Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol

We studied the effect of several CDs on carvedilol’s solubility and chemical stability in various aqueous media. Our present results show that it is possible to achieve a carvedilol concentration of 5 mg/mL (12.3 mM) in the presence of 5 eq of γCD or RAMEB in an aqueous medium with an acceptable aci...

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Autores principales:	Sébastien Rigaud, David Mathiron, Tarek Moufawad, David Landy, Florence Djedaini-Pilard, Frédéric Marçon
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	carvedilol cyclodextrins pharmaceutical solutions NMR ITC Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/7c1d566c5a71477595bfcbcc809255f9
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id	oai:doaj.org-article:7c1d566c5a71477595bfcbcc809255f9
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spelling	oai:doaj.org-article:7c1d566c5a71477595bfcbcc809255f92021-11-25T18:40:20ZCyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol10.3390/pharmaceutics131117461999-4923https://doaj.org/article/7c1d566c5a71477595bfcbcc809255f92021-10-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1746https://doaj.org/toc/1999-4923We studied the effect of several CDs on carvedilol’s solubility and chemical stability in various aqueous media. Our present results show that it is possible to achieve a carvedilol concentration of 5 mg/mL (12.3 mM) in the presence of 5 eq of γCD or RAMEB in an aqueous medium with an acceptable acid pH (between 3.5 and 4.7). Carvedilol formed 1:1 inclusion complexes but those with RAMEB appear to be stronger (K = 317 M<sup>−1</sup> at 298 K) than that with γCD (K = 225 M<sup>−1</sup> at 298 K). The complexation of carvedilol by RAMEB significantly increased the drug’s photochemical stability in aqueous solution. These results might constitute a first step towards the development of a novel oral formulation of carvedilol.Sébastien RigaudDavid MathironTarek MoufawadDavid LandyFlorence Djedaini-PilardFrédéric MarçonMDPI AGarticlecarvedilolcyclodextrinspharmaceutical solutionsNMRITCPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1746, p 1746 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	carvedilol cyclodextrins pharmaceutical solutions NMR ITC Pharmacy and materia medica RS1-441
spellingShingle	carvedilol cyclodextrins pharmaceutical solutions NMR ITC Pharmacy and materia medica RS1-441 Sébastien Rigaud David Mathiron Tarek Moufawad David Landy Florence Djedaini-Pilard Frédéric Marçon Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
description	We studied the effect of several CDs on carvedilol’s solubility and chemical stability in various aqueous media. Our present results show that it is possible to achieve a carvedilol concentration of 5 mg/mL (12.3 mM) in the presence of 5 eq of γCD or RAMEB in an aqueous medium with an acceptable acid pH (between 3.5 and 4.7). Carvedilol formed 1:1 inclusion complexes but those with RAMEB appear to be stronger (K = 317 M<sup>−1</sup> at 298 K) than that with γCD (K = 225 M<sup>−1</sup> at 298 K). The complexation of carvedilol by RAMEB significantly increased the drug’s photochemical stability in aqueous solution. These results might constitute a first step towards the development of a novel oral formulation of carvedilol.
format	article
author	Sébastien Rigaud David Mathiron Tarek Moufawad David Landy Florence Djedaini-Pilard Frédéric Marçon
author_facet	Sébastien Rigaud David Mathiron Tarek Moufawad David Landy Florence Djedaini-Pilard Frédéric Marçon
author_sort	Sébastien Rigaud
title	Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_short	Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_full	Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_fullStr	Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_full_unstemmed	Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
title_sort	cyclodextrin complexation as a way of increasing the aqueous solubility and stability of carvedilol
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/7c1d566c5a71477595bfcbcc809255f9
work_keys_str_mv	AT sebastienrigaud cyclodextrincomplexationasawayofincreasingtheaqueoussolubilityandstabilityofcarvedilol AT davidmathiron cyclodextrincomplexationasawayofincreasingtheaqueoussolubilityandstabilityofcarvedilol AT tarekmoufawad cyclodextrincomplexationasawayofincreasingtheaqueoussolubilityandstabilityofcarvedilol AT davidlandy cyclodextrincomplexationasawayofincreasingtheaqueoussolubilityandstabilityofcarvedilol AT florencedjedainipilard cyclodextrincomplexationasawayofincreasingtheaqueoussolubilityandstabilityofcarvedilol AT fredericmarcon cyclodextrincomplexationasawayofincreasingtheaqueoussolubilityandstabilityofcarvedilol
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Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol

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