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本实验主要考察药物浓度、肠段、pH、P-糖蛋白(P-glycoprotein,P-gp)及Na+依赖型葡萄糖转运体(Na+-dependent glucose transporter,SGLT1)对小檗碱肠吸收的影响,并探索复方配伍环境中小檗碱的肠吸收情况。实验以酚红为标示物,采用大鼠在体单向肠灌流模型,运用高效液相色谱法考察小檗碱单体(36.70、46.17和92.33μg.mL?1)、黄连解毒汤模拟体系(主要指标成分单体混合物:小檗碱+黄芩苷+栀子苷,其中小檗碱浓度为92.33μg.mL?1)及黄连解毒汤全方(小檗碱浓度为92.33μg.mL?1)中小檗碱在大鼠各肠段的吸收变化情况。结果表明:小檗碱在一定浓度范围内(20～100μg.mL?1),部分大鼠小肠吸收速率参数(Ka)无显著性差异,提示药物的吸收机制可能为被动扩散,其转运过程可能受SGLT1和P-gp的影响;单体混合物和全方中小檗碱在各肠段的Ka和有效渗透系数(Peff)值均有显著性增加(P<0.05)。说明小檗碱在整个肠段均有吸收,具有广泛的吸收窗,其中结肠段吸收较好;配伍对小檗碱的大鼠肠吸收特性有一定影响,较单体而言,单体混合物和全方灌流时小檗碱在小肠中吸收更好。
In this study, the effects of drug concentration, intestinal segment, pH, P-glycoprotein (P-gp) and Na + -dependent glucose transporter (SGLT1) on intestinal absorption of berberine were investigated. And to explore the complex absorption of berberine in the environment of intestinal absorption. Experimental results showed that phenol red was used as the marker and the rat model of unilateral intestinal perfusion was established. The contents of berberine monomer (36.70,46.17 and 92.33μg.mL-1) The main index components monomer mixture: berberine + baicalin + geniposide, which berberine concentration of 92.33μg.mL? 1) and Huanglian Jiedu Tang full (berberine concentration of 92.33μg.mL? 1) in the barberry Alkaline absorption in various intestinal segments of rats. The results showed that there was no significant difference in berberine absorption rate parameters (Ka) in certain concentration range (20 ~ 100μg.mL? 1), suggesting that the drug absorption mechanism may be passive diffusion, the transport process may be The effects of SGLT1 and P-gp were significant (P <0.05). The Ka and the effective permeability coefficient (Peff) of each mixture of monomeric mixture and berberine were significantly increased (P <0.05). Berberine absorption in the entire bowel segment, with a wide range of absorption window, which colon segment absorption better; compatibility berberine rat intestinal absorption characteristics have a certain impact, compared to the monomer, the monomer mixture and Berberine absorbed better in the small intestine during perfusion.