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Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids

The manufacturing of solid pharmaceutical dosage forms composed of cocrystals requires numerous processes during which there is risk of dissociation into parent molecules. Resonant acoustic wet granulation (RAG) was devised in an effort to complete theophylline–citric acid (THPCIT) cocrystal formati...

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Autores principales: Tanaka, Ryoma, Osotprasit, Supisara, Peerapattana, Jomjai, Ashizawa, Kazuhide, Hattori, Yusuke, Otsuka, Makoto
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7823328/
https://www.ncbi.nlm.nih.gov/pubmed/33406659
http://dx.doi.org/10.3390/pharmaceutics13010056
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author Tanaka, Ryoma
Osotprasit, Supisara
Peerapattana, Jomjai
Ashizawa, Kazuhide
Hattori, Yusuke
Otsuka, Makoto
author_facet Tanaka, Ryoma
Osotprasit, Supisara
Peerapattana, Jomjai
Ashizawa, Kazuhide
Hattori, Yusuke
Otsuka, Makoto
author_sort Tanaka, Ryoma
collection PubMed
description The manufacturing of solid pharmaceutical dosage forms composed of cocrystals requires numerous processes during which there is risk of dissociation into parent molecules. Resonant acoustic wet granulation (RAG) was devised in an effort to complete theophylline–citric acid (THPCIT) cocrystal formation during the granulation process, thereby reducing the number of operations. In addition, the influence of granulation liquid was investigated. A mixture of anhydrous THP (drug), anhydrous CIT (coformer), and hydroxypropyl cellulose (granulating agent) was processed by RAG with water or ethanol as a granulation liquid. The purposes were to (i) form granules using RAG as a breakthrough method; (ii) accomplish the cocrystallization during the integrated unit operation; and (iii) characterize the final solid product (i.e., tablet). The RAG procedure achieved complete cocrystal formation (>99%) and adequately sized granules (d50: >250 μm). The granulation using water (GW) facilitated formation of cocrystal hydrate which were then transformed into anhydrous cocrystal after drying, while the granulation using ethanol (GE) resulted in the formation of anhydrous cocrystal before and after drying. The dissolution of the highly dense GW tablet, which was compressed from granules including fine powder due to the dehydration, was slower than that of the GE tablet.
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spelling pubmed-78233282021-01-24 Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids Tanaka, Ryoma Osotprasit, Supisara Peerapattana, Jomjai Ashizawa, Kazuhide Hattori, Yusuke Otsuka, Makoto Pharmaceutics Article The manufacturing of solid pharmaceutical dosage forms composed of cocrystals requires numerous processes during which there is risk of dissociation into parent molecules. Resonant acoustic wet granulation (RAG) was devised in an effort to complete theophylline–citric acid (THPCIT) cocrystal formation during the granulation process, thereby reducing the number of operations. In addition, the influence of granulation liquid was investigated. A mixture of anhydrous THP (drug), anhydrous CIT (coformer), and hydroxypropyl cellulose (granulating agent) was processed by RAG with water or ethanol as a granulation liquid. The purposes were to (i) form granules using RAG as a breakthrough method; (ii) accomplish the cocrystallization during the integrated unit operation; and (iii) characterize the final solid product (i.e., tablet). The RAG procedure achieved complete cocrystal formation (>99%) and adequately sized granules (d50: >250 μm). The granulation using water (GW) facilitated formation of cocrystal hydrate which were then transformed into anhydrous cocrystal after drying, while the granulation using ethanol (GE) resulted in the formation of anhydrous cocrystal before and after drying. The dissolution of the highly dense GW tablet, which was compressed from granules including fine powder due to the dehydration, was slower than that of the GE tablet. MDPI 2021-01-04 /pmc/articles/PMC7823328/ /pubmed/33406659 http://dx.doi.org/10.3390/pharmaceutics13010056 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tanaka, Ryoma
Osotprasit, Supisara
Peerapattana, Jomjai
Ashizawa, Kazuhide
Hattori, Yusuke
Otsuka, Makoto
Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids
title Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids
title_full Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids
title_fullStr Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids
title_full_unstemmed Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids
title_short Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids
title_sort complete cocrystal formation during resonant acoustic wet granulation: effect of granulation liquids
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7823328/
https://www.ncbi.nlm.nih.gov/pubmed/33406659
http://dx.doi.org/10.3390/pharmaceutics13010056
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