Chongqing Key Laboratory of Biochemistry & Molecular Pharmacology, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Carbohydr Polym. 2013 Feb 15;92(2):2218-23. doi: 10.1016/j.carbpol.2012.11.105. Epub 2012 Dec 16.
This study developed and evaluated a colon-specific pulsatile capsule with tablet of self-microemulsifying drug delivery system (SMEDDS). This system is based on an impermeable capsule containing a rapid-disintegrating curcumin-loaded SMEDDS tablet inside it, and a highly methoxylated pectin (H-pectin)/lactose tablet plugged in the capsule mouth. The SMEDDS tablet enhanced the solubility of curcumin, a water-insoluble drug. An in vitro release study of the pulsatile capsule showed a typical pulsatile release profile with a specific lag time. The lag time, which determines the efficiency of colon-specific delivery, could be regulated by varying the H-pectin/lactose ratio. Pectinase and rat cecal contents added to the release medium significantly shortened the erosion time, which proved that the H-pectin plug is sensitive to enzyme degradation. These results show that the pulsatile capsule with SMEDDS tablet has potential for the colon-specific delivery of water-insoluble drugs.
本研究开发并评估了一种具有自微乳药物传递系统（SMEDDS）片的结肠定位脉冲胶囊。该系统基于不透水胶囊，内部含有速崩型姜黄素载药 SMEDDS 片，胶囊口处塞有高度甲氧基化果胶（H-果胶）/乳糖片。SMEDDS 片提高了水不溶性药物姜黄素的溶解度。脉冲胶囊的体外释放研究显示出典型的脉冲释放特征，具有特定的滞后时间。滞后时间决定了结肠定位传递的效率，可以通过改变 H-果胶/乳糖的比例进行调节。释放介质中添加果胶酶和大鼠盲肠内容物显著缩短了侵蚀时间，这证明 H-果胶塞对酶降解敏感。这些结果表明，具有 SMEDDS 片的脉冲胶囊具有传递水不溶性药物的潜力。
