TABLE 2

Individual pharmacokinetic parameters of raltegravir and radioactivity after administration of a single oral dose of [14C]raltegravir to healthy volunteers


Subject

Raltegravir

Radioactivity

Raltegravir/Radioactivity
AUC0-t ha
Cmax
Tmax
AUC0-t h
Cmax
Tmax
AUC
Cmax
μM · h μM h μM Eq · h μM Eq h
1 9.45 3.39 1.0 11.41 3.96 1.0 0.83 0.86
2 4.04 1.92 1.0 7.33 2.80 1.0 0.55 0.69
3 15.69 4.86 1.0 19.33 5.70 1.0 0.81 0.85
4 7.95 4.11 1.0 12.10 5.58 1.0 0.66 0.74
5 9.05 5.51 0.5 13.01 6.60 0.5 0.70 0.83
6 16.76 5.53 1.0 23.34 6.99 1.0 0.72 0.79
7 14.21 7.46 0.5 19.14 8.26 0.5 0.74 0.90
8 13.09 6.77 1.0 22.45 9.54 1.0 0.58 0.71
Mean 11.28 4.94 0.9 16.01 6.18 0.9 0.70 0.80
S.D.
4.36
1.80
0.2
5.82
2.18
0.2
0.10
0.08
  • a t represents the last time point at which concentrations were above the limit of quantitation (20-24 h for raltegravir, 12-20 h for radioactivity).