Abstract
Objective To investigate the pharmacokinetics of drospirenone (DRSP) and ethinylestradiol (EE) in Caucasian and Japanese women.Method Three open-label, non-randomised studies were performed to assess the pharmacokinetics following single doses of EE 0.02 mg/DRSP 3 mg or DRSP monotherapy (1, 3 or 6 mg) in Caucasian (Study 1) and Japanese (Study 2) women, and daily doses with EE 0.02 mg/DRSP 3 mg over 21 consecutive days in Caucasian and Japanese women (Study 3).Results In Studies 1 and 2, there was a linear dose-dependent increase in DRSP Cmax and systemic exposure across the range of doses used in both ethnic groups. The co- administration of EE had no relevant effect on the pharmacokinetic parameters of 3 mg DRSP. In Study 3, steady-state DRSP concentrations were achieved after about eight days of treatment in both ethnic groups with approximately a threefold accumulation. There was about a twofold EE accumulation over 21 days in both ethnic groups. There were no differences in DRSP or EE exposure at day 21 between ethnic groups; the ratio of the geometric means (Japanese/Caucasian) of the AUC0–24h were 1.05 (90% CI: 0.95–1.17) and 1.02 (90% CI: 0.76–1.38), respectively.Conclusion Ethnic origin had no clinically relevant influence on the pharmacokinetics of DRSP and EE.
Highlights
Ethinylestradiol (EE) and drospirenone (DRSP) are the active components of several oral contraceptives (OCs).The standard dose is EE 0.03 mg/DRSP 3 mg (e.g., OcellaTM, Barr Laboratories, Inc.; SyedaTM, Sandoz; Yasmin®, Bayer HealthCare Pharmaceuticals; Zarah®, Watson Pharmaceuticals) and a low-dose EE/DRSP formulation has been developed consisting of EE 0.02 mg within betacyclodextrin clathrate in combination with DRSP 3 mg (EE 0.02 mg/DRSP 3 mg, e.g., GianviTM, Teva Pharmaceuticals; LorynaTM, Sandoz; Yaz®, Bayer HealthCare Pharmaceuticals)
The inclusion of EE within a betadex-clathrate when combined with DRSP does not affect single-dose pharmacokinetics and the relative bioavailability of either EE or DRSP1
Some early studies suggested that ethnic differences may alter the pharmacokinetics of contraceptive steroids[2,3,4], whereas others pointed to the absence of such an effect[5,6]
Summary
Ethinylestradiol (EE) and drospirenone (DRSP) are the active components of several oral contraceptives (OCs).The standard dose is EE 0.03 mg/DRSP 3 mg (e.g., OcellaTM, Barr Laboratories, Inc.; SyedaTM, Sandoz; Yasmin®, Bayer HealthCare Pharmaceuticals; Zarah®, Watson Pharmaceuticals) and a low-dose EE/DRSP formulation has been developed consisting of EE 0.02 mg within betacyclodextrin (betadex) clathrate in combination with DRSP 3 mg (EE 0.02 mg/DRSP 3 mg, e.g., GianviTM, Teva Pharmaceuticals; LorynaTM, Sandoz; Yaz®, Bayer HealthCare Pharmaceuticals). In the clinical development of the EE 0.02 mg/ DRSP 3 mg OCs, three studies were performed in Caucasian and Japanese women with the aim of comparing the pharmacokinetic profile between the two ethnic groups.These studies included pharmacokinetic analysis of single and multiple doses of 0.02 mg/DRSP 3 mg as well as single doses of DRSP (1, 3, and 6 mg). The results of these studies are reported here
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