栀子大黄汤有效成分在体肠吸收研究  

Intestinal Absorption Studies of the Active Components in Zhi-Zi-Da-Huang Decoction

作　　者：李允[1] 郎巧玲 冯芳[1,2] 史清水[3] 

机构地区：[1]中国药科大学药物分析教研室,南京210009 [2]中国药科大学药物质量与安全预警教育部重点实验室,南京210009 [3]江苏省食品药品检验所,南京210008

出　　处：《药学与临床研究》2014年第3期197-200,共4页Pharmaceutical and Clinical Research

基　　金：国家自然科学基金项目(No.81274063)

摘　　要：目的:研究栀子大黄汤中栀子苷、柚皮苷、橙皮苷和新橙皮苷4种有效成分的大鼠在体肠吸收动力学。方法:运用大鼠在体单向灌流重量法进行肠吸收实验,考察不同吸收部位和药物浓度下的肠吸收动力学,采用HPLC法测定有效成分的浓度。结果:栀子苷、柚皮苷和新橙皮苷在小肠的吸收速率常数(Ka)和有效渗透系数(Peff)显著大于结肠(P<0.05);橙皮苷在十二指肠和空肠吸收参数显著大于回肠和结肠(P<0.05);药物浓度在一定范围内对栀子苷、柚皮苷和新橙皮苷的Ka和Peff无显著影响(P>0.05),橙皮苷的Ka和Peff随浓度的升高先增加后降低。结论:栀子大黄汤中4种有效成分在全肠道均有吸收;栀子苷、柚皮苷和新橙皮苷的吸收机制为被动扩散,橙皮苷在吸收过程中存在高浓度饱和现象,推测吸收机制为主动转运或易化扩散。Objective： To study the in vivo intestinal absorption kinetics of geniposide（GE）, naringin（NA）, hesperidin（HE） and neohesperdin（NE） in Zhi-Zi-Da-Huang Decoction（ZZDHD）. Methods： The in situ single-pass perfusion gravimetric method was adopted to investigate the influence of absorption site and drug concentration on the rat intestinal absorption. The HPLC was used to measure the contents of GE,NA, HE and NE. Results： For GE, NA and NE, their absorption parameters, the Kaand Peff, in the small intestines were significantly different from those in the colon（P〈0.05）; the absorption of HE decreased significantly in ileum and colon than in duodenum and jejunum（P〈0.05）. Within a certain range of concentration, GE, NA and NE had no significant variation of Kaand Peff（P〉0.05）, while the absorption of HE first increased and then decreased with the increase of drug concentration（P〈0.05）. Conclusion： The four active components in ZZDHD could be absorbed in the whole intestinal canal of rats. The absorption of GE, NA and NE in rat intestine appeared to be by the passive diffusion mechanism while that of the HE was prelimnarily determined to be by an active transport or facilitated diffusion mechanism.

关 键 词：栀子大黄汤 活性成分 在体单向灌流 HPLC法 

分 类 号：R965[医药卫生—药理学]