The pleiotropic functions of aspirin: mechanisms of action

Recent studies have suggested that aspirin and aspirin-like compounds have a variety of actions in addition to their well-studied ability to inhibit cyclooxygenases. These actions include inhibition of the uncoupling of oxidative phosphorylation, decreases in adenosine triphosphate stores, increases in extracellular adenosine, downregulation of the expression and activity of inducible nitric oxide synthetase, inhibition and/or stimulation of various mitogen-activated protein kinase activities and inhibition of nuclear factor binding κB site (NF-κB) activation. Moreover, aspirin-like compounds have recently been shown to have previously unappreciated clinical and biological effects, some apparently independent of cyclooxygenase. In this review we discuss the various mechanisms of action of aspirin-like compounds and their relevance to clinical disease and therapy. Received 1 February 1999; received after revision 1 April 1999; accepted 7 May 1999     

Partition coefficients of drugs in bilayer lipid membranes

The oil/water partition coefficient of drugs is widely accepted as a key parameter in drug design. The coefficients are usually determined using a bulk octanol phase to represent the lipid. The physiologically and pharmacologically relevant structure is, of course, the bilayer lipid membrane, but until now there has been no convenient means of measuring the partition coefficients of small molecules into a single bilayer. This paper demonstrates that the partition coefficient may be calculated from the change in membrane refractive index which occurs when a drug molecule partitions into the membrane. The refractive index is determined by an integratedoptics technique ideally suited to an ultra-thin structure such as a lipid bilayer.     

利用聚钙黄绿素薄膜修饰电极测定阿司匹林

利用聚钙黄绿素薄膜修饰电极(PCALE)对阿司匹林(AS)的电催化作用,建立了对AS含量进行定量分析的方法.在0.05 mol/L KH2PO4-Na2HPO4(pH=6.8)+0.2 mol/L KNO3体系中,AS的浓度在4.5×10 7～1.2×10 5mol/L范围内与峰电流呈良好的线性关系,线性回归方程和线性相关系数分别为:ip=1.75×105C 1.51;γ=0.997 7,检出限可达9.1×10 8mol/L.利用该法对阿司匹林样品进行定量分析,得到满意结果.八次样品分析结果的相对标准偏差为2.0%,样品回收率为98.4%～100.4%,完全满足微量分析的要求.     

阿司匹林对在体及离体气管平滑肌的影响

目的:研究阿司匹林对在体及离体气管平滑肌的影响.方法:观察不同剂量的阿司匹林对乙酰胆碱/磷酸组织胺诱发在体及离体豚鼠气管平滑肌收缩的影响.结果:阿司匹林对乙酰胆碱/磷酸组织胺诱发的体内外气管平滑肌收缩的对抗作用具有明显的剂量差异,即随着剂量增加,阿司匹林对抗气管平滑肌收缩的作用越来越弱,而沙丁胺醇且有很好的扩张气管平滑肌的作用.结论:适宜浓度的阿司匹林具有扩张气管平滑肌的作用.     

乙酰水杨酸合成的微型化设计与实践

介绍了乙酰水杨酸的微型化合成方法，微型化重结晶方法和产品的检验．并对实验装置和操作方法的改进作了探索．     

化学计量学法测定阿司匹林与布洛芬

用紫外分光光度法对阿司匹林及布洛芬进行直接测定,用化学计量学中的主成分分析法(PCR)、偏最小二乘法(PLS)对数据进行处理。波长范围为250nm-330nm,隔1nm采集数据,方法操作简无需过多的分离,其相对标准偏差分别为1.36%、0.76%。     

微波辐射合成阿司匹林的研究

以水杨酸和乙酸酐为原料,选用不同催化剂,用微波法快速合成阿司匹林.通过实验考察了原料用量比、不同催化剂、微波辐射功率、辐射时间等因素对产率的影响,得到了最佳合成工艺条件:水杨酸和乙酸酐量的比为1∶1.5,微波功率为550 W,用乙酸钾作催化剂,辐射时间5 min时,纯化后产物产率高达81.46%.     

阿司匹林软膏制备工艺及稳定性试验研究

目的:比较不同类型的基质对阿司匹林软膏稳定性的影响,确定基质类型和制备工艺.方法:采用对比研究的方法制备处方并进行稳定性试验.结果:阿司匹林软膏宜采用乳化法制备W/O型乳剂基质.结论:W/O型阿司匹林软膏稳定性好,制备工艺简单,方便易行.     

低分子肝素与阿斯匹林治疗不稳定心绞痛疗效对比观察

目的探讨低分子肝素治疗不稳定型心绞痛(UAP)的疗效及安全性。方法将116例UAP患者随机单盲分为对照组(常规治疗)和治疗组(常规治疗 低分子肝素)分别为58例。结果4周后总有效率:治疗组为91.38%,对照组为68.97%(P<0.05);观察4周治疗组无1例发生心肌梗死,无1例死亡;对照组发生心肌梗死5例(占8.62%),死亡4例。治疗组未发生明显不良反应。结论在常规抗凝治疗基础上加用低分子肝素能更有效的控制并预防心绞痛发作频率,并能减低心肌梗死的发生率。