[Topic]温度操作で医療用医薬品を再結晶 Recrystallization of acetaminophen by tempering



More, in English (prepared by YS, undergrad. student) …

「特殊な温度操作 、”Tempering”」とは、II型を得るための経験的な方法で、融けたチョコレートの冷却や固化に使用されています。しかし、活性医薬成分のための「特殊な温度操作」の研究は不十分であり、包括的な操作ガイドラインが提案されていません。


この研究は、製薬分野への貢献が見込まれます。詳しくはJournal of Industrial and Engineering Chemistryをご覧ください。


The improvement in solubility of pharmaceutical crystals is indispensable because of the bioavailability enhancement. Acetaminophen (ACM), which is active pharmaceutical ingredient, has crystal polymorphism; form I (the stable form) and form II (the metastable form). A metastable form has advantages in not only the improvement of solubility but also the characteristics of pharmaceutical preparation. On the other hand, the metastable form is difficult to produce and therefore selective manufacture is a serious problem.

“Tempering operation” is an empirical method to obtain a metastable form by adding reheating operation when melt chocolate is cooled and solidified. However, engineering studies on the tempering operation for the active pharmaceutical ingredient are not sufficient. The comprehensive guidelines for these operations have not been suggested.

Okude & Takiyama investigated the relationships among tempering operation conditions, thermodynamical changes and crystal structure changes by using “XRD–DSC” experiments, which is to obtain the operating guidelines for tempering operation for selective manufacturing technique of the polymorphic form. Through this research, four requirements are defined to determine the operating conditions for crystallization of ACM metastable polymorph. Moreover, the operating guidelines for production method of ACM metastable polymorph were proposed.

This study is expected to contribute to the pharmaceutical field. For further reading :Journal of Industrial and Engineering Chemistry

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