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41.
Elionai Cassiana de Lima Gomes Izabella Ercole de Carvalho Silvia Ligório Fialho Jamile Barbosa Maria Irene Yoshida Armando da Silva Cunha Júnior 《Journal of Thermal Analysis and Calorimetry》2018,131(3):2123-2128
Most of the pharmaceutical products are formulated as solid dosage form, which may present drug–excipient interactions that lead to changes in the chemical nature of the drug, such as solubility and bioavailability and may compromise its safety and effectiveness. Differential scanning calorimetry (DSC) is a widely used method for the rapid evaluation of the drug-excipient compatibility and the stability of the mixture formed; however, there is no consensus on the preparation methods of the drug–excipient mixtures. The aim of this study was to investigate the influence of the mixing method on the drug–excipient compatibility studies by means of DSC analysis, using tenofovir disoproxil fumarate as a drug model. Statistical analysis revealed significant differences in the heat of fusion of the drug in the mixtures prepared by several mixing methods. Vortex Mixer with a Pop-Off Cup used for 3 min proved to be very satisfactory for these studies. A polymorphic transition was observed in the mixture prepared with the mortar and pestle. Therefore, this method should be avoided since it may induce errors in the interpretation of DSC results. In this way, the mixing method used to prepare a mixture for studies of interactions between the API and the excipients in a pharmaceutical formulation has a great influence on the results and it must be chosen carefully. 相似文献
42.
Dimitrios Pavlidis Jefferson L. M. A. Gomes Zhihua Xie James R. Percival Christopher C. Pain Omar K. Matar 《国际流体数值方法杂志》2016,80(4):256-282
This paper develops methods for interface‐capturing in multiphase flows. The main novelties of these methods are as follows: (a) multi‐component modelling that embeds interface structures into the continuity equation; (b) a new family of triangle/tetrahedron finite elements, in particular, the P1DG‐P2(linear discontinuous between elements velocity and quadratic continuous pressure); (c) an interface‐capturing scheme based on compressive control volume advection methods and high‐order finite element interpolation methods; (d) a time stepping method that allows use of relatively large time step sizes; and (e) application of anisotropic mesh adaptivity to focus the numerical resolution around the interfaces and other areas of important dynamics. This modelling approach is applied to a series of pure advection problems with interfaces as well as to the simulation of the standard computational fluid dynamics benchmark test cases of a collapsing water column under gravitational forces (in two and three dimensions) and sloshing water in a tank. Two more test cases are undertaken in order to demonstrate the many‐material and compressibility modelling capabilities of the approach. Numerical simulations are performed on coarse unstructured meshes to demonstrate the potential of the methods described here to capture complex dynamics in multiphase flows. Copyright © 2015 John Wiley & Sons, Ltd. 相似文献
43.
Haroldo G. Santos Túlio A. M. Toffolo Rafael A. M. Gomes Sabir Ribas 《Annals of Operations Research》2016,239(1):225-251
This work presents integer programming techniques to tackle the problem of the International Nurse Rostering Competition. Starting from a compact and monolithic formulation in which the current generation of solvers performs poorly, improved cut generation strategies and primal heuristics are proposed and evaluated. A large number of computational experiments with these techniques produced the following results: the optimality of the vast majority of instances was proved, the best known solutions were improved by up to 15 % and strong dual bounds were obtained. In the spirit of reproducible science, all code was implemented using the Computational Infrastructure for Operations Research. 相似文献
44.
Adilson Beatriz Roberto da Silva Gomes Mauricio Gomes Constantino Gil Valdo José da Silva Kleber Thiago de Oliveira 《Tetrahedron letters》2014
A bicyclo[6.2.1]undecane model compound of the core structure of the biologically active furanoheliangolide sesquiterpene was synthesized. This new and short route was developed by using a solvent-free Diels–Alder reaction between cyclopentadiene and 3-nitro-2-cyclohexenone, followed by simple transformations. Theoretical calculations were performed in order to understand reactivity aspects of the cycloaddition. 相似文献
45.
A systematic study of glycopeptide esterification for the semi‐quantitative determination of sialylation in antibodies 下载免费PDF全文
46.
Rapid and sensitive ultra‐high‐pressure liquid chromatography method for quantification of antichagasic benznidazole in plasma: application in a preclinical pharmacokinetic study 下载免费PDF全文
Marcelo Gomes Davanço Michel Leandro de Campos Rosângela Gonçalves Peccinini 《Biomedical chromatography : BMC》2015,29(7):1008-1015
Benznidazole (BNZ) and nifurtimox are the only drugs available for treating Chagas disease. In this work, we validated a bioanalytical method for the quantification of BNZ in plasma aimed at improving sensitivity and time of analysis compared with the assays already published. Furthermore, we demonstrated the application of the method in a preclinical pharmacokinetic study after administration of a single oral dose of BNZ in Wistar rats. A Waters® Acquity UHPLC system equipped with a UV–vis detector was employed. The method was established using an Acquity® UHPLC HSS SB C18 protected by an Acquity® UHPLC HSS SB C18 VanGuard guard column and detection at 324 nm. The mobile phase consisted of ultrapure water–acetonitrile (65:35), and elution was isocratic. The mobile phase flow rate was 0.55 mL/min, the volume of injection was 1 μL, and the run time was just 2 min. The samples were kept at 25°C until injection and the column at 45°C for the chromatographic separation. The sample preparation was performed by a rapid protein precipitation with acetonitrile. The linear concentration range was 0.15–20 µg/mL. The pharmacokinetic parameters of BNZ in rats were determined and the method was considered sensitive, fast and suitable for application in pharmacokinetic studies. Copyright © 2014 John Wiley & Sons, Ltd. 相似文献
47.
Gomes João Pedro Agra Mourão Eduard David Simões dos Anjos Janaina Versiani de Alencar Filho Edilson Beserra 《Structural chemistry》2020,31(6):2501-2512
Structural Chemistry - In this paper, we present a quantitative structure–activity relationships modelling for two series of heterocyclic synthetic compounds with larvicidal activity against... 相似文献
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Optimal orientation angles and aspect ratios of a grain are presented for the attenuation of a longitudinal pressure wave
by elastic stresses that arise from the rotation of a grain. A computer program in C++ allows the grain to be a two-dimensional
ellipse of several orientations with respect to the incoming load. The program also varies the aspect ratio of the grain.
The induced elastic stresses from the rotation of the grain are calculated with complex variable methods that do not require
meshes and elements. Low aspect ratios of 5/3, 10/7 and 5/4 were particularly effective in halting the stress from the pressure
wave when the major axis of the grain was tilted between 15° and 45° and again above 70° with respect to the line of the incoming
load. Attenuation was found to be more sensitive to grain orientation than to aspect ratio. The conclusion is supported by
numerous switches in the extent of wave blockage over small angular variations in the orientation of the grain. 相似文献