901 resultados para bioavailability
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
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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.
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Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Antioxidants are substances that may protect cells from the damage caused by unstable molecules known as free radicals. The capacity of natural antioxidant from phytochemical has increase attention from researchers and public. However, the extraction process is affecting the activity and the bioavailability of bioactive compounds. The Solanum lycocarpum is a plant of the Brazilian “cerrado”, popularly used as a hypoglycemic, hypocholesterolemic and control of metabolic diseases. Its effects are attributed to the presence of several glycoalkaloids (solamargine, solasonina) and solasodine. Therefore, the purpose of this communication was, investigate the optimization of extraction condition and evaluation of antioxidant activity from fruits of Solanum lycocarpum. The extracts were obtained using different solvent systems, i.e., water, 50% ethanol, ethanol absolute and ethyl ether (1:10 and 1:20) and different extraction processes: maceration with constant agitation at room temperature, maceration with constant agitation and heating at 30°C and ultrasound. The extracts were characterized by the amount of material extracted (1, 6 and 24 h) and the action of antioxidant activity by DPPH method. The results showed that the polar solvent (50% ethanol) and extractive process maceration with agitation to ambient temperature showed higher contents of extractable of fruits of S. lycocarpum (3.4 g %) and also showed higher antioxidant activity (88.57±2.41% de inhibition). This action whether the presence of glycoalkaloids (solamargine, solasonine and solasodine) in fruits S. lycocarpum which are polar compounds and may explain this increased antioxidant action of this extract.
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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
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Pós-graduação em Ciências Farmacêuticas - FCFAR
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Due to the high incidence and prevalence of hypertension, especially in the elderly population, several studies have been developed to understand the relationship between etiological factors and blood pressure control. It has been demonstrated that hypertensive patients tend to present a status of hyperuricemia. This result suggested that there is a relationship between blood pressure and uric acid concentrations. However there is still a lack of studies that focus on this relationship, and especially how physical exercise could affect the relationship between both of them. Thus, the purpose of this study is to review and discuss the relationship between hypertension and uric acid concentration pointing the oxidative stress as the main factor of this relationship and discuss the physical exercise as the main preventive factor of high uric acid concentrations and oxidative stress. It has been described an increase in oxidative stress during the uric acid pathway because the high production of anions superoxide. This in turn, increases the activation of renin-angiotensin system and decreases nitric oxide bioavailability which will compromise the vasodilatation mechanism. However physical exercises have been associated with improvements in antioxidant capacity and nitric oxide production and bioavailability which will improve the blood pressure control.
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Pós-graduação em Química - IQ
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Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)