Draper M, Savage M, Collett J H, Attwood D, Price C, Booth C, Wang Q G
Manchester Polymer Centre, University of Manchester, UK.
Pharm Res. 1995 Aug;12(8):1231-7. doi: 10.1023/a:1016232514650.
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.
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.
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.
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.
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。
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。
获得了EGPC曲线，显示在药物的洗脱体积处有空位峰，清楚地证明了它们的增溶作用。此外，可随时监测共聚物表面活性剂的胶束 - 分子平衡。由于在选定共聚物的溶液中分子未完全转化为胶束，因此无法对溶质在胶束和溶剂相之间的分配进行定量测定。
EGPC技术为药物在Synperonic F127水溶液中的增溶作用提供了证据；要更全面地评估其在增溶定量测量方面的潜力，需要使用在使用条件下完全（或至少主要）处于胶束状态的表面活性剂。
