Study of the Pseudo-Crystalline Transformation from Form I to Form II of Thiamine Hydrochloride (Vitamin B1)
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概要
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The purpose of the current study was to evaluate the rate of the pseudo-crystalline transformation of thiamine hydrochloride form I to form II depending on the temperature and humidity. Changes in the appearance and weight of form I crystals were observed under humidified conditions using a water vapor sorption system equipped with a CCD camera. The form I crystals and tablets were stored under various temperature and humidity conditions (the saturation salt desiccator method), and the pseudo-crystalline transformation was observed using X-ray powder diffractometry with our laboratory equipment for drug substances and using synchrotron X-ray powder diffractometry for tablets. It was confirmed that the activation energy in the pseudo-crystalline transformation rate from form I to form II was dependent on humidity, and the calculated values were 121—155 kJ/mol at 70—90% relative humidity. Moreover, when thiamine hydrochloride was formulated as tablets, it was confirmed that the transformation rate was slower compared with the drug substances alone. The pseudo-crystalline transformation rate therefore declined after formulation in tablet form, perhaps due to the shielding effects of thiamine hydrochloride crystal from contact with water molecules by excipients, compaction, etc.
著者
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FUJII Kotaro
Department of Chemistry, Tokyo Institute of Technology
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UEKUSA Hidehiro
Department of Chemistry, Tokyo Institute of Technology
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Masuda Katsuhiko
Department I, Medicinal Chemistry Research Laboratory I, Research Division, Mitsubishi Tanabe Pharma
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Ishige Takayuki
Department I, Medicinal Chemistry Research Laboratory I, Research Division, Mitsubishi Tanabe Pharma
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Yamada Hiroyuki
CMC Research Center, Mitsubishi Tanabe Pharma Corporation
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Miura Keiko
Industrial Application Division, Japan Synchrotron Radiation Research Institute
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Yonemochi Etsuo
School of Pharmaceutical Sciences, Toho University
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Terada Katsuhide
School of Pharmaceutical Sciences, Toho University
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Fujii Kotaro
Department Of Chemistry Tokyo Institute Of Technology
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Uekusa Hidehiro
Department Of Chemistry And Material Science Tokyo Institute Of Technology
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Yonemochi Etsuo
School Of Pharmaceutical Sciences Toho Univ.
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Terada Katsuhide
School Of Pharmaceutical Sciences Toho Univ.
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Ishige Takayuki
Department I, Medicinal Chemistry Research Laboratory I, Research Division, Mitsubishi Tanabe Pharma Corporation
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Fujii Kotaro
Department of Chemistry and Materials Science, Tokyo Institute of Technology
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Masuda Katsuhiko
Department I, Medicinal Chemistry Research Laboratory I, Research Division, Mitsubishi Tanabe Pharma Corporation
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