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COMPOSITION AND METHOD OF PRODUCTION OF NANOPARTICULATED SYSTEMS FOR MODIFIED RELEASE OF BENZNIDAZOLE

机译:苯达唑修饰释放的纳米微粒体系的组成和生产方法

摘要

The invention relates to the composition and method of preparing nanoparticulate systems for modified release of benznidazole (n-benzyl-2- (2-nitroimidazol-1-yl) acetamide), which are in the form of polymeric nanoparticles based on polymers such as methacrylic acid derivatives (eudragit® r100, e100), poly (lactic acid) (pla), poly (lactic-co-glycolic acid) (plga) or lipids, and may have the surface of the particles functionalized with cationic agents, sialic acid, cholesterol or other molecules. These systems obtained by the solvent displacement / nanoprecipitation and / or solvent evaporation emulsification method, in order to enable oral and / or parenteral administration, modifying the bioavailability of the drug in relation to the available forms of administration, being efficient for the treatment. in the chronic phase of Chagas disease that allows to overcome natural biological barriers, which act in directing the drug to the infected cells and / or the parasite.
机译:本发明涉及组合物和制备用于改进释放苯并硝唑(n-苄基-2-(2-硝基咪唑-1-基)乙酰胺)的纳米颗粒体系的组合物和方法,其为基于诸如甲基丙烯酸的聚合物的聚合物纳米颗粒的形式酸衍生物(eudragit®r100,e100),聚乳酸(pla),聚乳酸-乙醇酸(plga)或脂质,并且颗粒表面可能被阳离子试剂,唾液酸官能化,胆固醇或其他分子。通过溶剂置换/纳米沉淀和/或溶剂蒸发乳化方法获得的这些系统,以便能够口服和/或肠胃外给药,相对于可用的给药形式改变药物的生物利用度,对于治疗是有效的。在查加斯病的慢性阶段,它可以克服自然的生物屏障,这种屏障可以将药物导向感染的细胞和/或寄生虫。

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