HPLC metabolite profiles of tibolone in plasma pools of postmenopausal volunteers after daily oral administration of 2.5 mg of tibolone for 5 days, followed by a single dose of 2.5 mg of [14C]tibolone
| Time2-a | ||||||||
|---|---|---|---|---|---|---|---|---|
| 1 h | 1.5 h | 2 h | 3 h | 4 h | 6 h | 8 h | 24 h | |
| Total radioactivity2-b | 42.5 | 90 | 110 | 115.1 | 105.2 | 85.8 | 92.6 | 56.3 |
| Metabolite | ||||||||
| 3α,17β-Disulfate tibolone | 0 | 6.3 | 9.3 | 10.2 | 8.4 | 12.7 | 16.8 | 17.7 |
| 2α-Hydroxy-3α-sulfate tibolone | 0 | 0 | 6.7 | 10.8 | 6.4 | 0 | 0 | 0 |
| 3α-Hydroxy-17β-sulfate tibolone | 0 | 11.3 | 29.8 | 37.5 | 33.2 | 36.7 | 42.5 | 22.1 |
| 3α-Sulfate tibolone | 7.9 | 29.3 | 23.2 | 21 | 17 | 16.3 | 14.3 | 10.2 |
| Unknown 1 | 8 | 10.2 | 10.9 | 10.1 | 6.4 | 0 | 0 | 0 |
| Δ4-Tibolone | 6.1 | 7.9 | 9.1 | 9.3 | 9.9 | 13.8 | 13.9 | 6.4 |
| 3α-Hydroxy tibolone | 11.7 | 15.4 | 13.9 | 11.3 | 9 | 6.3 | 5.1 | 0 |
| 3β-Hydroxy tibolone/tibolone | 0 | 9.6 | 7.1 | 4.9 | 0 | 0 | 0 | 0 |
| Unknown 2 | 8.8 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |