TABLE 2

Concentrations (ng/ml) of tibolone and nonsulfated and sulfated metabolites and percentages in monkey urine samples

See Table 1 footnotes. The mean (±S.D.) urine volume is 101 ± 6 ml and 123 ± 11 ml after sd and md, respectively.

Sampling Time
Mean Level (±S.D.) of Metabolite Measured (ng/ml)
Percentage
Tibolone
3αOH-tib
3βOH-tib
Δ4-tib
3αS,17βOH-tib
3αS,17βS-tib
3βS,17βOH-tib
3βS,17βS-tib
Sulfated
Mono-S
Single dose
Predose 0.0 0.0 0.0 0.0 0.0 0.0 0.0 0.0 N.C. N.C.
0-24 h 0.0 0.0 0.3 ± 0.4 0.6 ± 0.2 4.3 ± 5.2 95.0 ± 80.6 2.7 ± 3.8 48.0 ± 26.3 99.0 4.6
24-48 h 0.0 0.7 ± 1.4 1.7 ± 3.7 0.1 ± 0.2 1.7 ± 1.4 46.2 ± 34.0 0.8 ± 0.9 8.8 ± 6.0 95.4 4.4
48-72 h 0.0 1.0 ± 1.1 0.6 ± 1.0 0.1 ± 0.2 0.4 ± 0.3 6.0 ± 4.3 0.2 ± 0.2 1.0 ± 0.4 81.1 7.2
72-96 h 0.0 0.1 ± 0.2 0.1 ± 0.1 0.0 0.1 ± 0.1 1.3 ± 1.1 0.0 0.2 ± 0.1 86.4 5.7
96-120 h 0.0 0.0 0.0 0.0 0.0 0.2 ± 0.2 0.0 0.1 ± 0.1 85.1 8.8
120-144 h 0.0 0.0 0.0 0.0 0.0 0.0 0.0 0.0 N.C. N.C.
144-168 h 0.0 0.0 0.0 0.0 0.0 0.0 0.0 0.0 N.C. N.C.
0-168 h 0.0 ± 0.0 1.9 ± 2.2 2.8 ± 3.6 0.9 ± 0.3 6.4 ± 5.6 148.7 ± 77.5 3.8 ± 3.9 58.1 ± 27.9 96.4 ± 2.8 4.5 ± 2.5
Multiple dose
-24-0 h 0.0 ± 0.1 3.7 ± 7.2 6.7 ± 14.3 2.2 ± 2.3 2.5 ± 3.0 97.7 ± 66.5 4.7 ± 11.0 42.8 ± 27.4 91.3 4.9
0-24 h 0.2 ± 0.5 2.4 ± 4.0 2.0 ± 2.5 2.0 ± 1.6 2.1 ± 1.9 130.5 ± 57.1 1.4 ± 1.6 59.4 ± 27.9 95.9 1.8
144-168 h 0.2 ± 0.3 5.2 ± 10.6 6.3 ± 13.4 5.5 ± 5.8 2.3 ± 2.4 81.5 ± 77.6 3.1 ± 5.6 48.1 ± 53.8 87.0 4.0
Mean ± S.D.
0.1 ± 0.3
3.8 ± 7.4
5.0 ± 11.0
3.2 ± 3.9
2.3 ± 2.3
103.2 ± 66.8
3.1 ± 6.9
50.1 ± 36.7
91.4 ± 4.5
3.6 ± 1.6