Patent EA-003751-B1 (EA)
Title: Solid thermoformable controlled-release pharmaceutical composition
Inventor: WUTHRICH PATRICK
IPC: A61P3/10
Filed: 2000-06-27
Abstract: 1. A solid controlled-release pharmaceutical composition, wherein the composition consists of a thermoformable mixture of at least one active ingredient and of one or more pH independent polymers selected from the group consisting of the polymethacrylates, which belong to the family of the Eudragit (RTM) products RL and/or RS, the release of the active ingredient(s) being controlled solely by the nature of the polymethacrylate(s) used, by the amount thereof relative to the active ingredient(s), and by the technique employed in the manufacture of the composition. 2. A solid controlled-release pharmaceutical composition according to claim 1, wherein the polymethacrylate(s) used in the thermoformable mixture composition belong(s) belong to the family of the Eudragit (RTM) products RL and/or RS. 3. A solid controlled-release pharmaceutical composition according to claim 1, wherein the thermoformable mixture comprises Eudragit (RTM) of type E, alone or in association with one or more of the Eudragit (RTM) products mentioned hereinbefore. 4. A solid controlled-release pharmaceutical composition according to claim 1, wherein the thermoformable mixture comprises Eudragit (RTM) of type L100, L-100-55 and/or S100 alone or in association with one or more of the Eudragit (RTM) products mentioned hereinbefore. 5. A solid controlled-release pharmaceutical composition according to claim 1, wherein the composition is administrable by one of the routes selected from the oral, buccal, sublingual, ocular, vaginal, rectal and parenteral routes. 6. A solid controlled-release pharmaceutical composition according to any one of claims 1 to 5, wherein the composition is administrable by the oral route. 7. A solid controlled-release pharmaceutical composition according to claim 1, wherein the temperature of thermoforming of the mixture is 60 degree C. to 150 degree C. 8. A solid controlled-release pharmaceutical composition according to claim 8, wherein the temperature of thermoforming of the mixture is 80 degree C. to 130 degree C. 9. A solid controlled-release pharmaceutical composition according to claim 1, wherein the mixture is thermoformed according to the technique of extrusion. 10. A solid controlled-release pharmaceutical composition according to claim 1, wherein the mixture is thermoformed according to the technique of injection. 11. A solid controlled-release pharmaceutical composition according to claim 1, wherein the mixture is thermoformed according to the technique of coextrusion, the inner layer of the composition in this case being composed of the mixture and the outer layer of the composition being composed either of one or more polymethacrylate(s) or of one or more polymethacrylate(s) in admixture with one or more active ingredient(s), which may be the same as or different than that/those contained in the inner layer. 12. A solid controlled-release pharmaceutical composition according to claim 1, wherein the mixture is thermoformed according to the technique of coinjection, the outer layer of the composition being composed either of one or more polymethacrylate(s) or of one or more polymethacrylate(s) in admixture with one or more active ingredient(s), which may be the same as or different than that/those contained in the central portion. 13. A solid controlled-release pharmaceutical composition according to claim 1, wherein the composition optionally contains one or more pharmacologically acceptable excipients selected from anti-oxidants, flavorings, colorings, preservatives, sweeteners and anti-adherents. 14. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient(s) is/are selected from anti-infective agents including penicillins, cephalosporins, cyclines, beta-lactamase inhibitors, aminosides, quinolones, nitroimidazole compounds, sulphamides or antibacterials, or antihistamines, anti-allergics, anaesthetics, steroidal or nonsteroidal anti-inflammatories, antalgics having local or systemic action, antispasmodics, anti-cancer agents, diuretics, beta-blockers, antihypertensives, anti-angina agents, anti-arrythmics, vasodilators, bradycardiacs, calcium inhibitors, sedatives, cardiotonics, antifungals, antiulcerative agents, venotonics, vasculoprotectors, anti-ischaemics, antiemetics, anticoagulants, antithrombotics, immunosuppressors, immunomodulators, antivirals, antidiabetics, hypolipidaemic agents, antiobesity agents, anticonvulsants, hypnotics, antiparkinsonian agents, antimigraine agents, neuroleptics, anxiolytics, antidepressants, antipsychotics, psychostimulants, memory-enhancers, bronchodilators, antitussives, anti-osteoporotics, peptide hormones, steroids, enzymes, enzyme inhibitors, and melatoninergic agonists and antagonists. 15. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is benfluorex hydrochloride. 16. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is rilmenidine dihydrogenphosphate. 17. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is fenspiride hydrochloride. 18. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is (1R)-1-({-[[(2R)-2-(acetylamino)-3-phenylpropanoyl](cyclopentyl)amino]acety l}amino)-4-{[amino(imino)methyl]amino}butylboronic acid hydrochloride. 19. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is gliclazide. 20. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is piribedil. 21. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is 2-({2-methoxy-2-[3-(trifluoromethyl)phenyl]ethyl}amino)ethyl-4-2-(2-{[2-(9 H-fluoren-9-yl)acetyl]amino}ethyl)benzoate L-tartrate. 22. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is 3a,10-dihydro-5,5-dioxo-4H-(S)-pyrrolidino[1,2-c][1,2,4]benzothiadiazine. 23. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is N-[2-(5-ethyl-1-benzothien-3-yl)ethyl]acetamide. 24. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is indapamide. 25. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is tertatolol. 26. A solid controlled-release pharmaceutical composition according to claim 1, wherein the active ingredient is N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide.