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KMID : 0043319970200040358
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Archives of Pharmacal Research
1997 Volume.20 No. 4 p.358 ~ p.362
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Metabolism and Excretion Study of DW116, A New Fluoroquinolone, in Rats
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Jung Byung-Hwa
Park Young-Han
Park Jong-Sei
Chung Bong-Chul
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Abstract
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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, F-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 and of the administered dose and the corresponding biliary recoveries were and , respectively.
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KEYWORD
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Fluoroquinolone, DW116, Metabolism, Pharmacokinetics
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