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. Author manuscript; available in PMC: 2011 Apr 28.
Published in final edited form as: Pharm Res. 2009 Jun 4;26(8):1942–1951. doi: 10.1007/s11095-009-9909-z

Table III.

Fexofenadine disposition in single-pass perfused TR rat livers. Mean ± SD (n = 3–4 per group).

0.5 µM
Fexofenadine
0.5 µM Fexofenadine
without TC
0.5 µM Fexofenadine +
2 µM GF120918
0.5 µM Fexofenadine +
5 µM Bosentan
Css,out (pmol/mL) # 92.3 ± 29.4 135 ± 21 172 ± 59* 209 ± 19*

Cliver (pmol/mL) 7295 ± 786 7156 ± 1529 8159 ± 720 5561 ± 873

Cliver, unbound (pmol/mL) 1389 ± 196 1282 ± 142 1631 ± 620 1235 ± 369

Cliver, unbound / Css,out 16.2 ± 5.4 9.53± 0.46 10.8 ± 6.0 6.05 ± 2.34*

Extraction Ratio 0.82 ± 0.06 0.73 ± 0.04 0.66 ± 0.12* 0.58± 0.04*

Biliary Excretion Rate
(pmol/min/g liver)
218 ± 66 136 ± 34* 55.6 ± 6.4* 142 ± 29

Cl’biliary (mL/h/g liver) 8.57 ± 2.00 6.56 ± 2.27 2.36 ± 1.12* 7.52 ± 2.78
*

p< 0.05 fexofenadine ± modulator vs. fexofenadine alone.

#

Total concentration determined based on 50–60-min collection interval. Perfusate buffer contained 5 µM taurocholate (TC), unless otherwise noted.