大鼠体内大承气汤蒽醌成分的药代动力学研究

Pharmacokinetic studies of anthraquinone in rats after intragastric gavage of Dachengqi Decoction

目的:阐明大承气汤经灌胃给药后,5种游离蒽醌成分在大鼠体内的药代动力学特性。方法:大鼠灌胃给药大承气汤9g/kg后,采集血浆、尿液,采用HPLC法测定血浆中芦荟大黄素、大黄酸、大黄素、大黄酚及大黄素甲醚的含量,并用DAS 2.0软件进行数据分析,计算药动学参数。结果:大鼠灌胃给予大承气汤后,血浆中检测到芦荟大黄素、大黄酸、大黄素、大黄酚及大黄素甲醚,尿中检测到芦荟大黄素、大黄酸,血液和尿液均以芦荟大黄素和大黄酸含量最高。大鼠灌胃大承气汤后,血浆中芦荟大黄素、大黄酸、大黄素、大黄酚及大黄素甲醚的T1/2(Ka)(h)依次是0.36、1.03、1.92、1.89、0.66;T1/2(Ke)(h)依次是0.31、1.17、2.33、2.19、0.81;Cmax(mg/L)依次是48.47、21.69、10.49、5.76、38.76;Tmax(h)依次是4、4、6、4、2;AUC0-t(mg.L-1.h-1)依次是85.73、66.73、65.91、41.84、96.40。结论:大承气汤中蒽醌类成分可以吸收进入体内,其中以芦荟大黄素和大黄酸为主;体内葸醌类成分以尿排泄为主。同时建立经灌胃大承气汤后大鼠血浆中5种游离蒽醌含量的测定方法,并阐明其药动学特性;为大承气汤的体内成分研究提供实验依据。

Objective：To study the pharmacokinetics of propertyes in rats after ig of Dachengqi Dection.Methods：SD rats were given a single ig dose of Dachengqi Dection 9g/kg.Anthraquinone components in plasma,urine and plasma concentrations of aloe-emodin,rhein,emdin,chysophanol and physcion were measured with HPLC.Pharmacokinetics parameters were determined from the plasma concentration-time data with the DAS2.0 software package.Results：After ig Dachengqi Dection in rats,aloe-emodin,rhein,emdin,chysophanol and physcion were detected in plasma and aloe-emodin,rhein in urine.After intragastic gavage of Dachengqi Dection 9g/kg,T1/2（Ka）（h） were 0.362,1.034,1.918,1.89,0.656;T1/2（Ke）（h） were 0.311,1.173,2.33,2.188,0.81;Cmax（mg/L） were 48.47,21.69,10.49,5.76,38.76;Tmax（h） were 4,4,6,4,2;AUC0-t（mg·L-1·h-1） were 85.733,66.726,65.91,41.84,96.401;Conclusion：Athraquinones（mainly aloe-emodin and rhein） can be absorbed after ig administration of Dachengqi Dection in rats.The anthraquinones were mainly excreted through urine.The method for determining aloe-emodin,rhein,emdin,chysophanol and physcion in plasma had been established,and the pharmacokinetic parameters can be instructive for clinic application.