Physicochemical property and pharmacokinetic parameters
Values are the mean ± S.E.M.
| Parameters | RUT | EOD | DHED |
|---|---|---|---|
| LogP | 2.40 | 2.34 | −2.30 |
| pKa | 3.43 | 4.29 | — |
| Pe (cm/s) (pH = 7.4) | 2.10 × 10−4 | 2.06 × 10−4 | 2.00 × 10−7 |
| Intrinsic solubility (mg/ml) (pH = 7.4) | 0.02 | 0.01 | 0.14 |
| TPSA (Ǻ2) | 48.5 | 39.3 | 39.1 |
| T1/2 (minutes) | 56.4 ± 4.23 | 69.3 ± 0.1 | 64.0 ± 3.45 |
| Tmax (minutes) | 54.0 ± 3.66 | 66.0 ± 5.74 | 60.0 ± 0.1 |
| Cmax (μg/ml) | 0.80 ± 0.54*** | 0.34 ± 0.22### | 12.8 ± 2.39 |
| AUC0∼t (μg/ml ·min) | 80.2 ± 4.89*** | 151 ± 5.78### | 3450 ± 34.6 |
| AUC0∼∞ (μg/ml ·min) | 83.4 ± 4.64*** | 186 ± 6.02### | 4760 ± 36.1 |
Pe, permeability; TPSA, topological polar surface area.
↵*** P < 0.001, RUT group vs. DHED group; ###P < 0.001, EOD group vs. DHED group.