文献类型：期刊文献

英文题名：Cocrystals of Oxymatrine: Reducing Hygroscopicity and Affecting the Dissolution Rate

作者：Qi, Ming-Hui[1,2];Li, Heng[1,2];Zhu, Bin[1,2];Hong, Minghuang[1,2];Ren, Guo-Bin[2,3,4]

机构：[1]East China Univ Sci & Technol, Engn Res Ctr Pharmaceut Proc Chem, Minist Educ, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Lab Pharmaceut Crystal Engn & Technol, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[4]East China Univ Sci & Technol, Shanghai Key Lab New Drug Design & Engn, Res Ctr Pharmaceut Proc Chem, Minist Educ, Shanghai 200237, Peoples R China

年份：2021

卷号：21

期号：7

起止页码：3874

外文期刊名：CRYSTAL GROWTH & DESIGN

收录：;EI(收录号：20212610551104);WOS:【SCI-EXPANDED(收录号:WOS:000672584000023)】；

基金：This work was supported by the National Natural Science Foundation of China (Nos. 22078094, 21776073, and 21706064) and the Fundamental Research Funds for the Central Universities (No. 222201814049).

语种：英文

外文关键词：Dissolution - Hydrogen bonds - Metabolism

摘要：Oxymatrine (OMT) is mainly used for the treatment of hepatitis B. In this work, one anhydrous form and three hydrates of OMT are reported and their transformational relationship is clarified. It is revealed that OMT has high hygroscopicity and fast release characteristics. In order to improve these physical properties, cocrystallization of OMT was performed. Five cocrystals of OMT with urea (OMT-Urea-DH), sulfanilamide (OMT-SUA), theophylline (OMT-THP), 2-ketoglutaric acid (OMT-KTA-MH), and 3-hydroxy- 2- naphthoic acid (OMT-HNA) were obtained and characterized. According to the DVS tests, OMT-SUA, OMT-KTA-MH, and OMT-HNA enhance the hydroscopic stability of OMT by forming new hydrogen bonds. The dissolution rate of OMT has been drastically reduced through cocrystallization with THP and HNA.