The behavior such as absorption and stability in gastrointestinal tract and the biliary excretion of acemetacin were examined in rats, and compared with those of indomethacin. Acemetacin was absorbed quickly from gastric and intestinal loops. The formation of indomethacin from acemetacin during the permeation across the gastrointestinal tract was small. From the results by using the homogenates of liver, it was assumed that the liver was a main part for the formation of indomethacin. After the intraduodenal administration of acemetacin, unconjugated indomethacin and desmethylindomethacin glucuronide were excreted in 0-24 bile as major metabolites. When indomethacin was administered, conjugated indomethacin was also excreted in bile. Enterohepatic circulation of indomethacin was observed after the administration of acemetacin and indomethacin.