Pharmaceutical Applications of Shellac: Moisture-Protective and Taste-Masking Coatings and Extended-Release Matrix Tablets
Pharmaceutical Applications of Shellac: Moisture-Protective and Taste-Masking Coatings and Extended-Release Matrix Tablets
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DOI：
10.1081/ddc-120024188
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发表时间：
2003-01
影响因子：
3.4
通讯作者：
Nantharat Pearnchob;J. Siepmann;R. Bodmeier
中科院分区：
文献类型：
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作者：
Nantharat Pearnchob;J. Siepmann;R. Bodmeier
摘要紫胶是一种天然高分子材料，在医药领域被用作肠溶包衣材料。本研究的主要目的是研究虫胶用于其他用途的潜力，即提供保湿和掩味涂层以及缓释骨架片。将虫胶实现防潮和掩味的效率与最常用于这些目的的羟丙基甲基纤维素（HPMC）的效率进行比较。在相同的包衣水平下，贝壳包衣片剂的吸水率低于HPMC包衣系统。与HPMC包衣系统相比，虫胶包衣片剂中乙酰水杨酸的稳定性更高，与储存湿度无关。因此，需要较低的虫胶涂层水平来实现相同程度的药物保护。虫胶涂层有效地掩盖了对乙酰氨基酚片剂的不良味道。与HPMC相比，再次需要较低的包衣水平来实现类似的效果。薄虫胶包衣不会显著改变所得到的药物在模拟胃液中的释放，薄虫胶包衣由于包衣片芯的溶胀而迅速破裂。此外，虫胶被发现是一个合适的基质形成剂的延长释放片剂。后者可以通过直接压缩或通过使用乙醇或氨化虫胶粘合剂水溶液的湿法制粒来制备。由此产生的药物释放模式可以有效地改变不同的配方和工艺参数。
Abstract Shellac is a natural polymer, which is used as enteric coating material in pharmaceutical applications. The major objective of the present study was to investigate the potential of shellac for other purposes, namely to provide moisture-protective and taste-masking coatings as well as extended-release matrix tablets. The efficiency of shellac to achieve moisture protection and taste masking was compared with that of hydroxypropyl methylcellulose (HPMC), which is most frequently used for these purposes. Shellac-coated tablets showed lower water uptake rates than HPMC-coated systems at the same coating level. The stability of acetylsalicylic acid was higher in tablets coated with shellac compared with HPMC-coated systems, irrespective of the storage humidity. Therefore, lower shellac coating levels were required to achieve the same degree of drug protection. Shellac coatings effectively masked the unpleasant taste of acetaminophen tablets. Compared to HPMC, again lower coating levels were required to achieve similar effects. The resulting drug release in simulated gastric fluid was not significantly altered by the thin shellac coatings, which rapidly ruptured due to the swelling of the coated tablet core. In addition, shellac was found to be a suitable matrix former for extended-release tablets. The latter could be prepared by direct compression or via wet granulation using ethanolic or ammoniated aqueous shellac binder solutions. The resulting drug-release patterns could effectively be altered by varying different formulation and processing parameters.