Formulation and Comparative Release Kinetic Study of Dexamethasone Matrix Tablets on Colon Targeting

Abstract: In the present study guar gum based matrix tablet of dexamethasone were prepared as colon - targeted drug delivery system for prevention of inflammatory bowel disease. Matrix tablets with different proportion of gum:drug were prepared by direct compression technique. In-vitro release kinetic studies of formulations were performed with and without caecal content for 24 hrs and compared against the control and with the immediate release formulation. Release study for immediate release tablets were carried out in 0.1 N HCl (2h). The cumulative percent of Dexamethasone released from formulations at different time periods with and without rat caecal contents (control) was compared. All the matrix tablets showed zero order release kinetics.It was concluded that the formulations prolonged the release of drug effectively and thus can be used to target dexamethasone to colon.
 
Introduction
The treatment of several colonic diseases (ulcerative colitis and crohn's disease). Corticosteroids have traditionally formed the basis of treating inflammatory bowel disease. However chronic treatment of inflammatory bowel disease with steroids, while often effective, is plagued by a number of serious side-effects (e.g. acne, moonface, striae, hypertension, peptic ulcer, impaired glucose tolerance and mood disturbances. If these undesired side effects could be overcome or markedly reduced in both subchronic and chronic dosing regimes. Corticosteroids would have the potential of being ideal therapeutic treatments of inflammatory bowel disease.
 
A potential matrix material for colonic drug delivery is guar gum. Owing to its high viscosity, this polysaccharide may be capable to carry certain drugs to the large intestine without appreciable release in the stomach or small intestine. Once in the large intestine, the guar gum matrix is degraded by specific enzymes produced by the gut microflora (i.e, a-galactosidases and b-mannanase) to initiate drug release.
 
The anti-inflammatory property of Dexamethasone is useful in the treatment of inflammatory bowel diseases (IBD). 75mg of Dexamethasone is equivalent in anti-inflammatory activity to about 5mg of Prednisolone for inflammatory bowel diseases (IBD).

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