Solvent-Mediated Polymorphic Transformation of Famoxadone from Form II to Form I in Several Mixed Solvent Systems
Dan Du,
Guo-Bin Ren,
Ming-Hui Qi,
Zhong Li,
Xiao-Yong Xu
Affiliations
Dan Du
Shanghai Key Laboratory of Chemical Biology, Laboratory of Pharmaceutical Crystal Engineering & Technology, School of Pharmacy, East China University of Science and Technology, No. 130, MeiLong Road, XuHui District, Shanghai 200237, China
Guo-Bin Ren
Shanghai Key Laboratory of Chemical Biology, Laboratory of Pharmaceutical Crystal Engineering & Technology, School of Pharmacy, East China University of Science and Technology, No. 130, MeiLong Road, XuHui District, Shanghai 200237, China
Ming-Hui Qi
Shanghai Key Laboratory of Chemical Biology, Laboratory of Pharmaceutical Crystal Engineering & Technology, School of Pharmacy, East China University of Science and Technology, No. 130, MeiLong Road, XuHui District, Shanghai 200237, China
Zhong Li
Shanghai Key Laboratory of Chemical Biology, Laboratory of Pharmaceutical Crystal Engineering & Technology, School of Pharmacy, East China University of Science and Technology, No. 130, MeiLong Road, XuHui District, Shanghai 200237, China
Xiao-Yong Xu
Shanghai Key Laboratory of Chemical Biology, Laboratory of Pharmaceutical Crystal Engineering & Technology, School of Pharmacy, East China University of Science and Technology, No. 130, MeiLong Road, XuHui District, Shanghai 200237, China
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 °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.
