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C7-이환체 구조를 갖는 새로운 플루오로퀴놀론계 항생물질의 흰쥐 체내동태와 조직분포
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  • C7-이환체 구조를 갖는 새로운 플루오로퀴놀론계 항생물질의 흰쥐 체내동태와 조직분포
저자명
조재열,한승희,김병오,남권호,손호정,이재욱,유영효,박명환
간행물명
The journal of applied pharmacology : the official journal of the Korean Society of Applied Pharmacology
권/호정보
1997년|5권 4호|pp.419-425 (7 pages)
발행정보
한국응용약물학회
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

The pharmacokinetics of DWP20364 (1-cyclopropyl -5-amino-6,8-difluoro-7-(2,7-diazabiclo [3,3,0] oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a novel fluoroquinolone containing C7-bicyc-talc structure, were compared with those of ciprofloxacin (CPFX) after single intravenous (i.v.) and oral (p.o.) administration to rats using microbiological assay (bioassay). After i.v. administration to rats, the plasma concentrations of the two drugs declined biexponentially. The terminal half-lives (t$_{1}$2$eta$/) of DWP20364 were 110$pm$ 13.2 min and 117$pm$3.09 min after i.v. and p.o. administration, respectively, and they were significantly higher than those of CPFX (45.5$pm$9.52 min and 48.3$pm$ 12.1 min, respectively). Similar results were also obtained from plasma concentrations and area under the plasma concentration-time curves. The total body clearance of DWP20364, 7.82$pm$0.37 ml/min/kg was significantly slower than that of CPFX, 27.3 $pm$ 11.1 m1/ min/kg. Above data suggested that the antimicrobial activity of DWP20364 could be longer than that of CPFX. The urinary recovery after i.v. and p.o. administration of DWP20364 was significantly lower than those of CPFX suggesting that the effect of DWP20364 on urinary tract infection could be lower than that of CPFX. The serum protein binding values of DWP20364 at 2$mu$g/ml were apparently 91.5~93.1% in rats and human. DWP20364 was distributed by the order of liver, lung, kidney, sf)leon, heart, muscle and brain collected at 30 min after orally administered.