Microstructures and pharmaceutical properties of ferulic acid agglomerates prepared by different spherical crystallization methods

Hongbo Chen, Chenguang Wang, Hyunho Kang, Bo Zhi, Christy L. Haynes, Aktham Aburub, Changquan Calvin Sun

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3 Scopus citations

Abstract

Spherical agglomerates of an active pharmaceutical ingredient, ferulic acid (FA), were prepared using four different spherical crystallization methods, i.e., quasi-emulsion solvent diffusion (QESD), anti-solvent, pH shift, and the direct method. Both the as-received FA and spherical agglomerates were characterized in terms of specific surface area (SSA), primary crystal shape and size, granule morphology and size, powder flowability, tabletability at two distinct speeds, and dissolution (both powder and tablet). Results showed that the microstructure, which is affected by size, shape, and packing of primary crystals, was the key that determined the flowability, tabletability and dissolution. The QESD powder exhibited the best flowability and tabletability. Both powder and tablet dissolution of FA followed the order of as-received > QESD > anti-solvent > pH shift, which was consistent with the order of the surface area exposed to the dissolution medium and not SSA. Moreover, compression reduced differences in the rates of dissolution of FA powders due to the size reduction of agglomerates by fragmentation.

Original languageEnglish (US)
Article number118914
JournalInternational journal of pharmaceutics
Volume574
DOIs
StatePublished - Jan 25 2020

Bibliographical note

Funding Information:
This work was supported by a grant from Eli Lilly and Company through the Lilly Research Award Program. Part of this work was carried out in the Characterization Facility, University of Minnesota, which receives partial support from NSF through the MRSEC program. H.C. thanks the Chinese Scholarship Council for partial financial support. H.C. was also partially supported by a David and Marilyn Grant Fellowship in Physical Pharmacy (2019-2020), Department of Pharmaceutics, University of Minnesota. Contributions from H.K., B.Z., and C.L.H. were supported by the National Science Foundation under the Center for Sustainable Nanotechnology, CHE-1503408; the CSN is part of the Centers for Chemical Innovation Program. We acknowledge the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing the resources that contributed to the research results reported within this paper. URL: https://www.msi.umn.edu . Appendix A

Funding Information:
This work was supported by a grant from Eli Lilly and Company through the Lilly Research Award Program. Part of this work was carried out in the Characterization Facility, University of Minnesota, which receives partial support from NSF through the MRSEC program. H.C. thanks the Chinese Scholarship Council for partial financial support. H.C. was also partially supported by a David and Marilyn Grant Fellowship in Physical Pharmacy (2019-2020), Department of Pharmaceutics, University of Minnesota. Contributions from H.K. B.Z. and C.L.H. were supported by the National Science Foundation under the Center for Sustainable Nanotechnology, CHE-1503408; the CSN is part of the Centers for Chemical Innovation Program. We acknowledge the Minnesota Supercomputing Institute (MSI) at the University of Minnesota for providing the resources that contributed to the research results reported within this paper. URL: https://www.msi.umn.edu.

Publisher Copyright:
© 2019 Elsevier B.V.

Keywords

  • Anti-solvent
  • Dissolution
  • Ferulic acid
  • Flowability
  • Quasi emulsion solvent diffusion
  • Spherical crystallization
  • Tabletability
  • pH shift

PubMed: MeSH publication types

  • Journal Article

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