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Crystals 2019, 9(3), 161; https://doi.org/10.3390/cryst9030161

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

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
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Received: 2 March 2019 / Accepted: 13 March 2019 / Published: 20 March 2019
(This article belongs to the Special Issue Pharmaceutical Crystals)
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Abstract

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. View Full-Text
Keywords: famoxadone; solvent-mediated polymorphic transformation; hydrogen-bond-acceptance ability famoxadone; solvent-mediated polymorphic transformation; hydrogen-bond-acceptance ability
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Du, D.; Ren, G.-B.; Qi, M.-H.; Li, Z.; Xu, X.-Y. Solvent-Mediated Polymorphic Transformation of Famoxadone from Form II to Form I in Several Mixed Solvent Systems. Crystals 2019, 9, 161.

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