夏天无提取物中原阿片碱和延胡索乙素的大鼠肠吸收特性

摘要

Objective To study the rat intestine absorption characteristics of protopine( Pro) and tetrahydropainatine in extracts of RhizcmaCorydalis decum bentis. Methods The isolated everted intestinal sac was utilized to study the intestine absorption characteristics of protopine and tetrahydropamatine The sample' s concentration was determined by HPLC method. The apparent permeability coefficients (P app) and the mean cumulative permeation amount versus time curves were calculated and drawn TheP app of protopine and tetrahydropainatine was investigated and compared under different everted gut sacs, different concentrations and different pH values. Results The P app of protopine and tetrahydropalmatine in ileum was about 2. 58×10-5 cm· s-1 and3.15×10-5 cm· s-1, respectively, and the difference was remarkable compared to other intestine sacs (P＜0.05). The P app was decreased as Pro level increased,, and the cumulative permeation amount was non-linear increased in the duodenum, jejunum, and ileum When the pH value decreased from7.4 to5.4, the absorption of protopine and tetrahy-dropalmatine across intestinal membrane presented declining tendency Conclusion The absorption of protopine and tetrahydropalmatine in ileum is much better than that in other parts of intestine. The pH values could affect intestinal absorption of protopine and tetrahyd ropalmatine The absorption of protopine in duodenum, jejunum and ileum might be saturated.%目的 考察夏天无提取物中有效成分原阿片碱和延胡索乙素的大鼠肠吸收特性.方法 采用体外外翻肠囊模型研究原阿片碱和延胡索乙素的肠吸收特性.采用高效液相色谱(HPLC)法测定样品浓度,计算表观渗透系数(Papp),并绘制累积吸收量-时间曲线图.考察并比较原阿片碱和延胡索乙素在不同肠段、不同给药浓度、不同pH条件下的Papp.结果 原阿片碱和延胡索乙素在回肠段的Papp分别约为2.58×10-5和3.15×10-5 cm·s-1,与其他肠段比较,差异有统计学意义(P＜0.05).原阿片碱在十二指肠、空肠和回肠的Papp随着给药体系浓度的升高而降低,累计吸收量呈非线性增加.给药体系pH由7.4降低到5.4时,原阿片碱和延胡索乙素在各肠段的吸收均呈降低的趋势.结论 原阿片碱和延胡索乙素在回肠吸收较好,pH对于其在小肠内的吸收具有一定影响,原阿片碱的吸收在十二指肠、空肠和回肠可能存在饱和现象.