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含有经球磨处理的阿立哌唑-聚氧乙烯 407 固体分散体的口崩膜。

Orodispersible films containing ball milled aripiprazole-poloxamer®407 solid dispersions.

机构信息

Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.

School of Pharmacy, University of Birmingham, Edgbaston B15 2TT, United Kingdom.

出版信息

Int J Pharm. 2020 Feb 15;575:118955. doi: 10.1016/j.ijpharm.2019.118955. Epub 2019 Dec 13.

Abstract

This research aimed at developing ODFs containing an antipsychotic drug - aripiprazole (ARP). ARP, as a BCS II class molecule, requires enhancing its water solubility prior to formulating. Therefore, a solid dispersion of ARP - Poloxamer® 407 was prepared by ball milling, then incorporated into the films. It was found that co-processing led to an over 100-fold increase in drug solubility in comparison with pure drug. Moreover, ODFs with solid dispersion showed faster drug release (>95% below 15 min) and disintegration (<30 s), compared with raw ARP films. These results are believed to be due to the solubilization effect of poloxamer and enhanced wettability of the film. Films containing solid dispersions were found to possess smoother film surfaces and favorable mechanical properties - flexibility and strength. The ODF formulations, prepared by a casting method, were based on three different polymers (Kollicoat® IR, Kollicoat® Protect or PVA). It was found that not only the form of the incorporated drug, but also the type of film-forming polymer had an impact on the analyzed parameters. The use of PVA was beneficial in the film formulation with aripiprazole in comparison to other tested film-forming polymers.

摘要

本研究旨在开发含有抗精神病药物 - 阿立哌唑(ARP)的 ODFs。ARP 作为 BCS II 类分子,在制剂前需要提高其水溶性。因此,通过球磨制备了 ARP-聚氧乙烯 407 的固体分散体,然后将其掺入薄膜中。结果发现,与纯药物相比,共加工导致药物溶解度提高了 100 多倍。此外,与原始 ARP 薄膜相比,含有固体分散体的 ODF 表现出更快的药物释放(<15 分钟时释放超过 95%)和崩解(<30 秒)。这些结果归因于聚氧乙烯的增溶作用和薄膜的润湿性增强。发现含有固体分散体的薄膜具有更光滑的薄膜表面和有利的机械性能-柔韧性和强度。通过浇铸法制备的 ODF 制剂基于三种不同的聚合物(Kollicoat®IR、Kollicoat®Protect 或 PVA)。结果发现,不仅掺入药物的形式,而且成膜聚合物的类型也会对分析参数产生影响。与其他测试的成膜聚合物相比,在含有阿立哌唑的薄膜配方中使用 PVA 是有益的。

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