Concentrations of saxagliptin and M2 in tissues at 1 h after 0.1 or 2.5 mg/kg i.a. doses of saxagliptin to ZDF rats (n = 3)
S.D. is not given when at least one of the rats was found to have a concentration less than BLLQ in any given tissue. Lower limit of quantification: spleen, 1.8 ng/g; heart, 2.5 ng/g; pancreas, 22.3 ng/g; muscle, 0.8 ng/g; and brain, 0.77 ng/g.
Tissue | Dose | Saxagliptin | M2 | ||||
|---|---|---|---|---|---|---|---|
| Average Conc. | Tissue/Plasma Ratio | Average Conc. | Tissue/Plasma Ratio | ||||
| mg/kg | ng/g | ng/g | |||||
| Plasma | 0.1 | 14 ± 11 | 1 | 0.7 ± 0.03 | 1 | ||
| 2.5 | 148 ± 70 | 1 | 34 ± 7 | 1 | |||
| Small intestine | 0.1 | 164 ± 21 | 17 ± 9 | 29 ± 10 | 39 ± 15 | ||
| 2.5 | 759 ± 392 | 6 ± 4 | 943 ± 475 | 28 ± 15 | |||
| Large intestine | 0.1 | 81 ± 43 | 10 ± 8 | 18 ± 8 | 24 ± 11 | ||
| 2.5 | 1547 ± 524 | 13 ± 8 | 140 ± 63 | 4 ± 3 | |||
| Duodenum | 0.1 | 60 ± 13 | 6 ± 4 | 19 ± 8 | 24 ± 9 | ||
| 2.5 | 179 ± 74 | 1 ± 0.2 | 254 ± 119 | 7 ± 2 | |||
| Kidney | 0.1 | 923 ± 316 | 87 ± 34 | 20 ± 0.2 | 27 ± 1 | ||
| 2.5 | 2662 ± 340 | 21 ± 11 | 271 ± 41 | 8 ± 2 | |||
| Spleen | 0.1 | 139 ± 43 | 16 ± 12 | BLLQ | |||
| 2.5 | 1300 ± 656 | 9 ± 1 | 22 ± 9 | 0.7 ± 0.3 | |||
| Heart | 0.1 | 26 ± 9 | 8 ± 5 | BLLQ | |||
| 2.5 | 236 ± 108 | 3 ± 1 | 17 ± 5 | 0.5 ± 0.1 | |||
| Pancreas | 0.1 | 115 ± 70 | 36 ± 30 | BLLQ | |||
| 2.5 | 940 ± 671 | 10 ± 8 | BLLQ | ||||
| Brain | 0.1 | BLLQ | 9 | ||||
| 2.5 | 10 ± 1 | 0.07 ± 0.02 | 0.8 | 0.02 | |||
| Muscle | 0.1 | 23 ± 2 | 2 ± 1 | BLLQ | |||
|
| 2.5 | 500 ± 170 | 4 ± 0.5 | 5.6 ± 2 | 0.2 ± 0.04 | ||
BBLQ, below lower limit of quantification.