4.3 Article

Enhanced solubility and dissolution rate of amiodarone by complexation with β-cyclodextrin through different methods

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ELSEVIER
DOI: 10.1016/j.msec.2010.05.001

Keywords

Amiodarone; beta-Cyclodextrin; Complexation; Solubility

Funding

  1. Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
  2. Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)

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The aim of this work was to investigate the inclusion complexation between amiodarone (AMD), a practically water insoluble anti arrhythmic agent, and beta-cyclodextrin (pcD) in order to improve the solubility and the dissolution rate of the drug, in an attempt to enhance its bioavailability. The complexation was done through different methods: physical mixture (PM), coevaporated (CV), freeze-drying (FD) and spray-drying (SD). The data analysis indicated that the complexes produced by freeze-drying and spray-drying techniques resulted in amorphous samples (data obtained by DSC and XRPD), and showed a possible chemical interaction between OH-beta CD group and AMD tertiary amine (visualized by FT-IR). Also, they presented higher thermal stability (demonstrated by TG) and the improvement of the drug dissolution rate. (C) 2010 Elsevier B.V. All rights reserved.

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