米非司酮固体分散体的制备及性质研究

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.%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.