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.     

基于DSP的多元数据同步采集与存储系统的设计与实现

从硬件和软件两个角度出发,介绍基于DSP的多元数据同步采集与存储系统的组成、工作模式以及功能的测试。系统主要由上位机和数字采集与存储单元组成,其中数字采集与存储单元的硬件部分包括电源模块,值班电路模块,数据采集模块,数据存储模块,时钟同步模块。系统采用DSP作为中央处理芯片,利用经过同步后的秒脉冲作为触发信号,实现同步数据采集。以CF卡作为存储介质,实现数据自容式存储。软件部分实现自检、同步、数据采集存储功能。经过测试,系统工作稳定,功能正常,同步精度在100ns以内。     

碳含量对激光熔覆CoCrFeMnNiCx高熵合金涂层摩擦磨损和耐蚀性能的影响

采用激光熔覆技术在 45 钢基体上制备了不同碳含量(等摩尔比)的 CoCrFeMnNiC_x( x = 0,0. 03,0. 06,0. 09, 0. 12,0. 15)高熵合金涂层。 通过 X 射线衍射(XRD)、扫描电镜( SEM)、HVS-1000A 型显微硬度计、RST5000 型电化学工作站、UMT-2 型摩擦磨损试验机等表征和测试手段研究了不同碳含量对激光熔覆 CoCrFeMnNiC_x 高熵合金涂层物相结构、显微硬度、摩擦磨损及耐腐蚀性能的影响。 结果表明,当碳含量 x 由 0 逐渐增加至 0. 09 时,高熵合金相结构由 FCC 固溶体转变为 FCC 固溶体和 M23C6 相共存,合金微观组织变得细小;熔覆层硬度由 183. 20 HV_{0. 2} 增加至 223. 48 HV_{0. 2} ; 涂层的摩擦因数降低,耐磨性能变强;腐蚀电位由-469 mV 增大至-348 mV,腐蚀电流密度由 14. 95 μA·cm^-2 减小为 2. 29 μA·cm^-2 ,耐腐蚀性增强。 当碳含量 x 由 0. 09 逐渐增加至 0. 15 时,合金相结构再次转变为 FCC 固溶体,且合金微观组织恢复粗大状态;熔覆层硬度与耐腐蚀性降低,但耐磨性能却先减弱后增强。 合金在碳含量为 0. 09 时,硬度最高且耐腐蚀性能最强;在碳含量为 0. 15 时,耐磨性最强。     

A Simple and Effective Mass Spectrometric Approach to Identify the Adulteration of the Mediterranean Diet Component Extra-Virgin Olive Oil with Corn Oil

Extra virgin olive oil (EVOO) with its nutraceutical characteristics substantially contributes as a major nutrient to the health benefit of the Mediterranean diet. Unfortunately, the adulteration of EVOO with less expensive oils (e.g., peanut and corn oils), has become one of the biggest source of agricultural fraud in the European Union, with important health implications for consumers, mainly due to the introduction of seed oil-derived allergens causing, especially in children, severe food allergy phenomena. In this regard, revealing adulterations of EVOO is of fundamental importance for health care and prevention reasons, especially in children. To this aim, effective analytical methods to assess EVOO purity are necessary. Here, we propose a simple, rapid, robust and very sensitive method for non-specialized mass spectrometric laboratory, based on the matrix-assisted laser desorption/ionization mass spectrometry (MALDI-TOF MS) coupled to unsupervised hierarchical clustering (UHC), principal component (PCA) and Pearson’s correlation analyses, to reveal corn oil (CO) adulterations in EVOO at very low levels (down to 0.5%).     

粉煤灰砖抗折强度测量结果不确定度的评定

通过对粉煤灰砖抗折强度测量结果不确定度的评定,分析出影响试验结果的各种因素,为提高检测水平和精确度提供指导。     

激光脉冲编码抗有源干扰效果研究

激光脉冲编码是激光制导武器的抗干扰措施之一。角度欺骗式干扰和高重频干扰是目前半主动激光制导武器的主要有源干扰来源。为研究不同激光脉冲编码方式对激光半主动制导武器抗这两种干扰性能的影响,本文针对敌方激光告警机的识别算法与我方导引头的解码过程,提出自相关函数与归一化互相关函数评价方法,并对目前主要编码方式进行仿真,仿真结果表明:激光脉冲编码的抗角度欺骗式干扰能力受编码序列周期性与脉冲间隔随机性的影响；抗高重频激光干扰能力受编码序列脉冲间隔随机性的影响；LFSR状态码的抗角度欺骗式干扰与抗高重频干扰效果均优于其他编码方式。     

Operating Range Scheduled Robust Dahlin Algorithm to Typical Industrial Process with Input Constraint

International Journal of Control, Automation and Systems - There is a class of typical nonlinear industrial process, which can be characterized by a first-order inertia plus pure delay model in an...     

Synthesis of amino-cosubstituted polyorganophosphazenes and fabrication of their nanoparticles for anticancer drug delivery

The development of safe drug carriers is cardinal in cancer therapy, which can target the cancer cells and release the loaded drug on-demand without damaging the healthy cells of the body. In our work, we synthesized three different biodegradable polymers, poly[(ethyl aminobezoate) (ethyl glycinato) phosphazenes] (PABGPs), in different mole ratio of side groups. The successful synthesis of these PABGPs was confirmed by ¹H NMR, ³¹P NMR, FT-IR, and gel permeation chromatography. These PABGPs were fabricated into drug (camptothecin, CPT, a hydrophobic anticancer drug) loaded nanoparticles. These drug-loaded nanoparticles showed good drug release behaviors under normal physiological conditions (pH 7.4 and temperature 37°C). These PABGPs-based nanoparticles may find their application as effective drug carriers for cancer therapy.