Urinary tract infections Pharmacodynamic evaluation Uropatho

  本文关键词：新碳青霉烯类抗生素百纳培南的小鼠泌尿道感染药效学研究，由笔耕文化传播整理发布。

新碳青霉烯类抗生素百纳培南的小鼠泌尿道感染药效学研究

Pharmacodynamic evaluation of benapenem,a new carbapenem antibiotic,in mouse urinary tract infection model

[1] [2] [3] [4] [5] [6] [7] [8] [9] [10]

LU Xi, LI Cong-ran, PANG Jing, HU Xin-xin, NIE Tong-ying, YANG Xin-yi, LI Xue, LI Guo-qing, WANG Xiu-kun, YOU Xue-fu（ Department of Pharmacology, Institute of Medicinal Biote

中国医学科学院医药生物技术研究所药理室,北京100050

文章摘要：目的评价新碳青霉烯类抗生素百纳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0.05 ml浓度为1010cfu/ml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30 h皮下给药,感染后48 h处死动物,取肾剖面盖印并研磨计数,对百纳培南进行体内药效学评价,并与对照药美罗培南、厄他培南进行比较。结果对大肠埃希菌9612泌尿道上行性感染小鼠,百纳培南8、2和0.5 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）;8、2、0.5和0.125 mg/kg剂量组肾剖面盖印结果均与对照组有显著差异（P〈0.01或P〈0.05）。百纳培南与相同剂量美罗培南、厄他培南组相比,除0.125 mg/kg剂量组肾剖面盖印结果与厄他培南组有显著性差异（P〈0.01）外,其他剂量组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）。结论对于小鼠泌尿道大肠埃希菌9612上行性感染,百纳培南可显著降低小鼠的肾组织菌落计数和肾剖面盖印阳性率,疗效与美罗培南、厄他培南相近。

Abstr：Objective To evaluate the in vivo antibacterial efficacy of benapenem against the ascending urinary track infections caused by Escherichia coli in mice. Methods The urinary track infection model in mice was established by inserting a round-point needle transurethrally for injection of 0.05 ml of an E. coli 9612 suspension（challenge dose, 1010 cfu/ml） into the bladder. The compounds were administered subcutaneously at 6, 24, and 30 h post infection. 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 benapenem was evaluated and compared with that of meropenem and ertapanem. Results Benapenem showed good efficacy against the ascending urinary track infections caused by E. coli 9612 in mice. Significant decreases in kidney viable colony counts（P〈0.01） were observed in 8, 2 and 0.5 mg/kg groups in comparison with that of control group. The stamping results of 8, 2, 0.5 and 0.125 mg/kg groups were significant different（P〈0.01 or P〈0.05） from that of control group. When comparing the same dosing groups for different compounds, significant different stamping result（P〈0.01） was seen in 0.125 mg/kg benapenem group, compared with that of 0.125 mg/kg ertapenem group, while no significant difference（P〈0.05） in kidney stamping and viable colony counts of kidney homogenates was observed for other benapenem groups incomparison with the same dosing groups of meropenem and ertapenem. Conclusion Benapenem exhibits good antibacterial efficacy against the ascending urinary track infections in mice caused by E. coli 9612. The therapeutic efficacy of benapenem is generally similar to those of meropenem and ertapenem.

文章关键词：

Keyword：:Urinary tract infections Pharmacodynamic evaluation Uropathogenic Escherichia coli Benapenem

课题项目：“十二五”国家科技重大专项（2012ZX09301002-001、2012ZX09301002-005、2014ZX09507009-012）; 国家自然科学基金（81321004、81361138020）; 北京市重点实验室科技创新基地培育与发展工程（Z141102004414065）

  本文关键词：新碳青霉烯类抗生素百纳培南的小鼠泌尿道感染药效学研究，由笔耕文化传播整理发布。