清胰煎剂与颗粒中4种成分在大鼠体内的药动学比较

目的比较清胰煎剂与颗粒中主要有效成分药动学参数的一致性。方法两组大鼠分别灌胃给予同等生药量的清胰煎剂和颗粒后,采用液相色谱-串联质谱联用(LC-MS/MS)法同时测定不同时间点血浆中芦荟大黄素、大黄素、大黄酸、大黄酚的血药浓度,采用Pk Solver软件计算相关药动学参数。结果清胰煎剂组有效成分芦荟大黄素、大黄素、大黄酸、大黄酚的达峰时间(tmax)分别为0.72,0.45,0.60,0.20 h;血浆消除半衰期(t1/2)分别为9.36,9.68,5.18,5.47 h;峰浓度(Cmax)分别为107.27,14.92,1363.6,96.02 ng·m L-1;血药浓度-时间曲线下面积(AUC0-∞)分别为496.31,105.60,3831.79,481.75 ng·h·m L-1。清胰颗粒组有效成分芦荟大黄素、大黄素、大黄酸、大黄酚的tmax分别为0.08,0.18,0.18,0.47 h;t1/2分别为5.61,6.96,4.66,6.51 h;Cmax分别为96.83,11.46,1249.27,96.68 ng·m L-1;AUC0-∞分别为369.68,70.59,5536.66,435.77 ng·h·m L-1。清胰颗粒组4种成分主要药动学参数(tmax、t1/2、Cmax、AUC0-∞)与煎剂组比较均差异无统计学意义(均P>0.05)。结论清胰煎剂和颗粒具有相似的药动学特征。4种成分均吸收迅速,可为清胰制剂的临床应用提供参考。

Comparison of Pharmacokinetics of Four Components in Qingyi Decoction and Granules in Rat

Objective To compare the pharmacokinetics consistence of the main active ingredients between Qingyi decoction and granules.Methods After the gastric administration of Qingyi decoction and granules in rats,liquid chromatography-mass spectrometry(LC-MS/MS)was used to detect the content of aloe-emodin,emodin,rhein and chrysophanol in the plasma,and then Pk Solver software was used to calculate the pharmacokinetic parameters.Results In Qingyi decoction group,the peak time(tmax)of aloe emodin,emodin,rhein and chrysophanol were 0.72,0.45,0.60 and 0.20 h,respectively;the plasma elimination half-life(t1/2)were 9.36,9.68,5.18,5.47 h;the peak concentration(Cmax)were 107.27,14.92,1363.6,96.02 ng·m L-1,respectively;the area under the blood concentration time curve(AUC0-∞)were 496.31,105.60,3831.79,481.75 ng·h·m L-1。In Qingyi granule group,the tmaxof aloe emodin,emodin,rhein and chrysophanol were 0.08,0.18,0.18,0.47 h;t1/2were 5.61,6.96,4.66,6.51 h;Cmaxwere 96.83,11.46,1249.27,96.68 ng·m L-1;AUC0-∞were 369.68,70.59,5536.66,435.77 ng·h·m L-1,respectively.The main pharmacokinetic parameters(tmax,t1/2,Cmax,AUC0-∞)of the four components in Qingyi granule group were not significantly different from those in decoction group(all P>0.05).Conclusion Qingyi granules and decoctions had similar pharmacokinetic characteristics.The four components were absorbed rapidly.This study can provide reference for the clinical application of Qingyi preparation.