文献类型：期刊文献

英文题名：Solvent-Mediated Polymorphic Transformation of Famoxadone from Form II to Form I in Several Mixed Solvent Systems

作者：Du, Dan[1];Ren, Guo-Bin[1];Qi, Ming-Hui[1];Li, Zhong[1];Xu, Xiao-Yong[1]

机构：[1]East China Univ Sci & Technol, Lab Pharmaceut Crystal Engn & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, 130 MeiLong Rd, Shanghai 200237, Peoples R China

年份：2019

卷号：9

期号：3

外文期刊名：CRYSTALS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000464476400003)】；

基金：This work was supported by the National Key Research Program of China (No. 2017YFD0200505), the National Natural Science Foundation of China (No. 21706064), and the Fundamental Research Funds for the Central Universities (No. 222201718004, No. 222201814049).

语种：英文

外文关键词：famoxadone; solvent-mediated polymorphic transformation; hydrogen-bond-acceptance ability

摘要：This paper discloses six polymorphs of famoxadone obtained from polymorph screening, which were characterized by XRPD, DSC, and SEM. A study of solvent-mediated polymorphic transformation (SMPT) of famoxadone from the metastable Form II to the stable Form I in several mixed solvent systems at the temperature of 30 degrees C was also conducted. The transformation process was monitored by Process Analytical Technologies. It was confirmed that the Form II to Form I polymorphic transformation is controlled by the Form I growth process. The transformation rate constants depended linearly on the solubility difference value between Form I and Form II. Furthermore, the hydrogen-bond-donation/acceptance ability and dipolar polarizability also had an effect on the rate of solvent-mediated polymorphic transformation.