天麻苷元肠吸收特性的研究

目的:考察天麻苷元在大鼠肠道的吸收特性,为其口服制剂的开发提供依据。方法:分别应用大鼠离体外翻肠囊模型与在体肠灌流模型,考察天麻苷元在不同肠段的吸收特性,采用UPLC测定样品浓度,并计算相关肠吸收参数。结果:外翻肠囊实验结果表明,天麻苷元在各肠段的吸收无显著性差异,其累积吸收量随药物浓度升高呈线性增加,高质量浓度(400 mg.L-1)时,天麻苷元在十二指肠、空肠、回肠与结肠的累积吸收量(Q)分别为224.33,225.81,233.18,189.25μg;在体肠灌流实验结果也证实天麻苷元的吸收不存在肠段差异性,药物在各肠段的吸收率(A)分别为45.8%,48.39%,47.00%,54.35%。结论:天麻苷元在肠道中主要以被动转运的方式进入体内,在各肠段中吸收均较好,不存在肠段差异性。

Intestinal absorption characteristics of gastrodigenin in rats

Objective: To investigate the intestinal absorption characteristics of gastrodigenin.Method: In vitro everted gut sac model and in situ rat single-pass intestinal perfusion model were used to evaluate the absorption characteristics of gastrodigenin in the different intestinal segments.The concentrations of gastrodigenin in the samples were determined by Ultra Performance Liquid Chromatography(UPLC) method,and the relevant absorption parameters were calculated.Result: In the everted gut sac tests,no significant difference of absorption among the four segments was observed.A positive correlation was found between drug concentration and the accumulated absorption amount(Q).At the concentration of 400 mg·L-1,the Q of gastrodigenin in the duodenum,jejunum,ileum and colon were 224.33,225.81,233.18 and 189.25 μg,respectively.The in situ rat single-pass intestinal perfusion tests showed that there was also no significant difference of absorption among the four segments.The absorption rates(A) of gastrodigenin in the duodenum,jejunum,ileum and colon were 45.8%,48.39%,47.00%,54.35%,respectively.Conclusion: Gastrodigenin can be well absorbed via passive diffusion in the intestine.The absorption rates of gastrodigenin in the different intestinal segments show no regioselectivity.