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本文报道国产偶氮甲基利福霉素(FCE22250)对临床分离的357株革兰氏阳性、阴性菌体外抗菌活力及体内保护作用的研究。并与利福平、利福定和利福喷丁的抗菌活力进行比较。实验结果表明:偶氮甲基利福霉素对革兰氏阳性菌中的表葡球菌和金葡球菌的抑菌活力最强,在0.0005~0.125μg/ml浓度即可抑制73.96%的试验菌;对链球菌的抑菌活力不如金葡球菌好,MIC_(50)为2μg/ml;其次是粪链球菌和肠球菌。MIC_(50)均为8μg/ml。FCE22250对革兰氏阴性菌中的绿脓杆菌、大肠杆菌及肠杆菌属中的产气杆菌、阴沟杆菌亦均具有一定的抑菌活力,≤32μg/ml浓度即可抑制80%以上的试验菌,在0.25~16μg/ml浓度下可抑制所试的全部痢疾杆菌和伤寒杆菌。 偶氮甲基利福霉素体外抗金葡球菌的活力与利福喷丁一致,略低于利福平和利福定;对青霉素和甲氧西林耐药的金葡球菌敏感;在体内对金葡球菌感染具有很好的治疗活性。皮下与口服给药的ED_(50)分别为0.1和0.007mg/kg。体内抗金葡球菌的活力FCE22250不及福利平。
This article reports the in vitro antibacterial activity and in vivo protective effect of domestic azo-methyl-rifamycin (FCE22250) on 357 Gram-positive and -negative bacteria. And compared with the antibacterial activity of rifampin, rifadin and rifapentine. The experimental results showed that azo-methyl-rifamycin had the strongest antibacterial activity against Staphylococcus epidermidis and Staphylococcus aureus in the Gram-positive bacteria, and inhibited 73.96% of the test bacteria at the concentration of 0.0005-0.125 μg / ml ; Streptococcus antibacterial activity is not as good as Staphylococcus aureus, MIC_ (50) is 2μg / ml; followed by Streptococcus faecalis and Enterococcus. MIC 50 was 8 μg / ml. FCE22250 against Gram-negative bacteria Pseudomonas aeruginosa, Escherichia coli and Enterobacter aerogenes, cloacae also have a certain antibacterial activity, ≤ 32μg / ml concentration can inhibit more than 80% of the test bacteria , At a concentration of 0.25 ~ 16μg / ml all tested Shigella and Salmonella typhi. Azithromycin in vitro activity of anti-Staphylococcus aureus consistent with rifapentine, slightly lower than rifampin and rifampin; penicillin and methicillin-resistant Staphylococcus aureus sensitive; in vivo gold Staphylococcus aureus infection has a good therapeutic activity. The ED 50 of subcutaneous and oral administration were 0.1 and 0.007 mg / kg, respectively. In vivo activity of Staphylococcus aureus FCE22250 less than the welfare flat.