Table 3.
Mean 2-hydroxybenzylamine pharmacokinetic parameters after oral doses
| Parameter | 2-Hydroxybenzylamine acetate dose | |||
|---|---|---|---|---|
| 500 mg (n = 6) | 750 mg (n = 5–6) | |||
| Day 1 (first dose) | Day 15 (last dose) | Day 1 (first dose) | Day 15 (last dose) | |
| Ke | 0.28 ± 0.04 | 0.22 ± 0.05 | 0.34 ± 0.06 | 0.22 ± 0.01 |
| Half-life (h) | 2.53 ± 0.39 | 3.27 ± 0.61 | 2.10 ± 0.45 | 3.12 ± 0.08 |
| Vd/F | 162 ± 21 | 183 ± 58 | 225 ± 79 | 264 ± 85 |
| Cl/F | 44.9 ± 6.3 | 38.2 ± 6.7 | 73.9 ± 18.5 | 58.9 ± 19.9 |
| Tmax (h) | 1.17 ± 0.68 | 0.83 ± 0.61 | 1.75 ± 1.25 | 2.00 ± 1.22 |
| Cmax (ng/mL) | 1955 ± 422 | 3177 ± 1993 | 1916 ± 524 | 2292 ± 913 |
| Cavg (ng/mL) | 817 ± 88 | 1133 ± 225 | 798 ± 193 | 1190 ± 455 |
| Cmin (ng/mL) | 285 ± 113 | 324 ± 50 | 261 ± 133 | 484 ± 287 |
| PTF (%) | 207 ± 67 | 237 ± 110 | 215 ± 87 | 158 ± 58 |
| AUC0–8h (h·ng/mL) | 6536 ± 701 | 9063 ± 1796 | 6385 ± 1547 | 9523 ± 3638 |
| AUCinf (h·ng/mL) | 7620 ± 1230 | 10,605 ± 1740 | 7186 ± 1780 | 11,746 ± 4602 |
| Accumulation Index | 1.38 ± 0.15 | 1.52 ± 0.27 | ||
Ke, elimination rate constant; Vd/F, apparent volume of distribution; Cl/F, apparent clearance; Tmax, time to reach maximum plasma concentration; Cmax, maximum observed plasma concentration; Cavg, average observed plasma concentration; Cmin, minimum observed plasma concentration; PTF, peak-to-trough fluctuation; AUC0–8, area under the dosing interval curve; AUCinf, area under the concentration-time curve from zero to infinity.