Evaluation of hydroxyethyldiclofenac intestinal absorption in rats

The mechanism of intestinal mucosal transport of hydroxyethyldiclofcnac, an ester prodrug of diclofenac, in rats was investigated. Another objective was to identify optimal sites of absorption and then to identify the gastrointestinal toxicity. Both the parent drug and the prodrug were found to be passively absorbed from rat jejunum. The permeability coefficients of the prodrug were tenfold higher [p<0.05] than that of the parent drug in the three regions of rat small intestine [duodenum, jejunum and ileum]. In addition, the prodrug was found to be less ulcerogenic [p<0.05] after single and chronic dose than the parent drug. In conclusion, the prodrug was found a good candidate for oral delivery as compared to parent compound