酶降解-时滞型载姜黄素结肠定位胶囊的体外释药研究

In vitro release of enzymatic degradation and time-based capsule of curcumin for colon-specific delivery

目的研究以低酯果胶为材料的载姜黄素结肠定位栓塞型胶囊的体外释药情况,评价其结肠定位的释药特性。方法将非渗透性胶囊体、姜黄素自微乳微丸、栓塞片以及肠溶性囊帽组装成栓塞型胶囊,考察栓塞片处方中各因素对释药时滞的影响,评价其在模拟结肠环境中的体外释药行为。结果当羟丙甲纤维素的型号为K4M、低酯果胶∶羟丙甲纤维素=9.5∶0.5和片重为100 mg时,可达到结肠定位需要的释药时滞。具有相同处方栓塞片的胶囊在5%大鼠盲肠内容物溶液和0.5%果胶酶溶液中的释药时滞均缩短,说明其具有酶降解性。结论载姜黄素低酯果胶栓塞型胶囊具有酶降解-时滞型结肠定位释药特性。

Objective To investigate the in vitro release of curcumin from low methoxy pectin （LMP） plug capsule and evaluate its colon-specific drug delivery characteristics. Methods Plug capsule was assembled with impermeable capsule bodies, curcumin-loaded self-microemulsifying beads, plug tablet and enteric cap. The factors affecting the lag-time in the plug tablet were investigated, and in vitro release of curcumin was evaluated in the artificial medium of the colon. Results When the type of hydroxypropyl methylcellulose （HPMC） was K4M, the ratio of LMP/HPMC was 9.5∶0.5 and the weight of plug tablet was 100 mg, the lag-time was achieved to satisfy the colon-specific characteristics. The lag-time of the capsule was shortened in 5% rat cecal content solution and 0.5% pectinase solution, indicating the capsule having the property of enzymatic degradation. Conclusion The plug capsule may be an enzymatic degradation and time-based colon-specific drug delivery system.