Avaliação da qualidade e da compatibilidade fármaco-excipientes das formulações farmacêuticas sólidas do mercado contendo meloxicam

• Ano de defesa: 2017
• Autor(a) principal: Silveira, Lucas Melo da
• Tipo de documento: Dissertação
• Tipo de acesso: Acesso aberto
• Idioma: por
• Instituição de defesa: Universidade Federal do Espírito Santo; BR; Mestrado em Ciências Farmacêuticas; Centro de Ciências da Saúde; UFES; Programa de Pós-Graduação em Ciências Farmacêuticas
• Palavras-chave em Português: Intrinsic stability; Compatibility of pharmaceutical formulation; Degradation kinetics; Quality control; Cinética de degradação; Meloxicam; Estabilidade intrínseca; Compatibilidade de formulação farmacêutica; Estabilidade; Medicamentos; Cinética química; Controle de qualidade; Farmácia; 612
• Link de acesso: http://repositorio.ufes.br/handle/10/8356

Meloxicam (MLX) is a non-steroidal anti-inflammatory, cyclooxygenase (COX) inhibitor, used to relieve inflammation and pain. MLX have a preferential affinity for COX-2, which is associated with a lower incidence of gastrointestinal side effects. The drug belongs to Class II of the Biopharmaceutical Classification System (BCS) where dissolution is the bioavailability limiting step. In view of this classification, it is a fundamental to carry out further studies regarding the compatibility between drug and excipients, mechanisms and kinetics of degradation reactions, since any changes directly influence the quality of the product. The aim of the present work is to evaluate the solid pharmaceutical formulations containing MLX found on the market defining more suitable excipients to improve the stability of pharmaceutical formulations. Thermal analysis techniques were used to characterize and evaluate the compatibility between the drug and the excipients present in the market formulations. Method by high performance liquid chromatography was developed and validated for quantification of MLX and possible degradation products. Alternative method by UV spectrophotometry was validated for quantification of MLX in the formulations. In the study of compatibility between drug-excipient was found incompatibility with magnesium stearate, red iron oxide, povidone, sodium starch glycolate and mannitol. In the study of intrinsic stability, the drug was subjected to conditions of forced degradation where it was unstable in alkaline medium. In the evaluation of the solid state kinetics, the MLX degraded according to AvramiErofeyev A4 model, presenting a shelf life of about 6 years for the raw material under inert condition. In the evaluation of the quality control of the products of the market, it was observed that the Lab10 and Lab11 were disapproved in the dissolution test. As for the evaluation of the dissolution profile only two products have been shown to be pharmaceutical equivalents