【摘要】 目的研究3’单肟靛玉红(IMX)在大鼠体内的药物代谢动力学过程。方法利用高效液相色谱法(HPLC)测定大鼠血液中IMX的含量;分别研究静脉注射、腹腔注射2种给药途径后,IMX在大鼠体内的药物代谢动力学,应用3P87药物代谢动力学程序,计算出主要的药物代谢动力学参数;并进一步观察静脉给药后药物在动物体内主要器官心、肺、肾、脑组织中IMX的含量。结果鼠尾静脉注射IMX,药物代谢动力学符合二室模型。IMX在鼠体内吸收快、分布快、药物起效快,在体内主要以消除过程为主,药物在体内滞留时间较长。静脉注射10 mg/kg IMX,于不同时间处死,用HPLC测定各组织中IMX的含量,结果发现,IMX在心脏组织中含量较高,在1 h达峰值;脑组织、肺组织中IMX含量在0.5 h即达峰值;肾脏组织中IMX含量在3 h达峰值。IMX主要分布在体循环和血流丰富的脏器中。结论应用HPLC法测定大鼠血浆中IMX的浓度,操作简便、省时,精密度及重现性均较好。静脉注射IMX,药物代谢动力学符合二室模型,IMX在鼠血中主要以消除过程为主,IMX主要分布在血流丰富的组织中,分布速率较快。IMX易于透过血脑脊液屏障。更多还原

【Abstract】 Objective To investigate the pharmacokinetics of indirubin-3’-monxime(IMX) in rats by different administrations and distributions in tissues of IMX.Methods A high-performance liquid chromatography(HPLC) wasused to determine the plasma IMX concentration so as to study the pharmacokinetics of IMX in rats after intravenous.The main pharmacokinetics parameters were calculated.After intravenous injection of IMX,the distribution of IMX inheart,lung,kidney and brain was assessed.Results IMX pharmacokinetics was conformed to the two apartment openmodel.By intravenous administration IMX in rats,both absorption and distribution were fast,the velocity to effect was rapid,elimination was the main process,and the retention time was long.After intravenous administration(10 mg /kg),rats were killed at different times,2 g of each tissue in hearts,lungs,kidneys and brains were obtained to detect the concentration of IMX by HPLC.There was higher concentration of IMX in heart tissues,and the peak of its concentration appeared at 1 h after injection;and the peak in brain and lung tissues appeared at 0.5 h after injection;and in kidney tissues it was at 3 h after injection.Conclusion HPLC is simple and reliable to determine plasma concentration of IMXin rats.It is simple and credible that applying HPLC method to test plasma concentration of IMX in rats.The pharmacokinetics of IMX by intravenous administration was conformed to two apartment open model and the elimination of IMXis the main process after the injection of IMX.IMX is distributed mainly in systemic circulation and abundant blood supply organs.Furthermore,IMX can penetrate the blood brain barrier.更多还原