Table 3.
Relative BA of the DE tablet alone and under rabeprazole pretreatment: pharmacokinetic parameters of a single 110-mg DE tablet for total and unconjugated dabigatran
| DE under pretreatment | DE alone | |||
|---|---|---|---|---|
| gMean | gCV (%) | gMean | gCV | |
| Total dabigatran | ||||
| AUC0–tz (ng h/mL) | 192 (n = 35) | 109 | 667 (n = 36) | 123 |
| AUC0–∞ (ng h/mL) | 214 (n = 35) | 96.6 | 702 (n = 36) | 110 |
| Cmax (ng/mL) | 21.8 (n = 35) | 105 | 83.1 (n = 36) | 118 |
| tmax1 (h) | 2.00 (n = 35) | 1.00–4.00 | 2.00 (n = 36) | 1.00–3.00 |
| t½ (h) | 8.18 (n = 35) | 28.2 | 8.59 (n = 36) | 16.0 |
| Unconjugated dabigatran | ||||
| AUC0–tz (ng h/mL) | 164 (n = 35) | 110 | 588 (n = 36) | 119 |
| AUC0–∞ (ng h/mL) | 188 (n = 35) | 93.4 | 618 (n = 36) | 107 |
| Cmax (ng/mL) | 20.0 (n = 35) | 103 | 72.9 (n = 36) | 114 |
| tmax1 (h) | 2.00 (n = 35) | 1.00–4.00 | 2.00 (n = 36) | 1.00–4.00 |
| t½ (h) | 7.92 (n = 35) | 27.3 | 8.31 (n = 36) | 15.5 |
AUC0–tz area under the concentration–time curve from baseline to last quantifiable data point, AUC0–∞ area under the concentration–time curve from baseline extrapolated to infinity, BA bioavailability, Cmax maximum plasma concentration of dabigatran, DE dabigatran etexilate, gCV geometric coefficient of variation, gMean geometric mean, n number of subjects, tmax time from dosing to the maximum measured concentration of the analyte in plasma, t½ terminal half-life of the analyte in plasma
1For tmax, the median and range (minimum–maximum) values are provided