Effect of surfactants on absorption through membranes IV: effects of dioctyl sodium sulfosuccinate on absorption of a poorly absorbable drug, phenolsulfonphthalein, in humans.

To explore the effect of dioctyl sodium sulfosuccinate on drug absorption in humans, the urinary excretion of a poorly absorbable drug, phenolsulfonphthalein, administered in solution with and without the surfactant was determined. Coadministration of a therapeutic dose of the surfactant with the drug solution resulted in a significant increase in the initial rate of absorption. A small increase in the extent of absorption was also observed. Pretreatment with the surfactant for 6 nights, followed by administration of the drug on the 7th day, did not significantly change the rate of extent of absorption. The surfactant is thought to have a direct effect on the GI membrane, resulting in a temporary change in its permeability. This effect appears to be reversible after a few hours.