Pharmacokinetics of drospirenone and ethinylestradiol in Caucasian and Japanese women.
OBJECTIVE
To investigate the pharmacokinetics of drospirenone (DRSP) and ethinylestradiol (EE) in Caucasian and Japanese women.


METHODS
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.


CONCLUSIONS
Ethnic origin had no clinically relevant influence on the pharmacokinetics of DRSP and EE.
Bayer HealthCare Global R&D Centre, Beijing, China. hartmut.blode@bayer.com
Hartmut
H
Blode
Kristin
K
Kowal
Katrin
K
Roth
Stefanie
S
Reif
D000328:Adult; D000736:Androstenes / Q000008:administration & dosage / Q000493:pharmacokinetics*; D044466:Asian People; D004305:Dose-Response Relationship, Drug; D004997:Ethinyl Estradiol / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D012102:Reproductive Control Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D044465:White People
D000736:Androstenes; D012102:Reproductive Control Agents; C534342:drospirenone and ethinyl estradiol combination; D004997:Ethinyl Estradiol; C035144:drospirenone