Development of Colon Targetted Produg of Etodolac - Tapa blanda

Sinopsis

In the present study carboxylic group of Etodolac, responsible for gastric side effects, was masked temporarily not only to overcome the side effects but also to achieve colon specific delivery. Amide prodrug (Etodolac-glycine conjugate) was synthesized by coupling Etodolac with glycine The synthesized prodrug was characterized by melting point, thin layer chromatography, RM values, scanning electro microscopy, x-ray diffraction crystallography and High performance liquid chromatography. Aqueous solubilities and lipophilicity (log P) values were determined at different pH media namely HCl buffer pH 1.2, acid phthalate buffer pH 4.0, phosphate buffer pH 6.8 and pH 7.4. In vitro reversion of Etodolac-glycine conjugate to Etodolac was done at different pH including colonic environment. In vitro reversion, showed prodrug to remain intact in all the other tested pH except colonic pH, where the colonic microfloral enzymes (amidase) hydrolyzed Etodolac-glycine conjugate amide linkage, releasing the free drug.

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