枳实中黄酮成分及其提取物大鼠肠吸收特性研究

Intestinal absorption properties of flavones and extract of Fructus Aurantii Immaturus in rats

目的:考察枳实中3种活性黄酮成分柚皮苷、橙皮苷、新橙皮苷及枳实提取物在大鼠肠道的吸收特性。方法:采用大鼠肠灌流模型和肠道酶共孵育实验研究各成分及提取物在大鼠肠道的吸收代谢特性,同时测定各成分的表观油水分配系数。结果:柚皮苷、橙皮苷、新橙皮苷及枳实提取物在大鼠肠道的有效渗透系数Peff值均较小,柚皮苷在0.140～0.252,橙皮苷在0.156～0.268,新橙皮苷在0.154～0.285,化合物在不同肠段中的Peff值无显著差异,不同浓度间的Peff值也无显著差异;相同浓度下,枳实提取物中各成分的Peff值高于相应单一成分。各成分与肠道酶共孵育均未检测到代谢物。测得柚皮苷、橙皮苷、新橙皮苷的表观油水分配系数P分别为0.36,0.40,0.48,且pH对其影响不大。结论:柚皮苷、橙皮苷、新橙皮苷在大鼠肠道的渗透性较差是其吸收差的一个重要原因;枳实提取物中各成分较相应单一成分在大鼠肠道的吸收有提高,表明可能存在成分间的相互作用促进其吸收。

Objective： To investigate the intestinal absorption of naringin,hesperidin,neohesperidin and the extract of Fructus Aurantii Immaturus in rats.Method： The rat intestinal perfusion and enzymes incubation models were used,together with the determination of the n-octanol/water partition coefficient of the components（P）.Result： In perfusion model,the Peff of all components were low,and the Peff of naringin,hesperidin and neohesperidin were 0.140-0.252,0.156-0.268 and 0.1540.285,respectively.In four different regions of intestine of rat and with different concentration,the Peff of the components both had no significant difference,whereas the Peff of the extract were higher than the Peff of the single component.The metabolite of components was not detected in intestine.The P of naringin,hesperidin and neohesperidin were 0.36,0.40 and 0.48,respectively,and the pH of buffer solution had no influence to its distribution coefficient.Conclusion： Poor permeation contributed to the poor intestinal absorption of naringin,hesperidin and neohesperidin.The absorption of components in extract were increased,and the results suggest that the extract may enhance the intestinal absorption of the components.