Pharmacokinetic study of single and multiple oral administrations of 2 mg dienogest in healthy Korean women

Abstract

BackgroundThe progestin dienogest was developed for oral contraception, endometriosis treatment and menopause management. Dienogest's pharmacokinetics have been primarily studied in Caucasian women. This study evaluated the single- and multiple-dose pharmacokinetics of dienogest in Korean women. Study DesignSixteen healthy Korean adult women received a single administration of 2 mg dienogest, followed by multiple once-daily administrations for 14 days. The single-dose administration and the final dose of the multiple administrations were each followed by blood sampling over 60 h. ResultsThe mean (SD) maximum serum concentration after multiple doses of dienogest was slightly increased compared with that after a single dose [from 51.6 (9.6) to 56.6 (11.9) ng/mL], as was the area under the concentration–time curves (AUC)0–24h [from 503 (56.3) to 613 (90.7) ng∙h/mL]. The linearity factor calculated by AUCs of single and multiple doses is 1.00±0.14, and the terminal half-life remained unchanged when single dosing and multiple dosing were compared. ConclusionsThe present study described the single- and multiple-dose pharmacokinetic profiles of dienogest in Korean women and showed linear pharmacokinetics of dienogest at steady state.