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Passivation of high-surface-energy sites of milled ibuprofen crystals via dry coating for reduced cohesion and improved flowability.
J Pharm Sci. 2013 Jul; 102(7):2282-96.JP

Abstract

Ibuprofen micronization with dry coating is investigated to examine its influence on passivation/stabilization of high-surface-energy sites and reduced cohesion. A fluid energy mill was used to micronize ibuprofen particles down to 5-28 μm with or without simultaneous nanosilica coating. Powder flow property and dispersibility were characterized using FT4 powder tester and Rodos/Helos laser diffraction particle sizer. Surface energy was characterized using a next generation inverse gas chromatography instrument. Uncoated micronized ibuprofen showed an increased Lifshitz-van der Waals (LW) dispersion component of surface energy with increasing milling intensity. In contrast, dry-coated milled powders showed a significant reduction in the LW component, whereas physical mixture of uncoated micronized ibuprofen and silica exhibited no reduction in surface energy, indicating that dry coating is necessary for the passivation of high-energy sites of ibuprofen created during micronization. Surface energy of pure micronized ibuprofen was highly heterogeneous, whereas dry-coated ibuprofen had greatly reduced heterogeneity. Micronization with dry coating also improved flowability and bulk density as compared with pure active pharmaceutical ingredient micronization without coating, or just blending with silica. Overall, dry coating leads to decreased cohesion and improved flowability because of reduced LW dispersive component of surface energy and creating nanoscale surface roughness.

Links

Publisher Full Text
linkinghub.elsevier.com
onlinelibrary.wiley.com

Authors+Show Affiliations

Han X
New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Newark, New Jersey 07102, USA.
Jallo L
No affiliation info available
To D
No affiliation info available
Ghoroi C
No affiliation info available
Davé R
No affiliation info available

MeSH

Analgesics, Non-NarcoticCrystallizationDrug CompoundingIbuprofenParticle SizeRheologySolubilitySurface Properties

Pub Type(s)

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

Language

eng

PubMed ID

23658057

Citation

Han, Xi, et al. "Passivation of High-surface-energy Sites of Milled Ibuprofen Crystals Via Dry Coating for Reduced Cohesion and Improved Flowability." Journal of Pharmaceutical Sciences, vol. 102, no. 7, 2013, pp. 2282-96.
Han X, Jallo L, To D, et al. Passivation of high-surface-energy sites of milled ibuprofen crystals via dry coating for reduced cohesion and improved flowability. J Pharm Sci. 2013;102(7):2282-96.
Han, X., Jallo, L., To, D., Ghoroi, C., & Davé, R. (2013). Passivation of high-surface-energy sites of milled ibuprofen crystals via dry coating for reduced cohesion and improved flowability. Journal of Pharmaceutical Sciences, 102(7), 2282-96. https://doi.org/10.1002/jps.23589
Han X, et al. Passivation of High-surface-energy Sites of Milled Ibuprofen Crystals Via Dry Coating for Reduced Cohesion and Improved Flowability. J Pharm Sci. 2013;102(7):2282-96. PubMed PMID: 23658057.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Passivation of high-surface-energy sites of milled ibuprofen crystals via dry coating for reduced cohesion and improved flowability. AU - Han,Xi, AU - Jallo,Laila, AU - To,Daniel, AU - Ghoroi,Chinmay, AU - Davé,Rajesh, Y1 - 2013/05/08/ PY - 2013/02/06/received PY - 2013/04/10/revised PY - 2013/04/16/accepted PY - 2013/5/10/entrez PY - 2013/5/10/pubmed PY - 2014/1/7/medline SP - 2282 EP - 96 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 102 IS - 7 N2 - Ibuprofen micronization with dry coating is investigated to examine its influence on passivation/stabilization of high-surface-energy sites and reduced cohesion. A fluid energy mill was used to micronize ibuprofen particles down to 5-28 μm with or without simultaneous nanosilica coating. Powder flow property and dispersibility were characterized using FT4 powder tester and Rodos/Helos laser diffraction particle sizer. Surface energy was characterized using a next generation inverse gas chromatography instrument. Uncoated micronized ibuprofen showed an increased Lifshitz-van der Waals (LW) dispersion component of surface energy with increasing milling intensity. In contrast, dry-coated milled powders showed a significant reduction in the LW component, whereas physical mixture of uncoated micronized ibuprofen and silica exhibited no reduction in surface energy, indicating that dry coating is necessary for the passivation of high-energy sites of ibuprofen created during micronization. Surface energy of pure micronized ibuprofen was highly heterogeneous, whereas dry-coated ibuprofen had greatly reduced heterogeneity. Micronization with dry coating also improved flowability and bulk density as compared with pure active pharmaceutical ingredient micronization without coating, or just blending with silica. Overall, dry coating leads to decreased cohesion and improved flowability because of reduced LW dispersive component of surface energy and creating nanoscale surface roughness. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/23658057/Passivation_of_high_surface_energy_sites_of_milled_ibuprofen_crystals_via_dry_coating_for_reduced_cohesion_and_improved_flowability_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)31041-8 DB - PRIME DP - Unbound Medicine ER -