头孢哌酮/三唑巴坦的体内外抗菌活性研究

In vitro and in vivo antibacterial activities of cefoperazone/tazobactam

目的 :评价头孢哌酮 /三唑巴坦体内外抗菌活性。方法 :采用平皿二倍稀释法测定头孢哌酮 /三唑巴坦对临床分离菌体外抗菌作用 ;采用小鼠腹腔感染模型 ,观察头孢哌酮 /三唑巴坦对金葡球菌、大肠埃希菌和肺炎克雷白杆菌感染小鼠体内疗效。结果 :头孢哌酮 /三唑巴坦 4∶1和 8∶1对 72 1株临床分离菌均有较强抗菌作用 ,两者抗菌活性相近 ,稍弱于头孢哌酮 /三唑巴坦 1∶1和 2∶1,强于头孢哌酮 /三唑巴坦 16∶1和头孢哌酮 ,与头孢哌酮 /舒巴坦相近 ,对多数细菌尤其对肠杆菌属的抗菌活性强于哌拉西林 /三唑巴坦。头孢哌酮 /三唑巴坦 4∶1和 8∶1对产 β 内酰胺酶金葡球菌、大肠埃希菌、肺炎克雷白杆菌、奇异变形杆菌、醋酸钙不动杆菌、阴沟肠杆菌、产气肠杆菌、聚团肠杆菌、异型枸橼酸杆菌和黏质沙雷菌的抗菌活性比头孢哌酮强 2～ 4倍 ,对产超广谱酶 (ESBLs)大肠埃希菌和肺炎克雷白杆菌的抗菌活性比头孢哌酮强 8～ 32倍以上。头孢哌酮 /三唑巴坦 4∶1和 8∶1对金葡球菌、大肠埃希菌和铜绿假单胞菌显示杀菌作用 ,不同 pH值、接种量和血清对头孢哌酮 /三唑巴坦 4∶1和 8∶1抗金葡球菌和大肠埃希菌的活性无明显影响。头孢哌酮 /三唑巴坦 4∶1和 8∶1对金葡球菌、大肠埃希菌和肺炎克雷白杆菌感染小鼠具有较强和相近?

Objective:To evaluate the in vitro and in vivo antibacterial activities of cefoperazone/tazobactam.Methods:The in vitro antibacterial activity of cefoperazone/tazobactam was determined by use of clinical isolated bacteria and standard agar dilution method.Its in vivo antibacterial activity was determined in mice with experimental systemic infection caused by S.aureus,E.coli and K.pneumoniae.Results:The antibacterial activities of cefoperazone/tazobactam 4∶1 and 8∶1 were superior to those of 16∶1 and cefoperazone,inferior to those of 1∶1 and 2∶1 against 721 clinical isolated bacteria.The activities of cefoperazone/tazobactam 4∶1 and 8∶1 were 2 to 4 times stronger than those of cefoperazone against β-lactamases-producing S.aureus,E.coli,K.pneumoniae,P.mirabilis,A.calcoacetius,E.cloaceae,E.aerogenes,E.agglomerans,C.diversus and S.marcescens,and 8 to 32 times stronger than those of cefoperazone against ESBLs-producing E.coli and K.pneumoniae.The MBCs of cefoperazone/tazobactam 4∶1 and 8∶1 were similar to the MICs against S.aureus,E.coli and Ps.aeruginosa.The inoculum size,pH and serum have no effect on the MICs of cefoperazone/tazobactam 4∶1 and 8∶1 against S.aureus and E.coli.The in vivo antibacterial activities of cefoperazone/tazobactam 4∶1 and 8∶1 were similar to that of cefoperazone/sulbactam and superior to those of cefoperazone and piperacillin/tazobactam in mice infected with S.aureus,E.coli and K.pneumoniae.Conclusion:Cefoperazone/tazobactam 4∶1 and 8∶1 had excellent and similar antibacterial activities.The antibacterial activities of cefoperazone against the clinical isolated bacteria were improved by combination of tazobactam.