Novel Solid Solution of the Antiretroviral Drugs Lamivudine and Emtricitabine

Autor(es)

Fonseca, Jessica de Castro ^[1] ; Tenorio Clavijo, Juan Carlos ^[2] ; Alvarez, Natalia ^[3] ; Ellena, Javier ^[2] ; Ayala, Alejandro Pedro ^[4]

Afiliação do(s) autor(es)

^[1] Univ Fed Ceara, Dept Farm, BR-60455970 Fortaleza, Ceara - Brazil

^[2] Univ Sao Paulo, Inst Fis Sao Carlos, BR-13566590 Sao Carlos, SP - Brazil

^[3] Univ Republica, Fac Quim, Montevideo 11800 - Uruguay

^[4] Univ Fed Ceara, Dept Fis, BR-60455970 Fortaleza, Ceara - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Crystal Growth & Design; v. 18, n. 6, p. 3441-3448, JUN 2018.
• Citações Web of Science: 3

Resumo

Solid solutions could represent a viable alternative to better understand and control structure-property relationships of drugs, in order to optimize their properties for practical applications. Lamivudine (3TC) and emtricitabine (FTC) are nucleoside analogue reverse transcriptase inhibitor antiretroviral drugs, which have similar molecular structures, differing by a single fluorine atom, which is only present in the FTC molecule. Due to these similarities in structure and molecular resemblances, lamivudine and emtricitabine are good candidates for producing a solid solution with physicochemical properties controlled by the stoichiometry. Following this hypothesis, the formation of a nonconventional solid solution was verified, whose crystalline structure is not defined by any of the individual constituents but by the one of the lamivudine hydrate with emtricitabine as a solute. The crystalline structures of two members of the solid solution were determined showing a nonuniform distribution of the solute among the independent molecules of the asymmetric unit of the lamivudine hydrate structure. Thermal analysis investigations confirmed that physicochemical properties could be controlled through the variation of the emtricitabine content. (AU)

• Processo FAPESP: 13/07581-9 - Planejamento, Síntese e Caracterização de Novas Formas Sólidas de Fármacos Antirretrovirais anti-HIV.
• Beneficiário: Juan Carlos Tenorio Clavijo
• Modalidade de apoio: Bolsas no Brasil - Doutorado