避孕药微球制备工艺的研究  

STUDIES ON PREPARATION TECHNOLOGY OF MICROSPHERFS OF CONTRACEPTIVES

作　　者：雷永[1] 陆彬[1] 

机构地区：[1]华西医科大学药学院

出　　处：《药学学报》1993年第4期296-301,共6页Acta Pharmaceutica Sinica

基　　金：国家计划生育委员会资助

摘　　要：采用可生物降解醚酯嵌段共聚物poly(ethylglycol—lactide)(简称PEGL)为载体,以溶剂蒸发法制备了避孕药左旋18-甲基炔诺酮(LNG)和雌二醇(E_2的PEGL微球。筛选出最佳制备微球的工艺,微球的平均容积径约为30μm,包封率为75～82%。体外释药试验结果表明,避孕药微球能减慢主药的释放,且其释放速度随载药量的降低而减慢。避孕药微球可使小鼠抗生育时间维持6个月以上,证实该微球具有缓释延效的作用。Contraceptive poly ethylglycol- lactide (PEGL), an artificial biodegradable polymer microsphere was prepared by a solvent evaporation process using levonorgestrel (LNG) and estradiol (E_2) as model drugs and PEGL as the core material. The experimental conditions were optimized, the mean volume diameter obtained being 30 μm and rate of encapsulation 75～82%. In vitro, it was found that the drug release rate decreased with decreasing drug content in the microspheres. The microspheres of the contraceptive maintained anticonception duration in mice for over 6 months, indicating that the microspheres have remarkablely long acting sustained release action.

关 键 词：避孕药 缓释给药系统 雌二醇 

分 类 号：TQ460.6[化学工程—制药化工]