医薬品の分解とその安定化(第9報)アミノアルキルエステルの安定性におよぼす添加物の影響

概要

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The effect of additives on the stabilization, i.e., retardation of hydrolysis of aminoalkyl esters of phenylacetic acid [chemical formula] was examined. Among the esters I(R^1=H, R^2=H), II(R^1=H, R^2=CH_3), III(R^1=CH_3,R^2=H), IV(R^1=n-C_3H_7,R^2=H), V(R^1=n-C_4H_9,R^2=H), VI(R^1=sec-C_4H_9,R^2=H), VII(R^1=sec-C_4H_9,R^2=CH_3), VIII(R^1=C_6H_5,R^2=H), IX(R^1=m-CH_3O-C_6H_4,R^2=H), the hydrolysis rate of VI was remarkably decreased by the presenced of nicotinamide, N-(hydroxyethyl) lactamide, and glutathione. The effect of these additives on the ester hydrolysis rate was studied in terms of complexation. The complex formation was examined by a kinetic procedure, solubility, partition, ultraviolet spectrum, and nuclear magnetic resonance spectrum. Among these, kinetic procedure and solubility method showed the formation of 1 : 1 complex.
公益社団法人日本薬学会の論文
1974-08-25