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新喹诺酮类抗菌药左氟沙星(Levofloxa-cin,DR3355)是消旋体氧氟沙星的光学异构体[S-(-)-氧氟沙星].它对一般细菌的抗菌谱与氧氟沙星相同.而抗菌活性为氧氟沙星的2倍.以氧氟沙星为首的一部分新喹诺酮类抗菌药具有优良的体外抗结核杆菌活性,而且在临床上也是有效的.因此研究了左氟沙星的体外抗结核杆菌活性.在进行左氟沙星的药物敏感性试验时,同时以氧氟沙星和司帕沙星作为对照药.首先将各药物100mg用0.1mol/L NaOH溶解,再以灭菌的精制水稀释后,加到1%小川培养基,制备成含有5、2.5、1.25和0.63ug/ml药物浓度的小川培养基.另将由患者痰中分离得到的结核杆菌菌株置于小川培养基上培养2～3周后制成2mg/ml的菌悬液,吸取0.025ml(菌量0.05mg)接种到含有药物的小川培养基上.进行培养和评价抗结核杆菌活性.氧氟沙星在2.5μg/ml浓度时20株中有20株(100%),在1.25μg/ml时,20株中有10株(50%)的生长被完全抑制.左氟沙星在1.25μg/ml浓度时20株中有20株(100%),0.63μg/ml时20株有5株(25%)的生长被完全抑制.左氟沙星的体外抗结核杆菌活性约为氧氟沙星的2倍.然而司帕沙星在0.63μg/ml时20株中17株(85%)的生长被完全抑制.左氟沙星的抗结核杆菌活性没有超过司帕沙星.对于氧氟沙星耐药菌株,左氟沙星在5μg/ml浓度时14株?
The new quinolone antibacterial agent Levofloxa-cin (DR3355) is an optical isomer of ofloxacin [S - (-) - ofloxacin] Ofloxacin the same, while the antibacterial activity of ofloxacin 2 times. Ofloxacin as part of the new quinolone antibacterials have excellent anti-tuberculosis activity in vitro and is also clinically effective. Therefore, the study Levofloxacin in vitro activity of anti-tuberculosis in the drug susceptibility testing of levofloxacin, both ofloxacin and sparfloxacin as a control drug.First, each drug 100mg with 0.1mol / L NaOH dissolved, and then diluted with sterile purified water, added to 1% Ogawa medium, prepared containing 5,2.5,1.25 and 0.63ug / ml drug concentration Ogawa medium will be separated from the patient’s sputum tuberculosis Bacillus strains were placed on the Ogawa culture medium for 2 to 3 weeks after the formation of 2mg / ml of bacterial suspension, 0.025ml (0.05mg) were inoculated to drug-containing Ogawa medium for culture and evaluation of anti-tuberculosis bacilli Ofloxacin at 2.5μg / ml concentration of 20 out of 20 (100%) at 1.25μg / ml, 20 out of 10 (50%) growth was completely inhibited.Lefloxacin 20 (100%) out of 20 at 1.25 μg / ml and 5 out of 20 (25%) at 0.63 μg / ml were completely grown Inhibition of levofloxacin in vitro activity of anti-tuberculosis is about 2 times of ofloxacin.While sparfloxacin at 0.63μg / ml 20 out of 17 strains (85%) of the growth was completely inhibited .Left fluorine The activity of anti-tuberculosis bacitracin did not exceed that of sparfloxacin.For the ofloxacin-resistant strains, of levofloxacin at the concentration of 5μg / ml 14 strains?