吲哚美辛结肠靶向胶囊的制备及体外释药评价

    Preparation and in Vitro Evaluation of Indometacin Capsule for Colon-specific Delivery

    • 摘要: 目的 开发一种结肠靶向胶囊,使吲哚美辛达到结肠部位实现靶向释放。方法 以蘸胶工艺制备不溶性半透膜囊体,灌装药物后以果胶片封住囊体,外套上普通胶囊壳后外包肠溶衣,进行体外释放试验。结果 该给药系统在人工胃液中不变形,药物不释放,采用PEG-2 000∶CA为60%的不溶性囊体,包衣增重90%,药物∶NaCl为1∶1制备的胶囊,药物在人工肠液中3 h释放<10%,在人工结肠液中10 h药物释放超过70%,基本释放完全,达到结肠定位释放要求。结论 吲哚美辛结肠靶向胶囊能实现在结肠定位释放药物。

       

      Abstract: OBJECTIVE To develop a colon-targeted capsule to achieve targeted release in colon of indometacin. METHODS The insoluble semi-permeable capsule body was prepared by dipping-drying process. After filling with drugs, the capsule body were stuffed by pectin tablet. The insoluble body was capped into a stomach-soluble capsule, following with the enteric coating outside the capsule. Then in vitro release was investigated. RESULTS The system was undeformed and no drug released in artificial gastric fluid. The indometacin capsule made of PEG-2 000∶CA 60% insoluble capsule body, coating weight gain 90% and drugs:NaCl 1∶1, reached to colon specific release completely, with drugs released <10% in artificial intestinal juice in 3 h, and >70% in artificial colonal juice in 10 h. CONCLUSION The indomethacin colon-targeted capsule can realize releasing drugs in the colon target position.

       

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