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目的:制备塞来昔布的乳酸-羟基醋酸共聚物[Poly(lactide-co-glycolide),PLGA]缓释微球,并评价其在体外释药特征。方法:采用乳化-溶剂挥发法制备微球。用正交设计考察影响微球性质的工艺条件。以微球的粒径,载药量,包封率和体外释放特征为指标,对微球的质量进行考察。结果:微球外观圆整,表面光滑,平均粒径为1.5μm,载药量为(8.7±0.3)%,包封率为(94.90±0.20)%。其体外释药曲线可用Higuchi方程拟合,40d累积释药达69.1%。结论:制备方法可行,塞来昔布PLGA微球形态完整,体外释放有良好的缓释效果。
OBJECTIVE: To prepare celecoxib poly (lactide-co-glycolide) (PLGA) sustained release microspheres and evaluate its in vitro release characteristics. Methods: The microspheres were prepared by emulsion-solvent evaporation method. Orthogonal design was used to investigate the process conditions affecting the microsphere properties. The microsphere size, drug loading, encapsulation efficiency and in vitro release characteristics as an indicator of the quality of microspheres were investigated. Results: The microspheres were round in appearance and smooth in surface. The average diameter of the microspheres was 1.5 μm. The drug loading was (8.7 ± 0.3)% and the entrapment efficiency was (94.90 ± 0.20)%. Its in vitro release curve fitting Higuchi equation, 40d cumulative release of up to 69.1%. Conclusion: The preparation method is feasible. The morphology of celecoxib PLGA microspheres is intact and release in vitro has a good sustained-release effect.