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

ABSTRACT: 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.

SUBMITTER: Rigaud S

PROVIDER: S-EPMC8620534 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature

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

Rigaud Sébastien S Mathiron David D Moufawad Tarek T Landy David D Djedaini-Pilard Florence F Marçon Frédéric F

Pharmaceutics 20211020 11

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). ...[more]

PMID: 34834163

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