Mechanical Properties and Tableting Behavior of Amorphous Solid Dispersions

Sarsvat Patel, Xiang Kou, Hao (Helen) Hou, Ye (Bill) Huang, John C. Strong, Geoff G.Z. Zhang, Changquan Calvin Sun

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)217-223
Number of pages7
JournalJournal of Pharmaceutical Sciences
Volume106
Issue number1
DOIs
StatePublished - Jan 1 2017

Bibliographical note

Funding Information:
We thank Dr. Sathyanarayana R. Perumalla for technical support in characterizing solid state properties of ASD samples. This work was supported by a grant from AbbVie .

Publisher Copyright:
© 2016 American Pharmacists Association®

Copyright:
Copyright 2017 Elsevier B.V., All rights reserved.

Keywords

  • amorphous
  • compaction
  • dispersion
  • glass transition
  • hardness
  • mechanical properties
  • physical characterization
  • solid state
  • tablet

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