理中汤提取物中5种主要活性成分在体肠吸收特征研究

The intestinal absorption characteristics of five active components in Lizhong Decoction

通过建立大鼠在体单向肠灌流模型,采用UPLC-TQ-MS测定不同肠段灌流液中理中汤提取物5种主要活性成分(甘草酸、异甘草素、6-姜酚、人参皂苷Rb1和白术内酯-I)的含量。动物福利和实验过程均遵循南京中医药大学动物伦理委员会的规定。以吸收速率常数(K_a)和有效渗透系数(P_(eff))为评价指标,分析以上5种成分的肠吸收特点。结果显示,甘草酸、异甘草素和6-姜酚的最佳吸收部位分别为回肠、结肠和十二指肠,差异均具有统计学意义(P<0.05);人参皂苷Rb1和白术内酯-I在不同肠段的吸收参数无显著性差异(P>0.05),提示这两种活性成分在大鼠全肠段均有吸收,不受吸收部位影响。且5种指标成分在全肠段吸收均较好(P_(eff)>1.0×10^(-3)cm·min^(-1)),结果提示:理中汤适宜于制备成缓控释、肠溶制剂等。

The intestinal absorption properties of the main effective components(glycyrrhizic acid,isoliquiritigenin,6-gingerol,ginsenoside Rb1,atractylode-I)in Lizhong decoction(LZD)extracts were investigated with an in situ single-pass intestinal perfusion model in rats.UPLC-TQ-MS was used to determine the concentration of the five components in the intestinal perfusion.Animal welfare and experimental procedures were in accordance with the regulations of the Animal Ethics Committee of Nanjing University of Chinese Medicine.As evaluation indexes for the intestinal absorption characteristics,the absorption rate constant(Ka)and the apparent permeability coefficient(P_(eff))of the five main ingredients were analyzed.Results showed that the best absorption sites for glycyrrhizic acid,isoliquiritin and 6-gingerol were the ileum,colon and duodenum,respectively,and the differences between different intestinal segments were statistically significant(P<0.05).There was no notable difference in Kaand Peff between ginsenoside Rb1 and atractylode-I in the different intestinal segments(P>0.05),suggesting that they were absorbed throughout.The five components were well-absorbed in the whole intestine(P_(eff)>1.0×10^(-3) cm·min^(-1)),indicating that LZD is suitable for preparing sustained,controlled release and enteric-coated preparations.