Effect of the Interaction of Drug-β-cyclodextrin Complex with Bile Salts on the Drug Absorption from Rat Small Intestinal Lumen

Abstract

This investigation was concerned with the change of the bioavailabiiity of a drug owing to the interaction of the drug-α -cyclodextrin complex with bile salts in rat intestinal lumen. The absorption of sulfamethizole (SMZ) from rat intestinal lumen after administration of SMZ-α -cyclodextrin complex was determined by a closed-loop method in the presence or absence of bile. The blood level of SMZ after administration of SMZ-cyclodextrin complex was significantly decreased in comparison with that after administration of SMZ alone in bile duct-ligated rats. On the other hand, the blood level of SMZ after SMZ-α-cyclodextrin administration in intact rats (bile duct non-ligated) or on the addition of sodium cholate was similar to the level in the case of SMZ alone. Thus, bile salts were found to act as a competing agent in the gastrointestinal tract. © 1989, The Pharmaceutical Society of Japan. All rights reserved.