956 resultados para POORLY SOLUBLE API


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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

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Herbal medicines have been widely used around the world since ancient times. The advancement of phytochemical and phytopharmacological sciences has enabled elucidation of the composition and biological activities of several medicinal plant products. The effectiveness of many species of medicinal plants depends on the supply of active compounds. Most of the biologically active constituents of extracts, such as flavonoids, tannins, and terpenoids, are highly soluble in water, but have low absorption, because they are unable to cross the lipid membranes of the cells, have excessively high molecular size, or are poorly absorbed, resulting in loss of bioavailability and efficacy. Some extracts are not used clinically because of these obstacles. It has been widely proposed to combine herbal medicine with nanotechnology, because nano-structured systems might be able to potentiate the action of plant extracts, reducing the required dose and side effects, and improving activity. Nanosystems can deliver the active constituent at a sufficient concentration during the entire treatment period, directing it to the desired site of action. Conventional treatments do not meet these requirements. The purpose of this study is to review nanotechnology- based drug delivery systems and herbal medicines.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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Pós-graduação em Engenharia Mecânica - FEG

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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

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Bioactive components in rice vary depending on the variety and growing condition. Fat-soluble components such as gamma-oryzanol, tocopherols, tocotrienols, carotenoids, and fatty acids were analyzed in brown, sugary brown, red, and black rice varieties using established high-performance liquid chromatography (HPLC) and GC methodologies. In addition, these colored rice varieties were further analyzed using a high-resolution liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) (LTQ-Orbitrap XL) to identify the [M-H](-) ions of gamma-oryzanol, ranging from m/z 573.3949 to 617.4211. The highest content of tocopherols (alpha-, 1.5; gamma-, 0.5 mg/100 g) and carotenoids (lutein 244; trans-beta carotene 25 mu g/100 g) were observed in black rice; tocotrienols (alpha-, 0.07; gamma-, 0.14 mg/100 g) in red rice, and gamma-oryzanol (115 mg/100 g) in sugary brown rice. In all colored rice varieties, the major fatty acids were palmitic (16:0), oleic (18:1n-9), and linoleic (18:2n-6) acids. When the gamma-oryzanol components were further analyzed by LC-MS/MS, 3, 10, 8, and 8 triterpene alcohols or sterol ferulates were identified in brown, sugary brown, red, and black rice varieties, respectively. Such structural identification can lead to the elucidation of biological function of each component at the molecular level. Consumption of colored rice rich in beneficial bioactive compounds may be a useful dietary strategy for achieving optimal health.

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Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy. of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.

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This research project focused primarily on assessing the impact toughness of the weld and the base material of a steel pipe API 5L X70 submerged arc welded, used to conduct remote oil and gas (linepipes). The analysis followed strictly the Specification for Line Pipe - API 5L Standard, regarding the removal of the specimens of regions-of-proof-long section of the pipe, at 90o and 180o from the welded joint, and mechanical properties of toughness and Charpy-V, both the joint welded as the base material. Specimens of steel tube supplied by Tenaris Confab-SA were sized for tensile and Charpy-V, according to ASTM E 8M and ASTM E23, respectively. The result obtained showed that the API X70 steel tube has high Charpy-V toughness, near to each other at both 90o and 180o from the welded joint of the tube, and both higher than the weld metal. Microstructural and microhardness analysis complemented the present study

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Because of the great metallurgical advances, the welded tubes by HF / ERW (High Frequency / Electrical Resistance Welding) have played a more active role in the oil and gas, gradually replacing tubes produced by other processes (UOE, SAW, and others) to deep water applications, in high and extremely low temperatures, highpressure conditions and in highly corrosive environments. However, studies have revealed that defects in the welded joints are in one of main causes of failures in pipelines. Associated with damage external and the stringent requirements of this sector, the welded joints become particularly critical for his toughness and the determination of this particular property is fundamental. This study aims to evaluate the toughness of the HF / ERW pipes in HSLA steel API X70 class, used in pipelines transport systems of gas and oil from data obtained with CTOD tests (Crack Tip Opening Displacement). The main objectives of this project are: mechanical and microstructural characterization of steels API X70 manufactured in Brazil; and evaluation of the toughness of weld process by HF / ERW steel API X70 national. After having the tests done, mechanical, chemical and metallurgical, we have the conclusion that those pipe are in agreement to API 5L 42ª edition for X70MO and the toughness behaves like the expected

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Studies about structural integrity are very important when it desires to prevent disasters associated with flaws inherent in materials used in structural components. The welded joints in steel pipes used to conduction and distribution of oil and gas correspond to the regions most susceptible to flaw. Aiming to contribute to this research line, the present study was designed to assess experimentally the structural integrity of welded joints in steel pipes API 5L X70 used in pipeline systems. This assessment is given from tests of CTOD, whose aim is simulate in laboratory the real behaviour of crack from of his propagation on the welded joint obtained by high frequency electric resistance welding. In this case, the analyses are performed from specimens SE(B) obtained directly of steel pipe API 5L X70. The proposed methodology involves tests of CTOD at lower temperature, in order to assess the toughness of material in critical operation conditions. From performance of CTOD tests, was possible assess the toughness of welded joints in terms of quantity through CTOD parameter and in terms of quality from behaviour of curve load versus CMOD. In this study, also, sought to compare CTOD’s results obtained through rules ASTM E1820 (2008) and BS 7448 (1991). Although the two standards cited previously have adopted different parameters to calculated the value of CTOD, concluded that the values of CTOD tend to converge for a common value

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On the grounds of the great advances achieved over recent years, the process HF/ERW (High-Frequency/Electric Resistance Welding)welded pipe have played an active role in the oil and gas industry for deep water applications, at high and extremely low temperatures, under high pressure and in highly corrosive environments, gradually replacing manufactured pipes by other processes. However, studies have shown that defects in the welded joints are a the leading causes of pipelines failures, which has required the determination of toughness values in this region, in compliance with the strict recommendations of the codes and standards with manufacturers and construction companies, on the oil and gas sector. As part of the validation process required toughness values, this research project focuses on a microstructural analysis in HF / ERW tubes microalloyed, steel grade API 5CT P110, designed to explore oil and gas in deep waters, the subject of strategic relevance to the country because of the recent discoveries in the Santos mega fields: Tupi and Libra (pre-salt). In this scientific work will be presented and discussed the results of mechanical tensile and Charpy, a few CTOD tests curves (showing the trend of toughness values to be obtained), and the microstructures of the base material obtained by optical microscopy, with special emphasis on the formation of nonmetallic inclusions in the welded joint