Table 2 The geometric mean ratios of primary pharmacokinetic parameters for ezetimibe, ezetimibe glucuronide, and total ezetimibe and their 90%CIs under fasting and fed conditions
Geometric mean | T/R(%) | Intra-CV(%) | 90%CIs | ||
|---|---|---|---|---|---|
T | R | ||||
Ezetimibe, fasting | |||||
Cmax (ng/mL) | 2.96 | 3.12 | 94.89 | 21.71 | 86.26 ~ 104.38 |
AUC0-t (ng·h/mL) | 53.59 | 54.93 | 97.56 | 20.81 | 89.04 ~ 106.9 |
AUC0-∞(ng·h/mL) | 62.48 | 63.69 | 98.09 | 20.19 | 89.77 ~ 107.19 |
Ezetimibe glucuronide, fasting | |||||
Cmax (ng/mL) | 52.02 | 56.98 | 91.30 | 15.28 | 85.37 ~ 97.63 |
AUC0-t (ng·h/mL) | 469.63 | 486.21 | 96.59 | 18.22 | 89.16 ~ 104.64 |
AUC0-∞(ng·h/mL) | 551.63 | 575.92 | 95.78 | 15.84 | 89.35 ~ 102.68 |
Total ezetimibe, fasting | |||||
Cmax (ng/mL) | 54.69 | 60.07 | 91.05 | 14.87 | 85.29 ~ 97.19 |
AUC0-t (ng·h/mL) | 550.93 | 567.13 | 97.14 | 16.35 | 90.41 ~ 104.38 |
AUC0-∞(ng·h/mL) | 610.67 | 622.30 | 98.13 | 17.66 | 90.81 ~ 106.05 |
Ezetimibe, fed | |||||
Cmax (ng/mL) | 4.92 | 5.11 | 96.28 | 24.53 | 86.27 ~ 107.45 |
AUC0-t (ng·h/mL) | 64.16 | 69.71 | 92.05 | 18.56 | 84.71 ~ 100.02 |
AUC0-∞(ng·h/mL) | 78.42 | 82.51 | 95.04 | 22.01 | 86.13 ~ 104.88 |
Ezetimibe glucuronide, fed | |||||
Cmax (ng/mL) | 70.49 | 72.97 | 96.60 | 26.93 | 85.63 ~ 108.97 |
AUC0-t (ng·h/mL) | 368.83 | 409.26 | 90.12 | 17.03 | 83.51 ~ 97.25 |
AUC0-∞(ng·h/mL) | 489.44 | 515.02 | 95.03 | 20.88 | 86.56 ~ 104.34 |
Total ezetimibe, fed | |||||
Cmax (ng/mL) | 76.12 | 78.40 | 97.10 | 26.20 | 86.36 ~ 109.17 |
AUC0-t (ng·h/mL) | 454.24 | 501.94 | 90.50 | 14.12 | 84.96 ~ 96.40 |
AUC0-∞(ng·h/mL) | 520.82 | 561.0 | 92.84 | 18.89 | 85.32 ~ 101.02 |