Table 3.
Pharmacokinetic parameters for phases A and B
| Phase | Parameter | Normal | Mild | Moderate | Severe |
|---|---|---|---|---|---|
| A | AUCt [h*μg/mL] | ||||
| N | 8 | 8 | 8 | 6 | |
| Mean (SD) | 7.818 (2.677) | 14.594 (6.905) | 14.439 (7.181) | 26.245 (20.419) | |
| Geometric mean (CV%) | 7.423 (35.56) | 12.720 (67.99) | 12.919 (54.29) | 19.818 (108.50) | |
| AUC∞ [h*μg/mL] | |||||
| N | 8 | 8 | 8 | 6 | |
| Mean (SD) | 8.038 (2.664) | 14.842 (6.914) | 14.728 (7.247) | 27.080 (21.423) | |
| Geometric mean (CV%) | 7.655 (34.46) | 13.024 (65.55) | 13.213 (53.49) | 20.447 (107.30) | |
| Cmax [μg/mL] | |||||
| N | 8 | 8 | 8 | 6 | |
| Mean (SD) | 1.561 (0.635) | 2.246 (1.125) | 1.891 (1.316) | 2.402 (1.433) | |
| Geometric mean (CV%) | 1.384 (66.80) | 1.951 (67.70) | 1.414 (113.69) | 1.871 (113.94) | |
| tmax [h] | |||||
| N | 8 | 8 | 8 | 6 | |
| Median | 1.250 | 1.008 | 0.758 | 1.000 | |
| Min–max | 0.500–6.000 | 1.000–2.500 | 0.500–2.000 | 0.500–2.000 | |
| t½ [h] | |||||
| N | 8 | 8 | 8 | 6 | |
| Median | 9.209 | 11.675 | 12.414 | 14.633 | |
| Min–max | 7.778–11.124 | 8.100–16.390 | 10.393–20.046 | 10.483–21.915 | |
| B | AUCτ,ss [h*μg/mL] | ||||
| N | 17 | 8 | 8 | 8 | |
| Mean (SD) | 9.829 (4.418) | 14.879 (6.282) | 12.007 (5.702) | 12.532 (5.921) | |
| Geometric mean (CV%) | 8.679 (59.84) | 13.567 (51.07) | 10.701 (57.85) | 10.798 (75.71) | |
| Cmax,ss [μg/mL] | |||||
| N | 17 | 8 | 8 | 8 | |
| Mean (SD) | 1.960 (0.992) | 2.456 (1.242) | 1.801 (0.858) | 1.554 (0.786) | |
| Geometric mean (CV%) | 1.652 (74.96) | 2.167 (59.29) | 1.584 (63.73) | 1.242 (107.89) | |
| tmax,ss [h] | |||||
| N | 17 | 8 | 8 | 8 | |
| Median | 1.000 | 1.000 | 1.250 | 1.500 | |
| Min–max | 0.500–2.000 | 0.500–4.000 | 0.500–2.500 | 0.500–2.000 | |
| t½,ss [h] | |||||
| N | 17 | 8 | 8 | 8 | |
| Median | 9.654 | 13.637 | 14.016 | 17.176 | |
| Min–max | 6.264–19.560 | 8.034–28.219 | 9.722–17.161 | 11.105–25.749 | |
SD standard deviation, CV% percentage coefficient of variation, AUC area under the plasma concentration-time curve, AUCt AUC during a dosing interval, AUC∞ AUC extrapolated to infinity, Cmax maximum plasma concentration, tmax time to Cmax, min minimum, max maximum, t½ apparent terminal elimination half-life, AUCτ,ss AUC during a dosing interval at steady-state, Cmax,ss maximum plasma concentration at steady state, tmax,ss time to maximum plasma concentration at steady state, t½,ss apparent terminal elimination half-life at steady state