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

Autor:	Sébastien Rigaud, David Mathiron, Tarek Moufawad, David Landy, Florence Djedaini-Pilard, Frédéric Marçon
Jazyk:	angličtina
Rok vydání:	2021
Předmět:	carvedilol cyclodextrins pharmaceutical solutions NMR ITC Pharmacy and materia medica RS1-441
Zdroj:	Pharmaceutics, Vol 13, Iss 11, p 1746 (2021)
Druh dokumentu:	article
ISSN:	1999-4923
DOI:	10.3390/pharmaceutics13111746
Popis:	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−1 at 298 K) than that with γCD (K = 225 M−1 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.
Databáze:	Directory of Open Access Journals
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