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Elucidating the Impact of Material Properties on Tablet Manufacturability for Binary Paracetamol Blends

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Abstract

Purpose

Although the mechanical properties of paracetamol and MCC are extensively described in literature, there still is a need for a better understanding of the material properties impacting them. Thus, this study systematically analyzed material properties of paracetamol-MCC blends to elucidate their influence on the mechanical tablet properties in roller compaction and direct compression with special focus on surface properties.

Methods

Multiple material characteristics of binary mixtures of paracetamol and MCC with varying drug loads were analyzed, with particular emphasis on specific surface area and surface energy. Subsequently, mechanical tablet properties of the materials in direct compression and after roller compaction were examined.

Results

It was demonstrated that the impact of the initial material properties on mechanical tablet properties prevailed over the impact of processing route for paracetamol-MCC blends, underlining the importance of material characterization for tabletability of oral solid dosage forms. By applying bivariate as well as multivariate analysis, key material properties influencing the tabletability of paracetamol, MCC and its mixtures such as surface area, surface energy, effective angle of internal friction and density descriptors were identified.

Conclusions

This study highlighted the importance of comprehensive assessment of different material characteristics leading to a deeper understanding of underlying factors impacting mechanical tablet properties in direct compression and after roller compaction by the example of paracetamol-MCC mixtures with varying drug loads. Furthermore, it was shown that multivariate analysis could be a valuable extension to common bivariate analysis to reveal underlying correlations of material properties.

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Data Availability

All data supporting the findings of this study are available within the paper and its Supplementary Material A and B.

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Acknowledgements

The authors gratefully acknowledge Axel Becker and Anke Marx for providing analytical support in conducting the inverse gas chromatography measurements and the scientific discussion.

Funding

No funding was received for conducting this study.

Author information

Authors and Affiliations

  1. Institute of Pharmaceutical Technology and Biopharmaceutics, Technische Universität Braunschweig, 38106, Braunschweig, Germany

    Lena Mareczek & Stephan Reichl

  2. The Healthcare Business of Merck KGaA, 64293, Darmstadt, Germany

    Lena Mareczek, Carolin Riehl & Meike Harms

Authors
  1. Lena Mareczek
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  2. Carolin Riehl
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  3. Meike Harms
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  4. Stephan Reichl
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Contributions

Lena Mareczek: Conceptualization, Investigation, Formal analysis, Writing – original draft. Carolin Riehl: Conceptualization, Supervision, Writing – review & editing. Meike Harms: Software, Writing – review & editing. Stephan Reichl: Conceptualization, Supervision, Writing – review & editing.

Corresponding author

Correspondence to Carolin Riehl.

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Mareczek, L., Riehl, C., Harms, M. et al. Elucidating the Impact of Material Properties on Tablet Manufacturability for Binary Paracetamol Blends. Pharm Res 41, 185–197 (2024). https://doi.org/10.1007/s11095-023-03626-6

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  • DOI: https://doi.org/10.1007/s11095-023-03626-6

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