Liu Jing, Zhang Liangke, Hu Wenjing, Tian Rui, Teng Yongzhen, Wang Chengyuan
Chongqing Key Laboratory of Biochemistry & Molecular Pharmacology, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Chongqing Key Laboratory of Biochemistry & Molecular Pharmacology, School of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Carbohydr Polym. 2012 Jan 4;87(1):377-382. doi: 10.1016/j.carbpol.2011.07.062. Epub 2011 Aug 5.
The current study aims to develop and evaluate a colon-specific, pulsatile drug delivery system based on an impermeable capsule. A pulsatile capsule was prepared by sealing a 5-aminosalicylic acid rapid-disintegrating tablet inside an impermeable capsule body with a konjac glucomannan (KGM)-hydroxypropyl methylcellulose (HPMC)-lactose plug. The drug delivery system showed a typical pulsatile release profile with a lag time followed by a rapid release phase. The lag time was determined by the KGM/HPMC/lactose ratio, the type of HPMC, and the plug weight. The addition of β-glucanase and rat cecal contents into the release medium shortened the lag time significantly, which predicted the probable enzyme sensitivity of the KGM plug. The in vivo studies show that the plasma drug concentration can only be detected 5h after oral administration of the capsule, which indirectly proves the colon-specific characteristics. These results indicate that the pulsatile capsule may have therapeutic potential for colon-specific drug delivery.
当前研究旨在开发并评估一种基于不透性胶囊的结肠特异性脉冲式药物递送系统。通过将5-氨基水杨酸速崩片密封在具有魔芋葡甘露聚糖（KGM）-羟丙基甲基纤维素（HPMC）-乳糖塞的不透性胶囊体内制备脉冲式胶囊。该药物递送系统呈现出典型的脉冲式释放曲线，先是有一个滞后时间，随后是快速释放阶段。滞后时间由KGM/HPMC/乳糖比例、HPMC类型和塞子重量决定。向释放介质中添加β-葡聚糖酶和大鼠盲肠内容物可显著缩短滞后时间，这预示着KGM塞子可能具有酶敏感性。体内研究表明，口服该胶囊5小时后才能检测到血浆药物浓度，这间接证明了结肠特异性特征。这些结果表明，脉冲式胶囊可能具有结肠特异性药物递送的治疗潜力。
