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b--吡啶 pyridine 巴比妥酸:barbituric acid 比电导conductance 不规则的:irregular 崩解剂disintegrant
c--萃取 extraction 成团:agglomeration 测量仪measurement 肠液:intestinal fluid d--胆固醇cholestero 对映体:enantiomer 电极electrode 代谢:metabolism f--反相渗透reverse osmosis 分布:disposition g--构象:conformation 固化:solidize
j--甲苯 toluene 静脉注:intravenous injection 挤压:compress 聚集:aggregate 胶囊capsule
l--粒子:particle 立体选择性:stereoselectivity 利用率:availability m--灭菌产品sterile products n--粘合剂adhesive
p--偏振光:polarized light 片剂tablet 配剂elixir 排泄:excretion q--起始原料starting materials(raw materials) q醛 aldehyde r--溶解度:solubility 乳剂emulsion 润滑剂lubricant
s--释放:release 渗液solution 生物膜:biologic membrane 生物碱alkaloid, t---糖浆syrup 甜味剂sweetener
w--丸剂pill 微生物microorganism 胃液:gastric fluid 稳定态:steady-state
x--旋光异构现象:optical isomerism 悬浮液suspension 香味剂flavor 稀释剂diluent 形状:shape 吸收:absorption 消除:elimination y--胰岛素 insulin 压片:tablet compression
z--中间体intermediate 重结晶 recrystallization 左旋:levorotation 蒸馏distillation 组织tissue
a--asymmetric carbon不对称碳 absorption吸收 action动作 adhesive粘合剂 c--contamination污染 chirality:手性 compress压缩 composite合成的
compressibility:可压缩性 compaction:压紧 contamination specialize特殊污染 conductivity电导率 control:控制 clinical:临床的 d-- design:设计 dry:干燥 delivery:传送 e-- extend:延长 epoxide:环氧化物
f-- formulation:制剂 fluidity:流动性 function:功能 g-- geometric isomerism:几何异构
h-- hormone激素 hydrolysis diastereoisomer:水解非对映异构体 heterogeneous catalyst多相催化剂, i-- irrigating冲洗
m-- metabolite代谢物 medication药物治疗 medicine内服药 mill:研磨
measure尺寸 mix:混合 microorganisms微生物 o-- ophthalmic眼药
p-- polysaccharide多糖 peptide肽 plasma血浆 penicillin青霉素,
precursor:前体 partition coefficient:狭义分配系数 pharmaceutical制药的 parenteral注射药物 pycogens热源 procedure:程序 q-- quality性质 quantity数量
s-- steroid甾类 steric effect:空间效应 stereoselectivity:立体选择性 screening:过筛 sustain :维持 t-- treat治疗 therapy:治疗
u--uniformity目标 v--vaccine疫苗
Unit1 P7
1、 Answer the following questions:
(1) How many groups can pharmaceutical agents be split into
depending on their production or origin?
①totally synthetic materials(synthetics)②natural products③products from partial syntheses(semi-synthetic products)
(2)Can you illustrate any significant examples of pharmaceutical agents obtained by total synthesis?
L-amine,chleramphomical,caffeine,Dopamine,Epinephrine,
Lerodapa,peptide,hormones.Prestaglanding,P_Pouricollamine,Vincamine,
(3)What is the difference between the synthetic drugs and traditional Chinese herbal medicine?
synthetic drugs include the most important of synthetics and semi-sythetic products, however, natural products are frequently needed as starting materials or intermediates for important synthetic products. 2、生物碱
4、Introduction of Nucleic acids
Nucleic acids are polyanionic molecules of high molecular weight. These polymers are composed of a sequence of subunits or nucleotides so that the whole is usually termed a polynucleotide. The nucleic acids are of two main varieties, ribonucleic (RNA) and deoxyribonucleic (DNA). DNA is found primarily in the chromatin to the cell nucleus, whereas 90% of RNA is presented in the cell cytoplasm and 10% in the nucleolus. The two classes of nucleic acids are distinguished primary on basis of the five-carbon atom sugar of pentose present. Two general kinds of bases are found in all nucleic acids. One type is a derivative of the parent compound purine. Principle examples are guanine and adenine. The second class of bases found in all nucleic acid is derived from the parent compound pyrimidine. 介绍核酸
核酸是超高分子量聚阴离子分子。这些聚合物组成,亚基或核苷酸,使整个通常称为多核苷酸序列。核酸有两种,主要品种核糖核酸(RNA)和脱氧核糖核酸(DNA)的。 DNA是主要存在于细胞核内的染色质,而90%的RNA在细胞质现在和10%的核仁。核酸类的两个主要的区别在于对目前的五个戊糖碳原子的糖基础。一般两个种基地发现,在所有核酸。一类是母体化合物嘌呤的衍生物。原理是鸟嘌呤和腺嘌呤的例子。在所有发现核酸碱基第二类是来自母体化合物嘧啶。 Unit2 P23
1、Answer the following questions:
(1) What is quantitative structure-activity relationship (QSAR) of pharmacologic agents?
quantitative descriptions of physical properties of compounds and the response of the biological system under consideration.
(2) How many steric factors influence on the pharmacologic activity?
Three major headings.(1)Optical and Geometric Isomerism and Pharmacologic Activity.(2)Confrontational Isomerism and Pharmacologic Activity.(3)Isomerism
and Pharmacologic Activity.
(3) Why do enantiomophric pairs (optical isomers) exhibit different
biological activities?
difference in biologic activity may be due to a difference in the distribution of the isomers or to a difference in the properties of the drug-receptor combination of less them the optimal number of binding groups is suitably located for binding. 2、静脉注射
4、The finding of a novel drug molecule is a long, expensive, and tortuous process with no guarantee of success. Clearly, out of the almost in finite number of possible compounds, only a finite(few, small) number can ever be selected for testing within a given time and the skill of medicinal chemist is in deciding which of those compounds to make first. Of course, there is then the major problem of how to synthesize them! In order to make that decision, the mass of biological data produced for compounds already tested needs to be analyzed in such a way that features which are important for the biological activity/activities can be identified and then for future molecules. The goal of quantitative structure-activity relationship (QSAR) is to find predicative effect between quantitative descriptions of physical properties of compounds and the response of the biological system under consideration. Hopefully the resulting QSAR will lead to an definition of the molecular features/properties most important in derterming activity, and guide the research of biological activity within the compound series.
发现了新的药物分子是一个长期的,昂贵的,曲折的过程没有成功的保证。显然,出了几乎无限多的可能,只有有限的(很少,小)数量能被选定为测试在给定的时间和技能的药用化学家在决定哪些是这些化合物使第一。当然,有那么主要问题是如何合成!为了使这一决定,大规模的生物数据产生的化合物已经测试需要分析的方式,特点,是重要的生物活性/活动可确定,然后为未来的分子。目的定量构效关系(构效关系)是找到预测作用之间的定量描述化合物的物理性质和反应的生物系统的思考。希望由此产生的构效关系将导致一个定义的分子功能/性能最重要的derterming活动,并指导研究生物活性的化合物系列。 Unit11 P120
1、Answer the following questions:
(1)How many kinds of the route of drug administration are there? ①oral route②parenteral route③topical route
(2)Can you present these usual dosages for us of the drug that are administered orally?
①tablets②capsules③liquid oral
(3)How is an evaluation of a tablet’s properties made?
The actual physical design, manufacturing pracess, and complete chemical makeup of the tablet can have a profound effect on the efficacy of the drug being administered 2、Solid oral dosage forms are delivery systems presented as solid dose units readily administered by mouth. The group includes tablets, capsules, pills, and turunda(suppository), as well as bulk or unit-dose powder and granules. The group constitutes the most popular form of presentation, and tablets and capsules account for the greatest number of preparations in this category. The prime
reasons for this popularity includes: easy of accurate (yet versatile) measurement, good physical and chemical stability, competitive unit production costs, and an elegant distinctive appearance resulting in a high level of patient acceptability. Among the potential disadvantages are irritant effects on the gastrointestinal mucosa by some solids and the possibility of bioavailability problems caused by the fact that both effectivity (in most causes) and stability must take place before the drug is a available for absorption.
固体口服剂型的运载系统作为固体剂量单位容易管理的嘴。该集团包括片剂,胶囊,丸,和栓剂(栓),以及体积或单位剂量的粉末和颗粒。该组的最流行的形式,介绍,和片剂和胶囊占最大数量的筹备工作在这个类别。主要原因包括:容易普及准确(但多才多艺)测量,物理和化学稳定性好,具有竞争力的单位生产成本,和优雅的独特的外观,导致高水平的病人接受。其中潜在的缺点是刺激性影响胃肠粘膜的某些固体和可能的生物利用度的问题造成的事实,既有效性(在大多数的原因)和稳定之前必须发生的药物是一种可吸收。 4、片剂 Unit12 P127
1、Answer the following questions:
(1)Have you ever know the general methods and processes of the manufacture of tablet? Yes
(2)What is the importance of manufacture granulation which tables are made from?
Such as compactness, physical stabiling, rapod production, capubilty chemical stability and efficacy, are in general distated primarily by the qualities of the granmlation from which it is made
(3)What components are included in general excipients in a tablet’s formula? All nondrug components
(4) Have you understood the principle of tablet compression operation?
2、One of the commonly used dosage forms oral is tablet, the components in tablet’s formulation include general diluent, binder, disintegrant, lubricant, and making the granulation is an important process of tablet’s manufacture, the characteristics of a tablet depend basically on the qualities of the granulation, which must possess two characteristic: fluid ity and compressibi lity
.The wet g ranulation is a commonly used method of granulation, which involves wet massing of the powers, wet sizing or milling and drying. The idesl physical form of tablet materials is spheres .unfortunately, most materials do not asily form spheres, which must be processed by granulation for forming sphere like or regularly shaped agg regates.
一个常用的剂型口服片剂,片剂的配方成分包括稀释剂,粘合剂,崩解剂,润滑剂,和造粒的过程是一个重要的片的制作,特色的一片基本上取决于质量的造粒,其必须具备的特征:流动性和可压缩性。湿造粒方法常用的是肉芽组织,其中包括湿集结的权力,或研磨和干燥的湿上浆。理想的物理形式的片材料领域。不幸的是,大多数材料不容易形成领域,必须处理的肉芽组织形成球形或定期形成聚集体。 4 粒子
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