Pharmacokinetic profile of the isoflavone puerarin after acute and repeated administration of a novel kudzu extract to human volunteers.
OBJECTIVE
This study was undertaken to assess the pharmacokinetic profile of puerarin, the major isoflavone found in a kudzu (Pueraria lobata) extract after acute and repeated administration.


METHODS
Participants were given either single or repeated doses of kudzu extract, and blood samples were collected for either 8 or 72 hours for subsequent pharmacokinetic analyses of puerarin.


RESULTS
Using WinNonlin pharmacokinetic data analysis software, puerarin was found to be rapidly absorbed via the oral route, reach peak levels at 2 hours, and have a half-life of approximately 4.3 hours. The elimination half-life was not significantly altered after repeated administration.


CONCLUSIONS
A formulation of kudzu extract delivers a large amount of the principal isoflavone in a rapid manner. The elimination rate constants and the mono-exponential decline in blood levels suggest that a one compartment model adequately explains how puerarin is handled by the body. Three times a day dosing is recommended as accumulation will not occur, and plasma levels remain at levels that are biologically active, even 8 hours after the last steady-state dose.
Penetar
David M
DM
Behavioral Psychopharmacology Research Laboratory, McLean Hospital, Belmont, MA 02478, USA. dpenetar@mclean.harvard.edu
Teter
Christian J
CJ
Ma
Zhongze
Z
Tracy
Michael
M
Lee
David Y-W
DY
Lukas
Scott E
SE
D000284:Administration, Oral; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007529:Isoflavones / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D029908:Pueraria; D012016:Reference Values; D015203:Reproducibility of Results; D014665:Vasodilator Agents / Q000097:blood / Q000493:pharmacokinetics*
D007529:Isoflavones; D014665:Vasodilator Agents; C033607:puerarin