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α-(壬基苯基)-ω-羟基癸(氧乙烯)、正烷基胺和脂肪酸的水性胶束溶液中胆固醇一水合物溶解速率的研究

Cholesterol monohydrate dissolution rate studies in aqueous micellar solutions of alpha-(nonylphenyl)-omega-hydroxydeca(oxyethylene), n-alkylamines, and fatty acids.

作者信息

Gupta S L, Higuchi W I, Ho N F

出版信息

J Pharm Sci. 1985 Nov;74(11):1172-7. doi: 10.1002/jps.2600741108.

Abstract

The influences of electrical and nonelectrical factors in the interfacially controlled dissolution of cholesterol monohydrate by mixed micelles of alpha-(nonylphenyl)-omega-hydroxydeca(oxyethylene) (polyoxyethylene [10]-nonylphenol ether; POEPE; 1) in combination with long-chain n-alkylamines or fatty acids were investigated and quantified under pH conditions where the amines and fatty acids exist in their charged and uncharged forms. The experimental findings were generally consistent with a mechanism involving micelle collision with the cholesterol surface. A significant interfacial barrier was found with neutral micelles; however, the magnitude of the barrier was smaller with uncharged mixed micelles than with the simple micelles of 1. With charged micelles, the interfacial mass transfer resistance decreased with the addition of sodium chloride to the extent that the interfacial barrier was essentially abolished and the dissolution kinetics became convective/diffusion controlled. The results are consistent with the phenomena of diffusion of charged micelles toward a charged surface, following the classical collision kinetic theory of colloids. The ease in the transfer of cholesterol monohydrate molecules from the crystal surface and into the micelles during the collision step was examined by considering factors affecting the crystal surface as well as those associated with the hydrophobic-hydrophilic structure of the micelle of 1 and the distribution of charged and uncharged amphipathic additives within the basic micelle structure of 1.

摘要

研究并量化了α-(壬基苯基)-ω-羟基癸(氧乙烯)(聚氧乙烯[10]-壬基酚醚;POEPE;1)与长链正烷基胺或脂肪酸形成的混合胶束在界面控制胆固醇一水合物溶解过程中电因素和非电因素的影响,实验是在胺和脂肪酸分别以带电和不带电形式存在的pH条件下进行的。实验结果总体上与胶束与胆固醇表面碰撞的机制一致。发现中性胶束存在显著的界面屏障;然而,不带电混合胶束的屏障幅度比1的简单胶束小。对于带电胶束,添加氯化钠会降低界面传质阻力,直至界面屏障基本消除,溶解动力学变为对流/扩散控制。这些结果与带电胶束根据经典胶体碰撞动力学理论向带电表面扩散的现象一致。通过考虑影响晶体表面的因素以及与1的胶束疏水-亲水结构以及带电和不带电两亲添加剂在1的基本胶束结构内的分布相关的因素,研究了碰撞步骤中胆固醇一水合物分子从晶体表面转移到胶束中的难易程度。

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