Corticosteroid水溶性誘導体の製剤学的研究(第1報) : 水溶液中におけるHydrocortisone21-Hemiester類の安定性

概要

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In order to solubilize the sparingly soluble hydrocortisone, 16 kinds of its 21-hemiester derivative were systematically synthesized and their apparent pKa values were measured. These derivatives were all found to be soluble in water and their behavior to hydrolysis in alkaline aqueous solution was examined kinetically. All the derivatives underwent apparent first-order hydrolysis, and the effect of substituents on their stability included not only their steric effect but the position of terminal carboxyl group was found to be important. From the pH profile of the decomposition rate constant in an alkaline range, these derivatives were assumed to be decomposed by the catalytic effect of the hydroxyl ion. Effect of inoic strength and temperature on the decomposition rate constant was examined with several of the derivatives.
1971-08-25