Table 2.
Substrate (Enzyme) | PK parameter | Day 0 | Day 22 | %Change in mean | GR (22:0) | 90% CI | p-value |
---|---|---|---|---|---|---|---|
Caffeine (CYP1A2) |
AUC (h*μg/L) | 10.00 ± 0.07 | 9.97 ± 0.10 | 0.74 | 0.97 | (0.82; 1.15) | 0.932 |
T1/2 (h) | 1.65 ± 0.07 | 1.56 ± 0.08 | −7.59 | 0.91 | (0.80; 1.05) | 0.310 | |
Tmax (h) | −0.57 ± 0.16 | −0.70 ± 0.10 | −23.81 | 0.87 | (0.62; 1.24) | 0.324 | |
Cmax (μg/L) | 7.98 ± 0.07 | 8.12 ± 0.07 | 13.92 | 1.15 | (1.04; 1.27) | 0.0355 | |
CL/F (L/h) | 1.51 ± 0.07 | 1.54 ± 0.10 | 6.51 | 1.03 | (0.87; 1.21) | 0.566 | |
Tolbutamide (CYP2C9) |
AUC (h*μg/L) | 12.90 ± 0.09 | 12.93 ± 0.08 | 1.74 | 1.03 | (0.97; 1.09) | 0.637 |
T1/2 (h) | 2.16 ± 0.05 | 2.20 ± 0.05 | 4.12 | 1.04 | (0.99; 1.10) | 0.195 | |
Tmax (h) | 1.24 ± 0.16 | 1.37 ± 0.13 | 9.09 | 1.14 | (0.91; 1.42) | 0.433 | |
Cmax (μg/L) | 10.15 ± 0.06 | 10.17 ± 0.06 | 1.91 | 1.01 | (0.92; 1.12) | 0.735 | |
CL/F (L/h) | −0.47 ± 0.09 | −0.50 ± 0.08 | −3.91 | 0.97 | (0.91; 1.03) | 0.252 | |
Dextromethorphan (CYP2D6) |
AUC (h*μg/L) | 3.33 ± 0.22 | 3.34 ± 0.20 | −3.10 | 1.01 | (0.85; 1.21) | 0.726 |
T1/2 (h) | 2.20 ± 0.08 | 2.24 ± 0.08 | 3.62 | 1.04 | (0.97; 1.12) | 0.322 | |
Tmax (h) | 0.76 ± 0.11 | 0.91 ± 0.10 | 14.89 | 1.17 | (0.95; 1.44) | 0.366 | |
Cmax (μg/L) | 1.13 ± 0.19 | 1.11 ± 0.19 | 3.41 | 0.98 | (0.75; 1.27) | 0.815 | |
CL/F (L/h) | 6.98 ± 0.22 | 6.97 ± 0.20 | −7.69 | 0.99 | (0.83; 1.18) | 0.615 | |
Alprazolam (CYP3A4/5) |
AUC (h*μg/L) | 6.34 ± 0.06 | 6.36 ± 0.06 | 2.77 | 1.03 | (0.98; 1.08) | 0.295 |
T1/2 (h) | 2.79 ± 0.05 | 2.80 ± 0.06 | 0.43 | 1.00 | (0.95; 1.06) | 0.880 | |
Tmax (h) | −0.03 ± 0.20 | −0.40 ± 0.08 | −48.78 | 0.69 | (0.46; 1.04) | 0.0723 | |
Cmax (μg/L) | 3.35 ± 0.08 | 3.54 ± 0.09 | 24.45 | 1.22 | (1.08; 1.36) | 0.0121 | |
CL/F (L/h) | 1.27 ± 0.06 | 1.24 ± 0.06 | −3.15 | 0.97 | (0.93; 1.02) | 0.241 |