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可生物降解的聚(D,L-丙交酯-co-乙交酯)(PLGA)微球用于利培酮的持续释放:零级释放配方。

Biodegradable poly(D, L-lactide-co-glycolide) (PLGA) microspheres for sustained release of risperidone: Zero-order release formulation.

机构信息

College of Life Science, Jilin University, Changchun, China.

出版信息

Pharm Dev Technol. 2011 Aug;16(4):377-84. doi: 10.3109/10837451003739297. Epub 2010 Apr 7.

Abstract

The preparation and investigation of sustained-release risperidone-encapsulated microspheres using erodible poly(D, L-lactide-co-glycolide) (PLGA) of lower molecular weight were performed and compared to that of commercial Risperdal Consta™ for the treatment of schizophrenia. The research included screening and optimizing of suitable commercial polymers of lower molecular weight PLGA50/50 or the blends of these PLGA polymers to prepare microspheres with zero-order release kinetics properties. Solvent evaporation method was applied here while studies of the risperidone loaded microsphere were carried out on its drug encapsulation capacity, morphology, particle size, as well as in vitro release profiles. Results showed that microspheres prepared using 50504A PLGA or blends of 5050-type PLGAs exerted spherical and smooth morphology, with a higher encapsulation efficiency and nearly zero-order release kinetics. These optimized microspheres showed great potential for a better depot preparation than the marketed Risperdal Consta™, which could further improve the patient compliance.

摘要

采用低分子量可蚀性聚(D,L-丙交酯-共-乙交酯)(PLGA)对利培酮进行包封微球的制备和研究,并与商业的利培酮长效注射剂(Risperdal Consta)进行比较,以治疗精神分裂症。研究包括筛选和优化合适的低分子量商业聚合物 PLGA50/50 或这些 PLGA 聚合物的混合物,以制备具有零级释放动力学特性的微球。本文采用溶剂蒸发法,研究了载利培酮微球的药物包封能力、形态、粒径以及体外释放曲线。结果表明,采用 50504A PLGA 或 50 型 PLGA 混合物制备的微球呈球形且表面光滑,包封效率较高,接近零级释放动力学。与市售的利培酮长效注射剂(Risperdal Consta)相比,这些优化后的微球具有更好的长效制剂潜力,可进一步提高患者的顺应性。

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