Solubility Measurement of Crystal Form II and Form V Ticagrelor in Several Pure Organic Solvents

被引:5
作者
Yang, Shunping [1 ]
Wu, Yanfang [1 ]
Zhang, Hao [1 ]
Sun, Jin [1 ]
Liu, Yan [1 ]
机构
[1] East China Univ Sci & Technol, Sch Pharm, Minist Educ, Engn Res Ctr Pharmaceut Proc Chem, Shanghai 200237, Peoples R China
关键词
CLOPIDOGREL HYDROGEN SULFATE; ERLOTINIB HYDROCHLORIDE; METASTABLE POLYMORPH; WATER; ISOPROPANOL;
D O I
10.1021/acs.jced.0c01073
中图分类号
O414.1 [热力学];
学科分类号
摘要
Ticagrelor (TCG) is a P2Y(12) platelet inhibitor and has several crystal forms including Form II and Form V. In this work, it has been confirmed that Form II TCG would gradually transform to Form V in selected solvents. According to the crystal form stability, a dynamic method was adopted to measure the solubility of Form II TCG in six pure solvents (n-propanol, isopropanol, n-butanol, 2-butanol, ethyl acetate, and isopropyl acetate). The solubility of Form V TCG in 12 pure solvents (methanol, ethanol, n-propanol, isopropanol, n-butanol, 2-butanol, methyl acetate, ethyl acetate, isopropyl acetate, acetone, 2-butanone, and cyclohexanone) was measured by a static method. The solubility measurement temperature range was from 273.15 to 313.15 K. The experimental solubility data were correlated by the modified Apelblat model and the lambda h model. It was shown that the calculated solubility was consistent with the experimental data.
引用
收藏
页码:2022 / 2033
页数:12
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