The therapeutic effect of pazufloxacin mesilate (PZFX mesilate), a new parenteral quinolone, against systemic infection with
Pseudomonas aeruginosa S-406 in mice was evaluated and compared with that of ciprofloxacin (CPFX) and ceftazidime (CAZ).
1. The 50% effective dose (ED
50) of PZFX mesilate administered in a single dose and divided into 2 doses, and 4 doses, was 0.0991, 0.161, and 0.239mg/mouse, respectively. The ED
60 of PZFX mesilate and CPFX was significantly increased by divided administration (P<0.05), but that of CAZ decreased significantly (P<0.05).
2. Whether given in a single or divided dose, the C
max/MIC ratios in serum at the ED
50s were the same for each fluoroquinolone. The AUC
0-24h/MIC ratios of PZFX mesilate were similar to those of CPFX in each dosing regimen.
3. The ED
50 of PZFX mesilate and CPFX administered 7-hours post-infection was 2.20 times and 7.11 times, respectively, higher than at 1-hour post-infection. With the high inoculum size, ED
50 values of PZFX mesilate and CPFX were 35.3 times and 53.6 times, respectively, higher than with the low inoculum size. The ED
50 values of CPFX were more influenced than those of PZFX mesilate with both delayed treatment and high inoculum size.
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