Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos

• Autor(a) principal: Carvalho, Murilo Ferreira de
• Data de Publicação: 2020
• Tipo de documento: Tese
• Idioma: por
• Título da fonte: Repositório Institucional da UFG
• dARK ID: ark:/38995/0013000003vvv
• Texto Completo: http://repositorio.bc.ufg.br/tede/handle/tede/10852
• topic: Voltametria; Espectroscopia de impedância eletroquímica; Bloqueador de receptores adrenérgicos; Tecnologia farmacêutica; Formulação; Excipientes; Voltammetry; Electrochemical impedance spectroscopy; Adrenergic receptor blocker; Pharmaceutical technology; Formulation; Excipients; CIENCIAS BIOLOGICAS::FARMACOLOGIA::FARMACOLOGIA GERAL

Introduction: The pharmaceutical industry faces a major challenge to improve the solubility of some active ingredients. Carvedilol (CRV) is the drug of therapeutic choice in cardiovascular diseases. CRV presents low water solubility and low bioavaliability. Several researches were performed in order to increase the oral bioavailability, where selfemulsifying appeared as viable alternatives. Objective: The objective of this work was to evaluate interactions between CRV and its excipients, detecting the oxidative potential of these substances, thus, providing predictive data for the oxidation that may affect the stability and bioavailability of the drug system. Methodology: In the carbon pastes preparation were used 70 mg (graphite) and 30 mg (oil). Six excipients, oleic acid, canola, capmul, safflower, sesame and Plurol isoestearique. The following proportions were used in the making of the paste: 30:0, 20:10, 15:15, 10:20 and 0:30 of liquid excipient (sample): mineral oil (mg:mg) and 1.5:68.5, 3:67 and 7:63 of solid excipient (sample): graphite (mg:mg). CRV was incorporated in the oil moiety for solubilization and after used in solidstate analysis in the carbon paste. The techniques used were cyclic voltammetry, differential pulse voltammetry and electrochemical impedance spectroscopy. Results and Discussions: The Isostearique Plurol® was found to be electro-active in the studied potential, however, this oil oxidizes in different potentials from CRV. The results show that Isostearique Plurol®, liquid excipient, isoestearique acid and the solid excipient presented the greatest variations of anodic potential and were considered the best excipients for the CRV formulation. CRV presented higher stability at room temperature (25 ºC), whereas, it presented higher stability at 50 ºC when mixed with 7% estearique acid. Conclusions: Evidences of incompatibility were not found, relative to the increase of oxidation vulnerability, when in the presence of these excipients. The employment of electroanalysis for CRV compatibility studies show promising viability.