Pharmacokinetic parameters of sitagliptin in rats and dogs after oral 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-∞ | Cmax | Tmax | F |
|---|---|---|---|---|---|
| mg/kg | μM · h | μM | h | % | |
| Rat | 2 | 1.20 ± 0.178 | 0.210 ± 0.132 | 0.5-4 | 59 |
| 20 | 15.2 ± 2.04 | 4.00 ± 0.384 | 0.5-1 | N.D. | |
| 60 | 60.9 ± 6.78 | 17.1 ± 6.57 | 0.5-1 | N.D. | |
| 180 | 217 ± 26.9 | 27.8 ± 6.73 | 0.5-2 | N.D. | |
| Dog | 0.4 | 1.62 ± 0.503 | 0.247 ± 0.080 | 1.0-2.0 | 89 ± 20 |
| 1.6 | 7.18 ± 1.56 | 1.32 ± 0.240 | 0.5-1.0 | 97 ± 29 | |
| 10 | 54.2 ± 13.4 | 10.3 ± 2.05 | 0.5-1.0 | N.D. | |
|
| 30 | 156 ± 29.2 | 26.5 ± 6.23 | 0.5-1.0 | N.D. |
N.D., not determined.