TABLE 2

Mean pharmacokinetic parameters of total circulating radioactivity and zoniporide 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 Sprague-Dawley rats and Beagle dogs were administered a bolus of [¹⁴C]zoniporide at a dose of 10 mg/kg (50 μCi) and 3 mg/kg (150 μCi), respectively.

Pharmacokinetic Parameters	Healthy Male Volunteers				Sprague-Dawley Rats				Beagle Dogs
	Radioactivity*		Zoniporide		Radioactivity*		Zoniporide		Radioactivity*		Zoniporide
	Mean	S.D.	Mean	S.D.	Mean	S.D.	Mean	S.D.	Mean	S.D.	Mean	S.D.
T_max (h)	1.0	0.0	1.0	0.0
C_max (ng/ml)	899	237	590	44.2
AUC_0–tlast (ng-h/ml)	2925	223	833	33.4	3570	323	1390	287	3160	672	2009	582
AUC_0–∞ (ng-h/ml)	3250	122	839	34.2	3650	307	1490	273	3330	673	2370	683
t_1/2 (h)	6.7	3.3	2.0	0.4	2.00	0.83	0.4	0.10	2.80	0.34	2.51	0.59
Cl (ml/min/kg)			21.0	1.2			113	22			21	4.7
V_ss (l/kg)			1.7	0.4			2.2	0.58			3.7	0.59

↵* The radioactivity was expressed as ng-Eq/ml.