三唑巴坦/哌拉西林的体内外抗菌活性研究  

In vitro and in vivo antibacterial activities of tazobactam/piperacillin

作　　者：游雪甫[1] 娄人慧[1] 张伟新[1] 闫桂华[1] 陈慧贞[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所,北京100050

出　　处：《中国新药杂志》2003年第9期711-716,共6页Chinese Journal of New Drugs

摘　　要：目的:评价三唑巴坦/哌拉西林的体内外抗菌活性。方法:采用平皿二倍稀释法测定三唑巴坦/哌拉西林对临床分离菌的体外抗菌作用;采用小鼠腹腔感染模型,观察三唑巴坦/哌拉西林对金葡球菌、大肠埃希菌、肺炎克雷伯杆菌感染小鼠的体内抗菌作用。结果:国产和进口三唑巴坦/哌拉西林对甲氧西林敏感的金葡球菌、甲氧西林耐药的金葡球菌、产β-内酰胺酶的金葡球菌、表皮葡萄球菌、大肠埃希菌、奇异变形杆菌、肺炎克雷伯杆菌、醋酸钙不动杆菌、阴沟肠杆菌、产气肠杆菌、聚团肠杆菌、异型枸橼酸杆菌、弗劳地枸橼酸杆菌和黏质沙雷菌的抗菌活性比哌拉西林强2～4倍。三唑巴坦/哌拉西林对金葡球菌和大肠埃希菌显示杀菌作用,不同pH值、接种量和血清浓度对三唑巴坦/哌拉西林抗金葡球菌和大肠埃希菌的活性无明显影响。国产和进口三唑巴坦/哌拉西林对金葡球菌、大肠埃希菌和肺炎克雷伯杆菌感染小鼠具有较好保护作用,两者疗效相近,对产酶的金葡球菌15,金葡球菌44,大肠埃希菌12,肺炎克雷伯杆菌7和肺炎克雷伯杆菌13感染小鼠的疗效明显均优于哌拉西林,对不产酶大肠埃希菌1515感染小鼠的疗效与哌拉西林无显著性差异。结论:国产和进口三唑巴坦/哌拉西林具有较强和相同的体内外抗菌活性。Objective:To evaluate the in vitro and in vivo antibacterial activities of tazobac-tam/piperacillin. Methods:The minimal inhibitory concentrations (MICs) of tazobactam/piperacillin a-gainst clinical isolates of bacteria was tested by stardard agar dilution method. The in vivo antibacterial activities of tazobactam/piperacillin were determined in mice with experimental systemic infection caused by S. aureus,E. coli and K. pneumoniae. Results:The antibacterial activities of domestic and im-ported tazobactam/piperacillin were two to four times stronger than those of piperacillin against MSSA,MRSA,and β-lactamase- producing S. aureus,S. epidermilis,E. coli,P. mirabilis,K. pneumoniae,calcoacetius, E. cloacae, E. aerogenes, E. agglomerans, C. diversus, C. freundi and S. marcescens. The MBCs of domestic tazobactam/piperacillin were similar to the MICs against S. aureus and E. coli. The inoculum size, pH and serum have no effect on the MICs of domestic tazobactam/piperacillin a-gainst S. aureus and E. coli. The in vivo antibacterial activities of domestic and imported tazobactam/ piperacillin were superior to those of piperacillin in mice infected with β-lactamase - producing S. aureus 15,S.aureus 44,E.coli 12,K. pneumoniae 7 and K. pneumoniae 13,and similar to that of piperacillin in mice infected with β-lactamase - negative E.coli 1515. Conclusion:Domestic and imported tazobactam/piperacillin had excellent and similar antibacterial activity. The combination of piperacillin with tazobactam improved the antibacterial activity of piperacillin against β-lactamase - producing clinical isolates of bacteria.

关 键 词：三唑巴坦/哌拉西林 哌拉西林 三唑巴坦 最低抑菌浓度 半数有效量 

分 类 号：R965[医药卫生—药理学] R978.11[医药卫生—药学]