马蔺子甲素的药物动力学研究

Pharmacokinetics of Irisquinone A in Rat

采用HPLC方法测定生物样品中的马蔺子甲素浓度。大鼠ig100、200和800mg／kg3个剂量的药代动力学研究表明体内代谢非常快，血药浓度不呈线性消除特征，药物吸收非常迅速，消除快。达峰时间（tpeak）分别为30、30和15min，浓度-时间曲线下的面积（AUC）分别为100．1、3238.1和4509．9ng·min／mL，半衰期（t1/2）分别为66．6、101．9和133．3min。组织分布试验表明，在大鼠ig200mg／kg后1、2、4h，心、肝、脾等组织测不出原型药物。排泄试验在大鼠ig200mg／kg后，36h内从粪中测不到原型药物及代谢产物，36h内测不出从尿中排出的原型药物；其代谢产物12h内排出总量的78％以上，马蔺子甲素是一蛋白结合率非常高的药物，平均蛋白结合率为90．9％。

Pharmacokinetics of irisquinone A was studied in rat.After oral administration, it was rapidly absorbed and eliminated.At doses of 100, 200 and 800 mg/kg, the tpeak were 30, 30 and 15 min; Cmax 1. 1, 24. 3 and 40 ng/mL;AUC 100. 1、3 238. 1 and 4 509. 9 ng·min/ml and t1/2 66. 6、101.9 and 133. 3 min respectively.At 1、2 and 4 h following ig dose,the original form of the drug could not be detected in heart,liver and spleen,nor in urine and faeces after 36 h.More than 78% of the total metabolites were excreted from urine within 12 h.The protein binding ratio was 90.9%.