Table 9.
The pharmacokinetic parameters of WXFL-152 in beagle plasma after single or multi-doses (n = 6, 3 male and 3 female, mean ± SD).
| Parameter | 2 mg/kg (single dose, i.v.) | 10 mg/kg (single dose, p.o.) | 30 mg/kg (single dose, p.o.) | 30 mg/kg/day (multi-doses, p.o., 7th day) | 100 mg/kg (single dose, p.o.) |
|---|---|---|---|---|---|
| Cmax (μmol/L) | 4.36 ± 0.96 | 6.28 ± 6.57 | 16.20 ± 16.50 | 6.97 ± 5.26 | 47.80 ± 20.80 |
| Tmax (h) | / | 1.25 ± 0.612 | 0.917 ± 0.585 | 1.08 ± 0.736 | 2.33 ± 0.816 |
| t1/2 (h) | 4.91 ± 2.18 | 5.77 ± 2.17 | 5.25 ± 1.03 | 12.30 ± 12.60 | 2.99 ± 0.70 |
| Vdss (L/kg) | 1.45 ± 0.33 | / | / | / | / |
| CL (mL/min/kg) | 14.5 ± 2.74 | / | / | / | / |
| AUC0–last (μmol/L·h) | 5.1 ± 0.9 | 19.6 ± 20.2 | 50.0 ± 58.8 | 23.7 ± 16.1 | 199.0 ± 90.5 |
| AUC0–inf (μmol/L·h) | 5.13 ± 0.9 | 20.2 ± 20.2 | 51.8 ± 62.3 | 37.9 ± 31.9 | 230.0 ± 51.5 |
| Bioavailability (%) | / | 76.9 | 65.4 | / | 78.0 |
Cmax, maximum plasma concentration; Tmax, time the maximum concentration occurred; Vdss, volume of distribution at steady state; CL, systemic clearance; AUC, area under the plasma concentration–time curve.