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目的观察国产司帕沙星、妥舒沙星及其它四种氟喹诺酮类抗菌药对成都地区780株临床分离菌的体外抗菌活性,并比较司帕沙星、妥舒沙星和环丙沙星对金葡球菌、大肠埃希菌和铜绿假单胞菌感染小鼠的体内抗菌活性。方法用琼脂稀释法测定国产司帕沙星和妥舒沙星的MIC50和MIC90,并与其它四种氟喹诺酮类抗菌药进行了比较。本文还测定了抗菌药对金葡球菌、大肠埃希菌和铜绿假单胞菌感染小鼠治疗的ED50。结果体外试验表明司帕沙星和妥舒沙星能有效抑制或杀灭革兰阳性、革兰阴性菌及厌氧菌,显示了广谱抗菌活性。司帕沙星和妥舒沙星对革兰阳性菌的抗菌活性是环丙沙星的2~8倍,氧氟沙星和氟罗沙星的4~16倍,是诺氟沙星的16~32倍。司帕沙星对MRSA的抗菌活性与妥舒沙星相似,但优于环丙沙星、氧氟沙星、氟罗沙星和诺氟沙星。司帕沙星对大多数革兰阴性菌的抗菌活性与环丙沙星和妥舒沙星相似,是氧氟沙星、氟罗沙星和诺氟沙星的2~8倍。两药对厌氧菌的抗菌活性也较环丙沙星强。口服或皮下注射司帕沙星对金葡球菌和大肠埃希菌所致小鼠全身性感染的保护作用优于环丙沙星和妥舒沙星。同一给药途径下司帕沙星对铜绿假单胞菌所致小鼠全身性感染的保护作用与妥舒沙星和环丙沙星相似。三种受试药对金葡球菌和大肠埃希菌所致小鼠全身性感染的保护作用优于铜绿假单胞菌所致感染。结论司帕沙星和妥舒沙星对革兰阳性菌和厌氧菌的体外抗菌活性优于环丙沙星和其它药物,对大多数革兰阴性菌的抗菌活性与环丙沙星相似,但优于其它受试药。司帕沙星对金葡球菌和大肠埃希菌所致小鼠全身性感染的体内保护作用优于环丙沙星和妥舒沙星。同一给药途径下司帕沙星对铜绿假单胞菌所致小鼠全身性感染的保护作用与妥舒沙星和环丙沙星相似。
OBJECTIVE To investigate the in vitro antibacterial activity of domestic sparfloxacin, tosufloxacin and four other fluoroquinolone antibacterials against 780 clinically isolated isolates from Chengdu and to compare sparfloxacin, tosufloxacin and ciprofloxacin In vivo antibacterial activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa-infected mice. Methods The MIC50 and MIC90 of domestic sparfloxacin and tosufloxacin were determined by agar dilution method and compared with the other four fluoroquinolone antibacterials. This article also tested the ED50 of antimicrobial agents for Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa infected mice. Results In vitro tests showed that sparfloxacin and tosufloxacin can effectively inhibit or kill gram-positive, gram-negative bacteria and anaerobic bacteria, showing broad-spectrum antibacterial activity. Sparfloxacin and tosufloxacin antibacterial activity of Gram-positive bacteria is 2 to 8 times that of ciprofloxacin, ofloxacin and fleroxacin 4 to 16 times, is norfloxacin 16 to 32 Times Sparfloxacin MRSA antibacterial activity and tosufloxacin similar, but superior to ciprofloxacin, ofloxacin, fleroxacin and norfloxacin. Sparfloxacin antibacterial activity of most gram-negative bacteria and ciprofloxacin and tosufloxacin similar toloxacin, fleroxacin and norfloxacin 2 to 8 times. Antimicrobial activity of two drugs than ciprofloxacin strong. Sparfloxacin is superior to ciprofloxacin and tosufloxacin for systemic or systemic infection in mice caused by Staphylococcus aureus and Escherichia coli. The same route of administration of sparfloxacin Pseudomonas aeruginosa mice with systemic protective effect of tosufloxacin and ciprofloxacin similar. Three kinds of tested drugs on Staphylococcus aureus and Escherichia coli-induced systemic infection in mice is better than Pseudomonas aeruginosa infection. Conclusion Sparfloxacin and tosufloxacin have better antibacterial activity against gram-positive and anaerobic bacteria than ciprofloxacin and other drugs in vitro, and antibacterial activity against most gram-negative bacteria is similar to ciprofloxacin, But superior to other test drugs. Sparfloxacin against Staphylococcus aureus and Escherichia coli-induced systemic infection in mice in vivo protection than ciprofloxacin and tosufloxacin. The same route of administration of sparfloxacin Pseudomonas aeruginosa mice with systemic protective effect of tosufloxacin and ciprofloxacin similar.