be processed for example by extrusion.
A fundamental difficulty in the production of solid drug forms by extrusion of active substance-containing melts is that the polymers used for matrix formation must, on the one hand, have adequate melt-processability but, on the other hand, remain dimensionally stable in the finished drug form even on prolonged storage. Polymers with good melt-processability are, in particular, those which either have relatively low molecular weights and thus relatively low glass transition temperatures and/or contain plasticizing monomers such as vinyl acetate, ie. precisely these polymers result in the unwanted phenomenon of cold flow on processing to solid drug forms.
It is an object of the present invention to find storage-stable solid drug forms which are obtainable in a simple manner by extrusion of active substance-containing melts and subsequent shaping.
We have found that this object is achieved by the drug forms defined at the outset.
Examples of suitable active substances are:
betamethasone, thioctic acid, sotalol, salbutamol, norfenefrine, silymarin, dihydroergotamine, buflomedil, etofibrate, indometacin, oxazepam, beta-acetyldigoxin, piroxicam, haloperidol, ISMN, amitriptyline, diclofenac, nifedipine, verapamil, pyritinol, nitrendipine, doxycycline, bromhexine, methylprednisolone, clonidine, fenofibrate, allopurinol, pirenzepine, levothyroxine, tamoxifen, metildigoxin, o-(beta-hydroxyethyl)rutoside, propicillin, aciclovir mononitrate, paracetamol, naftidrofuryl, pentoxyfylline, propafenone, acebutolol, L-thyroxine, tramadol, bromocriptine, loperamide, ketotifen, fenoterol, Ca dobesilate, propranolol, minocycline, nicergoline, ambroxol, metoprolol, beta-sitosterol, enalapril hydrogen maleate, bezafibrate, ISDN, gallopamil, xantinol nicotinate, digitoxin, flunitrazepam, bencyclane, dexpanthenol, pindolol, lorazepam, diltiazem, piracetam, phenoxymethylpenicillin, furosemide, bromazepam, flunarizine, erythromycin, metoclopramide, acemetacin, ranitidine, biperiden, metamizole, doxepin, dipotassium chlorazepate, tetrazepam, estramustine phosphate, terbutaline, captopril, maprotiline, prazosin, atenolol, glibenclamide, cefaclor, etilefrine, cimetidine, theophylline, hydromorphone, ibuprofen, primidone, clobazam, oxaceprol, medroxyprogesterone, flecainide, Mg pyridoxal-5-phosphate glutamate, hymechromone, etofylline clofibrate, vincamine, cinnarizine, diazepam, ketoprofen, flupentixol, molsidomine, glibornuride, dimethindene, melperone, soquinolol, dihydrocodeine, clomethiazole, clemastine, glisoxepide, kallidinogenase, oxyfedrine, baclofen, carboxymethylcysteine, thioridazine, betahistine, L-tryptophan, myrtol, bromelaines, prenylamine, salazosulfapyridine, astemizole, sulpiride, benserazide, dibenzepine, acetylsalicylic acid, miconazole, nystatin, ketoconazole, Na picosulfate, colestyramine, gemfibrozil, rifampicin, fluocortolone, mexiletine, amoxicillin, terfenadine, mucopolysaccharide polysulfates, triazolam, mianserin, tiaprofenic acid, amezinium metilsulfate, mefloquine, probucol, quinidine, carbamazepine, Mg L-aspartate, penbutolol, piretanide, amitriptyline, cyproterone, Na valproate, mebeverine, bisacodyl, 5-aminosalicylic acid, dihydralazine, magaldrate, phe

REFERENCES:
patent: 4520180 (1985-05-01), Barabas et al.
patent: 4801460 (1989-01-01), Goertz et al.

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