Contraception
Volume 53, Issue 1 , Pages 41-47, January 1996

Can grapefruit juice influence ethinylestradiol bioavailability?

  • A. Weber

      Affiliations

    • Department of Clinical Pharmacology Jena, Germany
    • ,
  • R. Jäger

      Affiliations

    • Clinic of Gynaecology Jena, Germany
    • ,
  • A. Börner

      Affiliations

    • Institute of Clinical Chemistry Jena, Germany
    • ,
  • G. Klinger

      Affiliations

    • Clinic of Gynaecology Jena, Germany
    • ,
  • R. Vollanth

      Affiliations

    • Department of Medical Informatics Jena, Germany
    • ,
  • K. Matthey

      Affiliations

    • Friedrich Schiller University of Jena, Jena, Germany
    • Jenapharm GmbH, Jena, Germany
    • ,
  • A. Balogh

      Affiliations

    • Corresponding Author InformationName and address for correspondence: A. Balogh, Ph.D., M.D., Department of Clinical Pharmacology, Friedrich Schiller University, Bachstr. 18, 07740 Jena, Germany
    • Department of Clinical Pharmacology Jena, Germany

Received 1 June 1995; received in revised form 2 October 1995; accepted 6 October 1995.

Abstract 

The effects of grapefruit juice on the bioavailability of 17α-ethinylestradiol (EE2) after a single oral administration of 50 μg EE2 have been investigated. The pharmacokinetics of EE2 were studied in an open, randomized, cross-over study in which 13 healthy volunteers were administered the drug with herbal tea or grapefruit juice (naringin, 887 mg/ml).

In contrast to herbal tea, grapefruit juice increased the peak plasma concentration (Cmax) significantly to 137% (mean; range 64% to 214%, p=0.0088) and increased the area under plasma concentration-time curve from 0 to 8 hours (AUC0–8) to 128% (mean; range 81% to 180%, p=0.0186).

This study shows that grapefruit juice increases the bioavailable amount of EE2. A possible explanation may be that grapefruit juice inhibits the metabolic degradation of EE2. Whether the increased bioavailability of EE2 following grapefruit juice administration is of clinical importance should be investigated in long-term studies.

Keywords:  17α-ethinylestradiol, pharmacokinetics, grapefruit juice, flavonoids, naringenin, cytochrome P450, food-drug interactions

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PII: 0010-7824(95)00252-9

Contraception
Volume 53, Issue 1 , Pages 41-47, January 1996

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