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聚乙烯醇(PVA)对 PVA-聚-N-羟乙基天冬酰胺(PVA-PHEA)微晶固体分散体薄膜的影响。

Influence of Polyvinyl Alcohol (PVA) on PVA-Poly-N-hydroxyethyl-aspartamide (PVA-PHEA) Microcrystalline Solid Dispersion Films.

机构信息

King's College London, London, UK.

University of Study of Palermo, Palermo, Italy.

出版信息

AAPS PharmSciTech. 2020 Oct 2;21(7):267. doi: 10.1208/s12249-020-01811-z.

Abstract

This study was conducted to formulate buccal films consisting of polyvinyl alcohol (PVA) and poly-N-hydroxyethyl-aspartamide (PHEA), to improve the dissolution of the drug through the oral mucosa. Ibuprofen sodium salt was used as a model drug, and the buccal film was expected to enhance its dissolution rate. Two different concentrations of PVA (5% w/v and 7.5% w/v) were used. Solvent casting was used to prepare films, where a solution consisting of drug and polymer was cast and allowed to dry. Attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM) were used to investigate the properties of films. In vitro dissolution studies were also conducted to investigate drug release. SEM studies showed that films containing a higher concentration of PVA had larger particles in microrange. FTIR studies confirmed the presence of the drug in films and indicated that ibuprofen sodium did not react with polymers. DSC studies confirmed the crystalline form of ibuprofen sodium when incorporated within films. In vitro dissolution studies found that the dissolution percentage of ibuprofen sodium alone was increased when incorporated within the film from 59 to 74%. This study led to the development of solid microcrystalline dispersion as a buccal film with a faster dissolution rate than the drug alone overcoming problem of poor solubility.

摘要

本研究旨在制备包含聚乙烯醇(PVA)和聚-N-羟乙基天冬酰胺(PHEA)的颊膜,通过口腔黏膜提高药物的溶解率。布洛芬钠盐被用作模型药物,预计颊膜会提高其溶解速率。使用了两种不同浓度的 PVA(5%w/v 和 7.5%w/v)。溶剂浇铸法用于制备薄膜,将包含药物和聚合物的溶液浇铸并干燥。衰减全反射傅里叶变换红外光谱(ATR-FTIR)、差示扫描量热法(DSC)和扫描电子显微镜(SEM)用于研究薄膜的性能。还进行了体外溶解研究以研究药物释放。SEM 研究表明,含有较高浓度 PVA 的薄膜在微范围内具有较大的颗粒。FTIR 研究证实了薄膜中存在药物,并且表明布洛芬钠没有与聚合物发生反应。DSC 研究证实了布洛芬钠在掺入薄膜内时的结晶形式。体外溶解研究发现,当布洛芬钠单独掺入薄膜中时,其溶解百分比从 59%增加到 74%。这项研究导致了固体微晶分散体作为颊膜的开发,其溶解速率比单独使用药物更快,克服了溶解度差的问题。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0209/7532132/3523c6a4ea14/12249_2020_1811_Fig1_HTML.jpg

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