Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol
Sébastien Rigaud,
David Mathiron,
Tarek Moufawad,
David Landy,
Florence Djedaini-Pilard,
Frédéric Marçon
Affiliations
Sébastien Rigaud
Laboratoire de Glycochimie des Antimicrobiens et des Agroressources UMR 7378 CNRS, Université de Picardie Jules Verne, 33 Rue Saint-Leu, F-80039 Amiens, France
David Mathiron
Plateforme-Analytique, Université de Picardie Jules Verne, 33 Rue Saint-Leu, F-80039 Amiens, France
Tarek Moufawad
Unité de Chimie Environnementale et Interactions sur le Vivant (UCEIV, UR 4492), ULCO, F-59140 Dunkerque, France
David Landy
Unité de Chimie Environnementale et Interactions sur le Vivant (UCEIV, UR 4492), ULCO, F-59140 Dunkerque, France
Florence Djedaini-Pilard
Laboratoire de Glycochimie des Antimicrobiens et des Agroressources UMR 7378 CNRS, Université de Picardie Jules Verne, 33 Rue Saint-Leu, F-80039 Amiens, France
Frédéric Marçon
Laboratoire AGIR UR4294, Université de Picardie Jules Verne, 1 Rue des Louvels, F-80039 Amiens, France
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.
