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头孢唑林和头孢氨苄在水溶液中的降解动力学。

Kinetics of degradation of cefazolin and cephalexin in aqueous solution.

作者信息

Rattie E S, Guttman D E, Ravin L J

出版信息

Arzneimittelforschung. 1978;28(6):944-8.

PMID:35181
Abstract

The kinetics of degradation of cefazolin and cephalexin in aqueous solution were investigated at 60 degrees C and constant ionic strength over the entire pH range. The observed degradation rates were obtained by measuring the residual cephalosporin and were shown to follow pseudo-first-order-kinetics. They were influenced significantly by solvolytic and hydroxide ion catalysis. No primary salt effect was observed in the acid or basic pH region. Of the buffer systems employed in the kinetics studies only the phosphate buffer system showed a catalytic effect. The pH-rate profile for cefazolin showed a degradation minimum between pH 5.5 and 6.5. Cephalexin did not show a pH minimum in that region. The apparent energies of activation were determined for cefazolin and cephalexin at pH 5.5 and were calculated to be 24.3 Kcal/mole and 26.2 Kcal/mole, respectively. The agreement between the calculated theoretical pH-rate profiles and the experimental points for both compounds support the hypothesis presented concerning the reactions involved in their respective degradation pathways.

摘要

在60℃和恒定离子强度下,在整个pH范围内研究了头孢唑林和头孢氨苄在水溶液中的降解动力学。通过测量残留的头孢菌素获得观察到的降解速率,并表明其遵循准一级动力学。它们受到溶剂解和氢氧根离子催化的显著影响。在酸性或碱性pH区域未观察到一级盐效应。在动力学研究中使用的缓冲系统中,只有磷酸盐缓冲系统显示出催化作用。头孢唑林的pH-速率曲线在pH 5.5至6.5之间显示出降解最小值。头孢氨苄在该区域未显示出pH最小值。在pH 5.5下测定了头孢唑林和头孢氨苄的表观活化能,计算得出分别为24.3千卡/摩尔和26.2千卡/摩尔。两种化合物计算出的理论pH-速率曲线与实验点之间的一致性支持了所提出的关于它们各自降解途径中涉及的反应的假设。

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