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本文研究了环丙氟哌酸的体外抗菌作用、体内保护作用、小鼠和大鼠一次给药的半数致死量和安全试验。结果表明,环丙氟哌酸对革兰氏阴性菌的MIC范围为0.005～0.19μg/ml,抗菌活性强于氟哌酸、氟啶酸和吡哌酸;对革兰氏阳性菌的 MIC为0.045～1.50μg/ml,其抗革兰氏阳性菌活性明显强于上述对照药。小鼠分别感染金葡球菌、大肠杆菌和绿脓杆菌后的半数有效量明显优于氟哌酸、氟啶酸和吡哌酸。小鼠一次给药的半数致死量,口服LD_(50)为2991.52mg/kg; 静脉为223.88mg/kg;肌肉和皮下的LD_(50)分别为831.08mg/kg和1133.42mg/kg. 大鼠口服LD_(50)>5000mg/kg,静脉LD_(50)>200mg/kg;肌肉和皮下分别为>1000mg/kg和>1200mg/kg。狗口服50mg/kg日服三次为期2日和口服100mg/kg日服一次为期7日,未见毒性反应和功能改变,也未见病理组织学变化。
In this paper, in vitro antibacterial effects of ciprofloxacin, in vivo protection, half-lethality and safety trials of once-administered mice and rats were studied. The results showed that the MIC range of Ciprofloxacin to Gram-negative bacteria was 0.005-0.19 μg / ml, and its antibacterial activity was stronger than that of norfloxacin, flunarizine and pipemidic acid. The MIC to gram-positive bacteria was 0.045 ~ 1.50μg / ml, the activity of Gram-positive bacteria was significantly stronger than the above reference drug. The effective dose of mice infected with Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa was significantly superior to norfloxacin, fiuidic acid and pipemidic acid. The LD50 of oral administration was 2991.52 mg / kg for oral administration and 223.88 mg / kg for intravenous administration. The LD 50 of muscle and subcutaneous administration were 831.08 mg / kg and 1133.42 mg / kg respectively Oral LD_ (50)> 5000mg / kg, intravenous LD_ (50)> 200mg / kg; muscle and subcutaneous> 1000mg / kg and> 1200mg / kg respectively. Dog oral administration of 50mg / kg three times a day on the 2nd and 100mg / kg orally for a period of 7 days, no toxic reactions and functional changes, and no histopathological changes.