Pharmacokinetics and safety of sitafloxacin after single oral doses in healthy volunteers

摘要

Objective: Sitafloxacin is a new fluoroquinolone with a broad spectrum of antibacterial activity, including grampositive and gram-negative bacteria. This study was to evaluate the pharmacokinetic characteristics of a single dose of sitalloxacin in healthy Chinese volunteers. Methods: This was a single-center, open-label, randomized-sequence study conducted in 12 subjects. Subjects were randomly assigned to receive single doses of 50, 100, and 200 mg of sitafloxacin in a 3-way crossover design with a 7-day washout period between administrations. Quantification was carried out using a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method. Pharmacokinetic parameters were calculated and analyzed statistically. Safety assessments were conducted throughout the study. Results: After administration of single doses of 50, 100, and 200 mg, geometric mean estimate for sitafloxacin C-max were 0.72, 1.62, and 2.73 mu g/mL and the mean of AUC(last) were 3.97, 8.71, and 18.03 mu gxh/mL, respectively. Sitafloxacin was rapidly absorbed, reaching C-max ranged from 0.85 to 1.21 hours. The terminal half-life ranged from 5.19 to 6.28 hours. The C-max and AUC(last) were proportional to the doses. The mean clearance, the half-life, and the volume of distribution were constant, irrespective of the dose. Conclusion: In healthy Chinese subjects, single dosing of sitafloxacin resulted in linear plasma pharmacokinetics.