Abstract

Intestinal absorption characteristics of atenolol (AT) were measured by the plasma concentrations after oral and small intestinal administrations and monitoring its disappearance from in situ intestinal loops in anesthetized rat. Relative AUC of AT after oral administration in rat was 24% as compared to AUC value of intravenous administration. However, relative AUC for small intestinal administration in the anesthetized rat was 76%. Following administration of AT into duodenal, jejunal and ileal loops, AUC calculated from blood levels was 705, 613, and 838μg·min/ml, respectively, and the order was consistent with the absorption rate.Disappearance rate constants were 3-0.5h-1. The result shows that there is no difference in absorption from each segment of intestine. Rat intestinal AT transport showed concentration dependency, especially up to 25μg/ml in the mucosal medium, in an experiment using in vitro everted rat intestinal sac prepared from duodenum, jejunum and ileum.

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