Co-spray Drying with HPMC as a Platform to Improve Direct Compaction Properties of Various Tablet Fillers

被引:16
作者
Li, JinZhi [1 ,2 ]
Zhao, LiJie [3 ]
Lin, Xiao [1 ]
Shen, Lan [1 ]
Feng, Yi [3 ]
机构
[1] Shanghai Univ Tradit Chinese Med, Coll Chinese Mat Med, Shanghai 201203, Peoples R China
[2] Zhejiang Pharmaceut Coll, Coll Chinese Mat Med, Ningbo 315100, Zhejiang, Peoples R China
[3] Shanghai Univ Tradit Chinese Med, Engn Res Ctr Modern Preparat Technol TCM, Minist Educ, Shanghai 201203, Peoples R China
基金
中国国家自然科学基金;
关键词
hydroxypropyl methylcellulose; starch; calcium hydrogen phosphate dihydrate; mannitol; spray drying; co-processed excipients; HYDROXYPROPYL METHYLCELLULOSE; DISINTEGRANT EFFICIENCY; DIRECT COMPRESSION; DESIGN; POWDER; EXCIPIENTS; SOLUBILITY; MECHANISMS; OPTIMIZE; RECOVERY;
D O I
10.1208/s12249-017-0794-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:3105 / 3115
页数:11
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