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11.
Dr. Li Di Prof. Per Artursson Dr. Alex Avdeef Prof. Leslie Z. Benet Prof. J. Brian Houston Dr. Manfred Kansy Edward H. Kerns Prof. Hans Lennernäs Dr. Dennis A. Smith Prof. Kiyohiko Sugano 《ChemMedChem》2020,15(20):1862-1874
Passive permeability is a key property in drug disposition and delivery. It is critical for gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance mechanisms and drug-drug interactions. Passive diffusion rate is translatable across tissues and animal species, while the extent of absorption is dependent on drug properties, as well as in vivo physiology/pathophysiology. Design principles have been developed to guide medicinal chemistry to enhance absorption, which combine the balance of aqueous solubility, permeability and the sometimes unfavorable compound characteristic demanded by the target. Permeability assays have been implemented that enable rapid development of structure-permeability relationships for absorption improvement. Future advances in assay development to reduce nonspecific binding and improve mass balance will enable more accurately measurement of passive permeability. Design principles that integrate potency, selectivity, passive permeability and other ADMET properties facilitate rapid advancement of successful drug candidates to patients. 相似文献
12.
Based on the phase transformation theories, especially the T0 concept of bainite transformation, alloy optimisation of bainitic steel with carbides has been carried out aiming at the produce of plastic mould with large cross-section. The effect of manganese and silicon on proeutectoid ferrite and bainite transformation is explored by dilatometric analysis, XRD and different microscopy techniques. The results show that after the alloy optimisation, the transformation of proeutectoid ferrite is suppressed and when the cooling rate is lower than 0·1°C?s??1, the new lower bainite transformation appears by decreasing carbon capacity of austenite and promoting carbide precipitation. Industrial production proves that the optimised alloy SDP1 can meet the demand for the plastic mould with the thickness of 1050?mm. 相似文献
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Popular biorthogonal wavelet filters via a lifting scheme and its application in image compression 总被引:2,自引:0,他引:2
Cheng L. Liang D.L. Zhang Z.H. 《Vision, Image and Signal Processing, IEE Proceedings -》2003,150(4):227-232
A technique using a lifting scheme is presented for constructing compactly supported wavelets whose coefficients are composed of free variables locating in an interval. An efficient approach-based wavelet for image compression is developed by selecting the coefficients of the 9-7 wavelet filter and associated lifting scheme. Furthermore, the rationalised coefficients wavelet filter that can be implemented with simple integer arithmetic is achieved and its characteristic is close to the well known original irrational coefficients 9-7 wavelet filters developed by A. Cohen et al. (Commun. Pure Appl. Maths., vol.45, no.1, p.485-560, 1992). To reduce the computational cost of image coding applications further, an acceleration technique is proposed for the lifting steps. Software and hardware simulations show that the new method has very low complexity, and simultaneously preserves the high quality of the compressed image. 相似文献
15.
In colloidal suspensions of silica, particles undergo constant collisions. By controlling various parameters, the repulsive barrier can be reduced, thereby substantially increasing the number of collision‐induced dimerization events. Xia and co‐workers report on p. 1627 that the dimers could be arrested and then permanently fixed by introducing a small amount of fresh tetraethylorthosilicate into the colloidal suspension, with monodisperse dimer yields of up to 50 %. This yield could be increased to 80 % by centrifugation in a density gradient medium. When fresh tetraethylorthosilicate is introduced into a colloidal suspension of silica spheres, it hydrolyzes and condenses in situ to arrest and fix the dimers resulting from constant collisions between the spheres. By optimizing the experimental parameters (including the length of aging time) and the diameter of the silica spheres, as well as the concentrations of counterions, water, and ammonia, it is possible to routinely produce monodisperse dimers with a yield as high as 50 %. When combined with centrifugation using a density gradient medium, the yield of such dimers could be further increased to 80 %. It is believed that this method will provide a simple and versatile approach to the high‐volume production of dimers from spherical colloids composed of different materials. These dimers may find widespread use in a range of applications such as fabrication of photonic crystals and fundamental studies related to colloidal science. 相似文献
16.
The vapour phase compositions of a series of pack powder mixtures containing elemental Al and Hf or W powders as depositing sources and CrCl3·6H2O or AlF3or CrF3as activators were analysed in an attempt to further develop the pack cementation process to codeposit Al and Hf or W to form diffusion coatings on nickel base superalloys. The results suggested that Al could be codeposited with Hf, but not with W, from the vapour phase. Compared with both AlF3and CrF3, CrCl3·6H2O has been shown to be a more suitable activator for codepositing Al with Hf. The optimum coating temperature was identified to be in the range of 1050°C to 1150°C. Based on the thermochemical analysis, a series of coating deposition studies were undertaken, which confirmed that codeposition of Al and Hf could be achieved at a deposition temperature of 1100°C in the CrCl3·6H2O activated packs containing elemental Al and Hf powders. The coating obtained had a multilayer structure consisting of a Ni7Hf6Al16top layer and a NiAl layer underneath, followed by a diffusion zone, which revealed that the coating was formed by the outward Ni diffusion. It is suggested that the compositions suitable for codeposition of Al and Hf could be effectively identified by comparing the vapour pressures of HfCl4and HfCl3with that of AlCl in the packs activated by chloride salts. It has also been experimentally demonstrated that, although W could not be deposited from the vapour phase, a high volume of fine W particles can be entrapped into the outer NiAl coating layer formed by the outward Ni diffusion using a modified pack configuration. This leads to the formation of a composite coating layer with W particles evenly distributed in a matrix of NiAl. It is suggested that this modified pack process could be similarly applied to develop nickel aluminide coatings containing other refractory metals that may not be codeposited with Al from the vapour phase. 相似文献
17.
Several kinds of waveguide components such as curved waveguide bends, arbitrary angle waveguide bends and T-junctions have been analyzed with boundary element method in this paper. A new discretization method for the boundary element method to solve the waveguide discontinuities has been given. The numerical results obtained agree well with the experimental results and numerical results in other literature. Especially, the scattering characteristics of Forded E-, H-plane T-junctions in 3mm band have been analyzed using boundary element method and the calculation results are presented. 相似文献
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19.
H. L. Du S. R. Rose Z. D. Xiang P. K. Datta X. Y. Li 《Materialwissenschaft und Werkstofftechnik》2003,34(4):421-426
The oxidation/sulphidation behaviour of a Ti‐46.7Al‐1.9W‐0.5Si alloy with a TiAl3 diffusion coating was studied in an environment of H2/H2S/H2O at 850oC. The kinetic results demonstrate that the TiAl3 coating significantly increased the high temperature corrosion resistance of Ti‐46.7Al‐1.9W‐0.5Si. The SEM, EDX, XRD and TEM analysis reveals that the formation of an Al2O3 scale on the surface of the TiAl3‐coated sample was responsible for the enhancement of the corroison resistance. The Ti‐46.7Al‐1.9W‐0.5Si alloy was also modified by Nb ion implantation. The Nb ion implanted and as received sampels were subjected to cyclic oxidation in an open air at 800oC. The Nb ion implantation not only increased the oxidation resistance but also substantially improved the adhesion of scale to the substrate. 相似文献
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