Pharmacokinetic variables of gemfibrozil and gemfibrozil 1-O-β-glucuronide in 10 healthy volunteers after a single dose of 30, 100, 300, or 900 mg of gemfibrozil, which was taken 1 h before administration of repaglinide
Values are mean ± S.D., except for Tmax data, which are given as median and range. Statistical comparisons were performed only for Tmax, t1/2, and glucuronide/gemfibrozil AUC0-∞ ratio data.
| Variable | Gemfibrozil Dose | |||
|---|---|---|---|---|
| 30 mg | 100 mg | 300 mg | 900 mg | |
| Gemfibrozil | ||||
| C1 h (μg/ml) | 1.0 ± 0.5 | 3.7 ± 2.0 | 8.5 ± 5.7 | 32.9 ± 8.8 |
| Cmax (μg/ml) | 1.4 ± 0.4 | 4.8 ± 0.7 | 15.2 ± 4.5 | 48.0 ± 10.1 |
| Tmax (min) | 60 (30–105) | 67.5 (60–105) | 97.5 (60–120)*,† | 90 (75–105)*,† |
| t1/2 (h) | 1.9 ± 0.4 | 1.9 ± 0.2 | 1.9 ± 0.5 | 1.8 ± 0.4 |
| AUC0–10 h (μg · h/ml) | 2.0 ± 0.4 | 8.8 ± 1.9 | 30.6 ± 7.2 | 125.4 ± 25.8 |
| AUC0-∞ (μg · h/ml) | 2.1 ± 0.4 | 9.0 ± 2.0 | 31.3 ± 7.1 | 128.5 ± 26.6 |
| Gemfibrozil-1-O-β-glucuronide | ||||
| C1 h (μg/ml) | 0.3 ± 0.2 | 1.3 ± 0.9 | 2.4 ± 1.7 | 9.0 ± 2.5 |
| Cmax (μg/ml) | 0.5 ± 0.1 | 2.5 ± 0.4 | 7.8 ± 1.4 | 21.6 ± 4.5 |
| Tmax (min) | 67.5 (30–120) | 90 (75–140) | 130 (90–140)*,† | 140 (90–160)*,† |
| t1/2 (h) | 1.8 ± 0.4 | 1.7 ± 0.3 | 1.7 ± 0.6 | 1.9 ± 0.4 |
| AUC0–10 h (μg · h/ml) | 0.9 ± 0.2 | 5.7 ± 1.1 | 21.9 ± 4.1 | 86.7 ± 18.6 |
| AUC0-∞ (μg · h/ml) | 0.95 ± 0.17 | 5.8 ± 1.2 | 22.6 ± 4.2 | 91.5 ± 19.9 |
| Glucuronide/gemfibrozil AUC0-∞ ratio | 0.47 ± 0.08 | 0.66 ± 0.12** | 0.74 ± 0.15**,† | 0.73 ± 0.17**,† |
C1 h, plasma concentration 1 h after gemfibrozil intake (i.e., at the time of repaglinide administration); AUC0-∞, area under the plasma concentration-time curve from time 0 to infinity; AUC0–10 h, area under the plasma concentration-time curve from time 0 to 10 h.
* P < 0.05 vs. 30 mg;
** P < 0.001 vs. 30 mg;
† P < 0.05 vs. 100 mg.