目的 基于中药整体观，以葛根Puerariae Lobatae Radix自身作为整体，考察葛根异黄酮类成分对葛根素溶解度及渗透性的调节作用，探讨单味中药所含成分发挥作用时的“自洽性”。方法 选取葛根中3种高含量黄酮类成分3'-羟基葛根素、大豆苷元和染料木苷，设计人工多成分环境，采用平衡溶解度的研究方法考察pH 7.4磷酸盐缓冲液中多成分环境下葛根素溶解度的变化；采用在体单向肠灌流模型考察葛根异黄酮类成分对葛根素肠吸收的调节作用。结果 实验结果表明，不同成分背景、不同成分组合及其不同比例的3'-羟基葛根素、大豆苷元、大豆苷和染料木苷对葛根素溶解度与渗透性均有一定的影响。采用递进式进行2成分及3成分背景的溶解度研究，表明葛根素溶解度和渗透性变化均存在“叠加性”和“饱和性”的特点，溶解性方面：以葛根自身成分为整体，在水溶液体系中各异黄酮类成分对葛根素溶解度提高了42.60%，在pH 7.4缓冲液体系中提高了18.62%。渗透性方面：葛根素的肠渗透性具有“叠加效应”。以葛根自身成分为整体，主要异黄酮类成分3'-羟基葛根素、染料木苷及大豆苷元对葛根素的肠渗透系数表观渗透系数（apparent permeability coefficients，P_app）、肠吸收速率常数（absorptive promoter，K_a）、肠吸收分数（intestinal absorption fraction，F_a）分别提高220%、236%、213%，即对葛根素的肠渗透性提升了约220%。结论 以上研究表明，葛根异黄酮类成分在人体作用时可能存在“叠加效应”，葛根素在葛根自身多组分环境中具有部分“自洽性”，从而改善了葛根素生物利用度。

Objective Based on the integrality of traditional Chinese medicine, took Gegen (Puerariae Lobatae Radix) itself as a whole, the effects of isoflavones from Puerariae Lobatae Radix on the solubility and permeability of puerarin were investigated to discuss “self-consistency” of the compounds within single Chinese medicine. Methods Three high content components in pueraria flavonoid group, including 3'-hydroxypuerarin, daidzein and genistin, were selected to design an artificial multi-component environment. The method of equilibrium solubility was employed to measure the solubility of puerarin in pH 7.4 phosphate buffer. The effects of the pueraria isoflavone on the permeability of puerarin were investigated by means of single-pass intestinal perfusion technique. Results The results showed that the solubility and permeability of puerarin were affected by different composition backgrounds, different composition combinations and different proportions of 3'-hydroxypuerarin, daidzein, daidzein and genistein. The solubility of two-component and three-component backgrounds was studied by a progressive formula. The results showed that the solubility and permeability of puerarin both had the characteristics of “superposition” and “saturation”. Solubility: Taking the components of pueraria as a whole, the solubility of pueraria was increased by 42.60% by different flavonoids in the aqueous solution system. The increase rate was 18.62% in pH 7.4 buffer liquid system. Permeability: The intestinal permeability of puerarin had a “superposition effect”. The intestinal permeability coefficients P_app, K_a and F_a of puerarin were increased by 220%, 236% and 213% respectively by isoflavones 3'-hydroxypuerarin, genitin and daidzein taking the root itself as the whole. That is, the intestinal permeability of puerarin was increased by about 220%. Conclusion The above studies indicated that the isoflavones from pueraria may have a “superposition effect” in the human body, and pueraria is partially “self-consistent” in the multi-component environment of pueraria itself, thus improving the bioavailability of pueraria.

R283.6

国家重点研发计划重点专项（2017YFC1702904）；江西省现代农业产业技术体系建设专项资金资助（JXARS-16）；江西省重点研发计划项目（20192BBG70074）