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目的:制备利培酮长效注射微球并考察其体外释放行为。方法:使用乳酸-羟基乙酸共聚物(PLGA)为材料,采用乳化-溶剂挥发法制备利培酮微球,观察微球的形态及粒径,测定微球的载药量和包封率,考察微球的体外释放情况。结果:利培酮微球表面圆整,粒径集中在40～80μm之间。微球的包封率较高,达到80%以上,以低分子量PLGA(50:50)制备的微球,体外突释很高达到40%以上;以高分子量PLGA(75:25)制备的微球,在高载药量时突释较小,可持续释放达3周以上。结论:以高分子量PLGA制备的高载药量的利培酮微球,体外突释较小可缓释达3周以上。
OBJECTIVE: To prepare long-acting injection microspheres of risperidone and investigate its in vitro release behavior. Methods: Risperidone microspheres were prepared by emulsion-solvent evaporation method using lactic acid-glycolic acid copolymer (PLGA) as the material. Morphology and particle size of the microspheres were observed. The drug loading and entrapment efficiency of the microspheres were measured. In vitro release of microspheres. Results: The surface of risperidone microspheres was round and the particle size was concentrated in the range of 40 ~ 80μm. The encapsulation efficiency of microspheres was higher than 80%, and the microspheres prepared with low molecular weight PLGA (50:50) had a high in vitro release rate of over 40%. The microspheres prepared by high molecular weight PLGA (75:25) The ball, in the high drug dose burst release smaller, sustainable release for more than 3 weeks. Conclusion: The high drug loading risperidone microspheres prepared by high molecular weight PLGA can be slowly released for more than 3 weeks.