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Effect of pharmaceutical adjuvants on the rectal permeability to drugs. IV. Effect of pharmaceutical adjuvants on the rectal permeability to macromolecular compounds in the rat.

The effect of adjuvants such as sodium deoxycholate (SDC), sodium lauryl sulfate (SLS), disodium ethylenediaminetetraacetate (EDTA) and tetracycline hydrochloride (TC) on the permeability to water-soluble compounds with various molecular weights through the rat rectal membrane was evaluated by using an in situ technique. Creatinine, 14C-inulin, 125I-insulin, 125I-polyvinylpyrrolidone and 125I-albumin were selected as marker drugs. Significant increases in the permeability of the rectal membrane to the marker drugs were observed in the cases of SDC and SLS. On the other hand, the effect of EDTA, and especially TC, became smaller as the molecular weight of the marker drugs increased. The order of effectiveness of adjuvants on the permeability was SDC>SLS>EDTA>TC.