Purpose: The local absorption kinetics of levofloxacin from the intestinal tract was quantitatively evaluated by simultaneously measuring the portal and venous plasma concentrations in a conscious rat.
Methods: The venous and upper portal blood vessels were cannulated through the jugular and pyloric veins, respectively. After oral or intravenous administration of levofloxacin, portal and venous concentrations of levofloxacin were simultaneously monitored. The absorption rate from the intestine into the portal system was calculated from the portal-venous difference in the plasma concentration of levofloxacin, considering the distribution of levofloxacin into erythrocytes. Portal blood flow rate was newly measured by an electromagnetic flow meter.
Results: There was little portal-venous difference after an intravenous dose of levofloxacin. In contrast, after oral administration, the plasma concentration in the portal vein was constantly higher than that in the jugular vein, demonstrating that this difference was caused by the intestinal absorption of levofloxacin.
Conclusions: Approximately 90% levofloxacin was absorbed as the intact form from the intestinal tract into the portal system. By considering the bioavailability of levofloxacin in rat, the hepatic extraction ratio in vivo of levofloxacin was estimated to be 30%. The mean local absorption time (Ta) was 1.44 hr which coincided almost with the mean absorption time (MAT).