TABLE 3.
Pharmacokinetic parameters of total vutiglabridin after single and multiple administrations
| Dose groups | N | Tmax (Tmax,ss) (h) | Cmax (Cmax,ss) (μg/L) | AUClast (AUCtau) (h∙μg/L) | AUCinf (h∙μg/L) | t 1/2 (h) | CL/F (L/h) | Vd/F (L) | PTF (%) | Accumulation ratio |
|---|---|---|---|---|---|---|---|---|---|---|
| Single ascending dose study | ||||||||||
| 30 mg | 8 |
2.50 [2.00–4.02] |
119 ± 40.9 | 1220 ± 485 | 1710 ± 670 | 72.6 ± 9.33 | 20.1 ± 7.60 | 2100 ± 769 | ‐ | ‐ |
| 60 mg | 8 |
2.00 [1.00–5.00] |
181 ± 47.9 | 1680 ± 292 | 2280 ± 348 | 77.6 ± 40.0 | 26.8 ± 3.91 | 2880 ± 1130 | ‐ | ‐ |
| 120 mg | 8 |
1.50 [1.00–4.00] |
295 ± 98.0 | 3220 ± 723 | 3670 ± 965 | 77.7 ± 26.4 | 34.5 ± 8.18 | 3690 ± 1100 | ‐ | ‐ |
| 240 mg (fasted) | 7 |
2.00 [1.00–2.00] |
579 ± 263 | 5700 ± 2190 | 6320 ± 2490 | 71.5 ± 16.8 | 41.5 ± 10.5 | 4310 ± 1740 | ‐ | ‐ |
| 240 mg (fed) | 7 |
3.00 [2.00–4.00] |
1680 ± 650 | 13,900 ± 4090 | 15,900 ± 4810 | 87.6 ± 16.6 | 16.1 ± 4.01 | 2020 ± 559 | ‐ | ‐ |
| 480 mg | 8 |
2.00 [1.00–3.00] |
763 ± 142 | 9360 ± 1960 | 10,600 ± 2350 | 79.3 ± 23.4 | 47.2 ± 10.2 | 5370 ± 1840 | ‐ | ‐ |
| 720 mg | 8 |
2.00 [1.00–4.00] |
1030 ± 414 | 13,700 ± 4380 | 16,300 ± 6380 | 85.4 ± 25.7 | 49.1 ± 15.3 | 5730 ± 1730 | ‐ | ‐ |
| Multiple ascending dose study | ||||||||||
| Korean subjects 240 mg | 8 |
2.01 [1.00–4.00] |
624 ± 93.6 | 6540 ± 1460 | ‐ | 107 ± 37.6 | 38.7 ± 10.8 | 5840 ± 2020 | 169 ± 30.3 | 2.20 ± 0.40 |
| Korean subjects 480 mg | 7 |
2.00 [1.00–4.00] |
1110 ± 240 | 11,700 ± 2270 | ‐ | 113 ± 33.7 | 42.5 ± 8.64 | 7080 ± 2960 | 167 ± 61.8 | 2.70 ± 0.89 |
| White subjects 480 mg | 8 |
1.50 [1.00–4.00] |
923 ± 195 | 8320 ± 2610 | ‐ | 72.8 ± 22.9 | 61.8 ± 15.9 | 6120 ± 1010 | 213 ± 66.4 | 2.76 ± 0.85 |
Note: Data are shown as the mean ± standard deviation except for Tmax, which is shown as the median [minimum – maximum].
Abbreviations: AUCinf: area under the plasma concentration‐time curve from 0 h to infinity; AUClast, area under the plasma concentration‐time curve from 0 h to the last measurable time point; AUCtau, area under the plasma concentration‐time curve for a dosing interval at steady state; CL/F, apparent clearance; Cmax, maximal plasma concentration; Cmax,ss, maximal plasma concentration at steady state; PTF, peak trough fluctuation; t 1/2, elimination half‐life after a single dose; Tmax, time for the maximal plasma concentration; Tmax,ss, time for the maximal plasma concentration at steady state; Vd/F, apparent volume of distribution.