Solid-State Form Characterization of Riparin I.

Autor: de Moura EA; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. elisanamoura@yahoo.com.br., Terto MVC; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. viniciuscahino@hotmail.com., de Moura Mendonça EA; Biotechnology Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. elisdoc@gmail.com., Procópio JVV; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. jose.procopio@ltf.ufpb.br., de O Costa VC; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. vicente@ltf.ufpb.br., Barbosa Filho JM; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. jbarbosa@ltf.ufpb.br., Chavez Gutierrez SJ; Pharmaceutical Sciences Departament, Federal University of Piauí, Teresina PI 64600-000, Brazil. stanley@ltf.ufpb.br., Tavares JF; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. josean@ltf.ufpb.br., Oliveira Macedo R; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. ruimacedo@ccs.ufpb.br., da Silva MS; Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil. marcelosobral.ufpb@gmail.com.
Jazyk: angličtina
Zdroj: Molecules (Basel, Switzerland) [Molecules] 2017 Oct 09; Vol. 22 (10). Date of Electronic Publication: 2017 Oct 09.
DOI: 10.3390/molecules22101615
Abstrakt: Riparin I is an alkamide with potential anxiolytic activity in preclinical studies. The characterization and understanding of solid-state properties play an importance role in drug development. For this work, the solid state of five riparin I batches (RIP-1, RIP-2, RIP-3, RIP-4, and RIP-5), obtained by the same synthesis process, were characterized by Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), DSC-photovisual, Thermogravimetry (TG), Fourier Transform Infrared (FTIR), Pyrolysis (Pyr-GC/MS), X-ray Powder Diffraction (PXRD), and Solid-State Nuclear Magnetic Resonance (ssNMR) techniques. Batches of riparin I with different crystal habits resulting in crystallization impurities were observed, which can be attributed to the presence of triethylamine. The main differences were observed by DSC, PXRD, and ssNMR analysis. DSC curves of RIP-2 and RIP-3 presented endothermic peaks at different temperatures of fusion, which can be attributed to the mixture of different crystalline forms. PXRD and ssNMR results confirmed crystallinity differences. The results offer evidence of the importance of controlling the reproducibility of the synthesis in order to obtain the adequate morphology for therapeutic efficacy and avoiding future problems in quality control of riparin I products.
Competing Interests: The authors declare no conflict of interest.
Databáze: MEDLINE
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