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松香树脂和 Eudragit® RS PO 作为功能性薄膜包衣材料的评价。

Evaluation of Rosin Gum and Eudragit® RS PO as a Functional Film Coating Material.

机构信息

Postgraduate in Pharmaceutical Sciences, State University of Maringá, Colombo Avenue, 5790, Maringá, PR, CEP 87020-900, Brazil.

Departament of Pharmacy, Laboratory of Pharmaceutical Nanotechnology, Midwestern State University/UNICENTRO, Guarapuava, PR, Brazil.

出版信息

AAPS PharmSciTech. 2017 Nov;18(8):2854-2861. doi: 10.1208/s12249-017-0766-5. Epub 2017 Apr 14.

Abstract

Polymers are essential tools in the research and development of new therapeutic devices. The diversity and flexibility of these materials have generated high expectations in the composition of new materials with extraordinary abilities, especially in the design of new systems for the modified release of pharmaceutically active ingredients. The natural polymer rosin features moisture protection and pH-dependent behavior (i.e., it is sensitive to pH > 7.0), suggesting its possible use in pharmaceutical systems. The synthetic polymer Eudragit® RS PO is a low-permeability material, the disintegration of which depends on the time of residence in the gastrointestinal tract. The present study developed a polymeric material with desirable physicochemical characteristics and synergistic effects that resulted from the inherent properties of the associated polymers. Isolated films were obtained by solvent evaporation and subjected to a water vapor transmission test, scanning electron microscopy, calorimetry, Fourier transform-infrared (FT-IR) spectroscopy, micro-Raman spectroscopy, and mechanical analysis. The new polymeric material was macroscopically continuous and homogeneous, was appropriately flexible, had low water permeability, was vulnerable in alkaline environments, and was thermally stable, maintaining an unchanged structure up to temperatures of ∼400°C. The new material also presented potentially suitable characteristics for application in film coatings for oral solids, suggesting that it is capable of carrying therapeutic substances to distal regions of the gastrointestinal tract. These findings indicate that this new material may be added to the list of functional excipients.

摘要

聚合物是新治疗设备研发中的重要工具。这些材料的多样性和灵活性使得人们对具有非凡能力的新材料的组成寄予厚望,特别是在设计用于药物活性成分控释的新系统方面。天然聚合物松香具有保湿性和 pH 依赖性(即,对 pH 值 > 7.0 敏感),这表明它可能用于药物系统。合成聚合物 Eudragit® RS PO 是一种低渗透性材料,其崩解取决于在胃肠道中的停留时间。本研究开发了一种具有理想物理化学特性和协同作用的聚合物材料,这是由于相关聚合物的固有特性所致。通过溶剂蒸发获得分离膜,并进行水蒸气传输测试、扫描电子显微镜、差示扫描量热法、傅里叶变换红外(FT-IR)光谱、微拉曼光谱和机械分析。新的聚合物材料宏观上是连续且均匀的,具有适当的柔韧性、低水渗透性、在碱性环境中易受损,并且热稳定,其结构在约 400°C 的温度下保持不变。该新材料还表现出适用于口服固体制剂薄膜包衣的潜在特性,表明其能够将治疗物质输送到胃肠道的远端区域。这些发现表明,这种新材料可能被添加到功能性赋形剂列表中。

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