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Solid-State Characterization and Insight into Transformations and Stability of Apatinib Mesylate Solvates
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2017-10-18 00:00:00 , DOI: 10.1021/acs.cgd.7b01123
Bin Zhu , Qi Zhang 1 , Guobin Ren , Xuefeng Mei 1
Affiliation  

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.

中文翻译:

固态表征和对甲磺酸阿帕替尼溶剂化物的转化和稳定性的了解

获得了两种类型的抗血管生成药物甲磺酸阿帕替尼的溶剂化物,并通过单晶X射线衍射确定了它们的晶体结构。这些溶剂化物的性质通过粉末X射线衍射,动态蒸气吸附,差示扫描量热法和热重分析进行了充分表征。对溶剂合物进行了实验和理论研究,以了解由热和湿度引起的相变。阐明了不可逆的湿度诱导的单晶至单晶从乙醇溶剂化物(II型)到一水合物(I型)的转变。研究了这些溶剂化物的稳定性,包括对水分的依赖性和热稳定性。
更新日期:2017-10-18
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