Table 2.
Observed and simulated mean plasma PK parameters of buagafuran.
| Species | Oral dosing |
Tmax (h) |
Cmax (ng/mL) |
MRT(0-∞) (h) |
AUC0-t (ng⋅h/mL) |
AUC0-∞ (ng⋅h/mL) |
|||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Observed | Simulated | Observed | Simulated | Observed | Simulated | Observed | Simulated | Observed | Simulated | ||
| Rat | 4 mg/kg | 0.25 | 0.28 | 5.31 | 5.06 | 3.54 | 1.68 | 6.69 | 6.14 | 11.43 | 7.44 |
| 8 mg/kg | 0.25 | 0.28 | 10.64 | 10.13 | 1.21 | 1.68 | 14.15 | 12.28 | 15.06 | 14.87 | |
| Human | Single dosing/30 mg | 1.00 | 1.12 | 19.47 | 19.73 | 3.33 | 8.43 | 47.62 | 50.13 | 54.91 | 55.79 |
| Single dosing/60 mg | 1.00 | 1.12 | 39.77 | 39.55 | 4.87 | 8.42 | 92.40 | 100.24 | 95.38 | 111.54 | |
| Single dosing/120 mg | 1.00 | 1.20 | 81.64 | 76.20 | 5.28 | 8.50 | 246.48 | 200.43 | 271.68 | 222.99 | |
| Multiple dosing/first dosing | 2.00 | 1.20 | 27.08 | 31.59 | 9.94 | 7.15 | 99.40 | 104.19 | 113.48 | 111.65 | |
| Multiple dosing/last dosing | 3.00 | 1.20 | 32.00 | 32.58 | 20.89 | 13.58 | 163.30 | 124.56 | 230.74 | 152.98 | |
Observed PK parameters were calculated from plasma drug concentration-time profiles by WinNonlin v6.0 (Pharsight Corporation, Mountain View, CA, United States), while simulated ones were performed using GastroPlusTM software, version 8.5 (Simulations Plus, Inc., Lancaster, CA, United States).