Formulation and Characterization of Expandable Tablet of Diacerein using Swellable Polymers

Abstract

Some of the drugs have poor absorption because of a narrow absorption window in the gastrointestinal tract (GIT). To improve the absorption of such drugs in the GIT, gastro-retentive drug delivery techniques play an important role. Diacerein is an antirheumatic drug used for joint pain and arthritis. The expandable gastro-retentive tablets were prepared to attain an extended therapeutic action of Diacerein. Expandable tablets were formulated to prolong gastric retention, enhance the bioavailability of the drug candidate and attain a desirable size greater than the diametric size of the pyloric sphincter (i.e., 13 mm in diameter) of the tablet after administration by expandable technique. The expandable tablet was formulated using swellable polymers and polyelectrolytes, i.e., HPMCK 100, PEO, chitosan, and carbopol. The proposed expandable tablets were evaluated by preliminary evaluation parameters, micromeritic investigations, all physicochemical evaluations including swelling index, weight variation, drug content, in-vitro release studies and their release kinetics. Method: The wet granulation method is used for the preparation of expandable tablets of Diacerein. Result: The release of Diacerein from all formulations was studied in phosphate buffer pH 1.2 at 37±5°C. The net results conclude that the formulation having HPMC K 100, PEO with the addition of carbopol (formulation C1) showed the maximum swelling index as compared to others. And it was found that formulation C1 is the most superior and reliable formulation in terms of all physicochemical parameters and in-vitro drug release studies. The best formulation obtained from in-vitro drug release studies was shown.
 Keywords: Gastro retentive, expandable system, noval drug delivery system, controlled drug delivery system, gastric transit time, swellable polymers, GIT.