制藥工程專(zhuān)業(yè)英語(yǔ)--1單元

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)依據(jù)其生產(chǎn)或來(lái)源，藥物制劑可以分為三類(lèi)：I.完全的合成材料（人工合成材料），II.天然產(chǎn)物，和III.源自部分合成的產(chǎn)品（半合成產(chǎn)品）。2. The emph

2、asis of the present book is on the most important compounds of groups I and III-thus Drug synthesis.翻譯：所以本書(shū)的重點(diǎn)是I和III部分的藥物合成。本書(shū)的重點(diǎn)是在于和類(lèi)中最重要的化合物藥物合成。3. This does not mean, however , that natural products or other agents are less important.然而這并不意味著，天然產(chǎn)物和其他試劑不重要。4. they can serve as 

3、valuable lead structures,  and they are frequently  needed as starting materials or as intermediates for important synthetic products.它們可以作為有價(jià)值的先導(dǎo)結(jié)構(gòu)，他們常常作為重要的合成產(chǎn)品的起始原料或中間體產(chǎn)品。5：Table 1 gives an overview of the d

4、ifferent methods for obtaining pharmaceutical agents. 表1列出了獲取藥物制劑的不同方法的概述。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.最初從天然資源庫(kù)獲得的幾個(gè)重要治療作用的天然產(chǎn)品，今天可以通過(guò)全合成更有效地

5、，即更經(jīng)濟(jì)地被制備出來(lái)。7.Such example include L-amino acids, Chloramphenicol , Caffeine, Dopamine, Epinephrine, Levodopa, peptide hormorres, Prostaglandins, D-Penicillamine, Vincamine, and practically all vitamins. 這樣的例子包括L-氨基酸、氯霉素、咖啡因、多巴胺、腎上腺素、左旋多巴、肽類(lèi)激素、前列腺素、D -青霉胺、長(zhǎng)春胺，以及幾乎所有的維生素。8.Over the last few years fer

6、mentationi.e. microbiological processeshas become extremely important.在過(guò)去的幾年里，發(fā)酵，即微生物過(guò)程，變得極其重要。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.通過(guò)現(xiàn)代技術(shù)和基因選擇導(dǎo)致的微生物的高性能突異變種的結(jié)果，發(fā)酵已成為選擇寬范圍物質(zhì)的方法。 10.Both Eukaryonts (yeasts and moulds) and Prokaryonts (single bacterial cells,and actinomycetes) are used as microorganisms . 真核細(xì)胞（酵母菌和霉菌）和原核細(xì)胞（單細(xì)胞細(xì)菌，放線菌）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)翻譯：下列產(chǎn)品類(lèi)型可以得到：    1。細(xì)胞的物質(zhì)（單細(xì)胞蛋白），  2。酶， 3。初級(jí)降解產(chǎn)物（初級(jí)代謝物），  4。二級(jí)降解產(chǎn)物（次生代謝物）。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.盡管

10、從諸如腸膜狀明串球菌的某些微生物的黏膜可以生產(chǎn)葡萄聚糖，但第2和3類(lèi)產(chǎn)品類(lèi)型只與藥品生產(chǎn)的有關(guān)。  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5萬(wàn)10萬(wàn)，可用作血漿代用品。 14.Among the primary metabolites the L-amino acids from mutants of  Cory

11、nebacterium glutamicum and Brevibacterium flavum are especially  interesting.而來(lái)自谷氨酸棒桿菌和黃色短桿菌突變體的初級(jí)代謝產(chǎn)物中，L-氨基酸尤其令人感興趣。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. 從這些生物體中，可以生產(chǎn)約35萬(wàn)噸L-谷氨酸單鈉鹽（味精，食品添加劑）和約70,000噸L-賴(lài)氨酸（用于植物蛋白補(bǔ)充物質(zhì)）。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，重要的初級(jí)代謝產(chǎn)物還有嘌呤核苷酸、有機(jī)酸、乳酸、檸檬酸和維生素，例如源自謝氏丙酸桿菌

13、的維生素B12。17、Among the secondary metabolites the antibiotics must be mentioned first.在次生代謝產(chǎn)物中首先必須提到的是抗生素。 18、The following five groups represent a yearly worldwide value of US-17 billion:以下五組藥品代表了全球每年價(jià)值170億美元：penicillins (Penicillium chrysogenum),青霉素（青霉）cephalosporins (Cephalosporium acremonium),

14、頭孢菌素（頭孢枝頂）tetracyclines (Streptomyces aureofaciens),四環(huán)素（金色鏈霉菌）erythromycins (Streptomyces erythreus),紅霉素類(lèi)（紅霉素鏈霉菌）aminoglycosides(e.g.streptomycin from Streptomyces griseus).氨基糖苷類(lèi)（如 鏈霉素從灰色鏈霉菌）19.About 5000 antibiotics have already been isolated from microorganisms, but of these only somewhat fewer th

15、an 100 are in therapeutic use.從微生物中已分離出約5000種抗生素，但其中只有不到100種有治療用途。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，必須記住，許多衍生物已通過(guò)部分合成法來(lái)修飾以

16、獲得治療用途；在過(guò)去的十年里，采用半合成方法已從ß-內(nèi)酰胺獲得了約50,000種制劑。21. To avoid contamination of the microorganisms with phages etc , the whole process has to be performed under sterile conditions.為了避免受到噬菌體等微生物的污染，（發(fā)酵）全過(guò)程都必須在無(wú)菌條件下進(jìn)行。22. Fermentations are carried out in stainless steel fermenters with volumes up to 400

17、 m3.發(fā)酵是在體積高達(dá)400m3的不銹鋼發(fā)酵罐中進(jìn)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，發(fā)酵只在有氧條件下才能發(fā)生；因此，需要提供有足夠量的氧氣或（無(wú)菌）空氣。23.Carbon dioxide sources include carbohydrates ,e.g. molasses, saccharides, and glucose.二氧化碳的

18、來(lái)源包括糖類(lèi)（碳水化合物），如廢糖漿、低聚糖類(lèi)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，微生物必須要培養(yǎng)在有含氮化合物的生長(zhǎng)培養(yǎng)基中，例如，硫酸銨，氨水或者尿素，也需要無(wú)機(jī)磷酸鹽。24. Furthermore，constant optimal

19、 pH and temperature are required.此外，必需有的恒定的最適pH值和溫度。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為例，發(fā)酵過(guò)程在200小時(shí)后完成，細(xì)胞群經(jīng)過(guò)濾而分離。26. The desired active agents are isolated from the filtrate by absorption or extraction pr

20、ocesses 從濾液中經(jīng)吸收或提取工藝而分離出所需要的活性制劑。利用吸附或者萃取工藝將需要的活性物質(zhì)從濾液中分離。27.The cell mass, if not the desired product, can be further used as an animal feedstuff owing to its high protein content.細(xì)胞群，如果并非目的產(chǎn)品，由于其高蛋白質(zhì)含量，可進(jìn)一步用作動(dòng)物飼料 。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. 利用現(xiàn)代重組技術(shù)，已獲得的微生物可以生產(chǎn)原始基因中并未編碼的多肽。利用現(xiàn)代的重組技術(shù)，可以獲得能夠生產(chǎn)其本身沒(méi)有編碼該基因的肽類(lèi)的微生物。29.       Modified E.coli bacteria make it thus possible to produce Aand Bchains of human insulin or proinsulin analogs 修飾過(guò)的

22、大腸桿菌使得產(chǎn)生人類(lèi)胰島素或前胰島素原類(lèi)似物的A-和B-鏈成為可能。30.The disulfide bridges are formed selectively after isolation ,and the final purification is effected by chromatographic procedures.經(jīng)分離后再選擇性形成二硫鍵，其最終提純由色析（譜）工序來(lái)實(shí)現(xiàn)。胰島素分離后可以選擇性地形成二硫鍵，最終的提純可以通過(guò)色譜分離過(guò)程實(shí)現(xiàn)。31.In the way human insulin is obtained totally independently fro

23、m any pancreatic material taken from animals.通過(guò)這種方式，完全可以不受限制地從任意的動(dòng)物胰腺原料獲得人類(lèi)胰島素。利用這種方法可以完全不依賴(lài)任何動(dòng)物來(lái)源的胰腺材料獲得人胰島素。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，如人生長(zhǎng)激素（HGH），神經(jīng)活性肽，生長(zhǎng)抑素，干擾素，組織纖溶酶原激活劑（TPA），淋巴因子，鈣調(diào)節(jié)劑如鈣調(diào)蛋白，蛋白疫苗，以及作為診斷用的單克隆抗體，也是采用這種方法合成的。33.The enzymes or enzymatic systems  whi

25、ch are present in a singlemicroorganism can be used for directed stereospecific and regiospecific chemical reactions. 在單一的微生物中所存在的酶或酶系統(tǒng)可用于定向的立體專(zhuān)一性和區(qū)域?qū)Ｒ恍缘幕瘜W(xué)反應(yīng)。在單細(xì)胞微生物中存在的酶或酶體系可以用于定向的立體選擇性和區(qū)域選擇性的化學(xué)反應(yīng)。34.This principle is e

26、specially useful in steroid chemistry.這個(gè)原理在類(lèi)固醇化學(xué)反應(yīng)中特別有用。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這里我們僅僅只提及黃體酮的微生物11-位羥基化反應(yīng)制得11-羥基黃體酮，一種用于合成可的松的關(guān)鍵產(chǎn)品。這里我們僅僅涉及黃體酮的微生物11-a-羥基化生成11-a-羥基黃體酮，11-a-羥基黃體酮是一種合

27、成可的松的關(guān)鍵產(chǎn)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。如今分離出的酶很

28、重要的，不僅因?yàn)榈矸鄣拿阜ㄌ腔夹g(shù)和葡萄糖異構(gòu)化成果糖的重要性 。 如今分離的酶是重要的，不僅僅因?yàn)槊复呋牡矸鄣奶腔推咸烟堑焦堑漠悩?gòu)化技術(shù)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它們?cè)诖罅吭\斷疾病的檢測(cè)程序和監(jiān)測(cè)治療的酶法分析過(guò)程中也很重要。38.A number of enzymes are themselves used as active ingredients.許多酶本身可以被作為活性成分。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劑產(chǎn)品，大多與合成的抗酸劑相配合以促進(jìn)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 鏈激酶和尿激酶在溶解血栓劑中是重要的，而天冬酰胺酶用作治療白血病中的細(xì)胞生長(zhǎng)抑制劑。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為生物催化劑在化學(xué)反應(yīng)中的應(yīng)用，在化學(xué)反應(yīng)中，酶的立體專(zhuān)一性和選擇性可以被使用。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?；?D,L-氨基酸的外消旋體而生成L-氨基酸，從芐基青霉素經(jīng)青霉素酰胺酶作用生

34、產(chǎn)6-氨基青霉烷酸，以及天門(mén)冬氨酸酶催化立體專(zhuān)一性的氨水和反丁烯二酸加成反應(yīng)以生產(chǎn)L-天門(mén)冬氨酸。 43.In these applications the enzymes can be used in immobilized forms somehow bound to carriers- and used as heterogeneous catalysts.在這些應(yīng)用中，酶可以以某種方式連接在載體上，以固定化的形式來(lái)使用，也可以用作多相催化劑。44.This is advantageous because they can then easily be separated from th

35、e reaction medium and recycled for further use.因?yàn)楣潭ɑ缚梢院苋菀讖姆磻?yīng)介質(zhì)中分離并回收再利用，這是固定化酶的優(yōu)勢(shì)。45.Another important process depending on the specific action of proteases is applied for the production of semisynthetic human insulin。依賴(lài)于蛋白酶的特殊功能的另一個(gè)重要工藝是應(yīng)用于半合成人胰島素的生產(chǎn)。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.這從豬胰島素開(kāi)始，其中在鏈的30-位的丙氨酸由于胰蛋白酶的選擇性作用下被蘇氨酸叔丁基酯替換。47.This insulin ester is separated, hydrolyzed to human insulin and finally purif

37、ied chromatographic procedures  這種被分離的胰島素酯，水解為人胰島素，最后經(jīng)色譜層析過(guò)程而純化。  48. Sources for enzymes include not only microorganisms but also vegetable and animal materials. 酶的來(lái)源不僅包括微生物，也包括植物和動(dòng)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，已經(jīng)顯示，有超過(guò)75藥物制劑是經(jīng)全合成而獲得的。50.Therefore knowledge of the synthetic routes is useful. 因此，合成路線的知識(shí)是有用的 .51. Understanding also makes it possible to recognize contamination of the agents by intermediate and by products這樣的理解也使我們能夠識(shí)別出中間體和副產(chǎn)品對(duì)制劑的污染成為可能。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. 為了有效的質(zhì)量控制，許多國(guó)家的登記機(jī)關(guān)要求有生產(chǎn)工藝過(guò)程中完整的證明文件，來(lái)作為注冊(cè)藥物的基本要素。53.Knowledge of drug syntheses provides the R&D chemist with valuable stimulation as well。藥

40、物合成的知識(shí)也給研發(fā)化學(xué)家提供了有益的鼓勵(lì)。54.There are neither preferred structural classes for all pharmaceutically active compounds nor preferred reaction types。這里既沒(méi)有首選的所有具有藥物活性組分的結(jié)構(gòu)類(lèi)型，也沒(méi)有推薦的反應(yīng)類(lèi)型。55.This implies that pracyically the whole field of organicand in part also organometallic chemistry is covered.這意味著（藥物合成知

41、識(shí)）幾乎涉及了有機(jī)化學(xué)和部分金屬有機(jī)化學(xué)領(lǐng)域。56.英語(yǔ)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間體更為常用；所以了解從初始化合物制備它們的可能性是有用的。57. For this reason it is appropriate som

42、ewhere in this book to illustrate a tree of especially important intermediates.基于這個(gè)原因，在本書(shū)闡明特別重要的中間體的制備是合適的。58.These latter intermediates are the key compounds used in synthetic processes leading to an enormous number of agents這些后面的中間體在

43、大量的制劑合成過(guò)程中是關(guān)鍵的化合物。59. For the most part chemicals are involved which are producted in large amounts .因?yàn)椋ê竺娴闹虚g體）涉及了大部分產(chǎn)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，對(duì)基于工業(yè)化的芳香族化合物甲苯、苯酚和氯苯的中間體，這也是確切

44、的。61Further key compounds may be shown in a table which can be useful in tracing cross-relationships in syntheses.更多的關(guān)鍵化合物可以在表中顯示，這個(gè)表在追蹤化學(xué)合成的交叉關(guān)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.除了實(shí)際的起始原料和中間體，作為反應(yīng)溶媒和重結(jié)晶純化都需要溶劑。63.Frequently used solvents are methanol，ethanol，isopropanol，butanol，acetone，ethyl acetate，benzene，toluene and xylene.常用的溶劑是甲醇、乙醇、異丙醇、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.在較小程度上，乙醚、四氫呋喃、乙二醇醚、N,N-二甲基甲酰胺（DMF）和二甲基亞砜（DMSO）用于特殊的反應(yīng)。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).大量使用的試劑，不僅是酸（鹽酸，硫酸，硝酸，醋酸），還有無(wú)機(jī)和有機(jī)堿（氫氧化鈉、氫氧化鉀、碳酸鉀、碳酸氫鈉、氨水、三乙胺、吡啶）。66.Further auxiliary chemicals include active charcoal and catalysts.此外的輔助化學(xué)藥品包括活性炭和催化劑。67. All of these supplementary chemicals (like the intermediates) can be a source of imp

48、urities in the final product.所有這些輔助的化學(xué)藥品（像中間體）都可能成為最終產(chǎn)物雜質(zhì)的來(lái)源。 68.In 1969 the WHO published a treatise on Safeguarding Quality in Drugs'.1969年，世界衛(wèi)生組織（WHO）出版了“藥品質(zhì)量安全管理”的專(zhuān)題論文。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).附錄二涉及“正確的制備程序和藥品質(zhì)量安全管理”（參見(jiàn)世界衛(wèi)生組織技術(shù)報(bào)告NO. 418，1969年，附錄二；技術(shù)報(bào)告NO. 567，1975年，附錄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