2011Zhonghua zhongyiyao zazhiRequires access

Study on pharmacokinetics of puerarin in rats by following different methods of administration of puerariae extract

Huixian Zhang

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Abstract

Objective: To study pharmacokinetics of Puerarin in Rats Following Different Methods of Administration of Puerarin Extract.Methods: Rats received 20 mg/kg puerarin extract by caudal vein injection,20 mg/kg puerarin extract by nasal administration and 200 mg/kg puerarin extract by oral administration.Plasma samples were extracted with methanol and the plasma concentration of puerarin was analyzed by RP-HPLC.The pharmacokinetic parameters and bioavailability were calculated with Kinetica software.Results: Within range of(0.05315-53.1500) mg/L,puerarin presented a fine linear relationship(r=0.9999).The average recovery of puerarin was 95.72% with RSD 2.3%.The main pharmacokinetic parameters were as follows: caudal vein injection: AUC=(795.41±59.85)mg·L-1·min-1,Cmax=(65.74±7.71)μg/mL,MRT=(18.96±2.08)min,t1/2=(16.95±3.55)min,nasal administration: AUC=(227.34±19.42)mg·L-1·min-1,Cmax=(3.78±1.80)μg/mL,Tmax=(7.50±2.74)min,MRT=(117.09±38.37)min,t1/2=(22.50±10.60)min;oraladministration: AUC=(732.48±471.57)mg·L-1·min-1,Cmax=(3.53±1.32)μg/mL,Tmax=(27.00±16.43)min,MRT=(394.22±209.24)min,t1/2=(237.84±112.39)min.Conclusion: There were significant differences among the main pharmacokinetic parameters of puerarin following different methods of administration of puerarin extract,nasal administration could lead to a quick absorption and its bioavailability was higher than oral administration,this result can provide some scientific basises for the method of administration and the reform of dosage form of puerarin extract.

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Objective: To study pharmacokinetics of Puerarin in Rats Following Different Methods of Administration of Puerarin Extract.Methods: Rats received 20 mg/kg puerarin extract by caudal vein injection,20 mg/kg puerarin extract by nasal administration and 200 mg/kg puerarin extract by oral administration.Plasma samples were extracted with methanol and the plasma concentration of puerarin was analyzed by RP-HPLC.The pharmacokinetic parameters and bioavailability were calculated with Kinetica software.Results: Within range of(0.05315-53.1500) mg/L,puerarin presented a fine linear relationship(r=0.9999).The average recovery of puerarin was 95.72% with RSD 2.3%.The main pharmacokinetic parameters were as follows: caudal vein injection: AUC=(795.41±59.85)mg·L-1·min-1,Cmax=(65.74±7.71)μg/mL,MRT=(18.96±2.08)min,t1/2=(16.95±3.55)min,nasal administration: AUC=(227.34±19.42)mg·L-1·min-1,Cmax=(3.78±1.80)μg/mL,Tmax=(7.50±2.74)min,MRT=(117.09±38.37)min,t1/2=(22.50±10.60)min;oraladministration: AUC=(732.48±471.57)mg·L-1·min-1,Cmax=(3.53±1.32)μg/mL,Tmax=(27.00±16.43)min,MRT=(394.22±209.24)min,t1/2=(237.84±112.39)min.Conclusion: There were significant differences among the main pharmacokinetic parameters of puerarin following different methods of administration of puerarin extract,nasal administration could lead to a quick absorption and its bioavailability was higher than oral administration,this result can provide some scientific basises for the method of administration and the reform of dosage form of puerarin extract.

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Available abstract

Objective: To study pharmacokinetics of Puerarin in Rats Following Different Methods of Administration of Puerarin Extract.Methods: Rats received 20 mg/kg puerarin extract by caudal vein injection,20 mg/kg puerarin extract by nasal administration and 200 mg/kg puerarin extract by oral administration.Plasma samples were extracted with methanol and the plasma concentration of puerarin was analyzed by RP-HPLC.The pharmacokinetic parameters and bioavailability were calculated with Kinetica software.Results: Within range of(0.05315-53.1500) mg/L,puerarin presented a fine linear relationship(r=0.9999).The average recovery of puerarin was 95.72% with RSD 2.3%.The main pharmacokinetic parameters were as follows: caudal vein injection: AUC=(795.41±59.85)mg·L-1·min-1,Cmax=(65.74±7.71)μg/mL,MRT=(18.96±2.08)min,t1/2=(16.95±3.55)min,nasal administration: AUC=(227.34±19.42)mg·L-1·min-1,Cmax=(3.78±1.80)μg/mL,Tmax=(7.50±2.74)min,MRT=(117.09±38.37)min,t1/2=(22.50±10.60)min;oraladministration: AUC=(732.48±471.57)mg·L-1·min-1,Cmax=(3.53±1.32)μg/mL,Tmax=(27.00±16.43)min,MRT=(394.22±209.24)min,t1/2=(237.84±112.39)min.Conclusion: There were significant differences among the main pharmacokinetic parameters of puerarin following different methods of administration of puerarin extract,nasal administration could lead to a quick absorption and its bioavailability was higher than oral administration,this result can provide some scientific basises for the method of administration and the reform of dosage form of puerarin extract.

Key concepts: Puerarin, Pharmacokinetics, Cmax, Bioavailability, Oral administration, Pharmacology, High-performance liquid chromatography, Absorption (acoustics)

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