Table 7.
Pharmacokinetic parameters (mean ± SD) of compounds 31 and 44 after intravenous (n = 3) and oral (n = 3) administration (10 mg/kg) to SD male rats.a
| 31 |
44 |
|||
|---|---|---|---|---|
| Intravenous | Oral | Intravenous | Oral | |
| AUC0–∞ (mg min/mL) |
330.66 ± 93.61 | 26.59 ± 22.32 | 1070.23 ± 114.39 | 614.11 ± 120.15 |
| AUClast (mg min/mL) |
273.60 ± 64.45 | 11.67 ± 5.99 | 1058.16 ± 109.82 | 487.49 ± 87.29 |
| Terminal half-life (min) | 173.83 ± 32.38 | 448.10 ± 27.60 | 80.17 ± 9.34 | 199.34 ± 134.70 |
| Cmax (mg/mL) | – | 0.04 ± 0.02 | – | 2.11 ± 0.91 |
| Tmax (min) | – | 48 (30 ∼ 60) |
– | 72 (60 ∼ 120) |
| CL (mL/mim/kg) | 32.53 ± 10.08 | – | 9.43 ± 1.05 | – |
| Vss (mL/kg) | 7736.8 ± 1114.3 | – | 785.49 ± 39.64 | – |
| F (%) | 8.0 | 78.4 | ||
aAUC0–∞, total area under the plasma concentration–time curve from time zero to time infinity; AUClast, total area under the plasma concentration–time curve from time zero to last measured time; Cmax, peak plasma concentration; Tmax, time to reach Cmax; CL, time-averaged total body clearance; Vss, apparent volume of distribution at steady state; F, bioavailability.