示差走査熱量計を用いたセラトロダスト結晶多形の転移の速度論的研究

概要

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Seratrodast [(±)-7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7-phenylheptan-oic acid], a thromboxane A_2 antagonist, developed as an antiasthmatic, has two crystalline forms, form I and form II. Form I was a stable form and form II was metastable form since the crystalline form was transformed into form I by heating. By differential scanning calorimetry, form I showed only an endothermic peak at about 130℃ with melting but form II additionally showed an exothermic peak at about 90℃. This exothermic peak was the transition point of form II to form I. A method for the determination of the ratio of form II in seratrodast was established from the ratio of the exothermic calorific value to the endothermic calorific value on the differential scanning calorimetric curve. The transition of form II to form I appeared to follow the zero-order mechanism. The activation energy of this transition was 270kJ/mol calculated from the Arrhenius plots.
公益社団法人日本薬学会の論文
1995-11-25