Enhancing tabletability of high-dose tablets by tailoring properties of spray-dried insulin particles

Research output: Contribution to journalJournal articleResearchpeer-review

  • Mahdieh Dagina Pedersen
  • Andrew Megarry
  • Kaisa Naelapää
  • Rades, Thomas
  • Jenni Pessi

The oral delivery of proteins and peptides provides an attractive dosing option due to its high patient compliance. However, as oral formulations of such macromolecules require the addition of typically poorly compactable permeation enhancers, the compression behaviour in tableting processes can become challenging. In this study, we show that poor compression behaviour can be overcome by tailoring the properties of peptide or protein particles, especially in high-dose tablet formulations. Spray-dried particles with varying particle size and morphology were produced and characterized. The particles were then evaluated for tabletability in well- and poorly tabletable formulations. Tabletability was found to be enhanced most with small and non-hollow spray-dried insulin particles in both formulations. The enhancement was more pronounced in the poorly tabletable formulation than in the well-tabletable one. Thus, the API particle properties play a key role, when evaluating manufacturability of poorly tabletable formulations.

Original languageEnglish
Article number122526
JournalInternational Journal of Pharmaceutics
Number of pages8
Publication statusPublished - 2023

Bibliographical note

Funding Information:
The authors wish to thank René Jensen for conducting the ring shear test experiments.

Publisher Copyright:
© 2022 Elsevier B.V.

    Research areas

  • High-dose formulations, Insulin, Magnesium stearate (CAS: 557-04-0), Maltitol (CAS: 585-88-6), MCC (CAS: 9004-34-6), Oral drug delivery, Oral peptide formulations, Oral protein formulations, Sorbitol (CAS: 50-70-4), Spray-dried particles, Starch (CAS: 9005-25-8), Tablet manufacturing, Tabletability

ID: 332996291