Mrestani Y, Neubert R H
Institute of Pharmaceutics and Biopharmaceutics, Martin-Luther-University Halle-Wittenberg, Halle/S., Germany.
J Pharm Biomed Anal. 2001 Feb;24(4):637-43. doi: 10.1016/s0731-7085(00)00441-6.
Micellar affinity capillary electrophoresis (MACE) was introduced to evaluate the affinity of various kinds of drugs as benzoic acid, salicylic acid, trinitrophenol, p-hydroxybenzoic acid and o-acetylsalicylic acid. Non-ionic micelles as Brij 35 (polyethylenglycol dodecylether), Tagat (polyoxyethylene (20) glycerol monooleate) and Tween 20 (polyoxyethylen sorbitan monolaurate) were used as a pseudostationary phase in capillary electrophoresis. For polyvinyl alcohol (PVA) coated capillary was used in this examinations. The drugs had negative electrophoretic mobilities at a pH value of pH 7.2. The negatively charged drugs migrated toward the anode and were related by their interaction with the micelles. The difference in the mobility of the drugs owing to the presence of the micelles reflected the interaction between these drugs and the micelles. Equations were derived to calculate the capacity factor k' from the migration times in the presence of micelles t' and in the absence of micelles t, the partition coefficients Pwm and the Gibbs free energy. The drugs show different interaction and affinity with the micelles in the systems. Strong interaction was observed between benzoic acid and the micelles. Furthermore, a linear relationship (R = 0.999) was obtained between deltaG(o) and ln Pwm in the micellar solubilization of drugs. These results show that deltaG(o) can give us information on the affinity and on the partition behaviour of the drugs in these systems.
胶束亲和毛细管电泳(MACE)被用于评估苯甲酸、水杨酸、三硝基苯酚、对羟基苯甲酸和邻乙酰水杨酸等各类药物的亲和力。非离子胶束如Brij 35(聚乙二醇十二烷基醚)、Tagat(聚氧乙烯(20)甘油单油酸酯)和吐温20(聚氧乙烯山梨醇单月桂酸酯)在毛细管电泳中用作假固定相。本次实验使用了聚乙烯醇(PVA)涂层毛细管。在pH值为7.2时,这些药物具有负电泳迁移率。带负电荷的药物向阳极迁移,并通过它们与胶束的相互作用而被关联。由于胶束的存在而导致的药物迁移率差异反映了这些药物与胶束之间的相互作用。推导了根据存在胶束时的迁移时间t'和不存在胶束时的迁移时间t、分配系数Pwm和吉布斯自由能来计算容量因子k'的方程。在这些体系中,药物与胶束表现出不同的相互作用和亲和力。观察到苯甲酸与胶束之间存在强烈的相互作用。此外,在药物的胶束增溶中,δG(o)与ln Pwm之间获得了线性关系(R = 0.999)。这些结果表明,δG(o)可以为我们提供有关这些体系中药物的亲和力和分配行为的信息。