The solubility of ball-milled amobarbital and the stability of its amorphous state.
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概要
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Amobarbital was ball-milled with methylcellulose (MC), microcrystalline cellulose, or dextran. The analysis of the IR spectra indicated that hydrogen bonds were formed between the C=O groups of amobarbital and the OH groups of the diluents upon ball-milling. It was also shown that formation of the bonds was more predominant with MC than with dextran. After suspensions of various kinds of samples in distilled water had been set aside for a week after the time of preparation, the solid state of the amobarbital remaining undissolved in the suspension was compared with the state before dissolution. There are three kinds of polymorphs for amobarbital: Crystals I, II, and III. Crystal I is given by heating Crystal II (at 150 °C), which has been recrystallized from a 25 v/v% aqueous ethanol solution. Crystal III is given by freeze-drying an aqueous solution. The above comparison suggests that Crystal III and the amorphous part are transformed into Crystal I in the absence of any diluent. It seems that the presence of dextran ball-milled with amobarbital prevents Crystal III from being transformed into Crystal I. The presence of MC ball-milled with amobarbital also seems to prevent both the amorphous part from crystallization and Crystal III from transformation into Crystal I. The solubility of amobarbital in distilled water increased remarkably upon ball-milling with diluents; this was attributed to the stabilization of the amorphous state by the interaction with diluents.
- 公益社団法人 日本化学会の論文
著者
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Hayakawa Sohachiro
Department Of Applied Physics Faculty Of Science Tokyo Institute Of Technology
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Ikekawa Akiko
Faculty of Pharmaceutical Sciences, Showa University
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