Zeiler H J, Voigt W H
Am J Med. 1987 Apr 27;82(4A):87-90.
The granuloma pouch model in mice infected with Escherichia coli or Pseudomonas aeruginosa was used to investigate the bactericidal effect of ciprofloxacin in vivo on bacteria in the stationary growth phase. Ciprofloxacin caused a rapid decline in the number of colony-forming units (cfu) of E. coli shortly after initiation of therapy (40 mg/kg, intraperitoneally). Ciprofloxacin was more effective than norfloxacin or pefloxacin and comparable in efficacy to ofloxacin. The drugs penetrated well into the pouch exudate, exceeding the minimal inhibitory concentrations (MICs) of the infecting organisms. The concentrations of pefloxacin or ofloxacin were higher than those of norfloxacin or ciprofloxacin. Ciprofloxacin also showed good killing effects in pouches infected with one strain of P. aeruginosa (ICB 7453, MIC of 0.06 micrograms/ml). However, with another P. aeruginosa strain (ICB 7933), which has a MIC of 0.5 micrograms/ml, killing of stationary cells in vivo was not very pronounced. Electron microscopic evaluation of the pouch exudate revealed that phagocytosed and non-phagocytosed E. coli cells were severely damaged in comparison with untreated control cells. The earliest ultrastructural changes could be observed 15 minutes after initiation of therapy. The results demonstrate that ciprofloxacin is effective in mice for the treatment of a local inflammatory abscess harboring a stationary population of E. coli or P. aeruginosa. This specific kind of killing occurs in vivo when drug concentrations are at least eight to 10 times higher than the MIC.
采用感染大肠杆菌或铜绿假单胞菌的小鼠肉芽肿袋模型，研究环丙沙星在体内对处于稳定生长期细菌的杀菌作用。治疗开始后不久（40mg/kg，腹腔注射），环丙沙星使大肠杆菌的菌落形成单位（cfu）数量迅速下降。环丙沙星比诺氟沙星或培氟沙星更有效，与氧氟沙星疗效相当。药物能很好地渗透到袋状渗出物中，超过感染菌的最低抑菌浓度（MIC）。培氟沙星或氧氟沙星的浓度高于诺氟沙星或环丙沙星。环丙沙星在感染一株铜绿假单胞菌（ICB 7453，MIC为0.06μg/ml）的袋囊中也显示出良好的杀菌效果。然而，对于另一株铜绿假单胞菌（ICB 7933），其MIC为0.5μg/ml，在体内对静止期细胞的杀伤作用并不十分明显。对袋状渗出物的电子显微镜评估显示，与未处理的对照细胞相比，被吞噬和未被吞噬的大肠杆菌细胞受到严重损伤。治疗开始后15分钟即可观察到最早的超微结构变化。结果表明，环丙沙星对小鼠体内携带稳定期大肠杆菌或铜绿假单胞菌的局部炎性脓肿有效。当药物浓度至少比MIC高8至10倍时，这种特异性杀伤在体内发生。
