Pharmacokinetics of drospirenone and ethinylestradiol in Caucasian and Japanese women

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 C_max 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 AUC_0–24h 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.

Keywords:

• Drospirenone
• Ethinylestradiol
• Pharmacokinetics
• Ethnic origin

Acknowledgements

Funding for these studies was provided by Bayer HealthCare Pharmaceuticals, Berlin, Germany. Medical writing assistance for the development of this manuscript was provided by Danielle Turner and Amy Evans of inScience Communications with the financial support of Bayer HealthCare Pharmaceuticals. The authors would also like to thank Timo Piironen, Vesa Rämö and Terttu Kleimola for bioanalytical support and Susanne Reschke for her support regarding the pharmacokinetic data analyses.

Declaration of interest: Hartmut Blode, Kristin Kowal, Katrin Roth and Stefanie Reif are employees of Bayer HealthCare Pharmaceuticals, the sponsor of this study.