Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties Analysis

Drug cocrystals and salts have promising applications for modulating the physicochemical properties and solubility of pharmaceuticals. In this study, a cocrystal and two salts of febuxostat (FEB) with pyridine nitrogen coformers, including 4, 4′-bipyridine (BIP), 3-aminopyridine (3AP) and 4-hydroxyp...

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Main Authors: Lei Gao, Xianrui Zhang
Format: Article
Language:English
Published: Wiley 2021-01-01
Series:Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2021/3834368
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author Lei Gao
Xianrui Zhang
author_facet Lei Gao
Xianrui Zhang
author_sort Lei Gao
collection DOAJ
description Drug cocrystals and salts have promising applications for modulating the physicochemical properties and solubility of pharmaceuticals. In this study, a cocrystal and two salts of febuxostat (FEB) with pyridine nitrogen coformers, including 4, 4′-bipyridine (BIP), 3-aminopyridine (3AP) and 4-hydroxypyridine (4HP), were designed to improve the solubility of FEB. The single-crystal structures were elucidated, and their physical and chemical properties were investigated by IR, PXRD, and DSC. In addition, drug-related properties, including the solubility and powder dissolution rate were assessed. The solubility and powder dissolution studies showed that the FEB-BIP cocrystal and FEB-3AP salt have superior dissolution compared to FEB.
format Article
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publishDate 2021-01-01
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record_format Article
series Journal of Chemistry
spelling doaj-art-4eb0696ffe6d468e95aab51ccece583f2025-08-20T02:05:35ZengWileyJournal of Chemistry2090-90712021-01-01202110.1155/2021/3834368Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties AnalysisLei Gao0Xianrui Zhang1College of Chemical Engineering and Resource RecyclingCollege of Chemical Engineering and Resource RecyclingDrug cocrystals and salts have promising applications for modulating the physicochemical properties and solubility of pharmaceuticals. In this study, a cocrystal and two salts of febuxostat (FEB) with pyridine nitrogen coformers, including 4, 4′-bipyridine (BIP), 3-aminopyridine (3AP) and 4-hydroxypyridine (4HP), were designed to improve the solubility of FEB. The single-crystal structures were elucidated, and their physical and chemical properties were investigated by IR, PXRD, and DSC. In addition, drug-related properties, including the solubility and powder dissolution rate were assessed. The solubility and powder dissolution studies showed that the FEB-BIP cocrystal and FEB-3AP salt have superior dissolution compared to FEB.http://dx.doi.org/10.1155/2021/3834368
spellingShingle Lei Gao
Xianrui Zhang
Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties Analysis
Journal of Chemistry
title Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties Analysis
title_full Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties Analysis
title_fullStr Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties Analysis
title_full_unstemmed Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties Analysis
title_short Cocrystallization of Febuxostat with Pyridine Coformers: Crystal Structural and Physicochemical Properties Analysis
title_sort cocrystallization of febuxostat with pyridine coformers crystal structural and physicochemical properties analysis
url http://dx.doi.org/10.1155/2021/3834368
work_keys_str_mv AT leigao cocrystallizationoffebuxostatwithpyridinecoformerscrystalstructuralandphysicochemicalpropertiesanalysis
AT xianruizhang cocrystallizationoffebuxostatwithpyridinecoformerscrystalstructuralandphysicochemicalpropertiesanalysis