Table 1 The main pharmacokinetic parameters after oral administration of 25, 50, and 100 mg/kg for MOIG, and 1650 mg/kg for MO or intravenous administration of 25 mg/kg MOIG in male rats (n = 3, mean ± SD)
Parameters | Component | po-MOIG-25 | po-MOIG-50 | po-MOIG-100 | po-MO-1650 | iv-MOIG-25 |
|---|---|---|---|---|---|---|
AUC0-t (μg·h/L) | MON | 832 ± 322 | 1505 ± 189 | 1777 ± 537 | 875 ± 182 | 21,501 ± 4877 |
DA | 2010 ± 545 | 3262 ± 423 | 3366 ± 753 | 2220 ± 820 | 10,239 ± 2044 | |
AUC0-∞ (μg·h/L) | MON | 872 ± 334 | 1585 ± 279 | 1812 ± 550 | 877 ± 182 | 21,500 ± 4859 |
DA | 2069 ± 557 | 3301 ± 411 | 3397 ± 748 | 2286 ± 773 | 10,239 ± 2044 | |
AUMC0-∞ (μg·h/L) | MON | 5121 ± 2698 | 8645 ± 5804 | 5011 ± 2132 | 3064 ± 882 | 15,255 ± 5098 |
DA | 14,739 ± 5191 | 17,844 ± 2090 | 15,476 ± 3663 | 12,867 ± 5938 | 8079 ± 2340 | |
MRT (h) | MON | 5.71 ± 1.96 | 5.17 ± 2.58 | 2.68 ± 0.40 | 3.47 ± 0.43 | 0.70 ± 0.09 |
DA | 7.03 ± 0.68 | 5.41 ± 0.24 | 4.58 ± 0.15 | 5.43 ± 0.94 | 0.78 ± 0.09 | |
t1/2 (h) | MON | 4.60 ± 1.41 | 7.11 ± 2.18 | 2.76 ± 1.84 | 3.00 ± 0.45 | 1.85 ± 1.67 |
DA | 4.80 ± 0.62 | 3.80 ± 1.01 | 3.76 ± 0.64 | 3.65 ± 1.16 | 2.90 ± 0.65 | |
Tmax (h) | MON | 1.00 ± 0.00 | 0.92 ± 0.14 | 0.92 ± 0.52 | 1.17 ± 0.29 | 0.03 ± 0.00 |
DA | 2.33 ± 0.76 | 2.00 ± 0.87 | 1.5 ± 0.00 | 2.17 ± 0.76 | 0.03 ± 0.00 | |
Vd (L/g) | MON | 0.20 ± 0.04 | 0.32 ± 0.04 | 0.22 ± 0.13 | 8.51 ± 2.61 | 0.004 ± 0.004 |
DA | 0.09 ± 0.04 | 0.08 ± 0.03 | 0.17 ± 0.06 | 3.90 ± 0.90 | 0.011 ± 0.004 | |
CL (L/g·h) | MON | 0.031 ± 0.010 | 0.032 ± 0.006 | 0.059 ± 0.020 | 1.932 ± 0.361 | 0.001 ± 0.000 |
DA | 0.013 ± 0.004 | 0.015 ± 0.002 | 0.030 ± 0.006 | 0.791 ± 0.310 | 0.003 ± 0.001 | |
Cmax (μg/L) | MON | 203 ± 34 | 451 ± 35 | 605 ± 114 | 265 ± 82 | 39,748 ± 3398 |
DA | 236 ± 54 | 624 ± 63 | 664 ± 89 | 379 ± 91 | 19,126 ± 1461 | |
F (%) | MON | 4.06 ± 1.55 | 3.69 ± 0.65 | 2.11 ± 0.64 | 2.04 ± 0.42 | – |
DA | 20.21 ± 5.44 | 16.12 ± 2.01 | 8.29 ± 1.83 | 11.16 ± 3.77 | – |