TABLE 1

Pharmacokinetic parameters of linagliptin in plasma, CD1790 in plasma, and total radioactivity in plasma and whole blood after intravenous infusion of 5 mg of [14C]linagliptin and oral administration of 10 mg of [14C]linagliptin

Results are presented as geometric means (gMeans).

ParameterRoute of AdministrationLinagliptinCD1790 (Plasma)Total RadioactivityTotal Radioactivity (Whole Blood)
gMeanCVgMeanCVgMeanCVgMeanCV
%%%%
AUC0–24 (nmol · h/l)ai.v.35613.634.129.65526.713755.64
AUC0–264 (nmol · h/l)a94717.9—*—*14306.66—*—*
Cmax (nmol/l)b82.718.85.3042.7112.014.084.311.8
Tmaxc (h)1.251.0–1.52.141.75–3.01.501.0–1.51.501.0–1.5
CL (ml/min)15017.290.17.0134110.0
t½ (h)14219.115.961.519314.815.815.0
AUC0–24 (nmol · h/l)aOral19132.634.263.634238.821626.3
AUC0–120 (nmol · h/l)a51019.2—*—*82227.1—*—*
Cmax (nmol/l)b16.373.84.283.531.064.423.648.9
Tmaxc (h)2.750.5–4.02.261.0–4.01.751.0–4.01.500.5–4.0
CL/F (ml/min)37418.624326.0120043.1
t (h)15516.210.847.313727.39.7798.4
  • CL, total clearance; CL/F, total clearance divided by bioavailability.

  • * Not calculated as no data beyond 24 h.

  • Not calculated.

  • a Unit for total radioactivity = (nmol · eq · h/l).

  • b Unit for total radioactivity = (nmol · eq/l).

  • c Median and range.