Department of Pharmaceutical Technology and Biopharmaceutics, Jagiellonian University Medical College, Kraków, Poland.
Polim Med. 2022 Jan-Jun;52(1):19-29. doi: 10.17219/pim/150267.
As the number of new drug candidates that are poorly soluble in water grows, new technologies that enable the enhancement of their solubility are needed. This is the case with amorphous solid dispersions (ASDs) that, nowadays, not only ensure the solubility, but can also be used to control the release rate of poorly soluble drugs. However, this dosage form must overcome the major disadvantage of ASDs, which is limited stability upon storage. Thus, a thorough knowledge on polymeric carriers that can enhance drug solubility while ensuring stability in the amorphous form is necessary. In this review, the state of the art in the application of Kollidon® VA 64 (copovidone) and Soluplus® (graft copolymer of polyvinyl caprolactam-polyvinyl acetate and poly(ethylene glycol) (PEG)) in the manufacturing of ASDs over the last 20 years is presented. Apart from the classical methods, namely solvent evaporation or melting, more advanced technologies such as pulse combustion drying, high-speed electrospinning and single-step 3D printing are described. It has been shown that both the dissolution rate (in vitro) and enhancement in bioavailability (in vivo) regarding poorly soluble active ingredients of natural or synthetic origin are possible using these matrix-forming polymers.
随着越来越多的新候选药物在水中的溶解度较差，需要开发新的技术来提高它们的溶解度。无定形固体分散体（ASD）就是这种情况，它不仅可以确保溶解度，还可以控制难溶性药物的释放速度。然而，这种剂型必须克服 ASD 的主要缺点，即在储存时稳定性有限。因此，需要深入了解可以提高药物溶解度同时确保无定形形式稳定性的聚合物载体。在这篇综述中，介绍了过去 20 年来 Kollidon® VA 64（共聚维酮）和 Soluplus®（聚维酮己内酯-聚醋酸乙烯酯和聚（乙二醇）接枝共聚物（PEG））在 ASD 制造中的应用现状。除了经典的方法，如溶剂蒸发或熔融，还描述了更先进的技术，如脉冲燃烧干燥、高速静电纺丝和单步 3D 打印。已经表明，使用这些基质形成聚合物可以提高天然或合成来源的难溶性活性成分的溶解速率（体外）和生物利用度（体内）。
