药学英语,课后翻译

药学英语
Unit 1
Inflammatory reaction induced by local ischemic injury is one of the important pathophysiological characteristics after ischemic stroke, so anti-inflammatory therapy may be an effective strategy for acute ischemic stroke. Enlimomab, an anti-ICAM-1 murine monoclonal antibody, can inhibit the recruitment and activity of polymorphonuclear leukocytes, reduce their adhesion and decrease cerebral infarct size in experimental stroke models. However, a much larger efficacy trial including 625 acute ischemic stroke patients has shown that enlimomab was ineffective on ischemic stroke patients even with a worsening outcome. The therapeutic time window of rt-PA is within 3 hours of ischemic onset. Administration of the drug after more than 3 hours of ischemic onset has no significant therapeutic implications and may even end up with an increased hemorrhagic risk. A study using the animal ischemic model indicated that combination of anti-inflammatory therapy and rt-PA could significantly and might as well extend the therapeutic time window of thrombolysis.
局部脑缺血损伤引起的炎症反应是缺血性脑卒中发生后的重要病理生理特征，因此，抗炎治疗策略可能是治疗急性缺血性脑卒中的一种有效方法。

恩莫单抗是一种抗细胞间黏附分子-1的单克隆抗体，在实验性脑缺血模型上，能抑制多形核白细胞的募集和活化，减少其黏附，降低脑梗死范围。

然而，一项由625例急性缺血性脑
卒中患者参加的大规模的有效性临床试验却显示，使用恩莫单抗治疗，对缺血性脑卒中患者无效，且可能使病情恶化。

rt – PA的治疗时间窗为脑缺血发病后3小时，超过3小时后用药则无明显治疗意义，并有可能增加出血性风险。

一项在动物脑卒中模型上的研究表明，将抗炎治疗与rt-PA治疗联合应用，能显著减少梗死范围，改善神经功能结果，而不增加出血性风险，还可能延长溶栓治疗的时间窗。

Unit 2
Drug discovery is the identification of novel active compounds, which are typically found by screening many compounds (from compound library) for the desired biological properties. In general, drug discovery is a very time-consuming and expensive process. Estimates of the average time required to bring a drug to the market range from12-15 years at an average cost of about $800 million. For approximately every 10000 compounds that are evaluated in animal studies, 10 will make it to human clinical trials in order to get 1 compound on the market. This is why the cost to purchase a drug is so high.
The search of lead compound and the structural modification of lead compound for pharmacological optimization are the important two steps for new drug research in medicinal chemistry.
课文翻译：药物发现通常是从许多化合物中（从化合物库中）
鉴定和筛选具有所需药理作用的新型活性化合物的过程。

一般而言，药物发现是一个非常耗时和昂贵的过程。

一种新药的研发和投放市场平均需要约12-15年的时间，其成本约8亿美元。

一般用动物实
验来评价药理活性的每10000个化合物中，只有10个才能进入人体临床试验，而最后1个能被开发成药物而投放市场。

这就是为什么新药研发的成本如此之高。

以新型先导化合物的发现及先先导化合物的结构优化来改善药理活性是药物化学中新药研究的两步重要过程。

Unit 3
With suspensions of amine salts, both solubility and rate of degradation are functions of pH. The pH of optimum stability will be that at which the product of solubility and rate is a minimum. In addition, anything which reduces the solubility of the salt will aid stability, e.g., addition of a soluble salt of the amine, salting out, etc. From the reports available to date ampicillin might be most stable penicillin available, in both acid and neutral solution. Ampicillin, at pH 7.0 and room temperature, maintains 80% of its activity for I week. Whereas one would suspect that the other newer penicillins would show a dependence of rate of loss of activity on pH similar to that of penicillin G, one might also speculate that ampicillin might be different because of its zwitterionic character at almost neutral Ph.
对于铵盐的悬浮液，其溶解性和降解率都受到pH值功能的调节。

最稳定的pH值可以使产品的溶解性和降解率达到最低。

此外，任
何降低盐溶解性的物质都将有助于其保持稳定性，例如，加入胺的
可溶性盐，盐析等。

据报道可以得知氨苄青霉素可能是现存在中性
及酸性条件下最稳定的青霉素。

氨苄青霉素在中性溶液以及室温条
件下保存1星期其活性维持在80%左右。

然而有人发现其他的一些
新型青霉素和青霉素G一样，活性依赖于pH值的高低，也有人推
断氨苄青霉素可能不一样，因为在近乎中性的条件下它是两性离子。

Unit 4
Comparison of HPLC to gas chromatography (GC) is instructive in pointing out similarities and differences. In both methods, the separation of components in a mixture is achieved in flowing stream. The mechanisms of retention differ greatly but parallels can be drawn in many cases. In both HPLC and GC, components which preferentially interact with the stationary phase will be retained longer. In GC, the mobile phase, or carrier gas, has little effect on the separations (other than the flow rate). Consequently, separations are achieved by manipulation of the stationary phase or the sample (e.g. derivatization to improve volatility). A large number of stationary phases have been developed and are commercially available. In essence, GC can be characterized as having one mobile
phase and many stationary phases. On the other hand, HPLC has developed with relatively few stationary phases. It is the mobile phase that gives great diversity to HPLC. Binary, ternary, and occasionally quaternary mobile phase compositions are used. Buffers are added to control PH, and ion-pairing reagents are added to modify the retention. In GC, temperature programming, and even flow programming, can be used to increase the separative power of the system. In HPLC, the mobile phase composition is changed in a programmed fashion in order to achieve comparable effects.
高效液相色谱法与气象色谱法（GC）两者既有相似点又有区别。

两者都通过流动相进行混合物的分离，虽然分离机制不同，但从众
多例子中可发现其相似性。

对两者来说，化合物越容易与固定相结
合其保留时间越长。

对于气相色谱法，流动相或载气种类（不包括
流速）对分离效能的影响小，因此，多通过改变固定相或样品的挥
发性质（如进行衍生化等）来改善分离，现在已开发了种类繁多的
可以买到的固定相。

实质上气相色谱可认为是具有一种流动相和多
种固定相的特征。

而对于高效液相色谱法，仅有相对的几种固定相，流动相的变化很大。

通常流动相用二元、三元溶剂混合，也有四元
溶剂的，多加入缓冲溶液控制pH，用离子对试剂调整保留值。

气象色谱法采用程序升温的方式提高系统分离能力，高效液相色谱法采
取梯度洗脱凡是改善分离效能。