Table 2.
Summary of pharmacokinetic parameters (mean±s.d.) following single (5 and 20 mg day−1) and multiple (10, 40, 80 and 120 mg day−1) doses of ziprasidone in healthy male subjects in the fed state.
| Ziprasidone | ||||
|---|---|---|---|---|
| 10 mg day−1 | 40 mg day−1 | 40–80 mg day−1 | 40–120 mg day−1 | |
| Day 1 | ||||
| Number of subjects | 6 | 8 | 8 | 7 |
| Dose (mg) | 5 | 20 | 20 | 20 |
| Cmax (ng ml−1) | 12.2 ± 4.1 | 26.6 ± 18.9 | 60.0 ± 33.8 | 34.3 ± 13.1 |
| tmax (h) | 5.0 ± 1.1 | 4.8 ± 1.3 | 3.8 ± 1.8 | 4.0 ± 1.7 |
| AUC(0,12 h) (ng ml−1 h) | 73.7 ± 18.7 | 175.7 ± 134.0 | 314.6 ± 166.8 | 215.0 ± 77.1 |
| AUC(0, ∞) (ng ml−1 h) | 86.7 ± 22.1 | 226.3 ± 174.8 | 376.7 ± 190.9 | 308.4 ± 125.9 |
| λz (h−1) | 0.220 ± 0.048 | 0.143 ± 0.049 | 0.172 ± 0.034 | 0.161 ± 0.040 |
| t½,z (h)a | 3.2 | 4.8 | 4.0 | 4.3 |
| Predicted accumulation ratio | 1.18 ± 0.08 | 1.29 ± 0.10 | – | – |
| Day 18 | ||||
| Number of subjects | 6 | 6 | 6 | 6 |
| Final dose (mg day−1) | 10 | 40 | 80 | 120 |
| Cmax (ng ml−1) | 14.8 ± 6.7 | 44.6 ± 48.1 | 118.6 ± 80.1 | 139.4 ± 81.2 |
| tmax (h) | 5.2 ± 1.3 | 3.8 ± 2.2 | 3.7 ± 0.8 | 4.7 ± 1.5 |
| AUC(0,12 h) (ng ml−1 h) | 109.8 ± 46.7 | 259.2 ± 213.3 | 658.0 ± 334.6 | 1027.9 ± 446.8 |
| λz (h−1) | 0.175 ± 0.054 | 0.145 ± 0.027 | 0.079 ± 0.040 | 0.069 ± 0.049 |
| t½,z (h)a | 4.0 | 4.8 | 8.8 | 10.0 |
| Accumulation ratio | 1.49 ± 0.39 | 1.48 ± 0.67 | – | – |
a
Calculated as ln 2/mean λz.