Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India.
Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark.
Adv Drug Deliv Rev. 2016 May 1;100:116-25. doi: 10.1016/j.addr.2015.12.009. Epub 2016 Jan 21.
Co-amorphous drug delivery systems have recently gained considerable interest in the pharmaceutical field because of their potential to improve oral bioavailability of poorly water-soluble drugs through drug dissolution enhancement as a result of the amorphous nature of the material. A co-amorphous system is characterized by the use of only low molecular weight components that are mixed into a homogeneous single-phase co-amorphous blend. The use of only low molecular weight co-formers makes this approach very attractive, as the amount of amorphous stabilizer can be significantly reduced compared with other amorphous stabilization techniques. Because of this, several research groups started to investigate the co-amorphous formulation approach, resulting in an increasing amount of scientific publications over the last few years. This study provides an overview of the co-amorphous field and its recent findings. In particular, we investigate co-amorphous formulations from the viewpoint of solid dispersions, describe their formation and mechanism of stabilization, study their impact on dissolution and in vivo performance and briefly outline the future potentials.
共无定形药物传递系统最近在制药领域引起了相当大的兴趣,因为它们有可能通过提高药物的溶解度来改善水溶性差的药物的口服生物利用度,这是由于材料的无定形性质。共无定形系统的特点是仅使用低分子量的成分,将其混合到均匀的单相共无定形混合物中。仅使用低分子量共成型剂使这种方法非常有吸引力,因为与其他无定形稳定技术相比,可以显著减少无定形稳定剂的用量。正因为如此,几个研究小组开始研究共无定形配方方法,导致过去几年的科学出版物数量不断增加。本研究概述了共无定形领域及其最新发现。特别是,我们从固体分散体的角度研究了共无定形制剂,描述了它们的形成和稳定机制,研究了它们对溶解和体内性能的影响,并简要概述了未来的潜力。