黄芩苷-小檗碱复合物纳米晶的制备和在体肠吸收评价

Preparation and in vivo intestinal absorption evaluation of baicalin-berberine complex nanocrystals

关键词:  中药  纳米晶  黄芩苷  小檗碱  在体单向肠灌流模型  吸收

Key words:  traditional Chinese medicine  nanocrystals  baicalin  berberine  in situ single-pass intestinal perfusion model  absorption

摘要:

[目的] 研究纳米晶对黄芩苷-小檗碱复合物的肠吸收促进作用。[方法] 使用抗溶剂法结合高压均质法制备黄芩苷-小檗碱复合物纳米晶，进行初步体外评价。建立在体单向肠灌流模型，评价纳米晶对复合物吸收的促进效果。[结果] 制备了黄芩苷-小檗碱复合物纳米晶。体外评价结果表明，黄芩苷-小檗碱复合物纳米晶为圆柱状，粒径为（225.10±9.12）nm，多分散系数为（0.27±0.04）。在十二指肠、空肠、回肠、结肠4个肠段，纳米晶组黄芩苷的有效渗透系数（P_eff）分别是复合物组的2.99、2.00、2.66、5.58倍，纳米晶组小檗碱的P_eff分别是复合物组的1.25、1.18、1.53、1.80倍。[结论] 纳米晶提高了黄芩苷-小檗碱复合物的在体肠吸收。

Abstract:

[Objective] To investigate the intestinal permeability improvement of baicalin-berberine complex nanocrystals.[Methods] Baicalin-berberine complex nanocrystals were prepared by anti-solvent methodfollowed by high pressure homogenization, and the in situ single-pass intestinal perfusion model was established to evaluate the absorption enhancement of the complex nanocrystals.[Results] Baicalin-berberine complex nanocrystals were prepared and characterized. The baicalin-berberine complex nanocrystals were cylindrical with the particle size at (225.10±9.12) nm, and the Polymer dispersity index was (0.27±0.04). In duodenum, jejunum, ileum and colon, the effective permeability coefficients (P_eff) of baicalin in nanocrystals group were 2.99, 2.00, 2.66 and 5.58 times higher than that of coarse suspension group, separately. The P_eff of berberine in nanocrystals group were 1.25, 1.18, 1.53 and 1.80 times higher than that of coarse suspension group, respectively.[Conclusion] Nanocrystals could improve the oral absorption of baicalin-berberine complex.