Yoshizumi S, Domon H, Miyazaki S, Yamaguchi K
Department of Microbiology, Toho University School of Medicine, Tokyo, Japan.
Antimicrob Agents Chemother. 1998 Apr;42(4):785-8. doi: 10.1128/AAC.42.4.785.
The in vivo activity of HSR-903, a new fluoroquinolone, against major bacteria which cause respiratory tract infections was evaluated. HSR-903 was active against experimental respiratory tract infections in mice challenged with penicillin-susceptible and penicillin-resistant Streptococcus pneumoniae and Haemophilus influenzae strains. Treatment with HSR-903 reduced the bacterial numbers in infected murine lungs. In accord with the pulmonary clearance results, the rates of survival for mice treated with HSR-903, sparfloxacin, levofloxacin, ciprofloxacin, and benzylpenicillin were 50, 30, 10, 0, and 0%, respectively, 14 days after being infected with penicillin-resistant S. pneumoniae. A pharmacokinetic study with pneumonic mice showed that the levels of HSR-903 in the lungs were seven to eight times higher than those in the plasma. These results indicate that clinical studies of HSR-903 against respiratory tract infections may be warranted.
对新型氟喹诺酮类药物HSR-903针对引起呼吸道感染的主要细菌的体内活性进行了评估。HSR-903对受到青霉素敏感和耐药肺炎链球菌以及流感嗜血杆菌菌株攻击的小鼠实验性呼吸道感染具有活性。用HSR-903治疗可减少感染小鼠肺部的细菌数量。与肺部清除结果一致，在用耐青霉素肺炎链球菌感染14天后，接受HSR-903、司帕沙星、左氧氟沙星、环丙沙星和苄青霉素治疗的小鼠的存活率分别为50%、30%、10%、0%和0%。对肺炎小鼠的药代动力学研究表明，肺部的HSR-903水平比血浆中的水平高7至8倍。这些结果表明，HSR-903针对呼吸道感染的临床研究可能是必要的。
