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国产麻保沙星的毒性及体外抗菌活性研究
张玲玲1, 潘 安2, 郭 宽1
1.南京农业大学 动物医学院;2.浙江国邦药业有限公司
摘要:
[目的]探讨国产麻保沙星的毒性作用,及其对常见临床分离菌的抑菌效果,评价其临床用药安全性.[方法]设计了国产麻保沙星对小鼠的经口急性毒性试验、精子畸形试验、微核试验、亚慢性毒性试验, 来研究其毒性,并采用微量稀释法检测麻保沙星的体外抑菌活性.[结果]国产麻保沙星经口LD50为887.8 mg/kg,属低毒类化合物;其致精子畸形与小鼠骨髓微核试验结果均为阴性,表明其无致突变作用.国产麻保沙星按178,89和18 mg/kg剂量连续灌胃30 d,小鼠未见死亡,各用药组较阴性对照组体质量增加差异不显著(P>0.05),对脏器系数、血常规指标、血液生化指标有显著影响(P<0.05),但均在正常值范围之内.体外抑菌试验表明,乳酸麻保沙星对临床分离的鸡、猪大肠杆菌,鸭李氏杆菌,猪链球菌和金黄色葡萄球菌很敏感,其最小抑菌浓度(MIC)均小于0.5μg/mL,最小杀菌浓度(MBC)均小于4μg/mL.[结论]国产麻保沙星按临床剂量使用安全,临床常见菌对其敏感.
关键词:  国产麻保沙星  昆明种小鼠  LD50  致突变性  亚慢性毒性  体外抑菌活性
DOI:
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基金项目:国家“十一五”科技支撑计划项目(O200812)
Research on the toxicity and antibacterial activity in vitro of homemade marbofloxacin
Abstract:
【Objective】 The study was to find out the toxicity and antibacterial activity of homemade marbofloxacin and evaluate the clinical danger.【Method】 Acute oral toxicity test,acute toxicity test,sperm abnormality test,bone marrow micronucleus test and subchronic toxicity test were carried out with mice,and simultaneously microdilution test was used to evaluate antibacterial activity against bacterial strains from clinic.【Result】 The LD50 of homemade marbofloxacin was 887.8 mg/kg,belonging to hypotoxicity substance;the results of sperm abnormality test and bone marrow micronucleus test were negative,indicating marbofloxacin was non mutagenicity.Marbofloxacin was given to mice at doses of 178,89,18 mg/kg by oral administration for 30 days respectively,and no mouse died.No significant differences were observed in body weight(P>0.05),while light effects on organ coefficients,hematology indices,blood biochemical indices(P<0.05),which were in normal value.Antibacterial activity test showed that marbofloxacin inhibited efficiently chick and pig Escherichia coli,duck Listeria monocytogenes,Streptococcus,Staphylococcus aureus,and MIC was all under 0.5μg/mL,MBC under 4μg/mL. 【Conclusion】 Homemade marbofloxacin is safe at the clinical recommendation dosage and sensitive to common bacteria.
Key words:  marbofloxacin  Kunming mouse  LD50  mutagenicity  subchronic toxicity  antibacterial activity in vitro

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