Physicochemical Analyses of Phase Transition and Dehydration Processes of a New Oral 1β-Methylcarbapenem Antibiotic Agent, CS-834
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概要
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The characterizations of the anhydrate (A-form), monohydrate (B1-form), and dihydrate (B2-form) of CS-834 were investigated by powder X-ray diffraction, differential scanning calorimetry (DSC), thermogravimetry-differential thermal analysis (TG-DTA), infrared spectroscopy, and Karl Fischer moisture titration. The typical DSC curve of the B2-form showed five endothermic peaks at 35.0, 46.4, 56.2, 99.2, and 190.4℃ and an exothermic peak at 123.4℃. In TG-DTA analysis, the three peaks at 35.0, 46.4, and 56.2℃ had a total weight loss of 7.3%, corresponding to the release of two water molecules. From morphological observation under thermomicroscopy, the endothermic peak at 99.2℃ was attributed to the melting of the dehydrous crystals (B0-form) and the exothermic peak at 123.4℃ to the recrystallization to the A-form crystals. The endothermic peak at 190.4℃ was due to the melting of the A-form crystals. After incubation for 6.0 h at 35, 50, 60, and 80℃, the powder X-ray diffraction patterns of the B2-form indicated that it was converted into the A-form via the B1-form and B0-form. Thus CS-834 exists in homologous hydrous crystal forms in multiple-phase transformations with the dehydration of two water molecules.
- 公益社団法人日本薬学会の論文
- 2002-12-01
著者
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小林 匡子
東北薬科大学生薬学教室
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Kobayashi Kyoko
Tohoku Pharmaceutical University
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UEKUSA Hidehiro
Department of Chemistry, Tokyo Institute of Technology
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SEKINE Akiko
Department of Chemistry and Materials Science Tokyo Institute of Technology
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OHASHI Yuji
Department of Chemistry and Materials Science Tokyo Institute of Technology
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Ohashi Y
Department Of Chemistry And Materials Science Tokyo Institute Of Technology
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Sekine A
Department Of Chemistry And Materials Science Tokyo Institute Of Technology
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Hata Toshiyuki
Biotechnology Fukuyama University
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Uekusa H
Department Of Chemistry And Materials Science Tokyo Institute Of Technology
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Ohashi Y
Kyoto Univ. Kyoto
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Uekusa Hidehiro
Department Of Chemistry And Material Science Tokyo Institute Of Technology
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KOBAYASHI Katsuhiro
Process Development Laboratories, Sankyo Co., Ltd.
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FUKUHARA Hiroshi
Process Development Laboratories, Sankyo Co., Ltd.
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HATA Tadashi
Biomedical Research Laboratories, Sankyo Co., Ltd.
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KAWAMOTO Isao
Medicinal Chemistry Research Laboratories, Sankyo Co. Ltd.
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Fukuhara Hiroshi
Process Development Laboratories Sankyo Co. Ltd.
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Kawamoto Isao
Research Laboratories Sankyo Co. Ltd
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Kawamoto Isao
Research Laboratories Sankyo Co. Ltd
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Kawamoto Isao
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
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Kawamoto Isao
Research Laboratories Sankyo Co. Ltd.
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Kawamoto Isao
Tsukuba Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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Hata Tadashi
Biomedical Research Laboratories Sankyo Co. Ltd.
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Ohgo Y
Niigata College Of Pharmacy
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Ozawa Yoshiki
Department Of Material Science Graduate School Of Material Science University Of Hyogo
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Hata Taeko
Biotechnology, Fukuyama University
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