ABSTRACT
What is it? Darunavir is a protease inhibitor used in the treatment of HIV infection. It is an important drug of therapy cocktail for patients infected with the virus. On the market there are darunavir ethanolate tablets of 75, 150, 300, 400, 600 and 800mg, because this is the most stable form. It is commercialized by Janssen-Cilag with the name PrezistaTM. Why we started? This drug has low water solubility and poor bioavailability, therefore requires administration in doses relatively high to the success of the therapeutic effect. The complexation of drugs by using cyclodextrin is welcome in this respect to improve the solubility and hence increase the dissolution rate of poorly soluble drugs. A monograph about this compound has not been described, thus it is an extremely important quality control of darunavir to demonstrate its effectiveness and safety. What we did? Some existing analytical techniques have been discussed in this manuscript, focusing on bioanalytical and pharmaceutical quality control applications. What we found? This review showed the published analytical methods reported for the determination of darunavir and discuss about its characteristics and complexation with cyclodextrin.
ABSTRACT
O darunavir é um inibidor de protease utilizado para o tratamento da infecção pelo HIV. Trata-se de um dos pilares da terapia de coquetel para pacientes portadores do vírus. O controle de qualidade na indústria farmacêutica, para identificação do teor de substância ativa e estudo das características físico-químicas do fármaco, é de fundamental importância para garantir a qualidade do produto final. O darunavir, até então, não possui métodos de análise padronizados em compêndios oficiais. Este fato justifica novas pesquisas nesta área para o desenvolvimento e validação de métodos analíticos, bem como a análise químico-farmacêutica para este fármaco tanto na matéria-prima como no produto acabado. Dessa forma, neste trabalho foram realizados (a) peso médio; (b) determinação do ponto de fusão; (c) cromatografia em camada delgada; (d) análise na região do ultravioleta; (e) análise na região do infravermelho e (f) cromatografia líquida de alta eficiência. Através do desenvolvimento das técnicas propostas é possível avaliar qualitativamente a qualidade de darunavir em comprimidos.
Darunavir is a protease inhibitor used in the treatment of HIV infection. It is a pillar of the drug cocktail for patients diagnosed with the virus. Quality control in the pharmaceutical industry, to verify the content of active substance and study the physicochemical characteristics of the drug, is essential to ensure final product quality. Until now, standardized methods for the analysis of darunavir have not been available in official compendia. This justifies new research, to develop and validate analytical methods, as well as physicochemical and pharmaceutical analysis for this drug, both as a raw material and a finished product. Thus, in this study, (a) the average weight of darunavir tablets and (b) the melting point of the pure drug were determined, and the following analytical techniques were performed: (c) thin-layer chromatography, (d) ultraviolet spectroscopy, (e) infrared spectroscopy and (f) high performance liquid chromatography. By developing the above techniques, it is possible to make a qualitative assessment of the quality of darunavir tablets.