头孢哌酮及其复合制剂血清杀菌活性研究  

A study of bactericidal activity of serum after administration of cefoperazone and its complex compound

作　　者：王培兰[1] 苏伟[2] 刘又宁[1] 王睿[3] 

机构地区：[1]解放军总医院呼吸科,北京100853 [2]兰州军区乌鲁木齐总医院心内科 [3]解放军总医院临床药理研究室,北京100853

出　　处：《解放军医学杂志》2006年第1期48-50,共3页Medical Journal of Chinese People's Liberation Army

摘　　要：目的评价头孢哌酮(CPZ)、头孢哌酮/舒巴坦(CPZ/SBT,1∶1)与头孢哌酮/他唑巴坦(CPZ/TZBT,2∶1)的体内抗菌活性。方法12名健康男性志愿者,采用随机分组、自身前后对照方法,分别静脉滴注CPZ1.5g、CPZ/SBT3.0g和CPZ/TZBT2.25g,于给药后0.5h(峰浓度)、7h(谷浓度)采血,测定血清杀菌活性(SBA)。结果3种抗生素对产β内酰胺酶的金黄色葡萄球菌、表皮葡萄球菌、阴沟肠杆菌、大肠埃希菌的峰时SBA中位数均≥1∶8,差异无统计学意义;而CPZ/SBT、CPZ/TZBT对产超广谱β内酰胺酶(ESBLs)的肺炎克雷伯、大肠埃希菌的SBA较CPZ高2～4倍(P<0.01)。结论CPZ及其复合制剂对临床常见致病菌具有良好的血清杀菌活性,对产超广谱β内酰胺酶的肺炎克雷伯菌、大肠埃希菌,CPZ复合制剂的SBA优于CPZ。Objective To evaluate the bactericidal and bacteriostatic activity （SBA, SRS） of the serum after the administration of Cefoperazone （CPZ）, Cefoperazone/Sulbactam （CPZ/SBT） and Cefoperazone/Tazobactam （CPZ/TZBT） against clinical isolates to study synergistic effect of Cefoperazone and enzyme-inhibitor Sulbactam and Tazobactam in vivo. Methods A randomized self-control clinical study was performed in 12 healthy male volunteers, and 1.5g CPZ or 3. 0g CPZ/SBT and 2. 25g CPZ/TZBT was administered to them by iv route, To determine the SBA and SBS of the above three drugs, blood samples were taken 0.5h （peak blood level） and 7h （trough blood leved） after administration. Results At the peak level of SBA and SBS of three drugs, the median SBS against β-lactamase positive S. anreus, S. epidermidis, E. cloacae and E. coil was all ≥1：8 （P〉0. 01）, no significant differences were observed. The peak SBA of CPZ/ SBT and CPZ/TZBT against ESBLs positive K. pneumoniae and E. coli were shown to be slightly stronger than that of CPZ by 2-4 times （P〈0.01）. There was no significant difference against P. aeruginosa among three antibiotics. Conclusions Cefoperazone and Cefoperazones showed good antimicrobial activity in vivo against clinical β-lactamase positive isolates. The in vivo antibacterial activities of CPZ/SBT and CPZ/TZBT against clinical extend spectrum β-lactamases positive isolates are stronger than that of CPZ. Enzyme inhibitors, Sulbactam and Tazobactam, protect cefoperazone from hydrolysis.

关 键 词：头孢哌酮 Β内酰胺酶类 血清杀菌活性 

分 类 号：R978.11[医药卫生—药品]