降解型长效孕激素缓释注射埋植剂的制备方法

A method for the preparation of degradable long-acting progesterone sustained-release injectable implant

目的 :研究降解型长效孕激素缓释注射埋植剂的制备方法。方法 :以左旋聚乳酸及己内酯改性聚乳酸来调节含有孕激素微球的降解速率,以溶媒挥发法为制剂的制备方法。结果及结论 :经优化改良后,制得的制剂分散性好,二氯甲烷残留量符合国家药典标准,制剂体外释放实验结果表明,3个月后仍能稳定释放达40μg。

Objective： To establish a method for the preparation of degradable long-acting progesterone sustained- release injectable implant. Methods： The degradation rate of microspheres containing progesterone was regulated by poly-L- lactic acid and caprolactone-modified polylactic acid. The implant was prepared by solvent evaporation. Results： The prepared formulation showed an excellent dispensability and the residue of methylene chloride conformed to Chinese pharmacopoeia standard. The results of in vitro release of the formulation demonstrated that the stable release could be maintained at 40μg within three months.