氟罗沙星体内外抗菌活性及抗生素后效应研究

The antibacterial activity in vitro and in vivo and postantibiotic effects of fleroxacin

目的：对比研究氟罗沙星（ＦＬＲＸ）与其它氟喹诺酮类药物对临床分离致病菌的体内外抗菌活性及抗生素后效应（ＰＡＥ）。方法：应用琼脂平板稀释法测定最低抑菌浓度（ＭＩＣ），微量稀释法测定血清杀菌效价（ＳＢＡ），吸光度法测定ＰＡＥ。结果：ＦＬＲＸ对金葡菌、大肠埃希菌、肺炎克雷伯菌、绿脓假单胞菌均具很强的体内外抗菌活性，与氧氟沙星（ＯＦＬＸ）相似，而强于洛美沙星（ＬＦＬＸ）；ＦＬＲＸ对上述受试菌的峰时ＳＢＡ与ＯＦＬＸ和ＬＦＬＸ相似，但谷时ＳＢＡ多在１∶１以上，高于ＯＦＬＸ和ＬＦＬＸ。ＦＬＲＸ无论对革兰阳性或阴性菌均具较长的ＰＡＥ，呈显著的浓度依赖性，除金葡菌外，对其它受试菌的ＰＡＥ均长于ＯＦＬＸ。结论：ＦＬＲＸ抗菌谱广，体内外抗菌活性强，具有较长时间的ＰＡＥ。

OBJECTIVE: To study the antibacterial activity in vitro and in vivo and postantibiotic effect (PAE) of fleroxacin (FLRX) against clinical isolates. METHODS: MIC was determined by using of agar dilution method, SBA was assayed by microdiluted method, PAE was measured by spectrophotometric method. RESULTS: Antibacterial effects in vitro of FLRX against S. aureus, E. coli, K. pneumonia, and Ps. aeruginosa were better than those of LFLX and similar to those of OFLX. The peak SBA of FLRX against above tested isolates was high, and similar to that of OFLX and LFLX, but the trough SBA was more than 1∶1, higher than OFLX and LFLX. The PAEs induced by FLRX against both Gram positive and negative isolates were long and dependent on the concentrations of the drug. The PAE induced by FLRX was longer than that of OFLX except against S. aureus. CONCLUSION: The activity of FLRX in vitro and in vivo was powerful. PAE induced by FLRX was long. The once daily schedule of FLRX was recommended in the treatment of various bacterial infections.