Table 3.
Pharmacokinetics parameters after a repeat (7-day) rising dose in healthy volunteers.
| 50 mg every day
|
100 mg every day
|
200 mg every day
|
100 mg twice a day
|
||||||
|---|---|---|---|---|---|---|---|---|---|
| Dose | Day 1 | Day 7 | Day 1 | Day 7 | Day 1 | Day 7 | Day 1a | Day 7a | |
| Cmax | (ng/mL) | 56 ± 5 | 67 ± 5 | 124 ± 9 | 135 ± 10 | 322 ± 26 | 283 ± 16 | 116 ± 15 | 182b ± 17 |
| Cmin | (ng/mL) | 2.4 ± 0.2 | 3.5 ± 0.2 | 4.1 ± 0.3 | 5.5 ± 0.3 | 10.2 ± 1.3 | 12.0 ± 1.4 | 17.7 ± 1.6 | 30.9 ± 2.6 |
| tmax | (h) | 2.5 ± 0.5 | 2.1 ± 0.4 | 2.6 ± 0.4 | 2.8 ± 0.34 | 2.4 ± 0.4 | 2.6 ± 0.4 | 2.8 ± 0.4 | 3.1 ± 0.6 |
| AUC0-t | (ng • h/mL) | 369 ± 23 | 452 ± 20 | 771 ± 27 | 891 ± 32 | 1875 ± 102 | 1,907 ± 130 | 1,326 ± 148 | 1,084 ± 84 |
| Half-life | (h) | — | 7.31 ± 0.16 | — | 6.47 ± 0.22 | — | 6.54 ± 0.16 | — | — |
a
First daily dose.
b
Statistically significant difference (P < 0.05) from day 1 Cmax.