Quantitation of celecoxib and four of its metabolites in rat blood by UPLC-MS/MS clarifies their blood distribution patterns and provides more accurate pharmacokinetics profiles

摘要: A sensitive UPLC-MS/MS method was established and validated for the quantitation of celecoxib its metabolites in rat blood. The analytes were extracted from blood samples by a salting-out liquid-liquid extraction followed UPLC chromatography. mass analysis effluent performed on an API 5500 Qtrap spectrometer via multiple reactions monitoring (MRM). linear response ranges 0.3-20000nM celecoxib, 1.2-20000nM, 0.3-20000nM, 2.0-2000nM, 1.5-6000nM carboxycelecoxib (M2), hydroxycelecoxib (M3), glucuronide (M1), (M5), respectively. inter-day intra-day accuracies within 85-115%, precision acceptable (<12%) all analytes. Recoveries above 70% no obvious matrix effects observed. successfully applied to pharmacokinetics study oral (20mg/kg) Sprague-Dawley rats, concentrations (0-48h) two M2 M3 determined. Using same method, we also showed preferential distributions cells as compared plasma. In conclusion, our results that LC-MS/MS can be used pharmacokinetic studies are very important compartment this drug such profiles whole will more comprehensive accurate representation their vivo than