氟哌酸前药IMB—85210的药效与毒理

PHARMACOLOGICAL STUDY OF NORFLOCACIN PRODRUG-IMB-85210

氟哌酸前药IMB-85210的药效学和毒理学研究表明,在体外对革兰氏阴性菌和革兰氏阳性菌的活性比氟哌酸和甲氟哌酸为弱,但对感染肺炎杆菌和金葡球菌小鼠的效果(ED_(50))比氟哌酸强1.7倍和2.4倍;对感染大肠杆菌和绿脓杆菌小鼠的效果比氟哌酸强1.4倍,小鼠和大鼠口服LD_(50)>400mg/kg;致畸胎试验和致突变试经均为阴性。结果表示,IMB-85210的动物保护效果明显强于氟哌酸,而毒性低,是值得进一步研究的新药。

IMB-85210 is a new norfloxacin prodrug with in vitro and in vivo activities. In vitro activity of IMB-85210 was less than norfloxacin and pefloxacin against gram-negative and gram-positive bacteria. In the experimental infected Mice, the efficacy of IMB-85210 was similar with pefloxacin and more effective than norfloxacin. The LD50 values in mice and rats were >4000 mg/kg (po), respectively. Teratogenity test and dominant lethal test in mice were negative. These results suggest that IMB-85210 would be worthy to study further.