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Desenvolvimento de um medicamento genérico analgésico e antipirético em saquetas aplicando Quality by Design
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Este trabalho teve como objetivo desenvolver um medicamento genérico analgésico e antipirético em pó para solução oral, visando preencher a lacuna no mercado português. Na primeira fase, foram analisadas formulações existentes nos outros mercados e na escolha de excipientes, definindo o medicamento de referência. O estudo de formulação utilizou o desenho de experiências para avaliar a influência de adoçante, deslizante, diluente e substância ativa (API) nas propriedades físico-químicas do pó, resultando em 18 experiências. Concluiu-se que o diluente Pearlitol®200 SD, representando 87% da formulação, é o fator crítico para um escoamento adequado. Duas formulações foram escolhidas, de acordo com o escoamento. Os ensaios de solubilidade demonstraram que o API é muito solúvel, confirmando que esta substância ativa pertence à Classe I do Sistema BCS.
As formulações preparadas apresentaram características físico-químicas semelhantes ao medicamento de referência, mas com menor agradabilidade sensorial pela ausência de aromatizante. As análises de granulometria e perda por secagem confirmaram a semelhança entre as formulações. Os resultados de doseamento da substância ativa apresentam valores conformes, entre 95% e 103%. A análise de impurezas por HPLC mostrou resultados dentro das especificações, sendo a impureza C com 0,18%, a que se encontra em maior quantidade, devido este ser metabolito ativo do API, a impureza A com 0,02% apenas presente no medicamento de referência e uma impureza desconhecida com 0,04%. As amostras de matriz analítica e API confirmaram a ausência de interferências nos resultados. A formulação final escolhida contém ciclamato de sódio como adoçante, aroma de groselha, deslizante, Pearlitol®200 SD e API, otimizando sabor e propriedades físico-químicas.
The aim of this study was to develop a generic analgesic and antipyretic drug in powder form for oral solution, with the primary goal of filling a gap in the Portuguese market. Firstly, existing formulations in other markets were analysed and the choice of excipients, defining the reference drug. The Design of experiments (DoE) was employed in the formulation study to assess the influence of sweetener, glidant, diluent and active pharmaceutical ingredient (API) on the powder's physicochemical properties, yielding a total of 18 experimental runs. It was concluded that the diluent Pearlitol®200 SD, representing 87% of the formulation, is the critical factor for adequate flowability. Two formulations were selected, according to the flowability. Solubility tests showed that the API is very soluble, confirming that this active substance belongs to Class I of the BCS System. The formulations prepared exhibited similar physicochemical characteristics to the reference drug, however, the absence of flavouring resulted in a less favourable sensory experience. Analyses of particle size and loss on dying confirmed the similarity between the formulations. The active substance dosage results showed values in range of 95% and 103%. The analysis of impurities by HPLC demonstrated the results were within the specifications, with impurity C of 0.18% in greater quantity, due to this being an active metabolite of the API, impurity A of 0.02% only present in the reference drug and an unknown impurity of 0.04%. The analytical matrix and API samples confirmed the absence of interference in the results. The final formulation chosen contains sodium cyclamate as a sweetener, blackcurrant flavouring, glidant, Pearlitol®200 SD and API, optimising taste and physicochemical properties.
The aim of this study was to develop a generic analgesic and antipyretic drug in powder form for oral solution, with the primary goal of filling a gap in the Portuguese market. Firstly, existing formulations in other markets were analysed and the choice of excipients, defining the reference drug. The Design of experiments (DoE) was employed in the formulation study to assess the influence of sweetener, glidant, diluent and active pharmaceutical ingredient (API) on the powder's physicochemical properties, yielding a total of 18 experimental runs. It was concluded that the diluent Pearlitol®200 SD, representing 87% of the formulation, is the critical factor for adequate flowability. Two formulations were selected, according to the flowability. Solubility tests showed that the API is very soluble, confirming that this active substance belongs to Class I of the BCS System. The formulations prepared exhibited similar physicochemical characteristics to the reference drug, however, the absence of flavouring resulted in a less favourable sensory experience. Analyses of particle size and loss on dying confirmed the similarity between the formulations. The active substance dosage results showed values in range of 95% and 103%. The analysis of impurities by HPLC demonstrated the results were within the specifications, with impurity C of 0.18% in greater quantity, due to this being an active metabolite of the API, impurity A of 0.02% only present in the reference drug and an unknown impurity of 0.04%. The analytical matrix and API samples confirmed the absence of interference in the results. The final formulation chosen contains sodium cyclamate as a sweetener, blackcurrant flavouring, glidant, Pearlitol®200 SD and API, optimising taste and physicochemical properties.
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Medicamento genérico Desenho de experiências Escoamento Solubilidade Métodos analíticos