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3-偶氮甲基利福霉素又称FCE22250,在国内首先由四川抗菌素工业研究所研制成功,本文报道它的体内外抗结核菌活性及其在小鼠体内血药浓度的变化。 实验表明:(一)FCE22250对人型结核分枝杆菌H37Rv的抑菌作用与利福平、利福喷丁相近或略强。(二)FCE22250体内抗结核菌活性显著强于利福平,略优于利福喷丁。(三)FCE22250呈显著长效抗结核活性,给小鼠一次灌胃12mg/kg其抗结核活性的有效浓度可维持10～12天,而利福平在同样条件下最长维持1天,利福喷丁可维持7天。(四)FCE22250的小鼠血浆半衰期达37.7小时,利福平为4.0小时,利福喷丁为31小时。FCE22250给小鼠灌胃12mg/kg,9天后血浆中药物浓度的实测值为0.19微克/毫升(仍可达到其体外最小抑菌浓度)。FCE22250是迄今血浆半衰期最长的抗结核菌药物。
3-azo-methyl-rifamycin, also known as FCE22250, was first successfully developed in China by the Sichuan Institute of Antibiotics, and its anti-TB activity in vivo and in vitro as well as its plasma concentration in mice were reported in this paper. Experiments show that: (a) FCE22250 on human Mycobacterium tuberculosis H37Rv antibacterial effect and rifampicin, rifapentine similar or slightly stronger. (B) FCE22250 in vivo anti-TB activity was significantly stronger than rifampin, slightly better than rifapentine. (C) FCE22250 showed significant long-acting anti-tuberculosis activity, once a mouse intragastric administration of 12mg / kg effective concentration of its anti-TB activity can be maintained for 10 to 12 days, and rifampin in the same conditions up to 1 day, Lee Fu Ben Ding can be maintained for 7 days. (D) FCE22250 mouse plasma half-life of 37.7 hours, rifampin for 4.0 hours, rifapentine for 31 hours. FCE22250 was given intragastrically to mice at a dose of 12 mg / kg. After 9 days, the measured value of the drug concentration in plasma was 0.19 μg / ml (the minimum inhibitory concentration in vitro was still achievable). FCE22250 is by far the longest plasma half-life of anti-tuberculosis drugs.