Effect of Pharmaceutical Adjuvants on the Rectal Permeability of Drugs. I. Effect of Pharmaceutical Additives on the Permeability of Sulfaguanidine from the Rat Rectum

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Abstract
The effect of additives such as sodium deoxycholate, sodium lauryl sulfate, disodium EDTA, polyethylene glycol 400 and polysorbate 80 on the rectal permeability was compared by measuring the rectal absorption of sulfaguanidine from the perfused solution and the apparent rectal clearance of i.v. injected sulfaguanidine in the rat. The absorption and apparent rectal clearance of sulfaguanidine in the rat rectum were increased by the addition of these additives, except for the lower concentration of polyethylene glycol 400. There was a very favorable correlation between the increasing ratio of apparent absorption rate and ratio of apparent rectal clearance of sulfaguanidine. The simultaneous change in permeability in both directions (rectum to blood, blood to rectum) was clarified. The cause was apparently due to a histological change in the tissue of the rectum, and these changes differed according to the natures of the additives.