黄芩与五味子配伍对黄芩苷、五味子酯甲代谢动力学的影响

Effect of Radix Scutellariae and Fructus Schisandrae on Pharmacokinetic Parameters of Baicalin and Wuweizi Ester A Indica in Rats

目的:研究黄芩与五味子配伍对黄芩苷和五味子酯甲的大鼠药代动力学规律的影响。方法:大鼠灌胃黄芩提取物2.5 g.kg-1﹑五味子提取物2.5 g.kg-1和黄芩提取物加五味子提取物各2.5 g.kg-1,分别于0.25,1,2,4,8,12,24 h取血分离血浆,采用HPLC测定其黄芩苷﹑五味子酯甲的含量,结果运用DAS 3.0计算其药动学参数。结果:测定黄芩组黄芩苷的药动学参数分别为t1/2=(6.203±3.324)h,AUC=(41.868±28.254)μg.L-1.h-1,Cmax=(2.883±0.684)μg.L-1,MRT=(11.697±4.108)h,Vd=(568 112.69±81 364.658)L.kg-1,CL=(98 526.569±93 774.892)L.h-1.kg-1;黄芩+五味子组黄芩苷的药动学参数分别为t1/2=(10.686±1.533)h,AUC=(53.064±30.047)μg.L-1.h-1,Cmax=(3.168±1.312)μg.L-1,MRT=(16.147±1.79)h,Vd=(2 240 724.1±1 824 718.9)L.kg-1,CL=(139 855.27±107 995.59)L.h-1.kg-1;黄芩+五味子组五味子酯甲的药动学参数分别为t1/2=(21.544±14.611)h,AUC=(11.554±5.516)μg.L-1.h-1,Cmax=(0.311±0.074)μg.L-1,MRT=(34.139±18.532)h,Vd=(12 153 917±5 806 489.8)L.kg-1,CL=(564 758.71±384 128.86)L.h-1.kg-1;五味子组五味子酯甲的药动学参数分别为t1/2=(4.926±5.371)h,AUC=(4.988±3.029)μg.L-1.h-1,Cmax=(0.287±0.071)μg.L-1,MRT=(12.002±6.854)h,Vd=(3 091.656±1 585.602)L.kg-1,CL=(615.571±250.643)L.h-1.kg-1。结论:黄芩与五味子配伍,可以促进黄芩苷和五味子酯甲在血液中的吸收,并可延长这两种成分的半衰期,使其血药浓度维持在较高水平,达到协同增效的目的。

Objective: To explore the absorption,distribution,metabdism and excretion(ADME) of baicalin from Radix Scutellariae and wuweizi ester A from Fructus Schisandrae in rats.Method: SD rats were orally administration of the extracts from Radix Scutellariae 2.5 g·kg-1,Fructus Schisandrae 2.5 g·kg-1,or Radix Scutellariae 2.5 g·kg-1 with Fructus Schisandrae 2.5 g·kg-1 once separately.Then the blood samples were collected at 0.25,1,2,4,8,12,24 h after treatment.Baicalin and wuweizi ester A were analyzed by HPLC.The data were processed with DAS 3.0 pharmacokinetic program.Result: The pharmacokinetic parameters of baicalin of Radix Scutellariae group were as follows: t1/2=(6.203±3.324)h,AUC=(41.868±28.254) μg·L-1·h-1,Cmax=(2.883±0.684) μg·L-1,MRT=(11.697±4.108) h,Vd=(568 112.69±81 364.658) L·kg-1,CL=(98 526.569±93 774.892)L·h-1·kg-1,and the Radix Scutellariae with Fructus Schisandrae group: t1/2=(10.686±1.533)h,AUC=(53.064±30.047) μg·L-1·h-1,Cmax=(3.168±1.312) μg·L-1,MRT=(16.147±1.79) h,Vd=(2 240 724.1±1 824 718.9)L·kg-1,CL=(139 855.3±107 995.6)L·h-1·kg-1.The pharmacokinetic parameters of wuweizi ester A of the Radix Scutellariae with Fructus Schisandrae group were as follows: t1/2=(21.544±14.611)h,AUC=(11.554±5.516) μg·L-1·h-1,Cmax=(0.311±0.074) μg·L-1,MRT=(34.139±18.532) h,Vd=(12 153 917±5 806 489.8)L·kg-1,CL=(564 758.71±384 128.86) L·h-1·kg-1;And the fructus schisandrae group were as follows: t1/2=(4.926±5.371)h,AUC=(4.988±3.029)μg·L-1·h-1,Cmax=(0.287±0.071)μg·L-1,MRT=(12.002±6.854)h,Vd=(3 091.656±1 585.602)L·kg-1,CL=(615.571±250.643)L·h-1·kg-1.Conclusion: The results indicated that the compatibility of Radix Scutellariae with Fructus Schisandrae can increase the blood concentration and prolong half-life of baicalin and wuweizi ester A,it may be related to the synergy protective action of Radix Scutellariae with Fructus Schisandrae on liver fibrosis.