Table 8

Pharmacokinetic parameters of total radioactivity, ritonavir and metabolites in rat, dog, and human plasma after iv and oral administration of [14C]ritonavir

ParameterRatDogHuman
OralIV
MaleFemaleMaleFemaleOralIVOral
Total 14C
 Cmax(μg eq/ml)1.433.703.865.0218.8220.4314.0
 Tmax (hr)680.10.110.14.4
 AUC (μg eq · hr/ml)12.6830.736.599.47151.648.13135.0
[14C]Ritonavir
 Cmax (μg eq/ml)1.433.703.845.0217.9120.0213.70
 Tmax (hr)680.10.110.14.4
 AUC (μg eq · hr/ml)12.6830.733.855.1071.0922.8395.64
M-1
 Cmax (μg eq/ml)0.080.0370.701.17
 Tmax(hr)21.513
 AUC (μg eq · hr/ml)0.060.033.342.64
M-2
 Cmax (μg eq/ml)0.280.220.67
 Tmax(hr)31.58.8
 AUC (μg eq · hr/ml)0.970.323.19
G-1
 Cmax (μg eq/ml)0.130.26
 Tmax(hr)1–20.5
 AUC (μg eq · hr/ml)0.330.34
  • All total radioactivity values were determined over a 0–72 hr (rat and dog) or 0–24 hr (human) plasma time course. All values of [14C]ritonavir and metabolites were determined over a 0–2 (rat) or 0–3 (dog) hr plasma time course after intravenous dosing and a 0–8 (rat), 0–6 (dog) and 2–12 (human) hr plasma time course after oral dosing.

  • — = metabolite not detected.