Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol - Université de Picardie Jules Verne
N°Spécial De Revue/Special Issue Pharmaceutics Année : 2021

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

Résumé

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 gamma CD 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 = 317M(-1) at 298 K) than that with gamma CD (K = 225M(-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.
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Dates et versions

hal-03684092 , version 1 (18-01-2024)

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Sebastien Rigaud, David Mathiron, Tarek Moufawad, David Landy, Florence Djedaini-Pilard, et al.. Cyclodextrin Complexation as a Way of Increasing the Aqueous Solubility and Stability of Carvedilol. Pharmaceutics, 13 (11), pp.1746, 2021, Special Issue Novel Cyclodextrin Based Systems for Drug Delivery and Related Issues, ⟨10.3390/pharmaceutics13111746⟩. ⟨hal-03684092⟩
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