Anti-fibrosis attributes: UHPLC-MS/MS-based pharmacokinetics profiling of a novel autotaxin inhibitor with excellent in vivo efficacy in rat

3,4-Difluorobenzyl(1-ethyl-5-(4-((4-hydroxypiperidin-1-yl)-methyl)thiazol-2-yl)-1H-indol-3-yl)carbamate (NAI59), a small molecule with outstanding therapeutic effectiveness to anti-pulmonary fibrosis, was developed as an autotaxin inhibitor candidate compound. To evaluate the pharmacokinetics and plasma protein binding of NAI59, a UPLC–MS/MS method was developed to quantify NAI59 in plasma and phosphate-buffered saline. The calibration curve linearity ranged from 9.95 to 1990.00 ng/mL in plasma. The accuracy was −6.8 to 5.9%, and the intra- and inter-day precision was within 15%. The matrix effect and recovery, as well as dilution integrity, were within the criteria. The chromatographic and mass spectrometric conditions were also feasible to determine phosphate-buffered saline samples, and it has been proved that this method exhibits good precision and accuracy in the range of 9.95–497.50 ng/mL in phosphate-buffered saline. This study is the first to determine the pharmacokinetics, absolute bioavailability, and plasma protein binding of NAI59 in rats using this established method. Therefore, the pharmacokinetic profiles of NAI59 showed a dose-dependent relationship after oral administration, and the absolute bioavailability in rats was 6.3%. In addition, the results of protein binding showed that the combining capacity of NAI59 with plasma protein attained 90% and increased with the increase in drug concentration.     

疏水缔合悬浮稳定剂的合成及其对固井水泥浆稠度和悬浮稳定性的影响

针对大温差条件下固井水泥浆在固井过程中可能存在的悬浮失稳问题，本研究采用水溶液自由基聚合法来合成具有疏水缔合结构的聚合物作为悬浮稳定剂(PAAN)。通过红外光谱仪、凝胶渗透色谱仪、热重分析仪、高温流变仪、SEM、紫外分光光度计等表征PAAN的结构，发现PAAN随温度升高，形成分子间疏水缔合网状结构，保证了体系的粘度，从而起到有效的悬浮稳定作用。研究发现在40~110 ℃下，0.6%加量的PAAN可以保证固化后的水泥石柱顶部和底部密度差<0.01 g/cm³，且水泥浆稠化时间基本不变，表明PAAN可以保证水泥浆体系具有良好的悬浮稳定效果，且对水泥浆的其他性能无不良影响。     

砂土串囊式充气锚杆承载力的研究

在砂土地层中,串囊式充气锚杆的研究还比较少,其承载特性及受力机理尚不明确。本文基于莫尔-库仑模型和Vesic圆孔扩张理论法,分别对圆柱体、球体、组合体、椭球体假设下的串囊式充气锚杆的扩大段进行计算分析。并将计算结果与试验得到的实测值进行对比。结果表明:四种形状假设中椭球体的形状假设理论值与实测值的误差最小,仅为8.35%。通过拟合试验数据,并引入与端阻力和侧摩阻力有关的两个系数对承载力公式进行修正,得到了抗拔承载力的经验公式。     

Space-Confined Atomic Clusters Catalyze Superassembly of Silicon Nanodots within Carbon Frameworks for Use in Lithium-Ion Batteries

Incorporating nanoscale Si into a carbon matrix with high dispersity is desirable for the preparation of lithium-ion batteries (LIBs) but remains challenging. A space-confined catalytic strategy is proposed for direct superassembly of Si nanodots within a carbon (Si NDs⊂C) framework by copyrolysis of triphenyltin hydride (TPT) and diphenylsilane (DPS), where Sn atomic clusters created from TPT pyrolysis serve as the catalyst for DPS pyrolysis and Si catalytic growth. The use of Sn atomic cluster catalysts alters the reaction pathway to avoid SiC generation and enable formation of Si NDs with reduced dimensions. A typical Si NDs⊂C framework demonstrates a remarkable comprehensive performance comparable to other Si-based high-performance half LIBs, and higher energy densities compared to commercial full LIBs, as a consequence of the high dispersity of Si NDs with low lithiation stress. Supported by mechanic simulations, this study paves the way for construction of Si/C composites suitable for applications in future energy technologies.     

Integral Representations of the Large and Little Schröder Numbers

In the paper, the authors establish several integral representations for the generating functions of the large and little Schröder numbers and for the large and little Schröder numbers.     

Mesoscopic Modeling of Capillarity-Induced Two-Phase Transport in a Microfluidic Porous Structure

Mesoscopic modeling at the pore scale offers great promise in exploring the underlying structure transport performance of flow through porous media. The present work studies the fluid flow subjected to capillarity-induced resonance in porous media characterized by different porous structure and wettability. The effects of porosity and wettability on the displacement behavior of the fluid flow through porous media are discussed. The results are presented in the form of temporal evolution of percentage saturation and displacement of the fluid front through porous media. The present study reveals that the vibration in the form of acoustic excitation could be significant in the mobilization of fluid through the porous media. The dependence of displacement of the fluid on physicochemical parameters like wettability of the surface, frequency along with the porosity is analyzed. It was observed that the mean displacement of the fluid is more in the case of invading fluid with wetting phase where the driving force strength is not so dominant.     

Three-term polynomial progressions in subsets of finite fields

We prove that the group of diffeomorphisms of the interval [0, 1] contains surface groups whose action on (0, 1) has no global fix point and such that only countably many points of the interval (0, 1) have non-trivial stabiliser.     

Bi-2223/Ag异质结的光生电压效应研究

在50 ～ 340 K不同温度下,利用紫色激光(λ=405 nm)对银/铋锶钙铜氧2223异质结界面进行辐照,观测到明显的光生电压效应,发现光生电压的极性分别在超导转变温度TC与320 K附近发生了反转,排除了激光产生的热电势是产生光生电压的原因,分析表明银/铋锶钙铜氧2223异质结界面处存在内建电场:光生电压由异质结界面处的内建电场分离光生电子-空穴对产生的.超导转变温度TC之下以及320 K以上,内建电场方向从超导体指向金属电极;超导转变温度TC与反向温度320 K之间,内建电场从金属指向超导体.