In vitro Release Characteristics of Hard Shell Capsule Products Coated with Aqueous- and Organic-Based Enteric Polymers
In vitro Release Characteristics of Hard Shell Capsule Products Coated with Aqueous- and Organic-Based Enteric Polymers
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水基和有机基肠溶聚合物包衣的硬壳胶囊产品的体外释放特性
DOI：
10.1177/088532828800300103
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发表时间：
1988
影响因子：
2.9
通讯作者：
M. Fawzi
中科院分区：
文献类型：
--
作者：
K. S. Murthy;Daniel A. Kubert;M. Fawzi
在这篇文章中，概述了使用肠溶包衣（EC）剂型的基本原理。讨论了使用各种聚合物的水分散体和有机溶液来产生这些产品的固有优点和缺点。在加速储存条件下评估了以水性分散体或有机溶液形式施用的用肠溶聚合物包衣的硬壳胶囊产品的比较溶出稳定性。聚甲基丙烯酸甲基丙烯酸酯共聚物、邻苯二甲酸乙酸纤维素（CAP）和聚乙酸乙烯酯邻苯二甲酸酯（PVAP）沿着相应的市售水性分散体Eudragit® L30 D、Aquateric®和Coateric™在这些研究中用作肠溶聚合物。邻苯二甲酸二乙酯（DEP）用作增塑剂，盐酸普鲁卡因胺250 mg胶囊用作基质。将包衣胶囊在37°C/80%RH和45°C下储存2个月表明，虽然Eudragit® L30 D包衣的稳定性与相应的有机基包衣相当或上级，但当与通过使用有机载体施加的PVAP包衣相比时，Coateric™膜明显不稳定。在37°C/80%RH下储存后，仅当存在保护性密封涂层时，基于Aquateric®的胶囊表现出与CAP有机基涂层相当的稳定性。储存时发生的胶囊性能失效主要导致胃阻力损失。不同涂层的扫描电子显微镜（SEM）和热机械分析（TMA）揭示了聚合物膜的成膜特性的差异，并提供了对涂层胶囊储存期间发生的变化的解释。
In this article, an overview of the rationale for the use of enteric coated (EC) dosage forms is presented. The benefits and disadvantages inherent in the use of aqueous dispersions and organic solutions of the various polymers to generate these products are discussed. The comparative dissolution stability of a hard shell capsule product coated with enteric polymers applied as either aqueous dispersions, or as organic solutions, were assessed under accelerated conditions of storage. Polymethacrylic acid methacrylate copolymer, cellulose acetate phthalate (CAP) and polyvinyl acetate phthalate (PVAP), along with the corresponding commercially available aqueous dispersions, Eudragit® L30D, Aquateric®, and Coateric™, were employed in these studies as enteric polymers. Diethyl phthalate (DEP) was used as the plasticizer and procainamide HCl 250 mg capsules served as the substrate. Storage of the coated capsules at 37°C/80% RH and at 45°C for 2 months revealed that, while the stability of Eudragit® L30D coatings are comparable or superior to the corresponding organic-based coatings, Coateric™ films are markedly unstable when compared with PVAP coatings applied through the use of organic vehicles. After storage at 37°C/80% RH, Aquateric®-based capsules demonstrated stability comparable to CAP organic-based coatings only when a protective seal coat was present. The performance failures of the capsules that occur upon storage primarily result in a loss of gastric resistance. Scanning Electron Microscopy (SEM) and thermomechanical analysis (TMA) of the different coatings revealed differences in the film-forming properties of the polymer films and provide an explanation for the changes that occur during storage of the coated capsules.