Parent | Cplasmass1-aμM | CLtot1-bml/min/kg | CLbileplasma1-c ml/min/kg | CLbileliver1-cml/min/kg | CLurineplasma1-e ml/min/kg | CLurinekidney1-eml/min/kg | Cliverss1-gμM | Ckidneyss1-gμM | fu1-h |
---|---|---|---|---|---|---|---|---|---|
R-GPFX | 4.50 ± 0.29 | 11.0 ± 0.5 | 0.487 ± 0.082 | 0.0357 ± 0.0068 | 1.12 ± 0.30 | 0.0799 ± 0.0219 | 46.9 ± 9.0 | 68.6 ± 10.3 | 0.706 ± 0.039 |
S-GPFX | 4.57 ± 0.32 | 10.9 ± 0.7 | 0.399 ± 0.089 | 0.0460 ± 0.0026 | 0.927 ± 0.166 | 0.0658 ± 0.0063 | 50.5 ± 7.3 | 69.8 ± 10.3 | 0.676 ± 0.038 |
Glucuronide | CplasmassμM | CLbileplasma1-d ml/min/kg | CLbileliver1-dml/min/kg | CLurineplasma1-f ml/min/kg | CLurinekidney1-fml/min/kg | Cliverss μM | CkidneyssμM | fu | |
---|---|---|---|---|---|---|---|---|---|
R-GPFX-Glu | 0.22 ± 0.04 | — | 163 ± 9 | 7.58 ± 1.12 | 11.1 ± 2.4 | 0.638 ± 0.189 | 4.32 ± 0.66 | 3.79 ± 0.65 | 0.770 ± 0.054 |
S-GPFX-Glu | 0.29 ± 0.07 | — | 82.0 ± 27.1* | 4.02 ± 1.37* | 8.99 ± 1.88 | 0.614 ± 0.100 | 5.56 ± 0.94 | 3.39 ± 0.40 | 0.776 ± 0.022 |
Each represents the obtained parameter ± S.E. of three different rats.
↵1-a Plasma concentration at steady state (mean of plasma concentrations at 70, 90, 120 and 150 min).
↵1-b Total body clearance obtained by dividing the infusion rate by Cplasmass.
↵1-c Biliary excretion clearance based on the plasma or tissue concentration of corresponding GPFX.
↵1-d Biliary excretion clearance based on the plasma or tissue concentration of corresponding glucuronide.
↵1-e Urinary excretion clearance based on the plasma or tissue concentration of corresponding GPFX.
↵1-f Urinary excretion clearance based on the plasma or tissue concentration of corresponding glucuronide.
↵1-g Tissue concentration at steady state.
↵1-h Plasma unbound fraction.
* P < .05 (significantly different from R-GPFX-Glu using Student’s t test).