愈风宁心片中葛根素在Beagle犬体内药动学研究

Pharmacokinetics and bioavailability of Yufeng Ningxin Tablet in Beagle dog

目的:研究愈风宁心片(葛根总黄酮)中主要有效成分葛根素在狗体内的药-时曲线,计算其在狗体内的药动学参数;并与静注葛根素注射液比较,研究愈风宁心片中葛根素的绝对生物利用度。方法:本文应用自身对照设计试验法,单剂量一次给予狗静脉注射葛根素注射液或口服愈风宁心片。采用HPLC法测定狗血浆中葛根素的浓度,应用PK solu-tions 2.0程序计算药动学参数和生物利用度。结果:静脉注射葛根素注射液(9 mg/kg)的药动学参数分别为:t1/2E=(72.11±3.69)m in,CL=(4.19±0.25)mL/m in,AUC(0-∞)=(2 172.42±123.02)μg/m in/mL。口服愈风宁心片(相当于葛根素10.49 mg/kg)的药动学参数分别为t1/2E=(271.80±7.94)m in,CL=(48.52±2.20)mL/m in,Cm ax=(0.43±0.06)μg/mL,Tm ax=150 m in,AUC(0-∞)=(185.77±8.20)μg/m in/mL,绝对生物利用度为7.03%。结论:狗口服愈风宁心片片中葛根素在狗体内的吸收较少,生物利用度较低。

AIM ： The plasma concentration-time curve, pharmacokinetic parameters and bioavilability of puerarin, the main active constituent of Yufeng Ningxin Tablets （total flavone of Radix Puerariae Lobatae） in dog by oral administration was determined, and the pharmacokinetics was compared with puerarin injection by intravenous injection individually. METHODS： A single dose （the puerarin amount to 10.49 mg/kg） of Yufeng Ningxin Tablets by oral administration and puerarin injection by intravenous injection （9 mg/kg） were given to dogs in a autocontrol way. The concentration of puerarin in plasma was determined by HPLC. The PK solutions 2.0 program, a non-compartmental model software, was applied to calculate the pharmacokinetic parameters. RESULTS： 1. The pharmacokinetic parameters of puerarin in dog showed that the t1/2E f puerarin injection （9 mg/kg） by i. v was 72.11 ± 3.69 min, CL was 4.19 ± 0.25 mL/min, AUC（0-∞）was 2172.42 ± 123.02 μg/min/mL, and the t1/2E of puerafin in Yufeng Ningxin Tablets （ 10.49 mg/kg） by oral administration was 271.80 ± 7.94 min, CL was 48.52 ±2.20 mL/Mmin,Cmax was 0.43 ± 0.06 μg/mL, T was 150 min, AUC（0-∞） was 185.77 ± 8.20 μg/min/mL,and bioavailability was 7.03% compared to puerarin injection by intravenous injection. CONCLUSION： The absorption of puerafin in Yufeng Ningxin Tablets by oral administration comparing with puerarin injection by intravenous injection in dog is very poor, and the bioavailabilites is also low.