格列吡嗪缓释微球的制备及释药特性考察

摘要

目的 采用球晶造粒技术制备格列吡嗪缓释微球并考察体外释药特性.方法 以乙基纤维素和水溶性高分子材料聚乙二醇6000为载体,采用球晶造粒技术制备格列吡嗪缓释微球,对微球的形状、粒径分布、载药量、包封率和体外释药等进行了考察.结果 该法所制微球外观圆整、流动性好,粒度分布在40～190 μm内的微球占总数的99％,载药量为35.6％,包封率为89.5％,体外释药行为符合Higuchi方程,24h累计释药量96％.结论 该法可用于制备格列吡嗪缓释微球.%Objective To prepare glipizide sustained-release microspheres using spherical crystallization technique and to observe their in vitro drug release. Methods The spherical crystallization technique was used to prepare glipizide sustained-release microspheres with ethyl cellulose (EC) and water soluble material of PEC 6000. The characteristics such as conformation, particle size distribution, drug loading, incorporation efficiency and in vitro release of microspheres were observed. Results The preparation method was favorable, which was manifested by round appearance, good flowability, the diameters of 99% microspheres in the range of 40-190 μm, durg loading being 35.6% and incorporation efficiency being 89.5%, in vitro release behavior consistent with Higuchi equation, and drug release being 96% within 24 h. Conclusion This method could be used to prepare glipizide sustained-release micro-spheres.