去甲氧基姜黄素羟丙基-β-环糊精在体肠吸收特征

Intestinal absorption characteristics of demethoxycurcumin hydroxypropyl-β-cyclodextrin in rats

目的研究去甲氧基姜黄素羟丙基-β-环糊精(DECD)及去甲氧基姜黄素(DE)的在体肠吸收情况。方法使用DE以环糊精包合技术制备DECD,光谱法测定其理化性质,显微照相观察其形态,马尔文粒径测定仪测定DECD的zeta电位。采用大鼠在体肠段单向灌流模型,并建立紫外分光光度法测定DECD及DE在大鼠体内各肠段的吸收速率常数(Ka)、表观渗透系数(Papp)和吸收百分率。结果成功制得DECD,其溶解度为2.30g/L,是DE的38.33倍;zeta电位为-32.2mV。在体肠吸收实验显示DECD的Ka及Papp皆为回肠>十二指肠>空肠>结肠,且其Ka、Papp与吸收百分率较DE均有所提高。结论 DECD能够明显改善DE在大鼠小肠内的吸收情况。

Objective To study the intestinal absorption characteristics of demethoxycurcumin hydroxypropyl-β- cyclodextrin （DECD） and demethoxycurcumin （DE） in rats. Methods DECD was prepared by cyclodextrin inclusion technique and characterized by spectroscopic method. The morphology of DECD was observed by microphotograph and zeta potential was examined by Maivern laser particle sizer. In vivo single-pass intestinal perfusion rat model was adopted; the absorption rate constant （Ka）, effective permeability （Papp） and percent absorption of DECD and DE were determined using the ultraviolet spectrophotometry. Results DECD was successfully prepared, with a solubility of 2. 30 g/L, which was 38. 33 times that of DE. Zeta potential of DECD was -32. 2 inV. The results of intestinal absorption experiment showed that the Ka and Papp values of DECD decreased in order in the ileum, duodenum, jejunum, and colon. In addition, the Ka, Papp values and percent absorption of DECD were higher than that of DE. Conclusion DECD can markedly improve the intestinal absorption of DE in rats.