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Toward a Molecular Understanding of the Impact of Crystal Size and Shape on Punch Sticking.
Mol Pharm. 2020 04 06; 17(4):1148-1158.MP

Abstract

Punch sticking during tablet manufacturing is a common problem facing the pharmaceutical industry. Using several model compounds, effects of crystal size and shape of active pharmaceutical ingredients (API) on punch sticking propensity were systematically investigated in this work to provide molecular insights into the punch-sticking phenomenon. In contrast to the common belief that smaller API particles aggravate punch sticking, results show that particle size reduction can either reduce or enhance API punch sticking, depending on the complex interplay among the particle surface area, plasticity, cohesive strength, and specific surface functional groups. Therefore, other factors, such as crystal mechanical properties, surface chemistry of crystal facets exposed to the punch face, and choice of excipients in a formulation, should be considered for a more reliable prediction of the initiation and progression of punch sticking. The exposure of strong electronegative groups to the punch face facilitates the onset of sticking, while higher plasticity and cohesive strength aggravate sticking.

Authors+Show Affiliations

Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, Minnesota 55455, United States.Pfizer Worldwide Research and Development, Sandwich CT13 9ND, U.K.Pfizer Worldwide Research and Development, Groton, Connecticut 06340, United States.Pfizer Worldwide Research and Development, Groton, Connecticut 06340, United States.Pfizer Worldwide Research and Development, Sandwich CT13 9ND, U.K.Pfizer Worldwide Research and Development, Groton, Connecticut 06340, United States.Pfizer Worldwide Research and Development, Groton, Connecticut 06340, United States.Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, Minnesota 55455, United States.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

32058728

Citation

Paul, Shubhajit, et al. "Toward a Molecular Understanding of the Impact of Crystal Size and Shape On Punch Sticking." Molecular Pharmaceutics, vol. 17, no. 4, 2020, pp. 1148-1158.
Paul S, Taylor LJ, Murphy B, et al. Toward a Molecular Understanding of the Impact of Crystal Size and Shape on Punch Sticking. Mol Pharm. 2020;17(4):1148-1158.
Paul, S., Taylor, L. J., Murphy, B., Krzyzaniak, J. F., Dawson, N., Mullarney, M. P., Meenan, P., & Sun, C. C. (2020). Toward a Molecular Understanding of the Impact of Crystal Size and Shape on Punch Sticking. Molecular Pharmaceutics, 17(4), 1148-1158. https://doi.org/10.1021/acs.molpharmaceut.9b01185
Paul S, et al. Toward a Molecular Understanding of the Impact of Crystal Size and Shape On Punch Sticking. Mol Pharm. 2020 04 6;17(4):1148-1158. PubMed PMID: 32058728.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Toward a Molecular Understanding of the Impact of Crystal Size and Shape on Punch Sticking. AU - Paul,Shubhajit, AU - Taylor,Lisa J, AU - Murphy,Brendan, AU - Krzyzaniak,Joseph F, AU - Dawson,Neil, AU - Mullarney,Matthew P, AU - Meenan,Paul, AU - Sun,Changquan Calvin, Y1 - 2020/03/05/ PY - 2020/2/15/pubmed PY - 2021/5/29/medline PY - 2020/2/15/entrez KW - mechanical property KW - morphology KW - particle size KW - punch sticking KW - surface chemistry SP - 1148 EP - 1158 JF - Molecular pharmaceutics JO - Mol Pharm VL - 17 IS - 4 N2 - Punch sticking during tablet manufacturing is a common problem facing the pharmaceutical industry. Using several model compounds, effects of crystal size and shape of active pharmaceutical ingredients (API) on punch sticking propensity were systematically investigated in this work to provide molecular insights into the punch-sticking phenomenon. In contrast to the common belief that smaller API particles aggravate punch sticking, results show that particle size reduction can either reduce or enhance API punch sticking, depending on the complex interplay among the particle surface area, plasticity, cohesive strength, and specific surface functional groups. Therefore, other factors, such as crystal mechanical properties, surface chemistry of crystal facets exposed to the punch face, and choice of excipients in a formulation, should be considered for a more reliable prediction of the initiation and progression of punch sticking. The exposure of strong electronegative groups to the punch face facilitates the onset of sticking, while higher plasticity and cohesive strength aggravate sticking. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/32058728/Toward_a_Molecular_Understanding_of_the_Impact_of_Crystal_Size_and_Shape_on_Punch_Sticking_ L2 - https://doi.org/10.1021/acs.molpharmaceut.9b01185 DB - PRIME DP - Unbound Medicine ER -