Development, Formulation and Evaluation of 5 Fluorouracil Tablet as a Viable Colon Targeted Drug Delivery System using Compression Coat of Polymer(s)
Considering limitation of pH dependent system and time dependent system, microbial degradation at the required site is effective for treatment. Solventless compression coating is one of the strategies for delivering drugs to the colon based on microbial degradation. The aim of the research was to develop a polymer based compression coated tablet of 5-Fluorouracil and to identify the most suitable polymer either alone or in combinations for colonic delivery. Core tablets of 5-Fluorouracil were compression coated with various proportions of Guar gum, Xanthum gum and Chitosan. Further, 32 full factorial designs were devised using coat weight and proportion of polymers in coat as variables. Drug release studies were performed in simulated gastric fluid (SIG) for 2 hours followed by simulated intestinal fluid (SIF) up to 24 hours, demonstrating that the rate of drug release is dependent upon the nature and concentration of polymer and the pH of environment. The coat containing guar gum or xanthum gum alone showed 30-40% drug release in 8 hours in SIF while guar gum with xanthum gum showed 30-35% drug release in 8 hours in SIF. The coat containing all three polymers showed 45 to 50% drug release in SIF. Further, in vitro dissolution studies performed in the dissolution media with 2% rat ceacal content showed significantly increased drug release because of microbial polysaccharidase enzyme.