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该研究根据生物药剂学分类系统(biopharmaceutics classification system,BCS),研究山柰酚、橙皮苷、芹菜素、染料木素等4种黄酮类中药有效成分的溶解性和渗透性,并对其进行BCS分类;同时对其吸收机制进行研究。参照《中国药典》2010年版中溶解度测定方法对4种黄酮类成分进行溶解度的测定,采用体外细胞培养法建立Caco-2细胞模型,利用MTT法筛选出合适的给药浓度进行细胞转运实验来检测表观渗透系数(Papp)以判断渗透性,并根据BCS对其进行分类;采用Caco-2细胞模型,选择高、中、低3组不同浓度化合物进行双向转运实验研究吸收机制。实验表明山柰酚、橙皮苷、芹菜素、染料木素等具有低溶解性、高渗透性,属于BCSⅡ类,其中山柰酚为主动转运吸收机制,而橙皮苷、芹菜素、染料木素等为被动吸收。该研究针对中药黄酮类单体有效成分的特性,对其溶解性及渗透性的评价方法进行了摸索,为进一步完善中药生物药剂学分类体系提供了理论依据。
According to the biopharmaceutics classification system (BCS), this study studied the solubilities and permeabilities of active ingredients of Chinese flavonoids such as kaempferol, hesperidin, apigenin and genistein, BCS classification; at the same time its absorption mechanism to study. According to the Chinese Pharmacopoeia (2010 edition), the solubility of four flavonoids was determined. The Caco-2 cell model was established by in vitro cell culture method. The appropriate concentration of drug was screened by MTT method to detect the cell viability. The apparent permeability coefficient (Papp) was used to determine the permeability and classified according to BCS. The Caco-2 cell model was used to select the high, middle and low concentrations of three different concentrations of compounds for bidirectional transport study of absorption mechanism. Experiments show that kaempferol, hesperidin, apigenin, genistein and other low solubility, high permeability, belonging to the BCS Ⅱ class, of which kaempferol is the active transport and absorption mechanism, and hesperidin, apigenin, dye wood Su and other passive absorption. The research aimed at the characteristics of the active ingredients of Chinese traditional medicine flavonoids and explored the evaluation methods of their solubility and permeability, which provided the theoretical basis for further perfecting the classification system of traditional Chinese medicine biopharmaceutics.