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

doi:10.1016/j.ijpharm.2019.118914

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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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 language	English (US)
Article number	118914
Journal	International journal of pharmaceutics
Volume	574
DOIs	https://doi.org/10.1016/j.ijpharm.2019.118914
State	Published - 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.

Copyright:
Copyright 2019 Elsevier B.V., All rights reserved.

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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10.1016/j.ijpharm.2019.118914

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title = "Microstructures and pharmaceutical properties of ferulic acid agglomerates prepared by different spherical crystallization methods",

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.",

keywords = "Anti-solvent, Dissolution, Ferulic acid, Flowability, Quasi emulsion solvent diffusion, Spherical crystallization, Tabletability, pH shift",

author = "Hongbo Chen and Chenguang Wang and Hyunho Kang and Bo Zhi and Haynes, {Christy L.} and Aktham Aburub and Sun, {Changquan Calvin}",

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: {\textcopyright} 2019 Elsevier B.V. Copyright: Copyright 2019 Elsevier B.V., All rights reserved.",

year = "2020",

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doi = "10.1016/j.ijpharm.2019.118914",

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AU - Chen, Hongbo

AU - Wang, Chenguang

AU - Kang, Hyunho

AU - Zhi, Bo

AU - Haynes, Christy L.

AU - Aburub, Aktham

AU - Sun, Changquan Calvin

N1 - 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. Copyright: Copyright 2019 Elsevier B.V., All rights reserved.

PY - 2020/1/25

Y1 - 2020/1/25

N2 - 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.

AB - 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.

KW - Anti-solvent

KW - Dissolution

KW - Ferulic acid

KW - Flowability

KW - Quasi emulsion solvent diffusion

KW - Spherical crystallization

KW - Tabletability

KW - pH shift

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ER -

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

Abstract

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Keywords

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