Table 1.
Pharmacokinetic parameters for ethinyl oestradiol, 17-desacetyl norgestimate, and norgestrel in Cycles A and B
| Hormone Parameter (units) | Summary statistic | Cycle A OCS alone n = 18 | Cycle B OCS + rosuvastatin n = 18 | Treatment effecta | 90% confidence interval of the treatment effect |
|---|---|---|---|---|---|
| Ethinyl oestradiol (EO) | gmean (CV%) | 1339 (35) | 1690 (31) | 1.26 | 1.19–1.34 |
| AUC(0–24) (pg·h/ml) | gmean (CV%) | 1339 (35) | 1690 (31) | 1.26 | 1.19–1.34 |
| Cmax (pg/ml) | gmean (CV%) | 159 (41) | 198 (36) | 1.25 | 1.17–1.33 |
| tmax (h) | Median (range) | 1.0 (1.0–4.0) | 1.0 (1.0–4.0) | NA | NA |
| t1/2 (h) | Mean (s.d.) | 13.8 (3.31)b | 16.6 (3.68)b | 2.37 | 0.89–3.85 |
| 17-desacetyl norgestimate(DesAc-NGM) | gmean (CV%) | 19.1 (16) | 22.0 (16) | 1.15 | 1.10–1.20 |
| AUC(0–24) (ng·h/ml) | gmean (CV%) | 19.1 (16) | 22.0 (16) | 1.15 | 1.10–1.20 |
| Cmax (ng/ml) | gmean (CV%) | 2.47 (33.9) | 2.53 (19.3) | 1.03 | 0.91–1.16 |
| tmax (h) | Median (range) | 1.0 (0.5–4.0) | 1.0 (1.0–3.0) | NA | NA |
| t1/2 (h) | Mean (s.d.) | 23.7 (4.22) | 24.0 (4.71)c | 0.71 | −0.50–1.91 |
| Norgestrel (NG) | gmean (CV%) | 62.0 (44) | 82.8 (48) | 1.34 | 1.25–1.43 |
| AUC(0–24) (ng·h/ml) | gmean (CV%) | 62.0 (44) | 82.8 (48) | 1.34 | 1.25–1.43 |
| Cmax (ng/ml) | gmean (CV%) | 3.46 (41.0) | 4.27 (44.8) | 1.23 | 1.14–1.33 |
| tmax (h) | Median (range) | 2.0 (0.5–8.0) | 3.0 (0.5–10.0) | NA | NA |
| t1/2 (h) | Mean (s.d.) | 31.2 (3.31)d | 29.5 (NC)d | 1.20 | NC |
Geometric mean of the ratio (OCS + rosuvastatin)/OCS for AUC(0–24) and Cmax; arithmetic mean of the difference (OCS + rosuvastatin)-OCS for t1/2
t1/2 data in both Cycles A and B were available for 16 volunteers
t1/2 data in Cycle B were available for 15 volunteers
t1/2 data in Cycle A were available for 3 volunteers; data in Cycle B were available for 1 volunteer (because half-life could not be characterized over 2 full half-lives with the sampling schedule used).
AUC(0–24), Area under the plasma concentration-time curve from time zero to 24 h; Cmax, Maximum observed plasma drug concentration; CV%, Coefficient of variation expressed as a percentage of the gmean (geometric mean); NA, Not applicable; NC, Not calculable; OCS, Oral contraceptive steroid; s.d, Standard deviation; t1/2, terminal elimination half-life; tmax, time of Cmax