Glass-State Amorphous Salt Solids Formed by Freeze-Drying of Amines and Hydroxy Carboxylic Acids : Effect of Hydrogen-Bonding and Electrostatic Interactions
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概要
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We studied effect of molecular interactions on the physical properties of binary freeze-dried solids and frozen aqueous solutions using model chemicals containing various functional groups (amino, carboxyl, hydroxyl). Thermal analysis of frozen solutions containing alkyl diamines and hydroxy di- or tricarboxylic acids showed thermal transitions (T_g' : glass transition of maximally freeze-concentrated phase) at temperatures higher than those of the individual solutes. A binary frozen solution containing 80mM 1,3-diamino-2-hydroxypropane (single-solute T_g'<-60℃) and 120mM citric acid (single-solute T_g' : -55.0℃) made the transition at -30.8℃. The molecular weight of the solutes had smaller effects on the transition temperatures of the frozen mixture component solutions. Lyophilization of some high T_g' mixture frozen solutions (e.g., 1,3-diamino-2-hydroxypropane and citric acid) resulted in cake-structure amorphous solids with glass transition temperatures (T_g) higher than those of the individual components. Networking of intense hydrogen-bondings and electrostatic interactions between the heterogeneous molecules through the multiple functional groups was suggested to reduce the component mobility in the amorphous freeze-concentrated phase and the freeze-dried solids. Controlling the interactions should be a key to optimizing the physical properties of multi-component amorphous freeze-dried pharmaceutical formulations.
- 公益社団法人日本薬学会の論文
- 2008-06-01
著者
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Kawanishi Toru
National Institute Of Health Sciences
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YONEMOCHI Etsuo
Faculty of Pharmaceutical Sciences, Chiba University
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Yonemochi Etsuo
Faculty Of Pharmaceutical Sciences Toho University
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Yonemochi Etsuo
School Of Pharmaceutical Sciences Toho Univ.
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TERADA Katsuhide
Faculty of Pharmaceutical Sciences, Toho University
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YOMOTA Chikako
National Institute of Health Sciences
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Terada Katsuhide
Faculty Of Pharmaceutical Sciences Chiba University
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Terada Katsuhide
Faculty Of Pharmaceutical Sciences Toho University
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Terada Katsuhide
School Of Pharmaceutical Sciences Toho Univ.
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IZUTSU Ken-ichi
National Institute of Health Sciences
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KADOYA Saori
Faculty of Pharmaceutical Sciences, Toho University
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Kadoya Saori
Faculty Of Pharmaceutical Sciences Toho University
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