琥珀酸美托洛尔缓释微囊的制备和体外释药

 目的 探讨琥珀酸美托洛尔缓释微囊的制备工艺。方法 以乙基纤维素作为囊材,采用乳化-溶剂扩散法,应用均匀设计优化处方和制备工艺,并研究其体外释药特性。结果 在优化条件下制备的琥珀酸美托洛尔缓释微囊,外形圆整光滑,分布均匀,不粘连,平均粒径为80~90 μm,包封率达83.16%,18 h体外释放百分率为96.1%。结论 优化条件下可制备的缓释微囊外观较好、包封率高,在体外具有良好的缓释效果。

Preparation and in Vitro Release Evaluation of Metoprolol Succinate Sustained-Release Microcapsules

OBJECTIVE To prepare sustained-release microcapsules of metoprolol succinate（MS） and to investigate the influencing factors. METHODS The sustained-release microcapsules of metoprolol succinate were prepared with ethyl cellulose（EC） in one step by the emulsion-solvent diffusion method. Uniform design was used to optimize the formulation and preparation technique. Its release behavior in vitro was studied. RESULTS All microcapsules prepared under the optimum condition were spherical and smooth with the mean particle size in the range of 80-90 μm. The entrapment efficiency was 83.16% and drug release from the MS microcapsules during 18 h reached 96.1% in vitro. CONCLUSION The microcapsules have good morphological characteristics, high entrapment efficiency and sustained-release effect in vitro.