Division of Pharmaceutical Technology, Department of Chemistry, University of Hamburg , Hamburg , Germany.
Division of Pharmaceutical Technology, Roha Arzneimittel GmbH , Bremen , Germany.
Pharm Dev Technol. 2019 Dec;24(10):1210-1217. doi: 10.1080/10837450.2019.1648509. Epub 2019 Aug 23.
The objective of this study was to investigate the efficiency of moisture protection of hot-melt coatings solely and in combination with an enteric coating on hygroscopic tablet cores containing a spray-dried Sennae fructus extract. Tablet cores were subcoated with different hot-melt coating materials: medium chain tryglycerides, stearic acid, Precirol ATO 5, and Compritol 888 ATO, at varying amounts and coated with Eudragit L 30D-55 for enteric resistance. Subcoating penetration, tablet disintegration, dissolution times, tablet hygroscopicity, and tablet properties such as weight, height, diameter, and hardness were analyzed. 3 mg/cm of tablet surface seemed to be sufficient if sustained release is not required. Thereby, hot-melt coating did not adversely affect the tablet properties with regard to subsequent processing steps. Compared to the tablet cores it was possible to reduce the moisture uptake by 85% at 75% relative humidity with tablets coated with a combination of Precirol ATO 5 and Eudragit L 30D-55. This combination was more efficient than high amounts of Eudragit L 30D-55. Hot-melt coating proved to be a suitable technique for the application of subcoating material to tablet cores serving as a barrier against water permeation into hygroscopic tablet cores without exceeding the required disintegration times.
本研究的目的是研究热熔包衣在保护含有喷雾干燥番泻叶提取物的吸湿片剂芯的防潮性能方面的效率，单独使用以及与肠溶包衣结合使用的效果。片剂芯采用不同的热熔包衣材料进行次涂层：中链甘油三酯、硬脂酸、Precirol ATO 5 和 Compritol 888 ATO，用量不同，并包衣以获得肠溶抗性的 Eudragit L 30D-55。分析了次涂层的穿透性、片剂崩解时间、溶解时间、片剂吸湿性以及片剂的重量、高度、直径和硬度等特性。如果不需要持续释放，则 3mg/cm 的片剂表面似乎就足够了。因此，热熔包衣不会对后续加工步骤中的片剂特性产生不利影响。与片剂芯相比，用 Precirol ATO 5 和 Eudragit L 30D-55 的组合包衣的片剂可以将在 75%相对湿度下的吸水量减少 85%。这种组合比大量使用 Eudragit L 30D-55 更有效。热熔包衣被证明是一种将次涂层材料应用于作为防潮片剂芯的渗透屏障的片剂芯的合适技术，而不会超过所需的崩解时间。
