Table 3.
Pharmacokinetic parameters of 20n after intravenous and oral administration (10 mg/kg) to SD male rats.
| Parameters | Intravenous | Oral |
|---|---|---|
| AUC0–∞ (μg min/mL) | 339.17 ± 34.01 | 61.89 ± 27.81 |
| AUClast (μg min/mL) | 273.03 ± 31.96 | 49.52 ± 20.31 |
| Terminal half-life (min) | 204.19 ± 26.24 | 193.03 ± 45.4 |
| Cmax (μg/mL) | – | 0.20 ± 0.09 |
| Tmax (min) | – | 68 (30 ∼ 120)a |
| CL (mL/min/kg) | 29.71 ± 2.97 | – |
| MRT (min) | 130.34 ± 8.92 | – |
| Vss (mL/kg) | 7665.84 ± 1424.27 | – |
| Plasma concentration (μg/mL) at 2 h | 0.45 ± 0.03 | 0.16 ± 0.05 |
| Brain concentration (μg/mL) at 2 h | 3.9575 ± 0.2125 | 0.0211 ± 0.0062 |
| Brain-to-plasma ratio (B/P) at 2 h | 8.78 | 0.15 |
| F (%) | 18.2 |
Values are presented as mean ± SD. AUC: area under the plasma concentration versus time curve); Cmax: peak plasma concentration; Tmax: time to reach Cmax; CL: time-averaged body clearance; MRT: mean residence time; Vss: apparent volume of distribution at steady state; F: oral bioavailability.
aMedian (range) for Tmax.