Table 2

[3H]FU and [3H]FUdR levels in inferior vena cava (IVC) and in hepatic veins (HV) of rats intravenously injected with the free or L-HSA-conjugated drugs

DrugMeans of AdministrationDoseTimeLevelsLevels in HV/Levels in IVC
IVCHV
μg/g h ng/ml
Free FUdRBolus0.50.5BML2-a BML
2.50.25360.2  ± 24.354.1  ± 5.5*** 0.2
1-h Infusion0.553.1  ± 4.4BML<0.4
Conjugated FUdRBolus0.50.545.6  ± 2.954.8  ± 4.21.2
128.0  ± 1.147.5  ± 5.21.7
1-h Infusion0.25BML BML
0.526.3  ± 1.337.8  ± 2.61.4
128.4  ± 0.530.3  ± 1.51.1
Free FUBolus0.50.2550.6  ± 8.5BML<0.4
0.5BML BML
152-b 0.254344.0  ± 130.0748.6  ± 55.2*** 0.2
0.5347.4  ± 30.055.8  ± 8.3*** 0.2

Data were obtained from three rats and are given as mean ± S.E. When the difference between the drug level in IVC and HV is statistically significant (Student's t test), it is indicated by asterisks (***p < 0.001).

  • 2-a  Below measurable level (<20 ng/ml).

  • 2-b  Commonly used dose in human chemotherapy with FU (Heriot and Kumar, 1998).