College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, People's Republic of China.
College of Chinese Materia Medica, Zhejiang Pharmaceutical College, Ningbo, 315100, People's Republic of China.
AAPS PharmSciTech. 2017 Nov;18(8):3105-3115. doi: 10.1208/s12249-017-0794-1. Epub 2017 May 18.
Many commonly used tablet fillers are not suitable for direct compaction process due to insufficient properties, mainly of flowability and compactability. This work therefore aimed to use co-spray drying with HPMC as a platform to improve direct compaction properties of various tablet fillers. Starch, calcium hydrogen phosphate dihydrate (DCPD), and mannitol were chosen as a representative of three types of commonly used fillers (i.e. organic macromolecules, water-insoluble inorganic salts, and water-soluble small molecular carbohydrates), respectively. The five-level central composite design-response surface methodology was used (i) to investigate the effects of HPMC level and solid content of the feed on various powder, tableting, and tablet properties of composite excipients, and (ii) to optimize the composition. The results showed that the impacts of the two factors on various properties of composite excipients showed great similarity, despite of significantly different primary properties of the parent fillers, and the HPMC level was the main contributor to the majority of the impacts. An increase in HPMC level significantly improved tablet tensile strength and various tableting parameters. For all the three fillers, their optimized composite excipients provided by the established models showed excellent performances as predicted. The platform suggested is confirmed to be effective and promising.
由于性质不足，许多常用的片剂填充剂不适合直接压片工艺，主要是流动性和可压缩性。因此，本工作旨在使用羟丙甲纤维素共喷雾干燥作为平台来改善各种片剂填充剂的直接压片性能。淀粉、磷酸氢钙二水合物（DCPD）和甘露醇分别被选为三种常用填充剂（即有机大分子、水不溶性无机盐和水溶性小分子碳水化合物）的代表。使用五水平中心组合设计响应面法（i）研究 HPMC 水平和进料固含量对复合赋形剂的各种粉末、压片和片剂性质的影响，以及（ii）优化组成。结果表明，尽管原填充剂的主要性质明显不同，但这两个因素对复合赋形剂的各种性质的影响非常相似，HPMC 水平是大多数影响的主要贡献者。HPMC 水平的增加显著提高了片剂的拉伸强度和各种压片参数。对于所有三种填充剂，由所建立的模型提供的优化复合赋形剂的性能均如预测的那样优异。所提出的平台被证实是有效和有前途的。
