薬剤の非同等性に関する研究(第8報)メルカプトプリンの結晶多形および水和物と溶解性について

概要

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Physicochemical properties of the polymorphs and hydrate of 6-mercaptopurine were investigated. Its crystal habits were slightly changed and form I-TX was obtained by the addition of 6-thioxanthine and/or 2,6-dithioxanthine and subsequent recrystallization. It was found that when Form I-TX was heated at 240°, this form transformed to Form III which was found to have a solubility about 6-7 times that of Form I. The mutual transition of 6-mercaptopurine polymorphs and hydrate under various conditions of heating and suspending in water was also studied. The transition temperature and the heat of transition between Form I-TX and Form II-TX_<hyd> were determined to be 127°and 2.15 kcal/mol, respectively, by the solubility measurement. It was expected that if the transition of Form III could be suppressed, more bioavailable preparation of 6-mercaptopurine would be obtained.
社団法人日本薬学会の論文
1979-07-25