Diet-controlled blood levels of oltipraz in healthy male subjects.

The bioavailability of the new antischistosomal agent, oltipraz, was examined under three different dietary conditions in seven healthy males. Oltipraz tablets (500 mg) were administered in single doses (25 mg/kg) under fasting conditions, with a low fat meal (less than 5% fat) and a high fat meal (24% fat). The extent and rate of oltipraz bioavailability were significantly increased by concurrent administration of the drug with food, as demonstrated by the increase in the plasma peak concentration, the area under the plasma concentration vs. time curve and the absorption rate constant. The plasma peak concentration was also reached earlier. Oltipraz plasma concentrations, following its administration under fasting conditions, were almost negligible. The likely mechanisms underlining oltipraz-food interaction are discussed.