Table 1.
Non-compartmental pharmacokinetic parameters of injection site, plasma, popliteal lymph nodes (PLNs), iliac lymph nodes (ILNs) and renal lymph nodes (RLNs) in the SN-38-Lips group and SN-38-Lips group combined with S-BO in the concentrations of 1, 2 and 5 mg/mL following s.c. administration at the dosing of 4 mg/kg (mean ± SD, n = 6).
SN-38-Lips | SN-38-Lips+ | SN-38-Lips+ | SN-38-Lips+ | ||
---|---|---|---|---|---|
1-S-BO | 2-S-BO | 5-S-BO | |||
Injection site |
|||||
AUC0–24 h | mg/kg·h | 8235.673 | 6290.983 | 5496.435 | 5657.746 |
AUC0–∞ | mg/kg·h | 16,269.832 | 13,223.539 | 7295.406 | 10,560.689 |
MRT0–24 h | h | 10.659 | 13.073 | 9.962 | 10.547 |
MRT0–∞ | h | 34.043 | 31.302 | 18.592 | 33.085 |
t1/2 | h | 23.571 | 16.524 | 14.524 | 24.32 |
CLz/F | L/h/kg | 0 | 0 | 0 | 0 |
Tmax | h | 1 | 6 | 4 | 6 |
Cmax | mg/kg | 473.299 | 312.632 | 328.568 | 407.063 |
Plasma |
|||||
AUC0–24 h | μg/kg·h | 201.643 | 97.848 | 290.345 | 163.285 |
AUC0–∞ | μg/kg·h | 228.936 | 159.59 | 406.256 | 163.31 |
MRT0–24 h | h | 1.866 | 3.462 | 11.387 | 0.375 |
MRT0–∞ | h | 2.685 | 3.958 | 12.104 | 0.375 |
t1/2 | h | 1.898 | 0.516 | 2.436 | 0.172 |
CLz/F | L/h/kg | 17.472 | 25.064 | 9.846 | 24.493 |
Tmax | h | 0.083 | 4 | 0.5 | 0.5 |
Cmax | μg/kg | 85.093 | 77.891 | 217.385 | 251.644 |
PLNs |
|||||
AUC0–24 h | mg/kg·h | 19.619 | 8.75 | 66.703 | 29.632 |
AUC0–∞ | mg/kg·h | 20.412 | 14.127 | 96.423 | 30.273 |
MRT0–24 h | h | 2.964 | 4.562 | 5.803 | 4.887 |
MRT0–∞ | h | 3.448 | 5.513 | 9.504 | 5.423 |
t1/2 | h | 2.323 | 0.355 | 4.027 | 4.298 |
CLz/F | L/h/kg | 0.196 | 0.210 | 0.041 | 0.132 |
Tmax | h | 1 | 1 | 1 | 1 |
Cmax | mg/kg | 6.369 | 2.326 | 17.413 | 8.661 |
ILNs |
|||||
AUC0–24 h | mg/kg*h | 12.818 | 6.662 | 117.857 | 23.099 |
AUC0–∞ | mg/kg*h | 13.498 | 8.633 | 119.797 | 39.276 |
MRT0–24 h | h | 2.982 | 4.833 | 8.023 | 8.428 |
MRT0–∞ | h | 3.630 | 5.256 | 8.361 | 24.511 |
t1/2 | h | 2.345 | 5.422 | 3.365 | 14.5 |
CLz/F | L/h/kg | 0.296 | 0.463 | 0.033 | 0.102 |
Tmax | h | 1 | 1 | 6 | 1 |
Cmax | mg/kg | 5.612 | 1.067 | 17.726 | 7.308 |
RLNs |
|||||
AUC0–24 h | mg/kg*h | 15.773 | 19.577 | 163.102 | 12.049 |
AUC0–∞ | mg/kg*h | 35.653 | 28.307 | 166.637 | 13.963 |
MRT0–24 h | h | 15.006 | 10.373 | 9.125 | 5.233 |
MRT0–∞ | h | 21.116 | 20.955 | 9.551 | 7.002 |
t1/2 | h | 15.176 | 14.334 | 3.602 | 4.253 |
CLz/F | L/h/kg | 0.112 | 0.141 | 0.024 | 0.286 |
Tmax | h | 4 | 6 | 6 | 0.167 |
Cmax | mg/kg | 2.722 | 1.134 | 18.485 | 4.631 |
The following parameters were included AUC: area under the plasma–time curve; MRT: the mean residence time; t1/2: the half-life; V: the distribution volumes of the compartment; CL: clearance; Cmax: maximum plasma concentration; Tmax: time to reach the maximum plasma concentration.