Table 1.
Summary of pharmacokinetic parameters of tegoprazan and M1 after a single oral administration of tegoprazan 50 mg in the fasted state, at 30 min before a high‐fat meal or at 30 min after a high‐fat meal
|
Fasted (N = 12) |
30 min before meal (N = 12) |
30 min after meal (N = 12) |
|||
|---|---|---|---|---|---|
| Parameter a | Parameter a |
GMR b (90% CI) |
Parameter a |
GMR c (90% CI) |
|
| Tegoprazan | |||||
| Cmax, μg/L |
803.00 ± 156.23 [580.00–1698.10] |
775.92 ± 162.61 [522.00–1010.00] |
0.9631 (0.7517–1.2340) |
492.00 ± 293.94 [173.00–1250.00] |
0.5396 (0.4211–0.6914) |
| AUClast, h∙μg/L |
2837.32 ± 1054.64 [1618.61–5095.97] |
2669.82 ± 1022.94 [1424.13–4788.40] |
0.9388 (0.8674–1.0160) |
3017.05 ± 1193.95 [2915.98–5190.38] |
1.0455 (0.9661–1.1316) |
| AUCinf, h∙μg/L |
3137.75 ± 1166.15 [1702.07–5657.24] |
2917.65 ± 1084.47 [1521.26–5162.56] |
3321.58 ± 1219.48 [1784.05–5620.45] |
||
| Tmax, h | 1.00 [0.50–2.00] | 0.48 [0.48–1.00] | 3.00 [0.50–8.00] | ||
| t1/2, h |
4.10 ± 1.38 [2.78–7.47] |
4.16 ± 1.06 [3.02–6.10] |
5.00 ± 1.55 [3.00–8.02] |
||
| M1 | |||||
| Cmax, μg/L |
198.83 ± 58.26 [122.00–359.00] |
146.42 ± 19.41 [122.00–187.00] |
0.7551 (0.6609–0.8627) |
142.16 ± 30.21 [78.90–181.00] |
0.7214 (0.6314–0.8242) |
| AUClast, h∙μg/L |
4461.94 ± 1008.27 [2061.41–5908.94] |
3497.93 ± 951.53 [1685.18–4614.80] |
0.7743 (0.7176–0.8355) |
3796.57 ± 915.63 [1429.14–4902.04] |
0.8432 (0.7815–0.9099) |
| AUCinf, h∙μg/L |
5133.81 ± 1207.21 [2939.16–7726.26] |
4178.02 ± 1055.77 [2633.51–6116.44] |
5324.01 ± 2138.92 [3595.68–11,648.14] |
||
| Tmax, h | 8.00 [3.83–8.00] | 8.00 [6.00–8.02] | 8.00 [6.00–24.00] | ||
| t1/2, h |
15.36 ± 3.28 [11.95–23.86] |
15.75 ± 3.37 [11.49–24.26] |
24.82 ± 26.25 [12.74–107.65] |
||
| MR d |
1.74 ± 0.44 [1.20–2.79] |
1.51 ± 0.35 [1.11–2.31] |
1.90 ± 1.51 [1.00–6.53] |
||
Abbreviations: AUCinf, area under the concentration–time curve from time zero to infinity; AUClast, area under the concentration–time curve from time zero to the last quantifiable time point; CI, confidence interval; Cmax, maximum plasma concentration; GMR, geometric mean ratio; M1, active metabolite of tegoprazan; MR, metabolic ratio; Tmax, the time to reach maximum plasma concentration; t1/2, terminal elimination half‐life.
All parameters are expressed as mean ± SD [range], except Tmax, which is expressed as median [range].
GMR indicates 30 min before a high‐fat meal/fasted.
GMR indicates 30 min after a high‐fat meal/fasted.
MR represents metabolic ratio of tegoprazan (AUCinf, M1/AUCinf, Tegoprazan).