TABLE 3.
Pharmacokinetic parameters and bioavailability of ASD in rats after intravenous and intragastrical administration (n = 5).
Parameter | Administration | Parameter value (Mean ± SD) | |||||
---|---|---|---|---|---|---|---|
IV, 10 mg/kg NS | PO, 100 mg/kg NS | PO, 100 mg/kg + Vegetable oil | PO, 100 mg/kg + Metronidazole | PO, 100 mg/kg + Verapamil | PO, 100 mg/kg + Urea | ||
t1/2 | (h) | 2.54 ± 1.60 | 2.27 ± 0.60 | 3.01 ± 2.04 | 4.79 ± 0.79 | 2.00 ± 0.85 | 1.58 ± 0.23 |
Tmax | (h) | 0.03 ± 0.00 | 0.25 ± 0.00 | 0.44 ± 0.49 | 0.33 ± 0.14 | 0.83 ± 1.01 | 0.42 ± 0.14 |
Cmax | (μg/ml) | 59.40 ± 33.54 | 0.039 ± 0.027 | 0.34 ± 0.48 | 0.18 ± 0.21 | 0.036 ± 0.044 | 0.092 ± 0.017* |
Vz | (L/kg) | 2.35 ± 1.90 | 8,099 ± 4,870 | 3,214 ± 2,612 | 11,061 ± 13,466 | 6,220 ± 4,274 | 1,037 ± 133 |
Cl | (L/h/kg) | 0.63 ± 0.37 | 2,376 ± 1,014 | 709 ± 547 | 1,428 ± 1,594 | 2,376 ± 1,381 | 461 ± 91 |
MRT(0-t) | (h) | 0.50 ± 0.06 | 1.90 ± 0.11 | 1.97 ± 0.61 | 2.33 ± 1.86 | 2.14 ± 0.27 | 2.14 ± 0.40 |
AUC(0-t) | (h*μg/ml) | 19.05 ± 8.64 | 0.047 ± 0.030 | 0.27 ± 0.30 | 0.18 ± 0.20 | 0.058 ± 0.047 | 0.22 ± 0.043* |
AUC(0-∞) | (h*μg/ml) | 19.06 ± 8.65 | 0.050 ± 0.028 | 0.28 ± 0.30 | 0.19 ± 0.20 | 0.063 ± 0.054 | 0.22 ± 0.044* |
F | % | / | 0.025 | 0.14 | 0.094 | 0.030 | 0.12 |
NC: Not calculated; t1/2: Terminal half-life; Cmax: Peak plasma concentration; Tmax: Time of Cmax; Vz: The apparent volume of distribution; Cl: Clearance; MRT: Mean Residue Time; AUC: Area under the curve.*p < 0.05 vs. PO 100 mg/kg NS group.