利他唑酮注射剂体内抗菌作用研究  

Studies on antibacterial activity of litazolid injecti on in vivo

作　　者：朱珍真[1] 陈贞[1] 王琪[2] 李岳 郎丽巍[1] 王红艳[1] 魏振满[1] 鲁韬 Zhu Zhen-zhen Chen zhen Wang Qi Li Yue Lang Li-wei Wang Hong-yan Wei Zhen-man Lu Tao(302 Military Hospital of China, Pharmaceutical Department, Drug Clinical Trial Center, Beijing 100039 Peking University Health Science Center, Institute of Clinical Pharmacology, Beijing 100191 Sichuan Saizhuo Pharmacy Co.,Ltd, Mianyang 621000)

机构地区：[1]解放军第三〇二医院药学部药物临床试验中心,北京100039 [2]北京大学第一医院临床药理研究所,北京100191 [3]四川赛卓药业股份有限公司,绵阳621000

出　　处：《中国抗生素杂志》2016年第11期865-868,共4页Chinese Journal of Antibiotics

基　　金：国家十二五重大新药创制;国家重大科技专项课题(No.2014ZX09201001-008)

摘　　要：目的研究利他唑酮(LT-01)注射剂对小鼠细菌感染的保护作用,以此来评价LT-01的体内抗菌效果。方法用LT-01注射剂及利奈唑胺注射液对2株革兰阳性菌感染小鼠败血症模型进行保护作用研究,记录小鼠的存活数,并用DAS2.1.1软件计算半数有效量(ED_(50))等参数,并比较两药的差异。结果 LT-01注射剂对万古霉素耐药肠球菌(VRE)感染小鼠败血症模型的ED_(50)=1.036mg/kg,对耐甲氧西林金黄色葡萄球菌(MRSA)感染小鼠败血症模型ED_(50)=1.271mg/kg,与市售利奈唑胺注射液相比均无显著差异(P>0.05)。结论实验结果表明LT-01对革兰阳性球菌有很好的抗菌作用,提示LT-01是一种可用于临床治疗耐药革兰阳性球菌感染的药物,值得进一步开发研究。Objective To study the protective effect of litazolid （LT-01） injection in mouse infection models, and to evaluate the antibacterial effect of LT-01 in vivo. Methods This paper investigated protective effect of litazolid and linezolid injection in systemic infection models caused by two strains of gram positive bacteria and survival number of mouse was recorded, and used the software of DAS2.1.1 to calculate the parameters such as 50% effective doses （ED50）, then compared the difference between the two drugs. Results In the systemic vanomycin- resistant enterococci （VRE） and methicillin resistant Staphylococcus aureus （MESA） infections, LT-01 50% effective doses （ED50） were 1.036 and 1.271mg/kg, which were equivalent to linezolid （P〉0.05）. Conclusion The experimental results showed that LT-01 has a good antibacterial effect on Gram-positive bacteria, suggested that LT- 01 is a new drug that can be used in the clinical treatment of drug resistant Gram-positive bacteria infection, which is worthy to further research.

关 键 词：利他唑酮 利奈唑胺 败血症模型 耐药革兰阳性球菌 

分 类 号：R978.1[医药卫生—药品]