Jornal de Bioequivalência e Biodisponibilidade

Abstrato

Effect of Superdisintegrating Agent and Osmogens on Metronidazole Loaded Colon Targeting Drug Delivery System

Jain CP and Abhishek Kumar Jain

Site-specific drug delivery mainly colon-targeting delivery system is mostly used for the treatment of colonic diseases and provides local delivery of drug for the treatment of colonic diseases like inflammatory bowel disease (ulcerative colitis and crohn’s disease) and colon cancer, where it is necessary to attain high drug concentration. The Site-specific colon targeted system containing metronidazole using various natural biodegradable polymers i.e. guargum, xanthan gum, carragennan and pectin alone or in combination as a coating material. The polymeric films were characterized for their physical appearance, influence of disintegrating agents on the water uptake, hardness, and disintegration time and in-vitro release. In vitro dissolution studies showed that metronidazole bearing tablets coated with polymeric blend containing guar gum, xanthan gum and carrageenan in ethanol: water 50:50 solvent released drug in simulated gastrointestinal conditions mainly at colonic environment. The release of drug was drastically reduced; regression coefficient value r2 and T lag time of the formulations were varied due to presence of disintegrating agents and osmogens. Results indicated that the nature of drug transport of coated formulations showed supercase-II type release. Statistical analysis of release data indicated that release pattern of metronidazole is significantly affected by the nature of polysaccharide used for coating and coating composition. The presence of superdisintegrant/osmotic agent inside core formed time-controlled drug delivery systems that could facilitate drug delivery into different segments of the gastro intestinal tract [GIT] depending upon the coat weight and the type of these agents. The result concluded that the formulations containing superdisintegrating agent (24 mg) showed a best drug delivery system for colon targeting.