Pharmacokinetic profile of nomegestrol acetate and 17β-estradiol after multiple and single dosing in healthy women

BackgroundThe pharmacokinetics of the monophasic oral contraceptive nomegestrol acetate (NOMAC) plus 17β-estradiol (E2) were investigated after a single dose and multiple dosing.Study designNOMAC/E2 (2.5 mg/1.5 mg) was administered daily to healthy women (18–50 years, n= 23) for 24 days; blood samples for pharmacokinetic analysis were obtained on Day 24 and again, after a 10-day pill-free interval, on Day 35 after a single dose.ResultsNOMAC reached steady state after 5 days with mean ± standard deviation (SD) trough NOMAC concentration (Cav) of 4.4±1.4 ng/mL. On Day 24, mean±SD peak NOMAC concentration (Cmax, 12.3±3.5 ng/mL) was reached in mean 1.5 h (tmax); the mean±SD elimination half-life (t½) was 45.9±15.3 h. After a single dose, NOMAC mean±SD Cmax was 7.2±2.0 ng/mL and mean±SD t½ was 41.9±16.2 h. On Day 24, E2 mean±SD Cav was 50.3±25.7 pg/mL; mean±SD Cmax was 86.0±51.3 pg/mL. After a single dose, mean±SD E2Cmax was 253±179 pg/mL.ConclusionsThese data demonstrate that NOMAC/E2 has a pharmacokinetic profile consistent with once-daily dosing.