表面活性剂在溶解水溶性差的药物方面的局限性和创新应用方法。

Gang Jin, Jie Wang, Jie Xu, Qing Jin, Jian-Fei Xue, Lin-Han Li
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引用次数: 0

摘要

药物溶解度低会导致生物利用率和治疗效率低下。很大一部分未被开发和上市供患者使用的药物就是因为其溶解度极低。因此,提高水溶性差的药物的溶解度是药物研究领域最重要的方面之一。随着越来越多制剂技术和辅料应用的不断发展,包括 pH 微环境调节技术、包合络合物、固体分散技术、纳米技术和表面活性剂的应用等,都可以在一定程度上改善水溶性差的药物的溶解度,从而获得更好的药代动力学和药效学。但其中应用最广泛的是表面活性剂的应用。这种技术可以降低表面张力,改善润湿性,形成胶束后具有显著的增溶能力。然而,人们也发现表面活性剂在增溶方面有一定的局限性。本综述从几个方面总结了影响表面活性剂增溶和限制其应用的因素。这些因素包括药物、添加剂和介质。同时也提出了一些解决这些应用限制的思路,为今后表面活性剂的更广泛应用奠定了基础。
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Limitations and Innovative Application Methods of Surfactants for Solubilization of Poorly Water-Soluble Drugs.

Poor solubility of drugs leads to poor bioavailability and therapeutic efficiency. A large proportion of drugs that are not developed and marketed for use by patients are due to their extremely low solubility. Therefore, improving the solubility of poorly water-soluble drugs is one of the most important aspects of the field of drug research. With the continuous development of more and more formulation techniques and excipient applications, the solubility of poorly water-soluble drugs can be improved to a certain extent to obtain better pharmacokinetics and pharmacodynamics, including pH microenvironment regulation technology, inclusion complex, solid dispersion, nanotechnology, and application of surfactants. However, the most widely used among them is the application of surfactants. This technique can reduce the surface tension, improve wettability, and have a remarkable solubilizing ability after forming micelles. However, surfactants have also been found to possess certain limitations in solubilization. In this review, the factors affecting the solubilization of surfactants and limiting their application have been summarized from several aspects. These factors include drugs, additives, and media. Some ideas to solve these application limitations have also been put forward, which can lay a foundation for the wider application of surfactants in the future.

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