Studies on Pharmacokinetics and Bioavailability of Puerarin in Yufeng Ningxin Tablet in Mice / 中药新药与临床药理

Objective To evaluate the pharmacokinetic parameters and bioavailability of puerarin in Yufeng Ningxin tablets in mice by determining dose-time curve and by comparing with the pharmacokinetics of puerarin injection.Methods NIH mice were randomized into different groups. 6 %HClO4 was used to precipitate plasma protein and the plasma concentration of puerarin in mice was determined by HPLC.The PK solutions 2.0 program,a non-compartmental model software,was applied to calculate the pharmacokinetic parameters and bioavailability.Results The main pharmacokinetic parameters of puerarin injection by i.v.in mice were:t1/2=98.359 min,CL=35.548 mL?min-1,AUC(0-∞)=281.3 ?g?min?mL-1;the main pharmacokinetic parameters of puerarin in Yufeng Ningxin tablets by o.p.were:t1/2 =35.562 min,CL=898.685 mL?min-1,Cmax=9.3 ?g?mL-1,Tmax=30 min,AUC(0-∞)=222.5 ?g?min?mL-1 ,F(bioavailability value)=3.95 %comparing to puerarin injection.Conclusion As compared with puerarin injection,the absorptive content of puerarin in Yufeng Ningxin tablets is very poor and the bioavailability is also low,indicating that enhancement of bioavailability of Yufeng Ningxin tablets will be beneficial to the clinical application.

Pharmacokinetics and bioavailability of Yufeng Ningxin Tablet in Beagle dog / 中成药

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 auto-control 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 t_(1/2E) 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 ?g/min/mL,and the t_(1/2E) of puerarin in Yufeng Ningxin Tablets(10.49 mg/kg) by oral administration was 271.80?7.94 min, CL was 48.52?(2.20) mL/min,C_(max) was 0.43?0.06 ?g/mL, T_(max) was 150 min, AUC_((0-∞)) was 185.77?8.20 ?g/min/mL,and bioavailability was 7.03% compared to puerarin injection by intravenous injection. CONCLUSION: The absorption of puerarin 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.