Table 2.
Pharmacokinetic parameters of drospirenone (DRSP) after different single doses of DRSP (1, 3 and 6 mg) (Studies 1 and 2) and after single administration (Studies 1–3) and repeated 21-day administration (Study 3) of ethinylestradiol (EE) 0.02 mg/DRSP 3 mg in healthy Caucasian and Japanese women. Results are presented as the geometric mean (geometric coefficient of variation), with the exception of tmax which is given as the median (range).
| 1 mg DRSP | 3 mg DRSP | 6 mg DRSP | EE 0.02 mg/DRSP 3 mg (single dose) | EE 0.02 mg/DRSP 3 mg (day 21) | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Parameter | Study 1 Caucasian (n − 6) | Study 2 Japanese (n − 6) | Study 1 Caucasian (n − 6) | Study 2 Japanese (n − 6) | Study 1 Caucasian (n − 6) | Study 2 Japanese (n − 6) | Study 1 Caucasian (n − 18) | Study 2 Japanese (n − 18) | Study 3 Caucasian (n − 23) | Study 3 Japanese (n − 24) | Study 3 Caucasian (n − 23) | Study 3 Japanese (n − 24) |
| Cmax (ng/mL) | 9.85 (19%) | 13.0 (29%) | 33.9 (20%) | 44.4 (21%) | 62.5 (20%) | 92.6 (13%) | 30.9 (27%) | 35.7 (31%) | 38.4 (26%) | 38.9 (32%) | 70.3 (15%) | 78.9 (23%) |
| tmax (h) | 1.25 (1.0−2.0) | 1.25 (1.0−1.5) | 1.5 (1.0−2.0) | 1.0 (1.0−1.5) | 1.75 (1.5−2.0) | 1.5 (1.0−2.0) | 1.5 (1.0−4.0) | 1.5 (0.5−4.0) | 1.5 (1.0−2.0) | 1.5 (1.0−2.0) | 1.5 (1.0−2.0) | 1.5 (1.0−2.0) |
| t½ (h) | 25.5 (20%) | 30.1 (34%) | 28.5 (16%) | 24.2 (24%) | 26.3 (16%) | 28.5 (21%) | 27.7 (18%) | 26.6 (19%) | ND | ND | 30.8 (22%) | 29.1 (18%) |
| AUC(ng·h/mL) | 140 (9%) | 182 (28%) | 506 (22%) | 458 (18%) | 1007 (21%) | 1051 (15%) | 458 (18%) | 494 (17%) | ND | ND | 1811 (33%) | 1852 (32%) |
| CL/F (mL/min) | 119 (9%) | 91.3 (28%) | 98.7 (22%) | 109 (18%) | 99.3 (21%) | 95.2 (15%) | 109 (18%) | 101 (17%) | ND | ND | ND | ND |
| AUC(0−24h) (ng·h/mL) | ND | ND | ND | ND | ND | ND | ND | ND | 268 (19%) | 271 (22%) | 763 (17%) | 803 (24%) |
AUC, area under the curve extrapolated to infinity; AUC(0–24h), area under the curve up to 24 h after dosing; CL/F, total oral clearance; Cmax, maximum serum concentration; ND, not determined; t½, terminal half-life; tmax, time to Cmax