Abstract

Levofloxacin (LVFX) is a rapidly absorbed new quinolone and (S) - (-) -ofloxacin. The effects of metal cations on the urinary excretion of Levofloxacin (LVFX) were investigated in five healthy volunteers at the time of differential administration by measuring the unmetabolites of LVFX in urine and the findings of LVFX were then compared with those of long-acting Sparfloxacin (SPFX). Magnesium oxide (MgO) containing Mg2+ and sucralfate containing Al3+ are examined as metal cations.Urine samples were collected for 10 and 24 hours after a single oral administration of LVFX and SPFX, respectively. The unmetabolites concentrations of LVFX and SPFX in urine were determined using HPLC.The urinary excretion of LVFX decreased significantly after the simultaneous administration with MgO and sucralfate and at 1 hour after the administration of LVFX (p<0.05) but was not affected at 2 hours after administration. The administration of MgO and sucralfate within 2 hours after the administration of SPFX resulted in a significant decrease in SPFX urinary excretion (p<0.05). However, the decrease in SPFC urinary excretion was less than that in LVFX. Sucralfate decreased the LVFX urinary excretion more than MgO although the difference was not significant. The effect of sucralfate on SPFX urinary excretion was the same as that for MgO.These results suggest that the interactions between LVFX and metal cations are avoidable by the administration of metal cations at 2 hours after the administration of LVFX and the administration of metal cations must be avoidable within 2 hours after the administration of SPFX.

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