Table 2.
PHARMACOKINETIC PARAMETERS |
FLBZ |
R-FLBZ |
||||
---|---|---|---|---|---|---|
FLBZ-CDs(1)i.r. treatment | FLBZ-CMC(1)i.r. treatment | FLBZ-CDs(2)i.a. treatment | FLBZ-CDs(1)i.r. treatment | FLBZ-CMC(1)i.r. treatment | FLBZ-CDs(2)i.a. treatment | |
T½abs/for (h) |
3.67 ± 1.57 |
2.92 ± 0.94 |
0.40 ± 1.43* |
3.00 ±1.21 |
4.95 ± 1.72 |
0.90 ± 0.30* |
Cmax (μg/mL) |
0.05 ± 0.01 |
0.03 ± 0.01 |
0.07 ± 0.04* |
0.23 ± 0.04 |
0.14 ± 0.03* |
0.35 ± 0.09* |
Tmax (h) |
12.0 ± 3.79 |
12.5 ± 2.95 |
2.75 ± 2.36* |
10.5 ± 4.93 |
11.5 ± 1.22 |
2.75 ± 1.50* |
AUC0-t (μg.h/mL) |
1.35 ± 0.34 |
0.78 ± 0.53 |
0.65 ± 0.29 |
6.82 ± 1.77 |
4.92 ± 1.46 |
3.83 ± 1.86* |
T½el (h) |
25.8 ± 14.0 |
19.2 ± 15.1 |
15.1 ± 8.27* |
17.0 ± 5.19 |
18.4 ± 3.74 |
6.73 ± 3.70* |
MRT (h) | 41.6 ± 19.0 | 34.5 ± 20.3 | 19.7 ± 9.73* | 28.8 ± 8.58 | 35.4 ± 3.90 | 10.8 ± 4.07* |
The pharmacokinetic parameters obtained after the intra-abomasal (i.a.) administration of FLBZ (3.8 mg/kg, n = 4) formulated as a cyclodextrin-based solution (FLBZ-CDs), is also shown (Experiment 2). T½abs/for: FLBZ absorption or metabolite formation half life; Cmax: peak plasma concentration; Tmax: time to the Cmax; AUC0-t: Area under the plasma concentration vs. time curve from 0 to the detection time; T½el: elimination half-life; MRT: mean residence time (obtained by non-compartmental analysis of the data). *Significantly different from the FLBZ-CDs i.r. treated group at P < 0.05.
1Experiment 1: crossover design (n = 6) sheep were treated with the HPβCD-FLBZ solution (FLBZ-CDs) or the CMC-FLBZ suspension (FLBZ-CMC) by the i.r. route at the same dose rate (3.8 mg/kg).
2Experiment 2: intraabomasal (i.a.) administration of the FLBZ-CDs solution (3.8 mg/kg, n = 4).