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Thermal behavior and molecular mobility studies in the supercooled liquid and glassy states of carvedilol and loratadine.
Viciosa, M Teresa; Moura Ramos, Joaquim J; Diogo, Hermínio P.
Affiliation
  • Viciosa MT; CQE - Centro de Química Estrutural, Complexo I, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal; IN - Institute of Nanoscience and Nanotechnology, Instituto Superior Tecnico, University of Lisbon, Avenida Rovisco Pais, 1049-001 Lisbon, Portugal.
  • Moura Ramos JJ; CQE - Centro de Química Estrutural, Complexo I, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal.
  • Diogo HP; CQE - Centro de Química Estrutural, Complexo I, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal.
Int J Pharm ; 584: 119410, 2020 Jun 30.
Article in En | MEDLINE | ID: mdl-32445909
ABSTRACT
The thermal behavior of carvedilol and loratadine was studied by differential scanning calorimetry (DSC). The glass-forming ability, as well as the the tendency for crystallization from the glass (glass stability) and from the metastable and equilibrium melt were also investigated by DSC. In addition this technique was also used to characterize the glass transition of carvedilol and loratadine by determining the activation energy of the structural relaxation, the dynamic fragility, and the heat capacity jump associated with the glass transformation. Different aspects of the molecular mobility in carvedilol and loratadine were analyzed by Thermally Stimulated Depolarization Currents (TSDC), while in carvedilol the Dielectric Relaxation Spectroscopy (DRS) technique was also used. Carvedilol stands out for its high values of specific heat jump and dynamic fragility, which has been attributed to the particular mobility of this glass-former in the glass transformation region, a consequence of specific characteristics of its molecular structure. These molecular features are also at the origin of a relaxation above Tg that has been detected and characterized by TSDC; the DRS investigation allowed to better understand the molecular dynamics in carvedilol in the amorphous solid, in the metastable liquid state and in the glass transformation region. Finally, the secondary relaxations in loratadine were studied by TSDC, while those in carvedilol were studied by the two dielectric techniques and the results were compared and discussed.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Chemistry, Pharmaceutical / Loratadine / Molecular Dynamics Simulation / Carvedilol Language: En Journal: Int J Pharm Year: 2020 Document type: Article Affiliation country: Portugal

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Chemistry, Pharmaceutical / Loratadine / Molecular Dynamics Simulation / Carvedilol Language: En Journal: Int J Pharm Year: 2020 Document type: Article Affiliation country: Portugal