Determination of febuxostat in human plasma using ultra‐performance liquid chromatography tandem mass spectrometry

Abstract

A rapid and sensitive liquid chromatography-tandem mass spectrometry method has been developed and validated for the determination of febuxostat in human plasma. The liquid-liquid extraction technique was used for the extraction of febuxostat from human plasma using trandolapril as the internal standard (IS). Chromatography was performed on a ultra-performance liquid chromatography (UPLC) BEH C18, 50 mm X 2.1 mm, 1.7 µm particle size column, with the mobile phase consisting of 0.1% formic acid and acetonitrile (in a 25:75 ratio), followed by detection using mass spectrometry. The method involves a simple reversed isocratic chromatography condition and mass spectrometry detection, which enables detection at sub-microgram levels. The method was validated and the lower limit of quantification for febuxostat was found to be 0.075 µg/ml. The mean recovery for febuxostat ranged from 100.9 to 106.5%. This method increased the sensitivity and selectivity; resulting in high-throughput analysis of febuxostat using commercially available IS for pharmacokinetic, bioavailability, and bioequivalence studies, with a chromatographic run time of 1.5 min only.

Simultaneous determination of febuxostat and its three active metabolites in human plasma by liquid chromatography–tandem mass spectrometry and its application to a pharmacokinetic study in Chinese healthy volunteers

“…HPLC with fluorescence detection (HPLC-FD) [7,8] and LC-MS/MS [9][10][11][12] methods have been previously developed to determine febuxostat in human plasma for pharmacokinetic study of febuxostat. The quantification of metabolites 67M-1, 67M-2 and 67M-4 in human plasma has been accomplished by two groups of researchers using LC-MS/MS methods [6,8].…”

Bioanalysis of Febuxostat in Human Plasma by Liquid Chromatography/Tandem Mass Spectrometry

“…It inhibits xanthine oxidase, thus reducing production of uric acid in the body [1,2] . Febuxostat was well tolerated at once-daily doses of 10-240 mg. Febuxostat on oral administration, rapidly absorbed and reach maximum plasma concentration around 0.5-1.3 h. Febuxostat was extensively metabolised and renal function did not seem to play an important role in its elimination from the body Few LC-MS/MS methods [5][6][7][8] have been reported for Febuxostat quantification in plasma. The author Vakaet al, 2013 [5] published a method for the determination of febuxostat in human plasma with a run time of >5 min.…”

Green Electroanalytical Method for Fast Measurement of Xanthine Oxidase Inhibitor Febuxostat

“…Only a few analytical methods have been described for the determination of FBX, including LC-MS methods for pharmacokinetic applications, [12][13][14][15] HPLC methods with UV detection applied in bioequivalence studies, 16,17 stability-indicating MEKC 18 and RP-HPLC methods 19,20 for quantification in pharmaceutical formulation, spectrofluorometry, 21 HPTLC and spectrophotometry. 22 Compared with those methods, electrochemical techniques have several advantages such as simplicity, low-cost, short analysis time and high sensitivity.…”