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Objective: The aim of the study was to observe the characteristic of permeation of capsaicin across jejunum, ileum and colon in the rat, and to investigate the role of transient receptor potential cation channel (TRPV1).The interaction of capsaicin with P-glycoprotein (P-gp), multidrug resistance-associated protein 2 (MRP2) and breast cancer resistance protein (BCRP) was also investigated.