Effect of the interaction of drug-beta-cyclodextrin complex with bile salts on the drug absorption from rat small intestinal lumen.
This investigation was concerned with the change of the bioavailability of a drug owing to the interaction of the drug-beta-cyclodextrin complex with bile salts in rat intestinal lumen. The absorption of sulfamethizole (SMZ) from rat intestinal lumen after administration of SMZ-beta-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-beta-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-beta-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.
Nakanishi
K
K
Masada
M
M
Nadai
T
T
Miyajima
K
K
D000818:Animals; D001647:Bile Acids and Salts / Q000032:analysis*; D003505:Cyclodextrins / Q000032:analysis; D066298:In Vitro Techniques; D007408:Intestinal Absorption; D007421:Intestine, Small / Q000378:metabolism; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013419:Sulfamethizole / Q000032:analysis / Q000493:pharmacokinetics*; D013432:Sulfathiazoles / Q000493:pharmacokinetics*; D047392:beta-Cyclodextrins
D001647:Bile Acids and Salts; D003505:Cyclodextrins; D013432:Sulfathiazoles; D047392:beta-Cyclodextrins; D013419:Sulfamethizole; C031215:betadex