超氧化物歧化酶及其模拟物甲基多巴酰胺铜在大鼠体内的药代动力学

THE PHARMACOKINETICS OF SOD AND ITS IMITATOR Cu(MDP)_2

应用固相氧化法制备^(125)I—SOD及其模拟物^(125)I—Cu(MDP)_2,比较两药在大鼠体内的药代动力学。根据血样放射性—时间曲线,两药均符合开放型二房室模型,主要动力学参数(T_(1/2)、K、V_C)有明显差异。表明Cu(MDP)_2从血液向组织分布速度快于SOD,体内存留时间延长,在组织内分布较广泛。本文还比较了两药在体内的组织分布。

The pharmacokinetics of ^(125)I-SOD and ^(125)I-Cu(MDP)_2 was investigated in order to compare themetabolic differences between SOD and Cu(MDP)_2 in rats. After iv ^(125)I-SOD and ^(125)I-Cu(MDP)_2 res-pectively, both of their radioactivity-time curves in rats were found to be a two-compartment openmodel. In SOD, the distribution phase T_(1/2)=4.67±1.49 min, the elimination phase T_(1/2)(2)=78.15±49.15 min, and the rate constant of elimination K_(10)=0.0745±0.0228min^(-1); In Cu(MDP)_2 T_(1/2)(1)=2. 67±1. 18min, T_(1/2)(2)=191 .72±86.50min, and K_(10)=0.0091±0.0045min^(-1). This result showed thatthe elimination rate of Cu(MDP)_2 was more than two times slower than that of SOD. In addition, thehighest radioactivity was found in the kidney and the lowest in the heart both for SOD andCu(MDP)_2.