Table 2.
Pharmacokinetic parameters in the NCG and GUG rat plasma (x ± s, ng/mL).
| Unit | NC | GU | |||||||
|---|---|---|---|---|---|---|---|---|---|
| IGLNC | IGMNC | IGHNC | IVNC | IGLGU | IGMGU | IGHGU | IVGU | ||
| AUC(0−t) | ng/mL min | 117,685.099 ± 10,645.941 | 328,401.369 ± 34,148.983** | 528,549.285 ± 28,947.109** | 471,026.157 ± 29,839.445 | 220,780.166 ± 27,359.641++ | 424,498.194 ± 33,398.016##++ | 1,180,876.811 ± 211,944.621++ | 890,543.171 ± 108,695.234++ |
| AUC(0−∞) | ng/mL min | 121,549.465 ± 9,918.633 | 340,315.089 ± 32,473.007** | 548,524.618 ± 32,867.392** | 484,516.748 ± 30,279.257 | 27,359.641 ± 7,709.965++ | 428,796.759 ± 33,699.626##++ | 1,333,781.847 ± 199,053.201#++ | 897,925.201 ± 105,998.307++ |
| Cmax | ng/mL | 326.523 ± 63.865 | 784.399 ± 83.091** | 1,229.112 ± 213.197** | 6,855.744 ± 1,257.845 | 474.16 ± 75.487++ | 923.821 ± 104.033##+ | 1545.947 ± 156.336##++ | 9,666.664 ± 1,040.381++ |
| Tmax | min | 180.00 ± 0.00 | 180.00 ± 0.00 | 180.00 ± 0.00 | 5.00 ± 0.00 | 180.000 ± 0.000 | 180.00 ± 0.00 | 200.00 ± 30.98 | 5.00 ± 0.00 |
| t1/2 | min | 453.56 ± 85.81 | 503.38 ± 90.60 | 565.90 ± 112.53 | 210.79 ± 39.33 | 682.36 ± 113.85++ | 716.65 ± 138.35++ | 776.248 ± 110.877++ | 428.73 ± 60.64++ |
| MRT(0−t) | min | 527.16 ± 94.18 | 540.44 ± 106.97 | 622.42 ± 116.77 | 198.66 ± 30.16 | 529.26 ± 96.54 | 578.16 ± 82.43 | 617.53 ± 124.23 | 345.25 ± 31.34++ |
| MRT(0−∞) | min | 644.16 ± 108.00 | 704.16 ± 129.20 | 723.12 ± 128.71 | 246.24 ± 38.43 | 677.07 ± 89.26 | 768.87 ± 118.66 | 872.38 ± 142.51 | 577.07 ± 39.26++ |
| VRT(0−t) | min2 | 313,685.843 ± 21,475.069 | 400,932.399 ± 27,411.201** | 528,911.098 ± 37,994.956** | 105,439.586 ± 8,439.535 | 289,338.053 ± 22,390.161 | 392,313.407 ± 35,441.114## | 530,205.293 ± 7,134.658## | 78,199.978 ± 6,343.701++ |
| VRT(0−∞) | min2 | 597,386.345 ± 88,064.757 | 787,738.057 ± 75,689.412** | 992,300.21 ± 153,863.791** | 159,320.463 ± 18,482.736 | 540,628.627 ± 75,457.035 | 783,486.638 ± 59,120.039## | 1,155,356.02 ± 106,135.933## | 128,837.383 ± 16,109.524++ |
| Vz | L/kg | 0.102 ± 0.015 | 0.117 ± 0.024 | 0.123 ± 0.021 | 0.039 ± 0.004 | 0.069 ± 0.012++ | 0.061 ± 0.008++ | 0.064 ± 0.003++ | 0.012 ± 0.006++ |
| Ka | 1/min | 0.014 ± 0.002 | 0.019 ± 0.002 | 0.022 ± 0.003 | – | 0.039 ± 0.006++ | 0.045 ± 0.005++ | 0.054 ± 0.006++ | – |
| K10 | 1/min | 0.012 ± 0.002 | 0.018 ± 0.003 | 0.024 ± 0.005 | 0.071 ± 0.012 | 0.007 ± 0.001++ | 0.012 ± 0.002++ | 0.015 ± 0.003++ | 0.016 ± 0.003++ |
| AUC(0−t)/AUC(0−∞) | 96.79 ± 2.27 | 96.45 ± 1.86 | 96.40 ± 2.22 | 97.21 ± 0.65 | 98.47 ± 0.477 | 99.00 ± 0.30 | 88.64 ± 8.63 | 99.15 ± 1.83 | |
| Fa | 70.51 ± 8.33 | 48.13 ± 4.90++ | |||||||
*P < 0.05; **P < 0.01, compared with 20 mg/kg in the NCG. #P < 0.05; ##P < 0.01, compared with 20 mg/kg in the GUG. +P < 0.05; ++P < 0.01, compared with the same dose and administration in the NCG.