Novel chewable colon targeted tablets of bumadizone calcium for treatment of ulcerative colitis: Formulation and optimization

The aim of the present study was the formulation of a novel chewable tablet containing the non-steroidal anti-inflammatory bumadizone calcium (BZ) to deliver the drug to the colon for the local treatment of ulcerative colitis. Colon targeted granules were prepared following 32 full factorial design. The effect of two independent variables, namely, polymer type (Eudragit ® S100, Eudragit ® L100, and a mixture of both in the ratio of 4:1) and drug to polymer ratio (1:1, 1:3& 1:5) on the % of BZ released for 12 h was studied. In order to produce chewability, candidate formulae were then mixed with different amount of maize starch and mannitol, and compressed into tablets. F11 tablets(composed of drug: Eudragit S100 in the ratio of 1:3, 250 mg mannitol and 50 mg maize starch with a desirability of 0.925) achieved the required release profile i.e: lowest release before target area (pH 1.2 & 6.8) reaching only 11.00% at the end of the fourth hour, and 100.27% after 12 h (pH7.4). Histopathological studies results declared clearly the ability of the chewable colon targeted tablets F11 to locally treat acetic acid induced colitis. Furthermore, the measurements of myeloperoxidase enzyme activities in colon specimens showed that F11 achieved a significantly lower levels in comparison to both untreated group and group that received the marketed tablets (p<0.05). © 2016 Elsevier B.V. All rights reserved.