2011•Chinese Journal of New Drugs and Clinical RemediesRequires access

Studies on preparation and pharmacokinetics of puerarin solid dispersions in vivo

Jinming Li

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Abstract

AIM To study the preparation of puerarin solid dispersions and pharmacokinetics in rabbits so as to increase the bioavailability of puerarin for oral.METHODS Dissolution test was used to determine the preparation prescription,puerarin concentrations in blood were determined by HPLC,and pharmacokinetic parameters were calculated using 3P97 pharmacokinetic program software.RESULTS The best preparation prescription was puerarin:PEG6000:pluronicF-68 =1:4:1(m/m/m).The concentration-time profiles of puerarin and puerarin solid dispersions were shown to fit two-compartment model absorption.The main pharmacokinetics parameters of puerarin and puerarin solid dispersions were:α(2.040±0.327),(0.870±0.191)·h~(-1);β(0.212±0.021),(0.351±0.022)·h~(-1);AUC_(0-∞)(11.966±1.370),(91.419±3.531) mg·L~(-1)·h; t_(max)(0.491±0.026),(1.423±0.035) h;ρ_(max)(3.917±0.066),(20.416±1.870) mg·L~(-1).The relative bioavailability of puerarin solid dispersions was 763.99%.CONCLUSION Puerarin solid dispersions can effectively enhance puerarin absorption in rabbits in vivo.

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AIM To study the preparation of puerarin solid dispersions and pharmacokinetics in rabbits so as to increase the bioavailability of puerarin for oral.METHODS Dissolution test was used to determine the preparation prescription,puerarin concentrations in blood were determined by HPLC,and pharmacokinetic parameters were calculated using 3P97 pharmacokinetic program software.RESULTS The best preparation prescription was puerarin:PEG6000:pluronicF-68 =1:4:1(m/m/m).The concentration-time profiles of puerarin and puerarin solid dispersions were shown to fit two-compartment model absorption.The main pharmacokinetics parameters of puerarin and puerarin solid dispersions were:α(2.040±0.327),(0.870±0.191)·h~(-1);β(0.212±0.021),(0.351±0.022)·h~(-1);AUC_(0-∞)(11.966±1.370),(91.419±3.531) mg·L~(-1)·h; t_(max)(0.491±0.026),(1.423±0.035) h;ρ_(max)(3.917±0.066),(20.416±1.870) mg·L~(-1).The relative bioavailability of puerarin solid dispersions was 763.99%.CONCLUSION Puerarin solid dispersions can effectively enhance puerarin absorption in rabbits in vivo.

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Available abstract

AIM To study the preparation of puerarin solid dispersions and pharmacokinetics in rabbits so as to increase the bioavailability of puerarin for oral.METHODS Dissolution test was used to determine the preparation prescription,puerarin concentrations in blood were determined by HPLC,and pharmacokinetic parameters were calculated using 3P97 pharmacokinetic program software.RESULTS The best preparation prescription was puerarin:PEG6000:pluronicF-68 =1:4:1(m/m/m).The concentration-time profiles of puerarin and puerarin solid dispersions were shown to fit two-compartment model absorption.The main pharmacokinetics parameters of puerarin and puerarin solid dispersions were:α(2.040±0.327),(0.870±0.191)·h~(-1);β(0.212±0.021),(0.351±0.022)·h~(-1);AUC_(0-∞)(11.966±1.370),(91.419±3.531) mg·L~(-1)·h; t_(max)(0.491±0.026),(1.423±0.035) h;ρ_(max)(3.917±0.066),(20.416±1.870) mg·L~(-1).The relative bioavailability of puerarin solid dispersions was 763.99%.CONCLUSION Puerarin solid dispersions can effectively enhance puerarin absorption in rabbits in vivo.

Key concepts: Puerarin, Pharmacokinetics, Bioavailability, Chromatography, Absorption (acoustics), Chemistry, Pharmacology, In vivo

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