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![]() ![]() |
刊名 | JOURNAL OF PHARMACEUTICAL SCIENCES
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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 |
DOI | 10.1002/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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