Formulation development and Evaluation of Colon Specific Delivery System of Anti- amoebic Drug (Tinidazole) using different Polysaccharide carriers

Abstract

Amoebiasis is an infection of the large intestine caused by Entamoeba histolytica. Tinidazole is the preferred drug used in the treatment of intestinal amoebiasis. The conventional tablet dosage form provides minimal amount of drug in the colon with undesirable adverse effect due to variation in the transit time. Hence, to target the drug directly to the site of action in the colon, there is need to develop colon targeted drug delivery systems that will enhance the therapeutic drug level, increases the bioavailability of active medicament and reduce the dose of drug. The fast disintegrating core tablet of Tinidazole was prepared by direct compression method. The core tablet was evaluated for hardness, thickness, Friability, weight variation, drug content, in vitro disintegration time and in vitro drug release studies. Using the optimized formulation (C3), different formulations (F1-F6) of coated tablet was prepared by using different polymers like chitosan and xanthan gum. The formulated coated tablet were evaluated for various parameters like for hardness, thickness, Friability, weight variation, drug content, swelling study and in vitro dissolution study. The optimized formulation F3 shows 6.24% drug release in Stomach and Small Intestine and maximum drug release up to 96.53% in the colon. The kinetic data analysis of formulations indicated that it fits to Korsmeyer -Peppas Model and follows zero order release kinetics. The mechanism of drug release from the tablet followed non-Fickian (super case-11) transport. The stability studies of the optimized formulation were investigated as per ICH guidelines. There were no significant changes in thickness, hardness, weight variation, friability, drug content and in vitro drug release. These findings suggest that compression coated tablet using polysaccharide carriers provide more site specific delivery, reduced degradation and release of drug in stomach and small intestine.