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罗森假设对于研究胆酸氧乙基化产物的结构与亲脂性治疗药物(BCS II类和IV类)在平衡水溶液中的增溶过程之间关系的有用性。

Usefulness of Rosen's postulate for studying the relationship between the structure of cholic acid oxyethylation products and the process of solubilization of lipophilic therapeutic agents (BCS class II and IV) in aqueous solutions in equilibrium.

作者信息

Nachajski Michał Jakub, Kolodziejczyk Michał Krzysztof, Lukoseki Marek, Kosno Jacek, Kołodziejska Justyna, Zgoda Marian Mikołaj

出版信息

Acta Pol Pharm. 2014 Jul-Aug;71(4):637-45.

Abstract

We verified the usefulness of "Rosen's postulate", i.e., the logarithm of reciprocal concentration of surfactant--log(1/cPi=20) by which the surface tension of a solution can be decreased by 20 mJ/m2 in relation to water (physiological value gamma25 = 48-52 mJ/m2) in the evaluation of the applicatory properties of cholic acid oxyethylation products. Moreover, the values of deltaG0m for solubilizers and their micellar adducts with diclofenac, naproxen, and loratadine constituted the basis for estimating the thermodynamic value of "Rebinder's effect", associated with change in the state of matter of therapeutic agent. We determined critical micellar concentration for the aqueous products of oxyethylation and for micellar adducts with diclofenac, naproxen, and loratadine, and used these values to calculate (thermodynamic potential of micelle formation).

摘要

我们验证了“罗森假设”的实用性,即在评估胆酸乙氧基化产物的应用性能时,表面活性剂的倒数浓度的对数——log(1/cPi=20),通过该对数,溶液的表面张力相对于水(生理值gamma25 = 48 - 52 mJ/m2)可降低20 mJ/m2。此外,增溶剂及其与双氯芬酸、萘普生和氯雷他定的胶束加合物的deltaG0m值构成了估算与治疗剂物质状态变化相关的“雷宾德效应”热力学值的基础。我们测定了乙氧基化水性产物以及与双氯芬酸、萘普生和氯雷他定的胶束加合物的临界胶束浓度,并使用这些值来计算(胶束形成的热力学势)。

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