制药工程专业英语--1单元

1、Unit 11. Depending on their production or origin pharmaceutical agents can be split into three groups: Totally synthetic material (synthetics) Natural products ,and Product from partial syntheses (semi-synthetic products)依据其生产或来源，药物制剂可以分为三类：I.完全的合成材料（人工合成材料），II.天然产物，和III.源自部分合成的产品（半合成产品）。2. The emph

2、asis of the present book is on the most important compounds of groups I and III-thus Drug synthesis.翻译：所以本书的重点是I和III部分的药物合成。本书的重点是在于和类中最重要的化合物药物合成。3. This does not mean, however , that natural products or other agents are less important.然而这并不意味着，天然产物和其他试剂不重要。4. they can serve as 

3、valuable lead structures,  and they are frequently  needed as starting materials or as intermediates for important synthetic products.它们可以作为有价值的先导结构，他们常常作为重要的合成产品的起始原料或中间体产品。5：Table 1 gives an overview of the d

4、ifferent methods for obtaining pharmaceutical agents. 表1列出了获取药物制剂的不同方法的概述。6. Several therapeutically significant natural products which were originally obtained from natural sources are today more effectively -i.e. more economically -prepared by total synthesis.最初从天然资源库获得的几个重要治疗作用的天然产品，今天可以通过全合成更有效地

5、，即更经济地被制备出来。7.Such example include L-amino acids, Chloramphenicol , Caffeine, Dopamine, Epinephrine, Levodopa, peptide hormorres, Prostaglandins, D-Penicillamine, Vincamine, and practically all vitamins. 这样的例子包括L-氨基酸、氯霉素、咖啡因、多巴胺、肾上腺素、左旋多巴、肽类激素、前列腺素、D -青霉胺、长春胺，以及几乎所有的维生素。8.Over the last few years fer

6、mentationi.e. microbiological processeshas become extremely important.在过去的几年里，发酵，即微生物过程，变得极其重要。9.through modern technology and results from genetic selection leading to the creation of high performance mutants of microorganisms, fermentation has already become the method of choice for a wide range o

7、f substances.通过现代技术和基因选择导致的微生物的高性能突异变种的结果，发酵已成为选择宽范围物质的方法。 10.Both Eukaryonts (yeasts and moulds) and Prokaryonts (single bacterial cells,and actinomycetes) are used as microorganisms . 真核细胞（酵母菌和霉菌）和原核细胞（单细胞细菌，放线菌）都可用作微生

8、物。11.The following product types can be obtained: 1. cell material (single cell protein)， 2. enzymes，3. primary degradation products (primary metabolites)翻译：下列产品类型可以得到：    1。细胞的物质（单细胞蛋白），  2。酶， 3。初级降解产物（初级代谢物），  4。二级降解产物（次生代谢物）。12:Disregarding the

9、60;production of dextran from the mucous membranes of certain microorganisms e.g. Leuconostoc mesenteroides class 2 and 3 are the relevant ones for the preparation of drugs.尽管

10、从诸如肠膜状明串球菌的某些微生物的黏膜可以生产葡萄聚糖，但第2和3类产品类型只与药品生产的有关。  13Dextran itself , with a molecular weight of 50,000100,000, is used as a blood plasma substitute.葡聚糖自身的分子量5万10万，可用作血浆代用品。 14.Among the primary metabolites the L-amino acids from mutants of  Cory

11、nebacterium glutamicum and Brevibacterium flavum are especially  interesting.而来自谷氨酸棒杆菌和黄色短杆菌突变体的初级代谢产物中，L-氨基酸尤其令人感兴趣。15.From these organisms some 350000 tones of monosodium L-glutamate (food additive)and some 70000 tones of L-lysine(supplement for vegetable protein

12、s)are produced. 从这些生物体中，可以生产约35万吨L-谷氨酸单钠盐（味精，食品添加剂）和约70,000吨L-赖氨酸（用于植物蛋白补充物质）。16Further important primary metabolites are the purina nucleotides，organic acids， lactic acid，citric acid，and vitamins，for example vitamin B,12 from Propionibacterium shermanii.此外，重要的初级代谢产物还有嘌呤核苷酸、有机酸、乳酸、柠檬酸和维生素，例如源自谢氏丙酸杆菌

13、的维生素B12。17、Among the secondary metabolites the antibiotics must be mentioned first.在次生代谢产物中首先必须提到的是抗生素。 18、The following five groups represent a yearly worldwide value of US-17 billion:以下五组药品代表了全球每年价值170亿美元：penicillins (Penicillium chrysogenum),青霉素（青霉）cephalosporins (Cephalosporium acremonium),

14、头孢菌素（头孢枝顶）tetracyclines (Streptomyces aureofaciens),四环素（金色链霉菌）erythromycins (Streptomyces erythreus),红霉素类（红霉素链霉菌）aminoglycosides(e.g.streptomycin from Streptomyces griseus).氨基糖苷类（如 链霉素从灰色链霉菌）19.About 5000 antibiotics have already been isolated from microorganisms, but of these only somewhat fewer th

15、an 100 are in therapeutic use.从微生物中已分离出约5000种抗生素，但其中只有不到100种有治疗用途。20.It must be remembered，however that many derivatives have been modified by partial synthesis for therapeutic use some 50,000 agents have been semisythetically obtained from -lactams alone in the last decade.但是，必须记住，许多衍生物已通过部分合成法来修饰以

16、获得治疗用途；在过去的十年里，采用半合成方法已从ß-内酰胺获得了约50,000种制剂。21. To avoid contamination of the microorganisms with phages etc , the whole process has to be performed under sterile conditions.为了避免受到噬菌体等微生物的污染，（发酵）全过程都必须在无菌条件下进行。22. Fermentations are carried out in stainless steel fermenters with volumes up to 400

17、 m3.发酵是在体积高达400m3的不锈钢发酵罐中进行。23.Since the more important fermentations occur exclusively under aerobic conditions a good supply of oxygen or air(sterile)is needed.由于更重要的是，发酵只在有氧条件下才能发生；因此，需要提供有足够量的氧气或（无菌）空气。23.Carbon dioxide sources include carbohydrates ,e.g. molasses, saccharides, and glucose.二氧化碳的

18、来源包括糖类（碳水化合物），如废糖浆、低聚糖类和葡萄糖。24.Additionally the microorganisms must be supplied in the growth medium with nitrogen-containing compounds such as ammonium sulfate, ammonia , or urea , as well as with inorganic phosphates.另外，微生物必须要培养在有含氮化合物的生长培养基中，例如，硫酸铵，氨水或者尿素，也需要无机磷酸盐。24. Furthermore，constant optimal

19、 pH and temperature are required.此外，必需有的恒定的最适pH值和温度。25.In the case of penicillin G , the fermentation is finished after 200 hours , and the cell mass is separated by filtration.以青霉素G为例，发酵过程在200小时后完成，细胞群经过滤而分离。26. The desired active agents are isolated from the filtrate by absorption or extraction pr

20、ocesses 从滤液中经吸收或提取工艺而分离出所需要的活性制剂。利用吸附或者萃取工艺将需要的活性物质从滤液中分离。27.The cell mass, if not the desired product, can be further used as an animal feedstuff owing to its high protein content.细胞群，如果并非目的产品，由于其高蛋白质含量，可进一步用作动物饲料 。28.By modern recombinant techniques microorganisms have been obtained which also all

21、ow production of peptides which were not encoded in the original genes. 利用现代重组技术，已获得的微生物可以生产原始基因中并未编码的多肽。利用现代的重组技术，可以获得能够生产其本身没有编码该基因的肽类的微生物。29.       Modified E.coli bacteria make it thus possible to produce Aand Bchains of human insulin or proinsulin analogs 修饰过的

22、大肠杆菌使得产生人类胰岛素或前胰岛素原类似物的A-和B-链成为可能。30.The disulfide bridges are formed selectively after isolation ,and the final purification is effected by chromatographic procedures.经分离后再选择性形成二硫键，其最终提纯由色析（谱）工序来实现。胰岛素分离后可以选择性地形成二硫键，最终的提纯可以通过色谱分离过程实现。31.In the way human insulin is obtained totally independently fro

23、m any pancreatic material taken from animals.通过这种方式，完全可以不受限制地从任意的动物胰腺原料获得人类胰岛素。利用这种方法可以完全不依赖任何动物来源的胰腺材料获得人胰岛素。32.Other important peptides ,hormones ,and enzymes, such as human growth hormone(HGH),neuroma give peptides, somatostatin, interferons, tissue plasminogen activator(TPA), lymphokines ,calciu

24、m regulators like calmodulin, protein vaccines ,as well as monoclonal antibodies used as diagnostics ,are synthesized in this way.其他重要的肽，激素和酶，如人生长激素（HGH），神经活性肽，生长抑素，干扰素，组织纤溶酶原激活剂（TPA），淋巴因子，钙调节剂如钙调蛋白，蛋白疫苗，以及作为诊断用的单克隆抗体，也是采用这种方法合成的。33.The enzymes or enzymatic systems  whi

25、ch are present in a singlemicroorganism can be used for directed stereospecific and regiospecific chemical reactions. 在单一的微生物中所存在的酶或酶系统可用于定向的立体专一性和区域专一性的化学反应。在单细胞微生物中存在的酶或酶体系可以用于定向的立体选择性和区域选择性的化学反应。34.This principle is e

26、specially useful in steroid chemistry.这个原理在类固醇化学反应中特别有用。35、Here we may refer only to the microbes in eleven to 11 hydroxy progesterone xylation hydropower, a key product in the synthesis of cortisone这里我们仅仅只提及黄体酮的微生物11-位羟基化反应制得11-羟基黄体酮，一种用于合成可的松的关键产品。这里我们仅仅涉及黄体酮的微生物11-a-羟基化生成11-a-羟基黄体酮，11-a-羟基黄体酮是一种合

27、成可的松的关键产品。36.Isolated enzymes are important  today not only because of the importance of enzymatic saccharification technology of starch and the isomerization of glucose to fructose。如今分离出的酶很

28、重要的，不仅因为淀粉的酶法糖化技术和葡萄糖异构化成果糖的重要性 。 如今分离的酶是重要的，不仅仅因为酶催化的淀粉的糖化和葡萄糖到果糖的异构化技术方面的重要性，37.They are also significant in the countless test procedures used in diagnosing illness,and in enzymatic analysis which is used

29、60;in the monitoring of therapy它们在大量诊断疾病的检测程序和监测治疗的酶法分析过程中也很重要。38.A number of enzymes are themselves used as active ingredients.许多酶本身可以被作为活性成分。39,Thus preparations containing proteases (e.g.chymotrypsin,pepsin,and trypsin),amylases and lipases,m

30、ostly in combination with synthetic antacids,promote digestion因此，包含蛋白酶（如胰凝乳蛋白酶，胃蛋白酶和胰蛋白酶），淀粉酶和脂肪酶的制剂产品，大多与合成的抗酸剂相配合以促进消化。40,StreptoKinase and urokinase are important in thrombolytics,and asparaginase is used as a

31、60;cytostantic agent in the treament of leukemia 链激酶和尿激酶在溶解血栓剂中是重要的，而天冬酰胺酶用作治疗白血病中的细胞生长抑制剂。41,Finally mention must be made of the important use of enzymes as 'biocatalysts' in chemical re

32、actions where their stereospecificity and selectivity can be used . 最后提到的一定是酶作为生物催化剂在化学反应中的应用，在化学反应中，酶的立体专一性和选择性可以被使用。42.Known examples are the enzymatic cleavage of racemates of N-acety-D,L-amino acid

33、0;to give L-amino acids the production of 6-aminopenicillanic acid from benzylpenicillin by means of penicillinamidase and the aspartase-catalysed stereospecific addition of ammonia to fumaric acid in order to produce L-aspartic acid.著名例子有酶裂解N-乙酰基-D,L-氨基酸的外消旋体而生成L-氨基酸，从苄基青霉素经青霉素酰胺酶作用生

34、产6-氨基青霉烷酸，以及天门冬氨酸酶催化立体专一性的氨水和反丁烯二酸加成反应以生产L-天门冬氨酸。 43.In these applications the enzymes can be used in immobilized forms somehow bound to carriers- and used as heterogeneous catalysts.在这些应用中，酶可以以某种方式连接在载体上，以固定化的形式来使用，也可以用作多相催化剂。44.This is advantageous because they can then easily be separated from th

35、e reaction medium and recycled for further use.因为固定化酶可以很容易从反应介质中分离并回收再利用，这是固定化酶的优势。45.Another important process depending on the specific action of proteases is applied for the production of semisynthetic human insulin。依赖于蛋白酶的特殊功能的另一个重要工艺是应用于半合成人胰岛素的生产。46.This starts with pig insulin in which the al

36、anine in the 30-position of the-chain is replaced by a threonine tert -butyl ester by the selective action of trypsin.这从猪胰岛素开始，其中在链的30-位的丙氨酸由于胰蛋白酶的选择性作用下被苏氨酸叔丁基酯替换。47.This insulin ester is separated, hydrolyzed to human insulin and finally purif

37、ied chromatographic procedures  这种被分离的胰岛素酯，水解为人胰岛素，最后经色谱层析过程而纯化。  48. Sources for enzymes include not only microorganisms but also vegetable and animal materials. 酶的来源不仅包括微生物，也包括植物和动物材料49.In Table 1 it was already shown that over 75% of all pharmaceutical agents are obt

38、ained by total synthesis在表1中，已经显示，有超过75药物制剂是经全合成而获得的。50.Therefore knowledge of the synthetic routes is useful. 因此，合成路线的知识是有用的 .51. Understanding also makes it possible to recognize contamination of the agents by intermediate and by products这样的理解也使我们能够识别出中间体和副产品对制剂的污染成为可能。52For the reason of effectiv

39、e quality control the registration authorities in many countries demand as essentials for registration a thorough documentation on the production process. 为了有效的质量控制，许多国家的登记机关要求有生产工艺过程中完整的证明文件，来作为注册药物的基本要素。53.Knowledge of drug syntheses provides the R&D chemist with valuable stimulation as well。药

40、物合成的知识也给研发化学家提供了有益的鼓励。54.There are neither preferred structural classes for all pharmaceutically active compounds nor preferred reaction types。这里既没有首选的所有具有药物活性组分的结构类型，也没有推荐的反应类型。55.This implies that pracyically the whole field of organicand in part also organometallic chemistry is covered.这意味着（药物合成知

41、识）几乎涉及了有机化学和部分金属有机化学领域。56.英语原文：Neverthelese,a larger number of starting materials and intermediates are more frequently used,and so it is useful to know the possibilities for their preparration from primary chemicals.然而，大量的起始原料和中间体更为常用；所以了解从初始化合物制备它们的可能性是有用的。57. For this reason it is appropriate som

42、ewhere in this book to illustrate a tree of especially important intermediates.基于这个原因，在本书阐明特别重要的中间体的制备是合适的。58.These latter intermediates are the key compounds used in synthetic processes leading to an enormous number of agents这些后面的中间体在

43、大量的制剂合成过程中是关键的化合物。59. For the most part chemicals are involved which are producted in large amounts .因为（后面的中间体）涉及了大部分产量巨大的化合物。60.In a similar way this is also true for the intermediates based on the industrial aromatic compounds toluene, phenol and chlorobenzene.相似的情形，对基于工业化的芳香族化合物甲苯、苯酚和氯苯的中间体，这也是确切

44、的。61Further key compounds may be shown in a table which can be useful in tracing cross-relationships in syntheses.更多的关键化合物可以在表中显示，这个表在追踪化学合成的交叉关系中有用。62In addition to the actual starting materials and intermediates solvents are required both as a reaction medium and , for purification via recrystalli

45、zation.除了实际的起始原料和中间体，作为反应溶媒和重结晶纯化都需要溶剂。63.Frequently used solvents are methanol，ethanol，isopropanol，butanol，acetone，ethyl acetate，benzene，toluene and xylene.常用的溶剂是甲醇、乙醇、异丙醇、丁醇、丙酮、醋酸乙酯、苯、甲苯和二甲苯。 64.To a lesser extent diethyl ether，tetrahydrofuran，glycol ethers，dimethylformamide (DMF) and dimethyl sul

46、phoxide (DMSO) are used in special reactions.在较小程度上，乙醚、四氢呋喃、乙二醇醚、N,N-二甲基甲酰胺（DMF）和二甲基亚砜（DMSO）用于特殊的反应。65.Reagents used in larger amounts are not only acids (hydrochloric acid，sulfuric acid， nitric acid，acetic acid) but also inorganic and organic bases (sodium hydroxide，potassium hydroxide，potassium ca

47、rbonate，sodium bicarbonate，ammonia，triethylamine，pyridine).大量使用的试剂，不仅是酸（盐酸，硫酸，硝酸，醋酸），还有无机和有机碱（氢氧化钠、氢氧化钾、碳酸钾、碳酸氢钠、氨水、三乙胺、吡啶）。66.Further auxiliary chemicals include active charcoal and catalysts.此外的辅助化学药品包括活性炭和催化剂。67. All of these supplementary chemicals (like the intermediates) can be a source of imp

48、urities in the final product.所有这些辅助的化学药品（像中间体）都可能成为最终产物杂质的来源。 68.In 1969 the WHO published a treatise on Safeguarding Quality in Drugs'.1969年，世界卫生组织（WHO）出版了“药品质量安全管理”的专题论文。69.Appendix 2 is concerned with the Proper Practice for Reparation and Safeguarding Quality in Drugs' (WHO Technical Report No. 418，1969，Appendix 2;No. 567，1975，Appendix 1A).附录二涉及“正确的制备程序和药品质量安全管理”（参见世界卫生组织技术报告NO. 418，1969年，附录二；技术报告NO. 567，1975年，附录1A）。 70.This has in the meantime become known as Good Manufacturing Practices' or GMP rules，and these should now be obeyed in drug p