TABLE 3

Concentrations of tibolone and nonsulfated and sulfated metabolites and percentages in monkey feces samples

See Table 1 footnotes. The mean (± S.D.) weight of feces is 57 ± 4 g and 61 ± 4 g after sd and md, respectively.


Sampling Time

Mean Level (± S.D.) of Metabolite Measured (ng/g)

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 ± 0.1 0.4 ± 0.5 0.0 1 ± 1 0.0 0.1 ± 0.3 0.0 57.3 100.0
0-24 h 16 ± 23 250 ± 181 401 ± 462 70 ± 64 91 ± 81 71 ± 93 505 ± 505 67 ± 110 48.7 81.2
24-48 h 12 ± 8 280 ± 108 437 ± 247 57 ± 38 107 ± 54 59 ± 73 372 ± 259 43 ± 44 41.7 82.4
48-72 h 6 ± 5 150 ± 131 97 ± 94 25 ± 22 56 ± 20 44 ± 67 103 ± 80 22 ± 33 43.4 70.7
72-96 h 0 48 ± 47 14 ± 10 2 ± 1 15 ± 12 16 ± 24 32 ± 42 7 ± 12 53.5 68.8
96-120 h 0 22 ± 22 5 ± 5 1 ± 1 10 ± 8 7 ± 8 3 ± 3 2 ± 3 45.6 61.5
120-144 h 0 4 ± 4 1 ± 1 1 ± 1 2 ± 4 2 ± 2 1 ± 2 1 ± 1 45.6 52.0
144-168 h 0 8 ± 14 6 ± 14 4 ± 8 7 ± 11 2 ± 3 3 ± 8 2 ± 5 40.9 71.0
0-168 h 33 ± 14 762 ± 103 960 ± 226 126 ± 30 293 ± 48 201 ± 106 1020 ± 313 144 ± 80 44 ± 7 82 ± 4
Multiple dose
-24-0 h 33 ± 28 664 ± 238 707 ± 381 94 ± 121 236 ± 318 427 ± 495 248 ± 338 284 ± 345 43.5 40.5
0-24 h 38 ± 21 719 ± 395 654 ± 324 118 ± 49 415 ± 302 823 ± 875 377 ± 306 476 ± 493 56.7 37.9
144-168 h 63 ± 39 880 ± 485 716 ± 400 167 ± 126 273 ± 146 695 ± 491 252 ± 235 370 ± 263 45.5 33.0
Mean ± S.D.
44 ± 30
752 ± 371
690 ± 342
126 ± 103
308 ± 263
648 ± 630
292 ± 285
377 ± 365
42 ± 20
37 ± 21