DPP-4 inhibitors (gliptins) have shown a better glycaemic control even in more feeble cases such as elderly people, patients with high cardiovascular and hypoglycaemic risk and individuals with renal impairment. However, the plasma concentrations of selected drugs has to be estimated to correlate those results with various uncertainties during clinical studies. A simple and sensitive LC-QTOF/MS method was developed and validated to measure the human plasma concentrations of vildagliptin, saxagliptin, sitagliptin, linagliptin and teneligliptin, using pioglitazone as internal standard.Chromatographic separation of five gliptins was achieved on a Zorbax Eclipse Plus C-18 column Rapid Resolution HD (50 x 2.1 mm, 1.8 µ) using mobile phase consisting of 20 mM ammonium formate and acetonitrile in gradient mode. Detection was performed with positive ion electrospray ionization mass spectrometry using target ions in selective ion mode. Simpler protein precipitation was employed for sample extraction from human plasma. Low recovery of gliptins observed due to non-specific binding to glass was surpassed by using polypropylene. The mean recovery was found to be 96.82 ± 1.03 % (VIL), 94.32 ± 0.74 % (SAX), 95.37 ± 2.09 % (SIT), 91.67 ± 3.14 % (LIN) and93.29 ± 1.03 % (TEN) respectively. The proposed method will serve as an excellent tool for various clinical studies like therapeutic drug monitoring, pharmacokinetics, toxicological and protein binding studies.
This protocol demonstrates microwave-irradiated monohydroxylation on different heterocycles via C–H functionalization which leads into the development of biologically relevant molecules.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.