论文部分内容阅读
balofloxacin(Q-35)是在喹啉环的7位上由甲氨基哌啶基取代,8位由甲氧基取代的新化合物.其分子式为C_(20)H_(24)FN_3O_4·H_2O,分子量为425.46.白色～微黄色结晶性粉末,无臭、味苦、熔点180～183℃,水溶液pH7.27.本品对革兰阳性菌和阴性菌以及厌氧菌具有广抗菌谱.特别对耐甲氧西林金葡菌(MRSA)的抗菌作用强.血液中的半衰期为7～8h,原药由尿中排泄,48h的尿中排泄率为70%～86%.对中枢神经、呼吸、循环系统的影响比氧氟沙星稍弱,对幼犬的关节软骨的毒性也比氧氟沙星小,光毒性,与非类固醇抗炎药或茶硷并用使痉挛诱发作用减弱.食物对其吸收的影响小.
Balofloxacin (Q-35) is a novel compound substituted by methylaminopiperidyl and 8-methoxy in the 7-position of quinoline ring, and its molecular formula is C 20 H 24 FN 3 O 4 · H 2 O, molecular weight 425.46 white ~ yellowish crystalline powder, odorless, bitter taste, melting point 180 ~ 183 ℃, aqueous solution pH7.27. This product has a wide range of Gram-positive bacteria and anaerobic bacteria and antibacterial spectrum. The antibacterial activity of methicillin-resistant Staphylococcus aureus (MRSA) is strong, with a half-life of 7-8 h in blood, excretion of the original drug from the urine and urinary excretion of 70-86% over 48 h. Systematic effects weaker than ofloxacin slightly, the puppies articular cartilage toxicity than ofloxacin, phototoxicity, and non-steroidal anti-inflammatory drugs or theophylline with spasm-induced weakening effect of food on its absorption Little effect.