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理解 CMC 区域内聚山梨醇酯化合物的相互作用。

Understanding polysorbate-compound interactions within the CMC region.

机构信息

School of Applied Sciences, University of Huddersfield, Queensgate, Huddersfield, HD1 3DH, UK.

School of Applied Sciences, University of Huddersfield, Queensgate, Huddersfield, HD1 3DH, UK.

出版信息

J Chromatogr A. 2020 Jul 19;1623:461212. doi: 10.1016/j.chroma.2020.461212. Epub 2020 May 13.

DOI:10.1016/j.chroma.2020.461212
PMID:32505296
Abstract

Non-ionic surfactants such as polysorbates, known as Tween™ 20 and Tween™ 80, are routinely used within the healthcare and pharmaceutical industry to enhance solubility. This work focuses on analysing the two aforementioned polysorbates, each considered at three purity levels with four model compounds, across the critical micellar concentration (CMC) range for each surfactant. Such data is of interest to investigate the influence of micelle formation upon compound-polysorbate interaction. Two analytical techniques were utilised, namely spectroscopic solubility determination and micellar liquid chromatography (MLC). In all cases it was apparent that the maximum solubility for all four compounds increased substantially at concentrations greater than the CMC and that, in most cases, a different retention profile was observed using MLC once the CMC had been exceeded. This paper is the first to have used such techniques to investigate the behaviour of these polysorbates over a series of concentrations and three levels of polysorbate purity. The findings indicate that the solubilisation potential of polysorbates differs once the CMC has been surpassed and is dependent upon the level of purity selected, i.e. compound-surfactant interactions are partially a consequence of the presence of micelles rather than monomer as well as polysorbate purity. Thus, formulators should include such polysorbates at optimised concentrations and purity if they wish to maximise their solubilisation potential.

摘要

非离子表面活性剂,如聚山梨酯,通常被称为吐温™20 和吐温™80,在医疗保健和制药行业中被常规用于提高溶解度。这项工作专注于分析上述两种聚山梨酯,每种聚山梨酯都在三个纯度水平下与四种模型化合物进行分析,跨越每种表面活性剂的临界胶束浓度(CMC)范围。此类数据有助于研究胶束形成对化合物-聚山梨酯相互作用的影响。使用了两种分析技术,即光谱溶解度测定和胶束液相色谱(MLC)。在所有情况下,很明显,所有四种化合物的最大溶解度在 CMC 以上的浓度下大大增加,并且在大多数情况下,一旦超过 CMC,使用 MLC 就会观察到不同的保留曲线。本文首次使用这些技术在一系列浓度和三种聚山梨酯纯度水平下研究这些聚山梨酯的行为。研究结果表明,CMC 超过后,聚山梨酯的增溶潜力不同,并且取决于所选的纯度水平,即化合物-表面活性剂相互作用部分是胶束的存在而不是单体以及聚山梨酯纯度的结果。因此,如果希望最大限度地提高增溶潜力,配方师应在优化的浓度和纯度下包含此类聚山梨酯。

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