Exchange Resins as Therapeutic Bile Acid Sequestrants

Ion-Exchange Resins as Therapeutic Bile Acid Sequestrants 

The feeding of the bile acid-binding polymeric amines, cholacrylamine resin and cholestyramine resin, causes lowering of blood cholesterol in experimental animals (22), and in human subjects (58). These substances are 

Cholestyramine resin in the form of glycocholate or taurocholate salts did not inhibit cholesterol rise in plasma in cholesterol-fed cockerels (22), presumably because these forms of resin were already saturated with bile acids and could not take up more. The stearate salts of cholestyramine resins, however, were fully active. The therapeutic effectiveness of the resin depends on the selectivity between the bile salt anions and the chloride anion as well as the capacity for the organic ion. Studies have therefore been made (18, 19) to determine the separation factors for these ions on various resins in order to investigate some of the properties of the resin that are responsible for the high affinity of the large organic ions for the ion-exchange resins. Since the number of equivalents of cholate anion bound were equal to the number of equivalents of chloride ion released by the resin, within the limits 

With advance in our knowledge of the physical chemistry of bile acids and lipids, it may be possible to synthesize resins with still greater selectivity in vivo than cholestyramine, should this method prove to be an effective longterm therapeutic measure. The administration of cholestyramine to guinea pigs induces cholelithiasis (62) and isolated incidents of adverse affects have been reported in the clinical literature following long-term treatment with the resin (63). 

In addition to clinical use, cholestyramine has been employed in metabolic research to increase the turnover rate of the bile acid pool in the rat (64). 

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C. Ion-Exchange Resins as Therapeutic Bile Acid Sequestrants... 

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