pH-independent dissolution enhancement for multiple poorly water-soluble drugs by nano-sized solid dispersions based on hydrophobic–hydrophilic conjugates

The objective of this study was to achieve an optimal formulation of hydrophilic–hydrophobic conjugates for nano-sized solid dispersions (SDs) with enhanced dissolution of multiple drugs in different gastrointestinal (GI) tract environments. A new conjugate powder with an optimized process was used to fabricate SDs that contained three poorly water-soluble drugs that were also poorly soluble in different dissolution media. The self-assembled nanoparticle formation, drug crystallinity and SD molecular interactions were investigated by measuring the particle size during dissolution testing and physicochemical property analysis (powder X-ray diffraction and Fourier transform infrared spectroscopy). Drug release studies indicated that SD containing conjugated powder significantly improved the dissolution rates of these poorly water-soluble drugs in the GI tract. In addition, particle size analysis showed nano-sized particles in the dissolution media in the early stage with a tendency to reduce smaller particles over time. Physicochemical characterizations demonstrated almost amorphous drug states and hydrogen bonding interactions between the drugs and conjugates in the SD. This study optimized a promising material for SD, and the material was shown to have a promising performance under various pH medium conditions with poorly water-soluble drugs.     

Development and characterization of magnesium composites containing nano-sized silicon carbide and carbon nanotubes as hybrid reinforcements

Magnesium based hybrid composites containing nano-sized silicon carbide and carbon nanotubes reinforcements with minimal porosity were successfully fabricated using powder metallurgy technique with microwave sintering and hot extrusion. It was found that the addition of nano-sized silicon carbide and carbon nanotubes reinforcements lowered the coefficient of thermal expansion of magnesium. Moreover, increasing presence of silicon carbide particles led to a progressive reduction in coefficient of thermal expansion for a constant overall amount of reinforcements indicating that carbon nanotubes lowered the coefficient of thermal expansion to a lesser extent when compared to silicon carbide. Micro-hardness, 0.2% YS and UTS (except for Mg+1%CNT) showed improvement, while failure strain decreased when nano-sized silicon carbide and carbon nanotubes were added to magnesium. The failure mode of magnesium and magnesium composites was predominantly brittle exhibiting the presence of cleavage steps.     

头臂动脉夹层逆行撕裂至主动脉的治疗

目的对头臂分支动脉夹层逆行撕裂至主动脉的罕见病例进行初步探讨。方法近来收治并手术的3例患者,1例为特发性颈动脉夹层,2例为医源性锁骨下动脉夹层,均保守治疗无效而行手术,分别采用腔内治疗和外科旁路手术方法。结果患者术后疼痛明显改善,术后随访复查CTA显示头臂动脉夹层稳定,假腔内血栓形成。结论对于累及主动脉的头臂动脉夹层,腔内治疗和开放手术均为可采用的方法。     

A New Pixel Circuit Compensating for Brightness Variation in Large Size and High Resolution AMOLED Displays

A new pixel design and driving method for active-matrix organic light-emitting diode (AMOLED) display using low-temperature polycrystalline silicon thin-film transistor (LTPS-TFT) is proposed. The new circuit consists of five TFTs and one capacitor to eliminate the variation in the threshold voltage of the TFTs, and the drop in the supply voltage in a single frame operation. The proposed pixel circuit has been verified to realize uniform output current by the simulation work using HSPICE software. The simulated error rate of the output current is also discussed in this paper. The novel pixel design has great potential for use in large size and high resolution AMOLED displays.     

双层红外微测辐射热计的微桥结构仿真

非制冷红外探测器具有广阔的军事和民用前景。近年来,出现了一类性能优越的新型双层微测辐射热计型红外探测器。利用有限元分析方法和光学导纳矩阵法详细研究了两种类型的双层微测辐射热计的主要性能。结果表明,双层微测辐射热计的综合性能优于单层微测辐射热计。其中,双层S型结构的温升最优,但其力学稳定性较差,难以满足实践需要;双层U型结构的温升虽低于双层S型结构的温升,但明显优于单层微桥;重要的是,双层U型结构在光吸收性能、力学稳定性、器件制造等方面均优于双层S型结构。所以,双层U型结构的综合性能更优。还设计了一种综合性能更优的改进型双层U型结构。     

Comparison of the chronic toxicity of piroxantrone, losoxantrone and doxorubicin in spontaneously hypertensive rats

We have determined the time course, the spatial spread in brain tissue, and the intracellular distribution of biotin- and fluorescein-labeled phosphorothioate oligodeoxynucleotides (ODNs) following single injections into the rat striatum or the lateral ventricle. These time and space parameters were correlated with the ability of c-fos phosphorothioate antisense ODNs to suppress the induction of Fos protein by cocaine. A rapid and dose-dependent tissue penetration of labeled ODNs was observed following either intrastriatal or intraventricular injections of a constant sample volume. Inspection of tissue sections by confocal microscopy uncovered a distinct change in the intracellular disposition of labeled ODNs during the 24 h post-injection period. At 1, 6 and 12 h, the vast majority of the fluorescent signal was confined to the interstitial spaces throughout the zone penetrated by ODNs. Neuronal nuclei displayed faint labeling along the outer portion of the nucleus at 1 and 6 h post-injection. At these time-points, ODNs were not detected in the cytoplasm. By 16 h, ODNs were barely detectable in the extracellular space and absent from neuronal nuclei. Instead, ODNs were seen in large cytoplasmic granules of neurons throughout the tissue zone penetrated by the ODNs. Experiments with intrastriatal injections of antisense ODNs to c-fos mRNA revealed Fos suppression between 3 and 12 h, but not at 16 and 24 h. This combined analysis has revealed that (1) restricted tissue penetration by ODNs limits their antisense effects on protein expression, and (2) depletion of extracellular ODNs and sequestration of c-fos antisense ODNs into large intracellular granules coincides with the loss of their biological activity.     

Aspirin-triggered 15-epi-lipoxin A4 (ATL) generation by human leukocytes and murine peritonitis exudates: development of a specific 15-epi-LXA4 ELISA

Aspirin (ASA) triggers the formation of 15-epi-lipoxins (15-epi-LXs or ATL [ASA-triggered LX]), which are potent bioactive eicosanoids that may contribute to the therapeutic impact of ASA. To elucidate the role of these new compounds in vivo, it is essential to establish quick and sensitive detection methods. To this end, we prepared an enzyme-linked immunosorbent assay specific for 15-epi-LXA4 that proved to be highly sensitive (IC50 approximately 50 pg, minimum detection approximately 3.5 pg) and stereoselective. The amounts of 15-epi-LXA4 generated by human neutrophils from peripheral blood of healthy volunteers using this enzyme-linked immunosorbent assay were in agreement with those values obtained by liquid chromatography. Formation of 15-epi-LXA4 was cell ratio-dependent during THP-1 (a monocytic leukemia cell line)-neutrophil interactions with ASA-treated cells, and 15-epi-LXA4 was not detected with either cell type alone. Generation of 15-epi-LXA4 was also examined in murine peritonitis with ASA administration. Exudates from ASA-treated mice showed increased production of 15-epi-LXA4 that was diminished by indomethacin, a blocker of ASA-dependent acetylation of prostaglandin G/H synthase. A cytochrome P450 inhibitor administered in the presence of ASA did not prevent 15-epi-LXA4 formation, which suggests that P450 does not significantly contribute to formation of 15-epi-LXA4 in this murine model. These results indicate that the new enzyme-linked immunosorbent assay is both sensitive and selective for 15-epi-LXA4 and that 15-epi-LXA4 is produced by human leukocyte-leukocyte interactions. In addition, 15-epi-LXA4 is generated by inflammatory exudates when ASA is administered during murine peritonitis and when prostaglandin G/H synthase is upregulated and acetylated. This assay should provide rapid means to investigate 15-epi-LXA4 generation in both cellular and animal models.     

Production of recombinant SERA proteins of Plasmodium falciparum in Escherichia coli by using synthetic genes

We expressed two regions of the serine repeat antigen (SERA) protein of Plasmodium falciparum in Escherichia coli by synthesizing the genes with a changed codon usage. One of the synthetic gene sequences encodes amino acid residues 17-382 (SE47') and the other encodes amino acid residues 586-802 (SE50A). The products produced by the synthetic gene sequences in E. coli accounted for 15-30% of the total bacterial protein. Antisera against both the purified gene products prepared in rats inhibited malaria parasite growth in vitro. The anti-SE47' serum was significantly more inhibitory than the anti-SE50A serum. The described methods provide a large scale preparation of recombinant antigens for improving and producing malaria vaccine.     

Combined Removal of Carbon and Nitrogen in an Integrated UASB-Jet Loop Reactor Bioreactor System

An innovative anaerobic–aerobic integrated bioreactor system consisting of an upflow anaerobic sludge blanket (UASB) and a jet loop reactor was developed to investigate the feasibility of combined removal of carbon and nitrogen for a low-strength wastewater at different hydraulic retention times (HRTs) and recycle ratios. Total chemical oxygen demand (COD) removal of the integrated system increased from 87 to 92%, at a combined system HRT of 44?h, when the recycle ratio was increased from 100 to 400%, respectively. Denitrification efficiency of the integrated system increased from 49 to 86%, at all HRTs, when the recycle ratio was increased from 100 to 400%. The integrated system, on average, achieved more than 78% of total nitrogen at all HRTs. Nitrogen content of the biogas produced from the UASB reactor increased with increase in recycle ratios while the methane content exhibited a reverse trend, irrespective of the HRTs. Sludge volume index of the UASB reactor increased from 15?to?42?mL/g total suspended solids at the end of the study. Specific methanogenic activity of the granular sludge decreased from 1.3 to 0.8 g CH4–COD/g volatile suspended solids per day at the end of the study. Nitrogen and COD mass balance of the integrated system indicated that a substantial amount of influent nitrogen and COD was lost in the effluent as dissolved form.     

异步电机直接转矩控制磁链模型切换的研究

在分析各种切换模型的基础上,针对实际应用的高低速模型切换存在的问题,提出了一种采用速度差对时间积分的模型切换方法.实验结果表明:采用上述控制策略的调速系统具有良好的静、动态性能.