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Metabolism and excretion study of DW116, a new fluoroquinolone, in rats  [1997]

Jung, Byung Hwa Park, Young Han Park, Jongsei Chung, Bong Chul

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Abstract
Metabolite identification and urinary and biliary excretion of the new fluoroquinolone antibacterial agent DW116 [1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, hydrochloride] after oral administration have been studied in Sprague-Dawley rats. The excretion kinetics were monoexponential. Most of the drug was eliminated via the hepatic and renal routes. Mean renal clearance of DW116 was 73.4 ml/hr/kg and mean biliary clearance was 83.8 ml/hr/kg. The major metabolite excreted in the bile was identified as the glucuronide ester of the parent drug using base-hydrolysis of the conjugate metabolite followed by co-HPLC with standard compound,¹⁹F-NMR and LC-MS methods. The glucuronide conjugate was also found in urine. The mean urinary recoveries of free and total (free plus glucuronide ester) DW116 were 28.6±2.7% and 36.4±1.8% of the administered dose and the corresponding biliary recoveries were 14.4±5.5% and 37.0±7.6%, respectively.
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Other subjects

  • renal clearance
  • oral administration
  • excretion
  • drugs
  • urine
  • metabolism
  • fluoroquinolones
  • rats
  • administered dose
  • metabolites
  • antibiotics
  • bile

From the journal

Archives of pharmacal research

ISSN : 0253-6269

Other information

Language : English

Type : Journal Article

In AGRIS since : 2016

Volume : 20

Issue : 4

Start Page : 358

End Page : 362

Publisher : Pharmaceutical Society of Korea

All titles :

" Metabolism and excretion study of DW116, a new fluoroquinolone, in rats "