Advertisement

Disposition of quercetin in man after single oral and intravenous doses

  • R. Gugler
  • M. Leschik
  • H. J. Dengler
Article

Summary

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 α phase and 2.4±0.2 h for the β phase (predominant half life), respectively. Protein binding was >98%. The apparent volume of distribution was small at 0.34±0.03 l/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.

Key words

Quercetin flavonoids pharmacokinetics absorption disposition metabolism man 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    Courbat, P.: Quelques généralités sur les composés flavonoides. Angiologic9, 135–136 (1972)Google Scholar
  2. 2.
    Griffiths, L.A., Barrow, A.: The fate of orally and parenterally administered flavonoids in the mammal. Angiologic9, 162–174 (1972)Google Scholar
  3. 3.
    Griffiths, L.A., Smith, G.E.: Metabolism of myricetin and related compounds in the rat. Biochem. J.130, 141–151 (1972)Google Scholar
  4. 4.
    Griffiths, L.A., Smith, G.E.: Metabolism of apigenin and related compounds in the rat. Biochem. J.128, 901–911 (1972)Google Scholar
  5. 5.
    Griffiths, L.A.: Identification of the metabolites of (+)-catechin in rat urine. Biochem. J.92, 173–179 (1964)Google Scholar
  6. 6.
    Das, N.P., Scott, K.N., Duncan, J.H.: Identification of flavonone metabolites in rat urine by combined gas-liquid chromatography and mass spectrometry. Biochem. J.136, 903–909 (1973)Google Scholar
  7. 7.
    Das, N.P., Griffiths, L.A.: Metabolism of (+)-|14C|-catechin in the rat and guinea pig. Biochem. J.115, 831 (1969)Google Scholar
  8. 8.
    Das, N.P.: Studies on flavonoid metabolism. Absorption and metabolism of (+)-catechin in man. Biochem. Pharmacol.20, 3435–3445 (1971)Google Scholar
  9. 9.
    Clark, W.G., MacKay, E.M.: The absorption and excretion of rutin and related flavonoid substances. J. Amer. med. Ass.143, 1411–1415 (1950)Google Scholar
  10. 10.
    Porter, W.L., Dickel, D.F., Couch, J.F.: Determination of added rutin in urine. Arch. Biochem.21, 273 (1949)Google Scholar
  11. 11.
    Wienert, V., Gahlen, W.: Über die Ausscheidung von Trihydroxyäthylrutosid durch die Niere nach parenteraler und oraler Applikation. Hautarzt21, 278–279 (1970)Google Scholar
  12. 12.
    Gugler, R., Dengler, H.J.: Sensitive flurometric method for determination of quercetin in plasma or urine. Clin. Chem.19, 36–37 (1973)Google Scholar
  13. 13.
    Krieglstein, J., Kuschinsky, G.: Quantitative Bestimmungen der Eiweißbindung von Pharmaka durch Gelfiltration. Arzneimittel-Forsch.18, 287–289 (1968)Google Scholar
  14. 14.
    Riegelman, S., Loo, J.C.K., Rowland, M.: The shortcomings in pharmacokinetic analysis by conceiving the body to be a single compartment. J. pharm. Sci.57, 117–123 (1968)Google Scholar
  15. 15.
    Rescigno, A., Segre, G.: Drug and tracer kinetics, pp. 92–96. New York: Blaisdell Publishing Co. 1966Google Scholar
  16. 16.
    Wagner, J.G.: Pharmacokinetics, pp. 5–10. Grosse Pointe Park, Michigan: J.M. Richards Laboratory 1969Google Scholar
  17. 17.
    Barrow, A., Griffith, L.A.: The biliary excretion of hydroxyethylrutosides and other flavonoids in the rat. Biochem. J.125, 24 (1971)Google Scholar
  18. 18.
    Das, N.P., Sothy, S.P.: Biliary and urinary excretion of metabolites of (+)-[U-14C]-catechin. Biochem. J.125, 417–423 (1971)Google Scholar
  19. 19.
    Booth, A.N., Jones, F.T., DeEds, F.: Metabolic fate of hesperidin, eriodictyol, homoeriodictyol and diosmin. J. biol. Chem.230, 661–668 (1958)Google Scholar
  20. 20.
    Booth, A.N., Murray, C.W., Jones, F.T., DeEds, F.: The metabolic fate of rutin and quercetin in the animal body. J. biol. Chem.223, 251–257 (1956)Google Scholar
  21. 21.
    Gugler, R., Winther, D., Dengler, H.J.: unpublished results.Google Scholar

Copyright information

© Springer-Verlag 1975

Authors and Affiliations

  • R. Gugler
    • 1
  • M. Leschik
    • 1
  • H. J. Dengler
    • 1
  1. 1.Departments of MedicineUniversities of Giessen and BonnFederal Republic of Germany

Personalised recommendations