Table 3.
Pharmacokinetic parameters of prodrug (dabigatran etexilate) and intermediate metabolites (BIBR 1087 SE and BIBR 951 BS) after administration of dabigatran etexilate 150 mg, with and without rifampicin
| Treatment A: 150 mg DE day 1 | Treatment B: 150 mg DE day 9 and multiple doses of rifampicin | Treatment C: 150 mg DE day 16, 7 days after rifampicin | Treatment D: 150 mg DE day 23, 14 days after rifampicin | |||||
|---|---|---|---|---|---|---|---|---|
| gMean | gCV, % | gMean | gCV, % | gMean | gCV, % | gMean | gCV, % | |
| Dabigatran etexilate | ||||||||
| Cmax (ng ml−1) | 3.64 | 72.0 | 2.32 | 43.7 | 3.38 | 59.3 | 3.58 | 60.3 |
| tmax (h)* | 1.00 | 0.500–2.00 | 0.500 | 0.500–1.50 | 1.00 | 0.500–1.50 | 1.00 | 0.500–2.00 |
| BIBR 1087 SE | ||||||||
| Cmax (ng ml−1) | 2.07 | 40.7 | – | – | 1.67 | 35.6 | 1.93 | 37.0 |
| tmax (h)* | 1.00 | 1.00–2.00 | – | – | 1.00 | 0.500–1.50 | 1.50 | 0.500–2.00 |
| BIBR 951 BS | ||||||||
| Cmax (ng ml−1) | 2.75 | 67.2 | – | – | 1.86 | 44.6 | 2.14 | 28.1 |
| tmax (h)* | 1.50 | 1.00–3.00 | – | – | 1.50 | 1.00–2.00 | 1.50 | 1.00–2.00 |
Abbreviations: Cmax, maximal plasma concentration; DE, dabigatran etexilate; and tmax, time from dosing to maximal plasma concentration. *Median (range).