Research Laboratories, Toyama Chemical Co. Ltd., 4-1, Shimookui 2-chome, Toyama 930-8508, Japan. MASAHIRO
Int J Antimicrob Agents. 2011 Sep;38(3):226-30. doi: 10.1016/j.ijantimicag.2011.04.017. Epub 2011 Jul 2.
In this study, garenoxacin showed potent in vitro activity against clinical isolates of group G Streptococcus dysgalactiae subsp. equisimilis [minimum inhibitory concentration for 90% of the organisms (MIC(90)) = 0.125 μg/mL] and was superior to levofloxacin (MIC(90) = 1 μg/mL) and moxifloxacin (MIC(90)=0.25 μg/mL). In experimental pneumonia caused by group G S. dysgalactiae subsp. equisimilis in mice, the effective dose for 50% survival (ED(50)) of garenoxacin following single oral administration was 1.87 mg/kg, >10.7-fold and 4.6-fold less than the ED(50) values of levofloxacin (>20 mg/kg) and moxifloxacin (8.54 mg/kg), respectively. The area under the free serum concentration-time curve from 0-24 h (fAUC(0-24))/MIC ratio of garenoxacin in serum following oral administration of 20 mg/kg was 73.2, which was 8.7-11.4-fold and 1.4-fold greater than that of levofloxacin (6.44-8.46) and moxifloxacin (51.4), respectively. These results suggest that garenoxacin has potential for the treatment of infectious diseases caused by S. dysgalactiae subsp. equisimilis.
在这项研究中,加替沙星对无乳链球菌群 G 血清型菌株表现出强大的体外活性[对 90%的微生物的最小抑菌浓度 (MIC90) = 0.125 μg/mL],优于左氧氟沙星 (MIC90 = 1 μg/mL) 和莫西沙星 (MIC90 = 0.25 μg/mL)。在无乳链球菌群 G 血清型菌株引起的实验性肺炎小鼠模型中,单次口服加替沙星的 50%有效剂量 (ED50) 为 1.87 mg/kg,分别比左氧氟沙星 (>20 mg/kg) 和莫西沙星 (>8.54 mg/kg) 的 ED50 值低>10.7 倍和 4.6 倍。口服 20 mg/kg 加替沙星后血清中的游离血清浓度-时间曲线下面积 (fAUC0-24)/MIC 比值为 73.2,分别是左氧氟沙星 (6.44-8.46) 和莫西沙星 (51.4) 的 8.7-11.4 倍和 1.4 倍。这些结果表明,加替沙星具有治疗无乳链球菌群 G 血清型菌株引起的感染性疾病的潜力。