Human plasma exposure level of gatifloxacin eye gel / 中国药学杂志

ABSTRACT

OBJECTIVE: To determine gatifloxacin in human plasma, and study the exposure characteristics of gatifloxacin in Chinese healthy male volunteers who used Gatifloxacin Eye Gel for 7 d. METHODS: LC-MS/MS method was developed for the quantitation of gatifloxacin in human plasma After protein precipitation with methanol and dilution with water, the chromatographic separation was carried out on an Symmetry C18 column (4.6 mm × 100 mm, 5 μm) with a gradient mobile phase consisting of 0.1% formic acid in methanol and 0.1% formic acid in water at a flow rate of 0.5 mL · min-1. The quantitation analysis was performed using multiple reaction monitoring (MRM) at the specific ion transitions of m/z 376.2→261.0 for gatifloxacin and m/z 332.1→-288.1 for ciprofloxacin (internal standard) in the positive ion mode with electrospray ionization (ESI) source. Specificity, linearity, precision and accuracy, matrix effects, recovery and stability were investigated to validate the LC-MS/MS method. Plasma samples of different times from 10 Chinese healthy male volunteers were determined, who used Gatifloxacin Eye Gel for 7 d. RESULTS: The linear range was 2 -500 ng · mL-1. The intra- and inter-day precisions were less than 2.61% and 13.1%, and the accuracy was within ±5.0%. Matrix effective, recovery, specificity and stability were within ± 15.0%. The concentration of gatifloxacin in human plasma was below the lower limit of quantitation (2 ng · mL-1). CONCLUSION: This method is sensitive and accuracy for the determination of gatifloxa-cinin human plasma, and the plasma gatifloxacin level are all below the lower limit of quantitation (2 ng · mL-1) in all subjects.