TABLE 1

Pharmacokinetic parameters of sitagliptin in rats and dogs after intravenous administration

Male Sprague-Dawley rats and beagle dogs were dosed with a solution of the phosphate salt in saline. Mean ± standard deviation values are listed (n = 3 or 4). Dose is expressed in mg of free base/kg body weight.


Species

Dose

AUC0-∞

CLp

Vdss

t1/2
mg/kg μM · h ml/min/kg l/kg h
Rat 0.5 0.459 ± 0.100 46 ± 8.2 8.8 ± 3.4 1.7 ± 0.3
2 2.05 ± 0.051 40 ± 0.96 8.1 ± 2.0 1.9 ± 0.3
5 4.28 ± 0.318 48 ± 3.6 7.4 ± 1.2 1.8 ± 0.2
Dog 0.5 2.20 ± 0.36 9.3 ± 1.3 3.2 ± 0.1 4.0 ± 0.4

1.5
7.11 ± 1.35
8.8 ± 1.5
3.4 ± 0.5
4.2 ± 0.2