Dose | |||||||||||
Mouse type | IV | IP | Liver Cmax (MBq) | Liver Tmax (s) | Liver AUC (MBq⋅s) | Gallbladder/intestine Cmax (MBq) | Gallbladder emergence time (s) | Gallbladder/intestine AUC (MBq⋅s) | Blood AUC (MBq/mL⋅s) | T1/2, rapid-phase blood curve (s) | T1/2, slow-phase blood curve (s) |
WT | 19.17 ± 2.39 | 134 ± 41 | 6,507 ± 820 | 28.9 ± 1.00 | 147 ± 26 | 18,269 ± 4,349 | 1,411 ± 157 | 17 ± 2 | 332 ± 121 | ||
Slco1a/1b−/−/−/− | 3.44 ± 0.51 | 77.5 ± 23 | 1,926 ± 264 | NO | NO | NO | 6,771 ± 839 | 29 ± 7 | NO | ||
Abcc2−/− | 22.12 ± 1.71 | 212 ± 23 | 15,010 ± 1,382 | LI | 375 ± 63 | 3,916 ± 475 | 1,769 ± 212 | 18 ± 3 | 375 ± 63 | ||
Rifampicin-treated WT | 100 | 25 | 12.78 ± 3.00 | 747 ± 37 | 10,048 ± 2,355 | LI | 555 ± 65 | 1,639 ± 776 | 6,411 ± 544 | 40 ± 4 | 853 ± 273 |
50 | 12.5 | 16.32 ± 0.76 | 442 ± 65 | 11,297 ± 436 | LI | 385 ± 31 | 3,736 ± 858 | NI | NI | NI | |
37.5 | 9.37 | 14.50 ± 0.71 | 300 ± 47 | 9,700 ± 1,655 | LI | 457 ± 53 | 6,742 ± 3,201 | NI | NI | NI | |
25 | 6.25 | 17.13 ± 0.40 | 235 ± 26 | 9,686 ± 606 | LI | 240 ± 15 | 9,372 ± 411 | NI | NI | NI | |
12.5 | 3.12 | 16.40 ± 0.42 | 157 ± 12 | 6,282 ± 846 | LI | 240 ± 42 | 13,300 ± 2,149 | NI | NI | NI | |
Vehicle control (n = 3) | 18.69 ± 3.82 | 145 ± 31 | 6,120 ± 124 | 29.16 ± 0.51 | 140 ± 20 | 17,752 ± 688 | 1514 ± 140 | 15 ± 2 | 300 ± 21 |
IV = intravenous; IP = intraperitoneal; NO = not observable; LI = linear increase (no Cmax); NI = not investigated.
Data are mean (n = 3) ± SD.