In vitro evaluation and in vivo performance of lyophilized gliclazide

Enhancement of the dissolution rate of the poorly water-soluble hypoglycemic agent, gliclazide, by the aid of lyophilization was investigated. Mannitol, sodium lauryl sulfate (SLS) and polyvinyl pyrrolidone (PVP-k-30) were employed in different weight ratios (43%, 56% and 64% w/w, respectively) as water-soluble excipients in the formulation. Lyophilized systems were found to exhibit extremely higher in vitro dissolution rate compared to the unprocessed drug powder. Solid state characterization of the lyophilized systems using X-ray powder diffraction, Fourier transform infrared spectroscopy and differential scanning calorimetry techniques revealed that dissolution enhancement was attributable to transformation of gliclazide from the crystalline to an amorphous state in the solid dispersion formed during the lyophilization process. The gastrointestinal absorption and hypoglycemic effect of the lyophilized gliclazide/SLS system were investigated following oral administration to Albino rabbits. C_max and area under the plasma concentration–time curve of gliclazide (AUC_0–12) after administration of the lyophilized formulations were significantly higher than those obtained after administration of the unprocessed gliclazide.     

The Critical Role of Passive Permeability in Designing Successful Drugs

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.     

Study on the hydrogen storage properties of a TiZrNbTa high entropy alloy

High-entropy alloys (HEAs), as a new class of metallic materials, have received more and more attention due to its excellent mechanical properties. In this study, the hydrogen absorption properties, such as hydrogen absorption capacity, thermodynamics, kinetics and cyclic properties, as well as the hydride structure of a newly designed TiZrNbTa HEA were investigated. The results showed that multiple hydrides including ε-ZrH₂, ε-TiH₂ and β-(Nb,Ta)H were found in the TiZrNbTa HEA after hydrogenation. With the increase of temperature from 293 K to 493 K, the maximum hydrogen absorption capacity decreased from 1.67 wt% to 1.25 wt% and the plateau pressure related with β-(Nb,Ta)H hydrides increased from 1.6 kPa to 14.8 kPa. The formation enthalpy of β-(Nb,Ta)H hydride was determined to be −6.4 kJ/mol, which was less stable than that of NbH and TaH hydrides. The results also showed that the TiZrNbTa HEA exhibited a rapid hydrogen absorption kinetic even at the room temperature with a short incubation time, and the hydrogen absorption mechanism was determined to be the nucleation and growth mechanism. Moreover, the hydrogen absorption capacity at 293 K decreased slowly with the cycle numbers, and remained 86% capacity after 10 cycles. Cracking occurred after hydrogen absorption and became worse with cycles.     

Tuning effect of silicon substitution on magnetic and high frequency electromagnetic properties of R2Fe17 and their composites

In this work, we report the tuning effect of the Si substitution on the magnetic and high frequency electromagnetic properties of R₂Fe₁₇ compounds and their paraffin composites. It is found that the introduction of Si can remarkably improve the magnetic and electromagnetic properties of the R₂Fe₁₇ compounds, making the R₂Fe_17–xSi_x-paraffin composites excellent microwave absorption materials (MAMs). By introducing the Si element, their saturation magnetizations decrease slightly, while much higher Curie temperatures are obtained. Furthermore, better impedance match is reached due to the decrease of the high-frequency permittivity ε′ by about 40%–50%, which finally enhances the performance of the microwave absorption. The peak frequency (f_RL) of the reflection loss (RL) curve moves toward high frequency domain and the qualified bandwidth (QB, RL ≤ ?10 dB) increases remarkably. The maximum QB of 3.3 GHz (12.0–15.3 GHz) is obtained for the Sm_1.5Y_0.5Fe₁₅Si₂-paraffin composite (d = 1.0 mm) and the maximum RL of ?53.6 dB is achieved for Nd₂Fe₁₅Si₂-paraffin composite (d = 2.2 mm), both surpassing most of the reported MAMs. Additionally, a distinguished dielectric microwave absorption peak is observed, which further increases the QB in these composites.     

水文序列相依变异识别的RIC定阶准则——以自回归模型为例

水文过程相依性是水文变异的主要表现形式之一,应用自回归模型对其进行拟合时合理确定模型阶数是一个难点问题。本文在分析AIC和BIC准则的基础上,提出了一种以原序列与其相依成分的相关系数作为拟合度指标,同时借用信息熵形式的函数式,作为模型不确定性度量指标的自回归模型定阶准则(简称RIC准则)。以AR(1)、AR(2)、AR(3)和AR(4)模型为例进行统计试验,将不同序列长度下该准则的定阶准确率与其他定阶准则进行比较,试验结果表明,RIC准则对于上述模型均具有较好的适应性,且定阶准确率远高于AIC准则,其中对于前三阶模型RIC准则优于BIC准则,但四阶模型略低于BIC准则。RIC准则的优势是可以同时满足模型定阶、相依程度分级与模型检验的需求,将其应用于实测水文序列分析,结果显示,该准则能较准确地识别自回归模型的阶数,且符合提出的"相依有变异而残差无变异的最小阶数"的检验标准。     

An experimental study of forced convective heat transfer for fully developed Al 2 O 3 –water nanofluid in an annulus tube

Nanofluids have been known as practical materials to ameliorate heat transfer within diverse industrial systems. The current work presents an empirical study on forced convection effects of Al₂O₃–water nanofluid within an annulus tube. A laminar flow regime has been considered to perform the experiment in high Reynolds number range using several concentrations of nanofluid. Also, the boundary conditions include a constant uniform heat flux applied on the outer shell and an adiabatic condition to the inner tube. Nanofluid particle is visualized with transmission electron microscopy to figure out the nanofluid particles. Additionally, the pressure drop is obtained by measuring the inlet and outlet pressure with respect to the ambient condition. The experimental results showed that adding nanoparticles to the base fluid will increase the heat transfer coefficient (HTC) and average Nusselt number. In addition, by increasing viscosity effects at maximum Reynolds number of 1140 and increasing nanofluid concentration from 1% to 4% (maximum performance at 4%), HTC increases by 18%.     

Enhanced transduction coefficient in piezoelectric PZT ceramics by mixing powders calcined at different temperatures

Large transduction coefficient ($d_{33}\times g_{33}$) is difficult to obtain in piezoelectric ceramics because these two parameters show opposite trends with compositional modifications. Herein, the Pb(Zr_0.53Ti_0.47)O₃ ceramic powders were calcinated under different temperatures (A:830 °C, B:860 °C, and C:890 °C), and then mixed together according to different weight ratios (1A:1B:1C, 1A:2B:1C, 1A:2B:3C and 3A:2B:1C) for ceramics preparation. Both d₃₃ and g₃₃ are improved successfully, and the transduction coefficient with the weight ratio of 1A:2B:3C reaches up to 17,500 × 10⁻¹⁵ m²/N, which is 60 % higher than that with the powders calcinated under 830 °C, and at least twice those of commercial PZT-4, PZT-5A and PZT-8 ceramics. The improved transduction coefficient is owing to the enhanced piezoelectric constant and spontaneous polarization resulted from the increased grain size, relative density and the fraction of tetragonal phase. These results indicate that this is a simple but effective way to tailor the transduction coefficient in piezoelectric ceramics.     

对荷载规范中旋转壳顶的风载体型系数的研究

采用CFD数值模拟方法,研究了旋转壳顶在不同矢跨比、长宽比等参数影响下的风压分布特性,并得到风载体型系数,对现行风荷载规范作了一定的补充。     

灰局势决策在水利工程开发方案优选中的应用

针对水利工程开发方案优选具有多目标、多层次等特点,建立灰局势决策模型并应用变异系数法确定评价指标权重。利用该模型对灌区改建扩建规划方案进行优选,结果表明这是一种有效的方法。     

浅析HPT250轧机中滑移系数对轧制过程的影响

通过HPT250轧机在技术改造中遇到的一个问题，即滑移系数对冷轧元缝钢管在轧制过程中所起的作用。在实际生产中经过不断的技术研究和改进。使闲置多年的HPT250轧机为钢管公司的生产迭拉起到很大的作用。