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。     

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。     

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.     

基于实际井眼轨迹的抽油杆柱API设计方法

目前的抽油杆柱设计方法大都基于设计井眼轨迹或经验公式，因此设计的抽油杆柱与井眼的匹配性并没有达到最优，结果可能影响了抽油杆柱的受力特性和寿命。概述了目前现有的抽油杆柱设计方法，提出了基于实际井眼轨迹的抽油杆柱API设计方法，即考虑到在三维空间中井下粘滞阻力及动载的影响，利用微单元分析方法计算出轴向载荷与轴向应力，然后在此基础上进行杆柱组合设计，并给出了设计流程。以江苏油田永21-3井为例，对几种设计方法的设计结果进行了对比分析，结果表明，江苏油田目前采用的抽油杆柱设计方法包含了人为经验因素，并不是最优的杆柱设计结果，有待进一步改进。     

区域水土特性参数时空变异分布特征及相关分析

作者应用地质统计学原理与方法,在山东簸箕李引黄灌区开展大尺度区域水土特性参数时空变异性的研究,描述农田排水、地下水、表层土壤中含盐量的空间与时间变化分布趋势和特征,分析其间存在的相关关系。结果表明,在一个完整的水文循环年内,研究区域的水土特性参数之间具有相近的空间变异分布状态和特点,但却表现出不同的时间变异分布趋势与特征。农田排水和表层土壤的含盐量随季节变化的分布状态在灌区上、下游相对稳定,在中游却变化明显;地下水的盐分浓度在整个灌区的分布状况没有呈现出明显的时间变异性。在春季至初夏时段内,农田排水中含盐量的增加似乎对地下水水质的影响较小,而对表层土壤积盐状况影响较大。研究成果为灌区制定合理的水资源利用与农田水土管理策略提供了理论依据。