AISSMS College of Pharmacy, Kennedy Road, Pune, Maharashtra, India.
Drug Dev Ind Pharm. 2009 Jul;35(7):788-95. doi: 10.1080/03639040802596204.
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.
克罗恩病是一种炎症性肠病，常影响胃肠道的回肠-结肠区域。为了有效治疗这种疾病，在回肠-结肠区域需要一种靶向药物。布地奈德（BD）是一种合成的、非卤代的糖皮质激素，是治疗克罗恩病的首选药物。本研究旨在开发一种 BD 片剂的剂型，以实现回肠-结肠区域的靶向药物释放。BD 片剂用 Eudragit FS 30 D 包衣，这是一种在 pH 值 6.8 及以上时会特异性溶解的聚合物。进行了体外药物释放和体内片剂崩解（使用 X 射线摄影）研究。成功优化了包衣工艺。具有包衣厚度的片剂的体外性能表明，片剂直到 4.5 小时才崩解，这代表了到达回肠-结肠区域的转运时间。体内研究也证实，片剂持续了 4.5 小时。含有 0.5%超崩解剂和 10%包衣厚度的片剂能够将 BD 有效递送到回肠-结肠区域，因此成为治疗克罗恩病的有前途的药物传递系统。
