文献类型：期刊文献

英文题名：Solid-State Characterization and Insight into Transformations and Stability of Apatinib Mesylate Solvates

作者：Zhu, Bin[1];Zhang, Qi[3];Ren, Guobin[1,2];Mei, Xuefeng[3]

机构：[1]East China Univ Sci & Technol, Lab Pharmaceut Crystal Engn & Technol, Sch Pharm, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai 200237, Peoples R China;[3]Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China

年份：2017

卷号：17

期号：11

起止页码：5994

外文期刊名：CRYSTAL GROWTH & DESIGN

收录：;EI(收录号：20174504365537);WOS:【SCI-EXPANDED(收录号:WOS:000414506300046)】；

基金：We thank the National Natural Science Foundation of China (Grant Nos. 81273479 and 81402898), Youth Innovation Promotion Association CAS (Grant No. 2016257), CAS Key Technology Talent Program, and SANOFI-SIBS Scholarship for funding.

语种：英文

外文关键词：Differential scanning calorimetry - Single crystals - Thermogravimetric analysis - Quality control

摘要：Two types of solvates for the antiangiogenesis drug apatinib mesylate were obtained, and their crystal structures were determined by single-crystal X-ray diffraction. The properties of these solvates were fully characterized by powder X-ray diffraction, dynamic vapor sorption, differential scanning calorimetry, and thermogravimetric analysis. Experimental and theoretical studies were performed on the solvates to understand the phase transitions induced by heat and humidity. An irreversible humidity-induced single-crystal-to-single-crystal transformation from ethanol solvate (type II) to monohydrate (type I) was elucidated. The stability of these solvates, including moisture-dependent and thermal stability, was studied. The comprehensive investigation of the solvates and hydrate provided essential knowledge about quality control of this important drug.