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Eudragit:技术评估。

Eudragit: a technology evaluation.

机构信息

GVM College of Pharmacy, Sonipat, India.

出版信息

Expert Opin Drug Deliv. 2013 Jan;10(1):131-49. doi: 10.1517/17425247.2013.736962. Epub 2012 Oct 26.

Abstract

INTRODUCTION

Eudragit is the brand name for a diverse range of polymethacrylate-based copolymers. It includes anionic, cationic, and neutral copolymers based on methacrylic acid and methacrylic/acrylic esters or their derivatives.

AREAS COVERED

In this review, the physicochemical characteristics and applications of different grades of Eudragit in colon-specific/enteric-coated/sustained release drug delivery and taste masking have been addressed.

EXPERT OPINION

Eudragits are amorphous polymers having glass transition temperatures between 9 to > 150(o)C. Eudragits are non-biodegradable, nonabsorbable, and nontoxic. Anionic Eudragit L dissolves at pH > 6 and is used for enteric coating, while Eudragit S, soluble at pH > 7 is used for colon targeting. Studies in human volunteers have confirmed that pH drops from 7.0 at terminal ileum to 6.0 at ascending colon, and Eudragit S based systems sometimes fail to release the drug. To overcome the shortcoming, combination of Eudragit S and Eudragit L which ensures drug release at pH < 7 has been advocated. Eudragit RL and RS, having quaternary ammonium groups, are water insoluble, but swellable/permeable polymers which are suitable for the sustained release film coating applications. Cationic Eudragit E, insoluble at pH ≥ 5, can prevent drug release in saliva and finds application in taste masking.

摘要

简介

Eudragit 是一系列不同的基于甲基丙烯酸酯的共聚聚合物的商品名。它包括基于甲基丙烯酸和甲基丙烯酸/丙烯酸酯或其衍生物的阴离子型、阳离子型和中性共聚物。

涵盖领域

在这篇综述中,讨论了不同等级的 Eudragit 在结肠特异性/肠溶/缓释药物传递和掩味中的理化特性和应用。

专家意见

Eudragit 是无定形聚合物,玻璃化转变温度在 9 至 >150°C 之间。Eudragit 是非生物降解、不可吸收和无毒的。阴离子型 Eudragit L 在 pH>6 时溶解,用于肠溶包衣,而在 pH>7 时溶解的 Eudragit S 用于结肠靶向。人体志愿者的研究证实,pH 值从回肠末端的 7.0 下降到升结肠的 6.0,而基于 Eudragit S 的系统有时无法释放药物。为了克服这一缺点,已经提倡使用 Eudragit S 和 Eudragit L 的组合,以确保在 pH<7 时释放药物。带季铵基团的 Eudragit RL 和 RS 是不溶于水但可溶胀/可渗透的聚合物,适用于缓释薄膜包衣应用。阳离子型 Eudragit E 在 pH≥5 时不溶,可以防止药物在唾液中的释放,在掩味方面有应用。

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