Disposition of quercetin in man after single oral and intravenous doses

Eur J Clin Pharmacol. 1975 Dec 19;9(2-3):229-34. doi: 10.1007/BF00614022.

Abstract

The pharmacokinetics of quercetin, a flavonoid, have been studied in 6 volunteers after single intravenous (100 mg) and oral (4 g) doses. The data after iv administration were analyzed according to a two compartment open model with half lives of 8.8 +/- 1.2 min for the alpha phase and 2.4 +/- 0.2 h for the beta phase (predominant half life), respectively. Protein binding was greater than 98%. The apparent volume of distribution was small at 0.34 +/- 0.03 1/kg. Of the intravenous dose 7.4 +/- 1.2% was excreted in urine as a conjugated metabolite, and 0.65 +/- 0.1% was excreted unchanged. After oral administration no measurable plasma concentrations could be detected, nor was any quercetin found in urine, either unchanged or in a metabolized form. These results exclude absorption of more than 1% of unchanged drug. Recovery in faeces after the oral dose was 53 +/- 5%, which suggests extensive degradation by microorganisms in the gut. The data obtained show that oral administration of flavonoids may be of questionable value.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Adult
  • Blood Proteins / metabolism
  • Female
  • Flavonoids / metabolism*
  • Half-Life
  • Humans
  • Infusions, Parenteral
  • Kinetics
  • Male
  • Metabolic Clearance Rate
  • Protein Binding
  • Quercetin / administration & dosage
  • Quercetin / metabolism*

Substances

  • Blood Proteins
  • Flavonoids
  • Quercetin