【摘要】 目的:以聚乳酸-羟基乙酸共聚物(poly(lactic-co-glycolic acid),PLGA)为载体,采用乳化溶剂挥发法制备猴头菌素缓释微球,并对其体外药物释放行为进行考察。方法:通过单因素试验,以包封率为评价指标,考察影响微球质量的因素,采用响应面试验法进行优化,筛选出最佳工艺条件。结果:最佳工艺为芯壁比(猴头菌素与PLGA质量比)1∶1.64、PLGA质量分数15%、搅拌速率1 200 r/min。最佳条件制备的猴头菌素微球表面光滑圆整,包封率为99.66%,微球体外384 h累计释放率达84.30%。结论:以PLGA为载体材料,采用乳化-溶剂挥发法可以制备包封率较高的猴头菌素微球,体外释药实验也表明该微球具有明显的缓释作用。更多还原

【Abstract】 Purpose: To prepare slow-release erinacines microspheres with poly(lactic-co-glycolic acid)(PLGA) as carry using the emulsification solvent evaporation method and to investigate their release characteristics in vitro. Methods: The one-factor-at-a-time method was adopted to examine the factors affecting encapsulation efficiency, and their levels were optimized using response surface methodology. Results: The optimum preparation conditions were obtained as follows: erinacines to PLGA ratio, 1:1.64(g/g); concentration of PLGA in dichloromethane, 15%; and stirring speed, 1 200 r/min. The obtained microspheres were complete and smooth with an encapsulation efficiency of 99.66% and a cumulative release rate in vitro of 84.30% in 384 h. Conclusion: The emulsification solvent evaporation method has been successfully applied to prepare erinacines microspheres with high entrapment efficiency and good sustained release performance.更多还原