通过洗脱液凝胶渗透色谱法研究药物在胶束系统中的增溶作用。

Solubilisation of drugs in micellar systems studied by eluent gel permeation chromatography.

作者信息

Draper M, Savage M, Collett J H, Attwood D, Price C, Booth C, Wang Q G

机构信息

Manchester Polymer Centre, University of Manchester, UK.

出版信息

Pharm Res. 1995 Aug;12(8):1231-7. doi: 10.1023/a:1016232514650.

DOI:10.1023/a:1016232514650

PMID:7494839

Abstract

PURPOSE

The purpose of the study was to investigate the potential of a chromatographic method which is based on elution gel chromatography (EGPC) in the study of solubilisation of drugs in micellar solutions.

METHODS

The EGPC method differs from conventional GPC in the use of a solution of the associating surfactant as eluent (rather than solvent) and the injection of a small volume of solution of different concentration (or alternatively injection of solvent alone) to probe the association equilibrium in the eluent. The technique was applied to a study of the solubilisation of selected drugs in aqueous micellar solutions of a triblock copolymer (Synperonic-PE F127) composed of oxyethylene [E, OCH2CH2] and oxypropylene [P, OCH2CH(CH3)] units with nominal molecular formula E98P67E98.

RESULTS

EGPC curves were obtained showing vacancy peaks at the elution volumes of the drugs, clearly demonstrating their solubilisation. In addition, the micelle-molecule equilibrium of the copolymer surfactant could be monitored at all times. Quantitative determination of the partition of solute between micelles and solvent phase was not possible due to the incomplete conversion of molecules to micelles in solutions of the selected copolymer.

CONCLUSIONS

The EGPC technique provides evidence for the solubilisation of the drugs in aqueous solutions of Synperonic F127; a more thorough assessment of its potential for quantitative measurement of solubilisation requires the use of a surfactant which is wholly (or at least mainly) in the micellar state under the conditions of use.

摘要

目的

本研究旨在探讨一种基于洗脱凝胶色谱法（EGPC）的色谱方法在研究药物在胶束溶液中增溶作用方面的潜力。

方法

EGPC方法与传统凝胶渗透色谱法的不同之处在于，使用缔合表面活性剂溶液作为洗脱剂（而非溶剂），并注入少量不同浓度的溶液（或者仅注入溶剂）以探测洗脱剂中的缔合平衡。该技术应用于研究选定药物在由氧乙烯[E，OCH₂CH₂]和氧丙烯[P，OCH₂CH(CH₃)]单元组成、标称分子式为E98P67E98的三嵌段共聚物（Synperonic - PE F127）的水性胶束溶液中的增溶作用。