Factors Influencing Absorption and Excretion of Drugs. VI. Effect of Sodium Cholate on in Situ Rat Intestinal Absorption of Buformin

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The effect of sodium cholate on the absorption of strongly basic drug, buformin, was studied in the in situ rat small intestinal loops. In cases of either jejunum or ileum, the absorption of buformin significantly increased above the critical micelle concentration of sodium cholate. Since sodium cholate had little effect on the physico-chemical property such as the apparent partition coefficient of buformin, it became evident that the enhancement of buformin absorption was not caused by the intraluminal effect of the bile salt. The absorption of buformin was also enhanced in the jejunal and ileal loops pretreated with sodium cholate. On the absorptive surface, sodium cholate did not increase the affinity of buformin to the intestinal mucosal surface. In addition, the release of membrane components such as protein, total phosphorus, and phospholipid from the intestine was accelerated to greater extent by sodium cholate. From these results, it is suggested that sodium cholate alters the composition of the in situ rat intestinal membrane by producing a release of membrane components from the intestinal tissues, resulting in an increase in the permeability of the small intestine to buformin.
公益社団法人日本薬学会の論文
1977-06-25