Compound | Route | AUC0−∞1-a | AUC0−∞1-a | CL | VSS | T1/2λ1 | T1/2term | MRT | F |
---|---|---|---|---|---|---|---|---|---|
ng−eq*h/ml1-b | ng*h/ml1-c | ml/min | l/kg | h | h | h | % | ||
Rapamycin | Oral | 428 ± 12 | 172 ± 10 | 2.4 ± 0.5 | 24.3 ± 4.6 | 23.8 ± 5.3 | 10.0 | ||
SDZ-RAD | Oral | 606 ± 36 | 141 ± 43 | 2.7 ± 0.5 | 15.5 ± 1.5 | 16.4 ± 1.3 | 16.4 | ||
Rapamycin | i.v. | 1760 ± 30 | 1140 ± 90 | 3.0 ± 0.2 | 27 ± 3 | 1.9 ± 0.1 | 25.2 ± 2.6 | 34.5 ± 4.2 | |
SDZ-RAD | i.v. | 1350 ± 90 | 573 ± 32 | 6.2 ± 0.3 | 52 ± 4 | 3.4 ± 1.1 | 14.2 ± 0.4 | 15.9 ± 0.5 |
T1/2λ1 is half-life of main elimination phase, and T1/2term is half-life of the terminal phase based on the 0- to 48-h data only. Results are expressed as means ± S.E.M. of four to five rats.
↵1-a AUC0−∞ is extrapolated to infinity from 0- to 48-h data.
↵1-b ng−eq*h/ml refers to the total radioactivity measured in blood.
↵1-c ng*h/ml refers to the parent compound.