阿立哌唑缓释微球的制备及体外释放特性的研究

Preparation of Aripiprazole sustained-release microspheres and study on its in vitro release characteristics

目的制备阿立哌唑聚乳酸-羟基乙酸共聚物(PLGA)缓释微球并考察其体外释放特性。方法采用乳化-溶剂挥发法制备阿立哌唑缓释微球,通过正交试验优选最佳处方与制备工艺,并考察其载药量、包封率、粒径、形态和体外释放度。结果所得微球的载药量为20.28%±0.38%,包封率为81.12%±0.02%,平均粒径为19.38μm,形态圆整,30 d的体外累积释放度达88.73%。结论所得阿立哌唑缓释微球形态圆整,载药量与包封率较高,具较好的缓释效果。

OBJECTIVE To prepare Aripiprazole polylactic-co-glycolic acid（ PLGA） sustained-release microspheres and study on its release in vitro. METHODS PLGA microspheres loading Aripiprazole were prepared by emulsion-solvent evaporation method.The optimum preparation was selected with orthogonal experiments. The indicators were evaluated using loading efficiency,entrapment efficiency,particle size,morphology and the in vitro release characteristics. RESULTS The drug loading was 20. 28% ± 0. 38%,and the encapsulation efficiency was 81. 12% ± 0. 02%. The volume average particle size was 19. 38 μm and the microsphere was generally spherical. The microspheres release was 88. 73% in vitro for 30 days. CONCLUSION Aripiprazole PLGA microspheres have high loading efficiency,entrapment efficiency and sustained release characteristics.