乳化溶剂扩散法制备酮洛芬肠溶微球

Preparation of enteric ketoprofen microspheres by emulslon-solvent diffusion method

目的制备酮洛芬肠溶微球,并对其制备工艺进行考察。方法采用紫外分光光度法建立了微球的载药量及体外释放度测定方法。采用乳化溶剂扩散法制备酮洛芬肠溶微球,以载药量、包封率及微球外观为指标进行单因素考察优化处方,并以优化处方制备的微球进行体外溶出实验。结果最优处方下制得微球外观圆整,粒径较均匀,载药量与包封率分别为25.86%和45.09%,酮洛芬肠溶微球在人工胃液中2h释药百分率低于10%,在人工肠液中70min释放可达90%。结论该法制备工艺简单,可得到球形度好、粒径分布均匀的酮洛芬肠溶微球,并且微球在人工胃液中释放较少,在人工肠液中释放较快。

Objective To prepare ketoprofen microspheres and investigate the preparation process.Methods Drug loading and drug release in vitro of ketoprofen microspheres were determined using UV detector.The ketoprofen microspheres were prepared by emulsion-solvent diffusion method,and the drug loading,encapsulation efficiency and appearance were evaluated.The drug release in vitro of optimized microspheres was investigated.Results The microspheres were spherical and smooth in appearance;the particle size distribution was uniform.The drug loading and encapsulation efficiency of optimized preparation were found to be 25.86% and 45.09%,respectively.The cumulative drug release in simulated gastric fluid is less than 10% within 2 h,while it is more than 90% after 70 min in simulated intestinal fluid.Conclusion This preparation method is simple;the ketoprofen microspheres have spherical surface and uniform particle size distribution.The results of drug release in vitro reveal that the release rate of ketoprofen microspheres in simulated gastric fluid was slow,but it was fast in simulated intestinal fluid.