本文關鍵詞：新碳青霉烯類抗生素百納培南的小鼠泌尿道感染藥效學研究，由筆耕文化傳播整理發(fā)布。

新碳青霉烯類抗生素百納培南的小鼠泌尿道感染藥效學研究

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

中國醫(yī)學科學院醫(yī)藥生物技術研究所藥理室,北京100050

文章摘要：目的評價新碳青霉烯類抗生素百納培南對小鼠大腸埃希菌泌尿道上行性感染的體內療效。方法通過泌尿道鈍針頭插管法,向小鼠膀胱內注入0.05 ml濃度為1010cfu/ml的大腸埃希菌9612菌液,建立小鼠泌尿道感染模型。于感染后6、24和30 h皮下給藥,感染后48 h處死動物,取腎剖面蓋印并研磨計數(shù),對百納培南進行體內藥效學評價,并與對照藥美羅培南、厄他培南進行比較。結果對大腸埃希菌9612泌尿道上行性感染小鼠,百納培南8、2和0.5 mg/kg劑量組小鼠腎組織勻漿菌落計數(shù)明顯低于對照組（P〈0.01）;8、2、0.5和0.125 mg/kg劑量組腎剖面蓋印結果均與對照組有顯著差異（P〈0.01或P〈0.05）。百納培南與相同劑量美羅培南、厄他培南組相比,除0.125 mg/kg劑量組腎剖面蓋印結果與厄他培南組有顯著性差異（P〈0.01）外,其他劑量組腎組織勻漿菌落計數(shù)和腎剖面蓋印結果均無顯著性差異（P〉0.05）。結論對于小鼠泌尿道大腸埃希菌9612上行性感染,百納培南可顯著降低小鼠的腎組織菌落計數(shù)和腎剖面蓋印陽性率,療效與美羅培南、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.

文章關鍵詞：

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

課題項目：“十二五”國家科技重大專項（2012ZX09301002-001、2012ZX09301002-005、2014ZX09507009-012）; 國家自然科學基金（81321004、81361138020）; 北京市重點實驗室科技創(chuàng)新基地培育與發(fā)展工程（Z141102004414065）

  本文關鍵詞：新碳青霉烯類抗生素百納培南的小鼠泌尿道感染藥效學研究，由筆耕文化傳播整理發(fā)布。