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目的:研究中药单体丁香苦苷的在体肠吸收机制。方法:运用单向灌流模型、采用HPLC对药物的质量浓度进行检测,分别研究吸收部位、药物质量浓度、pH以P-糖蛋白抑制剂对丁香苦苷吸收的影响。结果:丁香苦苷在十二指肠、空肠、回肠、结肠的吸收速率常数分别为0.002 55,0.006 30,0.009 00,0.007 99 min-1;不同的药物质量浓度0.090,0.180,0.360g·L-1在小肠的吸收速率常数分别为0.003 70,0.007 08,0.006 94 min-1;不同的pH 7.4,6.8,5.0时在小肠的吸收速率常数分别为0.007 33,0.007 47,0.003 62 min-1。P-糖蛋白抑制剂对丁香苦苷肠吸收具有显著性影响(P<0.05)。结论:丁香苦苷在肠道下部吸收较好;药物浓度低时,吸收速率常数小,中、高浓度时,吸收速率常数增大;在pH 5.0～7.4,pH 5.0吸收速率常数较小,pH 6.8,7.4吸收速率常数增大,丁香苦苷为P-糖蛋白底物。
Objective: To study the in vivo intestinal absorption mechanism of traditional Chinese medicine syringin. Methods: Uni-directional perfusion model was used to detect the concentration of drug by HPLC. The absorption site, the concentration of drug and the inhibitor of P-glycoprotein on the absorption of syringin were studied. Results: The absorption rate constants of syringin in duodenum, jejunum, ileum and colon were 0.002 55,0.006 30,0.009 00,0.007 99 min-1, respectively. Different drug concentrations were 0.090,0.180,0.360g · L -1 in the intestine were 0.003 70,0.007 08,0.006 94 min-1, respectively. The absorption rate constants in the small intestine at different pH 7.4,6.8,5.0 were 0.007 33,0.007 47,0.003 62 min-1 . P-glycoprotein inhibitors had a significant effect on cloveine intestinal absorption (P <0.05). Conclusions: Syringomycin is better absorbed in the lower part of intestinal tract. At low drug concentration, the absorption rate constant is small at medium, medium and high concentration. At pH 5.0-7.4, 6.8,7.4 absorption rate constant increased syringomycin P-glycoprotein substrate.