不同配伍泻心汤对黄芩苷代谢动力学的影响

Pharmacokinetic effect of different extraction of Xiexin Decoction on baicalin in rats

目的 :研究泻心汤中大黄的不同提取方法对黄芩苷在大鼠体内代谢过程的影响。方法:大鼠分别灌胃大黄水煎液+黄芩苷+黄连总生物碱,大黄游离蒽醌+黄芩苷+黄连总生物碱以及黄芩苷后0.5、1、2、3、8、24小时取血,分离血浆,用高效液相仪测定黄芩苷的含量。结果:大黄水煎液+黄芩苷+黄连总生物碱组黄芩苷的药代动力学参数为t1/2=(54.19±112.67)h,AUC=(10982.33±17515.24)μg/L.h,Cmax=(9.88±7.95)μg/L,MRT=(95.86±54.24)h,Vd=(2318634.61±4588242.95)L/kg,CL=(29762.82±39003.52)L/h/kg,Tmax=(11.20±7.16)h;大黄游离蒽醌+黄芩苷+黄连总生物碱组黄芩苷的药代动力学参数为t1/2=(6.49±6.83)h,AUC=(3433.04±4193.84)μg/L.h,Cmax=(6.10±3.06)μg/L,MRT=(23.84±7.08),Vd=(652463.39±4930818.35)L/kg,CL=(36292.44±49581.85)L/h/kg,Tmax=(5.00±4.11)h;黄芩苷组黄芩苷的药代动力学参数为t1/2=(8.85±7.61)h,AUC=(439.05±370.73)μg/L.h,Cmax=(7.30±1.65)μg/L,MRT=(25.36±3.35)h,Vd=(188123.41±274588.24)L/kg,CL=(8759.87±11715.64)L/h/kg,Tmax=(2.00±3.36)h。结论:大黄、黄芩和黄连配伍可以促进黄芩苷在机体内的的吸收,大黄水煎液还可以显著延长黄芩苷在机体内的半衰期,使黄芩苷的血药浓度维持在较高水平。

Objective： To study the effect of different extraction of Rhubard in Xiexin Decoction on the pharmacokinetic parameters of baicalin in rats.Methods： SD rats were divided into 3 groups.Rats were administered intragastrically with Rhubard decoction＋baicalin＋ total alkaloid of Coptis chinensis,free anthraquinone of Rhubarb＋ baicalin＋ total alkaloid of Coptis chinensis,or baicalin separately.At 0.5,1,2,3,8,24 hours after treatment,the blood were collected and the baicalin were analyzed by HPLC.And the data were processed with DAS3.0 pharmacokinetic program.Results： The pharmacokinetic parameters of baicalin of the Rhubard decoction＋baicalin＋ total alkaloid of Coptis chinensis were as follows： t1/2=（54.19±112.67）h,AUC=（10982.33±17515.24）μg/L＊h,Cmax=（9.88±7.95）μg/L,MRT=（95.86± 54.24）h,Vd=（2318634.61±4588242.95）L/kg,CL=（29762.82±39003.52）L/h/kg,Tmax=（11.20±7.16）h;the free anthraquinone of Rhubarb＋ baicalin＋ total alkaloid of Coptis chinensis group： t1/2=（6.49±6.83）h,AUC=（3433.04±4193.84）μg/L＊h,Cmax=（6.10±3.06）μg/L,MRT=（23.84±7.08）,Vd=（652463.39±4930818.35）L/kg,CL=（36292.44±49581.85）L/h/kg,Tmax=（5.00±4.11）h;And the baicalin group： t1/2=（8.85±7.61）h,AUC=（439.05±370.73）μg/L＊h,Cmax=（7.30±1.65）μg/L,MRT=（25.36±3.35）h,Vd=（188123.41±274588.24）L/kg,CL=（8759.87±11715.64）L/h/kg,Tmax=（2.00±3.36）h.Conclusion： The results indicated that the compatibility of rhubard,coptis and scutellaria can promote the absorption of baicalin.And Rhubard decoction can significantly extend the half-life time of baicalin,and keep the blood concentration of baicalin at a higher level.