Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate

Qu, Li, Zhou, Qi (Tony), Gengenbach, Thomas, Denman, John A., Stewart, Peter J., Hapgood, Karen P., Gamlen, Michael and Morton, David A.V. 2015, Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate, Drug development and industrial pharmacy, vol. 41, no. 5, pp. 825-837, doi: 10.3109/03639045.2014.908901.

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Title Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate
Author(s) Qu, Li
Zhou, Qi (Tony)
Gengenbach, Thomas
Denman, John A.
Stewart, Peter J.
Hapgood, Karen P.ORCID iD for Hapgood, Karen P.
Gamlen, Michael
Morton, David A.V.
Journal name Drug development and industrial pharmacy
Volume number 41
Issue number 5
Start page 825
End page 837
Total pages 13
Publisher Taylor & Francis
Place of publication Abingdon, Eng.
Publication date 2015-05
ISSN 0363-9045
Keyword(s) Fine powder
mechanical dry powder coating
powder flow
tensile strength
Anti-Inflammatory Agents, Non-Steroidal
Chemistry, Pharmaceutical
Drug Compounding
Drug Liberation
Particle Size
Stearic Acids
Summary Intensive dry powder coating (mechanofusion) with tablet lubricants has previously been shown to give substantial powder flow improvement. This study explores whether the mechanofusion of magnesium stearate (MgSt), on a fine drug powder can substantially improve flow, without preventing the powder from being directly compacted into tablets. A fine ibuprofen powder, which is both cohesive and possesses a low-melting point, was dry coated via mechanofusion with between 0.1% and 5% (w/w) MgSt. Traditional low-shear blending was also employed as a comparison. No significant difference in particle size or shape was measured following mechanofusion. For the low-shear blended powders, only marginal improvement in flowability was obtained. However, after mechanofusion, substantial improvements in the flow properties were demonstrated. Both XPS and ToF-SIMS demonstrated high degrees of a nano-scale coating coverage of MgSt on the particle surfaces from optimized mechanofusion. The study showed that robust tablets were produced from the selected mechanofused powders, at high-dose concentration and tablet tensile strength was further optimized via addition of a Polyvinylpyrrolidone (PVP) binder (10% w/w). The tablets with the mechanofused powder (with or without PVP) also exhibited significantly lower ejection stress than those made of the raw powder, demonstrating good lubrication. Surprisingly, the release rate of drug from the tablets made with the mechanofused powder was not retarded. This is the first study to demonstrate such a single-step dry coating of model drug with MgSt, with promising flow improvement, flow-aid and lubrication effects, tabletability and also non-inhibited dissolution rate.
Language eng
DOI 10.3109/03639045.2014.908901
Field of Research 1115 Pharmacology And Pharmaceutical Sciences
Socio Economic Objective 0 Not Applicable
HERDC Research category C1.1 Refereed article in a scholarly journal
ERA Research output type C Journal article
Copyright notice ©2014, Informa Healthcare USA
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