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KMID : 0370219970410030312
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Yakhak Hoeji
1997 Volume.41 No. 3 p.312 ~ p.320
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Pharmacokinetics and Tissue Distribution of DWP20349 and DWP20351, New Quinolones Having 3-Amino-4-methyl thiomethylpyrrolidinyl Group on C7, in Rats
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조재열/Cho JY
남권호/유은숙/이재욱/유영효/박명환/Nam KH/Yoo ES/Lee JW/Yu YH/Park MH
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Abstract
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Pharmacokinetics and tissue distribution of DWP20349 and 20351, new quinolones, were examined in rats after a single intravenous and oral administration. Analyses of DWP20349 an d DWP20351 in plasma, tissue, and urine were determined by both HPLC and bioassay(microbiological assay). The plasma concentrations of the drugs declined biexponentially. The terminal half-lives (t1/2beta) of drugs were about 114 min (DWP20349) and 105 min (DWP20351) after intravenous dosing, and were 77 min (DWP20349) and 79 min (DWP20351) after oral dosing. The volume of distrbution at steady-state (Vdss) and total body clearances (Clt) of DWP20349 and DWP20351 were 760 ml/kg and 1126 ml/kg, and 5ml/min/kg and 10 ml/min/kg, respectively. The extents of bioavailability if DWP20349 and DWP20351 after oral administration were 29% and 28%, respectively. 24 h urinary recoveries measured by bioassay were 1.8% (DWP20349) and 1.3% (DWP20351) after oral dosing, and 2.4% (DWP20349) and 1.9% (DWP20351) after intravenous dosing. Plasma protein binding ratios ranged from 87%-90% (DWP20349) and 61%-68% (DWP20351). These drugs were highly distrbuted by the order of lung, kidney, liver and plasma (DWP20394), and lung, liver, kidney and plasma (DWP20351) after 1 hour orally administered.
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