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It was clearly shown that colestipol hydrochloride inhibits lymphatic absorption of not only endogenous but also exogenous cholesterol and triglyceride in thoracic duct cannulated rats. Inhibition of cholesterol absorption by colestipol hydrochloride was effectively blocked by administration of cholic acid. It was also suggested that colestipol hydrochloride inactivates bile acids which are essential for cholesterol absorption in the intestinal tract. Administration of colestipol hydrochloride to fasted rats decreased bile flow and biliary secretion of cholesterol and bile acids and increased fecal excretion of bile acids bound to colestipol hydrochloride. These results show that colestipol hydrochloride binds bile acids in the intestinal tract and interferes with bile acids reabsorption.

Effects of colestipol hydrochloride on cholesterol and bile acids absorption in the rat intestinal tract.