论文部分内容阅读
目的:采用固体分散技术提高孕二烯酮的溶解度和体外溶出速率,制备21 d缓释孕二烯酮固体分散体阴道环并进行相关研究。方法:为了提高孕二烯酮自阴道环中的释放量,将其制备成固体分散体,采用差示扫描量热法(DSC)、红外光谱法(IR)和粉末X-射线衍射法(XRD)考察药物在固体分散体中的状态,并同时考察其体外溶出特性。本实验以道康宁硅橡胶为药物载体,采用热压硫化法制备阴道环,然后进行了体外释放研究并对释放曲线进行拟合。结果:制备的固体分散体大大提高了孕二烯酮的溶出速率,药物与载体的最佳比例为1:1。药物在分散体中以无定形状态存在。孕二烯酮固体分散体阴道环中药物的释放呈21d缓慢释放。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,从而提高孕二烯酮阴道环中药物的释放。
OBJECTIVE: To improve the solubility of gestrinone and dissolution rate of gestrinone by solid dispersion technique, and prepare the vaginal ring of GeDoderone solid dispersions for 21 days. Methods: In order to improve the release of gestodene from the vaginal rings, it was prepared as a solid dispersion by differential scanning calorimetry (DSC), infrared spectroscopy (IR) and powder X-ray diffraction ) To examine the state of the drug in the solid dispersion and to examine its in vitro dissolution characteristics at the same time. In this study, Dow Corning silicone rubber as the drug carrier, the preparation of the vaginal ring by hot pressing method, and then carried out in vitro release studies and release curve fitting. Results: The prepared solid dispersion greatly improved the dissolution rate of gestodene. The optimal ratio of drug to carrier was 1: 1. The drug is present in the amorphous state in the dispersion. Gestodene solid dispersion vaginal ring drug release was slow release 21d. Conclusion: The solid dispersion prepared by solvent method can significantly improve the dissolution rate of drugs and improve the release of drugs in the gestodene vaginal ring.