Pharmacokinetic profile of the isoflavone puerarin after acute and repeated administration of a novel kudzu extract to human volunteers

J Altern Complement Med. Jul-Aug 2006;12(6):543-8. doi: 10.1089/acm.2006.12.543.

Abstract

Objectives: 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.

Publication types

  • Clinical Trial
  • Research Support, N.I.H., Extramural

MeSH terms

  • Administration, Oral
  • Adult
  • Chromatography, High Pressure Liquid
  • Dose-Response Relationship, Drug
  • Humans
  • Isoflavones / administration & dosage*
  • Isoflavones / blood
  • Isoflavones / pharmacokinetics*
  • Male
  • Pueraria*
  • Reference Values
  • Reproducibility of Results
  • Vasodilator Agents / blood
  • Vasodilator Agents / pharmacokinetics*

Substances

  • Isoflavones
  • Vasodilator Agents
  • puerarin