BOPTA and MEB pharmacokinetic parameters and concentrations in the presence of RIF (+RIF) and the absence of RIF (−RIF)
| Parameters | BOPTA | BOPTA+RIF | +RIF/−RIF Ratio | MEB | MEB+RIF | +RIF/−RIF Ratio |
|---|---|---|---|---|---|---|
| Cin (μM) | 200 | 200 | 64 | 64 | ||
| Cout,75min (μM) | 185 ± 3 | 196 ± 2 | 1.06 | 5 ± 2 | 31 ± 4 | 6.2 |
| CHC,75min (μM) | 566 ± 99 | 23 ± 19 | 0.04 | 2611 ± 498 | 5044 ± 693 | 1.93 |
| Cbile,75min (μM) | 16,791 ± 2085 | 92 ± 44 | 0.0005 | 97,017 ± 11,289 | 13,258 ± 8363 | 0.14 |
| Cbile,75min/CHC,75min | 30.6 ± 7.5 | 3.5 ± 2.9 | 0.11 | 38.4 ± 8.8 | 2.6 ± 1.6 | 0.07 |
| v75min (nmol/min)a | 464 ± 80 | 111 ± 47 | 0.24 | 1797 ± 61 | 1022 ± 113 | 0.57 |
| CL (ml/min)b | 2.32 ± 0.40 | 0.56 ± 0.24 | 0.24 | 28.12 ± 0.22 | 15.64 ± 1.77 | 0.56 |
| Ec | 0.08 ± 0.01 | 0.02 ± 0.01 | 0.25 | 0.93 ± 0.03 | 0.53 ± 0.06 | 0.57 |
| vbile,75min (nmol/min)d | 390 ± 84 | 1 ± 1 | 0.003 | 990 ± 166 | 105 ± 65 | 0.11 |
| fL CLint,bile (ml/min)e | 0.72 ± 0.23 | 0.04 ± 0.03 | 0.06 | 0.39 ± 0.11 | 0.02 ± 0.01 | 0.05 |
| fL CLef (ml/min)f | 0.13–0.07g | 0.41–0.00g | 0.01 ± 0.01 | 0.01 ± 0.01 | ||
| fB CLin (ml/min) | 2.69 ± 0.37 | 0.60 ± 0.20 | 0.22 | 28.54 ± 0.27 | 15.64 ± 1.77 | 0.55 |
↵a Drug removal rate from sinusoids (v) = QH ⋅ (Cin − Cout).
↵b Hepatic CL: QH ⋅ (Cin − Cout)/Cin.
↵c Extraction ratio (E) = Cin − Cout/Cin.
↵d vbile = Qbile ⋅ Cbile.
↵e CLint,bile (fL ⋅ CLint,bile) = vbile/CHC.
↵f CLef back to sinusoids (fL ⋅ CLef) = vef/CHC, with vef = QH ⋅ Cout.
↵g Mean ranges over time.