Table 1.
Species | Dose a (mg kg-1 or mg) |
The route of adminstration |
t1/2 (h) |
Tmax (h) |
Cmax
b (ng ml-1 or μg ml-1) |
AUC0-t
c (h·ng ml-1 or h μg ml-1) |
AUC0-∞c (h·ng ml-1 or h μg ml-1) |
Vd (L/kg) |
CL (L/h/kg) |
MRT0-t (h) |
MRT0-∞ (h) |
---|---|---|---|---|---|---|---|---|---|---|---|
Rat | |||||||||||
10.5 | p.o. | 0.328 ± 0.275 | 1.50 ± 2.35 | 31.7 ± 13.2 | 32.7 ± 27.7 | 35.7 ± 29.3 | 174 ± 98.3 | 624 ± 589 | 0.741 ± 0.423 | 1.22 ± 0.297 | |
21 | p.o. | 0.500 ± 0.493 | 1.53 ± 2.36 | 30.5 ± 16.3 | 34.2 ± 20.3 | 38.4 ± 21.4 | 322 ± 239 | 759 ± 753 | 1.18 ± 0.399 | 1.42 ± 0.621 | |
42 | p.o. | 0.463 ± 0.598 | 1.18 ± 1.78 | 52.6 ± 78.8 | 40.7 ± 51.3 | 45.1 ± 55.4 | 586 ± 394 | 1,410 ± 1,110 | 1.10 ± 0.381 | 1.24 ± 0.292 | |
168 | p.o. | 0.738 ± 0.781 | 2.85 ± 4.06 | 104 ± 77.5 | 140 ± 66.3 | 145 ± 66.4 | 639 ± 657 | 810 ± 417 | 2.01 ± 0.451 | 1.96 ± 1.08 | |
42 | i.v. | 1.62 ± 1.18 | 0.030 ± 0.000 | 88.5 ± 51.0 | 18.1 ± 7.58 | 18.1 ± 7.55 | 8.29 ± 10.0 | 2.90 ± 1.66 | 0.496 ± 0.382 | 0.570 ± 0.476 | |
Dog | |||||||||||
3.1 | p.o. | 1.84 ± 1.46 | 1.33 ± 0.258 | 39.9 ± 10.4 | 108 ± 58.8 | 129 ± 78.2 | 61.2 ± 23.0 | 31.2 ± 15.4 | 2.50 ± 1.05 | 3.38 ± 1.88 | |
12.4 | p.o. | 1.31 ± 0.581 | 1.00 ± 0.316 | 70.2 ± 16.9 | 124 ± 32.2 | 135 ± 35.5 | 171 ± 59.4 | 98.0 ± 27.2 | 1.77 ± 0.371 | 2.17 ± 0.633 | |
49.6 | p.o. | 1.31 ± 0.293 | 1.00 ± 0.447 | 107 ± 78.2 | 211 ± 92.1 | 224 ± 104 | 482 ± 173 | 267 ± 127 | 2.46 ± 1.11 | 2.73 ± 1.02 | |
12.4 | i.v. | 1.37 ± 0.347 | 0.080 ± 0.000 | 5.80 ± 0.946 | 2.92 ± 0.406 | 2.93 ± 0.403 | 8.69 ± 3.35 | 4.31 ± 0.604 | 0.703 ± 0.153 | 0.727 ± 0.143 | |
Human | |||||||||||
40 | p.o. | 2.48 ± 1.64 | 1.97 ± 1.11 | 2.24 ± 0.670 | 7.61 ± 3.50 | 9.99 ± 4.22 | 275 ± 167 | 67.0 ± 36.3 | 2.66 ± 0.443 | 4.90 ± 1.69 | |
80 | p.o. | 1.90 ± 1.22 | 2.09 ± 1.39 | 2.94 ± 1.17 | 9.27 ± 3.37 | 12.2 ± 3.19 | 295 ± 117 | 103 ± 49.9 | 2.80 ± 0.543 | 3.83 ± 1.69 | |
160 | p.o. | 3.64 ± 3.01 | 2.50 ± 1.41 | 4.29 ± 2.63 | 15.7 ± 7.51 | 22.4 ± 9.36 | 725 ± 568 | 144 ± 61.6 | 3.30 ± 1.12 | 6.54 ± 4.41 | |
160 (high- fat diet) d |
p.o. | 3.11 ± 1.95 | 2.66 ± 1.87 | 3.04 ± 1.15 | 12.8 ± 4.74 | 18.2 ± 5.81 | 755 ± 509 | 172 ± 64.3 | 3.45 ± 1.22 | 6.19 ± 2.77 | |
320 | p.o. | 2.51 ± 1.58 | 1.66 ± 0.990 | 10.9 ± 12.4 | 37.5 ± 32.2 | 39.8 ± 32.2 | 677 ± 505 | 202 ± 131 | 3.17 ± 0.677 | 4.01 ± 1.05 | |
480 | p.o. | 2.01 ± 0.498 | 1.66 ± 0.834 | 5.69 ± 2.80 | 19.4 ± 7.86 | 21.2 ± 7.95 | 1,360 ± 992 | 477 ± 372 | 3.08 ± 0.704 | 3.86 ± 0.779 |
The unit was mg kg-1 for rat and dog, and mg for human.
The unit was μg ml-1 for i.v. administration groups, and ng ml-1 for p.o. administration groups.
The unit was h μg ml-1 for i.v. administration groups, and h ng ml-1 for p.o. administration groups.
Compared to 160 mg group, the acceptable level of significance was established at P < 0.05*.