Sesamol, generally regarded as the main antioxidative component in sesame oil, can be generated from sesamolin by roasting sesame seed or bleaching sesame oil. This paper reports the bioavailability of sesamol in Sprague-Dawley (SD) rats. Biological fluid was sampled following a dose of sesamol of 50 mg/kg by gastric gavage (p.o.) or by intravenous injection. The pharmacokinetic data of sesamol were calculated by noncompartmental model. The tissue distribution of sesamol (p.o., 100 mg/kg) in SD rats was also investigated. The concentration changes of sesamol were determined in various tissues and plasma within a 24 h period after oral administration of sesamol. The results showed that the oral bioavailability of sesamol was 35.5 +/- 8.5%. Sesamol was found to be able to penetrate the blood-brain barrier and go through hepatobiliary excretion. Sesamol conjugated metabolites were widely distributed in SD rat tissues, with the highest concentrations in the liver and kidneys and the lowest in the brain. It is postulated that sesamol is incorporated into the liver first and then transported to the other tissues (lung, kidneys, and brain). The major metabolites of sesamol distributed in the lung and kidney were glucuronide and sulfate.