Ma L, Ramachandran C, Weiner N D
College of Pharmacy, University of Michigan, Ann Arbor 48109.
J Pharm Sci. 1992 Nov;81(11):1104-8. doi: 10.1002/jps.2600811113.
This study compares the bilayer-water distribution coefficients of a homologous series of n-alkyl p-aminobenzoates in liposomes with their respective distribution coefficients in octanol-water, oleyl alcohol-water, and hexane-water systems. The data indicate that the bilayer-water distribution coefficient is quite sensitive to changes in solute structure and to the structural organization of the bilayer and that octanol, oleyl alcohol, and hexane are able to reflect the partitioning changes that occur in the liposomal bilayer with respect to increasing the alkyl chain length of n-alkyl p-aminobenzoates. For this particular homologous series, the hexane-water system tended to underestimate the bilayer-water distribution coefficients, whereas octanol-water and oleyl alcohol-water systems overestimated solute partitioning into the bilayer. The similarity of the lipid environment, with respect to solute partitioning, in the organic solvent system and that in liposomes can be ascertained by using the Collander relationship.
本研究比较了一系列对氨基苯甲酸正烷基酯在脂质体中的双层-水分配系数与其在正辛醇-水、油醇-水和己烷-水体系中的各自分配系数。数据表明，双层-水分配系数对溶质结构的变化以及双层的结构组织相当敏感，并且正辛醇、油醇和己烷能够反映随着对氨基苯甲酸正烷基酯烷基链长度增加，脂质体双层中发生的分配变化。对于这个特定的同系物系列，己烷-水体系往往低估双层-水分配系数，而正辛醇-水和油醇-水体系则高估溶质在双层中的分配。通过使用科兰德关系，可以确定有机溶剂体系和脂质体中关于溶质分配的脂质环境的相似性。
