Micelle-enhanced spectrofluorimetric method for determination of sitagliptin and identification of potential alkaline degradation products using LC-MS

Luminescence. 2014 Feb;29(1):65-73. doi: 10.1002/bio.2503. Epub 2013 Apr 5.

Abstract

A novel, quick, simple and highly sensitive spectrofluorimetric method was developed and validated for the determination of sitagliptin (SG) in its pharmaceutical formulations. The proposed method is based on investigation of the fluorescence spectral behavior of sitagliptin in an SDS micellar system. In an aqueous solution of phosphate buffer pH 4.0, the fluorescence intensity of SG in the presence of SDS was greatly enhanced, by 200%, i.e. twofold enhancement. The fluorescence intensity of SG was measured at 300 nm after excitation at 270 nm. The method showed good linearity in the range 0.03-10.0 µg/mL with a good correlation coefficient (r = 0.9998). The limits of detection and quantitation values were 5.31 and 16.1 ng/mL, respectively. The proposed method was successfully applied to the analysis of SG in its single and co-formulated commercial tablets; the results were in good agreement with those obtained using a reference method. Application of the proposed method was extended to stability studies of SG after exposure to different forced degradation conditions according to the ICH guidelines, such as acidic, alkaline, thermal, photo- and oxidative stress. The chemical structure of certain potential degradation products (DPs) were investigated using LC-MS.

Keywords: LC-MS; degradation; pharmaceutical preparations; sitagliptin; spectrofluorimetry; stability indicating.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkalies / chemistry*
  • Chromatography, Liquid / methods*
  • Hypoglycemic Agents / analysis*
  • Limit of Detection
  • Mass Spectrometry / methods*
  • Micelles*
  • Pyrazines / analysis*
  • Sitagliptin Phosphate
  • Spectrometry, Fluorescence / methods*
  • Triazoles / analysis*

Substances

  • Alkalies
  • Hypoglycemic Agents
  • Micelles
  • Pyrazines
  • Triazoles
  • Sitagliptin Phosphate