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

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同肠吸收的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.

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

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 (K_a) and apparent absorption coefficient (P_app) 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 P_app 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 K_a 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.