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

摘要

Background: The pharmacokinetics of the monophasic oral contraceptive nomegestrol acetate (NOMAC) plus 17??-estradiol (E2) were investigated after a single dose and multiple dosing. Study design: NOMAC/E 2 (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. Results: NOMAC 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 (C max, 12.3??3.5 ng/mL) was reached in mean 1.5 h (t max); the mean??SD elimination half-life (t) was 45.9??15.3 h. After a single dose, NOMAC mean??SD Cmax was 7.2??2.0 ng/mL and mean??SD t 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 E2 Cmax was 253??179 pg/mL. Conclusions: These data demonstrate that NOMAC/E2 has a pharmacokinetic profile consistent with once-daily dosing. ? 2013 Elsevier Inc.