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Single-step Coprocessing of Cohesive Powder via Mechanical Dry Coating for Direct Tablet Compression.
J Pharm Sci. 2017 01; 106(1):159-167.JP

Abstract

This study aims at testing the feasibility of a single-step coating process to produce a powder formulation of active and inactive ingredients for direct compression. A cohesive ibuprofen powder was coprocessed with a coating material, a binder (polyvinylpyrrolidone K25), and a superdisintegrant (crospovidone). Magnesium stearate (MgSt), l-leucine, and silica were selected as coating materials (1% w/w). A coprocessed powder without any coating material was employed as a control. Coating with MgSt, l-leucine, or silica produced significantly improved powder flow in comparison to the control batch. Robust tablets were produced from the processed powders for each coating material. The tablets compacted using the coated powders with MgSt or l-leucine also exhibited significantly lower tablet ejection forces than the control batch, demonstrating their lubrication effect. Furthermore, the disintegration time and dissolution rates of these tablets made of the formulations coprocessed with lubricants were enhanced, even for those coated with the hydrophobic material such as MgSt that has been previously reported to inhibit dissolution. However, the tablets made with silica-coated powders would not disintegrate. This study indicated the feasibility of a single-step dry coating process to produce powders with both flow-aid and lubrication effects, which are suitable for direct compression.

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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, Victoria 3055, Australia.
Stewart PJ
Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3055, Australia.
Hapgood KP
Department of Chemical Engineering, Monash University, Clayton, Victoria 3800, Australia.
Lakio S
AstraZeneca R&D, Pepparedsleden 1, 43183 Mölndal, Sweden.
Morton DAV
Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3055, Australia. Electronic address: david.morton@monash.edu.
Zhou QT
Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, West Lafayette, Indiana 47907-2091. Electronic address: tonyzhou@purdue.edu.

MeSH

Anti-Inflammatory Agents, Non-SteroidalCompressive StrengthDrug CompoundingExcipientsIbuprofenLeucineLubricantsPovidonePowdersSilicon DioxideSolubilityStearic AcidsTablets, Enteric-Coated

Pub Type(s)

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

Language

eng

PubMed ID

27665128

Citation

Qu, Li, et al. "Single-step Coprocessing of Cohesive Powder Via Mechanical Dry Coating for Direct Tablet Compression." Journal of Pharmaceutical Sciences, vol. 106, no. 1, 2017, pp. 159-167.
Qu L, Stewart PJ, Hapgood KP, et al. Single-step Coprocessing of Cohesive Powder via Mechanical Dry Coating for Direct Tablet Compression. J Pharm Sci. 2017;106(1):159-167.
Qu, L., Stewart, P. J., Hapgood, K. P., Lakio, S., Morton, D. A. V., & Zhou, Q. T. (2017). Single-step Coprocessing of Cohesive Powder via Mechanical Dry Coating for Direct Tablet Compression. Journal of Pharmaceutical Sciences, 106(1), 159-167. https://doi.org/10.1016/j.xphs.2016.07.017
Qu L, et al. Single-step Coprocessing of Cohesive Powder Via Mechanical Dry Coating for Direct Tablet Compression. J Pharm Sci. 2017;106(1):159-167. PubMed PMID: 27665128.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Single-step Coprocessing of Cohesive Powder via Mechanical Dry Coating for Direct Tablet Compression. AU - Qu,Li, AU - Stewart,Peter J, AU - Hapgood,Karen P, AU - Lakio,Satu, AU - Morton,David A V, AU - Zhou,Qi Tony, Y1 - 2016/09/21/ PY - 2016/03/22/received PY - 2016/07/04/revised PY - 2016/07/20/accepted PY - 2016/9/26/pubmed PY - 2017/12/13/medline PY - 2016/9/26/entrez KW - direct compression KW - dissolution KW - fine cohesive powder KW - flowability KW - lubrication KW - mechanical dry coating SP - 159 EP - 167 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 106 IS - 1 N2 - This study aims at testing the feasibility of a single-step coating process to produce a powder formulation of active and inactive ingredients for direct compression. A cohesive ibuprofen powder was coprocessed with a coating material, a binder (polyvinylpyrrolidone K25), and a superdisintegrant (crospovidone). Magnesium stearate (MgSt), l-leucine, and silica were selected as coating materials (1% w/w). A coprocessed powder without any coating material was employed as a control. Coating with MgSt, l-leucine, or silica produced significantly improved powder flow in comparison to the control batch. Robust tablets were produced from the processed powders for each coating material. The tablets compacted using the coated powders with MgSt or l-leucine also exhibited significantly lower tablet ejection forces than the control batch, demonstrating their lubrication effect. Furthermore, the disintegration time and dissolution rates of these tablets made of the formulations coprocessed with lubricants were enhanced, even for those coated with the hydrophobic material such as MgSt that has been previously reported to inhibit dissolution. However, the tablets made with silica-coated powders would not disintegrate. This study indicated the feasibility of a single-step dry coating process to produce powders with both flow-aid and lubrication effects, which are suitable for direct compression. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/27665128/Single_step_Coprocessing_of_Cohesive_Powder_via_Mechanical_Dry_Coating_for_Direct_Tablet_Compression_ DB - PRIME DP - Unbound Medicine ER -