Impact of micromeritic properties of an active pharmaceutical ingredient on its compaction behavior

Abstract

Physical characteristics of an active pharmaceutical ingredient (API) can have a significant impact on the processability of a high drug loading formulation. This paper provides an example where different micromeritic properties of an API were obtained by crystallization under different conditions, resulting in different tableting behavior. While the API form purity was maintained during the crystallization process change, significant changes were incurred in the surface geometry, porosity and surface area of the API. The batches consisting of particles with greater surface irregularity and porosity gave tablets of higher mechanical strength.

• Compaction
• crystallization
• formulation
• mechanical properties
• morphology
• polymorphism
• pore volume
• surface area

Acknowledgements

Authors would like to thank Rodney Parsons, Pascal H. Toma, Paul A. Meenan, Darin Norwood and Barbara Stephens for their assistance with the API process development. We would also like to thank Tara Lee, Francisco Alvarez and David Buckley for their assistance during formulation development. Special thanks to Vrushali Waknis for her assistance with the literature search.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.