Studies on Absorption and Excretion of Drugs. V. On the Mechanism of Penetration of Sulfisomezole through the Intestinal Barrier in vitro

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1.The penetration of water and solutes though the intestinal barrier in vitro was investigated with the technique described by Smyth & Taylor. Sulfisomezole concentration in the fluid transported to the serosal surface was higher than that in the mucosal solution. This phenomenon was not observed with sulfathiazole or sulfaguanidine. 2. The uphill transport of sulfisomezole was demonstrated with the technique of Wilson & Wiseman employing everted sacs. 3. In experiments with the technique of Smyth & Taylor the level of sulfathiazole or sulfaguanidine concentration in the transported fluid was maintained approximately constant through the changes of the transport rate of fluid. On the other hand the increase of sulfisomezole concentration in the transported fluid corresponded to the increase of the transport rate of fluid, although the relationship between them was not linear. 4. No particular correlation was observed between the penetration of sulfisomezole and that of sodium ion. 5. It was suggested that the uphill transport of sulfisomezole was explainable from the view-point of pH-partition hypothesis and that 2,4-dinitrophenol might decrease the penetration of sulfisomezole after disturbing the mechanism of physiological pH maintenance at the absorptive surface.
社団法人日本薬学会の論文
1964-12-25