Vasconcelos Teófilo, Sarmento Bruno, Costa Paulo
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, Rua Aníbal Cunha 164, 4050-047 Porto, Portugal.
Drug Discov Today. 2007 Dec;12(23-24):1068-75. doi: 10.1016/j.drudis.2007.09.005. Epub 2007 Oct 30.
Solid dispersions are one of the most promising strategies to improve the oral bioavailability of poorly water soluble drugs. By reducing drug particle size to the absolute minimum, and hence improving drug wettability, bioavailability may be significantly improved. They are usually presented as amorphous products, mainly obtained by two major different methods, for example, melting and solvent evaporation. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the recent advances related on the area of solid dispersions.
固体分散体是提高难溶性药物口服生物利用度最具前景的策略之一。通过将药物粒径减小到绝对最小值,从而改善药物润湿性,可显著提高生物利用度。它们通常呈现为无定形产物,主要通过两种主要不同方法获得,例如熔融法和溶剂蒸发法。最近,已加入表面活性剂来稳定制剂,从而避免药物重结晶并增强其溶解度。还开发了获得固体分散体的新制造工艺以减少初始工艺的缺点。在本综述中,旨在讨论固体分散体领域的最新进展。