Table 3.
Mouse Pharmacokinetic Parameters. Mouse PK parameters correspond to a 100 mg/kg oral gavage dose in n = 3 mice. Doses were formulated in 100 mM acetate buffer (pH 4.5) for OXA, and 100 mM citrate buffer (pH 3.5) or 10% w:v Captisol for CIDD-72229.
| T1/2 |
Cmax |
Tmax |
AUC(0-∞) |
Cl/F |
F |
Cl |
|
|---|---|---|---|---|---|---|---|
| (min) | (μM) | (min) | (μM*h) | (ml/min/kg) | % | (ml/min/kg) | |
| OXA 3 mg/kg IV | 51 ± 6 | 2.2 ± 0.1 | 5 | 1.1 ± 0.0 | 157 ± 3 | ||
| OXA 100 mg/kg PO | 58 ± 6 | 11.8 ± 1.6 | 50 ± 10 | 26.1 ± 1.7 | 230 ± 14 | 69.5 ± 5.3 | 159 ± 3 |
| 72229 100 mg/kg (Citr) PO | 169 ± 14 | 2.1 ± 0.8 | 5 | 3.5 ± 0.9 | 1280 ± 268 | 1.6 ± 0.5 | 20.2 ± 2.5 |
| 72229 100 mg/kg (Capt) PO | 191 ± 37 | 9.0 ± 2.8 | 8.3 ± 3.3 | 18.9 ± 1.9 | 220 ± 22 | 9.6 ± 2.1 | 18.1 ± 0.6 |
Values are presented as “mean ± SEM”.
Abbreviations: T1/2, elimination half-life; Cmax, maximum plasma concentration; Tmax, time to maximum plasma concentration; AUC(0-ꝏ), area under the curve from time 0 extrapolated to infinity, Cl/F, apparent oral clearance; F oral bioavailability, Cl, clearance.
Citr, formulated in 100 mM citrate buffer, pH 3.5; Capt, formulated in 10% w:v Captisol.