Improving the granule strength of roller-compacted ibuprofen sodium for hot-melt coating processing

Amrit Paudel, Diogo Gomes Lopes, V. Garsuch, K. Becker , Andreas Zimmer, Sharareh Salar-Behzadi

Publikation: Beitrag in einer FachzeitschriftArtikelForschungBegutachtung

Abstract

Solvent-free hot-melt coating processing is a novel and cost-efficient approach to manufacturing taste-masked multiparticulate systems. However, most API powders are fine and cohesive and not processable by hot-melt coating. The aim of this study was to produce dense and abrasion-resistant granules with high drug content (>80%) via roller compaction for hot-melt coating process optimization. The selected API was ibuprofen sodium dihydrate, a salt of ibuprofen with improved bioavailability and poor intrinsic compactibility. The formulation and roller compaction process were developed for the production of granules with 94%w/w of API and low friability (∼30%), using sorbitol and isomalt as excipients. The strong bonding mechanism relied on powder jamming prior to the rollers and was investigated via scanning electron microscopy, differential scanning calorimetry and small and wide angle X-ray scattering. It was shown that sorbitol crystals are solubilized during roller compaction and recrystallize as sorbitol hydrate, acting as strong solid bridges. The robustness of the roller compaction process and the re-compaction of fines were investigated. A statistical design of experiments was conducted to evaluate the hot-melt coating process for taste masking of ibuprofen sodium granules. Taste masking required coating ratios higher than 40%w/w of granule batch, emphasizing the need for high-drug-content and abrasion-resistant granules.
Originalspracheenglisch
Seiten (von - bis)285-295
FachzeitschriftInternational Journal of Pharmaceutics
PublikationsstatusVeröffentlicht - 20 Aug 2016

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Sorbitol
Ibuprofen
Sodium
Powders
Excipients
Differential Scanning Calorimetry
Pharmaceutical Preparations
Electron Scanning Microscopy
Biological Availability
Salts
X-Rays
Costs and Cost Analysis

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Improving the granule strength of roller-compacted ibuprofen sodium for hot-melt coating processing. / Paudel, Amrit; Gomes Lopes, Diogo; Garsuch, V.; Becker , K.; Zimmer, Andreas; Salar-Behzadi, Sharareh.

in: International Journal of Pharmaceutics, 20.08.2016, S. 285-295.

Publikation: Beitrag in einer FachzeitschriftArtikelForschungBegutachtung

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abstract = "Solvent-free hot-melt coating processing is a novel and cost-efficient approach to manufacturing taste-masked multiparticulate systems. However, most API powders are fine and cohesive and not processable by hot-melt coating. The aim of this study was to produce dense and abrasion-resistant granules with high drug content (>80{\%}) via roller compaction for hot-melt coating process optimization. The selected API was ibuprofen sodium dihydrate, a salt of ibuprofen with improved bioavailability and poor intrinsic compactibility. The formulation and roller compaction process were developed for the production of granules with 94{\%}w/w of API and low friability (∼30{\%}), using sorbitol and isomalt as excipients. The strong bonding mechanism relied on powder jamming prior to the rollers and was investigated via scanning electron microscopy, differential scanning calorimetry and small and wide angle X-ray scattering. It was shown that sorbitol crystals are solubilized during roller compaction and recrystallize as sorbitol hydrate, acting as strong solid bridges. The robustness of the roller compaction process and the re-compaction of fines were investigated. A statistical design of experiments was conducted to evaluate the hot-melt coating process for taste masking of ibuprofen sodium granules. Taste masking required coating ratios higher than 40{\%}w/w of granule batch, emphasizing the need for high-drug-content and abrasion-resistant granules.",
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AU - Paudel, Amrit

AU - Gomes Lopes, Diogo

AU - Garsuch, V.

AU - Becker , K.

AU - Zimmer, Andreas

AU - Salar-Behzadi, Sharareh

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N2 - Solvent-free hot-melt coating processing is a novel and cost-efficient approach to manufacturing taste-masked multiparticulate systems. However, most API powders are fine and cohesive and not processable by hot-melt coating. The aim of this study was to produce dense and abrasion-resistant granules with high drug content (>80%) via roller compaction for hot-melt coating process optimization. The selected API was ibuprofen sodium dihydrate, a salt of ibuprofen with improved bioavailability and poor intrinsic compactibility. The formulation and roller compaction process were developed for the production of granules with 94%w/w of API and low friability (∼30%), using sorbitol and isomalt as excipients. The strong bonding mechanism relied on powder jamming prior to the rollers and was investigated via scanning electron microscopy, differential scanning calorimetry and small and wide angle X-ray scattering. It was shown that sorbitol crystals are solubilized during roller compaction and recrystallize as sorbitol hydrate, acting as strong solid bridges. The robustness of the roller compaction process and the re-compaction of fines were investigated. A statistical design of experiments was conducted to evaluate the hot-melt coating process for taste masking of ibuprofen sodium granules. Taste masking required coating ratios higher than 40%w/w of granule batch, emphasizing the need for high-drug-content and abrasion-resistant granules.

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