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注射用头孢哌酮/他唑巴坦的体外抗菌活性研究
引用本文:李忠思,张小娜,张琳,杨丽,彭小茹,吴霭.注射用头孢哌酮/他唑巴坦的体外抗菌活性研究[J].中国药师,2010,13(4):476-479.
作者姓名:李忠思  张小娜  张琳  杨丽  彭小茹  吴霭
作者单位:1. 广州白云山制药股份有限公司,广州,510515
2. 广州白云山化学药创新中心药理室
摘    要:目的:评价头孢哌酮/他唑巴坦(4:1和8:1)、头孢哌酮/舒巴坦(1:1和2:1)的抑酶增效作用,并比较同类复方制剂在临床常用量时的体外抗菌效果。方法:采用琼脂二倍稀释法对409株临床分离株进行药物敏感测定。结果:头孢哌酮/他唑巴坦(4:1和8:1)、头孢哌酮/舒巴坦(1:l和2:1)联合应用对金黄色葡萄球菌、表皮葡萄球菌、粪肠球菌等革兰阳性菌的MIC50/MIC90均较头孢哌酮钠单用时降低2~4倍。对大肠埃希菌(包括产ESBLs)、肺炎克雷伯菌(包括产(ESBLs)、铜绿假单胞菌、阴沟肠杆菌、鲍曼不动杆菌等革兰阴性杆菌的MIC50/MIC90分别较头孢哌酮钠单用时降低2~64倍和2~8倍,尤其对产ESBLs的大肠埃希菌和肺炎克雷伯菌其MIC50/MIC990也分别降低8~32倍和2—8倍。同类复方制剂对上述革兰阳性菌和革兰阴性杆菌的MIC50/MIC90在临床常用量的1/256—1/65536倍,MIC50和MIC90较按常规试验配比组分别降低3~33倍和4~87倍。结论:头孢哌酮与他唑巴坦或舒巴坦联合应用可不同程度地提高头孢哌酮的体外抗菌活性,头孢哌翮/他唑巴坦4:1和8:1的体外抗菌活性基本相当,均优于头孢哌酮/舒巴坦1:1和2:1。4种同类复方制剂的体外抗菌活性,注射用头孢哌酮/他唑巴坦亦优于注射用头孢哌酮/舒巴坦。

关 键 词:头孢哌酮  他唑巴坦  舒巴坦  β-内酰胺酶抑制剂

Study on Antibactreral Activity of Cefoperazone Sodium and Tazobactam Sodium in Vitro
Li Zhongsi,Zhang Xiaona,Zhang Lin,Yang Li,Peng Xiaoru,Wu Ai.Study on Antibactreral Activity of Cefoperazone Sodium and Tazobactam Sodium in Vitro[J].China Pharmacist,2010,13(4):476-479.
Authors:Li Zhongsi  Zhang Xiaona  Zhang Lin  Yang Li  Peng Xiaoru  Wu Ai
Institution:1. Guangzhou Baiyunshan Parmacential Co. Ltd, Guangzhou 510515, China;2. Department of Pharmacology, Guangzhou Baiyunshan Chemistry Medicine Innovation Center)
Abstract:Objective : To evaluate the synergistic effect of cefoperazone/tazobactam (4:1 and 8:1 ) and cefoperazone/sulbactam (1:1 and 2:1 ) on inhibiting Beta-lactamase, and the in vitro antimicrobial effect of the same compound preparations in clinical recom- mended dosages. Method: Bacterial susceptibility testing was performed on 409 strains of clinical isolated pathogens, AGAR dilution method twice was used. Result: The MICso/MIC90 of staphylococcus aureus, staphylococcus epidermidis, enterococcus faecalis and such Gram-positive bacteria on the combined application of cefoperazone/tazobactam (4:1 and 8:1 )and cefoperazone/sulbactam (1:1 and 2:1 ) were decreased with 2-4 times than the separate applications of cefoperazone. The MICs0/MICgo of escherichia coli ( including pro- duction ESBLs), Klebsiella pneumonia (including production ESBLs) ,pseudomonas aeruginosa, enterobater cloacae, aeinetobacter bau- mannii etc gram-negative bacilli on the combined application were decreased with 2-64 times and 2-8 times than the separate applica- tions of cefoperazone, especially for the ESBLs of eschereichia coli and Klebsiella pneumonia, the MICso and MICgo were respectively low- er 8-32 times and 2-8 times. The MICso/MIC~o of the Gram-pesitive and gram-negative bacilli on the same compound preparations were range in the 1/256 times-I~65536 times of clinical recommended dosages. The MICs0 and MICgo of the same compound preparations groups were respectively lower 3-33 times and 4-87 times than of the routine test group. Conclusion: In vitro antimicrobial activity of the cefoperazone/tazobactam (4:1 )is the same of the cefoperazone/tazobactam (8:1 ), and of all the cefoperazone/tazobactam were su- perior than of all the cefoperazone/sulbactam. Comparing in vitro antimicrobial activity of four kind of the same compound preparations, injectable cefoperazone/tazobactam, also were superior than injectable cefoperazone/sulbactam.
Keywords:Cefoperazone  Tazobactam  Sulbactam  Beta-lactamase inhibitors
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