Desenvolvimento farmacotécnico e analítico de comprimidos revestidos de montelucaste: equivalência farmacêutica e bioequivalência

• Ano de defesa: 2011
• Autor(a) principal: ALVES, Carina Pimentel Itapema
• Orientador(a): LIMA, Eliana Martins
• Tipo de documento: Tese
• Tipo de acesso: Acesso aberto
• Idioma: por
• Instituição de defesa: Universidade Federal de Goiás
• Programa de Pós-Graduação: Doutorado em Ciencias da Saude
• Departamento: Ciencias da Saude
• País: BR
• Palavras-chave em Português: Montelucaste; HPLC-UV; HPLC-MS/MS; desenvolvimento analítico; desenvolvimento farmacotécnico; validação; equivalência farmacêutica; bioequivalência
• Palavras-chave em Inglês: Montelukast; HPLC-UV; HPLC-MS/MS; analytical development; pharmaceutics; validation; pharmaceutical equivalence; bioequivalence
• Área do conhecimento CNPq: CNPQ::CIENCIAS DA SAUDE::MEDICINA::CLINICA MEDICA
• Link de acesso: http://repositorio.bc.ufg.br/tede/handle/tde/1548

Montelukast is a potent reversible selective inhibitor of cysteinilleukotrien- 1 receptor, avoiding that these mediators promote the asthmatic response. Its commercialization in Brazil, as a terminated product, is protected by patent up to 2010. Once the active ingredient Montelukast is recent in the pharmaceutical market and there is no methodology description in official compendiums capable to assure the quality of new formulations, the objective of this paper was the pharmaceutics of montelukast film coated tablets, the development and the validation of analytical and bioanalytical methodologies foreseeing the pharmaceutical equivalence and bioequivalence with the reference medication of the market. With this purpose, some physicalchemical parameters were characterized, assay and dissolution methodologies were developed and validated per high performance liquid chromatography with ultraviolet detection (HPLC-UV) for the quantification of montelukast present in 10.0mg film coated tablets. The quantification of montelukast sodium in human plasma was performed using Loratadine as internal standard and high performance liquid chromatography attached to mass detector (HPLC - MS / MS). The active ingredient was extracted from the human plasma using precipitation extraction. The results found for the parameters of specificity, linearity, accuracy, precision, quantification and detection limits and stability in the methodologies validation confirm they were adequate for the objective proposed. The analytical methodologies developed and validated were applied in the pharmaceutics of the tablets for the determination of the formulation similar to the market reference medication Singulair®. This formulation was submitted to stability assays to assure its quality and to allow the performance of pharmaceutical equivalence and bioequivalence with the purpose of registering as a generic medication.