Polymorphs and Hydrates of Apatinib Mesylate: Insight into the Crystal Structures, Properties, and Phase Transformations

doi:10.1021/acs.cgd.6b01230

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	Polymorphs and Hydrates of Apatinib Mesylate: Insight into the Crystal Structures, Properties, and Phase Transformations
	Zhu, Bin 2; Wang, Jian-Rong1 ; Ren, Guobin 2; Mei, Xuefeng1
刊名	CRYSTAL GROWTH & DESIGN
	2016-11
卷号	16 期号:11 页码:6537-6546
ISSN号	1528-7483
DOI	10.1021/acs.cgd.6b01230
文献子类	Article
英文摘要	Apatinib mesylate (ATM) is an orally administrated anticancer agent for the treatment of advanced gastric cancer. Single-crystal structures of four ATM solid forms, including two anhydrous polymorphs (I and II) and hydrates (HA and HB), were elucidated by single-crystal X-ray diffraction. The properties of these various forms were fully characterized by powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, and Raman spectroscopy. The discrepant molecule conformations, H-bonding interactions, and packing arrangements in the crystal. structures were analyzed associated with the hygroscopicity of forms I and II. Various form transformations induced by either moisture or solution conditions were examined, and the relative stability was established. The results revealed that HA is the Most thermodynamically stable form and is superior to the currently marketed form.
资助项目	National Natural Science Foundation of China[81273479] ; National Natural Science Foundation of China[81402898] ; National Natural Science Foundation of China[21576080] ; Youth Innovation Promotion Association CAS[2016257] ; CAS Key Technology Talent Program[00000000]
WOS关键词	NEGATIVE BREAST-CANCER ; DIFFERENT SOLVENTS ; GASTRIC-CANCER ; INHIBITOR ; HYDROCHLORIDE ; SOLUBILITY ; HUPERZINE ; STABILITY ; PIRACETAM ; DENSITY
WOS研究方向	Chemistry ; Crystallography ; Materials Science
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000387094600050
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275838]
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, Sch Pharm, Lab Pharmaceut Crystal Engn & Technol, Shanghai 200237, Peoples R China;
推荐引用方式 GB/T 7714	Zhu, Bin,Wang, Jian-Rong,Ren, Guobin,et al. Polymorphs and Hydrates of Apatinib Mesylate: Insight into the Crystal Structures, Properties, and Phase Transformations[J]. CRYSTAL GROWTH & DESIGN,2016,16(11):6537-6546.
APA	Zhu, Bin,Wang, Jian-Rong,Ren, Guobin,&Mei, Xuefeng.(2016).Polymorphs and Hydrates of Apatinib Mesylate: Insight into the Crystal Structures, Properties, and Phase Transformations.CRYSTAL GROWTH & DESIGN,16(11),6537-6546.
MLA	Zhu, Bin,et al."Polymorphs and Hydrates of Apatinib Mesylate: Insight into the Crystal Structures, Properties, and Phase Transformations".CRYSTAL GROWTH & DESIGN 16.11(2016):6537-6546.