PK parameters of TMCU as obtained after its i.v. (5 mg/kg), oral (20 mg/kg), and i.p. (20 mg/kg) administration to rats
Parameter | i.v. Bolus | Oral Administration | i.p. Administration |
|---|---|---|---|
| CL (l/h · kg) | 0.36 | ||
| CL/F (l/h · kg) | 0.43 | 0.40 | |
| CLr (ml/h) | 5.1 | 1.3 | 2.2 |
| CLm (l/h · kg) | 0.34 | ||
| CLint (l/h · kg) | 0.71 | ||
| Vz (l/kg) | 0.82 | ||
| Vz/F (l/kg) | 1.2 | 0.9 | |
| Vss (l/kg) | 0.87 | ||
| t1/2 (h) | 1.6 | 1.9 | 1.5 |
| AUC (mg/l/h) | 14.1 | 46.6 | 51.0 |
| AUMC (mg/l/h2) | 35 | 263 | 192 |
| MRT (h) | 2.5 | 5.6 | 3.8 |
| MAT (h) | 3.1 | 1.3 | |
| Cmax (mg/l) | 6.5 | 15.4 | |
| tmax (h) | 4 | 0.75 | |
| F (%) | 83 | 90 | |
| E (%) | 10.3 | ||
| fe (%) | 6.3 ± 0.8a | 1.2 ± 0.5 | 2.4 ± 0.7 |
| Am/D (Am/FD) | 29.4 ± 3.2 | 45.6 ± 2.2 | 42.1 ± 3.8 |
CL/F, oral clearance; CLr, renal clearance; CLm, metabolic clearance; CLint, intrinsic clearance; t1/2, half-life; tmax, time to reach Cmax; E, liver extraction ratio.
↵ a Mean ± SD