天钩降压胶囊中天麻苷在大鼠体内药动学研究

Pharmacokinetics of gastrodin from Tiangou Jiangya capsule in rats

研究天钩降压胶囊复方配伍及不同剂量对大鼠体内天麻苷药动学的影响。大鼠分别灌胃给予低、中、高剂量天钩降压胶囊(剂量分别相当于天麻苷8.410,16.82,33.64 mg·kg-1)及天麻提取物(剂量相当于天麻苷16.82 mg·kg-1),于不同时间点采集血浆。血浆样品经乙腈处理,HPLC测定天麻苷含量。平均血药浓度-时间数据用3P97药动学程序拟合,组间药动学参数用SPSS 16.0分析。结果显示,天麻苷口服给药在大鼠体内符合一室模型,天钩降压胶囊的Cmax,AUC与给药剂量成正比关系,t1/2Ka与剂量无关,表明天麻苷口服体内转运符合一级速度过程;与天麻提取物比较,等剂量天钩降压胶囊的Cmax,Ke显著减小,t1/2Ke,V/Fc显著增加,表明复方配伍能延缓天麻苷吸收,延长体内滞留时间,且有促进天麻苷体内分布的趋势,但对生物利用度无显著影响。

The paper aims to study the pharmacokinetic parameters of gastrodin in rats effected by compound compatibilitiy and different doses of Tiangou Jiangya capsule.The extracts from Gastrodiae Rhizoma（equivalent to gastrodin 16.82 mg · kg- 1） and Tiangou jiangya capsule（equivalent to gastrodin 8.410,16.82,33.64 mg·kg- 1） were oral administrated to rats respectively.The plasma were taken at various time points and treated with acetonitrile to measure the contents of gastrodin by HPLC method.The mean plasma concentration-time data were analyzed by 3P97 pharmacokinetic software and the pharmacokinetic parameters between groups were treated by SPSS 16.0.The results showed that gastrodin in rat was fitted to one-compartment model,Cmaxand AUC of Tiangou Jiangya capsule were in direct proportion to oral administration,and t1 /2Ka had nothing to do with doses,which indicated that gastrodin was fitted first-order rate transfter process in vivo.Morever,comparison with the Gastrodiae Rhizoma extract,isodose gastrodin in Tiangou Jiangya capsule showed a significant decrease for Cmax,Keand increase for t1 /2Ke,V/Fc,this indicated that compound compatibility can delay the absorbtion of gastrodin,prolong the resident time and promote the distribution in vivo,but its bioavailability is not significantly effected.