Reversible Solid-State Hydration/Dehydration of Paroxetine HBr Hemihydrate: Structural and Thermochemical Studies

Autor(es)

Carvalho, Jr., Paulo S. ^[1] ; de Melo, Cristiane C. ^{[1, 2]} ; Ayala, Alejandro P. ^[2] ; da Silva, Cecilia C. P. ^[1] ; Ellena, Javier ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Inst Fis Sao Carlos, CP 369, BR-13560970 Sao Carlos, SP - Brazil

^[2] Univ Fed Ceara, Dept Fis, CP 6030, BR-60455970 Fortaleza, Ceara - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Crystal Growth & Design; v. 16, n. 3, p. 1543-1549, MAR 2016.
• Citações Web of Science: 13

Resumo

For active pharmaceutical ingredients (API) in the solid state, the occurrence of hydration/dehydration phase transitions may have implications upon the efficiency of the pharmaceutical product, once they are often accompanied by Changes of physicochemical properties. Thus, it is important for pharmaceutical research and development to investigate these mechanisms based on the crystal structures of the API. In this work, beyond the structural characterization of a new salt of the antidepressant drug Paroxetine {[}an HBr hemihydrate, (PRX+BC-)center dot 0.5H(2)O], by single crystal X-ray diffraction (SXRD), thermal analysis (DSC/TGA), and hot stage microscopy (HSM), we were able to perform a complete investigation toward the reversible hydration/dehydration solid phase transitions occurring for this salt. In addition, solubility measurements for the anhydrous and hemihydrate solid foams of the new salt are compared with those of its isostructural hydrochloride hemihydrate salt, (PRX+Cl-)center dot 0.5H(2)O, for which hydration/dehydration processes are still not completely understood due to structure instability after dehydration. (AU)

• Processo FAPESP: 12/05616-7 - Caracterização no estado sólido de fármacos de ação anti-convulsionantes e antidepressivos: Planejamento de novas formas cristalinas.
• Beneficiário: Paulo de Sousa Carvalho Júnior
• Modalidade de apoio: Bolsas no Brasil - Doutorado