Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals

The aim of the study was the manufacturing and scale-up of theophylline-nicotinamide (THL-NIC) pharmaceutical cocrystals processed by hot-melt extrusion (HME). The barrel temperature profile, feed rate and screw speed were found to be the critical processing parameters with a residence time of appro...

Descripción completa

Detalles Bibliográficos
Autores principales: Ross, Steven A., Hurt, Andrew P., Antonijevic, Milan, Bouropoulos, Nicolaos, Ward, Adam, Basford, Pat, McAllister, Mark, Douroumis, Dennis
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8004052/
https://www.ncbi.nlm.nih.gov/pubmed/33804705
http://dx.doi.org/10.3390/pharmaceutics13030419
_version_ 1783671834166689792
author Ross, Steven A.
Hurt, Andrew P.
Antonijevic, Milan
Bouropoulos, Nicolaos
Ward, Adam
Basford, Pat
McAllister, Mark
Douroumis, Dennis
author_facet Ross, Steven A.
Hurt, Andrew P.
Antonijevic, Milan
Bouropoulos, Nicolaos
Ward, Adam
Basford, Pat
McAllister, Mark
Douroumis, Dennis
author_sort Ross, Steven A.
collection PubMed
description The aim of the study was the manufacturing and scale-up of theophylline-nicotinamide (THL-NIC) pharmaceutical cocrystals processed by hot-melt extrusion (HME). The barrel temperature profile, feed rate and screw speed were found to be the critical processing parameters with a residence time of approximately 47 s for the scaled-up batches. Physicochemical characterization using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction of bulk and extruded materials revealed the formation of high purity cocrystals (98.6%). The quality of THL-NIC remained unchanged under accelerated stability conditions.
format Online
Article
Text
id pubmed-8004052
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-80040522021-03-28 Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals Ross, Steven A. Hurt, Andrew P. Antonijevic, Milan Bouropoulos, Nicolaos Ward, Adam Basford, Pat McAllister, Mark Douroumis, Dennis Pharmaceutics Article The aim of the study was the manufacturing and scale-up of theophylline-nicotinamide (THL-NIC) pharmaceutical cocrystals processed by hot-melt extrusion (HME). The barrel temperature profile, feed rate and screw speed were found to be the critical processing parameters with a residence time of approximately 47 s for the scaled-up batches. Physicochemical characterization using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction of bulk and extruded materials revealed the formation of high purity cocrystals (98.6%). The quality of THL-NIC remained unchanged under accelerated stability conditions. MDPI 2021-03-20 /pmc/articles/PMC8004052/ /pubmed/33804705 http://dx.doi.org/10.3390/pharmaceutics13030419 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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/ (https://creativecommons.org/licenses/by/4.0/) ).
spellingShingle Article
Ross, Steven A.
Hurt, Andrew P.
Antonijevic, Milan
Bouropoulos, Nicolaos
Ward, Adam
Basford, Pat
McAllister, Mark
Douroumis, Dennis
Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals
title Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals
title_full Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals
title_fullStr Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals
title_full_unstemmed Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals
title_short Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals
title_sort continuous manufacture and scale-up of theophylline-nicotinamide cocrystals
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8004052/
https://www.ncbi.nlm.nih.gov/pubmed/33804705
http://dx.doi.org/10.3390/pharmaceutics13030419
work_keys_str_mv AT rossstevena continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals
AT hurtandrewp continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals
AT antonijevicmilan continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals
AT bouropoulosnicolaos continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals
AT wardadam continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals
AT basfordpat continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals
AT mcallistermark continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals
AT douroumisdennis continuousmanufactureandscaleupoftheophyllinenicotinamidecocrystals

Ejemplares similares