Development,In-Vitro Characterization and Preclinical Evaluation of Esomeprazole-Encapsulated Proniosomal Formulation for the Enhancement of Anti-Ulcer Activity

Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeutic efficacy. Method: EZL-PNs formulation was developed by slurry method and optimized by 33 box-Bhekhen statistical design software. Span 60 (surfactant), cholesterol, EZL concentration were taken as independent variables and their effects were evaluated on vesicle size (nm), entrapment efficiency (%, EE) and drug release (%, DR). Furthermore, optimized EZL-PNs (EZL-PNs-opt) formulation was evaluated for ex vivo permeation, pharmacokinetic and ulcer protection activity. Result: The EZL-PNs-opt formulation showed 616 ± 13.21 nm of vesicle size, and 81.21 ± 2.35% of EE. EZL-PNs-opt exhibited negative zeta potential and spherical confirmed scanning electron microscopy. EZL-PNs-opt showed sustained release of EZL (95.07 ± 2.10% in 12 h) than pure EZL dispersion. The ex-vivo gut permeation result exhibited a significantly (p < 0.05) enhanced flux than pure EZL. The in vivo results revealed 4.02-fold enhancement in bioavailability and 61.65% protection in ulcer than pure EZL dispersion (43.82%). Conclusion: Our findings revealed that EZL-PNs formulation could be an alternative delivery system of EZL to enhance oral bioavailability and antiulcer activity.     

声光栅正弦结构光投射器的光学系统设计

针对一种新型的声光波干涉测量技术,对声光栅正弦结构光投射器的三维测量工作原理进行了系统的分析,讨论了影响投射器光学系统结构的因素和影响接收屏上的光照度的因素,并进行了光学系统设计。在优化设计过程中,采用了限制光线最大入射角的方法,达到控制投射系统的球差和保证接收屏上照明均匀的要求。所设计的声光栅正弦光投射器具有很好的成像质量。应用该系统对在500mm处的石膏像上投射干涉条纹,可以得到能量比较均匀、变形量很小的干涉条纹图,利用该条纹图和相关的算法可以对具有复杂几何形状的物体进行有效的三维测量。     

强激光装置中玻璃疵病在线检测的光学系统设计

介绍了一种用于玻璃疵病在线检测的近摄工作距成像光学系统,其光组结构形式采用了光阑后置的准远心结构形式,主要光学参量为f′=14 mm;在物像距为250 mm约束条件下,物方视场达到90 mm（对角线）;F/number=3.56;光谱适应范围为400~800 nm,对应的空间分辨率为100 lp/mm时,调制传递函数大于0.29.     

光纤耦合数码系统传像特性

建立了光纤传像元件与光电阵列器件的匹配耦合模型,引入变动因子反映像素光纤排列的不确定性,进行了光纤耦合传像特性的仿真研究.针对9×9 μm2光敏元的阵列器件,分析了光纤传像元件结构参数变化对系统分辨率的影响,在光纤直径约为光敏元尺寸1/3时获得了相对经济合理的匹配结构,表明光纤耦合数码系统设计时必须考虑优化匹配问题.仿真结果还解释了系统的图像输出存在条纹和局部结构背景的原因,给出了相应的数值分析方法.     

基于作用距离的红外成像系统光学参数确定

作用距离是决定红外成像系统性能的重要指标,可直接影响红外成像光学系统的参数确定.基于作用距离的参数确定方法建立了探测器与作用距离、空间分辨率之间的关系,对光学系统的参数确定和性能评价具有重要作用.结合实例确定了红外成像系统光学的主要参数,采用非制冷凝视型长波红外探测器(工作波段为8mμ～12μm),在.特定的作用距离下,利用该方法确定的红外光学系统通光口径为90mm,F数值为1.     

某型器件工作状态记录仪的设计

为对某型器件工作状态中的几个重要参数进行全程监测和定量分析,并满足在高冲击等特殊环境下使用的要求,提出了一种基于CPLD为主控、以Flash为存储器的测试存储系统设计方案.详细阐述了硬件系统各组成模块的电路及其工作原理,给出了相应的程序设计流程图,介绍了采集中的编码方法和提高存储速度的方法.在实地测试过程中,记录仪达到...     

Arbitrary real-order cost functions for signals and systems

This work focuses on a new type of cost function based on fractional operators. To do so, the concept of definite integral is extended to arbitrary real-order. Some properties of this new fractional-order definite integral are studied and a fractional-order Barrow's rule is proposed. It is illustrated by an example (the design of an IIR filter) how this new kind of cost function can be a valuable tool in problems where optimal design methods are involved.     

Multiple Keys for a Single Lock: The Unusual Structural Plasticity of the Nucleotidyltransferase (4′)/Kanamycin Complex

The most common mode of bacterial resistance to aminoglycoside antibiotics is the enzyme‐catalysed chemical modification of the drug. Over the last two decades, significant efforts in medicinal chemistry have been focused on the design of non‐ inactivable antibiotics. Unfortunately, this strategy has met with limited success on account of the remarkably wide substrate specificity of aminoglycoside‐modifying enzymes. To understand the mechanisms behind substrate promiscuity, we have performed a comprehensive experimental and theoretical analysis of the molecular‐recognition processes that lead to antibiotic inactivation by Staphylococcus aureus nucleotidyltransferase 4′(ANT(4′)), a clinically relevant protein. According to our results, the ability of this enzyme to inactivate structurally diverse polycationic molecules relies on three specific features of the catalytic region. First, the dominant role of electrostatics in aminoglycoside recognition, in combination with the significant extension of the enzyme anionic regions, confers to the protein/antibiotic complex a highly dynamic character. The motion deduced for the bound antibiotic seem to be essential for the enzyme action and probably provide a mechanism to explore alternative drug inactivation modes. Second, the nucleotide recognition is exclusively mediated by the inorganic fragment. In fact, even inorganic triphosphate can be employed as a substrate. Third, ANT(4′) seems to be equipped with a duplicated basic catalyst that is able to promote drug inactivation through different reactive geometries. This particular combination of features explains the enzyme versatility and renders the design of non‐inactivable derivatives a challenging task.