Butyrospermol, a minor yet important compound in camellia oil, has anti-inflammatory effects. However, its absorption, elimination, and the influence of oil on its bioavailability remain unclear. This study investigated the logP, stability in simulated digestive fluids and liver tissue, absorption parameters of different forms of butyrospermol, and binding of butyrospermol to the Niemann-Pick C1-like 1-N-terminal domain (NPC1L1-NTD). Results indicated that butyrospermol remained stable in the simulated gastric and intestinal fluids but underwent degradation in rat liver tissue. The bioavailability of the butyrospermol suspension was low owing to its poor water solubility. Unexpectedly, the bioavailability of butyrospermol in oil was also low. This was due to incomplete emulsification and the inhibitory effects of other triterpene alcohols in the oil, which prevented butyrospermol from binding to NPC1L1-NTD. Our study provides theoretical insights into the functional application of butyrospermol and calls for further investigations into its bioactivity and that of camellia oil.