孕二烯酮缓释微针给药形式的处方前研究  

Research of dosage form of microneedle sustained released gestodene before prescription

作　　者：马佳男 宁美英 段雪艳 MA Jianan;NING Meiying;DUAN Xueyan(Centre of Drug and Medical Polymer Materials, Nationals Research Institute for Family Planning, Beijing, 100081;Graduate School of Peking Union Medical College)

机构地区：[1]国家卫生计生委科学技术研究所药物和医用材料研究中心,北京100081 [2]北京协和医学院研究生院

出　　处：《中国计划生育学杂志》2017年第12期832-837,共6页Chinese Journal of Family Planning

基　　金：中央级公益性科研院所基本科研业务费专项(2015GJZ06);2016年国家重点研发计划重点项目(2016YFC1000902)

摘　　要：目的:通过将孕二烯酮(GEST)制备成固体分散体,提高其溶解度和体外溶出速率,达到微针持续7d缓慢释放的要求,为GEST缓释微针的处方设计提供研究基础。方法:以聚乙烯吡咯烷酮(PVPK30)为载体,溶剂法制备GEST固体分散体,考察其体外溶出特性。同时采用红外光谱法(IR)、X-射线粉末衍射法(XRD)和差示扫描热量法(DSC)考察药物在固体分散体中的存在状态。并对GEST固体分散体制备的微针进行体外透皮释放试验。结果:固体分散体技术大大提高了GEST的溶出速率,最佳比例为1:4。GEST缓释微针透皮释放试验中固体分散体的平均释药速率为23.97μg/cm^2,原料药的为4.48μg/cm^2,固体分散体的平均释药速率大于原料药。结论:固体分散体技术能显著提高GEST的溶出速率,从而提高药物在微针给药系统中的释放速率。Objective：To achieve the slow releasing gestodene of microneedles for 7 days by increased the solubility and in vitro dissolution rate under solid dispersion technique,and to provide research evidence for designing dosage form of microneedle sustained released gestodene before prescription.Methods：The solid dispersion was prepared by the solvent evaporation method with PVPK30 as the carrier,and the in vitro dissolution characteristics of gestodenePVPK30 solid dispersion was determined by IR spectra,X-ray powder diffraction and DSC.And the in vitro transdermal release test was performed on the microneedles prepared by the gestodene solid dispersion.Results：The dissolution rate of gestodene was improved when it was dispersed in solid dispersion.The best proportion of solid dispersion was 1：4.The average release rate of the solid dispersion in the transdermal release test of gestodene sustained-release microneedles was about 23.97μg/cm^2,which was much greater than that of the drug whose average release rate was4.48μg/cm^2.Conclusion：The solid dispersion can improve the dissolution rate of gestodene significantly,which can improve the drug release from microneedle delivery system.

关 键 词：孕二烯酮 固体分散体 微针 

分 类 号：R943[医药卫生—药剂学]