Determination and Data Correlation of Solubility of Sofosbuvir Polymorphs in Ethyl Acetate + Toluene and Methyl <i>tert</i>-Butyl Ether Binary Solvents at the Temperature Range from 268.15 to 308.15 K

A gravimetric method was used to experimentally determine the (solid + liquid) equilibrium of sofosbuvir of crystalline forms A and B in both ethyl acetate + toluene and methyl <i>tert</i>-butyl ether (MTBE) + toluene binary solvents systems at atmosphere pressure. Experiments were carri...

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Bibliographic Details
Main Authors: Wei-Jie Ji, En-Fu Wang, Ming-Hui Qi
Format: Article
Language:English
Published: MDPI AG 2020-03-01
Series:Crystals
Subjects:
Online Access:https://www.mdpi.com/2073-4352/10/3/209
Description
Summary:A gravimetric method was used to experimentally determine the (solid + liquid) equilibrium of sofosbuvir of crystalline forms A and B in both ethyl acetate + toluene and methyl <i>tert</i>-butyl ether (MTBE) + toluene binary solvents systems at atmosphere pressure. Experiments were carried out at a temperature range of 268.15&#8722;308.15 K. Results show that the solubility of sofosbuvir increases with temperature, and the solubility of form B was higher than that of form A. The modified Apelblat model, the CNIBS/Redlich&#8722;Kister model, and the combined version of Jouyban&#8722;Acree model were employed to correlate the measured solubility data, respectively. Furthermore, an examination of the solid-state stability of the two polymorphs was conducted, finding that form A and form B exhibit good solid-state stability under high temperature, high humidity, and strong light exposure conditions.
ISSN:2073-4352