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米非司酮固体分散体的制备及性质研究
引用本文:陈凯,段雪艳,刘颖,张莹,王佳庆,李青山,宁美英.米非司酮固体分散体的制备及性质研究[J].中国新药杂志,2012(14):1681-1685,1693.
作者姓名:陈凯  段雪艳  刘颖  张莹  王佳庆  李青山  宁美英
作者单位:山西医科大学药学院;国家人口计生委科学技术研究所药物与医用材料研究中心
摘    要:目的:增加米非司酮的溶解度和体外溶出速率,为阴道环的成功制备奠定基础。方法:以PVPK30为载体,采用溶剂法制备米非司酮固体分散体。考察其体外溶出特性,并采用差示扫描量热法、红外光谱法和粉末X-射线衍射法鉴别药物在固体分散体中的存在状态。结果:固体分散体大大提高了米非司酮的溶出速率,最佳比例为1∶3。药物在分散体中以无定型状态存在。结论:溶剂法制备的固体分散体可显著提高药物的溶出速率,从而提高了阴道环中药物的释放量。

关 键 词:米非司酮  固体分散体  溶出速率  阴道药环

Studies on preparation and dissolution of mifepristone solid dispersion
CHEN Kai,DUAN Xue-yan,LIU Ying,ZHANG Ying,WANG Jia-qing,LI Qing-shan,NING Mei-ying.Studies on preparation and dissolution of mifepristone solid dispersion[J].Chinese Journal of New Drugs,2012(14):1681-1685,1693.
Authors:CHEN Kai  DUAN Xue-yan  LIU Ying  ZHANG Ying  WANG Jia-qing  LI Qing-shan  NING Mei-ying
Institution:1 School of Pharmaceutical Sciences,Shanxi Medical University,Taiyuan 030001,China;2 Centre of Drugs and Medical Polymer Materials,National Research Institute for Family Planning,Beijing 100081,China)
Abstract:Objective:To improve the solubility and dissolution rates of mifepristone,and for the success of mifepristone intravaginal ring preparation.Methods:The solid dispersion was prepared by the solvent evaporation method with PVPK-30 as the carrier and the vitro dissolution characteristics of mifepristone-PVPK30 solid dispersion was determined by IR spectra,DSC and powder X-ray diffraction.Results:The dissolution rate of mifepristone was improved when it was dispersed in solid dispersion.The best proportion of solid dispersion was 1∶3.Mifepristone exists as an amorphous state.Conclusion:The solid dispersion prepared by the solvent evaporation method could improve the dissolution rates of RU486 significantly and improve the RU486 release from the intravaginal ring.
Keywords:mifepristone  solid dispersion  dissolution rate  intravaginal ring
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