4种黄酮类中药有效成分BCS分类及吸收机制初步研究.docVIP

4种黄酮类中药有效成分BCS分类及吸收机制初步研究 　　[摘要]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Caco2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Caco2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。 　　[关键词]黄酮类中药有效成分；生物药剂学分类系统（BCS）；吸收机制；溶解性；渗透性 　　[Abstract]The solubility and permeability on four kinds of flavonoids （kaempferol， hesperidin， apigenin， genistein） were test according to the theory of biopharmaceutics classification system （BCS）， and their absorption mechanism The solubility was investigated by the method in determination of solubility of Chinese Pharmacopoeia 2010 To detect appearance permeability of compounds mentioned above， the appropriate concentrations were selected by the MTT method in cell transfer experiments in Caco2 cell model， which established by in vitro cell culture method Therefore， these compounds were classified with BCS according to solubility and permeability In addition， to explore absorption mechanisms， the experiments in three different concentrations of compounds in high， medium and low in bidirectional transformation methods in Caco2 cell model contacted The study indicated that all of kaempferol， hesperidin， apigenin， genistein have the characteristics in low solubility and high permeability， which belong to BCSⅡ， and the absorption mechanism of kaempferol was active transportation Whereas， hesperidin， apigenin， genistein were passive transportation In this study， it carried out initial explorations on establishment of determination for solubility and permeability in flavonoids， and provided theoretical reference for further research on BCS in traditional Chinese medicine 　　[Key words]flavonoids； biopharmaceutics classification system （BCS）； absorption mechanism； solubil