Current state of the art in HPLC methodology for lipophilicity assessment of basic drugs. A review
Current state of the art in HPLC methodology for lipophilicity assessment of basic drugs. A review
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DOI：
10.1080/10826070701665626
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发表时间：
2008-01-01
影响因子：
1.3
通讯作者：
Tsantili-Kakoulidou, Anna
中科院分区：
文献类型：
--
作者：
Giaginis, Costas;Tsantili-Kakoulidou, Anna
高效液相色谱法提供了一种用户友好、快速、节省化合物的方法，已成功应用于测定药物亲脂性。在合适的色谱条件下，等度和外推保留因子与正辛醇-水分配系数或分配系数相关性良好。本审查提供了一个概述的固定和移动的相，这是优选用于亲脂性评估主要是在碱性化合物的情况下。提出了困难的亲硅烷相互作用的干扰分配机制，并提出了面对这个问题的方法进行了讨论。注意外推程序和条件的标准化，以获得外推保留因子与logP或logD之间的1：1相关性。简要介绍了编码亲脂行为信息的其他色谱指数。一个单独的部分涉及IAM色谱的最新进展，其与反相HPLC和辛醇-水系统的相似性/差异性，以及其模拟与磷脂特异性相互作用的潜力。
HPLC provides a user's friendly, rapid, and compound sparing methodology, which is successfully applied to determine drug lipophilicity. Under suitable chromatographic conditions isocratic and extrapolated retention factors correlate well with octanol-water partition or distribution coefficients. The present review provides an overview of the stationary and mobile phases, which are preferably used for lipophilicity assessment mainly in the case of basic compounds. Difficulties raised by the interference of silanophilic interactions in the partition mechanism, and the ways proposed to face this problem are discussed. Attention has been given to the extrapolation procedure and the standardization of conditions to obtain 1:1 correlation between extrapolated retention factors and logP or logD. Other chromatographic indices encoding information on the lipophilic behavior are briefly presented. A separate section refers to recent advances in IAM Chromatography, its similarities/dissimilarities with reversed phase HPLC and the octanol-water system, as well as its potential to mimic specific interactions with phospholipids.