Pharmacokinetic parameters of the metabolites Ro 48-5033 and Ro 47-8634 following a single oral dose of 500 mg of 14C-labeled bosentan and following a single i.v. dose of 250 mg 14C-labeled bosentan
| Tmax | Cmax | AUC0-∞ | T1/2 | Cmax3-a | AUC3-a | |
|---|---|---|---|---|---|---|
| h | μg/l | μg · h/l | h | % | % | |
| Ro 48-5033 oral dose | ||||||
| Mean | 7.5 | 420.5 | 3089 | 10.3 | 11.1 | 12.7 |
| S.D. | 3.4 | 133.9 | 1269 | 4.7 | 1.9 | 1.9 |
| Median | 7.0 | 459.3 | 2546 | 10.9 | 11.2 | 12.9 |
| Intravenous dose | ||||||
| Mean | 1.3 | 459.3 | 2414 | 6.1 | 7.2 | |
| S.D. | 0.5 | 288.4 | 1861 | 0.8 | 2.3 | |
| Median | 1.0 | 492.3 | 1941 | 5.9 | 7.5 | |
| Ro 47-8634 oral dose | ||||||
| Mean | 5.5 | 171.7 | 1087 | 3.6 | 4.7 | 4.6 |
| S.D. | 1.0 | 30.4 | 321.9 | 1.6 | 1.1 | 0.9 |
| Median | 6.0 | 170.3 | 1066 | 3.5 | 4.6 | 4.3 |
| Intravenous dose | ||||||
| Mean | 0.8 | 286.0 | 844.9 | 2.9 | 2.6 | |
| S.D. | 0.2 | 111.4 | 550.3 | 0.9 | 0.3 | |
| Median | 0.8 | 279.3 | 654.5 | 2.9 | 2.6 |
↵3-a Relative to bosentan.