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尼美舒利聚乳酸微球作为一种治疗炎症性疾病的潜在缓释系统。

Nimesulide PLA microspheres as a potential sustained release system for the treatment of inflammatory diseases.

作者信息

Freitas M N, Marchetti J M

机构信息

Laboratory of Pharmaceutical Technology, Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Av. do Café s/n, 14040-903 Ribeirão Preto, SP, Brazil.

出版信息

Int J Pharm. 2005 May 13;295(1-2):201-11. doi: 10.1016/j.ijpharm.2005.03.003.

Abstract

Polylactic acid (PLA-L) microspheres were prepared as a biodegradable polymeric carrier for a non-steroidal anti-inflammatory drug, nimesulide. The preparation of this system was performed by the classical emulsion solvent-evaporation method. Size analysis of the microparticulate system showed that unloaded and loaded nimesulide-PLA microspheres had average diameters of about 42.9 nm and 2.1 microm, respectively. Scanning electron microscopy (SEM) of loaded and unloaded microsphere samples showed that the particles shape were perfectly spherical, the loading efficiency of nimesulide in PLA microspheres was 70%; Thus, the microparticle system evaluated in this work showed the potential to act as a sustained release system for nimesulide: in vitro dissolution profiles showed the PLA-L microparticles were able to sustain the release of the drug for a considerable period of time (28.7% within 108 h).

摘要

聚乳酸(PLA-L)微球被制备为一种用于非甾体抗炎药尼美舒利的可生物降解聚合物载体。该体系的制备采用经典的乳液溶剂蒸发法。微粒体系的尺寸分析表明,未负载和负载尼美舒利的PLA微球的平均直径分别约为42.9纳米和2.1微米。对负载和未负载微球样品的扫描电子显微镜(SEM)显示,颗粒形状为完美球形,尼美舒利在PLA微球中的负载效率为70%;因此,本研究中评估的微粒体系显示出作为尼美舒利缓释体系的潜力:体外溶出曲线表明PLA-L微颗粒能够在相当长的一段时间内维持药物释放(108小时内释放28.7%)。

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