TY - JOUR
T1 - Microstructures and pharmaceutical properties of ferulic acid agglomerates prepared by different spherical crystallization methods
AU - Chen, Hongbo
AU - Wang, Chenguang
AU - Kang, Hyunho
AU - Zhi, Bo
AU - Haynes, Christy L.
AU - Aburub, Aktham
AU - Sun, Changquan Calvin
N1 - Publisher Copyright:
© 2019 Elsevier B.V.
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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U2 - 10.1016/j.ijpharm.2019.118914
DO - 10.1016/j.ijpharm.2019.118914
M3 - Article
C2 - 31811924
AN - SCOPUS:85076284006
SN - 0378-5173
VL - 574
JO - International journal of pharmaceutics
JF - International journal of pharmaceutics
M1 - 118914
ER -