Pharmacokinetics and Tissue Distribution of DWP20349 and DWP20351, New Quinolones Having 3-Amino-4-methyl thiomethylpyrrolidinyl Group on C7, in Rats

C7위치에 3-아미노-4-메칠치오메칠피로리디닐기를 치환한 신규 퀴놀론계 항생물질 DWP20349 및 DWP20351의 흰쥐에서의 체내동태 및 조직분포

  • 조재열 ((주)대웅제약 중앙연구소) ;
  • 남권호 ((주)대웅제약 중앙연구소) ;
  • 유은숙 ((주)대웅제약 중앙연구소) ;
  • 이재욱 ((주)대웅제약 중앙연구소) ;
  • 유영효 ((주)대웅제약 중앙연구소) ;
  • 박명환 ((주)대웅제약 중앙연구소)
  • Published : 1997.06.01

Abstract

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 ($t_{1/2\beta}$) 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 ($Vd_{ss}$) and total body clearances ($Cl_t$) 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.

Keywords

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