LVFX与四种氟喹诺酮类药物的抗菌活性比较

1、    LVFX与四种氟喹诺酮类药物的抗菌活性比较        提要利用微量二倍稀释法测定左旋氧氟沙星(LVFX)对167株临床常见致病菌的体外抗菌活性，并与4种氟喹诺酮类药物进行比较。结果表明，5种氟喹诺酮药物对多数受试菌有较强的抗菌活性。关键词左旋氧氟沙星体外抗菌活性 ANTIBACTERIAL ACTIVITIES OF LEVOFLOXACIN ANDOTHER 4 FLUOROQUINOLONES IN VITROLin CaiLuo DongZhong L

2、52;hua(Department of Pharmacy,Southwest Hospital, Third Military Medical CollegeChongqing 400038)ABSTRACTThe antibacterial activity of levofloxacin (LVFX) against 167 clinical isolates was examined in vitro and compared with other 4 fluoroquinolones with broth microdilution method. The results showe

3、d that 5 fluoroquinolones exhibited high activity against mast of isolates. The MIC50 of LVFX against Strepticoccus was 1 g/ml, LVFX inhibited 50% of P.aeruginosa, S.aureus, E.coli,N.gonorrhoeae and K.Poneumoniae at a concentration of 0.5 g/ml. The MIC90 of LVFX ranged from 0.5 to 32 g/ml.LVFX was c

4、omparable to Ciprofloxacin against P.aeruginosa、N.gonorrhoeae and E.coli,and more active than Ciprofloxacin against S.aureus,Streptococcus and K.pneumoniae. LVFX was 28 times of Ofloxacin, and was 216 times of Norfloxacin and Lomefloxacin in the activity.Key WordsLevofloxacinAntibacterial activities

5、 in vitro左旋氧氟沙星(levofloxacin，LVFX，可乐必妥)为新型喹诺酮类广谱抗菌药。可用于呼吸道、外科、妇科、皮肤科感染等。现将左旋氧氟沙星对临床常见致病菌的体外抗菌活性进行测定并与其它4种喹诺酮类药物进行比较。1实验部分1.1药品、菌株和培养基左旋氧氟沙星、氧氟沙星(ofloxacin,OFLX，泰利必妥)(日本第一制药株式会社)；环丙沙星(ciprofloxacin,CPLX，南京药科大学制药厂)；洛美沙星(lomefloxacin,LMLX)、诺氟沙星(norfloxacin,NFLX)(西南合成制药厂)。所用临床分离菌株均由第三军医大学西南医院检验科细菌室分离鉴定，

6、其中金黄色葡萄球菌68株、绿脓假单胞菌28株、大肠艾希氏菌22株、淋病萘瑟氏菌19株、肺炎克雷伯氏菌12株、链球菌18株、共计167株；质控菌用金黄色葡萄球菌ATCC25923、大肠艾希氏菌ATCC25922。MH培养基(液体、固体，中国药品生物制品检定所)；淋球菌培养基(广西桂林皮肤病研究所)；链球菌的培养用5%脱纤维兔血加入MH培养基。1.2方法与结果1.2.1最小抑菌浓度(MIC)测定淋球菌采用平皿二倍稀释法，其它细菌采用微量二倍稀释法测定MIC。于含有系列浓度药液的96孔板中，加入菌液(最终浓度为105C FU/ml)，37培养18 h，未见细菌生长的最低浓度为其最小抑菌浓度。5种氟喹

7、诺酮类药物对6种临床常见致病菌的MIC结果见表1。Table 1The MIC of 5 fluoroquinolones against clinical isolatesOranism(No.of strains)DrugMIC50(g/ml)MIC50(g/ml)MIC range(g/ml)S.aureus(68)LVFX0.540.532CPLX0.5320.5128LMLX2640.5128NFLX0.5640.5128OFLX0.580.5128P.aeruginosa(28)LVFX0.50.50.51CPLX0.50.50.564LMLX240.5128NFLX0.50.50

8、.51OFLX0.510.51N.gonorrhoeae(19)LVFX0.2520.1252CPLX0.520.1252LMLX4160.12532NFLX140.1254OFLX1160.12516E.coli(22)LVFX4320.564CPLX4320.532LMLX321280.5128NFLX8640.5128OFLX16320.564Streptoccus(18)LVFX120.54CPLX240.54LMLX4160.532NFLX4160.516OFLX4818K.pneumoniae(12)LVFX0.510.51CPLX0.520.52LMLX0.540.54NFLX0

9、.540.532OFLX0.520.5641.2.2最低杀菌浓度(MBC)测定取MIC测定中未见细菌生长的微孔中培养液0.1 ml，接种于不含抗菌药物的MH琼脂平皿表面，37再孵育18 h，未见细菌生长的最低药物浓度为最低杀菌浓度。5种氟喹诺酮类物的MBC结果见表2。 Table 2The MBC of 5 fluoroquinolones(g/ml)Organism(strains)LVFXCPLXLMLXNFLXOFLXMIC90MBC90MIC90MBC90MIC90MBC90MIC90MBC90MIC90MBC90S.aureus(20)4832646412864128816P.aer

10、uginosa(10)0.540.542160.5418E.coli(10)816616323232641632Streptoccus(10)248888848K.pneumoniae(10)0.510.522411142讨论2.1LVFX对试验菌有良好的抗菌活性，对金黄色葡萄球菌、绿脓假单胞菌、肺炎克雷伯氏菌、淋球菌的MIC50均0.5 g/ml，对链球菌的MIC50为1 g/ml。对大肠艾希氏菌的MIC90为32 g/ml，对其它细菌的MIC900.58 g/ml。2.2LVFX与其它几种药物比较，对绿脓假单胞菌、淋球菌和大肠艾希氏菌的抗菌活性与CPLX相当，对金黄色葡萄球菌、链球菌和肺炎

11、克雷伯氏菌的抗菌活性比CPLX强。LVFX对试验菌的抗菌活性为OFLX的28倍，与文献1报道一致。LVFX的抗菌活性为NFLX和LMLX的216倍。与文献2比较，几种药物的MIC90都有所上升，可能与该类药物在临床广泛应用有关。2.3由MBC结果可见，LVFX、CPLX、LMLX、NFLX、OFLX对大肠艾希氏菌、链球菌、肺炎克雷伯氏菌、金黄色葡萄球菌的MBC90为MIC90的14倍，对绿脓假单胞菌的MBC90为MIC90的8倍。 作者单位：第三军医大学西南医院药剂科重庆 400038参考文献1Isao Haykawa, Shohgo Atarashi, Shuichi Yokohama, et al. Synthesis and antibacterial activities of optically active ofloxacin. The Japaness Journal of Antibit