Kollidon®VA 64和Soluplus®作为非晶固体分散体的现代聚合物载体。

Q3 Medicine Polimery w medycynie Pub Date : 2022-01-01 DOI:10.17219/pim/150267
Dominik Strojewski, Anna Krupa
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引用次数: 11

摘要

随着难溶于水的新候选药物数量的增加,需要能够提高其溶解度的新技术。无定形固体分散体(ASDs)就是这种情况,如今,它不仅可以保证溶解度,还可以用来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,即储存后的稳定性有限。因此,对聚合物载体的全面了解,可以提高药物的溶解度,同时确保在无定形的稳定性是必要的。在这篇综述中,介绍了过去20年来Kollidon®VA 64 (copovidone)和Soluplus®(聚乙烯-己内酰胺-聚醋酸乙烯和聚乙二醇的接枝共聚物)在asd制造中的应用现状。除了溶剂蒸发或熔融等经典方法外,还介绍了脉冲燃烧干燥、高速静电纺丝和单步3D打印等更先进的技术。研究表明,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体外溶出率和体内生物利用度。
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Kollidon® VA 64 and Soluplus® as modern polymeric carriers for amorphous solid dispersions.

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.

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来源期刊
Polimery w medycynie
Polimery w medycynie Medicine-Medicine (all)
CiteScore
3.30
自引率
0.00%
发文量
9
审稿时长
53 weeks
期刊最新文献
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