三黄片及大黄中大黄素大鼠体内药动学研究  

In Vivo Pharmacokinetics Comparison of Emodin from Sanhuang Tablets and Extracts of Crude Drug Rhubarb in Rats

作　　者：周彩虹[1] 姚永中[1] 张毕奎[1] 裴奇[1] 贾素洁[1] 

机构地区：[1]中南大学湘雅三医院药剂科,湖南长沙410013

出　　处：《实用预防医学》2010年第6期1193-1195,共3页Practical Preventive Medicine

摘　　要：目的利用反相高效液相色谱法,探讨中药制剂三黄片与生药大黄提取物中大黄素在大鼠体内的药代动力学差别,探讨中药制剂工艺和配伍对药效成分代谢的影响。方法 SD大鼠随机分为三黄片组和大黄组,每组5只,分别灌胃三黄片、大黄提取物后,于不同时间点尾静脉采血,通过建立的反相高效液相色谱及样品处理法,检测大鼠血浆中大黄素的浓度,采用药动学程序3P87对其进行统计处理,确定大黄素药动学模型及相关药代动力学参数。结果三黄片及大黄中大黄素在大鼠体内呈二室开放模型,主要药代动力学参数为,三黄片组:Cmax/μg.ml-1=3.528±0.72,t1/2(a)/h=1.429±0.201,t1/2(β)/h=4.620±0.536,t1/2(Ka)/h-1=0.405±0.097,Tmax/h=1.520±0.210,AUC0-∞/μg.h.ml-1=31.297±2.001,CL(s)/L.h-1.kg-1=0.018±0.002,Lagtime/h=0.041±0.006。大黄组:Cmax/μg.ml-1=2.547±0.214,t1/2(a)/h=1.501±0.929,t1/2(β)/h=4.598±0.541,t1/2(Ka)/h-1=0.389±0.101,Tmax/h=1.478±0.243,AUC0-∞/μg.h.ml-1=26.729±3.010,CL(s)/L.h-1.kg-1=0.024±0.002。结论与大黄组比较,三黄片中大黄素在大鼠体内的吸收增加,分布及达峰时间延长,血浆清除减少,生物利用度较大黄药材高,其原因可能与大黄素和复方其他成分的相互作用,或复方的制剂工艺有关。Objective To explore the effects of preparation technology and different compositions on the pharmacokinetic of emodin by comparison its pharmacokinetic parameters from Sanhuang tablets and crude drug rhubarb.Methods Sprague Dawley rats were randomly divided into two groups：Sanhuang tablet group and rhubarb group （each n=5）.The rats were administrated with Sanhuang tablets and Rhubarb （intragastric,i.g）,respectively.Blood samples were collected at different time points from tail veins.The plasma concentrations of emodin were measured by the established RP-HPLC method.The pharmacokinetic parameters and the pharmacokinetics of dimensional model were determined by pharmacokinetic program 3P87.Results The pharmacokinetic character of emodin fitted two-compartment open model.The pharmacokinetic parameters were as follows：Sanhuang tablets：Cmax/μg·ml^-1=3.528±0.72,t1/2（a）/h=1.429±0.201,t1/2（β）/h=4.620±0.536,t1/2（Ka）/h-1=0.405±0.097,Tmax/h=1.520±0.210,AUC0-∞/μg·h·ml^-1=31.297±2.001,CL（s）/L·h^-1·kg^-1=0.018±0.002,Lag time/h=0.041±0.006;rhubarb group：Cmax/μg·ml^-1=2.547±0.214,t1/2（a）/h= 1.501±0.929,t1/2（β）/h=4.598±0.541,t1/2（Ka）/h^-1=0.389±0.101,Tmax/h=1.478±0.243,AUC0-∞/μg·h·ml^-1=26.729±3.010,CL（s）/L·h-1·kg^-1=0.024±0.002.Conclusions Compared with emodin in Sanhuang tablets,the emodin in rhubarb shows improved absorption,prolonged distribution time and peak time,reduced plasma clearance and better bioavailability,which is possibly related to the interaction of other components and the technology of the preparation.

关 键 词：药代动力学 大黄素 三黄片 大黄 

分 类 号：R332[医药卫生—人体生理学]