신규 퀴놀론계 항생물질 DWQ-013의 흰쥐 및 생쥐에서의 체내동태

Abstract

The pharmacokinetics and tissue distribution of DWQ-013, a new quinolone, were examined in rats and mice following a single intravenous and oral administration. DWQ-013 in plasma and urine was determined by both HPLC and microbiological assay. The plasma concentration of the drug declined biexpohentially. The terminal half life of the drug was 1.11 +/- 0.14 hour after intravenous dosing. The volume of distribution at terminal elimination phase(Vdbeta) and total clearance of the drug were 1.29 +/- 0.15l/kg and 0.78 +/- 0.09 l/h/kg. The bioavailability of DWQ-013 after oral administration was 56.0%(HPLC) and 77.2%(bioassay), respectively. Twelve-hour urinary recovery of drug was measured by HPLC and bioassay to 0.035 +/- 0.009% and 4.71 +/- 0.66% after oral dosing, to 0.055 +/- 0.014% and 7.65 +/- 1.53% after intravenous dosing, which may indicate the presence of biologically active metabolites. Binding of the drug to plasma proteins ranged from 97%-99% at various concentrations. The drug was highly distributed in order of liver, kidney and lung after 1.5 hours in mice.