Effect of a standardized meal on the bioavailability of a single oral dose of tibolone 2.5 mg in healthy postmenopausal women

Pharmacotherapy
Cees J Timmer, Johannes A M Huisman

Abstract

To assess the effect of food on absorption and pharmacokinetic disposition of tibolone. Open-label, randomized, crossover study with a 1-week washout period. Institut für Klinische Pharmakologie, Hohenkirchen-Siegertsbrunn, Germany Twenty-four healthy, early postmenopausal women. Single doses of tibolone 2.5 mg were administered after subjects consumed a high-fat meal or fasted. Plasma concentrations of tibolone and its three primary metabolites, delta4-tibolone, 3alpha-hydroxytibolone, and 3beta-hydroxytibolone, were assayed by gas chromatography with mass spectrometry. Peak plasma concentration (Cmax), time to Cmax, area under the plasma concentration versus time curve from time zero to infinity (AUC(0-infinity)), and elimination half-life were calculated, and food effects were evaluated. Plasma concentrations of tibolone and delta4-tibolone were too low to estimate AUC(0-infinity) and half-life. Absorption or formation of 3alpha-hydroxytibolone and 3beta-hydroxytibolone was slower in fed participants than in fasting participants, but this was of no clinical relevance because of the long-term nature of tibolone treatment. Meal consumption did not affect AUC(0-infinity) or half-life for 3alpha-hydroxytibolone and 3beta-hydroxy...Continue Reading

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