Table 7

Distribution of parent drug and metabolites in rat, dog, and human urine after iv and oral administration of [14C]ritonavir

SpeciesRoute% of Total Dose Radioactivity
RitonavirM-1M-2M-5M-9M-10M-117-aG-1Other
Rativ0.50.60.10.67-b
oral0.60.50.20.77-b
Dogiv0.52.90.50.4
oral1.02.20.40.4
Humanoral
 Subj. 11.60.45.80.10.2
 Subj. 25.60.63.50.20.20.1
 Subj. 32.20.56.80.20.10.30.2
 Subj. 44.80.87.00.10.20.40.5
 Subj. 52.91.09.00.10.10.4
Mean3.50.66.40.10.10.30.2
SD1.80.22.00.10.10.10.2
  • 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.