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Carvedilol: decomposition kinetics and compatibility with pharmaceutical excipients

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Abstract

Carvedilol (CARVE) is an important cardiovascular drug with limited bioavailability. To improve its therapeutic performance, the investigation of new dosage forms is of great interest due its relevance in clinical applications. Therefore, the aim of this work was to evaluate the stability of CARVE and its drug–excipient compatibility to support its pharmaceutical development. Kinetic analysis under isothermal conditions using thermogravimetry was performed to determine the activation energy of CARVE through an Arrhenius plot. Differential scanning calorimetry, Fourier transform infrared spectroscopy, and optical microscopy were used to test binary mixtures of CARVE and selected excipients. The activation energy of CARVE was 81.2 kJ mol−1, and from the compatibility studies, all the excipients showed strong thermal interactions, presenting changes in the melting profile of the drug. In addition, analytical assays revealed no physical or chemical changes; because of this, all eight excipients studied are considered compatible and are recommended in formulations containing CARVE. All the evidence together attests to the low chemical reactivity of CARVE and provides useful information for the development of new pharmaceutical formulations containing CARVE.

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Acknowledgements

The authors gratefully acknowledge Universidade Federal de Ouro Preto (UFOP) for their financial support. AT and MTB are recipients of productivity awards from CNPq.

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Authors and Affiliations

  1. Departamento de Ciências Biológicas (NUPEB), Universidade Federal de Ouro Preto (UFOP), Campus Morro do Cruzeiro, Bauxita, Ouro Prêto, MG, 35400-000, Brazil

    André Talvani & Maria Terezinha Bahia

  2. Faculdade de Ceilândia, Universidade de Brasília (UnB), Ceilândia, DF, 70910-900, Brazil

    Lívia Cristina Lira de Sá-Barreto

  3. Faculdade de Farmácia, Universidade Federal de Goiás (UFG), Avenida Universitária, Setor Universitário, s/n, Goiânia, GO, 74605-220, Brazil

    Eliana Martins Lima

  4. Faculdade de Ciências da Saúde, Universidade de Brasília (UnB), Campus Universitário Darcy Ribeiro, Brasília, DF, 70910-900, Brazil

    Marcílio Sérgio Soares da Cunha-Filho

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  1. André Talvani
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  2. Maria Terezinha Bahia
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  3. Lívia Cristina Lira de Sá-Barreto
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  4. Eliana Martins Lima
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  5. Marcílio Sérgio Soares da Cunha-Filho
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Correspondence to Marcílio Sérgio Soares da Cunha-Filho.

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Talvani, A., Bahia, M.T., de Sá-Barreto, L.C.L. et al. Carvedilol: decomposition kinetics and compatibility with pharmaceutical excipients. J Therm Anal Calorim 115, 2501–2506 (2014). https://doi.org/10.1007/s10973-013-3491-7

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  • DOI: https://doi.org/10.1007/s10973-013-3491-7

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