Table 6.
Pharmacokinetics parameters of bufalin and its metabolites after a single oral administration of 10 mg/kg bufalin to rats (n = 3, mean ± SD).
| Parameters |
Cmax (ng/mL) |
Tmax (h) |
t1/2 (h) |
AUC0-t (ug/L∗h) |
MRT0-t (h) |
|---|---|---|---|---|---|
| Bufalin | 14.722 ± 4.681 | 0.25 ± 0.00 | 5.70 ± 3.06 | 37.31 ± 9.54 | 3.23 ± 0.37 |
| 3-epi-bufalin | 963.06 ± 284.76 | 0.42 ± 0.14 | 7.74 ± 3.87 | 2214.18 ± 460.31 | 3.21 ± 0.24 |
| Hydroxylated bufalin (RT = 1.29 min) | 57.37 ± 13.41 | 0.58 ± 0.14 | 2.23 ± 0.36 | 144.78 ± 23.41 | 2.41 ± 0.07 |
| Hydroxylated bufalin (RT = 1.63 min) | 13.90 ± 4.64 | 0.58 ± 0.14 | 1.90 ± 0.37 | 34.45 ± 8.82 | 2.41 ± 0.20 |
| Hydroxylated bufalin (RT = 2.02 min) | 299.56 ± 112.89 | 0.50 ± 0.00 | 3.13 ± 1.50 | 643.98 ± 173.93 | 2.46 ± 0.17 |
| Hydroxylated bufalin (RT = 3.42 min) | 107.36 ± 44.57 | 0.50 ± 0.00 | 2.32 ± 0.71 | 238.03 ± 64.08 | 2.30 ± 0.15 |
| Hydroxylated bufalin (RT = 3.81 min) | 15.28 ± 3.86 | 2.67 ±1.16 | 12.39 ± 9.22 | 83.59 ± 13.61 | 4.06 ± 0.17 |
| Dihydroxylated bufalin (RT = 0.84 min) | 6.14 ± 1.72 | 0.83 ± 0.29 | 2.49 ± 1.05 | 18.80 ± 2.74 | 2.84 ± 0.16 |
| Dihydroxylated bufalin (RT = 1.59 min) | 14.68 ± 6.52 | 1.67 ± 0.58 | 5.81 ± 3.68 | 72.20 ± 22.72 | 3.66 ± 0.14 |
| Dihydroxylated bufalin (RT = 2.68 min) | 3.25 ± 1.68 | 1.17 ± 0.76 | 2.03 ± 0.67 | 11.74 ± 5.11 | 2.91 ± 0.11 |