TABLE 1

Pharmacokinetic parameters for aliskiren in plasma and total radioactivity concentrations in blood and plasma

Values are shown as mean ± S.D. (n = 4) with the exception of tmax values, which are presented as the median (range).

Parameter
Plasma Aliskiren
Blood Total Radioactivity
Plasma Total Radioactivity
tmax (h) 3 (2-5) 2.5 (2-5) 3 (2-5)
Cmax (ng/ml)a 254 ± 163 171 ± 88 305 ± 193
tλ1 (h) 2.1 ± 0.8 1.9 ± 0.3b 1.8 ± 0.4
AUC0—t (ng · h/ml)c,d 1051 ± 547 427 ± 226 1310 ± 614
t λz (h) 48.7 ± 6.9 N.A. 44.3 ± 9.4
AUC0-∞ (ng · h/ml)c,d 1108 ± 546 591 ± 93b 1374 ± 638
% of 14C-AUC0-∞ plasma 81 ± 2 61 ± 12b (100)
CL/F (l/h)
380 ± 310
520 ± 860b
290 ± 210

  • N.A., not applicable.

  • ↵ a ng-Eq/ml for radioactivity.

  • ↵ b n = 3.

  • ↵ c ng-Eq · h/ml for radioactivity.

  • ↵ d AUC0-t was calculated using the linear trapezoidal rule. t (= tlast) was 96 to 168 h for plasma aliskiren, 4 to 12 h for blood radioactivity, and 144 h for plasma total radioactivity. AUC0-∞ was calculated as AUC0-t + AUCt-∞, where AUCt-∞ = Ct × t/ln(2).