In vitro drug release and in vivo human X-ray studies of ileo-cecal targeting budesonide fast disintegrating tablet

Crohn's disease is a type of inflammatory bowel disease that frequently affects the ileo-cecal region of the gastrointestinal tract. For effective treatment of this disease, a site-targeting drug in the ileo-cecal region is essential. Budesonide (BD) is a synthetic, non-halogenated glucocorticoid and is the drug of choice for the treatment of Crohn's disease. The present study is an attempt to develop the dosage form of a BD tablet to achieve targeted drug release in the ileo-cecal region. The BD tablets are coated with Eudragit FS 30 D, which is a polymer that specifically dissolves at and above pH 6.8. The in vitro drug release and in vivo tablet disintegration (using X-ray radiography) were carried out. The coating process was optimized successfully. The in vitro performance of the tablet with coating thickness showed that the tablet did not disintegrate till 4.5 hours, which represents the transit time to the ileo-cecal region. In vivo studies also established that the tablet lasted till 4.5 hours. The tablet containing 0.5% superdisintegrant and 10% coating thickness was able to deliver BD effectively to the ileo-cecal region, thus making it a promising drug delivery system for the treatment of Crohn's disease.