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Pharmacokinetics and safety of sitafloxacin after single oral doses in healthy volunteers
- Source :
- Int. Journal of Clinical Pharmacology and Therapeutics. 52:1037-1044
- Publication Year :
- 2014
- Publisher :
- Dustri-Verlgag Dr. Karl Feistle, 2014.
-
Abstract
- 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 sitafloxacin 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 Cmax were 0.72, 1.62, and 2.73 μg/mL and the mean of AUClast were 3.97, 8.71, and 18.03 μg x h/mL, respectively. Sitafloxacin was rapidly absorbed, reaching Cmax ranged from 0.85 to 1.21 hours. The terminal half-life ranged from 5.19 to 6.28 hours. The Cmax 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.
- Subjects :
- Adult
Male
Pharmacology
Volume of distribution
Sitafloxacin
Cross-Over Studies
business.industry
Cmax
Administration, Oral
Crossover study
Healthy Volunteers
Anti-Bacterial Agents
Pharmacokinetics
Area Under Curve
Healthy volunteers
Humans
Medicine
Female
Pharmacology (medical)
Dosing
Geometric mean
business
Fluoroquinolones
medicine.drug
Subjects
Details
- ISSN :
- 09461965
- Volume :
- 52
- Database :
- OpenAIRE
- Journal :
- Int. Journal of Clinical Pharmacology and Therapeutics
- Accession number :
- edsair.doi.dedup.....106d046875c1ab8388845c148b20c141