富马酸阿奇霉素的体内抗菌活性与安全性评价  

Experimental evaluation of in vivo antibacterial activities and safety of azithromycin fumarate in mice

作　　者：王丽[1] 孙丰斌 米宁[1] 辛晓明[1] 赵晓民[1] 高允生[1] 

机构地区：[1]泰山医学院药理学教研室,山东泰安271016 [2]山东泰邦生物制品有限公司,山东泰安271016

出　　处：《泰山医学院学报》2011年第5期337-339,共3页Journal of Taishan Medical College

摘　　要：目的评价富马酸阿奇霉素(AMF)的体内抗菌活性和安全性,并与阿奇霉素(AM)和红霉素(EM)进行比较。方法腹腔注射金黄色葡萄球菌(金葡菌)和乙型溶血性链球菌(链球菌)建立小鼠全身感染模型,观察AMF、AM和EM灌胃给药(ig)对感染小鼠的保护作用。正常小鼠一次性ig AMF,观察7天内的毒性反应和死亡情况。结果体内抗菌实验结果显示,AMF保护金葡菌和链球菌感染小鼠的ED50分别为33.38和18.25 mg?kg-1,AM为58.22和17.81 mg?kg-1,EM为116.92和47.51 mg?kg-1。AMF对正常小鼠ig的LD50为3273.4 mg?kg-1,对金葡菌和链球菌感染小鼠的化疗指数分别为98.1和179.4。结论 AMF和AM对金葡菌和链球菌感染小鼠的体内抗菌活性明显强于红霉素。AMF对金葡菌感染小鼠的保护作用优于AM,而两药对链球菌感染小鼠的保护作用相同。Objective： To evaluate the in vivo antibacterial activities and safety of azithromycin fumarate（AMF） in comparision with azithromycin（AM） and erythromycin（EM）.Methods： The mice general infection models were established by intraperitoneal injecting Staphylococcus aureus and Streptococcus hemolyticus,respectively.And the protective effects of AMF,AM and EM administered intragastically against the mice infected were investigated.After single intragastric dosing,the toxic symptoms and the number of deaths of azithromycin fumarate were observed for seven days in normal mice.Results： The ED50 values of AMF in mice infected by Staphylococcus aureus and Streptococcus hemolyticus were 33.38 and 18.25 mg？kg-1,AM were 58.22 and 17.81 mg？kg-1,EM were 116.92 and 47.51 mg？kg-1,respectively.The LD50 value of AMF administered intragastically was 3273.4 mg？kg-1 in normal mice.The chemotherapeutic indexes of AMF were 98.1 and 179.4 in mice infected by Staphylococcus aureus and Streptococcus hemolyticus.Conclusion： AMF and AM showed higher in vivo antibacterial activity against mice infected by Staphylococcus aureus and Streptococcus hemolyticus than EM.The protective effects of AMF against the mice infected by Staphylococcus aureus was better than AM,and both of them have similar effects on the mice infected by Streptococcus hemolyticus.

关 键 词：富马酸阿奇霉素 阿奇霉素 红霉素 体内抗菌活性 半数有效量 半数致死量 化疗指数 

分 类 号：R962[医药卫生—药理学]