R&D Formulation development Health Care Evonik India Private Limited, Krislon House Saki Vihar Road, Mumbai - 400072, India.
Int J Pharm. 2013 Dec 5;457(2):395-406. doi: 10.1016/j.ijpharm.2013.10.021. Epub 2013 Oct 20.
Taste masking and moisture protection of oral dosage forms contribute significantly to the therapeutic effect of pharmaceutical and nutraceutical formulations either by ensuring patient compliance or by providing stability through shelf life of the dosage form. Among different types of taste, bitter taste is the most relevant for patient acceptance because of the extremely high sensitivity. As hydrolysis is the most common mode of degradation of an active ingredient, moisture protection plays a vital role in the stability of the active during manufacturing and storage. Optimized oral dosage forms need to reliably hinder the release of bitter drug molecules in the mouth or ensure stability of the active compound, while also ensuring fast drug release in the stomach to enable early therapeutic onset. Besides different formulation concepts, film coating is found to be the most effective and commonly used approach for taste masking and moisture protection. Film coating can be achieved through the use of water-soluble, cationic, anionic or neutral insoluble polymers from different chemical structures. Cationic polymers provide efficient moisture protection as well as taste masking without influencing the release of the drug in the gastric fluids. Polymers may be sprayed onto various types of cores from dispersions or solutions in organic, solvents or water in drum or fluidzed bed coaters. Applied quantities need insuring complete coating thickness ranging from 0.5 to 50 μm or more finally. Insulating excipients, such as hydrophobic plasticizers, lipids, pigments or other insoluble substances will influence the functionality of films. Organoleptic tests are still common in testing the quality of taste-masked formulations. Recently, multi-channel taste sensors have been developed to quantify different types of taste. Dynamic vapor sorption technique and studies at elevated temperature provide effective concepts study the efficacy of the formulations. Efficient taste masking and reliable moisture protection of solid oral dosage forms can be achieved by film coating implementing the options of pharmaceutical polymers and processes.
味觉掩蔽和口服剂型的防潮保护对于药物和营养保健品制剂的治疗效果有重要贡献，既可以通过确保患者的依从性，也可以通过提供剂型的货架期稳定性来实现。在不同类型的味道中，苦味是与患者接受度最相关的，因为它的敏感度极高。由于水解是活性成分最常见的降解方式，防潮保护在活性成分的制造和储存过程中的稳定性方面起着至关重要的作用。优化的口服剂型需要可靠地阻止口中苦味药物分子的释放，或确保活性化合物的稳定性，同时确保药物在胃中的快速释放，从而实现早期治疗效果。除了不同的制剂概念外，薄膜包衣被发现是味觉掩蔽和防潮保护最有效和常用的方法。薄膜包衣可以通过使用来自不同化学结构的水溶性、阳离子、阴离子或中性不溶性聚合物来实现。阳离子聚合物提供有效的防潮保护和味觉掩蔽，而不影响药物在胃液中的释放。聚合物可以从分散体或溶液中喷涂到各种类型的核芯上，这些分散体或溶液存在于有机溶剂、水或水基溶剂中，在转鼓或流化床包衣机中进行喷涂。需要确保应用的量达到最终完整的涂层厚度为 0.5 至 50 μm 或更厚。绝缘赋形剂，如疏水性增塑剂、脂质、颜料或其他不溶性物质，会影响薄膜的功能。感官测试仍然是测试掩味配方质量的常用方法。最近，多通道味觉传感器已经被开发出来，用于量化不同类型的味道。动态蒸汽吸附技术和高温研究提供了评估配方效果的有效概念。通过实施药物聚合物和工艺的选择，可以实现固体口服剂型的高效味觉掩蔽和可靠防潮保护。
