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Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate.
Drug Dev Ind Pharm. 2015 May; 41(5):825-37.DD

Abstract

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.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Qu L
Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, VIC , Australia .
Zhou QT
No affiliation info available
Gengenbach T
No affiliation info available
Denman JA
No affiliation info available
Stewart PJ
No affiliation info available
Hapgood KP
No affiliation info available
Gamlen M
No affiliation info available
Morton DA
No affiliation info available

MeSH

Anti-Inflammatory Agents, Non-SteroidalChemistry, PharmaceuticalDrug CompoundingDrug LiberationExcipientsIbuprofenLubricantsParticle SizePovidonePowdersSolubilityStearic AcidsTabletsTensile Strength

Pub Type(s)

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

Language

eng

PubMed ID

24738790

Citation

Qu, Li, et al. "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, 2015, pp. 825-37.
Qu L, Zhou QT, Gengenbach T, et al. Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate. Drug Dev Ind Pharm. 2015;41(5):825-37.
Qu, L., Zhou, Q. T., Gengenbach, T., Denman, J. A., Stewart, P. J., Hapgood, K. P., Gamlen, M., & Morton, D. A. (2015). Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate. Drug Development and Industrial Pharmacy, 41(5), 825-37. https://doi.org/10.3109/03639045.2014.908901
Qu L, et al. Investigation of the Potential for Direct Compaction of a Fine Ibuprofen Powder Dry-coated With Magnesium Stearate. Drug Dev Ind Pharm. 2015;41(5):825-37. PubMed PMID: 24738790.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Investigation of the potential for direct compaction of a fine ibuprofen powder dry-coated with magnesium stearate. AU - Qu,Li, AU - Zhou,Qi Tony, AU - Gengenbach,Thomas, AU - Denman,John A, AU - Stewart,Peter J, AU - Hapgood,Karen P, AU - Gamlen,Michael, AU - Morton,David A V, Y1 - 2014/04/16/ PY - 2014/4/18/entrez PY - 2014/4/18/pubmed PY - 2016/3/2/medline KW - Fine powder KW - ibuprofen KW - mechanical dry powder coating KW - mechanofusion KW - powder flow KW - tableting KW - tensile strength SP - 825 EP - 37 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 41 IS - 5 N2 - 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. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/24738790/Investigation_of_the_potential_for_direct_compaction_of_a_fine_ibuprofen_powder_dry_coated_with_magnesium_stearate_ DB - PRIME DP - Unbound Medicine ER -