Effect of enzyme dependent polymers on the release profile of press coated esmeprazole colon targeted tablets

• Published in: Research journal of pharmacy and technology 2020-12, Vol.13 (12), p.6186-6194
• Main Authors: Thulluru, Ashok, Mahammed, Nawaz, Basha, S. Shakir, Mohan, K. Siva Jagan, Saravanakumar, K., Kumar, Ch. S. Phani
• Format: Article
• Language: English
• Subjects: Bioavailability; Caustic soda; Colon; Disease; Enzymes; Hydrochloric acid; Lactose; Polymers; Potassium; Sodium
• ISSN: 0974-3618; 0974-360X; 0974-306X
• DOI: 10.5958/0974-360X.2020.01079.3

The present study was aimed to formulate press-coated tablets of Esmeprazole for colon targeted delivery (EZCT). Press coated tablets aids to prevent the gastric degradation of drugs, there by improves its oral bioavailability. Various enzyme dependent polymers (pectin, xanthan gum and guar gum) were selected for extending the drug release by press coating the drug incorporated core tablets. Fourier Transform Infrared (FTIR) analysis was performed to check the compatibility of drug and polymers. Core and coating compositions were evaluated for pre- and post-compression studies. In vitro release studies were performed in three dissolution media without rat caecal content medium (RCCM) for first 2 h in 0.1 N HCl, next 3 h in pH 6.8 phosphate buffer and then for last 7 h in pH 7.4 phosphate buffer (total 12h). In vitro drug release studies, revealed that the tablets coated with enzyme dependent polymers showed no drug release up to initial 5 h, indicating cid Protection of EZ due to solid dispersion with MgO. The lead formulations with higher conc. (27.8%w/w) of enzyme dependent polymers extends the release of EZ up to 12 h with a better zero order release profile (r2 ~ 0.999), hence they are selected to perform the dissolution with RCCM, for to simulate the colonic environment. Among all the batches, EZCT9 (27.8% w/w guar gum), drug release kinetics fitted best to the zero order (r2=0.999); its drug release process is predominantly by diffusion and the mechanism of diffusion is by non-Fickian process in with and without RCCM, hence it is selected as optimized one. Optimized formulation (EZCT9) passes the test for stability as per ICH guidelines. Press coated colonic targeted EZ tablets were successfully developed with an aim to increase oral bioavailability and decrease production costs.