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Eudragit RL-based film coatings: How to minimize sticking and adjust drug release using MAS.
European Journal of Pharmaceutics and Biopharmaceutics ( IF 4.4 ) Pub Date : 2020-01-23 , DOI: 10.1016/j.ejpb.2020.01.011 Thitiphorn Rongthong 1 , Srisagul Sungthongjeen 2 , Florence Siepmann 3 , Juergen Siepmann 3 , Thaned Pongjanyakul 4
European Journal of Pharmaceutics and Biopharmaceutics ( IF 4.4 ) Pub Date : 2020-01-23 , DOI: 10.1016/j.ejpb.2020.01.011 Thitiphorn Rongthong 1 , Srisagul Sungthongjeen 2 , Florence Siepmann 3 , Juergen Siepmann 3 , Thaned Pongjanyakul 4
Affiliation
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Polymeric film coatings based on quaternary polymethacrylates (QPMs, e.g. Eudragits®) are frequently used for controlled release applications. However, their considerable sticking tendency is a major drawback in practice. In this study, different amounts of magnesium aluminum silicate (MAS) were added to the film coatings in order to overcome this hurdle. MAS is negatively charged and can electrostatically interact with the positively charged QPM. Different types of tablet cores were coated with aqueous Eudragit® RL 30D dispersions, optionally containing varying amounts of MAS. Dynamic changes in the wet mass of the systems as well as drug release upon exposure to 0.1 M HCl and phosphate buffer pH 6.8 were monitored. Propranolol HCl, acetaminophen, and diclofenac sodium were used as cationic, nonionic and anionic model drugs. The tablets were optionally cured for 12 h at 45 or 60 °C. Importantly, the addition of MAS to aqueous Eudragit® RL 30D dispersion substantially reduced the films' stickiness and led to stable inner coating structures, even without curing. Desired drug release rates can be adjusted by varying the QPM:MAS ratio and coating level.
中文翻译：
Eudragit RL基薄膜涂料：如何使用MAS最大限度地减少粘着并调整药物释放。
基于季聚甲基丙烯酸酯（QPM，例如Eudragits®）的聚合物薄膜包衣经常用于控释应用。然而，它们的相当大的粘附趋势是实践中的主要缺点。在这项研究中，为了克服这一障碍，将不同数量的硅酸铝镁（MAS）添加到了薄膜涂层中。MAS带负电，并且可以与带正电的QPM发生静电相互作用。用RL 30D水性水分散液包被不同类型的片剂核心，可选地包含不同量的MAS。监测系统湿质量的动态变化以及暴露于0.1 M HCl和pH 6.8磷酸盐缓冲液中的药物释放。盐酸普萘洛尔，对乙酰氨基酚和双氯芬酸钠被用作阳离子，非离子和阴离子模型药物。将片剂任选地在45或60℃下固化12小时。重要的是，在Eudragit®RL 30D水性分散体中添加MAS可以大大降低薄膜的粘性，即使不进行固化也可以形成稳定的内部涂层结构。可以通过改变QPM：MAS比和包衣水平来调整所需的药物释放速率。
更新日期：2020-01-23
中文翻译：
Eudragit RL基薄膜涂料：如何使用MAS最大限度地减少粘着并调整药物释放。
基于季聚甲基丙烯酸酯（QPM，例如Eudragits®）的聚合物薄膜包衣经常用于控释应用。然而，它们的相当大的粘附趋势是实践中的主要缺点。在这项研究中，为了克服这一障碍，将不同数量的硅酸铝镁（MAS）添加到了薄膜涂层中。MAS带负电，并且可以与带正电的QPM发生静电相互作用。用RL 30D水性水分散液包被不同类型的片剂核心，可选地包含不同量的MAS。监测系统湿质量的动态变化以及暴露于0.1 M HCl和pH 6.8磷酸盐缓冲液中的药物释放。盐酸普萘洛尔，对乙酰氨基酚和双氯芬酸钠被用作阳离子，非离子和阴离子模型药物。将片剂任选地在45或60℃下固化12小时。重要的是，在Eudragit®RL 30D水性分散体中添加MAS可以大大降低薄膜的粘性，即使不进行固化也可以形成稳定的内部涂层结构。可以通过改变QPM：MAS比和包衣水平来调整所需的药物释放速率。
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