Solid-State Characterization and Insight into Transformations and Stability of Apatinib Mesylate Solvates

被引:30
|
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
基金
中国国家自然科学基金;
关键词
PHASE-II; CRYSTAL; RATIONALIZATION; POLYMORPHISM; COMPACTION;
D O I
10.1021/acs.cgd.7b01123
中图分类号
O6 [化学];
学科分类号
0703 ;
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.
引用
收藏
页码:5994 / 6005
页数:12
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