Table 3. Pharmacokinetic parameters of YH4808 after single and multiple oral administrations.
| Day | PK parameters | Treatment | ||
|---|---|---|---|---|
| 100 BID (n = 10) | 200 QD (n = 10) | 200 BID (n = 10) | ||
| Day 1 | Tmax (h) | 4.00 (1.50–8.00) | 4.00 (2.00–6.00) | 3.50 (2.00–6.00) |
| Cmax (µg/L) | 43.80 ± 23.93 | 114.38 ± 54.20 | 107.62 ± 69.67 | |
| Cmax/D (µg/L/mg) | 0.44 ± 0.24 | 0.57 ± 0.30 | 0.54 ± 0.35 | |
| AUCτ (µg·h/L) | 159.86 ± 64.92 | 472.35 ± 210.50 | 332.64 ± 178.46 | |
| AUCτ/D (µg·h/L/mg) | 1.60 ± 0.65 | 2.36 ± 1.05 | 1.66 ± 0.89 | |
| Day 14 | Tmax,ss (h) | 4.00 (1.50–8.00) | 5.00 (2.00–8.00) | 4.00 (2.00–11.97) |
| Cmax,ss (µg/L) | 71.94 ± 21.03 | 121.44 ± 66.68 | 103.18 ± 54.84 | |
| Cmax,ss/D (µg/L/mg) | 0.72 ± 0.21 | 0.61 ± 0.33 | 0.52 ± 0.27 | |
| AUCτ,ss (µg·h/L) | 301.58 ± 81.34 | 658.04 ± 256.81 | 518.35 ± 217.60 | |
| AUCτ,ss/D (µg·h/L/mg) | 3.02 ± 0.81 | 3.29 ± 1.28 | 2.59 ± 1.09 | |
| Ctrough,ss (µg/L) | 13.24 ± 5.61 | 11.79 ± 4.36 | 26.25 ± 13.95 | |
| CLss/F (L/h) | 358.04 ± 110.78 | 349.98 ± 138.53 | 450.72 ± 183.28 | |
| Fluctuation | 2.46 ± 0.57 | 4.04 ± 1.40 | 3.83 ± 1.68 | |
| R | 2.03 ± 0.68 | 1.48 ± 0.40 | 1.83 ± 0.84 | |
Data are presented as mean ± standard deviation except for Tmax shown as median (main-max).
PK, pharmacokinetic; Tmax, the time to reach maximum plasma concentration; Cmax, the maximum plasma concentration; D, dose; AUCτ, the area under the time-concentration curve within a dosing interval; Tmax,ss, the time to reach maximum plasma concentration at the steady-state; Cmax,ss, the maximum plasma concentration at the steady-state; AUCτ,ss, the area under the time-concentration curve within a dosing interval; Ctrough,ss, trough plasma concentration at the steady-state; CLss, total clearance of the drug from the plasma at the steady-state; F, bioavailability of drug; Fluctuation, (Cmax,ss-Ctrough,ss)/Cavg,ss; R, accumulation index.