Pharmacokinetic parameters after i.v. infusion of temocaprilat
| Parameter | Unit of Measure | Mouse | Rat | Guinea Pig | Rabbit | Dog |
|---|---|---|---|---|---|---|
| Body weight | kg | 0.044 ± 0.002 | 0.26 ± 0.01 | 0.35 ± 0.01 | 3.47 ± 0.03 | 13.0 ± 0.0 |
| Bile flow | μl/min/kg | 32.3 ± 5.6 | 35.4 ± 2.9 | 158.1 ± 11.4 | 48.5 ± 0.9 | 3.4 ± 0.5 |
| Infusion rate | nmol/min/kg | 0.97 | 0.60 | 0.74 | 0.62 | 0.41 |
| fu,plasma | 0.15 ± 0.01 | 0.06 ± 0.01 | 0.03 ± 0.01 | 0.14 ± 0.01 | 0.10 ± 0.01 | |
| fu,liver | 0.17 ± 0.01 | 0.05 ± 0.01 | 0.19 ± 0.01 | 0.25 ± 0.01 | 0.28 ± 0.02 | |
| Cplasma | nM | 149 ± 18 | 46 ± 6 | 193 ± 25 | 80 ± 5 | 100 ± 2 |
| Cliver | pmol/g | 562 ± 129 | 267 ± 34 | 121 ± 7 | 73 ± 2 | 456 ± 90 |
| Cu,liver | pmol/g | 94 ± 19 | 12 ± 1 | 23 ± 1 | 18 ± 1 | 129 ± 27 |
| CLtot | ml/min/kg | 7.5 ± 0.6 | 12.5 ± 1.6 | 3.9 ± 0.5 | 7.9 ± 0.5 | 4.0 ± 0.1 |
| CLbile(plasma) | ml/min/kg | 5.9 ± 0.8 | 9.7 ± 1.2 | 1.1 ± 0.2 | 0.24 ± 0.02 | 1.0 ± 0.2 |
| CLbile(liver) | ml/min/kg | 1.6 ± 0.3 | 1.8 ± 0.2 | 1.7 ± 0.1 | 0.27 ± 0.02 | 0.22 ± 0.02 |
| CLbile(u,liver) | ml/min/kg | 9.8 ± 1.9 | 39.2 ± 3.3 | 9.2 ± 0.3 | 1.1 ± 0.1 | 0.80 ± 0.13 |
Temocaprilat was i.v. infused to experimental animals. The plasma concentration and the biliary excretion rate were determined under the steady-state condition. At the end of the experiments, the liver was removed to determine the concentration of temocaprilat. Results are mean ± S.E. of three independent experiments.