药学与临床研究
藥學與臨床研究
약학여림상연구
PHARMACEUTICAL AND CLINICAL RESEARCH
2014年
3期
197-200
,共4页
李允%郎巧玲%冯芳%史清水
李允%郎巧玲%馮芳%史清水
리윤%랑교령%풍방%사청수
栀子大黄汤%活性成分%在体单向灌流%HPLC法
梔子大黃湯%活性成分%在體單嚮灌流%HPLC法
치자대황탕%활성성분%재체단향관류%HPLC법
Zhi-Zi-Da-Huang Decoction%Active components%In situ single-pass perfusion%HPLC
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。
目的：研究梔子大黃湯中梔子苷、柚皮苷、橙皮苷和新橙皮苷4種有效成分的大鼠在體腸吸收動力學。方法：運用大鼠在體單嚮灌流重量法進行腸吸收實驗，攷察不同吸收部位和藥物濃度下的腸吸收動力學，採用HPLC法測定有效成分的濃度。結果：梔子苷、柚皮苷和新橙皮苷在小腸的吸收速率常數（Ka）和有效滲透繫數（Peff）顯著大于結腸（P<0.05）；橙皮苷在十二指腸和空腸吸收參數顯著大于迴腸和結腸（P<0.05）；藥物濃度在一定範圍內對梔子苷、柚皮苷和新橙皮苷的Ka和Peff無顯著影響（P>0.05），橙皮苷的Ka和Peff隨濃度的升高先增加後降低。結論：梔子大黃湯中4種有效成分在全腸道均有吸收；梔子苷、柚皮苷和新橙皮苷的吸收機製為被動擴散，橙皮苷在吸收過程中存在高濃度飽和現象，推測吸收機製為主動轉運或易化擴散。
목적：연구치자대황탕중치자감、유피감、등피감화신등피감4충유효성분적대서재체장흡수동역학。방법：운용대서재체단향관류중량법진행장흡수실험，고찰불동흡수부위화약물농도하적장흡수동역학，채용HPLC법측정유효성분적농도。결과：치자감、유피감화신등피감재소장적흡수속솔상수（Ka）화유효삼투계수（Peff）현저대우결장（P<0.05）；등피감재십이지장화공장흡수삼수현저대우회장화결장（P<0.05）；약물농도재일정범위내대치자감、유피감화신등피감적Ka화Peff무현저영향（P>0.05），등피감적Ka화Peff수농도적승고선증가후강저。결론：치자대황탕중4충유효성분재전장도균유흡수；치자감、유피감화신등피감적흡수궤제위피동확산，등피감재흡수과정중존재고농도포화현상，추측흡수궤제위주동전운혹역화확산。
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 Ka and 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 concen-tration, GE, NA and NE had no significant variation of Ka and 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.
