Effect of Nonsteroidal Anti-inflammatory Drugs on the Permeability of the Rectal Mucosa

Abstract

The effect of nonsteroidal anti-inflammatory drugs (NSAIDs) on the permeability to marker drugs, sulfanilic acid and creatinine, was investigated in rat rectum using the in situ perfusion technique. Indomethacin (IM), phenylbutanone (PB), diclofenac sodium (DF), and aspirin (ASA) were used as NSAIDs. The permeability-enhancing effect increased in the following order : ASA<PB<DF<IM. The effects were reversible. No marked histological changes were observed and, furthermore, protein release from the rectal mucosa was not increased. On the other hand, there was a good correlation between the permeability-enhancing effect and the NSAID amount accumulated in the rectum. Consequently, it is suggested that the accumulation of NSAID in the rectum plays and important role in the enhancement of the rectal permeability to drugs.