Table 2.
Main pharmacokinetic parameters (mean ± SEM) for CHF3567 in young healthy males (n = 12 per group) after different multiple oral doses of CHF3381 given twice daily
| 100 mg twice daily | 200 mg twice daily | 400 mg twice daily | ||||
|---|---|---|---|---|---|---|
| Pharmacokinetic parameter | Day 1 | Day 14 | Day 1 | Day 14 | Day 1 | Day 14* |
| Cmax (ng ml−1) | 384 ± 16 | 449 ± 17 | 719 ± 52 | 797 ± 51 | 1292 ± 02 | 1663 ± 188 |
| tmax (h)# | 4.0 (1.0–4.0) | 4.0 (3.0–4.0) | 4.0 (3.0–6.0) | 4.0 (3.0–4.0) | 4.0 (3.0–6.0) | 4.0 (3.0–6.0) |
| AUC(0,12 h) (ng ml−1 h) | 2515 ± 94 | 3272 ± 119 | 4807 ± 306 | 5959 ± 350 | 8869 ± 711 | 12 280 ± 1066 |
| AUC(0,∞) (ng ml−1 h) | 2971 ± 129 | 5773 ± 345 | 10 537 ± 815 | |||
| t1/2 (h) | 8.71 ± 0.74 | 7.4 ± 0.5 | 7.2 ± 0.4 | |||
| R | 1.31 ± 0.03 | 1.25 ± 0.04 | 1.38 ± 0.07 | |||
| AU (%) | 71.5 ± 3.3 | 58.5 ± 4.3 | 56.8 ± 4.6 | |||
| CLR (ml min−1) | 310.8 ± 16.7 | 288.4 ± 28.5 | 274.5 ± 28.4 | |||
R = accumulation ratio. AU = percent of dose recovered in urine in the 0–12 h period.
#
Median and range.
*
n = 11.