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.     

Physical Stability of Octenyl Succinate–Modified Polysaccharides and Whey Proteins for Potential Use as Bioactive Carriers in Food Systems

The high cost and potential toxicity of biodegradable polymers like poly(lactic‐co‐glycolic)acid (PLGA) has increased the interest in natural and modified biopolymers as bioactive carriers. This study characterized the physical stability (water sorption and state transition behavior) of selected starch and proteins: octenyl succinate–modified depolymerized waxy corn starch (DWxCn), waxy rice starch (DWxRc), phytoglycogen, whey protein concentrate (80%, WPC), whey protein isolate (WPI), and α‐lactalbumin (α‐L) to determine their potential as carriers of bioactive compounds under different environmental conditions. After enzyme modification and particle size characterization, glass transition temperature and moisture isotherms were used to characterize the systems. DWxCn and DWxRc had increased water sorption compared to native starch. The level of octenyl succinate anhydrate (OSA) modification (3% and 7%) did not reduce the water sorption of the DWxCn and phytoglycogen samples. The Guggenheim–Andersen–de Boer model indicated that native waxy corn had significantly (P < 0.05) higher water monolayer capacity followed by 3%‐OSA‐modified DWxCn, WPI, 3%‐OSA‐modified DWxRc, α‐L, and native phytoglycogen. WPC had significantly lower water monolayer capacity. All Tg values matched with the solid‐like appearance of the biopolymers. Native polysaccharides and whey proteins had higher glass transition temperature (Tg) values. On the other hand, depolymerized waxy starches at 7%‐OSA modification had a “melted” appearance when exposed to environments with high relative humidity (above 70%) after 10 days at 23 °C. The use of depolymerized and OSA‐modified polysaccharides blended with proteins created more stable blends of biopolymers. Hence, this biopolymer would be suitable for materials exposed to high humidity environments in food applications.     

Porous sunflower plate-like NiFe2O4/CoNi–S heterostructure as efficient electrocatalyst for overall water splitting

Constructing high-efficient and nonprecious electrocatalysts is of primary importance for improving the efficiency of water splitting. Herein, a novel sunflower plate-like NiFe₂O₄/CoNi–S nanosheet heterostructure was fabricated via facile hydrothermal and electrodeposition methods. The as-fabricated NiFe₂O₄/CoNi–S heterostructure array exhibits remarkable bifunctional catalytic activity and stability toward oxygen evolution reaction (OER) and hydrogen evolution reaction (HER) in alkaline media. It presents a small overpotential of 219 mV and 149 mV for OER and HER, respectively, to produce a current density of 10 mA cm^?2. More significantly, when the obtained electrodes are used as both the cathode and anode in an electrolyzer, a voltage of 1.57 V is gained at 10 mA cm^?2, with superior stability for 72 h. Such outstanding properties are ascribed to: the 3D porous network structure, which exposes more active sites and accelerates mass transfer and gas bubble emission; the high conductivity of CoNi–S, which provides faster charge transport and thus promotes the electrocatalytic reaction of the composites; and the effective interface engineering between NiFe₂O₄ (excellent performance for OER) and CoNi–S (high activity for HER), which leads to a shorter transport pathway and thus expedites electron transfer. This work provides a new strategy for designing efficient and inexpensive electrocatalysts for water splitting.     

影响煤层气开发效果的地质因素再认识

地质特征认识对煤层气开发效果起着重要作用。在资源特征相差不大的情况下,发现煤层气相邻井的产量差异仍较大。排除工程因素后,通过选取8类地质参数,细致比对了保德区块低产井与邻井的参数特征,筛查出其关键因素为煤层微幅构造与顶板封盖条件,其中以微幅构造为主。据此,重新认识并划分出区块新的次生褶皱背斜单元、向斜单元和斜坡单元,获得了不同次生褶皱构造单元的开发特征。结果表明,高、低产井分布与次生褶皱背斜、向斜相关性高达92%。其中:高产井主要分布在次生褶皱背斜变化较缓、呈隆起状的“平台”,且煤层顶板以泥岩、碳质泥岩为主,封盖性较好;低产井主要分布在次生褶皱向斜,同一井台各井开发效果差异表现为从向斜条带轴部—向斜条带内—向斜条带外的煤层气井平均单井产量不断增加,到向斜轴部的距离大于向斜曲率半径73.5%的范围为主力产气区,小于向斜曲率半径40.0%范围为产水主力区。这对煤层气新井部署、生产管理、开发调整等,具有一定的指导意义。     

Nickel foam-supported Fe,Ni-Polyporphyrin microparticles: Efficient bifunctional catalysts for overall water splitting in alkaline media

Developing highly active, stable and sustainable electrocatalysts for overall water splitting is of great importance to generate renewable H₂ for fuel cells. Herein, we report the synthesis of electrocatalytically active, nickel foam-supported, spherical core-shell Fe-poly(tetraphenylporphyrin)/Ni-poly(tetraphenylporphyrin) microparticles (FeTPP@NiTPP/NF). We also show that FeTPP@NiTPP/NF exhibits efficient bifunctional electrocatalytic properties toward both the oxygen evolution reaction (OER) and the hydrogen evolution reaction (HER). Electrochemical tests in KOH solution (1 M) reveal that FeTPP@NiTPP/NF electrocatalyzes the OER with 100 mA cm⁻² at an overpotential of 302 mV and the HER with 10 mA cm⁻² at an overpotential of 170 mV. Notably also, its catalytic performance for OER is better than that of RuO₂, the benchmark OER catalyst. Although its catalytic activity for HER is slightly lower than that of Pt/C (the benchmark HER electrocatalyst), it shows greater stability than the latter during the reaction. The material also exhibits electrocatalytic activity for overall water splitting reaction at a current density of 10 mA cm⁻² with a cell voltage of 1.58 V, along with a good recovery property. Additionally, the work demonstrates a new synthetic strategy to an efficient, noble metal-free-coordinated covalent organic framework (COF)-based, bifunctional electrocatalyst for water splitting.     

综放工作面防治水技术应用实践

为解决21000工作面采空区及顶板涌水问题,根据工作面出水点的不同情况,采取了集水器导水、老塘设挡水堰截水、挖排水沟疏水等多项治水措施,经统计排水量达33~42m3/h,有效控制了水情,确保了工作面正常生产。     

Antitumor Effects of Vitamin D Analogs on Hamster and Mouse Melanoma Cell Lines in Relation to Melanin Pigmentation

Deregulated melanogenesis is involved in melanomagenesis and melanoma progression and resistance to therapy. Vitamin D analogs have anti-melanoma activity. While the hypercalcaemic effect of the active form of Vitamin D (1,25(OH)₂D₃) limits its therapeutic use, novel Vitamin D analogs with a modified side chain demonstrate low calcaemic activity. We therefore examined the effect of secosteroidal analogs, both classic (1,25(OH)₂D₃ and 25(OH)D₃), and novel relatively non-calcemic ones (20(OH)D₃, calcipotriol, 21(OH)pD, pD and 20(OH)pL), on proliferation, colony formation in monolayer and soft-agar, and mRNA and protein expression by melanoma cells. Murine B16-F10 and hamster Bomirski Ab cell lines were shown to be effective models to study how melanogenesis affects anti-melanoma treatment. Novel Vitamin D analogs with a short side-chain and lumisterol-like 20(OH)pL efficiently inhibited rodent melanoma growth. Moderate pigmentation sensitized rodent melanoma cells towards Vitamin D analogs, and altered expression of key genes involved in Vitamin D signaling, which was opposite to the effect on heavily pigmented cells. Interestingly, melanogenesis inhibited ligand-induced Vitamin D receptor translocation and ligand-induced expression of VDR and CYP24A1 genes. These findings indicate that melanogenesis can affect the anti-melanoma activity of Vitamin D analogs in a complex manner.     

A facile method for preparation of PGS@ZB‐N and gas‐sol alternating synergistic effect for fire resistance of EVA

Through the simple precipitation of palygorskite (PGS) by zinc borate (ZB) (to make PGS@ZB) and the decoration of PGS@ZB by dodecylamine (N), a novel organic‐inorganic@inorganic hybrid flame retardant of PGS@ZB‐N was prepared and was incorporated with ethylene vinyl acetate copolymer (EVA) to improve its flame retardance. The structure and morphology of PGS@ZB‐N were characterized by Fourier transform infrared (FTIR) spectroscopy, X‐ray diffraction (XRD), and scanning electron microscopy (SEM), and it was confirmed that the PGS@ZB‐N hybrid had been successfully prepared. The flame retardancy and burning behavior of EVA/PGS@ZB‐N/EG (EG = expandable graphite) composite were studied through thermogravimetric analysis (TGA), limiting oxygen index (LOI), UL‐94 (by the vertical burning test), and cone calorimeter test (CCT) characterizations. The prepared EVA/PGS@ZB‐N/EG composite obtained an LOI value of 41.2% with the addition of 30 wt% PGS@ZB‐N/EG. It was found that EVA/PGS@ZB‐N/EG was protected through a gas phase and condensed phase alternating synergistic effect mechanism.     

Efficiency and effectiveness enhancement of an intercooler of two‐stage air compressor by low‐cost Al2O3/water nanofluids

The present study was aimed to utilize low‐cost alumina (Al₂O₃) nanoparticles for improving the heat transfer behavior in an intercooler of two‐stage air compressor. Experimental investigation was carried out with three different volume concentrations of 0.5%, 0.75%, and 1.0% Al₂O₃/water nanofluids to assess the performance of the intercooler, that is, counterflow heat exchanger at different loads. Thermal properties such as thermal conductivity and overall heat transfer coefficient of nanofluid increased substantially with increasing concentration of Al₂O₃ nanoparticles. Specific heat capacity of nanofluids were lower than base water. The intercooler performance parameters such as effectiveness and efficiency improved appreciably with the employment of nanofluid. The efficiency increased by about 6.1% with maximum concentration of nanofluid, that is, 1% at 3‐bar compressor load. It is concluded from the study that high concentration of Al₂O₃ nanoparticles dispersion in water would offer better heat transfer performance of the intercooler.