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The effect of mechanical dry coating with magnesium stearate on flowability and compactibility of plastically deforming microcrystalline cellulose powders.
Int J Pharm. 2018 Feb 15; 537(1-2):64-72.IJ

Abstract

Mechanofusion is a dry coating method that can be used to improve the flowability of cohesive powder by coating host particles with a lubricant, for example magnesium stearate (MgSt). It has been shown previously that fragmenting material can under some circumstances be mechanofused with MgSt without impairing compactibility of the powder and without reducing the dissolution rate of the resulting tablets. However, the effects on material with viscoelastic behaviour, known to be sensitive for the negative effects of MgSt, is not known. Therefore, mechanofusion of microcrystalline cellulose (MCC) with MgSt was investigated in this study. Four MCC grades were mechanofused with different MgSt concentrations and process parameters, and the resulting flowability and compactibility were studied. Starting materials and low-shear blended binary mixtures were studied as a reference. Mechanofusion improved the flow properties of small particle size MCC powders (d50 < 78 μm) substantially, but increasing the MgSt content consequently resulted in weaker tablets. Larger particle size MCC grades, however, fractured under the shear forces during the mechanofusion process and hence their flow properties were decreased. Improvement of the flow properties but also the negative effects on compactibility of small particle size grades were observed even at relatively mild mechanofusion parameters and low lubricant concentrations.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Koskela J
Division of Pharmaceutical Chemistry and Technology, 00014 University of Helsinki, P.O. Box 56, Helsinki, Finland. Electronic address: jaana.koskela@helsinki.fi.
Morton DAV
Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3055, Australia.
Stewart PJ
Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3055, Australia.
Juppo AM
Division of Pharmaceutical Chemistry and Technology, 00014 University of Helsinki, P.O. Box 56, Helsinki, Finland.
Lakio S
Orion Pharma, Orionintie 1, 02200 Espoo, Finland.

MeSH

CelluloseExcipientsLubricantsParticle SizePlasticsPowdersSolubilityStearic AcidsSurface PropertiesTablets

Pub Type(s)

Journal Article

Language

eng

PubMed ID

29198809

Citation

Koskela, Jaana, et al. "The Effect of Mechanical Dry Coating With Magnesium Stearate On Flowability and Compactibility of Plastically Deforming Microcrystalline Cellulose Powders." International Journal of Pharmaceutics, vol. 537, no. 1-2, 2018, pp. 64-72.
Koskela J, Morton DAV, Stewart PJ, et al. The effect of mechanical dry coating with magnesium stearate on flowability and compactibility of plastically deforming microcrystalline cellulose powders. Int J Pharm. 2018;537(1-2):64-72.
Koskela, J., Morton, D. A. V., Stewart, P. J., Juppo, A. M., & Lakio, S. (2018). The effect of mechanical dry coating with magnesium stearate on flowability and compactibility of plastically deforming microcrystalline cellulose powders. International Journal of Pharmaceutics, 537(1-2), 64-72. https://doi.org/10.1016/j.ijpharm.2017.11.068
Koskela J, et al. The Effect of Mechanical Dry Coating With Magnesium Stearate On Flowability and Compactibility of Plastically Deforming Microcrystalline Cellulose Powders. Int J Pharm. 2018 Feb 15;537(1-2):64-72. PubMed PMID: 29198809.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The effect of mechanical dry coating with magnesium stearate on flowability and compactibility of plastically deforming microcrystalline cellulose powders. AU - Koskela,Jaana, AU - Morton,David A V, AU - Stewart,Peter J, AU - Juppo,Anne M, AU - Lakio,Satu, Y1 - 2017/12/01/ PY - 2017/09/01/received PY - 2017/11/28/revised PY - 2017/11/29/accepted PY - 2017/12/5/pubmed PY - 2018/8/7/medline PY - 2017/12/5/entrez KW - Dry coating KW - Magnesium stearate KW - Mechanofusion KW - Microcrystalline cellulose KW - Plastic deformation SP - 64 EP - 72 JF - International journal of pharmaceutics JO - Int J Pharm VL - 537 IS - 1-2 N2 - Mechanofusion is a dry coating method that can be used to improve the flowability of cohesive powder by coating host particles with a lubricant, for example magnesium stearate (MgSt). It has been shown previously that fragmenting material can under some circumstances be mechanofused with MgSt without impairing compactibility of the powder and without reducing the dissolution rate of the resulting tablets. However, the effects on material with viscoelastic behaviour, known to be sensitive for the negative effects of MgSt, is not known. Therefore, mechanofusion of microcrystalline cellulose (MCC) with MgSt was investigated in this study. Four MCC grades were mechanofused with different MgSt concentrations and process parameters, and the resulting flowability and compactibility were studied. Starting materials and low-shear blended binary mixtures were studied as a reference. Mechanofusion improved the flow properties of small particle size MCC powders (d50 < 78 μm) substantially, but increasing the MgSt content consequently resulted in weaker tablets. Larger particle size MCC grades, however, fractured under the shear forces during the mechanofusion process and hence their flow properties were decreased. Improvement of the flow properties but also the negative effects on compactibility of small particle size grades were observed even at relatively mild mechanofusion parameters and low lubricant concentrations. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/29198809/The_effect_of_mechanical_dry_coating_with_magnesium_stearate_on_flowability_and_compactibility_of_plastically_deforming_microcrystalline_cellulose_powders_ DB - PRIME DP - Unbound Medicine ER -