Table 1. Pharmacokinetic parameters of rosiglitazone in 10 healthy male Korean subjects after a single oral administration of 8 mg rosiglitazone following pretreatment with placebo or 200 mg ketoconazole twice daily for 5 days.
| Variable | Placebo phase (control) | Ketoconazole phase | Mean difference between placebo and ketoconazole (95%CI) | P-value |
|---|---|---|---|---|
| Cmax (µg ml−1) | 0.70 ± 0.22 | 0.81 ± 0.21* | 0.11 (0.01, 0.20) | 0.03 |
| Percentage of control (range) | 100% | 117% (91–155%) | 117% (105, 129) | |
| tmax (h) | 1.0 (0.5–2.0) | 1.0 (0.5–2.5) | 0.47 | |
| Ke (h−1) | 0.20 ± 0.04 | 0.13 ± 0.02 | −0.07 (−0.09, −0.04) | 0.0004 |
| Half-life (h) | 3.55 ± 0.63 | 5.50 ± 1.35‡ | 1.75 (1.1, 2.4) | 0.0003 |
| Percentage of control (range) | 100% | 153% (120–252%) | 153% (130, 177) | |
| CL/F (l h−1) | 2.14 ± 0.53 | 1.53 ± 0.53‡ | −0.6 (−0.35, −0.86) | 0.0005 |
| Percentage of control (range) | 100% | 72% (44–95%) | 72% (62, 82) | |
| AUC(0,14) (µg hm l−1) | 3.69 ± 1.11 | 4.87 ± 1.60† | 1.18 (0.42, 1.94) | 0.007 |
| Percentage of control (range) | 100% | 133% (105–206%) | 133% (114, 151) | |
| AUC(0,∞) (µg hm l−1) | 4.01 ± 1.25 | 5.87 ± 2.24† | 1.86 (0.72, 3.00) | 0.0003 |
| Percentage of control (range) | 100% | 147% (109–229%) | 147% (123, 170) |
Data are mean values ± SD; tmax data are given as median with range; Cmax, peak plasma concentration; tmax, time to peak concentration; Ke, elimination rate constant; AUC, area under the plasma concentration–time curve.
*
P < 0.05 versus control;
†
P < 0.01 versus control; P < 0.001 versus control.