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MICROPARTICULATE ORAL GALENICAL FORM FOR THE DELAYED AND CONTROLLED RELEASE OF PHARMACEUTICAL ACTIVE PRINCIPLES
专利权人:
FLAMEL TECHNOLOGIES
发明人:
LEGRAND, VALERIE,CASTAN, CATHERINE,MEYRUEIX, REMI,SOULA, GERARD
申请号:
CA2463134
公开号:
CA2463134C
申请日:
2002.10.09
申请国别(地区):
CA
年份:
2012
代理人:
摘要:
The invention relates to a microparticulate system with controlled delayed release of active principles (PA) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring the release of the PA in a certain way thanks to a double release mechanism "time dependent" and "pH dependent". To achieve this goal, the invention provides a multimicrocapsular oral dosage form designed so that its therapeutic efficacy is guaranteed, and in which the release of the AP is governed by a double mechanism for triggering the release: "triggering time" and "triggering pH" This system is made up of microcapsules (200 to 600 ~ m) comprising a PA core covered with a coating film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax melting temperature = 40-90 ~ C) , with B / A between 0.2 and 1.5. These microcapsules have an in vitro dissolution behavior such that at constant pH 1.4, there is a lag phase of between 1 and 5 hours followed by release of the AP and such that the transition from pH 1.4 to pH 6,8 causes a release of the AP without latency time in vitro.L'invention conceme un système microparticulaire à libération retardéecontrolée de principes actifs (PA) dont la fenêtre d'absorption in vivo estessentiellement limitée aux parties hautes du tractus gastro-intestinal, cesystème étant destiné à une administration par voie orale. Le but del'invention est de foumir un système assurant la libération du PA de fasçoncertaine grâce à un double mécanisme de libération "temps dépendant" et "pHdépendant".Pour atteindre ce but, l'invention proposé une forme galéniqueorale multimicrocapsulaire conçue de telle sorte que son efficacitéthérapeutique soit garantie, et dans laquelle la libération du PA est régiepar un double mécanisme de déclenchement de la
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中国工程科技知识中心
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