Sesamol, generally regarded as a main antioxidative component in sesame oil, is generated from sesamolin upon roasting of sesame seed or during bleaching process of sesame oil. This investigation studied the bioavailability and excretion of sesamol in Sprague-Dawley rats. After oral administration of sesamol (p.o. 100 mg/kg) to SD rats, the changes in concentration of sesamol were determined in various excreta within 24 h period. Our results showed that sesamol conjugated metabolites were rapidly eliminated from urine and feces in 0-4 h. The majority of intact sesamol glucuronide was excreted in the urine. It is suggested that sesamol conjugated metabolites are primarily eliminated from the plasma via the kidney by active tubular secretion. LC-MS/MS analyses of rat excreta showed that sesamol can be converted to 2-methoxybenzene-1,4-diol and benzene-1,2,4-triol in vivo by rat.