A major issue of the pharmaceutical industry is the poor solubility, permeability, and bioavailability of most active ingredients. These properties also induce the accumulation of pharmaceuticals in groundwater, surface water, wastewater, soils and biota. Therefore, enhancing the solubility and bioavailability of pharmaceuticals could allow the prescription of lower doses, and could reduce environmental impact. Pharmaceutical solubility can be increased by pH modification, salt formation, ionization, complexation, and co-solvency. Here we report for the first time the use of cyclodextrin-based low-melting mixtures for the solubilization of four steroids: beclomethasone dipropionate, budesonide, fluticasone propionate and mometasone furoate. First, a low-melting mixture was prepared from sulfobutylether-β-cyclodextrin and levulinic acid, and characterized. Then, the shake flask method was used to determine the solubility of the drugs in this low-melting mixture. Results show a 4000-fold increase of the solubility of fluticasone propionate using the low-melting, cyclodextrin-based mixture versus water. This huge solubility enhancement could be explained by the formation of an inclusion complex with the cyclodextrin within the low-melting mixture.

制药工业的一个主要问题是大多数活性成分的溶解度、渗透性和生物利用度都很差。这些特性还诱导药物在地下水、地表水、废水、土壤和生物群中的积累。因此，提高药物的溶解度和生物利用度可以允许开出较低剂量的处方，并可以减少对环境的影响。药物溶解度可以通过改变 pH 值、形成盐、电离、络合和共溶解来增加。在这里，我们首次报道了使用基于环糊精的低熔点混合物来溶解四种类固醇：二丙酸倍氯米松、布地奈德、丙酸氟替卡松和糠酸莫米松。首先，由磺基丁基醚-β-环糊精和乙酰丙酸制备低熔点混合物，和特点。然后，使用摇瓶法测定药物在这种低熔点混合物中的溶解度。结果表明，与水相比，使用基于环糊精的低熔点混合物，丙酸氟替卡松的溶解度增加了 4000 倍。这种巨大的溶解度提高可以通过在低熔点混合物中与环糊精形成包合物来解释。