雷永, 陆彬. 避孕药微球制备工艺的研究J. 药学学报, 1993, 28(4): 296-301.
引用本文: 雷永, 陆彬. 避孕药微球制备工艺的研究J. 药学学报, 1993, 28(4): 296-301.
Y Lei, BLu. STUDIES ON PREPARATION TECHNOLOGY OF MICROSPHERFS OF CONTRACEPTIVESJ. Acta Pharmaceutica Sinica, 1993, 28(4): 296-301.
Citation: Y Lei, BLu. STUDIES ON PREPARATION TECHNOLOGY OF MICROSPHERFS OF CONTRACEPTIVESJ. Acta Pharmaceutica Sinica, 1993, 28(4): 296-301.

避孕药微球制备工艺的研究

STUDIES ON PREPARATION TECHNOLOGY OF MICROSPHERFS OF CONTRACEPTIVES

  • 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(E2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。

     

    Abstract: Contraceptive poly ethylglycol- lactide (PEGL), an artificial biodegradable polymer microsphere was prepared by a solvent evaporation process using levonorgestrel (LNG) and estradiol (E2) 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.

     

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