中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Solid-State Characterization and Transformation of Various Creatine Phosphate Sodium Hydrates

文献类型:期刊论文

作者Xu, Yun; Jiang, Linglei; Huang, Ying; Wang, Jian-Rong; Mei, Xuefeng
刊名JOURNAL OF PHARMACEUTICAL SCIENCES
出版日期2014-11
卷号103期号:11页码:3688-3695
关键词creatine phosphate sodium hydrates crystal structure physical characterization stability form transformation
ISSN号0022-3549
DOI10.1002/jps.24175
文献子类Article
英文摘要Creatine phosphate sodium (CPS) salt is a first-line cardiovascular drug for severe diastolic heart failure. The drug exists in different hydrate forms. The marketed drug form was determined as CPS4.5H(2)O (H1); however, the reference standard was supplied as CPS6H(2)O (H2). In this work, we present two newly identified hydrate forms: a thermodynamically stable low hydrate form, CPS1.5H(2)O (H3), and a pressure-sensitive transit form, CPS7H(2)O (H4). The hydrate forms were discovered through a comprehensive solid-state screening experiment and fully characterized using a range of analytical techniques including X-ray powder diffraction (XRPD), FTIR, Raman spectroscopy, hot-stage microscopy (HSM), thermogravimetric analysis, and differential scanning calorimetry. Stability tests revealed that H3 was the most stable hydrate under thermal stimulation. H4 is a pressure-sensitive hydrate and easily transforms to H2 and then H1 upon grinding. The form transformation process was closely monitored using the HSM, variable-temperature XRPD (VT-XRPD), and VT-Raman spectroscopy techniques. Specifically, the transformation of H4 to H1 is characterized in a single-crystal-to-single-crystal transformation process. The newly discovered hydrate form H3 has superior physicochemical properties than the marketed forms and is worthy of further development. (c) 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:3688-3695, 2014
WOS关键词INORGANIC-PHOSPHATE ; CRYSTAL-STRUCTURE ; WATER ACTIVITY ; FORM ; DRUG ; CARBAMAZEPINE ; THEOPHYLLINE ; POLYMORPHISM ; CONVERSION ; STABILITY
资助项目National Natural Science Foundation of China[81273479] ; Shanghai Institute of Materia Medica New-Star Plan B[00000000]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000344145200036
出版者WILEY
源URL[http://119.78.100.183/handle/2S10ELR8/276856]  
专题药物质量控制与固体化学研究中心
通讯作者Mei, Xuefeng
作者单位Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714
Xu, Yun,Jiang, Linglei,Huang, Ying,et al. Solid-State Characterization and Transformation of Various Creatine Phosphate Sodium Hydrates[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2014,103(11):3688-3695.
APA Xu, Yun,Jiang, Linglei,Huang, Ying,Wang, Jian-Rong,&Mei, Xuefeng.(2014).Solid-State Characterization and Transformation of Various Creatine Phosphate Sodium Hydrates.JOURNAL OF PHARMACEUTICAL SCIENCES,103(11),3688-3695.
MLA Xu, Yun,et al."Solid-State Characterization and Transformation of Various Creatine Phosphate Sodium Hydrates".JOURNAL OF PHARMACEUTICAL SCIENCES 103.11(2014):3688-3695.

入库方式: OAI收割

来源:上海药物研究所

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