新キノロン薬grepafloxacinの動物感染モデルにおける投与法の検討

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  • Administration method of a new quinolone antibiotic, grepafloxacin, in an animal infection model

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The administration method of a new quinolone antibiotic, grepafloxacin (GPFX), was examined in a neutropenic mouse thigh-infection model. As compared with ofloxacin (OFLX), GPFX showed a stronger antibacterial effect and longer effective regrowth time against Staphylococcus aureus infections. The antibacterial effect of OFLX on Klebsiella pneumoniae was superior to that of GPFX, but regrowth was soon observed due to its short half-life (T1/2). GPFX, in spite of differences in administration times, did not cause an extremely increased or decreased number of bacteria, and showed a slightly better result after 24 hours than OFLX. Concerning its pharmacokinetics in mice, GPFX had a lower Cmax and longer T1/2 in plasma than OFLX. In addition, GPFX showed less AUC in plasma but almost equal AUC in muscle tissues as compared with OFLX. These results indicate that GPFX has a long T1/2 in plasma and excellent penetration into tissue.

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