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

摘要

Background: The 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 Design: Sixteen 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. Results: The 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) nga??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. Conclusions: The present study described the single- and multiple-dose pharmacokinetic profiles of dienogest in Korean women and showed linear pharmacokinetics of dienogest at steady state.