Species | Route | % of Total Dose Radioactivity | ||||||||
---|---|---|---|---|---|---|---|---|---|---|
Ritonavir | M-1 | M-2 | M-5 | M-9 | M-10 | M-117-a | G-1 | Other | ||
Rat | iv | — | 0.5 | 0.6 | — | 0.1 | — | — | — | 0.67-b |
oral | — | 0.6 | 0.5 | — | 0.2 | — | — | — | 0.77-b | |
Dog | iv | — | 0.5 | 2.9 | — | — | — | — | 0.5 | 0.4 |
oral | — | 1.0 | 2.2 | — | — | — | — | 0.4 | 0.4 | |
Human | oral | |||||||||
Subj. 1 | 1.6 | 0.4 | 5.8 | 0.1 | — | — | 0.2 | — | — | |
Subj. 2 | 5.6 | 0.6 | 3.5 | — | — | 0.2 | 0.2 | — | 0.1 | |
Subj. 3 | 2.2 | 0.5 | 6.8 | 0.2 | — | 0.1 | 0.3 | — | 0.2 | |
Subj. 4 | 4.8 | 0.8 | 7.0 | 0.1 | — | 0.2 | 0.4 | — | 0.5 | |
Subj. 5 | 2.9 | 1.0 | 9.0 | 0.1 | — | 0.1 | 0.4 | — | — | |
Mean | 3.5 | 0.6 | 6.4 | 0.1 | — | 0.1 | 0.3 | — | 0.2 | |
SD | 1.8 | 0.2 | 2.0 | 0.1 | — | 0.1 | 0.1 | — | 0.2 |
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.
↵7-a Animal bile results indicate that this HPLC peak may contain small amounts of M-12 and/orM-13.
↵7-b Consists largely of an artifactual peak eluting near the column void volume caused by concentration of large volumes of urine for radio-HPLC analysis.