Interaction between Red Yeast Rice and CYP450 Enzymes/P-Glycoprotein and Its Implication for the Clinical Pharmacokinetics of Lovastatin
Table 3
Pharmacokinetic parameters of lovastatin and lovastatin acid in healthy subjects after a single dose of 1, 2, or 4 LipoCol Forte capsules and multiple doses of one LipoCol Forte capsule twice daily for 5 days in the fed state. The data are the mean ± SD for 14 subjects.
Single dose (one capsule)
Single dose (two capsules)
Single dose (four capsules)
Multiple doses (one capsule BID)
Lovastatin
(ng h/mL)
6.74 ± 3.27*
13.38 ± 6.07*
24.95 ± 14.25*
5.22 ± 2.60
(ng h/mL)
7.47 ± 3.44*
14.36 ± 6.30*
26.78 ± 15.36*
5.71 ± 2.68
(ng/mL)
1.61 ± 0.80*
3.36 ± 1.81*
5.70 ± 3.42*
1.41 ± 0.69
/dose
1.18 ± 0.57
1.17 ± 0.53
1.09 ± 0.63
0.92 ± 0.46
/dose
1.31 ± 0.60
1.26 ± 0.55
1.17 ± 0.67
1.00 ± 0.47
/dose
0.28 ± 0.14
0.30 ± 0.16
0.25 ± 0.15
0.25 ± 0.12
(h)
3.46 ± 1.28
3.29 ± 1.35
3.25 ± 0.78
3.39 ± 1.38
MRT (h)
5.55 ± 1.98
5.27 ± 1.42
5.51 ± 1.11
4.81 ± 1.24
(h)
2.36 ± 0.66
2.36 ± 0.68
2.42 ± 0.45
1.93 ± 0.43
CL/F (L/h)
941.7 ± 453.5
994.5 ± 548.8
1128.8 ± 624.4
1339.5 ± 763.3
/F (L)
3078.4 ± 1327.7
3380.7 ± 2049.5
3862.9 ± 1956.5
3569.5 ± 1801.1
Lovastatin acid
(ng h/mL)
33.0 ± 13.1*
79.1 ± 27.6*
158.3 ± 60.2*
32.4 ± 9.7
(ng h/mL)
38.3 ± 16.2*
85.4 ± 27.8*
169.1 ± 62.9*
33.7 ± 9.7
(ng/mL)
7.78 ± 4.12*
17.80 ± 9.21*
36.24 ± 17.12*
8.04 ± 3.24
/dose
5.75 ± 2.30
6.94 ± 2.42
6.94 ± 2.64
5.69 ± 1.70
/dose
6.72 ± 2.85
7.50 ± 2.44
7.42 ± 2.76
5.92 ± 1.70
/dose
1.37 ± 0.72
1.56 ± 0.81
1.59 ± 0.75
1.41 ± 0.57
(h)
5.07 ± 1.59
5.14 ± 1.70
5.00 ± 1.52
4.36 ± 0.93
MRT (h)
7.15 ± 3.30
6.43 ± 1.77
6.39 ± 1.43
5.59 ± 1.15
(h)
2.57 ± 1.74
2.07 ± 0.68
2.04 ± 0.68
1.92 ± 0.34
CL/F (L/h)
172.9 ± 68.1
145.7 ± 43.1
150.2 ± 45.9
192.3 ± 63.7
/F (L)
602.8 ± 336.8
438.4 ± 188.6
455.9 ± 265.2
544.1 ± 240.9
among the single dose of one, two, and four capsule groups.