Table 4 Pharmacokinetic parameters of AZD5305 after IV injection and oral gavage administration
Parameters | Dose | ||
|---|---|---|---|
0.1 mg/kg | 0.3 mg/kg | 1 mg/kg | |
a Intravenous bolus injection to ICR mice | |||
Tmax (h) | 0.0500 ± 0.000 | 0.0500 ± 0.000 | 0.0500 ± 0.000 |
Cmax (μg/mL) | 1.11 ± 0.133 | 3.42 ± 0.580 | 9.88 ± 1.44 |
t1/2 (h) | 5.97 ± 0.589 | 5.86 ± 0.873 | 5.99 ± 0.459 |
AUClast (μg∙h/mL) | 5.30 ± 0.502 | 19.2 ± 2.12 | 62.1 ± 3.46 |
AUCinf (μg∙h/mL) | 5.63 ± 0.615 | 20.4 ± 2.60 | 66.0 ± 3.23 |
MRT (h) | 7.60 ± 0.820 | 7.60 ± 1.10 | 7.63 ± 0.522 |
CL (mL/h/kg) | 17.9 ± 1.94 | 15.5 ± 1.65 | 15.2 ± 0.724 |
Vss (mL/kg) | 135 ± 6.89 | 117 ± 10.3 | 116 ± 11.1 |
Parameters | Dose | |||
|---|---|---|---|---|
0.1 mg/kg | 0.3 mg/kg | 1 mg/kg | 3 mg/kg | |
b Oral gavage administration to ICR mice | ||||
Tmax (h) | 0.300 ± 0.112 | 0.250 ± 0.000 | 0.250 ± 0.000 | 0.250 ± 0.000 |
Cmax (μg/mL) | 0.555 ± 0.166 | 2.42 ± 0.287 | 8.46 ± 0.867 | 26.9 ± 2.38 |
t1/2 (h) | 7.67 ± 1.50 | 6.85 ± 0.920 | 7.32 ± 1.11 | 6.37 ± 0.695 |
AUClast (µg∙h/mL) | 5.25 ± 0.981 | 17.6 ± 1.46 | 64.7 ± 6.95 | 179 ± 15.7 |
AUCinf (µg∙h/mL) | 5.89 ± 1.02 | 19.3 ± 2.03 | 71.9 ± 9.76 | 193 ± 16.8 |
MRT (h) | 10.1 ± 2.22 | 8.82 ± 1.17 | 9.48 ± 1.55 | 8.23 ± 0.692 |
F (%) | 105 ± 18.0 | 94.8 ± 9.96 | .109 ± 14.8 | 97.4 ± 8.48 |