8-Fluorociprofloxacin과 Ciprofloxacin의 시험관내 및 생체내 항균 효과와 약물동태의 비교

• 영문명: In vitro and in vivo Antibacterial Activities and Pharmacokinetics of 8-Fluorociprofloxacin and Ciprofloxacin
• 발행기관: 대한약학회
• 저자명: 최경업(Kyung Eob Choi) 정용환(Yong Hwan Jung) 김제학(Je Hak Kim)
• 간행물 정보: 『약학회지』제37권 제3호 (1993년), 235~242쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1993.06.30

영문 초록

8-Fluorociprofloxacin(8-FCP) is an investigational quinolone derivative that is substituted with fluorine at the C-8 position of ciprofloxacin(CP). It was found that the in vitro activity of 8-FCP against Gram(+) bacteria was more potent that of CP, but the opposite against Gram(-) bacteria was true. However, 8-FCP showed better in vivo efficacy than CP against representative Gram(-) organisms, E. coli and K pneumoniae. In an attempt to seek for factors causing this discrepancy in the antibacterial activities, a comparative pharmacokinetic study of 8-FCP and CP was conducted in mice and rats treated either intravenously or orally at a single dose of 30mg/kg. The pharmacokinetic parameters in mice were as follows; the mean peak serum concentrations(Cmax) following i.v. and oral doses were 12.4 and 5.3mcg/ml for 8-FCP, and 9.5 and 2.5mcg/ml for CP, respectively. The terminal half-life(tl/2beta) was 72.9 min for 8-FCP, and 98.2 min for CP, and the oral bioavailability(F) was 89.9% for 8-FCP, and 50.5% for CP. In rats, the mean (+/-SD) Cmax after i.v. administration were 11.6 +/- 1.6 mcg/ml for 8-FCP, and 10.2 +/- 1.3 mcg/ml for CP, whereas oral administration produced Cmax of 5.9 +/- 1.8 mcg/ml for 8-FCP and 1.1 +/- 0.9 mcg/ml for CP, respectively. The tl/2beta was 67.9 +/- 8.4 min for 8-FCP, and 76.4 +/- 7.2 min for CP. The F was 88.6 +/- 6.3% for 8-FCP, and 40.7 +/- 6.5% for CP. Marked differences were observed between the two quinolones in the Cmaxand the area under the concentration-time curve obtained after oral administration in mice and rats. The extent of 8-FCP absorption in both mice and rats was approximately 2-fold higher than that of CP, suggesting that the fluorine atom attached to C-8 plays an important role in facilitating oral absorption from the gastrointestinal tract.

키워드

8-Fluorociprofloxacin ciprofloxacin antibacterial activities pharmacokinetics.