2004•Traditional Chinese Drug Research and Clinical PharmacologyRequires access

Studies on Pharmacokinetics and Bioavailability of Puerarin in Yufeng Ningxin Tablet in Mice

Ji Lin

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Abstract

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 μg·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 μg·mL-1,Tmax=30 min,AUC(0-∞)=222.5 μg·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.

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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 μg·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 μg·mL-1,Tmax=30 min,AUC(0-∞)=222.5 μg·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.

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Available abstract

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 μg·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 μg·mL-1,Tmax=30 min,AUC(0-∞)=222.5 μg·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.

Key concepts: Puerarin, Bioavailability, Pharmacokinetics, Cmax, Pharmacology, Chemistry, Chromatography, High-performance liquid chromatography

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