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胶束电动毛细管色谱法表征胆汁盐与药物之间的相互作用。第一部分。

Characterization of interactions between bile salts and drugs by micellar electrokinetic capillary chromatography. Part I.

作者信息

Schwarz M A, Neubert R H, Dongowski G

机构信息

Institute of Pharmaceutics and Biopharmaceutics, Martin-Luther-University, Halle/Saale, Germany.

出版信息

Pharm Res. 1996 Aug;13(8):1174-80. doi: 10.1023/a:1016051917608.

Abstract

PURPOSE

The general properties of micellar electrokinetic capillary chromatography (MECC) were utilized to characterize the strength of interactions between bile salts and biological active substances.

METHODS

For that purpose various bile salts were used as micellar pseudostationary phase in the background electrolyte. Furthermore, a physicochemical model was applied and the effective partition coefficients between micellar and water phase were calculated in order to evaluate the strength of interactions between bile acids and the drugs.

RESULTS

It was found that the interactions between the selected drugs and bile salts depend both on the lipohilicity of the drugs and on the charge of the components. Only hydrophobic, cationic drugs such as quinine and propranolol are able to interact with these surface active agents.

CONCLUSIONS

MECC is a valuable method to characterize interactions such occurring between drugs and bile salts.

摘要

目的

利用胶束电动毛细管色谱法(MECC)的一般特性来表征胆汁盐与生物活性物质之间相互作用的强度。

方法

为此,将各种胆汁盐用作背景电解质中的胶束假固定相。此外,应用了一个物理化学模型,并计算了胶束相和水相之间的有效分配系数,以评估胆汁酸与药物之间相互作用的强度。

结果

发现所选药物与胆汁盐之间的相互作用既取决于药物的亲脂性,也取决于组分的电荷。只有疏水性阳离子药物,如奎宁和普萘洛尔,能够与这些表面活性剂相互作用。

结论

MECC是表征药物与胆汁盐之间此类相互作用的一种有价值的方法。

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