Pharmacokinetic parameters in plasma (VF) and bile following i.v. administration of 15 mg of ximelagatran (TIII; n = 4 pigs) or 15 mg of melagatran (TIV; n = 4 pigs) The values are presented as mean and S.D.
Ximelagatran | OH-melagatran | Ethylmelagatran | Melagatran | |
|---|---|---|---|---|
| AUC0–6 h (h · μM) | ||||
| TIII | 0.58 ± 0.07 | 0.03 ± 0.01 | 0.42 ± 0.34 | 0.73 ± 0.26 |
| TIV | N.A. | N.A. | N.A. | 3.71 ± 0.70 |
| AUC0-∞ (h · μM) | ||||
| TIII | 0.58 ± 0.07 | 0.04 ± 0.01 | 0.47 ± 0.37 | 1.03 ± 0.56 |
| TIV | N.A. | N.A. | N.A. | 3.86 ± 0.80 |
| t1/2 (h) | ||||
| TIII | 0.2 ± 0.02 | 0.7 ± 0.3 | 2.0 ± 0.5 | 3.0 ± 1.7 |
| TIV | N.A. | N.A. | N.A. | 1.5 ± 0.3 |
| fe, bile (% of dose) | ||||
| TIII | 0.05 ± 0.02 | 0.15 ± 0.20 | 10 ± 6.4 | 6.4 ± 3.8 |
| TIV | N.A. | N.A. | N.A. | 15 ± 7.9 |
| CLbile (ml/min/kg) | ||||
| TIII | 0.02 ± 0.01 | 0.50 ± 0.50 | 8.75 ± 7.61 | 1.83 ± 1.16 |
| TIV | N.A. | N.A. | N.A. | 1.15 ± 0.81 |
| CL (ml/min/kg) | ||||
| TIII | 34 ± 2.1 | N.A. | N.A. | N.A. |
| TIV | N.A. | N.A. | N.A. | 6.4 ± 2.0 |
| Vss (l/kg) | ||||
| TIII | 0.31 ± 0.05 | N.A. | N.A. | N.A. |
| TIV | N.A. | N.A. | N.A. | 0.51 ± 0.08 |
N.A., not applicable