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

doi:10.1021/acs.cgd.7b01123

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物质量控制与固体化学研究中心

	Solid-State Characterization and Insight into Transformations and Stability of Apatinib Mesylate Solvates
	Zhu, Bin 2; Zhang, Qi 1; Ren, Guobin 2,3; Mei, Xuefeng1
刊名	CRYSTAL GROWTH & DESIGN
	2017-11
卷号	17 期号:11 页码:5994-6005
ISSN号	1528-7483
DOI	10.1021/acs.cgd.7b01123
文献子类	Article
英文摘要	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.
资助项目	National Natural Science Foundation of China[81273479] ; National Natural Science Foundation of China[81402898] ; Youth Innovation Promotion Association CAS[2016257] ; CAS[00000000] ; SANOFI-SIBS Scholarship[00000000]
WOS关键词	CONFORMATIONAL POLYMORPHISM ; REGULATORY CONSIDERATIONS ; PHASE-TRANSFORMATIONS ; GASTRIC-CANCER ; RATIONALIZATION ; COMPACTION ; CRYSTALS ; ACID
WOS研究方向	Chemistry ; Crystallography ; Materials Science
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000414506300046
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/272422]
专题	药物质量控制与固体化学研究中心
通讯作者	Ren, Guobin; Mei, Xuefeng
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China 2.East China Univ Sci & Technol, Lab Pharmaceut Crystal Engn & Technol, Sch Pharm, Shanghai 200237, Peoples R China; 3.East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai 200237, Peoples R China;
推荐引用方式 GB/T 7714	Zhu, Bin,Zhang, Qi,Ren, Guobin,et al. Solid-State Characterization and Insight into Transformations and Stability of Apatinib Mesylate Solvates[J]. CRYSTAL GROWTH & DESIGN,2017,17(11):5994-6005.
APA	Zhu, Bin,Zhang, Qi,Ren, Guobin,&Mei, Xuefeng.(2017).Solid-State Characterization and Insight into Transformations and Stability of Apatinib Mesylate Solvates.CRYSTAL GROWTH & DESIGN,17(11),5994-6005.
MLA	Zhu, Bin,et al."Solid-State Characterization and Insight into Transformations and Stability of Apatinib Mesylate Solvates".CRYSTAL GROWTH & DESIGN 17.11(2017):5994-6005.