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Understanding of Relationship between Phospholipid Membrane Permeability and Self-Diffusion Coefficients of Some Drugs and Biologically Active Compounds in Model Solvents
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2017-09-08 00:00:00 , DOI: 10.1021/acs.molpharmaceut.7b00401 Svetlana V. Blokhina 1 , Tatyana V. Volkova 1 , Vasiliy A. Golubev 1 , German L. Perlovich 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2017-09-08 00:00:00 , DOI: 10.1021/acs.molpharmaceut.7b00401 Svetlana V. Blokhina 1 , Tatyana V. Volkova 1 , Vasiliy A. Golubev 1 , German L. Perlovich 1
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In this work we measured self-diffusion coefficients of 5 drugs (aspirin, caffeine, ethionamide, salicylic acid, and paracetamol) and 11 biologically active compounds of similar structure in deuterated water and 1-octanol by NMR. It has been found that an increase in the van der Waals volume of the molecules of the studied substances result in reduction of their diffusion mobility in both solvents. The analysis of the experimental data showed the influence of chemical nature and structural isomerization of the molecules on the diffusion mobility. Apparent permeability coefficients of the studied compounds were determined using an artificial phospholipid membrane made of egg lecithin as a model of in vivo absorption. Distribution coefficients in 1-octanol/buffer pH 7.4 system were measured. For the first time the model of the passive diffusion through the phospholipid membrane was validated based on the experimental data. To this end, the passive diffusion was considered as an additive process of molecule passage through the aqueous boundary layer before the membrane and 1-octanol barrier simulating the lipid layer of the membrane.
中文翻译：
了解模型溶剂中某些药物和生物活性化合物的磷脂膜通透性与自扩散系数之间的关系
在这项工作中，我们通过NMR测量了5种药物（阿司匹林，咖啡因，乙酰胺，水杨酸和对乙酰氨基酚）和11种结构相似的生物活性化合物在氘水和1-辛醇中的自扩散系数。已经发现，所研究物质的分子的范德华体积的增加导致它们在两种溶剂中的扩散迁移率降低。实验数据的分析表明分子的化学性质和结构异构化对扩散迁移率的影响。使用卵磷脂制成的人工磷脂膜作为体内吸收的模型，确定了所研究化合物的表观渗透系数。测量了在1-辛醇/缓冲液pH 7.4系统中的分配系数。首次基于实验数据验证了通过磷脂膜的被动扩散模型。为此，在膜和1-辛醇屏障模拟膜的脂质层之前，被动扩散被认为是分子通过水边界层的附加过程。
更新日期：2017-09-08
中文翻译：
了解模型溶剂中某些药物和生物活性化合物的磷脂膜通透性与自扩散系数之间的关系
在这项工作中，我们通过NMR测量了5种药物（阿司匹林，咖啡因，乙酰胺，水杨酸和对乙酰氨基酚）和11种结构相似的生物活性化合物在氘水和1-辛醇中的自扩散系数。已经发现，所研究物质的分子的范德华体积的增加导致它们在两种溶剂中的扩散迁移率降低。实验数据的分析表明分子的化学性质和结构异构化对扩散迁移率的影响。使用卵磷脂制成的人工磷脂膜作为体内吸收的模型，确定了所研究化合物的表观渗透系数。测量了在1-辛醇/缓冲液pH 7.4系统中的分配系数。首次基于实验数据验证了通过磷脂膜的被动扩散模型。为此，在膜和1-辛醇屏障模拟膜的脂质层之前，被动扩散被认为是分子通过水边界层的附加过程。
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