期刊
CARBOHYDRATE POLYMERS
卷 87, 期 1, 页码 377-382出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2011.07.062
关键词
Colon-specific drug delivery; Konjac glucomannan; Pulsatile capsule
资金
- Chongqing Yuzhong District Science and Technology Project [20100203]
- Chongqing Municipal Education Commission [KJ110323]
- Chongqing Board of Health [2010-2-202]
- Chongqing Natural Science Foundation [CSTC, 20081385397]
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 beta-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 5 h 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. (C) 2011 Elsevier Ltd. All rights reserved.
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