Percentage of circulating metabolites of zoniporide and their estimated exposure in healthy male volunteers, Sprague-Dawley rats, and Beagle dogs after intravenous administration of [14C]zoniporide
Healthy male volunteers were administered [14C]zoniporide by intravenous infusion for 1 h at a dose of 80 mg (100 μCi). The rats were administered a bolus of [14C]zoniporide at a dose of 10 mg/kg (50 μCi). The dogs were administered a bolus of [14C]zoniporide at a dose of 3 mg/kg (150 μCi). The estimated exposures were determined by multiplying percent circulating radioactivitymetabolite and AUC(0–tlast)radioactivity. The AUC(0–tlast)radioactivity is depicted in Table 2.
Metabolites | Human | Rat | Dog | |||
---|---|---|---|---|---|---|
Circulating Radioactivity | Estimated AUC(0–tlast) | Circulating Radioactivity | Estimated AUC(0–tlast) | Circulating Radioactivity | Estimated AUC(0–tlast) | |
% | ng-Eq-h/ml | % | ng-Eq-h/ml | % | ng-Eq-h/ml | |
M1 | 60 | 1755 | 46 | 1642 | ||
M3 | 6.4 | 187 | 9.0 | 321 | 3.7 | 117 |
M4 | 2.3 | 73 | ||||
M6 | ||||||
M8 | 8.5 | 303 | 5.4 | 171 | ||
M9 | 23 | 727 | ||||
M10 | 3.1 | 98 | ||||
Zoniporide | 30 | 878 | 36 | 1285 | 62 | 1959 |