吲哚美辛微球的制备及其包封率和释放性能

Preparation,entrapment efficiency,and release property of indomethacin microspheres

背景:吲哚美辛在眼内半衰期短,需要多次给药才能达到治疗作用。目的:制备吲哚美辛微球,并分析其包封率及缓释性能。方法:选择安全性好的聚乳酸-羟基乙酸共聚物和聚丙烯酸树脂类两种共聚物作为载体材料,以乳化溶剂挥发法制备含吲哚美辛微球,分析不同有机溶剂(二氯甲烷、丙酮)、不同载体材料比例、不同pH值及不同渗透压因素对微球包封率和体外释放性能的影响。结果与结论:微球表面光滑圆整,无孔,粒径分布表现出多分散性,粒径2.0～3.0μm。制备过程中发现,有机溶剂使用二氯甲烷、载体材料聚乳酸-羟基乙酸共聚物:聚丙烯酸树脂类的质量比例越小、水相中pH值越低、渗透压越低,载药微球的包封率越大。在聚乳酸-羟基乙酸共聚物:聚丙烯酸树脂类的质量比为1:3时,包封率最高,体外释放速率最慢。

BACKGROUND：Indomethacin requires multiple doses to achieve treatment effect because of its short half-life in ocular.OBJECTIVE：To prepare indomethacin microspheres and analyze its entrapment efficiency and release property.METHODS：Indomethacin microspheres were prepared by emulsion solvent evaporation using poly lactic acid-glycolic acid copolymer and polyacrylic acid resin based on their good safety.The influences of preparation parameters on encapsulation efficiency and release property were investigated,such as different organic solvent（dichlormethane,acetone）,different proportions of polymer,different pH values and osmotic pressures.RESULTS AND CONCLUSION：The microspheres were spherical shape with a smooth and imperforation surface,and had fine dispersibility at a diameter of 2-3 μm.The dichloromethane,lower weight of polyacrylic acid resin,lower pH and osmotic pressure in water medium could result in higher entrapment efficiency.The entrapment efficiency was the highest and the release rate was the slowest at 1：3 of poly lactic acid-glycolic acid copolymer and polyacrylic acid resin.