Parameters |
C1
(1.28 mg/kg) |
C1a
(1.65 mg/kg) |
C2
(0.98 mg/kg) |
C2a
(1.10 mg/kg) |
Total
(5.00 mg/kg) |
t1/2(h) |
1.54 ± 0.86a |
2.37 ± 0.65a,b |
3.32 ± 0.59b |
3.54 ± 0.45b |
2.21 ± 0.27a,b |
MRT (h) |
2.35 ± 0.56a |
3.26 ± 0.48a,b |
3.81 ± 0.35b |
4.09 ± 0.32b |
2.71 ± 0.20a,b |
Vdarea/F (ml/kg) |
217.89a ± 0.77 |
785.25b ± 0.50 |
586.99b,c ± 0.24 |
603.05b,c ± 0.35 |
443.63c ± 0.40 |
CLB/F (ml/hr/kg) |
98.20a ± 0.48 |
229.29b ± 0.34 |
122.49a ± 0.53 |
118.04a ± 0.36 |
139.07a ± 0.34 |
AUC0-∞/Dose (mg.h.kg/ml/mg) |
10.18 ± 0.48a |
4.36 ± 0.34b |
8.16 ± 0.53a |
8.47 ± 0.36a |
7.20 ± 0.34a |
Extrapolated AUC (%) |
11 ± 0.84 |
18 ± 0.44 |
15 ± 0.64 |
18 ± 0.56 |
3 ± 0.39 |
Bioavailability (%) |
81 ± 0.66a |
35 ± 0.65b |
92 ± 0.52a |
70 ± 0.43a |
69 ± 0.29a |
Cmax/Dose Median
(25th-75th percentile)
(µg/mL) |
4.74a (4.01-7.06) |
1.79b (1.35-1.87) |
2.81a (1.91-3.27) |
2.78a (2.08-3.80) |
2.85a (2.70-3.62) |
Tmax Median (25th-75th percentile)
(h) |
0.50
(0.50-1.00) |
1.00
(0.50-1.00) |
0.75
(0.50-1.00) |
0.50
(0.50-1.00) |
0.50
(0.50-1.00) |
a,bDifferent superscripts indicate statistically significant differences |