Distribution of parent drug and metabolites in rat, dog, and human feces after iv and oral administration of [14C]ritonavir
| Species | Route | % of Total Dose Radioactivity | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Ritonavir | M-1 | M-2 | M-3 | M-5 | M-8 | M-10 | M-116-a | Other | ||
| Rat | iv | 21.2 | 9.7 | 21.3 | 2.9 | 5.6 | — | 7.5 | 15.6 | 9.0 |
| oral | 45.9 | 9.5 | 13.6 | 2.3 | 3.6 | — | 7.5 | 9.4 | 3.8 | |
| Dog | iv | 12.9 | 8.9 | 6.2 | 6.5 | 4.9 | 29.9 | 0 | 14.3 | 12.4 |
| oral | 61.9 | 7.4 | 7.1 | 2.1 | 0 | 8.3 | 0 | 3.9 | 4.6 | |
| Human | oral | |||||||||
| Subj. 1 | 31.4 | 2.8 | 24.0 | 1.7 | 5.3 | — | — | 9.0 | 11.8 | |
| Subj. 2 | 47.0 | 5.4 | 17.0 | 0 | 2.5 | — | — | 4.8 | 7.9 | |
| Subj. 3 | 17.4 | 2.3 | 32.1 | 2.0 | 4.9 | — | — | 12.8 | 11.2 | |
| Subj. 4 | 35.7 | 3.5 | 25.6 | 1.7 | 3.6 | — | — | 9.0 | 9.8 | |
| Subj. 5 | 37.3 | 3.5 | 21.5 | 3.2 | 3.4 | — | — | 11.4 | 9.4 | |
| Mean | 33.8 | 3.5 | 24.0 | 1.7 | 3.9 | — | — | 9.4 | 10.0 | |
| SD | 10.8 | 1.2 | 5.5 | 1.1 | 1.1 | — | — | 3.0 | 1.8 | |
Dose: Rat and Dog: 20 mg/kg oral, 5 mg/kg iv; Human: 600 mg oral (∼9 mg/kg); — = not detected; For each dosage route,N = 2 males and 2 females for both rat and dog.
↵6-a Animal bile results indicate that this HPLC peak may contain small amounts of M-12 and/orM-13.