国产替考拉宁体内外抗菌作用研究

Study on the antibacterial activity of teicoplanin in vitro and in vivo

目的 为了评价国产替考拉宁对 5 10株临床分离菌的体内外抗菌活性 ,并与进口产品替考拉宁及万古霉素进行比较。方法 采用琼脂二倍稀释法和试管二倍稀释法测定药物的最低抑菌浓度 (MIC)及最低杀菌浓度 (MBC)。结果 国产替考拉宁的抗菌活性与万古霉素相似或略强。其对MRSA和MSSA的MIC50 分别为 4、1mg/L ,对MRSE和MSSE的MIC50 分别为 1、0 5mg/L。对所试大多数菌株MIC50 为 0 0 6～ 4mg/L,与进口的替考拉宁的抗菌活性无显著差异 ,替考拉宁在 2～ 4MIC浓度时呈杀菌作用。替考拉宁的MIC值随接种菌量增加升高 2～ 8倍 ,受 pH和血清浓度影响不大。体内保护试验表明 ,替考拉宁静脉和皮下给药对金葡球菌 98192 5、肺炎链球菌 9813 5和肠球菌 980 4所致小鼠全身感染的ED50 分别为 0 5 9、0 3 8、0 17mg/kg(静脉注射 )和 1 0 8、0 87、0 3 6mg/kg(皮下注射 )。其体内抗菌作用比万古霉素强 6～

The in vitro and in vivo antibacterial activity of domestic teicoplanin against 510 clinical isolates was compared with vancomycin and imported teicoplanin. Method The minimal inhibitory concentration (MIC) of teicoplanin was determined by the agar dilution method, minimal bactericide concentration (MBC) were measured by tube dilution method. Results The antibacterial activity of teicoplanin was similar or superior to that of vancomycin. The MIC 50 of teicoplanin against MRSA and MSSA was 4mg/L and 1mg/L respectively; Its MIC 50 against MRSE and MSSE was 1mg/L and 0 5mg/L respectively . There was no difference between the antibacterial activity of domestic teicoplanin and that of imported teicoplanin. The result of in vitro bactericide activity showed the MBC of teicoplanin was 2～4 higher than its MIC against the detected bacteria. The MIC of teicoplanin increased with increasement of the inoculum size; pH and concentration of serum protein did not affect the in vitro activity of teicoplanin. Its protective effects in systemic infections in mice were 6～12 times more potent than that of vanomycin, as active as that of imported teicoplanin. Its ED 50 against mice infected with S.aureus, Streptococcus pneumoniae and Enterococcus faecalis were 0 59, 0 38, 0 17mg/L by iv and were 1 08, 0 87, 0 36mg/L by s.c respectively.