In the present study, we aimed to investigate the pharmacokinetics and dosage proportionality for a single, intravenous utilization of Pazufloxacin Mesilate Sodium Chloride, an injectable synthetic fluoroquinolone antibacterial agent, in healthy Chinesevolunteers.In this open-labeled, three-dosage parallel study, subjects were randomized to receive a single dose of Pazufloxacin Mesilate at 150, 300 or 600 mg (n = 10, 10 and 10, respectively) administered as a 30-min intravenous infusion. Blood and urine samples were serially collected from 0 to 24 h after drug administration. Moreover, the sample’s drug concentrations were analyzed via validated RP-HPLC method.Subjects receiving a single dose of Pazufloxacin Mesilate 150, 300 or 600 mg were in accordance with the two compartment model. The Cmax for each dosage group was 2.37±0.89, 4.27±0.74 and 10.74±4.06 mg·mL–1, respectively; and the AUC0→∞ was 3.24±1.2, 5.89±1.51 and 13.32±2.35 mg·h·mL–1, respectively. In addition, Tmax for groups treated with 150, 300 and 600 mg was 0.48±0.08, 0.50±0.00 and 0.53±0.08 h, respectively. The correlation analysis for AUC0→∞, Cmax and dosage suggested that pazufolxacin mesilate displayed dose proportion at the dose ranging from 150 to 600 mg. The data suggested that all three different dosage regimens fit with the two compartment model. Meanwhile, it presented a linear correlation between AUC0→∞, Cmax and dosage over the range of 150–600 mg.
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