黄连生物碱在大鼠在体单向肠灌流模型中的转运特性研究

Studies on intestinal absorption of alkaloids in Coptis chinensis by in situ single-pass perfused rat intestinal model

目的:研究黄连中小檗碱和巴马汀在大鼠肠道的吸收动力学特征。方法:采用大鼠单向肠灌流模型,利用HPLC法分别测定小檗碱和巴马汀的量,计算2种生物碱的肠吸收速率常数(Ka)和表观吸收系数(Papp),分析肠吸收特征。结果:小檗碱和巴马汀在各肠段的吸收有显著性差异,小檗碱(50 mg.L-1)的Papp为回肠>十二指肠>空肠>结肠,巴马汀(160 mg.L-1)的Papp为回肠>结肠>空肠>十二指肠;质量浓度对小檗碱和巴马汀在回肠吸收的Papp有显著影响;相当浓度的小檗碱和巴马汀的在不同的灌流液中灌流Ka为戊己丸配伍方>黄连提取物>标准品。结论:小檗碱和巴马汀在大鼠各肠段均有吸收,在回肠段吸收最好;其吸收不是以简单的被动扩散起作用;以戊己丸和黄连粗提取物给药时可显著促进黄连中生物碱的肠吸收。

Objective： To study the absorption characteristics of alkaloids in Coptis chinensis in rat intestinal.Method： In situ single-pass perfused rat intestinal model was used and the concentrations of berberine and palmatine were determined by HPLC,the drug absorption rate constant（Ka） and apparent absorption coefficient（Papp） were tested to evaluate their absorption characteristics.Result：The absorption of berberine and palmatine in different regions of rat intestinals was significantly different.From bigness to smallness,the Papp value of berberine at 50 mg·L-1 were ileum,duodenum,jejunum and colon,of palmatine at 50 mg·L-1 were ileum,colon,jejunum and duodenum.The concentration of berberine and palmatine had distinctive effect on the Ka value of berberine and palmatine were ordered from larger to little as in Wujiwan compatibility,Coptis chinensis extractive and single compound.Conclusion： The berberine and palmatine were absroped at all regions of rat intestinal.The absorption characteristics of 2 alkaloids were not passive diffusion.The other ingredients in Wujiwan compatibility and Coptis chinensis extractive could promote the absorption of alkaloids.