Uptake clearance of drugs in rat kidney slices
Time-dependent uptake of drugs into rat kidney slices was measured in the presence of tracer amount of drugs in the incubation buffer (0.1 μM for [3H]pravastatin, [3H]pitavastatin, [3H]rosuvastatin, [3H]valsartan, and [3H]olmesartan; 6.3 μM for [14C]temocaprilat; 1.7 μM for [14C]PCG; 10 μM for enalaprilat, benazeprilat, cefmetazole, and ceftizoxime). The in vitro intrinsic uptake clearance (P1 kid) was calculated by dividing initial uptake velocity by the drug concentration in the incubation buffer. Each value is expressed as mean ± S.E. of triplicate determinations.
Compound | P1KID |
---|---|
ml/min/g kidney | |
Pravastatin | 0.236 ± 0.110 |
Pitavastatin | 0.912 ± 0.173 |
Rosuvastatin | 0.310 ± 0.110 |
Valsartan | 1.21 ± 0.29 |
Olmesartan | 0.644 ± 0.175 |
Candesartan | 0.796 ± 0.363 |
Temocaprilat | 0.290 ± 0.115 |
Enalaprilat | 0.220 ± 0.135 |
Benazeprilat | 0.122 ± 0.047 |
PCG | 0.521 ± 0.106 |
Ceftizoxime | 0.0415 ± 0.0272 |
Cefmetazole | 0.0953 ± 0.0176 |