Prediction of Passive Membrane Permeability of Linagliptin

Abstract

Linagliptin is a highly selective inhibitor of dipeptidyl peptidase-4 and therefore clinically utilized to treat adults with type 2 diabetes mellitus. The objective of this study was to predict how the ions normally found in extracellular or intracellular fluids within the body system will influence the linagliptin’s rate of passive diffusion across a cell membrane. The methodology involved measuring linagliptin partition coefficient in a chloroform-water system containing the salts at 25 oC by the shake flask method. The results indicate that at the highest concentration (0.5 M) of the salts studied, sodium chloride was found to give the highest partition coefficient value when compared to the control. In conclusion, physiological ions would have little or no effect on the drug’s molecular state within extracellular or intracellular fluid as the salts failed to significantly alter the partition coefficient of the drug, hence will not alter passive membrane permeability of linagliptin.