小鼠体内泻心汤中黄芩苷药代动力学  

Pharmacokinetics of baicalin in Xiexin Decoction

作　　者：严东明[1] 马越鸣[1] 王天明[1] 张宁[2] 朱恩圆[3] 

机构地区：[1]上海中医药大学中药药代动力学实验室 [2]上海中医药大学科技实验中心,上海201203 [3]上海中医药大学中药研究所,上海201203

出　　处：《中成药》2007年第4期493-496,共4页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(№90409008);上海市科委基金(№04DZ19844);上海市重点学科建设项目资助(№T0301)

摘　　要：目的:研究泻心汤(大黄、黄连、黄芩)中黄酮类成分在小鼠体内药代动力学规律。方法:小鼠灌胃给予泻心汤4.5、9、18g/kg后,用HPLC方法分析血浆中黄酮类成分、测定血浆中黄芩苷浓度经时变化,浓度-时间数据用DAS药代动力学软件进行分析,计算药动学参数。结果:小鼠灌服泻心汤后血浆中检测到黄芩苷、汉黄芩苷和另一黄酮类成分,其中黄芩苷含量最高。泻心汤灌胃给予4.5、9、18g/kg后,黄芩苷主要药代学参数分别为:T1/2=2.77、5.69、6.20h,AUC0-∞=9.09、23.49、39.57μg·h/mL,CL=12.52、6.962、11.50L·h/kg,Vd=50.11、79.56、102.95L/kg,Cmax1=1.89、3.32、4.79μg/mL(Tp1=0.08h),Cmax2=1.46、2.57、4.16μg/mL(Tp2=3h)。结论:泻心汤中黄酮类成分可以吸收进入体内,其中以黄芩苷为主。AIM： To study the pharmacokinetics of flavonoids in mice after ig administration of Xiexin Decoction （Radix et Rhizoma rhei, Rhizoma coptidis, Radix Scutellariae）. METHODS： Mice were given a single ig dose of Xiexin Decoction 4.5, 9.0 or 18.0 g/kg. Flavonoids in plasma were analysed by HPLC and plasma concentration of baibalin was determined. Pharmacokinetic parameters were calculated from the plasma concentrationtime data with the DAS software package. RESULTS ： After ig administration of Xiexin Decoction in mice, baicalin, baicalein and another flavonoid were detected in plasma and baicalin concentration was the highest of the three kinds of flavonoids in plasma. After a single ig dose of Xiexin Decoction 4.5, 9.0 or 18.0 g/kg, the pharmacokinetic parameters of baicalin were as follows ： T1/2 = 2.77,5.69,6.20 h, AUC0 - ∞ = 9.09,23.49,39.57 μg · h/mL, CL = 12.52,6. 962,11.50 L · h/kg, Vd = 50.11,79.56,102.95 L/kg, Cmax1 = 1. 89,3. 32,4. 79 μg/mL （ Tp1 = 0.08 h）, Cmax2 = 1.46,2.57,4.16 μg/mL（Tp2 =3 h）, respectively. CONCLUSION： Three kinds of flavonoids can be absorbed after ig administration of Xiexin Decoction in mice, of which baicalin is the major component.

关 键 词：泻心汤 黄芩苷 药动学 小鼠 

分 类 号：R285.6[医药卫生—中药学]