Excretion of total radioactivity after single oral or i.v. administration of 14C-irbesartan to rats and macaques expressed as a percentage of dose ± S.D.
| Animal | Dose | Route | Sex | Urine | Bile | Feces | Number of Animals | |||
|---|---|---|---|---|---|---|---|---|---|---|
| 0–24 h | 0–168 h | 0–24 h | 0–48 h | 0–24 h | 0–168 h | |||||
| mg/kg | ||||||||||
| Rat | 10 | p.o. | M | 7.3 ± 1.4 | 7.9 ± 13 | 70.2 ± 8.6 | 81.7 ± 1.1 | n = 4 | ||
| F | 5.1 ± 0.7 | 6.1 ± 0.8 | 56.9 ± 12.0 | 85.1 ± 2.0 | n = 4 | |||||
| 10 | p.o. | M | 73.8 ± 2.8 | 77.7 ± 2.1 | n = 4 | |||||
| F | 65.0 ± 6.7 | 71.6 ± 6.3 | n = 4 | |||||||
| 30 | p.o. | M | 3.4 ± 1.0 | 3.5 ± 1.0 | 93.2 ± 5.5 | 99.0 ± 3.9 | n = 3 | |||
| F | 4.2 ± 0.7 | 4.6 ± 0.8 | 85.3 ± 5.5 | n = 3 | ||||||
| 1 | i.v. | M | 4.8 ± 1.8 | 5.4 ± 1.8 | 74.0 ± 5.4 | 86.9 ± 4.8 | n = 4 | |||
| F | 7.4 ± 0.9 | 10.7 ± 1.3 | 53.1 ± 6.2 | 85.4 ± 5.8 | n = 4 | |||||
| 1 | i.v. | M | 51.6 ± 5.7 | 64.6 ± 5.5 | ||||||
| F | 35.9 ± 12.1 | 45.1 ± 11.3 | ||||||||
| Macaque | 10 | p.o. | M | 7.1 ± 1.4 | 10.1 ± 3.3 | 11.5 ± 9.3 | 81.5 ± 8.4 | n = 3 | ||
| 10 | p.o. | M | 12.1 ± 14.2 | 44.3 ± 20.0 | 48.1 ± 18.9 | n = 3 | ||||
| 1 | i.v. | M | 21.5 ± 20.7 | 57.5 ± 49.5 | 58.2 ± 49.3 | n = 3 | ||||
| 1 | i.v. | M | 8.9 ± 1.4 | 11.5 ± 2.3 | 0.1 ± 0.2 | 82.6 ± 8.2 | n = 3 | |||
Urine, bile, and feces were collected in portion of 0- to 6-, 6- to 24-, and subsequently in 24-h intervals up to 48 or 168-h after dosing. Bile was collected from conscious bile duct-cannulated animals. Radiolabeled contents were determined by direct liquid scintillation counting (urine and bile) or after combustion (feces).