Pharmacokinetics of Pazufloxacin Mesilate Sodium Chloride in healthy Chinese volunteers after intravenous injection

doi:10.5246/jcps.2019.01.005

Abstract

Abstract:

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 C_max for each dosage group was 2.37±0.89, 4.27±0.74 and 10.74±4.06 mg·mL^–¹, respectively; and the AUC_0→∞was 3.24±1.2, 5.89±1.51 and 13.32±2.35 mg·h·mL^–¹, respectively. In addition, T_max 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 AUC_0→∞, C_max 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 AUC_0→∞, C_max and dosage over the range of 150–600 mg.

Key words: Pazufloxacin Mesilate, Accumulative urine excretion rate, RP-HPLC, Pharmacokinetics

CLC Number:

R969.1

Supporting:

Wenjuan OuYang, Yalan Zhang, Pingsheng Xu, Zhiyong Dai, Hongying Ma, Qun Qin. Pharmacokinetics of Pazufloxacin Mesilate Sodium Chloride in healthy Chinese volunteers after intravenous injection[J]. Journal of Chinese Pharmaceutical Sciences, 2019, 28(1): 40-48.

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