仔猪口服牛蒡子提取物牛蒡苷元的药动学研究

Pharmacokinetic of Fructus arctii extract Arctigenin in piglets

牛蒡子又名大力子,是一种常用中药,牛蒡苷元为其直接有效成份。研究牛蒡子粉经水提处理后,提取物粉剂中有效成分牛蒡苷元在仔猪体内的药物代谢动力学特征,了解牛蒡子水体物中牛蒡苷元在仔猪体内的吸收、分布、代谢和排泄的变化规律,为牛蒡子提取物在兽医临床用药中提供参考和数据支撑。试验选取健康仔猪6头(30.0±5.0 kg),以1.0 g/kg.bw的提取物灌胃给药,给药后分别于不同设计的时间点采集前腔静脉血,利用HPLC法对仔猪血浆中的牛蒡苷元药物浓度进行检测分析。试验发现:灌胃给药后,牛蒡子水提物粉剂中有效成分牛蒡苷元在仔猪体内的药时曲线符合有吸收二室模型,吸收半衰期(t1/2ka)为0.098±0.006 h,分布半衰期(t1/2α)0.208±0.009 h;消除半衰期(t1/2β)23.816±2.151 h;表观分布容积(Vd)32.212±4.033 L/kg;清除率(CLb)2.384±1.589 L/(h.kg);达峰时间(tmax)为0.251±0.011 h,峰浓度(Cmax)为0.560±0.063μg/mL,药时曲线下面积(AUC)9.620±0.752μg.h/mL。结果表明:牛蒡子水提物中有效成分牛蒡苷元经仔猪口灌给药后,在其体内吸收迅速、分布极为广泛、代谢消除缓慢,能够较长时间发挥药理作用。

In order to study the pharmacokinetic characteristics of Arctigenin from water extract of Fructus arctii in piglets,understand its absorption,distribution,transformation and excretion in piglets,and provide theoretical reference for the development and clinical use of new veterinary drugs.Six healthy piglets(30.0±5.0 kg)were selected and administered by gavage with a 1.0 g/kg.bw Fructus arctii water extract.Blood was collected from the anterior vena cava at different time points.The concentration of Arctigenin in pig plasma was determined by HPLC.Perform analysis.After the absorption.The main pharmacokinetic parameters are:absorption half-life(t1/2ka)is 0.098±0.006 h,and distribution half-life(t1/2α)is 0.208±0.009 h;Elimination half-life(t1/2β)23.816±2.151 h;apparent volume of distribution(Vd)32.212±4.033 L/kg;apparent volume of distribution(Vd)32.212±4.033 L/kg;clearance(CLb)2.384±1.589 L/(h.kg);peak time(tmax)is 0.251±0.011 h,the peak concentration(Cmax)was 0.560±0.063μg/mL,and the area under the curve(AUC)at the time of drug administration was 9.620±0.752μg.h/mL.The experiment showed that the Arctigenin was orally irrigated in piglets after being irrigated,the distribution was very extensive,the metabolism was eliminated slowly,and the pharmacological effect could be exerted for a long time.