Tissue | Dose | Saxagliptin | M2 | ||||
---|---|---|---|---|---|---|---|
Average Conc. | Tissue/Plasma Ratio | Average Conc. | Tissue/Plasma Ratio | ||||
mg/kg | ng/g | ng/g | |||||
Plasma | 0.1 | 4 ± 2 | 1 | 1.3 ± 0.4 | 1 | ||
2.5 | 97 ± 23 | 1 | 48 ± 18 | 1 | |||
Small intestine | 0.1 | 159 ± 15 | 46 ± 18 | 28 ± 5 | 24 ± 10 | ||
2.5 | 942 ± 193 | 10 ± 1 | 2396 ± 348 | 55 ± 21 | |||
Large intestine | 0.1 | 71 ± 13 | 20 ± 5 | BLLQ | |||
2.5 | 2205 ± 411 | 24 ± 8 | 113 ± 20 | 3 ± 1 | |||
Duodenum | 0.1 | 50 ± 22 | 15 ± 9 | 15 ± 1 | 14 | ||
2.5 | 134 ± 10 | 1 ± 0.3 | 329 ± 106 | 7 ± 1 | |||
Kidney | 0.1 | 1243 ± 76 | 349 ± 102 | 68 ± 9 | 53 ± 9 | ||
2.5 | 1373 ± 282 | 14 ± 1 | 417 ± 110 | 9 ± 2 | |||
Spleen | 0.1 | 80 ± 23 | 21 ± 3 | 2 | 1 | ||
2.5 | 323 ± 50 | 4 ± 1 | 13 ± 9 | 0.3 ± 0.1 | |||
Heart | 0.1 | 39 ± 7 | 11 ± 3 | BLLQ | |||
2.5 | 224 ± 34 | 2 ± 0.3 | 27 ± 8 | 0.6 ± 0.1 | |||
Pancreas | 0.1 | 26 ± 5 | 7 ± 2 | 12 | 10 | ||
2.5 | 186 ± 20 | 2 ± 0.3 | 32 ± 5 | 0.7 ± 0.2 | |||
Brain | 0.1 | 1 | 0.1 | BLLQ | |||
2.5 | 8 ± 1 | 0.08 ± 0.01 | BLLQ | ||||
Muscle | 0.1 | 11 ± 0.5 | 3 ± 1 | BLLQ | |||
| 2.5 | 291 ± 21 | 3 ± 1 | 7 ± 4 | 0.1 ± 0.04 |
BLLQ, below lower limit of quantification.