联苯双酯胃漂浮缓释胶囊的制备及体外释放度的考察

Preparation of floating sustained-release capsule of bifendate and its in vitro drug release

目的:制备联苯双酯胃漂浮缓释胶囊,进行体外释放度的考察。方法:采用聚乙二醇6 000为联苯双酯固体分散体的载体、羟丙甲纤维素(HPMCK4M)等为胃漂浮材料制成缓释胶囊,以体外释放度和漂浮时间为指标优选最佳处方,并与普通滴丸进行对比。利用差示扫描量热法(DSC)考察药物在载体中的存在状态。结果:所得优化处方在0.3%十二烷基硫酸钠(SDS)的盐酸(0.1mol.L-1)溶液中释放符合一级动力学方程,漂浮时间达6h以上。结论:所制备的胶囊体外漂浮性能良好,释药行为具有良好的缓释特征。

OBJECTIVE To prepare floating sustained-release capsule of bifendate （DDE） and evaluate its releasing features in vitro. METHODS The formulation of the floating sustained release capsule of bifendate was selected by design using PEG6000 as the carrier of solid dispersion, HPMC as the matrix. According to the dissolution rate and floating capacity, the orthogonal design method was used to optimize of floating sustained-release capsule of bifendate, and the differential scanning calorimeter （DSC） was used to identify the state of the drug existence. RESULTS The release profile of floating sustained-release capsule of bifendate in vitro fitted into first-order kinetics. The floating sustained-release capsule of bifendate could mainrain floating in vitro at least 6 hours. CONCLUSION The floating sustained-release capsule of bifendate possessed good floating and sustained-released property.