期刊
STEROIDS
卷 159, 期 -, 页码 -出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.steroids.2020.108649
关键词
Mifepristone; Polymorphism; Solvent-free polymorph; Solubility; Dissolution; Oral bioavailability
资金
- CAMS Innovation Fund for Medical Sciences (CIFMS), China [2018-I2M-1-004]
- Non-profit Central Research Institute Fund of National Research Institute For Family Planing, China [2019GJZ01]
Mifepristone is one of potent anti-progesterone agents, which binds to progesterone receptors and glucocorticoid receptors. Until now, there are a lot of research focusing on enhancing the solubility and oral bioavailability of Mifepristone. However, poor solubility and oral bioavailability has some undesirable consequences. In this work, Mifepristone in form D was discovered for the first time and characterized by PXRD, TGA, DSC, FT-IR, SEM and S-S NMR. Form D was a metastable crystal type which manifested favorable stability under ambient conditions. Form D had better dissolution characteristic compared with commercial Mifepristone in 0.5% SDS solution. In addition, Mifepristone in form D exhibited a 1.43-fold higher peak plasma concentration (C-max) and 1.46-fold higher area under the curve (AUC) in rats. The work in this paper is a complement to the present understanding of drug polymorphism on the in vitro and in vivo behavior, and establishes the ground work for future development of Mifepristone in form D as a promising drug for the market.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据