Table 6.
In Vivo PK Profiles of Compounds 15b or 24f Following 20 mg/kg Oral and 10 mg/kg Intravenous Dosing in Ratsa
route | AUC0−∞ (ng h/mL) | t1/2 (h) | Tmax (h) | Cmax (ng/mL) | CL (L/h/kg) | Vss (L/kg) | F (%) |
---|---|---|---|---|---|---|---|
15b PO | 3535 ± 1411 | 1.1 ± 0.02 | 0.5 | 2212 ± 587 | 6.2 ± 2.1 | 9.6 ± 3.2 | 37.6 ± 15 |
15b IV | 4679 ± 1280 | 0.6 ± 0.2 | 6456 ± 988 | 2.3 ± 0.7 | 1.8 ± 0.1 | ||
24f PO | 662 ± 191 | 3.3 ± 1.5 | 1.0 | 192 ± 109 | nd | nd | 7.0 ± 2.0 |
24f IV | 4746 ± 268 | 0.7 ± 0.3 | 13733 ± 1358 | 35.2 ± 2.0 | 0.55 ± 0.08 |
Values are mean ± SD from n = 3 biological replicates.
Cmax, maximum concentration of drug in plasma; Tmax, time to maximum concentration of drug in plasma; AUC, area under the curve (t = 0 to 24 h); Vss, volume of distribution at steady state; CL, plasma clearance; t1/2, terminal half-life; F, absolute oral bioavailability; nd, not determined. Formulation for PO and IV: DMSO:20% HP-β-CD in saline = 1:9.