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中文摘要：
目的以金丝桃苷含量为主要指标研究鬼针草总黄酮（TFB）的大鼠肠道吸收机制,为研究开发TFB新制剂奠定生物药剂学基础。方法采用大鼠在体单向肠灌流试验,利用HPLC法测定灌流液中TFB中的金丝桃苷浓度,计算十二指肠、空肠、回肠和结肠各部位及高中低浓度下空肠的有效渗透系数（Peff）。结果TFB中的金丝桃苷在大鼠十二指肠、空肠、回肠和结肠的Peff分别为：（1.89±0.53）×10^-4、（1.29±0.32）×10^-4、（0.88±0.33）×10^-4、（0.86±0.34）×10^-4cm/s;TFB高、中、低3种浓度下,金丝桃的Peff〉0.2×10^-4cm/s,并且差异无统计学意义（P〉0.05）;加入P-糖蛋白（P-gp）抑制剂盐酸维拉帕米对金丝桃苷的肠吸收影响不大。结论TFB中的金丝桃苷属于高渗透性药物,在大鼠各肠段均有吸收,其吸收机制为被动扩散;P-gp抑制剂对药物的小肠吸收基本无影响,故提高其溶出速度和溶解度将有利于药物的吸收。
英文摘要：
Objective To study the absorption mechanism of hyperoside in hawthorn leaves flavonoids（TFB）in the rat intestine by the main index of the contents of hyperoside.This experiment adoptes the biopharmaceutics foundation for researching and developing new preparation of TFB.Methods The in situ rat single-pass intestinal perfusion model was used.The concentration of the index component of TFB,hyperoside in the perfusate,was determined by HPLC.The effective permeability coefficients（Peff）of the four segments of the rat intestine,duodenum,jejunum,ileum and colon,and the change at different concentraions including low,medium,high concentration were calculated.Results The Peff values of hyperoside in TFB were（1.89±0.53）×10^-4,（1.29±0.32）×10^-4,（0.88±0.33）×10^-4,（0.86±0.34）×10^-4 cm/s in duodenum,jejunum,ileum and colon.The Peff values for hyperoside in the rat jejunal perfusion at different concentraions including low,medium,high concentration were all over 0.2×10^-4 cm/s,and there were no significant differences in the Peff of hyperoside in TFB at different concentrations of TFB（P〉0.05）.There was no significance Peff between presence of P-gp inhibitor and no P-gp inhibitor（P〉0.05）.Conclusion Hyperoside can be classified into high penetrating drug.It is absorbed in all intestine segments of rats.Passive diffusion dominates the absorptive transport behavior of hyperoside in TFB.The inhibitors of P-gp has no distinctive effect on the absorption of small intestine.So raising the dissolution rate and dissolvability of TFB are favourable its absorption.
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