In Vitro Study and Pharmacokinetic Evaluation of Sitagliptin Phosphate Enantiomers in Rat Plasma

Abstract

Background: A chiral HPLC technique was developed to determine sitagliptin phosphate enantiomers in rat plasma in compliance with US FDA regulations. Methods & results: The technique used a Phenomenex column with a mobile phase consisting of a 60:35:5 (v/v/v) blend of pH4, 10-mM ammonium acetate buffer, methanol and 0.1% formic acid in Millipore water. The precision for both (R) and (S) sitagliptin phosphate varied between 0.246 and 1.246%, while the accuracy was 99.6–100.1%. A glucose uptake assay was used to assess enantiomers in 3T3-L1 cell lines through flow cytometry. Conclusion: Investigation of the pharmacokinetic impacts of sitagliptin phosphate racemic enantiomers in rat plasma revealed notable contrasts in R and S enantiomers in female albino Wistar rats, suggesting enantioselectivity for sitagliptin phosphate.