Matsushita T, Kouyama K, Yamaguchi T
Jpn J Antibiot. 1985 Jul;38(7):1819-26.
Bactericidal activities of aspoxicillin (ASPC) against E. coli (2 strains) and K. pneumoniae (1 strain) were compared with those of piperacillin (PIPC) using in vitro kinetic models simulating human serum levels. In the model of intravenous injection, both drugs exhibited bactericidal action against the strains of E. coli. The activity of ASPC was found to superior to PIPC and ASPC could decrease viable cell counts from 10(7) cells/ml to 10(8) cells/ml. On the other hand, the bactericidal activity of ASPC against K. pneumoniae was weaker than that of PIPC. In the model of intravenous drip infusion, ASPC showed a high level of bactericidal activity comparable to that observed in the intravenous model against E. coli. Interestingly, the bactericidal activity of ASPC against K. pneumoniae in this model was similar to that of PIPC, though the MIC value of ASPC was higher than that of PIPC. In the intravenous model, the effects of ASPC and PIPC on the morphology of E. coli KC-14 were examined with a phase contrast microscope. Exposure to PIPC caused only an elongation of the cells, but the treatment with ASPC resulted in the formation of spheroplast-like structure of the cells, which were finally subjected to bacteriolysis.
使用模拟人血清水平的体外动力学模型,比较了阿扑西林(ASPC)对大肠杆菌(2株)和肺炎克雷伯菌(1株)的杀菌活性与哌拉西林(PIPC)的杀菌活性。在静脉注射模型中,两种药物对大肠杆菌菌株均表现出杀菌作用。发现ASPC的活性优于PIPC,且ASPC可使活菌数从10⁷个细胞/毫升降至10⁸个细胞/毫升。另一方面,ASPC对肺炎克雷伯菌的杀菌活性弱于PIPC。在静脉滴注模型中,ASPC对大肠杆菌表现出与静脉注射模型相当的高水平杀菌活性。有趣的是,尽管ASPC的MIC值高于PIPC,但在该模型中ASPC对肺炎克雷伯菌的杀菌活性与PIPC相似。在静脉注射模型中,用相差显微镜检查了ASPC和PIPC对大肠杆菌KC - 14形态的影响。暴露于PIPC仅导致细胞伸长,但用ASPC处理导致细胞形成原生质球样结构,最终发生溶菌。