Table 1.
Pharmacokinetics of control rapamycin, rapamycin in PEG-b-PCL, and rapamycin in PEG-b-PCL + α-tocopherol in blood after IV administration in rats (mean ± SEM, n = 4) between both formulations
Pharmacokinetic parameter | Rapamycin control | Rapamycin in PEG-b-PCL | Rapamycin in PEG-b-PCL + α-tocopherol |
---|---|---|---|
AUCinf (μg h/ml) | 7.584 ± 0.887 | 8.556 ± 0.248 | 11.929 ± 0.412a,b |
AUC0-48h (μg h/ml) | 7.294 ± 0.992 | 8.378 ± 0.204 | 11.751 ± 0.399a,b |
Vdβ (l/kg) | 23.993 ± 3.466 | 26.696 ± 1.302 | 17.745 ± 1.272b |
CLrenal (l/h kg) | 0.053 ± 0.012 | 0.022 ± 0.002a | 0.012 ± 0.003a,b |
CLhepatic (l/h kg) | 1.284 ± 0.012 | 1.150 ± 0.035 | 0.828 ± 0.027a,b |
CLtot (l/h kg) | 1.337 ± 0.156 | 1.172 ± 0.034 | 0.840 ± 0.028a,b |
KE (h−1) | 0.056 ± 0.001 | 0.044 ± 0.002a | 0.048 ± 0.03 |
t1/2 (h) blood | 12.396 ± 0.346 | 15.820 ± 0.843 | 14.626 ± 0.812 |
t1/2 (h) urine | 10.296 ± 0.014 | 10.647 ± 0.061a | 21.393 ± 0.026a,b |
MRT (h) | 8.770 ± 3.120 | 4.833 ± 0.780 | 4.304 ± 0.355 |
Extraction ratio (ER) | 0.399 ± 0.045 | 0.357 ± 0.011 | 0.257 ± 0.008a,b |
Estimated bioavailability (%) | 60.123 ± 3.169 | 64.293 ± 1.092 | 74.297 ± 0.836a,b |
Denotes statistical significant difference (P < 0.05) between control and formulation
Denotes statistical significant difference (P < 0.05)