Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose

As amorphization may improve the solubility and bioavailability of a drug substance, the aim of this work was to assess to what extent the crystallinity of caffeine (CAF) and theophylline (TF) can be reduced by homogenization with a polymeric excipient. To realize this purpose, the physical mixtures...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Edyta Leyk, Marek Wesolowski
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	caffeine theophylline HPMC miscibility curves solubility curves DSC Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/e283acea960b40a68c5da3b18b9d866e
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:e283acea960b40a68c5da3b18b9d866e
record_format	dspace
spelling	oai:doaj.org-article:e283acea960b40a68c5da3b18b9d866e2021-11-25T18:41:02ZMiscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose10.3390/pharmaceutics131118361999-4923https://doaj.org/article/e283acea960b40a68c5da3b18b9d866e2021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1836https://doaj.org/toc/1999-4923As amorphization may improve the solubility and bioavailability of a drug substance, the aim of this work was to assess to what extent the crystallinity of caffeine (CAF) and theophylline (TF) can be reduced by homogenization with a polymeric excipient. To realize this purpose, the physical mixtures of both methylxanthines with hydroxypropyl methylcellulose (HPMC) were examined using differential scanning calorimetry (DSC), hot-stage microscopy (HSM), Fourier-transform infrared (FTIR) and Raman spectroscopy. Moreover, phase diagrams for the physical mixtures were calculated using theoretical data. Results of DSC experiments suggested that both CAF and TF underwent amorphization, which indicated proportional loss of crystallinity for methylxanthines in the mixtures with HPMC. Additionally, HSM revealed that no other crystalline or amorphous phases were created other than those observed for CAF and TF. FTIR and Raman spectra displayed all the bands characteristic for methylxanthines in mixtures with HPMC, thereby excluding changes in their chemical structures. However, changes to the intensity of the bands created by hydrogen bonds imply the formation of hydrogen bonding in the carbonyl group of methylxanthines and the methyl polymer group. This is consistent with data obtained using principal component analysis. The findings of these studies revealed the quantities of methylxanthines which may be dissolved in the polymer at a given temperature and the composition at which methylxanthines and polymer are sufficiently miscible to form a solid solution.Edyta LeykMarek WesolowskiMDPI AGarticlecaffeinetheophyllineHPMCmiscibility curvessolubility curvesDSCPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1836, p 1836 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	caffeine theophylline HPMC miscibility curves solubility curves DSC Pharmacy and materia medica RS1-441
spellingShingle	caffeine theophylline HPMC miscibility curves solubility curves DSC Pharmacy and materia medica RS1-441 Edyta Leyk Marek Wesolowski Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose
description	As amorphization may improve the solubility and bioavailability of a drug substance, the aim of this work was to assess to what extent the crystallinity of caffeine (CAF) and theophylline (TF) can be reduced by homogenization with a polymeric excipient. To realize this purpose, the physical mixtures of both methylxanthines with hydroxypropyl methylcellulose (HPMC) were examined using differential scanning calorimetry (DSC), hot-stage microscopy (HSM), Fourier-transform infrared (FTIR) and Raman spectroscopy. Moreover, phase diagrams for the physical mixtures were calculated using theoretical data. Results of DSC experiments suggested that both CAF and TF underwent amorphization, which indicated proportional loss of crystallinity for methylxanthines in the mixtures with HPMC. Additionally, HSM revealed that no other crystalline or amorphous phases were created other than those observed for CAF and TF. FTIR and Raman spectra displayed all the bands characteristic for methylxanthines in mixtures with HPMC, thereby excluding changes in their chemical structures. However, changes to the intensity of the bands created by hydrogen bonds imply the formation of hydrogen bonding in the carbonyl group of methylxanthines and the methyl polymer group. This is consistent with data obtained using principal component analysis. The findings of these studies revealed the quantities of methylxanthines which may be dissolved in the polymer at a given temperature and the composition at which methylxanthines and polymer are sufficiently miscible to form a solid solution.
format	article
author	Edyta Leyk Marek Wesolowski
author_facet	Edyta Leyk Marek Wesolowski
author_sort	Edyta Leyk
title	Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose
title_short	Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose
title_full	Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose
title_fullStr	Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose
title_full_unstemmed	Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose
title_sort	miscibility and solubility of caffeine and theophylline in hydroxypropyl methylcellulose
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/e283acea960b40a68c5da3b18b9d866e
work_keys_str_mv	AT edytaleyk miscibilityandsolubilityofcaffeineandtheophyllineinhydroxypropylmethylcellulose AT marekwesolowski miscibilityandsolubilityofcaffeineandtheophyllineinhydroxypropylmethylcellulose
_version_	1718410867602620416

Miscibility and Solubility of Caffeine and Theophylline in Hydroxypropyl Methylcellulose

Ejemplares similares