Avaliação farmacocinética de duas formulações orais de itraconazol em voluntários sadios do sexo masculino

• Ano de defesa: 2017
• Autor(a) principal: Soares, Marília Almeida
• Tipo de documento: Dissertação
• Tipo de acesso: Acesso aberto
• Idioma: por
• Palavras-chave em Português: Equivalência Terapêutica; Itraconazol; Similar
• Link de acesso: http://www.repositorio.ufc.br/handle/riufc/27597

Fungal infections, especially systemic, are progressively increasing in Brazil. Paracoccidioidomycosis, an example of systemic fungal disease, has presented between 1 and 3 cases per 100,000 inhabitants in endemic areas. Its main therapeutic regimen is the use of itraconazole associated with antibiotics. However, due to a shortage of effective antifungal drugs on the market and the high cost of available medicines, access to medicines is not viable for the poor. With a view to promoting health, RDC 134/2003 was approved, which requires that bioequivalence tests be carried out between similar medicines and their respective reference in order to ensure the efficacy and safety of the like. The objectives of this study were: to evaluate comparatively the bioavailability of two pharmaceutical formulations of itraconazole in order to determine its bioequivalence; draw a profile between the anthropometric parameters and investigate comparatively factors that may influence the bioavailability of itraconazole in the formulations evaluated. The study was carried out with 59 healthy male volunteers and consisted of an open, randomized, cross-over study with 2 treatments, 2 periods (two sequences) with a minimum interval of seven days between hospitalizations. Blood samples were collected at regular intervals to construct the plasma concentration versus time curves. Itraconazole concentrations were analyzed by High Efficiency Liquid Chromatography coupled to Mass Spectrometry (LC-MS / MS). The geometric mean Itraconazole test / Itraconazole reference and the 90% confidence interval (CI) for Cmax and ASC0-last were 82.79% (76.27-89.88%) and 59.73% (54.40-65 , 60%). Considering that the formulations studied were not within the ratio between C max and ASC0-last between 80% and 125%, and considering a 90% confidence interval, as proposed by the Food and Drug Administration and National Surveillance Agency It is concluded that the two formulations of itraconazole did not present similar bioavailabilities both in rate and extent of absorption and therefore are not bioequivalent.