艾帕培南的小鼠泌尿道上行性感染药效学研究  

Pharmacodynamic evaluation of apapenem in mouse urinary tract infection model

作　　者：庞晶[1] 王秀坤[1] 杨信怡[1] 胡辛欣[1] 宋坤改[1] 聂彤颖 卢曦[1] 李雪[1] 李聪然[1] 游雪甫[1] 

机构地区：[1]中国医学科学院医药生物技术研究所,北京100050

出　　处：《中国抗生素杂志》2014年第11期864-867,共4页Chinese Journal of Antibiotics

基　　金："十二五"国家科技重大专项(No.2012ZX09301002-001;No.2012ZX09301002-005;No.2014ZX09507009-012);国家基金项目(No.81321004;81361138020);北京科技专项(No.Z141102004414065)

摘　　要：目的评价艾帕培南对小鼠大肠埃希菌泌尿道上行性感染的体内疗效。方法通过泌尿道钝针头插管法,向小鼠膀胱内注入0.05m L浓度为1010CFU/m L的大肠埃希菌9612菌液,建立小鼠泌尿道感染模型。于感染后6、24和30h皮下给药,感染后48h处死动物,取肾剖面盖印和研磨计数,评价艾帕培南的疗效,并与对照药美罗培南、厄他培南进行比较。结果艾帕培南对小鼠的大肠埃希菌9612泌尿道上行性感染具有较好疗效,给药后0.5、2和8 mg/kg剂量组小鼠肾组织匀浆菌落计数明显低于对照组(P<0.01),0.125、0.5、2和8mg/kg剂量组肾剖面盖印结果均与对照组有显著差异(P<0.01)。艾帕培南与相同剂量组美罗培南、厄他培南相比,肾组织匀浆菌落计数和肾剖面盖印结果均无显著性差异(P>0.05)。结论艾帕培南对小鼠泌尿道大肠埃希菌9612上行性感染具有较好疗效,体内抗菌活性与美罗培南、厄他培南相近。Objective To evaluate the in vivo antibacterial efficacy of apapenem against the ascending urinary track infections in mice caused by Escherichia coli.Methods The urinary track infection model in mice was established by transurethrally injecting 0.05mL of an E.coli 9612 suspension （challenge dose,1010CFU/mL） into the bladder through a round-point needle.6,24 and 30h post infection,the compounds were subcutaneously administered The mice were sacrificed 48 h after infection.The kidney stamping was performed and viable colony counts of kidney homogenate samples were determined.The efficacy of apapenem was evaluated and compared with that of meropenem and ertapanem.Results Apapenem showed good efficacy against the ascending urinary track infections caused by E.coli 9612 in mice.0.5,2 and 8mg/kg groups showed significant decreases in kidney viable colony counts （P 〈0.01） in comparison to that of the control group.The stamping results of 0.125,0.5,2 and 8 mg/kg groups were significantly different （P 〈0.01） from that of the control group.No significant difference （P 〉0.05） in kidney stamping and viable colony counts of kidney homogenates was observed for apapenem groups in comparison to the same dosing groups of meropenem and ertapenem.Conclusion Apapenem exhibited good antibacterial efficacy against the ascending urinary track infections in mice caused by E.coli 9612.The therapeutic efficacy of apapenem was generally similar to those ofmeropenem and ertapenem.

关 键 词：艾帕培南 泌尿道上行性感染 药效学评价 

分 类 号：R965.1[医药卫生—药理学]