Butanoic acid is beneficial in the maintenance of colon health, and is the preferred energy substrate for the cells in the colon. Here, butanoic acid was covalently attached to β-cyclodextrin through ester linkage using sodium hydride as the deproton reagent, and the preliminary release behavior of butanoic acid in the colonic contents of rats was investigated at 37 °C. Butanoic acid was almost released 57.3% from the β-cyclodextrin conjugate after 12 h in the colonic contents of rats, via the biodegradation by glycosidases and hydrolases in the colon. This fact demonstrates that β-cyclodextrin could act as a carrier for an orally administered colon-targeting delivery of butanoic acid as a nutrient.