Desenvolvimento e validação de metodologia analítica e estudo de estabilidade de tigeciclina em produto farmacêutico
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Data
2012-08-31
Autores
Silva, Lucélia Magalhães da [UNESP]
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Editor
Universidade Estadual Paulista (Unesp)
Resumo
As glicilciclinas são uma nova classe de antibacterianos, análogos sintéticos das tetraciclinas, com atividade bacteriostática contra ampla variedade de bactérias e também contra micro-organismos resistentes às tetraciclinas. A tigeciclina é a primeira glicilciclina aprovada, distribuída comercialmente como Tygacil® pelo laboratório Wyeth, na forma farmacêutica pó liofilizado, com registro no Ministério da Saúde concedido em 2005. Este fármaco apresenta amplo espectro de ação contra bactérias Gram-positivas e Gram-negativas, aeróbicas e anaeróbicas, incluindo Staphylococcus aureus resistentes à meticilina e Enterococcus spp. resistentes à vancomicina, sendo indicada para o tratamento de infecções complicadas da pele, tecidos moles e intra-abdominais. A tigeciclina age na inibição da síntese proteica através da ligação à subunidade 30S do ribossomo bacteriano. Por ser um medicamento recente, existem poucos estudos relacionados às características físico-químicas, desenvolvimento de métodos analíticos e estudo de estabilidade, aplicados à tigeciclina. Assim, os objetivos desse trabalho foram desenvolver métodos para análise qualitativa e quantitativa de tigeciclina em pó liofilizado, bem como estudos de estabilidade. Para análise qualitativa estudaram-se os métodos por análise térmica, espectrofotometria nas regiões do infravermelho, ultravioleta e visível, cromatografia em camada delgada e cromatografia líquida de alta eficiência (CLAE), possibilitando a identificação da amostra. Para quantificação do fármaco validaram-se métodos por CLAE, microbiológicos e espectrofotométricos. O método por CLAE utilizou comprimento de onda de detecção de 280 nm, fase móvel composta por tampão fosfato de sódio monobásico (0,015 M) e ácido...
The glycylcyclines are a new class of antibacterials, sinthetic analogs of tetracyclines, with bacteriostatic activity against broad spectrum of bacterias and tetracyclines resistant organisms. The tigecycline is the first approved glycylcycline, commercially distributed in lyophilized powder pharmaceutical product as TygacilTM, by the Wyeth Pharmaceutical Laboratory, with register in the Brazilian Ministry of Healthy granted in 2005. This drug presents broad spectrum action, with activity against Gram-positive, Gram-negative, aerobic and anaerobic bacterias, including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus spp., indicated to treatment of complicated skin and skin structure infections and complicated intra-abdominal infections. Tigecycline binds to the bacterial 30S ribosome, preventing the bacterial protein synthesis. Take into account that tigecycline is a new product, there are few studies related to physicochemical characteristics, analytical methods development and stability studies, apllied to this drug. Thus, the aims of this work were to develop methods to qualitative and quantitative analysis of tigecycline in lyophilized powder as well as stability studies. To qualitative analysis, thermal analysis, infra-red, ultraviolet and visible spectrophotometry, thin layer chromatography and high performance liquid chromatography methods were studied, allowing the identification of samples. To drug quantification high performance liquid chromatography (HPLC), spectrophotometric and microbiological methods were validated. The HPLC method employed detection wavelength at 280 nm, mobile phase consisted of buffer containing sodium phosphate monobasic (0.015 M) and oxalic... (Complete abstract click electronic access below)
The glycylcyclines are a new class of antibacterials, sinthetic analogs of tetracyclines, with bacteriostatic activity against broad spectrum of bacterias and tetracyclines resistant organisms. The tigecycline is the first approved glycylcycline, commercially distributed in lyophilized powder pharmaceutical product as TygacilTM, by the Wyeth Pharmaceutical Laboratory, with register in the Brazilian Ministry of Healthy granted in 2005. This drug presents broad spectrum action, with activity against Gram-positive, Gram-negative, aerobic and anaerobic bacterias, including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus spp., indicated to treatment of complicated skin and skin structure infections and complicated intra-abdominal infections. Tigecycline binds to the bacterial 30S ribosome, preventing the bacterial protein synthesis. Take into account that tigecycline is a new product, there are few studies related to physicochemical characteristics, analytical methods development and stability studies, apllied to this drug. Thus, the aims of this work were to develop methods to qualitative and quantitative analysis of tigecycline in lyophilized powder as well as stability studies. To qualitative analysis, thermal analysis, infra-red, ultraviolet and visible spectrophotometry, thin layer chromatography and high performance liquid chromatography methods were studied, allowing the identification of samples. To drug quantification high performance liquid chromatography (HPLC), spectrophotometric and microbiological methods were validated. The HPLC method employed detection wavelength at 280 nm, mobile phase consisted of buffer containing sodium phosphate monobasic (0.015 M) and oxalic... (Complete abstract click electronic access below)
Descrição
Palavras-chave
Agentes antibacterianos, Tetraciclina
Como citar
SILVA, Lucélia Magalhães da. Desenvolvimento e validação de metodologia analítica e estudo de estabilidade de tigeciclina em produto farmacêutico. 2012. 186 f. Tese (doutorado) - Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, 2012.