新型载姜黄素结肠定位胶囊的制备及其体外释药行为研究

Preparation of novel curcumin-loaded colon-specific capsule and study on its in vitro release

目的制备载姜黄素结肠定位胶囊并对其体外释药行为进行研究。方法采用灌注法制备非渗透性胶囊体,滴制法制备载姜黄素自微乳微丸,粉末直接压片法压制柱塞片,将其组装成柱塞型胶囊,考察影响释药时滞的各种因素,评价其体外释药行为。结果该柱塞型胶囊的释药时滞随柱塞片中高酯果胶/乳糖比例的增加而延长,随柱塞片片质量的增加而延长。具有相同处方柱塞片的胶囊在0.5%果胶酶柠檬酸盐缓冲液和5%大鼠盲肠内容物溶液中的释药时滞明显缩短,说明其具有酶促发性。结论通过调节柱塞片处方组成及片质量可获得具有适当释药时滞的结肠定位胶囊。

Objective To prepare the curcumin-loaded colon-specific capsule and to study its in vitro release behaviors. Methods The impermeable capsule bodies were prepared by filling method, the curcumin-loaded self-microemulsifying beads were prepared by dropping method, the plug tablets were pressed by direct compression, and plug capsule was assembled with them. The factors affecting the lag-time were investigated, and the in vitro release behaviors ofcurcumin were evaluated. Results With the ratio of high methoxy pectin （HMP）/lactose （L） in the plug tablet and the weight of plug tablet increasing, the lag-time was prolonged. The lag-time of the capsule was obviously shortened in 0.5% pectinase citrate buffer and 5% rat cecal content solution, which indicated the capsule had the enzyme-triggered properties. Conclusion The capsule with colon-specific characteristics and a suitable lag-time could be achieved by adjusting the weight and formulation of the plug tablet.