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Article Dans Une Revue Pharmaceutics Année : 2021

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

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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.

Dates et versions

hal-03684092 , version 1 (01-06-2022)

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Citer

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, 2021, 13 (11), ⟨10.3390/pharmaceutics13111746⟩. ⟨hal-03684092⟩
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