TABLE 4

Biliary excretion, apparent biliary clearance, and comparison bile/plasma ratio of finasteride and M3 after intravenous and intrajejunal administration with (T2) and without (T1) ketoconazole coadministration

FinasterideM3
T1T2IntravenousT1T2Intravenous
Ae(bile, 0–6 h) (μmol)0.05 ± 0.050.09 ± 0.030.02 ± 0.011.7 ± 1.30.6 ± 0.40.8 ± 0.8a
0.03 (0.002–0.12)b0.09 (0.05–0.13)b0.02 (0.01–0.04)b1.2 (0.7–3.9)b0.7 (0.05–1.3)b0.6 (0.06–1.65)b
fbile (%)0.09 ± 0.090.18 ± 0.070.19 ± 0.103.1 ± 2.41.1 ± 0.85.5 ± 5.7
CLapp, bile (ml · min−1 · kg−1)0.009 ± 0.0070.010 ± 0.0040.014 ± 0.0062.4 ± 1.31.2 ± 0.43.6 ± 3.4
AUCbile, 0–6 h (μM · h)2.5 ± 1.94.2 ± 2.01.1 ± 0.5106 ± 6327 ± 2023 ± 20
Cmax (μM)1.3 ± 1.02.0 ± 0.90.5 ± 0.0437 ± 259.5 ± 7.28.2 ± 9.3
AUCbile/AUCVPc0.9 ± 0.60.7 ± 0.30.9 ± 0.3106 ± 74104 ± 69174 ± 134
AUCbile/AUCVHc14 ± 126 ± 37 ± 294 ± 6769 ± 35136 ± 103
Biliary flow (ml · min−1 · kg−1)0.010 ± 0.0040.016 ± 0.0080.015 ± 0.006
  • a ID8 had very low amount of excreted finasteride-ω-oic-acid (M3).

  • b Data are median (range).

  • c Plasma AUC for finasteride was corrected for fu = 0.17.