TABLE 2

Mean pharmacokinetics of 1 and total radioactivity in humans after a single 200-mg p.o. dose of [14C]1

1 Total Radioactivity
Tmax (h) 1.4 ± 0.7 3.2 ± 1.3
C max a 355 ± 173 615 ± 152
t1/2 (h) 9.2 ± 2.1 7.9 ± 1.5
AUC0-tlastb,c 2178 ± 605 5980 ± 1520
AUC0-∞b 2200 ± 607 7428 ± 1275
CLp/F (ml/min/kg) 23.2 ± 6.0 N.A.
CLRd (ml/min/kg) 2.33 ± 0.85 N.A.
(CLR/fu)/GFRe 5.8 ± 2.1 N.A.

  • N.A., not applicable.

  • ↵ a Units are ng/ml and ng-Eq/ml for 1 and total radioactivity, respectively.

  • ↵ b Units are ng · h/ml and ng-Eq · h/ml for 1 and total radioactivity, respectively.

  • ↵ c tlast was 48 h for 1 and 24 h for total radioactivity.

  • ↵ d Calculated by Ae0-48/AUC0-48 and subject weight-normalized.

  • ↵ e Plasma-free fraction (fu) was 0.23; GFR was assumed to be 120 ml/min (Davies and Morris, 1993) and subject weight-normalized.