药物的溶解性差导致差的生物利用度和治疗效率。大部分未开发和销售以供患者使用的药物是由于它们极低的溶解度。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。随着越来越多的配方技术和辅料应用的不断发展,在一定程度上提高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,包括pH微环境调节技术,包合物,固体分散体,纳米技术,和表面活性剂的应用。然而,其中最广泛使用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,还发现表面活性剂在溶解中具有某些限制。在这次审查中,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,和媒体。也提出了一些解决这些应用局限性的思路,为今后表面活性剂的广泛应用奠定了基础。
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.