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β-环糊精衍生物由于具有可与水溶性差的药物分子形成超分子包合物以提高药物溶解度等重要性能而被视为一种极具潜力和广泛用途的新型药用生物材料.然而,目前此类衍生物的常用合成方法大多存在反应步骤繁琐、成本昂贵、产出率低、使用有毒且可能造成环境污染的有机溶剂等诸多缺点.有鉴于此,探索高效、环保的新合成方法成为近年来研究的重要课题.报道一种在水溶液中一步合成β-环糊精衍生物的方法.利用这种方法成功制备了磺烷基醚-β-环糊精衍生物——磺丙基醚-β-环糊精(SPE-β-CD)和磺丁基醚-β-环糊精(SBE-β-CD),并对其进行了详细的材料表征和测定了其与常用抗真菌药氟康唑形成超分子包合物时对药物溶解度的增强作用.实验结果表明,在水溶液中一步合成的β-环糊精衍生物不仅在结构上相近于商品化的β-环糊精衍生物,而且在对药物溶解度的增强作用上也至少不低于商品化的β-环糊精衍生物.可见这一简单的一步合成法有可能为医药行业低成本地大量生产β-环糊精衍生物生物材料提供了一条有效的蹊径.
β-Cyclodextrin derivatives have been considered as a new potential medicinal biomaterial with wide application due to their ability to form supramolecular inclusion complexes with poorly water-soluble drug molecules to improve drug solubility, etc. However, At present, most of the commonly used synthetic methods of such derivatives have many shortcomings, such as cumbersome reaction steps, high cost, low yield, use of toxic organic solvents that may cause environmental pollution, etc. In view of this, the exploration of new synthetic methods of high efficiency and environmental protection has become In recent years, an important research topic reported.A report on a method for the synthesis of β-cyclodextrin derivatives in aqueous solution.With this method successfully prepared sulfoalkyl ether-β-cyclodextrin derivatives - sulfopropyl ether β-cyclodextrin (SPE-β-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD) were synthesized and characterized. The effect of fluconazole when forming supramolecular inclusion complex on drug solubility was enhanced.The experimental results show that β-cyclodextrin derivatives synthesized in one step in aqueous solution are not only structurally similar to the commercial β-cyclodextrin derivatives , But also on the solubility of the drug Strongly acting at least not less than the commercial beta-cyclodextrin derivatives. This shows that this simple one-step synthesis method for the pharmaceutical industry is likely to mass production of β-cyclodextrin derivatives of biomaterials provides an effective The path.