Mechanical Properties and Tableting Behavior of Amorphous Solid Dispersions

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• 作者：Sarsvat Patel¹ ; Xiang Kou¹ ; Hao (Helen) Hou² ; Ye (Bill) Huang² ; John C. Strong² ; Geoff G.Z. Zhang² ; ^{geoff.gz.zhang@abbvie.com} ; Changquan Calvin Sun¹ ; ^{sunx0053@umn.edu}
• 关键词：amorphous ; compaction ; dispersion ; glass transition ; hardness ; mechanical properties ; physical characterization ; solid state ; tablet
• 刊名：Journal of Pharmaceutical Sciences
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：106
• 期：1
• 页码：217-223
• 全文大小：1390 K
• 卷排序：106

文摘

Amorphous solid dispersions (ASDs) consisting of acetaminophen (APAP) and copovidone were systematically studied to identify effects of drug loading and moisture content on mechanical properties, thermal properties, and tableting behavior. ASDs containing APAP at different levels were prepared by film casting and characterized by differential scanning calorimetry and nanoindentation. The glass transition temperature (Tg) continuously decreased with increasing amount of APAP, but the hardness of ASDs was increased at a low APAP content and reduced at high APAP content. This in turn significantly influenced tablet quality. Water reduced both the hardness and Tg of ASDs, and the APAP loading level corresponding to the transition to the softening mechanism was lower at a higher relative humidity. Overall, the mechanical properties, rather than the thermal properties, better represent the plasticization/antiplasticization effect of small molecule to ASDs.