Abstract

Objective: The objective of this study was to develop and optimize a microflora-triggered colon targeted sustained-release dosage form using Gum Ghatti (GG) and Hydroxypropyl Methylcellulose (HPMC K100).

Methods: GG and HPMC K100 were used to prepare microflora triggered colon targeted sustained- release dosage form. For evaluation, two different tablets comprising metoprolol succinate and mesalamine as an active ingredient were used with the objective of developing a platform technology for various categories of drugs. The tablets were coated with Eudragit® L100 and Eudragit® S100 to provide enteric coating and evaluated for hardness, thickness, friability, weight variation, disintegration, and drug content. in vitro release studies for the prepared tablets were carried out mimicking the physiological transit time. Further, the effects of microflora were evaluated using rat cecal content.

Results: The in vitro dissolution profile of coated matrix tablets showed that 86.03±0.43% of metoprolol succinate and 80.26±0.67% of mesalamine were released at the end of 12 h. The ex vivo dissolution profile of coated matrix tablets showed that 96.50±0.27% of metoprolol succinate and 92.58±0.39% of mesalamine were released at the end of 12 h in the presence of rat ceacal content. The developed formulation was stable when subjected to the standard ICH stability study conditions.

Conclusion: The result of this study showed that gum ghatti together with hydroxypropyl methylcellulose could be successfully used for the preparation of microflora-triggered colon targeted matrix tablets.

Keywords: Gum ghatti, matrix tablet, mesalamine, metoprolol succinate, sustained release, oral drug delivery.

Graphical Abstract