甲基毒死蜱在大鼠体内的毒物代谢动力学

Toxicokinetics of chlorpyrifos-methyl in rats

给大鼠ｉｖ１７１ｍｇ·ｋｇ￣（－１）或ｉｇ６８４ｍｇ·ｋｇ￣（－１）甲基毒死蜱（ＣＭ）后，血中ＣＭ浓度的经时变化符合二室开放模型和一级吸收二室开放模型，ＣＭ经消化递吸收相半减期为１３．２ｍｍ、吸收率（Ｆ）为１７％。ＣＭ在体内呈全身分布，ｉｖＣＭ后的ｔ１／２ａ为２ｍｉｎ，ｔ１／２β为１．７４ｈ，全身清除率为０．８６Ｌ·ｋｇ￣（－１）·ｈ￣（－１）．大鼠ｉｖ１７１ｍｇ·ｋｇ￣（－１）ＣＭ后，血，肾和辜丸中ＣＭ浓度的经时变化呈二项指数函数曲线规律，而在肺，肝，脾，心，脑，肌肉和脂肪中的变化则符合叠加指数函数规律。根据靶向指数。靶向系数和综合靶向系数判断，肺和脂肪是ＣＭ选择分布的主要部位。体外代谢研究表明。ＣＭ主要是在肝脏被代谢转化。肝细胞的可溶性胞浆和微粒体是主要的代谢转化场所。

This study reveals that the maleSprague-Dawley rats were exposed chlorpyrifos-methyl(CM) by hypoglossal intravenous injection(171mg·kg￣(-1)) or oral intubation(684 mg·kg￣ (-1)),themetabolism of CM follows two-compartment openmodel. After iv. the data of concentration in bloodwere described by the following biexponentialequation:and half-life for distribution phase was 2 min,for elimination phase was 1.74 h. systematic clearance was0.86 L·kg·h￣(-1)After oral intubation,thC blood con-centration in rats could be described by:and half-life for absorption phase was 13.2 min,fordistribution phase was 23.4min, for elimination phasewas 2.56 h The blood concentration of CM reached ashigb as 35.52 mg·L￣(-1)in 37.2mm,andtheabsorptionrate was17% The concentration -time data of CM in blood,kid-ney and testis conformed to a binomial exponeritialfunction,in lung, liver, spleen, heart, brain, muscle andfat confonned to a multi-exponential function after171 mg·k￣(-1) CM iv was given in rats. According totargeting index, targeting efficiency and total targetingefficiency, it could be suggested that lung and fat werethe targeting distribution tissues for CM in rats. The liver is a mainplace ofmetabolism of CM. Inliver cellS, the main sites of metabolism are cytoplasmdnd microsomes.