Carvedilol : decomposition kinetics and compatibility with pharmaceutical excipients.
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Data
2014
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Resumo
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.
Descrição
Palavras-chave
Activation energy, Compatibility, Differential scanning calorimetry, Isothermal thermogravimetry
Citação
TALVANI, A. et al. Carvedilol: decomposition kinetics and compatibility with pharmaceutical excipients. Journal of Thermal Analysis and Calorimetry, v. 115, p. 2501-2506, 2014. Disponível em: <http://link.springer.com/article/10.1007/s10973-013-3491-7>. Acesso em: 19 fev. 2017.