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    • 2. 发明申请
    • MICROPARTICLES WITH MODIFIED RELEASE OF AT LEAST ONE ACTIVE PRINCIPLE AND ORAL GALENIC FORM COMPRISING SAME
    • 具有至少一个有效原则的修改释放的微生物和包含其中的口服糖尿病形式
    • WO2007036671A3
    • 2007-05-24
    • PCT/FR2006050944
    • 2006-09-27
    • FLAMEL TECH SADARGELAS FREDERICGUIMBERTEAU FLORENCECASTAN CATHERINEMEYRUEIX REMISOULA GERARD
    • DARGELAS FREDERICGUIMBERTEAU FLORENCECASTAN CATHERINEMEYRUEIX REMISOULA GERARD
    • A61K9/50A23L33/00A61K9/20A61K9/48A61K31/155A61K31/522
    • A61K9/5073A61K9/2077
    • The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel multimicroparticulate galenic system operating in accordance with a dual time-dependent and pH-dependent release mechanism, which enables the following three parameters to be adjusted independently of one another: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGIT® L100-55) and a hydrophobic compound (B2) (LUBRITAB®).The invention also concerns medicines based on said microparticules.
    • 本发明涉及具有口腔活性成分释放的微粒体系。 本发明的目的在于提供一种新颖的多分子盖仑系统,该系统根据双重时间依赖性和pH依赖性释放机制进行操作,这使得以下三个参数可以彼此独立地进行调整:a)释放之前的潜伏期 胃中的活跃原则; b)pH触发在肠中释放活性成分; c)有效原理的释放速度。 这通过使用由各自涂覆有两个涂膜A和B的活性成分的颗粒制成的涂覆微粒来实现.A包括:不溶于胃肠道流体的成膜(共)聚合物(A1) 可溶于胃肠道液体的乙基纤维素(共)聚合物(A2); 增塑聚乙烯吡咯烷酮(A3); 蓖麻油/任选的表面活性剂和/或硬脂酸镁润滑剂(A4)。 B包含带有中性pH离子化的亲水性聚合物(B1)(EUDRAGIT L100-55)和疏水性化合物(B2)。本发明还涉及基于所述微粒的药物。