Methanesulfonic Acid Derivative of Sulfonamides. I. Hydrolysis Rate in Vitro and Pharmacokinetics in Vivo

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概要

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• Various methanesulfonic acid derivatives of four sulfonamides, which are represented generally as R'NHSO_2C_6H_5NHCHRSO_3Na wer esynthesized and their hydrolysis rates in vitro and pharmacokinetics of blood concentration change in rabbit were investigated. When R is H the hydrolysis rate is so slow that the pharmacological activity of parental sulfonamide can not be expected. When R is alkyl, phenyl or HOCH_2 (CHOH)_4 the derivative has fast hydrolysis rate which may promise good availability of parental sulfonamide. The effect of R on hydrolysis rate was elucidated by linear free energy relationship. The dissociation of sulfonamide group hastens the hydrolysis. Dynamic process of appearance and disappearance of parental sulfonamide in blood was quantitatively explained by a scheme which assumes two compartment models for both of the derivative and parental sulfonamide respectively.

• 公益社団法人日本薬学会の論文
• 1972-05-25

著者

• 黒野 幸久

  神戸大学 大学院医学系研究科精神神経科学分野

• 池田 憲

  Faculty Of Pharmaceutical Sciences Nagoya City University

• 黒野 幸久

  Faculty of Pharmaceutical Sciences, Nagoya City University

• 塚本 長太郎

  Faculty Of Pharmaceutical Sciences Nagoya City University

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