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烟酸微球的设计与评价

Design and evaluation of niacin microspheres.

作者信息

Maravajhala Vidyavathi, Dasari Nirmala, Sepuri Asha, Joginapalli S

机构信息

Institute of Pharmaceutical Technology, Sri Padmavati Mahila Visvavidyalayam (Women's University), Tirupati-517502, India.

出版信息

Indian J Pharm Sci. 2009 Nov;71(6):663-9. doi: 10.4103/0250-474X.59549.

Abstract

Present study aims to prepare and evaluate niacin microspheres. Niacin-ethyl cellulose microspheres were prepared by water-in-oil-in-oil double emulsion solvent diffusion method. Spherical, free flowing microspheres having an entrapment efficiency of 72% were obtained. The effect of polymer-drug ratio, surfactant concentration for secondary emulsion process and stirring speed of emulsification process were evaluated with respect to entrapment efficiency, in vitro drug release behavior and particle size. FT-IR and DSC analyses confirmed the absence of drug-polymer interaction. The in vitro release profile could be altered significantly by changing various processing and formulation parameters to give a controlled release of drug from the microspheres. The percentage yield was 85%, particle size range was 405 to 560 mum. The drug release was controlled for 10 h. The in vitro release profiles from optimized formulations were applied on various kinetic models. The best fit with the highest correlation coefficient was observed in Higuchi model, indicating diffusion controlled principle. The in vitro release profiles of optimized formulation was studied and compared with commercially available niacin extended release formulation.

摘要

本研究旨在制备并评估烟酸微球。采用油包水包油双乳液溶剂扩散法制备了烟酸-乙基纤维素微球。获得了包封率为72%的球形、自由流动的微球。针对包封率、体外药物释放行为和粒径,评估了聚合物与药物的比例、二次乳化过程中表面活性剂的浓度以及乳化过程中的搅拌速度的影响。傅里叶变换红外光谱(FT-IR)和差示扫描量热法(DSC)分析证实不存在药物-聚合物相互作用。通过改变各种工艺和制剂参数,可以显著改变体外释放曲线,从而实现药物从微球中的控释。产率为85%,粒径范围为405至560微米。药物释放控制了10小时。将优化制剂的体外释放曲线应用于各种动力学模型。在Higuchi模型中观察到与最高相关系数的最佳拟合,表明为扩散控制原理。研究了优化制剂的体外释放曲线,并与市售烟酸缓释制剂进行了比较。

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