Table 1.
Pharmacokinetic parameters for pantoprazole, rabeprazole, and omeprazole under fasting and fed conditions. Among 71 volunteers receiving omeprazole, 35 were the same subjects. Data are expressed as mean ± standard deviation. *p ≤ 0.05 vs. men
| n | AUC0-∞ (ng·h/ml) | Cmax (ng/ml) | Tmax (h) | t1/2 (h) | Vd/F (l/kg) | Cl/F (L/h·kg) | Ke | |
|---|---|---|---|---|---|---|---|---|
| Pantoprazole (n = 81) | ||||||||
| Fast | 36 | 6951.4 ± 3293.2 | 2779.1 ± 861.6 | 3.0 ± 0.8 | 1.3 ± 0.6 | 0.17 ± 0.03 | 0.11 ± 0.04 | 0.61 ± 0.21 |
| Men | 18 | 6584.5 ± 3832.8 | 2316.4 ± 580.9 | 3.1 ± 0.8 | 1.5 ± 0.7 | 0.18 ± 0.03 | 0.11 ± 0.03 | 0.56 ± 0.23 |
| Women | 18 | 7318.4 ± 2711.6 | 3241.8 ± 858.8 | 2.9 ± 0.8 | 1.1 ± 0.3 | 0.16 ± 0.03 | 0.11 ± 0.05 | 0.65 ± 0.18 |
| Fed | 45 | 4633.5 ± 2022.7 | 2646.2 ± 603.1 | 7.0 ± 3.0 | 1.3 ± 0.6 | 0.26 ± 0.10 | 0.16 ± 0.06 | 0.63 ± 0.21 |
| Men | 23 | 4607.8 ± 2265.1 | 2590.7 ± 601.2 | 5.6 ± 1.1 | 1.3 ± 0.5 | 0.25 ± 0.08 | 0.15 ± 0.07 | 0.61 ± 0.23 |
| Women | 22 | 4660.4 ± 1787.8 | 2704.2 ± 613.6 | 8.4 ± 3.7* | 1.2 ± 0.7 | 0.28 ± 0.12 | 0.17 ± 0.05 | 0.65 ± 0.19 |
|
Fed vs. Fast ratio; 90% CI; p value |
65.6; 55.7–77.2 p = 0.0001 |
93.7; 85.5–102.7 p = 0.2412 |
227.2; 203.2–254.1 p = 0.0001 |
95.3; 82.8–109.8 p = 0.5749 |
147.1; 134.3–161.0 p = 0.0001 |
151.0; 128.7–177.2 p = 0.0001 |
104.9; 91.1–120.7 p = 0.5749 |
|
| Rabeprazole (n = 69) | ||||||||
| Fast | 35 | 971.9 ± 361.2 | 556.4 ± 176.2 | 3.7 ± 0.9 | 1.3 ± 0.5 | 0.60 ± 0.17 | 0.35 ± 0.11 | 0.60 ± 0.20 |
| Men | 18 | 836.3 ± 313.0 | 479.1 ± 139.7 | 3.6 ± 0.9 | 1.2 ± 0.5 | 0.55 ± 0.11 | 0.35 ± 0.13 | 0.64 ± 0.20 |
| Women | 17 | 1115.5 ± 361.4 | 638.3 ± 177.2 | 3.7 ± 0.9 | 1.4 ± 0.5 | 0.65 ± 0.20 | 0.35 ± 0.10 | 0.56 ± 0.20 |
| Fed | 34 | 1047.3 ± 382.3 | 675.8 ± 218.8 | 7.2 ± 2.6 | 2.2 ± 1.3 | 0.91 ± 0.45 | 0.34 ± 0.18 | 0.42 ± 0.22 |
| Men | 19 | 1045.8 ± 361.49 | 634.6 ± 144.8 | 6.9 ± 3.0 | 2.3 ± 1.3 | 0.91 ± 0.52 | 0.31 ± 0.18 | 0.38 ± 0.17 |
| Women | 15 | 1049.2 ± 420.3 | 727.9 ± 284.0 | 7.6 ± 2.0 | 2.0 ± 1.3 | 0.92 ± 0.37 | 0.38 ± 0.18 | 0.48 ± 0.27 |
|
Fed vs. Fast ratio; 90% CI; p value |
106.7; 91.3–124.8 p = 0.4886 |
121.3; 106.9–137.6 p = 0.0132 |
191.5; 172.2–212.9 p = 0.0001 |
153.1; 126.9–184.7 p = 0.0003 |
144.3; 125.6–165.9 p = 0.0001 |
93.1; 79.5–109.1 p = 0.4531 |
65.3; 54.1–78.8 p = 0.0003 |
|
| Omeprazole (n = 36) | ||||||||
| Fast | 35 | 2190.8 ± 2011.5 | 930.9 ± 434.6 | 2.0 ± 0.7 | 1.1 ± 0.6 | 0.64 ± 0.34 | 0.53 ± 0.38 | 0.76 ± 0.29 |
| Men | 17 | 2375.9 ± 2480.1 | 858.8 ± 432.6 | 2.1 ± 0.7 | 1.3 ± 0.8 | 0.65 ± 0.38 | 0.50 ± 0.44 | 0.70 ± 0.29 |
| Women | 18 | 2016.0 ± 1495.4 | 999.1 ± 437.7 | 1.9 ± 0.6 | 1.0 ± 0.4 | 0.63 ± 0.31 | 0.56 ± 0.34 | 0.82 ± 0.29 |
| Fed | 36# | 1928.3 ± 1878.5 | 682.6 ± 394.1 | 4.9 ± 1.1 | 1.3 ± 0.6 | 1.02 ± 1.07 | 0.64 ± 0.55 | 0.67 ± 0.32 |
| Men | 18 | 2135.8 ± 2282.7 | 725.0 ± 447.6 | 4.5 ± 0.9 | 1.3 ± 0.7 | 0.75 ± 0.52 | 0.57 ± 0.49 | 0.69 ± 0.35 |
| Women | 18 | 1720.9 ± 1402.0 | 640.2 ± 640.1 | 5.4 ± 1.0 | 1.3 ± 0.5 | 1.30 ± 1.38 | 0.73 ± 0.61 | 0.65 ± 0.30 |
|
Fed vs. Fast ratio; 90% CI; p value |
86.2; 81.2–91.6 p = 0.0002 |
63.0; 55.0–72.2 p = 0.0001 |
262.5; 232.6–296.2 p = 0.0001 |
117.6; 105.6–130.9 p = 0.0156 |
136.1; 105.6–130.9 p = 0.0029 |
116.1; 108.7–124.1 p = 0.0006 |
85.0; 76.4–94.7 p = 0.0156 |
|
#35 of the subjects participated in both fast and fed omeprazole clinical trials