Improvement in the Physicochemical Properties of Ketoconazole through Complexation with Cyclodextrin Derivatives

Highly-soluble cyclodextrin derivatives, such as hydroxypropyl-010l9465u/xxlarge946.gif" alt="beta" align="MIDDLE" BORDER="0">-cyclodextrin(HP-010l9465u/xxlarge946.gif" alt="beta" align="MIDDLE" BORDER="0">-CD) and methyl-010l9465u/xxlarge946.gif" alt="beta" align="MIDDLE" BORDER="0">-cyclodextrin (MEB), were tested as solubilizingagents for ketoconazole, with the aim of improving the physicochemical andbiopharmaceutical properties of this lipophilic imidazole antifungal agent. Productswere prepared in four molecular ratios by physical mixing, kneading and spray-dryingmethods. The kneaded products in a ratio of 1:2 and the spray-dried products exhibitedthe highest dissolution rates. The phase solubility diagrams of ketoconazole with thesecyclodextrins at 25 °C in water and in simulated intestinal medium wereconstructed. A solubility diagram of A_L type was obtained with HP-010l9465u/xxlarge946.gif" alt="beta" align="MIDDLE" BORDER="0">-CD, and one of A_P type with MEB. The complexes were characterized by thermal methods(DSC, TG, DTG and DTA). Multicomponent systems were prepared with tartaric acid.The effects of water-soluble polymers, e.g., polyvinylpyrrolidone, on the aqueous solubility of ketoconazole were investigated. Particle size distribution, surface area, partition coefficient, heat of dissolution and wettability studies were also carried out. The formation of inclusion complexes was observed by means of thermoanalytical studies.     

Intra-Nuclear Cascade (INC) code for simulation of meson photoproduction in nuclei

η meson photoproduction in the ¹⁴N nucleus was studied using simulations done with INC (Intra-Nuclear Cascade) code. The probability for mesons and nucleons to escape the nucleus on different steps of the reaction was evaluated. These results predict the possibility of studying elastic and inelastic η meson interactions with intra-nuclear nucleons using the recoil proton as a tag for the case of slow η meson and fast recoil proton.     

Effect of size and shape controlled biogenic synthesis of gold nanoparticles and their mode of interactions against food borne bacterial pathogens

In this study, size and shape controlled biogenic synthesis of gold nanoparticles and their antibacterial activity against food borne bacterial pathogens were investigated. Synthesis of gold nanoparticles was carried out using two medicinally important plants Cucurbita pepo and Malva crispa and the size and shape of the nanoparticles were controlled by altering various parameters in the reaction medium. Results obtained from UV–Vis, FE-SEM, EDS and HR-TEM analyses supported the nanoparticles formation. FT-IR analysis confirmed the presence of biomolecules in the plant leaves extracts responsible for reducing and capping agents. Interestingly, the plant extract synthesized gold nanoparticles showed effective inhibition zone against Gram-positive and Gram-negative pathogens. The minimum inhibitory concentration (MIC) of synthesized gold nanoparticles at 400 μg/ml concentration showed effective inhibitory activity against Escherichia coli and Listeria monocytogenes. Conductivity of the medium continuously increased during the nanoparticles treatment with food borne bacterial pathogens resulting in indirect indication of the disruption of bacterial cell membranes. In addition, mode of interactions of gold nanoparticles against food borne bacterial pathogens was demonstrated using Bio-TEM analysis which is clear evident for the disruption of bacterial cell membranes.     

基于TM010模介质谐振腔的小型化腔体滤波器

现用于4G基站的介质腔体滤波器都采用TE_01δ模介质谐振腔,虽然其品质因数Q值很高,但体积较大。为了小型化介质腔体滤波器,创新性地使用了TM₀₁₀模介质谐振腔,虽然其Q值比较低,但同样能满足高带外抑制的要求。对TM₀₁₀模介质谐振腔的端口耦合和两腔之间的磁耦合、电耦合进行分析研究,创新性地使用了介质窗的形式产生电耦合,避免了使用飞杆,易于加工,降低制造成本。最后设计了一个8腔TM₀₁₀模准椭圆函数介质腔体带通滤波器,在通带(TD-LTE频带,2570~2620 MHz)两端分别设计两个传输零点以提高带外抑制。调试结果表明,TM₀₁₀模介质腔体滤波器不仅能满足低插损、高带外抑制的要求,而且其体积大幅度缩小。     

Transformation of the Wiener measure under non-invertible shifts

Summary In this paper we consider the transformation of measure induced by a not-necessarily-invertible perturbation of the identity. The Radon-Nikodym density for the image of the Wiener measure and the associated Girsanov-type density are derived. An application of these results yields an extension of the degree theorem.     

Simulation and measurement of the resonant Schottky pickup

A resonant Schottky pickup with high sensitivity, built by GSI, will be used for nuclear mass and lifetime measurement at CSRe. The basic concepts of Schottky noise signals, a brief introduction of the geometry of the detector, the transient response of the detector, and MAFIA simulated and perturbation measured results of characteristics are presented in this paper. The resonant frequency of the pickup is about 243 MHz and can be slightly changed at a range of 3 MHz. The unloaded quality factor is about 1072 and the shunt impedance is 76 kΩ. The measured results of the characteristics are in agreement with the MAFIA simulations.     

Catalytic asymmetric synthesis of Leukotriene B4

Leukotriene B₄ 1 was prepared from two chiral synthons 8 and 14. The chiral secondary alcohols of 8 and 14 were constructed by BINOL/Ti(OiPr)₄ catalyzed enantioselective alkynylzinc addition to aldehydes.     

Density Functional Study on Adsorption of NO on AuSe (010) Surface

NO molecule adsorption on (010) surface of gold selenide (AuSe) has been studied with a periodic slab model by means of the GGA‐PW91 exchange‐correlation functional within the framework of density functional theory (DFT). Four different on‐top adsorption sites Au(1), Au(2), Se(1) and Se(2) were considered for α‐AuSe and three on‐top adsorption sites Au(1), Au(2) and Se(1) for β‐AuSe. N‐end and O‐end adsorptions of NO were investigated for the above sites. The results show that N‐end adsorptions are preferred for α‐ and β‐AuSe and O‐end adsorptions are not feasible and thought as physisorption with the weak adsorption energies from 6.0 to 10.8 kJ/mol. For the N‐end adsorptions on α‐ and β‐AuSe (010) surfaces, Au(2) sites are most favorable with the adsorption energies 89.0 and 78.0 kJ/mol for α‐ and β‐AuSe, respectively. However, the adsorptions at Au1 sites are very weak with the adsorption energies of 27.8 and 7.5 kJ/mol, respectively. In case of the adsorption of N‐down orientations of NO at Se sites for α‐ and β‐AuSe (010) surfaces, the adsorption activities of Se(1) and Se(2) sites on the α‐AuSe (010) surface and Se(1) site on the β‐AuSe (010) surface are almost the same with the adsorption energies 51.2, 52.7 and 49.2 kJ/mol. The geometric optimizations for adsorption configurations were calculated along with accounting for stretching frequency and density of states in our work.     

Catalytic asymmetric syntheses of (−)-oudemanisin A and its diastereomer

The first asymmetric catalytic synthesis of (?)-oudemanisin A 1a and its diastereomer 1b has been achieved. The key steps of our strategy involved the asymmetric alkynylation of an unsaturated aliphatic aldehyde catalyzed by Trost’s ProPhenol ligand, chemoselective oxidation of the olefinic diol, base-induced ring opening of the lactone, and acylation–alkylation of the ester.     

Copper(II) complexes of 2-(pyridine-2-yl)imidazolidine-4-thione derivatives for asymmetric Henry reactions

The preparation of a new series of 2-(pyridine-2-yl)imidazolidine-4-thione derivatives is described. Their corresponding copper(II) complexes were found to be highly enantioselective catalysts for asymmetric Henry reactions (up to 98% ee). Immobilization of these complexes by anchoring onto Merrifield? resin with respect to their use as recyclable catalysts was subsequently performed. The heterogeneous catalysts prepared in this way were tested in the asymmetric Henry reactions and showed high catalytic activity; they can be easily recycled, although their enantioselectivities were only moderate (～50% ee).