Table 1.
Pharmacokinetic data of ezetimibe and ezetimibe-glucuronide with and without comedication of 400 mg efavirenz in 12 healthy subjects
| Units | Ezetimibe | Ezetimibe + efavirenz single dose | Ratio (90% CI) | Ezetimibe + efavirenz multiple dose | Ratio (90% CI) | |
|---|---|---|---|---|---|---|
| Ezetimibe | ||||||
| AUC0–24 h | ng × h/ml | 51.9 ± 21.7 | 58.6 ± 23.8 | 1.146 (1.034, 1.270) | 51.1 ± 23.1 | 0.975 (0.850, 1.118) |
| AUC0–6 h | ng × h/ml | 13.6 ± 5.5 | 18.5 ± 8.1* | 1.346 (1.201, 1.508) | 14.6 ± 6.5 | 1.052 (0.880, 1.256) |
| Cmax | ng/ml | 4.82 ± 2.74 | 5.54 ± 2.65 | 1.194 (1.031, 1.382) | 4.46 ± 2.07 | 0.951 (0.730, 1.240) |
| CLR | ml/min | 1.38 ± 0.65 | 1.39 ± 1.35 | — | 1.41 ± 0.89 | — |
| Ezetimibe-glucuronide | ||||||
| AUC0–24 h | ng × h/ml | 466 ± 223 | 411 ± 195* | 0.885 (0.809, 0.968) | 325 ± 152* | 0.700 (0.608, 0.806) |
| AUC0–6 h | ng × h/ml | 205 ± 90 | 182 ± 87 | 0.872 (0.774, 0.982) | 141 ± 58* | 0.691 (0.592, 0.806) |
| Cmax | ng/ml | 78.9 ± 43.1 | 60.9 ± 29.5 | 0.776 (0.625, 0.963) | 45.3 ± 14.6* | 0.606 (0.469, 0.783) |
| CLR | ml/min | 24.7 ± 8.77 | 23.3 ± 7.61 | — | 21.7 ± 5.91 | — |
| Ezetimibe total | ||||||
| Aeurine | μg | 622 ± 195 | 565 ± 357 | — | 407 ± 210* | — |
| Aefeces | mg | 6.57 ± 2.17 | 8.03 ± 1.21 | — | 6.87 ± 2.99 | — |
Arithmetic means ± SD are given.
AUC, area under the concentration–time curve; CI, confidence interval; Cmax, maximum plasma concentration; CLR, renal clearance.
*
P < 0.025 for comparison with ezetimibe alone, Wilcoxon test with Bonferroni correction. Ratios of the pharmacokinetic parameters and 90% CIs are presented for equivalence analysis.