970 resultados para Drug Stability
Resumo:
Glasses in the x(BaO-TiO2)-B2O3 (x = 0.25, 0.5, 0.75, and 1 mol.) system were fabricated via the conventional melt-quenching technique. Thermal stability and glass-forming ability as determined by differential thermal analysis (DTA) were found to increase with increasing BaO-TiO2 (BT) content. However, there was no noticeable change in the glass transition temperature (T-g). This was attributed to the active participation of TiO2 in the network formation especially at higher BT contents via the conversion of the TiO6 structural units into TiO4 units, which increased the connectivity and resulted in an increase in crystallization temperature. Dielectric and optical properties at room temperature were studied for all the glasses under investigation. Interestingly, these glasses were found to be hydrophobic. The results obtained were correlated with different structural units and their connectivity in the glasses.
Resumo:
By using the lower-bound finite element limit analysis, the stability of a long unsupported circular tunnel has been examined with an inclusion of seismic body forces. The numerical results have been presented in terms of a non-dimensional stability number (gamma H/c) which is plotted as a function of horizontal seismic earth pressure coefficient (k (h)) for different combinations of H/D and I center dot; where (1) H is the depth of the crest of the tunnel from ground surface, (2) D is the diameter of the tunnel, (3) k (h) is the earthquake acceleration coefficient and (4) gamma, c and I center dot define unit weight, cohesion and internal friction angle of soil mass, respectively. The stability numbers have been found to decrease continuously with an increase in k (h). With an inclusion of k (h), the plastic zone around the periphery of the tunnel becomes asymmetric. As compared to the results reported in the literature, the present analysis provides a little lower estimate of the stability numbers. The numerical results obtained would be useful for examining the stability of unsupported tunnel under seismic forces.
Resumo:
Exponential compact higher-order schemes have been developed for unsteady convection-diffusion equation (CDE). One of the developed scheme is sixth-order accurate which is conditionally stable for the Peclet number 0 <= Pe <= 2.8 and the other is fourth-order accurate which is unconditionally stable. Schemes for two-dimensional (2D) problems are made to use alternate direction implicit (ADI) algorithm. Example problems are solved and the numerical solutions are compared with the analytical solutions for each case.
Resumo:
In the present investigation an attempt has been made to develop a new co-polymeric material for controlled release tablet formulations. The acrylamide grafting was successfully performed on the backbone of sago starch. The modified starch was tested for acute toxicity and drug-excipient compatibility study. The grafted material was used in making of controlled release tablets of lamivudine. The formulations were evaluated for physical characteristics such as hardness, friability, %drug content and weight variations. The in vitro release study showed that the optimized formulation exhibited highest correlation (R) value in case of Higuchi model and the release mechanism of the optimized formulation predominantly exhibited combination of diffusion and erosion process. There was a significant difference in the pharmacokinetic parameters (T-max, C-max, AUC, V-d, T-1/2 and MDT) of the optimized formulation as compared to the marketed conventional tablet Lamivir (R) was observed. The pharmacokinetics parameters were showed controlled pattern and better bioavailability. The optimized formulation exhibited good stability and release profile at the accelerated stability conditions. (c) 2013 Elsevier B.V. All rights reserved.
Resumo:
The most common valencies associated with K and O atoms are 1+ and 2-. As a result, one expects K2O to be the oxide of potassium which is the most stable with respect to its constituents. Calculating the formation energy within electronic structure calculations using hybrid functionals, one finds that K2O2 has the largest formation energy, implying the largest stability of this oxide of potassium with respect to its constituents. This is traced to the presence of oxygen dimers in the K2O2 structure which interact strongly resulting in a larger formation energy compared to the more ionic K2O.
Resumo:
Curcumin has shown promising therapeutic utilities for many diseases, including cancer; however, its clinical application is severely limited because of its poor stability under physiological conditions. Here we find that curcumin also loses its activity instantaneously in a reducing environment. Curcumin can exist in solution as a tautomeric mixture of keto and enol forms, and the enol form was found to be responsible for the rapid degradation of the compound. To increase the stability of curcumin, several analogues were synthesized in which the diketone moiety of curcumin was replaced by isoxazole (compound 2) and pyrazole (compound 3) groups. Isoxazole and pyrazole curcumins were found to be extremely stable at physiological pH, in addition to reducing atmosphere, and they can kill cancer cells under serum-depleted condition. Using molecular modeling, we found that both compounds 2 and 3 could dock to the same site of tubulin as the parent molecule, curcumin. Interestingly, compounds 2 and 3 also show better free radical scavenging activity than curcumin. Altogether, these results strongly suggest that compounds 2 and 3 could be good replacements for curcumin in future drug development.
Resumo:
Ni49.4Ti38.6Hf12 shape memory alloy has been characterized for structure, microstructure and transformation temperatures. The microstructure of the as-cast sample consists of B19' and R-phases, and (Ti,Hf)(2)Ni precipitate phase along the grain boundaries in the form of dendrites. The microstructure of the solution treated sample contains only B19' martensite phase, whereas a second heat treatment after solutionizing results in reappearance of the R-phase and the (Ti,Hf)(2)Ni grain boundary precipitate phase in the microstructure. A detailed microstructural examination shows the presence of precipitates having both coherent and incoherent interface with the matrix, the type of interface being dictated by the crystallographic orientation of the matrix phase. The present study shows that the (Ti,Hf)(2)Ni precipitates having coherent interface with the matrix, drive the formation of the R-phase in the microstructure. (C) 2013 Elsevier Ltd. All rights reserved.
Resumo:
We report a simple method to fabricate multifunctional polyelectrolyte thin films to load and deliver the therapeutic drugs. The multilayer thin films were assembled by the electrostatic adsorption of poly (allylamine hydrochloride) (PAH) and dextran sulfate (DS). The silver nanoparticles (Ag NPs) biosynthesized from novel Hybanthus enneaspermus leaf extract as the reducing agent were successfully incorporated into the film. The biosynthesized Ag NPs showed excellent antimicrobial activity against the range of enteropathogens, which could be significantly enhanced when used with commercial antibiotics. The assembled silver nano composite multilayer films showed rupture and deformation when they are exposed to laser. The Ag NPs act as an energy absorption center, locally heat up the film and rupture it under laser treatment. The antibacterial drug, moxifloxacin hydrochloride (MH) was successfully loaded into the multilayer films. The total amount of MH release observed was about 63% which increased to 85% when subjected to laser light exposure. Thus, the polyelectrolyte thin film reported in our study has significant potential in the field of remote activated drug delivery, antibacterial coatings and wound dressings. (C) 2013 Elsevier B.V. All rights reserved.
Resumo:
We demonstrate a nanoparticle loading protocol to develop a transparent, multifunctional polyelectrolyte multilayer film for externally activated drug and protein delivery. The composite film was designed by alternate adsorption of poly(allylamine hydrochloride) (PAH) and dextran sulfate (DS) on a glass substrate followed by nanoparticle synthesis through a polyol reduction method. The films showed a uniform distribution of spherical silver nanoparticles with an average diameter of 50 +/- 20 nm, which increased to 80 +/- 20 nm when the AgNO3 concentration was increased from 25 to 50 mM. The porous and supramolecular structure of the polyelectrolyte multilayer film was used to immobilize ciprofloxacin hydrochloride (CH) and bovine serum albumin (BSA) within the polymeric network of the film. When exposed to external triggers such as ultrasonication and laser light the loaded films were ruptured and released the loaded BSA and CH. The release of CH is faster than that of BSA due to a higher diffusion rate. Circular dichroism measurements confirmed that there was no significant change in the conformation of released BSA in comparison with native BSA. The fabricated films showed significant antibacterial activity against the bacterial pathogen Staphylococcus aureus. Applications envisioned for such drug-loaded films include drug and vaccine delivery through the transdermal route, antimicrobial or anti-inflammatory coatings on implants and drug-releasing coatings for stents. (C) 2013 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.
Resumo:
In aqueous binary mixtures, amphiphilic solutes such as dimethylsulfoxide (DMSO), ethanol, tertbutyl alcohol (TBA), etc., are known to form aggregates (or large clusters) at small to intermediate solute concentrations. These aggregates are transient in nature. Although the system remains homogeneous on macroscopic length and time scales, the microheterogeneous aggregation may profoundly affect the properties of the mixture in several distinct ways, particularly if the survival times of the aggregates are longer than density relaxation times of the binary liquid. Here we propose a theoretical scheme to quantify the lifetime and thus the stability of these microheterogeneous clusters, and apply the scheme to calculate the same for water-ethanol, water-DMSO, and water-TBA mixtures. We show that the lifetime of these clusters can range from less than a picosecond (ps) for ethanol clusters to few tens of ps for DMSO and TBA clusters. This helps explaining the absence of a strong composition dependent anomaly in water-ethanol mixtures but the presence of the same in water-DMSO and water-TBA mixtures. (C) 2013 AIP Publishing LLC.
Resumo:
Objectives: The ability to target conventional drugs efficiently inside cells to kill intraphagosomal bacteria has been a major hurdle in treatment of infective diseases. We aimed to develop an efficient drug delivery system for combating infection caused by Salmonella, a well-known intracellular and intraphagosomal pathogen. Chitosan dextran sulphate (CD) nanocapsules were assessed for their efficiency in delivering drugs against Salmonella. Methods: The CD nanocapsules were prepared using the layer-by-layer method and loaded with ciprofloxacin or ceftriaxone. Antibiotic-loaded nanocapsules were analysed in vitro for their ability to enter epithelial and macrophage cells to kill Salmonella. In vivo pharmacokinetics and organ distribution studies were performed to check the efficiency of the delivery system. The in vivo antibacterial activity of free antibiotic and antibiotic loaded into nanocapsules was tested in a murine salmonellosis model. Results: In vitro and in vivo experiments showed that this delivery system can be used effectively to clear Salmonella infection, CD nanocapsules were successfully employed for efficient targeting and killing of the intracellular pathogen at a dosage significantly lower than that of the free antibiotic. The increased retention time of ciprofloxacin in the blood and organs when it was delivered by CD nanocapsules compared with the conventional routes of administration may be the reason underlying the requirement for a reduced dosage and frequency of antibiotic administration. Conclusions: CD nanocapsules can be used as an efficient drug delivery system to treat intraphagosomal pathogens, especially Salmonella infection, This delivery system might be used effectively for other vacuolar pathogens including Mycobacteria, Brucella and Legionella.
Resumo:
This paper describes an ab initio design and development of a novel Fiber Bragg Grating (FBG) sensor based strain sensing plate for the measurement of plantar strain distribution in human foot. The primary aim of this work is to study the feasibility of usage of FBG sensors in the measurement of plantar strain in the foot; in particular, to spatially resolve the strain distribution in the foot at different regions such as fore-foot, mid-foot and hind-foot. This study also provides a method to quantify and compare relative postural stability of different subjects under test; in addition, traditional accelerometers have been used to record the movements of center of gravity (second lumbar vertebra) of the subject and the results obtained have been compared against the outcome of the postural stability studies undertaken using the developed FBG plantar strain sensing plate. (C) 2013 Elsevier Ltd. All rights reserved.
Resumo:
The stability of two long unsupported circular parallel tunnels aligned horizontally in fully cohesive and cohesive-frictional soils has been determined. An upper bound limit analysis in combination with finite elements and linear programming is employed to perform the analysis. For different clear spacing (S) between the tunnels, the stability of tunnels is expressed in terms of a non-dimensional stability number (gamma H-max/c); where H is tunnel cover, c refers to soil cohesion, and gamma(max) is maximum unit weight of soil mass which the tunnels can bear without any collapse. The variation of the stability number with tunnels' spacing has been established for different combinations of H/D, m and phi; where D refers to diameter of each tunnel, phi is the internal friction angle of soil and m accounts for the rate at which the cohesion increases linearly with depth. The stability number reduces continuously with a decrease in the spacing between the tunnels. The optimum spacing (S-opt) between the two tunnels required to eliminate the interference effect increases with (i) an increase in H/D and (ii) a decrease in the values of both m and phi. The value of S-opt lies approximately in a range of 1.5D-3.5D with H/D = 1 and 7D-12D with H/D = 7. The results from the analysis compare reasonably well with the different solutions reported in literature. (C) 2013 Elsevier Ltd. All rights reserved.
Resumo:
Aptamers, and the selection process known as Systematic Evolution of Ligands by Exponential Enrichment (SELEX) used to generate them, were first described more than twenty years ago. Since then, there have been numerous modifications to the selection procedures. This review discusses the use of modified bases as a means of enhancing serum stability and producing effective therapeutic tools, as well as functionalising these nucleic acids to be used as potential diagnostic agents.
Resumo:
A wobble instability is one of the major problems of a three-wheeled vehicle commonly used in India, and these instabilities are of great interest to industry and academia. In this paper, we studied this instability using a multi-body dynamic model and with experiments conducted on a prototype three-wheeled vehicle on a test track. The multi-body dynamic model of a three-wheeled vehicle is developed using the commercial software ADAMS/Car. In an initial model, all components including main structures such as the frame, the steering column and the rear forks are assumed to be rigid bodies. A linear eigenvalue analysis, which is carried out at different speeds, reveals a mode that has predominantly a steering oscillation, also called a wobble mode, with a frequency of around 5-6Hz. The analysis results shows that the damping of this mode is low but positive up to the maximum speed of the three-wheeled vehicle. However, the experimental study shows that the mode is unstable at speeds below 8.33m/s. To predict and study this instability in detail, a more refined model of the three-wheeled vehicle, with flexibilities of three important bodies, was constructed in ADAMS/Car. With flexible bodies, three modes of a steering oscillation were observed. Two of these are well damped and the other is lightly damped with negative damping at lower speeds. Simulation results with flexibility incorporated show a good match with the instability observed in the experimental studies. Further, we investigated the effect of each flexible body and found that the flexibility of the steering column is the major contributor for wobble instability and is similar to the wheel shimmy problem in aircraft.