Mechanism of Drug Absorption from Micellar Solution. II. Effect of Polysorbate 80 on the Absorption of Micelle-free Drugs

概要

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Effect of Polysorbate 80 on the intestinal absorption of nine micelle-free drugs was examined in the rat. Regardless of the ionic nature of the compounds, two levels of the effect were observed, namely an absorption enhancing effect at relatively low concentration range and a small inhibitory effect at higher concentrations of the surfactant. Pretreatment of the gut with the surfactant, mucosal uptake, and other absorption experiments revealed that the surfactant adsorbed onto the mucosal surface exerted an absorption modifying effect. Absorption promoting and inhibiting effects may be operative at the same time within the concentration range of the surfactant investigated and the observed net absorption modifying effect dependent on the relative magnitude of each. Absorption enhancing effect was dependent on the surfactant-mucosal surface contact time and increased steadily with the time after pretreatment with Polysorbate 80. Absorption studies on sulfisoxazole from the different segments of the intestine provided evidence that the enhancing effect of Polysorbate 80 could be explained by the degree of saturation of the surfactant on the mucosal surface regardless of the regions of the intestine.
公益社団法人日本薬学会の論文
1974-03-25