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重温pK_a-Flux方法来确定内在膜的透性

Carolin Dahley¹, Kai-Uwe Goss², Andrea Ebert¹

¹Department of Analytical Environmental Chemistry, Helmholtz Centre for Environmental Research (UFZ), Permoserstraße 15, Leipzig 04318, Germany.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

|September 26, 2023

概括

这项研究修订了pKa-Flux方法来确定内在膜透性,考虑到度转移效应. 建议使用iso-pH方法作为对脂友基的梯度-pH方法更准确的替代方法.

科学领域:

药理动力学药理动力学
生物物理化学生物物理化学
细胞生物学细胞生物学

背景情况:

内膜的透性对于肠道药物吸收至关重要.
使用跨井测定 (Caco-2/MDCK细胞) 的pKa-Flux方法是测量透性的标准.
现有的梯度-pH pKa-Flux方法忽略了度转移效应,导致不准确的透度值.

研究的目的:

开发一个修订的pKa-Flux方法,以纠正度转移效应.
评价iso-pH方法作为比梯度-pH方法更优越的替代方法.
为了比较内部膜透性的提取性,使用两种方法对脂友基进行比较.

主要方法:

修订的梯度-pH pKa-Flux方法,包括细胞质,过器和底侧边界层中的度转移效应.
拟议的iso-pH pKa-Flux方法仅考虑细胞度转移效应.
使用五种脂友基的实验验证:阿曼塔丁,诺基因,兰,文拉法辛和维拉帕米尔.

主要成果:

修订后的梯度-pH方法和iso-pH方法提供了更准确的内在膜透度值.
在确定脂友基的透性时,iso-pH方法是有利的.
在这项研究中确定的内膜透率明显高于之前报告的值.

结论:

度转移效应至关重要,必须在pKa-Flux分析中加以解决.
异位-pH方法为评估内在膜透性提供了更可靠的方法,特别是对于脂性化合物.
这项工作需要重新评估现有的肠道吸收和透率数据.

关键词:

水性边界层是一种水性边界层.在Caco-2中使用.度转移 - 度转移 - 度转移这就是MDCKK的MDCK.被动透性是一种被动的透性.pK(a) - 流量方法

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