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

ABSTRACT

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.