Table 1 The PK parameters of ezetimibe, ezetimibe glucuronide, and total ezetimibe under fasting and fed conditions

 C_max (ng/mL)

3.23 ± 1.41

3.48 ± 1.82

5.94 ± 4.12

5.81 ± 3.06

 AUC_0–t (ng·h/mL)

58.49 ± 25.76

59.52 ± 27.21

72.67 ± 36.74

76.0 ± 35.48

 AUC_0–∞ (ng·h/mL)

68.05 ± 28.60

68.62 ± 30.60

88.50 ± 43.95

88.98 ± 38.33

 T_max (h)

5.0 (0.50–24.0)

5.0 (0.33–12.0)

2.50 (0.50–6.0)

2.50 (0.33–5.0)

 T_1/2 (h)

18.03 ± 6.52

19.38 ± 11.41

25.89 ± 12.01

26.62 ± 15.12

 λ_z (h^− 1)

0.043 ± 0.015

0.048 ± 0.024

0.033 ± 0.018

0.033 ± 0.015

 C_max (ng/mL)

63.21 ± 47.14

68.55 ± 51.82

77.68 ± 37.25

79.22 ± 33.05

 AUC_0–t (ng·h/mL)

575.78 ± 408.26

598.91 ± 441.88

409.29 ± 191.89

445.64 ± 196.37

 AUC_0–∞ (ng·h/mL)

652.95 ± 407.06

690.65 ± 456.82

532.09 ± 214.84

550.38 ± 214.12

 T_max (h)

1.75 (0.33–5.0)

1.50 (0.33 ~ 5.0)

2.50 (0.50–6.00)

2.50 (0.50–5.0)

 T_1/2 (h)

20.36 ± 11.62

22.57 ± 21.67

31.05 ± 17.04

27.78 ± 13.71

 λ_z (h^− 1)

0.049 ± 0.041

0.051 ± 0.036

0.028 ± 0.015

0.030 ± 0.012

 C_max (ng/mL)

65.73 ± 47.14

71.32 ± 51.98

83.38 ± 38.95

84.74 ± 34.62

 AUC_0–t (ng·h/mL)

643.34 ± 400.77

668.49 ± 439.57

494.21 ± 208.65

536.69 ± 209.11

 AUC_0–∞ (ng·h/mL)

706.36 ± 410.92

734.23 ± 468.26

573.74 ± 252.74

604.75 ± 247.13

 T_max (h)

1.75 (0.33–5.0)

1.25 (0.33–5.0)

2.50 (0.50–5.0)

2.50 (0.50–6.0)

 T_1/2 (h)

17.09 ± 13.22

17.35 ± 12.14

22.56 ± 12.68

19.80 ± 15.59

 λ_z (h^− 1)

0.062 ± 0.042

0.061 ± 0.033

0.041 ± 0.022

0.052 ± 0.027