丹参、川芎与葛根配伍对葛根素的大鼠药动学影响  

Effect of Radix and Rhizome on the Pharmacokinetics of Puerarin from Tongmai Granules in Rats

作　　者：韩凤梅[1] 潘莹[1] 杜鹏[1] 陈勇[1] 

机构地区：[1]湖北大学中药生物技术省重点实验室,武汉430062

出　　处：《中国药学杂志》2009年第19期1497-1499,共3页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金重点项目(30630075)

摘　　要：目的研究丹参、川芎与葛根配伍对葛根素的大鼠药动学性质的影响。方法Wistar大鼠分别灌胃给予葛根和复方葛根提取物(相当于葛根素单体300 mg.kg-1)后,采用高效液相色谱法测定不同时间点大鼠血浆中葛根素的含量,绘制各时间点平均药-时曲线,采用3P97药动学软件对数据进行处理。结果葛根素在大鼠体内的药动学行为符合开放二室模型,主要药动学参数有些不同,结果如下:葛根提取物组t1/2(ka)=(9.48±3.94)min,t1/2α=(13.74±3.67)min,t1/2β=(136.65±26.00)min,t(peak)=(29.02±11.94)min,ρ(max)=(0.90±0.26)mg.L-1,AUC=(186.10±49.57)mg.min.L-1,CL/F(s)=(1.72±0.53)L.kg-1.min-1,V/F(c)=(241.57±94.64)L.kg-1;复方葛根提取物组t1/2ka=(11.12±2.78)min,t1/2α=(27.65±7.06)min,t1/2β=(610.34±293.58)min,t(peak)=(24.50±4.56)min,ρmax=(2.57±1.34)mg.L-1,AUC=(571.64±504.22)mg.min.L-1,CL/F(s)=(0.84±0.55)L.kg-1.min-1,V/F(c)=(79.45±38.23)L.kg-1。结论丹参、川芎与葛根配伍使用,可以促进葛根素的吸收,提高其血药浓度,延长其体内作用时间。OBJECTIVE To study the influence of the compatibility of radix and rhizome with pueraria on the pharmacokinetics of puerarin in rats. METHODS The blood samples were collected at different time points after oral administration of the extracts from pueraria and compound recipe of pueraria （equivalent to 300 mg·kg^-1 puerarin） to Wistar rats respectively, then purified and chromatographic analyzed for the content of puerarin. RESULTS The mean plasma concentration-time curves of puerarin after oral administration of the extracts from pueraria and compound recipe of pueraria were fitted to two compartment open model. There were somewhat difference in the major pharmacokinetic parameters. The pharmacokinetic parameters of the group treated with the extract of pueraria were as follows： t1/2（ka） （9.48±3.94） min, t1/2α （13.74±3.67） min, t1/2β=（136.65±26.00）min, t（peak）（29.02±11.94）min, Pmax（0.90±0.26）mg·L^-1, AUC（186.10±49.57）mg·min·L^-1, CL/F（s）（1.72±0.53）L·kg^-1·min^-1, V/F（c）（241.57±94.64）L·kg^-1. The pharmacokinetic parameters of the group treated with the extract of compound recipe of pueraria were as follows： tx/2ka（11.12±2.78）min, t1/2α（27.65±7.06）min, t1/2α（610.34±293.58）min, t（peak）（24.50±4.56）min, pmax（2.57±1.34）mg·L^-1, AUC=（571.64±504.22）mg·min·L^-1, CL/F（s）（0.84±0.55）L·kg^-1·min^-1, V/F（c）= （79.45±38.23） L·kg^-1. CONCLUSION The work proved that the compatibility of radix and rhizome with pueraria can promote the absorption, increase the blood drug concentration and prolong the action time of puerarin in vivo.

关 键 词：葛根 复方葛根 葛根素 药动学 

分 类 号：R969[医药卫生—药理学]