Table 4.
Summary of key pharmacokinetic parameters
| Parameter | Single dose | Multiple dose | ||
|---|---|---|---|---|
| 175 mg (n = 5) | 200 mg (n = 7) | 175 mg (n = 5) | 200 mg (n = 5) | |
| Geometric mean Cmax, nmol/L (%CV) | 503 (29.3) | 556 (37.8) | 821 (10.2) | 1134 (50.1) |
| Geometric mean AUC12, nmol/L·h (%CV) | 3394 (32.1) | 3878 (32.0) | 7010 (15.0) | 8100 (37.8)b |
| Geometric mean C8, nmol/L (%CV) | 213 (26.9) | 300 (41.0) | 534 (23.7) | 750 (59.0) |
| Median tmax, h (min, max) | 2.0 (1.9, 4.0) | 3.0 (1.9, 4.2) | 2.0 (2.0, 6.0) | 200 (1.0, 5.9) |
| Mean t½λz, h (SD) | 4.8 (0.4) | 7.3 (2.3)a | 7.3 (1.9)b | 7.4 (0.3)c |
| Geometric mean Ctrough, nmol/L (%CV) | NA | NA | 353 (23.9) | 570 (58.1) |
AUC12, area under the plasma concentration–time curve from time zero to 12 h, C8 plasma drug concentration at 8 h, Cmax maximum plasma drug concentration, Ctrough lowest plasma drug concentration, CV geometric coefficient of variation, max maximum, min minimum, NA not available, SD standard deviation, t½λz apparent terminal elimination, tmax time to reach maximum plasma concentration
an = 6
bn = 4
cn = 3