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Irbesartan desmotropes: Solid-state characterization, thermodynamic study and dissolution properties.
Araya-Sibaja, Andrea Mariela; Maduro de Campos, Carlos Eduardo; Fandaruff, Cinira; Vega-Baudrit, José Roberto; Guillén-Girón, Teodolito; Navarro-Hoyos, Mirtha; Cuffini, Silvia Lucía.
Afiliação
  • Araya-Sibaja AM; Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE, 1174-1200, Pavas, San José, Costa Rica.
  • Maduro de Campos CE; Escuela de Ciencia e Ingeniería de los Materiales, Tecnológico de Costa Rica, Cartago, 159-7050, Costa Rica.
  • Fandaruff C; Escuela de Química, Universidad de Costa Rica, San Pedro de Montes de Oca, 2060, San José, Costa Rica.
  • Vega-Baudrit JR; Programa de Pós-Graduação em Física, Universidade Federal de Santa Catarina, Florianópolis, Brazil.
  • Guillén-Girón T; Independent Researcher, 06472-005, Barueri, São Paulo, Brazil.
  • Navarro-Hoyos M; Laboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE, 1174-1200, Pavas, San José, Costa Rica.
  • Cuffini SL; Laboratorio de Investigación y Tecnología de Polímeros POLIUNA, Escuela de Química, Universidad Nacional de Costa Rica, Heredia, 86-3000, Costa Rica.
J Pharm Anal ; 9(5): 339-346, 2019 Oct.
Article em En | MEDLINE | ID: mdl-31929943
Irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible structures, 1H- and 2H-tautomers. The difference between them lies in the protonation of the tetrazole ring. In the solid-state, both tautomers can be isolated as crystal forms A (1H-tautomer) and B (2H-tautomer). Studies have reported that IBS is a polymorphic system and its forms A and B are related monotropically. These reports indicate form B as the most stable and less soluble form. Therefore, the goal of this contribution is to demonstrate through a complete solid-state characterization, thermodynamic study and dissolution properties that the IBS forms are desmotropes that are not related monotropically. However, the intention is also to call attention to the importance of conducting strict chemical and in solid-state quality controls on the IBS raw materials. Hence, powder X-ray diffraction (PXRD) and Raman spectroscopy (RS) at ambient and non-ambient conditions, differential scanning calorimetry (DSC), hot stage microscopy (HSM), Fourier transform infrared (FT-IR) and scanning electron microscopy (SEM) techniques were applied. Furthermore, intrinsic dissolution rate (IDR) and structural stability studies at 98% relative humidity (RH), 25 °C and 40 °C were conducted as well. The results show that in fact, form A is approximately four-fold more soluble than form B. In addition, both IBS forms are stable at ambient conditions. Nevertheless, structural and/or chemical instability was observed in form B at 40 °C and 98% RH. IBS has been confirmed as a desmotropic system rather than a polymorphic one. Consequently, forms A and B are not related monotropically.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: J Pharm Anal Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Costa Rica País de publicação: China
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: J Pharm Anal Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Costa Rica País de publicação: China