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Effect of Competing Anions on Binding of Bile Salts by Cholestyramine
Authors:Kos  Rosemary  White  Joe L  Hem  Stanley L  Borin  Marie T
Institution:(1) Department of Industrial and Physical Pharmacy, Purdue University, West Lafayette, Indiana, 47907;(2) Department of Agronomy, Purdue University, West Lafayette, Indiana, 47907;(3) The Upjohn Company, Kalamazoo, Michigan, 49001;(4) School of Pharmacy, Purdue University, West Lafayette, Indiana, 47907
Abstract:The binding of bile salts by cholestyramine may be influenced by other anions, as the Langmuir adsorption coefficients for three bile salts tested were similar to the model anion, citrate. However, the selectivity coefficient indicated preferential binding of cholate anion in comparison to citrate anion. Binding experiments confirmed cholestyramine's preference for bile salts as the presence of other anions reduced but did not prevent the binding of cholate anion. Binding of cholate anion was reduced in direct relationship to the citrate anion concentration. Prior exposure of cholestyramine to citrate anion caused the binding of cholate anion to decrease slightly. Sequential exposure of cholestyramine to simulated gastric fluid and simulated intestinal fluid containing cholate anion resulted in a decrease in cholate binding which was attributed to competition with anions present in the gastrointestinal fluids. Components of tomato juice and orange juice, fluids commonly used to enhance ingestion of cholestyramine, also reduced the binding of cholate anion.
Keywords:cholestyramine  bile salt binding  competitive binding
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