Antioxidants are currently used as efficient excipients that delay or inhibit the oxidation process of molecules. Excipients are often associated with adverse reactions. Stability studies can guide the search for solutions that minimize or delay the processes of degradation. The ability to predict oxidation reactions in different drugs is important. Methods: This study was conducted to assess the rational use of butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), sodium metabisulfite (SMB), propyl gallate (PG) and cysteine (CYS) in tablet formulations of simvastatin and ketoconazole. These antioxidants were evaluated according to stability parameters and the relationship between efficiency of the antioxidant and chemical structure of the drugs. Results were compared with DPPH tests and computational simulations. BHT was most efficient regarding simvastatin stability, and the most effective BHT concentrations for maintaining stability were 0.5 and 0.1%. In relation to ketoconazole, SMB was most efficient for maintaining content and dissolution profile. The evaluation by DPPH showed that the largest percentage of absorbance reduction was observed for PG, while SMB proved most efficient and had lower consumption of DPPH. The same pattern was observed, albeit with lower efficiency, for the other lipophilic antioxidants such as BHT and BHA. The results of the molecular modeling study demonstrated that electronic properties obtained were correlated with antioxidant activity in solution, being useful for the rational development of liquid pharmaceutical formulations but not for solid oral formulations. This study demonstrated the importance of considering stability parameters and molecular modeling to elucidate the chemical phenomena involved in antioxidant activity, being useful for the rational use of antioxidants in the development of pharmaceutical formulations.Uniterms: Antioxidants/rational use. Excipients/evaluation. Butylated hydroxyanisole/rational use. Butylated hydroxytoluene/rational use. Sodium metabisulfite/rational use. Propyl gallate/rational use. Cysteine/rational use. Simvastatin/tablets/evaluation. Ketoconazole/tablets/evaluation. Atualmente, antioxidantes são usados como excipientes eficientes, que retardam ou inibem o processo de oxidação de moléculas. Excipientes são frequentemente associados a efeitos adversos. Estudos de estabilidade podem ajudar na busca por possíveis soluções para minimizar ou retardar os processos de degradação. A habilidade de prever as reações de oxidação em diferentes fármacos é importante. O estudo foi conduzido com o objetivo de avaliar o uso racional de hidroxianisol butilado (BHA), hidroxitolueno butilado (BHT), metabissulfito sódico (SMB), galato de propila (PG) e cisteína (CYS) em formulações de comprimidos de sinvastatina e cetoconazol. Eles foram avaliados por parâmetros de estabilidade e pela relação entre a eficiência dos antioxidantes e a estrutura química do fármaco. Os resultados foram comparados com testes de DPPH e simulações em computador. BHT f...
Tapioca starch (TS) is produced from Cassaca roots and it is differentiated from other starches because it contains about 17-20% amylase and low amount of residual substances. Propranolol (POP) is a non-selective beta-adrenergic blocking agent and it is in the World Health Organization's List of Essential Medicines. The aim of this work was to investigate the potential of TS in the development of POP tablets by means of direct compression. Its evaluation was performed by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), Nuclear Magnetic Resonance (NMR) relaxometry, scanning electron microscopy (SEM), uniformity of weight, drug content, disintegration, friability, hardness, dissolution test and drug release kinetics. The TS granules were spherical with mean diameter of 10.09 ± 1.85 µm. The XRD, FTIR and NMR suggested physical interaction between TS and POP. The tablets presented average diameter of 1.1 ± 0.0 cm, 0.24 ± 0.02 cm thickness and average weight of 0.544 ± 0.003 g. The hardness of tablets was 10.98 ± 0.31 N and the percentage of friability was 25.74 ± 0.08%. POP was released after 45 min and the release kinetics properly fitted the Hixson-Crowell equation.
A necessidade por um sistema de educação centrado no estudante, visando a formação de profissionais críticos e capazes de construir conhecimento a partir da avaliação da informação disponível, traz a necessidade por novas metodologias educacionais. Nessa perspectiva, a disciplina de Farmacotécnica, além de constituir uma das disciplinas profissionalizantes do curso de Farmácia, contempla uma visão multidisciplinar e complexa, sendo necessário a utilização de metodologias que estimulem um processo ativo de aprendizado. Devido ao potencial que as metodologias ativas de ensino desempenham no processo de educação, este trabalho teve como objetivo conceituar e pontuar as principais estratégias metodológicas encontradas na literatura e usadas nas disciplinas do curso de farmácia, com ênfase na disciplina de Farmacotécnica. A fim de atingir o objetivo proposta, uma revisão integrativa da literatura foi realizada para concentrar os estudos que tivessem empregado e avaliado o uso de metodologias ativas. Um total de 15 trabalhos foram encontrados seguindo os critérios de inclusão e exclusão adotados neste estudo e poucos trabalhos objetivaram conceituar e pontuar o uso de metodologias ativas na disciplina de farmacotécnica. No entanto, apesar do número baixo de trabalhos que avaliarem a performance dessas metodologias, todos os estudos apontaram melhoras significativas no desempenho e assimilação de conteúdo dos alunos, evidenciando o grande potencial dessas metodologias de ensino. A partir dos resultados observados neste trabalho, pode-se concluir, que as metodologias ativas devem ser consideradas, estimuladas e, se necessário, adaptadas, para serem utilizadas desde o início da formação profissional, independentemente da disciplina.
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