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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 absorption characteristics of three kinds of active flavones flavonoids, naringin, hesperidin, neohesperidin and citrus aurantium, in the intestinal tract of rats. Methods: Rat intestine perfusion model was co-incubated with intestinal enzymes to study the absorption and metabolism of each component and extract in rat intestine. The apparent oil-water partition coefficient of each component was also determined. Results: The Peff value of naringin, hesperidin, neohesperidin and citrus aurantium extract in rat intestine was small, the naringin at 0.140 ~ 0.252, the hesperidin at 0.156 ~ 0.268, The new hesperidin at 0.154 ~ 0.285, compound in different bowel Peff value was no significant difference between the different concentrations of Peff value no significant difference; the same concentration, citrus aurantium extract Peff value of each component is higher than the corresponding Single component. Metabolites were not detected on incubation with intestinal enzymes. The apparent oil-water partition coefficients P of naringin, hesperidin and neohesperidin were 0.36, 0.40 and 0.48, respectively, and pH had little effect on them. CONCLUSION: The poor permeability of naringin, hesperidin and neohesperidin in the intestine of rats is an important reason for their poor absorption. Compared with the corresponding single component in the intestine of rat Absorption increased, indicating that there may be interaction between the ingredients to promote their absorption.