Formulation and evaluation of pectin-HPMC mesalamine tablets coated with eudragit l 100 for ulcerative colitis

[摘要] The potential of Eudragit L 100 as protective for drug in acidic environment and effectiveness of pectin for the sustained drug release has been demonstrated. Due to solubility and swelling properties of pectin in aqueous media, it is frequently coated with acid resistant polymers for targeting drugs to the colon. The aim of this study was to prepare and evaluate mesalamine matrix tablets containing pectin as bacterially-degradable and bioactive polysaccharide in combination with HPMC K4M which acts agonistically in the drug release.Wet granulation method was used for the preparation of tablets. 60 % of pectin was used and different combinations were prepared with polymers. Optimised formulation was selected and another same formulation was prepared and tried without Eudragit L 100 coat.Then the formulations were evaluated for various parameters like weight variation, friability, drug content, drug release etc.Formulations containing highest amount of pectin exhibited sustained drug release than the remaining formulations. Formulation without Eudragit L 100 coat has released the entire drug within 4 h as it had no protective coat for acidic pH. Formulations with highest amount of HPMC K4M showed poor flow properties due to sticking property caused by hydrophilic polymer. Formulation with highest amount of HPMC K4M showed highest swelling than the other formulations.Formulation containing pectin and HPMC K4M in the ration of 6:1 coated with Eudragit L 100 was a promising formulation for the targeted and sustained drug delivery to the colon.

[学科分类] 药理学