DOI: 10.36347/SAJP.2019.v08i11.004

Pages: 488-496

Pharmaceutical excipients improve the safety and homogeneity of pharmaceutical drugs, and, thus, increase their usefulness. By definition, pharmaceutical excipients must not disturb the influence of medical therapy with drugs; however, some have been shown to affect epithelial membrane proteins and induce changes in the structure of tight junctions and function of drug transporters, which may alter the disposition of drugs. To clarify alterations in the absorption behavior of drugs by pharmaceutical excipients, the present study examined the effects of pharmaceutical excipients on membrane transport via the transcellular route, which is the main membrane permeation route for lipophilic drugs. The effects of twenty common pharmaceutical excipients from different classes on the mucosal membrane were also investigated, and variations in these effects between different regions of the small intestine were assessed. The in vitro sac method was employed to examine the effects of pharmaceutical excipients on the membrane permeation of -naphthol in the rat jejunum and ileum. -Naphthol is a drug that permeates through the transcellular route. The membrane permeability of -naphthol was significantly altered under the dosage conditions of pharmaceutical excipients. Furthermore, the effects of pharmaceutical excipients were site-specific (jejunum and ileum) in the small intestine. The present results demonstrated that some pharmaceutical excipients altered membrane permeability via the transcellular route in the rat small intestine.