国产氧氟沙星的药理评价

PHARMACOLOGICAL EVOLUA TION OF OFLOXACIN

本文报道了氧氟沙星的体外抗菌活性,小鼠感染细菌保护作用,急性毒性和致畸试验。氧氟沙星对革兰氏阳性和阴性细菌抗菌活性与诺氟沙星相似,而强于依诺沙星、洛美沙星和吡哌酸。小鼠分别感染金葡球菌和大肠杆菌,本品保护效果与环丙沙星相似,优于诺氟沙星和依诺沙星;小鼠感染绿脓杆菌,本品逊于环丙沙星和依诺沙星,而优于诺氟沙星。小鼠口服、静脉、肌肉和皮下给药LD50分别为3467mg/kg、329mg/kg、>600mg/kg和>3000mg/kg。小鼠胚胎器官分化期给药未见致畸胎作用。

Antibacterial activities,in vitro and in vivo, acute toxicity and teratogenic test of ofloxacin were studied. Ofloxacin showed a broad spectrum activities against Gram-positive and negative bacteria. The antibaterial activity of ofloxacin was similar to that of norfloxacin and superior to those of enoxacin, lomefloxalin and pip-emidic acid. Ofloxacin uas highly effective with infections due to S. aureus and E. coli in mice and superior to those of norfloxacin and enoxacin. The protective effect of ofloxacin infected with P. aerugin-osa in mice was inferior to those of ciprofloxacin and enoxacin and superior to norfloxacin. The LD_(50) values of ofloxacin were, 3467mg/ kg(PO), 329mg/kg(IV), more than 600mg/kg(IM)and more than3000mg/ kg(SC)in mice, respectively. Ofloxacin was negative with teratogenic test in mice.