Zeiler H J, Metzger K G, Schacht P, Grohe K
Drugs Exp Clin Res. 1985;11(5):343-50.
The bactericidal activity of ciprofloxacin in active human serum was investigated using serum-resistant Escherichia coli C14 and Pseudomonas aeruginosa 220 as test organisms. In 100% or 80% human serum the growth rate of E. coli C14 was lower than in broth. This also influenced the killing rate of ciprofloxacin. Ciprofloxacin was more active in serum than norfloxacin or ofloxacin and killed Pseudomonas aeruginosa 220 much more rapidly than azlocillin or tobramycin. Rapid killing was also observed in vivo in the blood of intraperitoneally infected mice, ciprofloxacin being superior to norfloxacin, ofloxacin and sisomicin. In mouse protection studies with E. coli Neumann as infecting organism, the dose-effect ratio showed that, despite extremely low blood concentrations, ciprofloxacin had a full therapeutic effect at a dose of 2.5 mg/kg p.o. or less than or equal to 0.5 mg/kg s.c., whereas cefotaxime, despite similar low MIC values in vitro, had to be administered at a dose of 20 mg/kg s.c. in order to achieve 100% survival. These data indicate that ciprofloxacin is effective at low concentrations both in vitro and in vivo.
以血清耐药性大肠杆菌C14和铜绿假单胞菌220作为受试微生物，研究环丙沙星在活性人血清中的杀菌活性。在100%或80%的人血清中，大肠杆菌C14的生长速率低于在肉汤中的生长速率。这也影响了环丙沙星的杀菌速率。环丙沙星在血清中的活性高于诺氟沙星或氧氟沙星，并且杀灭铜绿假单胞菌220的速度比阿洛西林或妥布霉素快得多。在腹腔感染小鼠的血液中也观察到环丙沙星在体内具有快速杀菌作用，其优于诺氟沙星、氧氟沙星和西索米星。在以纽伦堡大肠杆菌作为感染微生物的小鼠保护研究中，剂量效应比表明，尽管血药浓度极低，但口服剂量为2.5mg/kg或皮下注射剂量小于或等于0.5mg/kg时，环丙沙星仍具有完全的治疗效果，而头孢噻肟尽管在体外具有相似的低MIC值，但皮下注射剂量为20mg/kg才能实现100%存活。这些数据表明，环丙沙星在体外和体内低浓度时均有效。
