Carvedilol : decomposition kinetics and compatibility with pharmaceutical excipients.

Silva, André Talvani Pedrosa da; Bahia, Maria Terezinha; Barreto, Lívia Cristina Lira de Sá; Lima, Eliana Martins; Cunha Filho, Marcílio Sérgio Soares da

Carvedilol : decomposition kinetics and compatibility with pharmaceutical excipients.

Date

2014

Authors

Silva, André Talvani Pedrosa da

Bahia, Maria Terezinha

Barreto, Lívia Cristina Lira de Sá

Lima, Eliana Martins

Cunha Filho, Marcílio Sérgio Soares da

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.

Keywords

Activation energy, Compatibility, Differential scanning calorimetry, Isothermal thermogravimetry

Citation

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.