制药工程专业英语 7单元

Unit 1 Production of DrugsAbout 5000 antibiotics have already been isolated from microorganisms，but of these only somewhat fewer than 100 are in therapeutic use. It must be remembered，however，that many derivatives have been modified by partial synthesis for therapeutic use;some 50，000 agents have been semisynthetically obtained from户lactams alone in the last decade. Fermentations are carried out in stainless steel fermentors with volumes up to 400 m3. To avoid contamination of the microorganisms with phages etc. the whole process has to be performed under sterile conditions. Since the more important fermentations occur exclusively under aerobic conditions a good supply of oxygen or air(sterile)is needed. Carbon dioxide sources include carbohydrates，e. g. molasses，saccharides，and glucose. 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. Furthermore，constant optimal pH and temperature are required. In the case of penicillin G，the fermentation is finished after 200 hours，and the cell mass is separated by filtration. The desired active agents are isolated from the filtrate by absorption or extraction processes. The cell mass，if not the desired product，can be further used as an animal feedstuff owing to its high protein content.关于5000抗生素已经分离出的微生物，但其中只有不到100有些治疗使用。

制药工程专业英语Unit 1production of drugs P1单词Compound 化合物intermediate 中间产物alkaloids 生物碱enzymes酶peptide 肽hormones 荷尔蒙modification 修饰chloramphenicol 氯霉素metabolites 代谢物substitute 替代品derivative衍生物active 活性absorption 吸收extraction 提取Recombinant 重组insulin 编码neuroactive 神经活性start materials 起始原料recrystallization 重结晶methanol 甲醇Ethanol 乙醇isopropanol 异丙醇butanol 丁醇benzene 苯翻译Known examples are the enzymatic cleavage of racemates of N-acetyl-D, L-amino acids 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.著名的例子是对N -乙酰- D，L -氨基酸消旋给予L -氨基酸酶裂解，从青霉素生产8 -氨基青霉烷酸的青霉素酰胺酶手段和天冬氨酸酶，催化氨立体除了富马酸为了酸生产L -天门冬氨酸。

Reading material 1 p7Antagonist 抑制剂receptor 受体clinical investigation 临床研究antibacterial抗菌的inhibition 抑制mercurial 水银dominate 占主导Unit 3 chemotherapy: an introduction P29单词chemotherapy化学治疗superstition 迷信pathogenic 致病的翻译The activity of the arsenical drugs is explained as due to a blocking of essential thiol groups.For example, lipoic acid dehydrogenase contains two cysteine molecules, while are kept near each other by folding of the molecule. As a result, an arsenical can react with these thiol groups and inactivate the molecule, as show in equation.对含砷药物活性被解释为由于阻塞必不可少的巯基。

制药工程专业英语课后练习题含答案题目一：Drug Substance Manufacturing1.What is Drug Substance Manufacturing?–A. It is the process of producing a finished drug product.–B. It is the process of producing the activeingredient or drug substance used in a drug product.–C. It is the process of packaging and labeling a finished drug product.–D. It is the process of performing clinical trials ona drug product.Answer: B. It is the process of producing the active ingredient or drug substance used in a drug product.2.What are the steps involved in Drug Substance Manufacturing?–A. Synthesis, isolation, and purification.–B. Packaging, labeling, and testing.–C. Clinical trials, manufacturing, and distribution.–D. None of the above.Answer: A. Synthesis, isolation, and purification.3.What is the mn purpose of Drug Substance Manufacturing?–A. To produce a finished drug product for human use.–B. To provide the active ingredient or drug substance used in a drug product.–C. To test and validate the safety and efficacy of a drug product.–D. To distribute a drug product to consumers.Answer: B. To provide the active ingredient or drug substance used in a drug product.题目二：Pharmaceutical Formulation1.What is Pharmaceutical Formulation?–A. It is the process of producing a finished drug product.–B. It is the process of selecting and combining ingredients to produce a drug product.–C. It is the process of packaging and labeling a finished drug product.–D. It is the process of performing clinical trials ona drug product.Answer: B. It is the process of selecting and combining ingredients to produce a drug product.2.What are the key considerations in PharmaceuticalFormulation?–A. Safety, efficacy, and stability.–B. Cost, avlability, and taste.–C. Appearance, texture, and smell.–D. None of the above.Answer: A. Safety, efficacy, and stability.3.What is the role of excipients in Pharmaceutical Formulation?–A. They are the active ingredients in a drug product.–B. They are the inactive ingredients in a drug product that help to improve its properties.–C. They are the ingredients in a drug product that are responsible for the color and flavor.–D. None of the above.Answer: B. They are the inactive ingredients in a drug product that help to improve its properties.题目三：Good Manufacturing Practice (GMP)1.What is Good Manufacturing Practice (GMP)?–A. It is a set of regulations and guidelines that ensure the quality and safety of pharmaceutical products.–B. It is a set of regulations and guidelines that ensure the efficacy of pharmaceutical products.–C. It is a set of regulations and guidelines that ensure the affordability of pharmaceutical products.–D. None of the above.Answer: A. It is a set of regulations and guidelines that ensure the quality and safety of pharmaceutical products.2.What are the key components of Good Manufacturing Practice(GMP)?–A. Quality control, documentation, and facility design.–B. Clinical trials, manufacturing, and distribution.–C. Cost control, inventory management, and customer service.–D. None of the above.Answer: A. Quality control, documentation, and facility design.3.Why is Good Manufacturing Practice (GMP) important?–A. It helps to ensure the quality and safety ofpharmaceutical products.–B. It helps to reduce the cost of producingpharmaceutical products.–C. It helps to increase the avlability ofpharmaceutical products.–D. None of the above.Answer: A. It helps to ensure the quality and safety of pharmaceutical products.总结本文介绍了制药工程专业英语中的几个重要概念和术语，包括Drug Substance Manufacturing（药品物质制造）、Pharmaceutical Formulation（制剂开发）以及Good Manufacturing Practice（良好生产规范）。

制药工程专业英语详细Unit..详细翻译————————————————————————————————作者：————————————————————————————————日期：Unit 1 Production of Drugs根据其生产或来源不同药物制剂可以分为三类：Ⅰ.人工合成材料（全合成材料）Ⅱ.天然产物，和Ⅲ.半合成天然产物（半合成药物）。

本书的重点是这些第一组和第三组化合物都是合成药物。

然而这并不意味着那些天然药物和其他药物就不重要。

他们可以作为很有价值的先导结构，并经常被用为重要合成药物的原料或中间体。

表1概述了获取药物制剂的不同方法。

Table 1 Possibilities for the preparation of drugs表1药物制备的可能性方法例子1.全合成75％以上的药物制剂都是全合成的（合成物）2.从天然产物中分离（天然产物）2.1植物生物碱;酶;强心甙；多聚糖；维生素E; 类固醇前体（薯蓣皂苷配基，谷甾醇）；柠檬醛（中间产物维生素A，E，K）2.2动物器官酶;多肽；激素;胆酸；胆汁;胰岛素来自胰腺；血清和疫苗2.3其他来源胆固醇来自羊毛油；L-氨基酸来自角蛋白和明胶水解3.发酵抗生素; L -氨基酸，葡聚糖；对甾类有定向的修饰，例如11 -羟基化;胰岛素，干扰素，抗体，肽类激素，酶，疫苗生物碱化合物；半合成内酰胺类抗生素；甾类;人胰岛素4.天然产物的半合成修改（半合成药物）几种最初来自于天然原料有治疗意义天然产物如今用更有效也就是经济的全合成法制备。

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，长春蔓胺，以及几乎所有的维生素。

在过去的几年里发酵（即微生物处理）变得极其重要。

通过现代技术和遗传选择的结果产生了高效能微生物突变株，发酵已成为广泛的底物（物质）都可以选择的一种方法。

真核微生物（酵母菌和霉菌）和原核微生物（单细胞细菌和放线菌）用于微生物。

Unit 1 Production of DrugsDepending on their production or origin pharmaceutical agents can be split into three groups:I .Totally synthetic materials (synthetics)，Ⅱ.Natural products，andⅢ.Products from partial syntheses (semi-synthetic products).The emphasis of the present book is on the most important compounds of groups I and Ⅲ一thus Drug synthesis. This does not mean，however，that natural products or other agents are less important. They can serve as valuable lead structures，and they are frequently needed as starting materials or as intermediates for important synthetic products.Table 1 gives an overview of the different methods for obtaining pharmaceutical agents.Table 1 Possibilities for the preparation of drugsMethods Examples1. Total synthesis -over 75 % of all pharmaceutical agents (synthetics)2. Isolation from natural sources (natural products):2.1 Plants -alkaloids;enzymes;heart glycosides;polysaccharides;tocopherol;steroid precursors (diosgenin, sitosterin);citral (intermediate product forvitamins A, E，and K)2.2 Animal organs一enzymes;peptide hormones;cholic acid from gall; insulin) from thepancreas;sera and vaccines2. 3 Other sources一cholesterol from wool oils;L-amino acids from keratin and gelatinehydrolysates3. Fermentation一antibiotics;L-amino acids;dextran; targeted modifications on steroids，e.g. 11-hydroxylation; also insulin, interferon, antibodies, peptidehormones，enzymes，vaccines4. Partial synthetic modification of natural products (semisynthetic agents):一alkaloid compounds;semisynthetic /3-lactam antibiotics;steroids;human insulinSeveral therapeutically significant natural products which were originally obtained from natural sources are today more effectively -i. e. more economically -prepared.. by total synthesis. Such examples include L-amino acids，Chloramphenicol，Caffeine, Dopamine，Epinephrine，Levodopa, peptide hormones，Prostaglandins，D-Penicillamine，Vincamine，and practically all vitamins.Over the last few years fermentation - i. e. microbiological processes has become extremely important. 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 of substances. Both Eukaryonts (yeasts and moulds)and Prokaryonts(single bacterial cells，and actinomycetes)are used microorganisms. The following product types can be obtained:1. cell material (single cell protein)，2. enzymes，3. primary degradation products (primary metabolites)，4. secondary degradation products (secondary metabolites).Disregarding the production of dextran from the mucous membranes of certain microorganisms，e. g. Leuconostoc mesenteroides，classes 2 and 3 are the relevant ones for the preparation of drugs. Dextran itself，with a molecular weight of 50,000 ~ 100,000，is used as a blood plasma substitute. Among the primary metabolites the L-amino acids from mutants of Corynebacterium glutamicum and Brevibacterium flavum are especially interesting. From these organisms some 350，000 tones of monosodium L-glutamate (food additive)and some 70，000 tones of L-lysine(supplement for vegetable proteins)are produced. Further important primary metabolites are the purina nucleotides，organic acids，lactic acid，citric acid，and vitamins，for example vitamin B,2 from Propionibacterium shermanii.Among the secondary metabolites the antibiotics must be mentioned first. The following five groups represent a yearly worldwide value of US-$17 billion:penicillins ( Penicillium chrysogenum )，cephalosporins ( Cephalosporium acremonium )，tetracyclines ( Streptomyces aureofaciens )，erythromycins ( Streptomyces erythreus )，aminoglycosides (e. g. streptomycin from Streptomyces griseus).About 5000 antibiotics have already been isolated from microorganisms，but of these only somewhat fewer than 100 are in therapeutic use. It must be remembered，however，that many derivatives have been modified by partial synthesis for therapeutic use;some 50，000 agents have been semisynthetically obtained from户lactams alone in the last decade. Fermentations are carried out in stainless steel fermentors with volumes up to 400 m3. To avoid contamination of the microorganisms with phages etc. the whole process has to be performed under sterile conditions. Since the more important fermentations occur exclusively under aerobic conditions a good supply of oxygen or air(sterile)is needed. Carbon dioxide sources include carbohydrates，e. g. molasses，saccharides，and glucose. 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. Furthermore，constant optimal pH and temperature are required. In the case of penicillin G，the fermentation is finished after 200 hours，and the cell mass is separated by filtration. The desired active agents are isolated from the filtrate by absorption or extraction processes. The cell mass，if not the desired product，can be further used as an animal feedstuff owing to its high protein content.By modern recombinant techniques microorganisms have been obtained which also allow production of peptides which were not encoded in the original genes. Modified E. coli bacteria make it thus possible to produce A- and B- chains of human insulin or proinsulin analogs. The disulfide bridges are formed selectively after isolation，and the final purification is effected by chromatographic procedures. In this way human insulin is obtained totally independently from any pancreatic material taken from animals.Other important peptides，hormones，and enzymes，such as human growth hormone (HGH)，neuroactive peptides，somatostatin，interferons，tissue plasminogen activator (TPA)，lymphokines，calcium regulators like calmodulin，protein vaccines，as well as monoclonal antibodies used as diagnostics，are synthesized in this way.The enzymes or enzymatic systems which are present in a single microorganism can be used for directed stereospecific and regiospecific chemical reactions. This principle is especially useful in steroid chemistry. Here we may refer only to the microbiological 11-a- hydro xylation of progesterone to 11-a-hydroxyprogesterone，a key product used in the synthesis of cortisone. Isolated enzymes are important today not only because of the technical importance of the enzymatic saccharification of starch，and the isomerization of glucose to fructose，They are also significant in the countless test procedures used in diagnosing illness，and in enzymatic analysis which is used in the monitoring of therapy.A number of enzymes are themselves used as active ingredients. Thus preparations containing proteases (e. g. chymotrypsin，pepsin，and trypsin)，amylases and lipases，mostly in combination with synthetic antacids，promote digestion. Streptokinase and urokinase are important in thrombolytics，and asparaginase is used as a cytostatic agent in the treatment of leukemia.Finally mention must be made of the important use of enzymes as `biocatalyst s’in chemical reactions where their stereospecificity and selectivity can be used. Known examples are the enzymatic cleavage of racemates of N-acetyl-D，L-amino acids to give L-amino acids，the production of 8-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.In these applications the enzymes can be used in immobilized forms-somehow bound to carriers - and so used as heterogeneous catalysts. This is advantageous because they can then easily be separated from the reaction medium and recycled for further use.Another important process depending on the specific action of proteases is applied for the production of semisynthetic human insulin. This starts with pig insulin in which the alanine in the 30-position of the B-chain is replaced by a threonine tert-butyl ester by the selective action of trypsin. The insulin ester is separated，hydrolyzed to human insulin and finally purified by chromatographic procedures.Sources for enzymes include not only microorganisms but also vegetable and animal materials.In Table 1 it was already shown that over 75%of all pharmaceutical agents are obtained by total synthesis. Thereforeknowledge of the synthetic routes is useful. Understanding also makes it possible to recognize contamination .of the agents by intermediates and by- products. For the reason of effective quality control the registration authorities in many countries demand as essentials for registration a thorough documentation on the production process. Knowledge of drug syntheses provides the R&D chemist with valuable stimulation as well.There are neither preferred structural classes for all pharmaceutically active compounds nor preferred reaction types. This implies that practically the whole field of organic and in part also organometallic chemistry is covered. Nevertheless，a larger number of starting materials and intermediates are more frequently used，and so it is useful to know the possibilities for their preparation from primary chemicals. For this reason it is appropriate somewhere in this book to illustrate a tree of especially important intermediates. These latter intermediates are the key compounds used in synthetic processes leading to an enormous number of agents. For the most part chemicals are involved which are produced in large amounts. In a similar way this is also true for the intermediates based on the industrial aromatic compounds toluene，phenol and chlorobenzene. Further key compounds may be shown in a table which can be useful in tracing cross-relationships in syntheses.fIn addition to the actual starting materials and intermediates solvents are required both as a reaction medium and ,for purification via recrystallization. Frequently used solvents are methanol，ethanol，isopropanol，butanol，acetone，ethyl acetate，benzene，toluene and xylene. To a lesser extent diethyl ether，tetrahydrofuran，glycol ethers，dimethylformamide (DMF) and dimethyl sulphoxide (DMSO) are used in special reactions.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 carbonate，sodium bicarbonate，ammonia，triethylamine，pyridine). Further auxiliary chemicals include active charcoal and catalysts. All of these supplementary chemicals (like the intermediates) can be a source of impurities in the final product.In 1969 the WHO published a treatise on `Safeguarding Quality in Drugs'.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). This has in the meantime become known as `Good Manufacturing Practices' or GMP rules，and these should now be obeyed in drug production. They form the basis for mutual recognition of quality certificates relating to the production of pharmaceuticals and for inspections of the production. facilities.For a long time the US drug authority，the Food and Drug Administration (FDA)，has issued regulations for the preparation of drugs analogous to the WHO rules，and it applies these strictly. Exports of drugs to the USA，like those of finished products，require regular inspection of the production facilities by the FDA. 5It may merely be noted here that such careful control applies not only to the products，but also to the raw materials (control of starting Materials)，and also to the intermediates. Clearly. the technical and hygienic equipment of the production and the storage areas have to fulfill set conditions.Since only a few compounds，such as acetylsalicylic acid，paracetamol and vitamins，are prepared in large amounts，most of the actual production takes place in multi-purpose (multi-product) facilities. .Special care has to be taken to avoid cross-contamination by other products what can be effected by good cleansing of used apparatus. A careful description and definition of all stored intermediates and products is needed.Selected -from H. J. Roth and A. Kleemann, Pharmaceutical Chemistry, Vol. 1，Drug Synthesis,Ellis Horwood Limited，England, 1988.Unit 5 Drug Development (I)1. IntroductionDrug Development is a very complex process requiring a great deal ofcoordination and communication between a wide range of different functionalgroups. It is expensive，particularly in the later phases of clinical development，where studies involve hundreds of patients. It is currently estimated that thedevelopment of a new drug costs about$230 million(1987 dollars)and takessomewhere between 7 and 10 years from initiation of preclinical development tofirst marketing (excluding regulatory delays). Drug development is a high-riskbusiness;although the rate is increasing，only about ONE out of every TEN newchemical entities studied in human beings for the first time will ever become a product. As a drug candidate progresses through development the risks of failure decrease as ‘hurdles’are overco me along the way. Typical reasons for failure include unacceptable toxicity，lack of efficacy，or inability to provide advantages over competitive products(Fig. 1).Attrition Rate of New Chemical Entities(NCE's) entering development. On averageonly about I in 400^1000 compoundssynthesized enters development.Reasons for termination of development of NCE's(excluding anti-infectives)1:Lack of efficacy2: Pharmacokinetics3: Animal toxicity4: Miscellaneous5: Adverse effects in man6: Commercial reasonsFig. 1 Attrition rates and reasons for terminations2. Planning for developmentAssessment of whether a drug candidate is likely to provide competitive advantages highlights the need first to have in place a set of product `goals' or target product profile. Particular attention should be paid to the differentiation from competitors. This is becoming 55 more and more critical with the increasing emphasis on limited formularies，healthcare costs，and pharmacoeconomics (discussed later in the chapter).A target profile will define the indication(s) that a drug candidate will be developed for，along with goals such as once a day dosing，faster onset of action，better side effect profile than a major competitor. The target profile can be refined and revised as a drug candidate moves through development and new data on the drug candidate or competitors become available. The logical next steps are to define the development strategy，for example，which indications to develop first，which countries to aim to market the drug in and then to define the core clinical studies necessary to achieve regulatory approval and commercial success.This chapter will describe the main activities required for successful development of a new drug. All these activities，many of which are interdependent，need to be carefully planned and co-ordinate. Speed to market with collection of high quality data is critical for success. The path of activities which determine the time it will take to get to registration is called，in project management terms，the critical path. It is vital to plan and prepare before studies begin and to monitor and manage problems so as to ensure that the critical path remains on schedule. With increased economic pressures and competitive intensity it is important for companies to explore ways to shorten this critical path. Running activities in parallel，or overlapping studies which would usually run sequentially，often involves an increase in risk but the dividends in time-saving can make such strategies worthwhile.The critical path for development of a new drug generally runs through the initial synthesis of compound，subacute toxicology studies，and then the clinical program. A chart showing the critical path activities for a typical drug candidate is shown in Fig. 2.Chemistry chemical Synthesis Route selection Pilot plant,scale up and stability testing Manufacturing plant productionToxicology Acute&subacute toxicology Long term and repro-toxicologyClinical Phase I Phase ll Phase lll Analysis data and report Phase lV ReviewRegulatory Submission and updating of clinical trial application prepare submit AuthorityMAA/NDA Regulatory ApprovalPost marketing SurverillancePharmaceuticsDevelopment and stability testing Prepare labellingDrug metabolismand pharmacokinetics Animal ADME* Healthy humans Human patientsActivities likely to be on the critical path are shown in bold* Absorption , Distribution , Metabolism , ExcretionFig. 2 The major processes in new drug developmentThe following sections highlight the objectives and activities of drug development work.Activities within each technical discipline are described broadly in chronological order.At any one time，work in all these disciplines may be proceeding in parallel. The timing and outcome of much of the work has direct impact on work in other disciplines. The major phases of drug development are Preclinical ( studies required before the compound can be dosed in humans)，Phase I (clinical studies usually in healthy human volunteers ) Phase Ⅱ( initial efficacy and safety and dose finding studies in patients)，and Phase Ⅲ(studies in several hundred patients). There then follows assembly of a marketing application dossier for subsequent review by country regulatory authorities.3. Chemical developmentRapid development of a drug candidate is dependent on the availability of sufficient quantity of the compound. The purity of compound needs to reach certain standards in order for it to be used in safety (toxicology)，pharmaceutical，and clinical studies. Initially，chemists will work on a small to medium scale to investigate production of the compound by several different methods so as to identify the optimum route for synthesizing the compound. ‘Optimum’here may mean a combination of several factors，for example，most efficient，cheapest safe，or that producing minimal waste. Analysis of the final product as well as intermediates and impurities plays a key role in identifying the best method of synthesis. Development and validation of analytical methods are necessary to support process development and guarantee the purity of the drug substance.In some cases levels of impurities may be unacceptably high and either improved purification procedures will need to be developed or the synthetic process may require significant alterations. The main aim is to ensure that the composition of compound is understood and that ultimately the material that is prepared is as pure as possible.As a drug candidate progresses through development，larger and larger amounts of compound are required. The amount of material required for different tests will often depend on the actual potency and dosage form of the compound.A pilot plant can be regarded as a mini-manufacturing set-up. Before transferring to a pilot plant，extensive evaluation and testing of the chemical synthesis is undertaken to ensure that any changes and hazards are minimized. Procedures are optimized，particular attention being paid to developing environmentally acceptable ways of disposing of waste products. Commercial production of bulk drug substance for production of a drug，once approved and marketed，will likely take place on a larger scale or at a registered manufacturing plant.4. Formulation developmentThe dosage form of a drug is the form by which it is administered to the patient. There are a vast array of possible dosage forms ranging from transdermal patches to inhalers to intranasal medicines. The more common dosage forms include oral tablets or capsules，oral liquids，topical ointments or creams，and injectables. The dosage form or forms chosen for a particular drug candidate will be defined in the target profile.Sometimes a more simple dosage form，for example an oral solution，is chosen for early 57 clinical studies in human beings. This may save time and upfront costs at an early，high-risk stage of the drug development process. Later clinical studies would use the expected marketed dosage form.Whatever the dosage form，the combination of drug and other materials which constitute it must fulfil certain criteria. One of the most important is that of adequate stability. That means a predetermined potency level must remain after，for example，two or three years. The stability data generated on a dosage form will determine its shelf-life and recommended storage conditions. Early in development the shelf-life may be limited to several months. This will not be a problem provided it is sufficient to cover use of the drug over the duration of the clinical study or studies.5. PharmacologyBefore a drug candidate is given to man，its pharmacological effects on major systems are often investigated in a number of species. The body systems studied include cardiovascular，respiratory，and nervous systems;the effects on gross behavior can also be studied.Experiments are sometimes conducted to see whether the drug candidate interferes with the actions of other medicines which，because of their specific effects or because of their common use，are likely to be taken concurrently with the drug candidate. Any synergism or antagonism of drug effects should be investigated，and any necessary warning issuedto clinical investigators.(It may be judged necessary to investigate such effects further in clinical studies，and any potential or proven drug interactions are likely to be noted in the product labeling for the drug.)It may also be appropriate to identify a substance for possible use in the management of overdosage，particularly if the therapeutic margin of the drug candidate is small.6. Safety evaluationThe objective of animal toxicology testing，carried out prior to the administration of a drug to man，is to reject compounds of unacceptable toxicity and to identify potential target organs and timings for adverse effects of the drug. This means that in early human studies these organs and tissues can be monitored with particular attention. It is important to establish whether toxic effects are reversible or irreversible，whether they can be prevented and，if possible，the mechanism of the toxicological effects. It is also important to interrelate drug response to blood levels in humans and blood levels in various animal species.The toxicological studies required for the evaluation of a drug candidate in man will be relevant to its proposed clinical use in terms of route of administration and duration of treatment of the clinical studies. The size and frequency of the doses and the duration of the toxicology studies are major determinants of permissible tests in man. Countries，including UK，USA，Australia，and Nordic countries，have regulatory guidelines which relate the duration of treatment allowed in man to the length of toxicity studies required in two species. Points from the guidelines are referenced in the subsequent sections.58 Initially，the pharmacological effects of increasing doses of the test substances are established in acute toxicity studies in small numbers of animals，generally using two routes of administration (one being that used in man). Results provide a guide to the maximum tolerated doses in subsequent chronic. toxicity tests，aid selection of dose levels，and identify target organs.The main aim of the subsequent sub-acute toxicity tests is to determine whether or not the drug candidate is adequately tolerated after administration to animals for a prolonged period as a guide to possible adverse reactions in man. Two to four week (daily dosing) studies are required，using the same route of administration as in man，in two species (one non-rodent)prior to administration of the compound to man. Three dose levels are usually necessary:the low daily dose should be a low multiple of the expected therapeutic dose，and the highest dose should demonstrate some toxicity.A general guide for the evaluation of new chemical entities would be that toxicology studies of a minimum duration of14 days are required to support single-dose exposure of a new drug candidate in normal volunteers in Phase 1. Toxicology studies of 30 days duration are required to support clinical studies of 7 to 10 days duration. Clinical studies of greater than 7 to 10 days up to 30 days duration require the support of at least 90 days toxicology studies. These requirements illustrate the need to plan ahead in drug development. The duration and approximate timings for future clinical trials need to be considered well in advance in order to schedule and conduct the appropriate toxicology studies to support the clinical program and avoid any delays.Two types of safety test are used to detect the ability of the drug candidate to produce tumours in man. The first are short-term in vitro genotoxicity tests，for example bacterial tests. The second are long-term animal carcinogenicity studies which are conducted in mice and rats;their length of often 2 years covers a large part of the lifespan of the animal. Mice and rats are used because of their relatively short life span，small size，and ready availability. Also，knowledge，which has accumulated concerning spontaneous diseases and tumours②in particular strains of these species，helps greatly in the interpretation of‘results.Long-term toxicology and carcinogenicity studies are conducted in order to obtain approval to test and finally to market a product for chronic administration to man. These studies may need to start during the late preclinical/ early clinical phase in order to `support' the subsequent clinical program. Long-term toxicity studies will normally include toxicity studies of six and twelve months duration in two species (one non-rodent).Any toxicity previously detected may be investigated more closely，for example extra enzymes looked at in blood samples.Reproductive toxicology is that part of toxicology dealing with the effect of compounds on reproduction-fertility，foetal abnormalities，post-natal development. Prior to clinical studies in women of child-bearing age，regulatory authorities require teratology data from two species (normally rat and rabbit)as well as clinical data from male volunteers. No reproductive data are required prior to clinical studies in male subjects. The effects of 59 compounds on reproduction differ with the period of the reproductive cycle in which exposure takes place and studies are designed to look at thesephases. Teratology`'' studies are designed to detect foetal abnormalities，fertility studies to investigate the compounds' effect on reproductive performance，And peri- and post-natal studies to study the development of pups.Unit 6 Isolation of Caffeine from TeaIn this experiment，Caffeine will be isolated from tea leaves. The major problem of the isolation is that caffeine does not occur alone in tea leaves，but is accompanied by other natural substances from which it must be separated. The major component of tea leaves is cellulose，which is the major structural material of all plant cells. Cellulose is a polymer of glucose. Since cellulose is virtually insoluble in water，it presents no problems in the isolation procedure. Caffeine，on the other hand，is water soluble and is one of the major substances extracted into the solution called "tea.”Caffeine comprises as much as 5 percent by weight of the leaf material in tea plants. Tannins also dissolve in the hot water used to extract tea leaves. The term tannin does not refer to a single homogeneous compound，or even to substances which have similar chemical structure. It refers to a class of compounds which have certain properties in common. Tannins are phenolic compounds having molecular weights between 500 and 3000. They a re widely used to "tan”leather. They precipitate alkaloids'z and proteins from aqueous solutions. Tannins are usually divided into two classes: those which can be hydrolyzed and those which cannot. Tannins of the first type which are found in tea generally yield glucose and gallic acid when they are hydrolyzed. These tannins are esters of gallic acid and glucose. They represent structures in which some of the hydroxyl groups in glucose have been esterified by digalloyl groups. The non-hydrolyzable tannins found in tea are condensation polymers of catechin. These polymers are not uniform in structure，but catechin molecules are usually linked together at ring positions 4 and 8.When tannins are extracted into hot water，the hydrolyzable ones are partially hydrolyzed，meaning that free gallic acid is also found in tea. The tannins，by virtue of their phenolic groups，and gallic acid by virtue of its carboxyl groups，are both acidic. If calcium carbonate，a base，is added to tea water，the calcium salts of these acids are formed. Caffeine can be extracted from the basic tea solution with chloroform，but the calcium salts of gallic acid and the tannins are not chloroform soluble and remain behind in the aqueous solution.The brown color of a tea solution is due to flavonoid pigments and chlorophylls，as well as their respective oxidation products. Although chlorophylls are somewhat chloroform soluble，most of the other substances in tea are not. Thus，the chloroform extraction of the basic tea solution removes nearly pure caffeine. The chloroform is easily removed by distillation(by 61'C)to leave the crude caffeine. The caffeine may be purified by recrystallization or by sublimation.68Catechin Gallic AcidIn a second part of this experiment，Caffeine will be converted to a derivative. A derivative of a compound is a second compound，of known melting point，formed from the original compound by a simple chemical reaction. In trying to make a positive identification of an organic compound，it is often customary to convert it into a derivative. If the first compound，Caffeine in this case，and its derivative both have melting points which match those reported in the chemical literature (e.g.，a handbook)，it is assumed that there is no coincidence and that the identity of the first compound，Caffeine，has been definitely established.Caffeine is a base and will react with an acid to give a salt. Using salicylic acid，a derivative salt of Caffeine，Caffeine salicylate，will be made in order to establish the identity of the Caffeine isolated from tea leaves.Special Instructions Be careful when handling chloroform. It is a toxic solvent，and you should not breathe it excessively or spill it on yourself. When discarding spent tea leaves，do not put them in the sink because they will clog the drain. Dispose of them in a waste container.Procedure Place 25g of dry tea leaves，25g of calcium carbonate powder，and 250ml of water in a 500ml three neck round bottom flask equipped with a condenser for reflux. Stopper the unused openings in the flask and heat the mixture under reflux for about 20 minutes. Use a Bunsen burner to heat. While the solution is still hot，filter it by gravity through a fluted filter using a fast filter paper such as E&D No. 617 or S&S No. 595. You may need to change the filter paper if it clogs.Cool the filtrate (filtered liquid)to room temperature and，using a separatory funnel，extract it twice with 25ml portions of chloroform. Combine the two portions of chloroform in a 100ml round bottom flask，Assemble an apparatus for simple distillation and remove the chloroform by distillation. Use a steam bath to heat. The residue in the distillation flask contains the caffeine and is purified as described below (crystallization). Save the chloroform that was distilled. You。

制药工程英语Pharmaceutical EngineeringThe pharmaceutical industry is a vital component of the global healthcare system, responsible for the development, production, and distribution of essential drugs and medical treatments. Pharmaceutical engineering, a specialized field within the broader pharmaceutical industry, plays a crucial role in ensuring the efficient and safe manufacture of these life-saving products.At the heart of pharmaceutical engineering lies the intricate process of drug development and production. This process begins with the identification of a therapeutic target, followed by the synthesis of a candidate drug molecule. Pharmaceutical engineers are tasked with designing and optimizing the manufacturing processes that transform these molecules into safe and effective medications.One of the primary responsibilities of pharmaceutical engineers is the development and implementation of robust and scalable production methods. This involves the design of specialized equipment and facilities that can consistently produce high-quality drugs in large quantities. This includes the selection and integrationof various unit operations such as fermentation, extraction, purification, and formulation.Ensuring the quality and purity of pharmaceutical products is of paramount importance, and pharmaceutical engineers play a crucial role in this regard. They develop and validate analytical methods to monitor the critical quality attributes of the drugs throughout the manufacturing process. This includes the identification and quantification of active pharmaceutical ingredients, as well as the detection and control of impurities and byproducts.In addition to process development and quality control, pharmaceutical engineers also contribute to the optimization of existing manufacturing processes. By leveraging their expertise in areas such as process modeling, simulation, and data analysis, they can identify opportunities for improved efficiency, reduced costs, and enhanced sustainability.Another crucial aspect of pharmaceutical engineering is the design and construction of state-of-the-art manufacturing facilities. These facilities must comply with strict regulatory requirements, such as those set forth by the Food and Drug Administration (FDA) and the European Medicines Agency (EMA), to ensure the safety and efficacy of the final products. Pharmaceutical engineers are responsible for the design, construction, and validation of these facilities, whichoften incorporate advanced technologies and automation to enhance productivity and minimize the risk of contamination.The role of pharmaceutical engineers extends beyond the manufacturing process itself. They also contribute to the development of innovative drug delivery systems, such as controlled-release formulations, transdermal patches, and targeted drug delivery mechanisms. These advancements not only improve the bioavailability and therapeutic efficacy of drugs but also enhance patient compliance and quality of life.In recent years, the pharmaceutical industry has witnessed a surge in the adoption of emerging technologies, such as continuous manufacturing, artificial intelligence, and blockchain, which have been driven by the efforts of pharmaceutical engineers. These innovations have the potential to revolutionize the industry, leading to faster drug development, more efficient production processes, and enhanced supply chain traceability.As the pharmaceutical industry continues to evolve, the demand for skilled and knowledgeable pharmaceutical engineers is expected to grow. These professionals must possess a deep understanding of various scientific disciplines, including chemistry, biology, engineering, and regulatory affairs, as well as the ability to collaborate effectively with cross-functional teams.In conclusion, pharmaceutical engineering is a dynamic and essential field that plays a pivotal role in the development, production, and distribution of life-saving drugs and medical treatments. By leveraging their expertise in process design, quality control, and facility management, pharmaceutical engineers are instrumental in ensuring the availability of safe and effective medications that improve the health and well-being of people around the world.。

UNIT1origin ['ɔridʒin] n. 出身；原点；起源original n. 原作；原型；原件adj. 原始的；最初的；独创的Pharmaceutical [,fɑ:mə'sju:tikəl] adj. 制药（学）的n. 药物pharmaceutical factory 药厂pharmaceutical analysis 药物分析pharmaceutical chemistry 药物化学pharmaceutical preparation 药物制剂pharmaceutical product 药用物品agent n. 代理人(商)；药剂（试剂）pharmaceutical agent 药物chemical agent 化学试剂synthetic [sin'θetik]adj. 合成的，人造的；综合的n. 合成物（synthetics）synthesis ['sinθisis] n. 综合，合成syntheses synthesis的复数形式natural product 天然产物synthetic material 合成材料semi- 半，部分semi-finalsemi-conductorsemi-synthesisserve as 起…作用；可作…用lead compound 先导化合物starting material：n. 起始物料，原料；原材料intermediate：n. 中间体Alkaloid ['alkəlɔid] n. 生物碱enzyme [‘enzaim] 酶;precursor [pri:’kə:sə] n. 先驱，前体；polysaccharide [pɔli‘sakəraid] n. 多糖；多聚糖类;steroid [‘sterɔid] n.甾类，类固醇；peptide [‘peptaid] 肽,缩氨酸；polypeptide 多肽；insulin [‘insjulin] n. 胰岛素vaccine ['vaksi:n] n. 疫苗citral ['sɪtral]n. [有化] 柠檬醛tocopherol [tɒ'kɒfərɒl]n. [生化] 生育酚；维生素Efermentation [,fə:men'teiʃən] n. 发酵Fermentor n. 发酵罐antibody ['anti,bɔdi]n. 抗体antibiotic [,antibai'ɔtik]adj. 抗生的；抗菌的 n 抗生素，抗菌素b-lactam(beta-lactam) [‘beitə-’laktam] n. 内酰胺amide ['amaid] n. 酰胺amine [ə'mi:n] n. 胺ammonia [ə'məunjə] n. 氨，阿摩尼亚ammonia water n. 氨水ammonium [ə'məunjəm] n. 铵；氨盐基dextran ['dekstran]n. [有化] 右旋糖酐；葡萄聚microbiological process: 微生物处理eukaryont [ju:'kariɔn]n. 真核；真核生物prokaryont [prəu'kari:əut]n. 原核生物yeast [ji:st]n. 酵母；酵母片bacteria [bak'tiəriə] n. 细菌bacterial [bak'tiriəl] adj. [微] 细菌的partial synthesis：半合成；部分合成semisynthetic[,sɛmaɪsɪn'θɛtɪk]adj. 半合成的lactam['laktam]n. [有化] 内酰胺stainless ['steinlis]adj. 未被玷污的；不锈的contamination [kən,tami'neiʃən]n. 污染，玷污；污染物phage [feidʒ]n. [病毒] 噬菌体sterile ['sterail, -rəl]adj. 不毛的；贫瘠的；不育的；无菌的exclusively [ik'sklu:sivli]adv. 唯一地；专有地；排外地aerobic [,eiə'rəubik]adj. 需氧的；aerobic exerciseby-product n. 副产物registration authority 登记机关（注册中心）demand as essential ：必需thorough ['θʌrə, 'θə:rəu]adj. 彻底的；十分的；周密的practically ['praktikəli]adv. 几乎；事实上；实际地nevertheless [,nevədə'les]adv. 然而，不过toluene ['tɔljui:n]n. [有化] 甲苯phenol ['fi:nɔl, fi'n-]n. [化]石碳酸，苯酚chlorobenzene [,klɔ:rəu'benzi:n]氯苯in addition to除…之外reaction medium：反应媒体（媒介）purification [,pjuərifi'keiʃən]n. 净化；提纯recrystallization n. 重结晶methanol ['meθənɔl] n. 甲醇（methyl alcohol）ethanol ['eθə,nɔl] n. 乙醇，酒精isopropanol [,aisə'prəupənɔl]n. 异丙醇butanol ['bju:tənɔl]n. 丁醇acetone ['asitəun]n. 丙酮ethyl acetate n. 乙酸乙酯benzene ['benzi:n]n. 苯toluene ['tɔljui:n]n. 甲苯xylene ['zaili:n]n. 二甲苯diethyl ether n. 乙醚tetra-hydro-furann. 四氢呋喃THFDMFn.二甲基甲酰胺sulphoxide [sʌl'fɔksaid]n. 二甲基亚砜potassium hydroxide 氢氧化钾potassium carbonate 碳酸钾sodium bicarbonate 碳酸氢钠triethylamine 三乙胺pyridine 吡啶auxiliary [ɔ:ɡ'ziljəri] adj. 辅助的active charcoal 活性炭catalyst ['katəlist] n. 催化剂impurity n. 杂质hydrochloric acid [,haidrəu'klɔrik] 盐酸sulfuric acid [sʌl‘fjuərik]硫酸nitric acid [‘naitrik]硝酸acetic acid [ə'si:tik]乙酸sodium hydroxide 氢氧化钠UNIT 3physiotherapy [,fiziəu'θerəpi]n. 物理疗法parasite ['parəsait]n. 寄生虫organism ['ɔ:ɡənizəm]n. 有机体；生物体；微生物literature ['litərətʃə]n. 文献；著作superstition [,sju:pə'stiʃən]n. 迷信trial and error反复试验compound [kəm'paund]n. 化合物；curative ['kjurətiv]adj. 有疗效的；治病的。

1、生产的药品其生产或出身不同药剂可以分为三类：Ⅰ.完全（合成纤维）合成材料，Ⅱ.天然产物，和Ⅲ.产品从（半合成产品）的部分合成。

本书的重点是团体的最重要的化合物Ⅰ和Ⅲ一所以药物合成。

这并不意味着，但是，天然产品或其他代理人并不太重要。

它们可以作为有价值的领导结构，他们常常为原料，或作为重要的合成中间体产品的需要。

表1给出了获取药剂的不同方法的概述。

（表1对药物的可能性准备）方法举例1、全合成，超过75％的药剂（合成纤维）2、分离（天然产物）天然来源：2.1植物-生物碱;酶;心甙，多糖，维生素E;类固醇的前体（薯蓣皂素，sitosterin），柠檬醛（中间产品维生素A，E和K）2.2动物器官一酶;肽激素;胆酸从胆;胰岛素）从胰脏;血清和疫苗2.3从角蛋白和明胶L -氨基酸;三一胆固醇从羊毛油脂的其他来源水解3.一抗生素发酵; L -氨基酸，葡聚糖，对类固醇有针对性的修改,例如11 -羟基化;也胰岛素，干扰素，抗体，肽激素，酶，疫苗4。

部分合成修改（半合成剂）天然产品: 一生物碱化合物;半合成/ 3-内酰胺类抗生素;类固醇;人胰岛素其中几个重要的治疗作用最初是从天然产品天然来源获得更有效的今天，我。

大肠杆菌更经济的准备..由全合成。

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。

在过去的几年里发酵-岛大肠杆菌微生物过程变得极其重要。

通过现代技术和基因选择的结果导致了突变体的微生物创造高性能，发酵，已成为首选方法各种各样的物质。

这两个Eukaryonts（酵母菌和霉菌）和Prokaryonts（单细胞细菌，放线菌和）用于微生物。

下列产品类型可以得到：1.细胞的物质（单细胞蛋白），2.酶，3.主要降解产物（主要代谢物），4.二级降解产物（次生代谢物）。

不顾来自某些微生物，大肠杆菌粘膜生产的葡聚糖克明串珠mesenteroides，2和3级是毒品有关的准备工作。

专业英语考试内容：单词10分句子翻译24分根据课文回答问题24分英译汉药品说明书21分翻译汉译英摘要21分Unit 11 Tablet (The Pharmaceutical Tablets Dosage Form)药片（医药片剂剂型）Role in TherapyA: The oral route of drug admininistration is the most important method of administering drugs ofr systemic effects.Except in cases of Insulin therapy.the parenteral route is not routinely used for self-administration of medication.The topical route of administration has only recently been employed to deliver drugs to the body for systemic effects,with two classes of marketed products:Nitroglycerin for the treatmint of angina and scopolamine for the treatment of motion sickness.Other drugs are certain to follow,but the topical route of administration is limited in its ability to allow effective drug absorption for systemic drug action.A:口服给药是全身效应用药方法中最为重要的。

除了胰岛素治疗，非肠道药途径不常用在自我服药方面。

7传统植物药物的发展第一段Over大约超过1/4个世纪各大陆上的大多数人依靠植物药物来解决健康问题。

在美洲大陆近乎1/3的药物处方源自植物药，超过120个处方药来自植物。

大多数药物从传统药物发展而来。

从经济上讲，意味着人们每年的这项开销达8000~10,000M美元。

最近，世界卫生组织研究数据表明超过30%的植物曾所谓源药资源，250,000种高科植物中，超过8000种可入药。

虽然传统药物应用广泛，一个民族不可或缺的文化。

它经过了成百上千年一代传一代人的亲手实践总结。

不幸的是很多古老的药物知识已失传和失误濒临灭绝。

因此，对传统药方的科研和传统药物的保存变得尤为重要。

第二段For在一段相当长的时期，植物药材的唯一应用方法是直接粗制利用。

随着本世纪有机化学的兴起，提取和分馏技术显著提高。

分离鉴定植物中的有效成分成为可能。

1940年，合成技术的进步合成很多植物成分及其衍生物。

在西方国家，通过合成药物有效成分比使用粗药来得更有效更经济。

近年表现尤其明显，然而有时候合成的类似物不如天然成分的效果。

而且，合成药物话费更多的时间金钱。

尤混合作用的灵感，加上一个事实，即许多药物具有复杂的结构可能是完全不可能的合成，现在有死灰复燃的趋势，返回自然药物开发第三段Ephedrine麻黄素是最传统最典型的从植物药物发展来的药物。

它提取自麻黄的叶子，5000年前在中国就被用于治疗哮喘和花粉过敏，在1942年才被陈和私密迪特合成出来。

麻黄素是一种十分贴近肾上腺素的生物碱，从药理应用来说，麻黄素管饭用于刺激交感神经类疾病。

它对治疗高血压有突出表现，对鼻充血也有缓解作用。

是基于这种药的药物作用及其对a和B肾上腺素受体的直接影响和内源性去甲肾上腺素的释放。

第四段Digitalis is one of洋地黄是常用于心脏衰竭心律不齐的药物。

它通过作用于心肌收缩和改善心血管阻力来达目的。

它也缓慢的传导通过心室和心房调节心房纤维颤动和心率节奏。

1、生产的药品其生产或出身不同药剂可以分为三类：Ⅰ.完全（合成纤维）合成材料，Ⅱ.天然产物，和Ⅲ.产品从（半合成产品）的部分合成。

本书的重点是团体的最重要的化合物Ⅰ和Ⅲ一所以药物合成。

这并不意味着，但是，天然产品或其他代理人并不太重要。

它们可以作为有价值的领导结构，他们常常为原料，或作为重要的合成中间体产品的需要。

表1给出了获取药剂的不同方法的概述。

（表1对药物的可能性准备）方法举例1、全合成，超过75％的药剂（合成纤维）2、分离（天然产物）天然来源：2.1植物-生物碱;酶;心甙，多糖，维生素E;类固醇的前体（薯蓣皂素，sitosterin），柠檬醛（中间产品维生素A，E和K）2.2动物器官一酶;肽激素;胆酸从胆;胰岛素）从胰脏;血清和疫苗2.3从角蛋白和明胶L -氨基酸;三一胆固醇从羊毛油脂的其他来源水解3.一抗生素发酵; L -氨基酸，葡聚糖，对类固醇有针对性的修改,例如11 -羟基化;也胰岛素，干扰素，抗体，肽激素，酶，疫苗4。

部分合成修改（半合成剂）天然产品: 一生物碱化合物;半合成/ 3-内酰胺类抗生素;类固醇;人胰岛素其中几个重要的治疗作用最初是从天然产品天然来源获得更有效的今天，我。

大肠杆菌更经济的准备..由全合成。

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。

在过去的几年里发酵-岛大肠杆菌微生物过程变得极其重要。

通过现代技术和基因选择的结果导致了突变体的微生物创造高性能，发酵，已成为首选方法各种各样的物质。

这两个Eukaryonts（酵母菌和霉菌）和Prokaryonts（单细胞细菌，放线菌和）用于微生物。

下列产品类型可以得到：1.细胞的物质（单细胞蛋白），2.酶，3.主要降解产物（主要代谢物），4.二级降解产物（次生代谢物）。

不顾来自某些微生物，大肠杆菌粘膜生产的葡聚糖克明串珠mesenteroides，2和3级是毒品有关的准备工作。

Developing drugs from traditional medicinal plantsOver three quarters of the world's population relies mainly on plants andplant extracts for health care .Approximately one third of the prescription drugs in the US contain plant components, and more than 120important prescription drugs are derived from plants. Most of these drugswere developed because of their use in traditional medicine. Economically,this represents $8000-10,000M of annual consumer spending. Recent World Health Organization (WHO) studies indicate that over 30 per cent of the world's plant species have at one time or another been used for medicinalpurposes. Of the 250,000 higher plant species on Earth, more than 80,000species are medicinal. Although traditional medicine is widespread throughout the world , it is an integral part of each individual culture.Its practice is based mainly on traditional beliefs handed down from generation to generation for hundreds or even thousands of years. Unfortunately, much of this ancient knowledge and many valuable plantsare being lost at an alarming rate. The scientific study of traditional medicines and the systematic preservation of medicinal plants are thusof great importance.For quite a long time, the only way to use plant medicines was either directapplication or the use of crude plant extracts. With the development of organic chemistry at the beginning of this century, extraction and fractionation techniques improved significantly. It became possible to isolate and identify many of the active chemicals from plants. In the 1940s,advances in chemical synthesis enabled the synthesis of many plant components and their derivatives. In western countries, it was thoughtthat chemical synthesis of drugs would be more effective and economical than isolation from natural sources. Indeed, this is true in many cases.However, in many other cases, synthetic analogues are not as effectiveas their natural counterparts. In addition, some synthetic drugs cost manytimes more than natural ones. Inspired by these realisations, coupled withthe fact that many drugs with complex structures may be totally impossibleto synthesise, there is now a resurgent trend of returning to natural resources for drug developmentImportant prescription drugs from plantsEphedrine is the oldest and most classic example of a prescription drug developed from a traditional medicinal plant. It is derived from Ma Huang ,a leafless shrub. Used to relieve asthma and hay fever in China for over 5000 years, it was introduced into western medicine in 1924 by Chen and Schmidt. Ephedrine is an alkaloid closely related to adrenaline, the major product of the adrenal gland. Pharmacologically, Ephedrine is usedextensively to stimulate increased activity of the sympathetic nervous system. It is used as a pressor agent to counteract hypotension associatedwith anaesthesia, and as a nasal decongestant. The drug action of this medicine is based both on its direct effect on [alpha] and [beta] adrenergic receptors and on the release of endogenous noradrenaline.Digitalis is one of the most frequently used medications in the treatmentof heart failure and arrhythmia. It increases the contractility of the heart muscle and modifies vascular resistance. It also slows conduction through the atrioventricular node in the heart, making it useful in the treatment of atrial fibrillation and other rapid heart rhythms.Digitalis is found in the leaves and seeds of Digitalis purpurea and Digitalis lanata, commonly known as the foxglove plant. Foxglove has beenused in traditional medicine in many parts of the world - by African natives as arrow poisons, by the ancient Egyptians as heart medicine, andby the Romans as a diuretic, heart tonic, emetic and rat poison. The Chinese, who found this ingredient not only in plants but also in the dryskin and venom of the common toad, used it for centuries as a cardiac drug.In the western world, the foxglove was first mentioned in 1250 in the writing of a physician, Walsh, and it was described botanically in the 1500s.Digitalis is a glycoside containing an aglycone, or genin, linked to between one and four sugar molecules. The pharmacological activity resides in the aglycone, whereas the sugar residues affect the solubilityand potency of the drug. The aglycone is structurally related to bile acids,sterols, sex hormones and adrenocortical hormones.and its derivatives are the most frequently used drugsd-Tubocurarinein operating rooms to provide muscle relaxation and prevent muscle spasm.These agents interrupt the transmission of the nerve impulse at the skeletal neuromuscular junction. Curare, the common name for South American arrow poisons, has a long and interesting history. It has been used for centuries by Indians along the Amazon and Orinoco rivers for hunting. It causes paralysis of the skeletal muscles of animals and finally results in death. The methods of curare preparation were a secretentrusted only to tribal doctors. Soon after their discovery of the American continent, European explorers became interested in curare. Inthe late 16th century, samples of native preparations were brought to Europe for investigation. Curare, an alkaloid (see Figure), was found invarious species of Strychnos and certain species of Chondrodendron. The first use of curare for muscle relaxation was reported in 1942 by Griffithand Johnson. This drug offers optimal muscular relaxation without the useof high doses of anaesthetics. It thus emerged as the chief drug for use in tracheal intubation and during surgery.Vinblastine and vincristine (see Figure) are two of the most potent antitumour drugs. They are obtained from Catharanthus roseus, commonly known as the rosy periwinkle. This plant, indigenous to Madagascar, is also cultivated in India, Israel and the US. It was originally examined for clinical use because of its traditional use in treating diabetis. Theleaves and roots of this plant contain more than 100 alkaloids. Fractionation of these extracts yields four active alkaloids: vinblastine, vincristine, vinleurosine and vinresidine. These alkaloids areasymmetric dimeric compounds referred to as vinca alkaloids, but of these,only vinblastine and vincristine are clinically important antitumour agents.[9] These two alkaloids are cell-cycle specific agents that blockmitosis (cell division). Vincristine sulphate is used to treat acute leukaemia in children and lymphocytic leukaemia. It is also effective against Wilm's tumour, neuroblastoma. rhabdomyosarcoma (tumour ofvoluntary or striped muscle cells), reticulum cells sarcoma and Hodgkin'sdisease. Vinblastine sulphate is used in the treatment of Hodgkin's disease, lymphosarcoma, choriocarcinoma, neuroblastoma, carcinoma ofbreast, lung and other organs, and in acute and chronic leukaemia Emerging plant medicinesArtemisinin is the most recent anti-malaria drug developed fromplant-based traditional medicine. It is isolated from the leaves and flowers of Artemisia annua L. (Compositae), commonly known as the sweet wormwood, a cousin of tarragon. Indigenous to China, the extract of thisplant is traditionally known as the qinghao. It has been used to treat malaria in China for over 2000 years. Its active component, artemisinin,was first isolated in the 1970s by Chinese scientists. Unlike quinine and chloroquine, this compound is non-toxic, rapid in effect, and safe for pregnant women. Furthermore, it is effective againstchloroquine-resistant Plasmodium falciparum malaria and in patients withcerebral malaria. It kills the parasites directly so parasitaemia is quickly controlled. This work was confirmed by the WHO in Africa and otherparts of Southeast Asia.Artemisinin is an endoperoxide of the sesquiterpene lactone. Thestructure of this compound is too complex to be synthesised effectively.Artemisia is also found in many parts of the US, abudantly along the Potomac River in Washington DC, but the drug content of these varietiesis only about half that of the Chinese variety. Currently, the WHO and the US are jointly engaged in the cultivation of Chinese Artemisia forworldwide use. The recent development offers renewed hope for using traditional medicine to provide new drugs for future medicines从传统发展药品药用的植物在世界上有四分之三的人口主要依靠植物和植物提取物的保健作用。

A: antibiotic 抗生的；抗生素antibody 抗体adverse 不利的相反的antitumour 抗癌的asymmetric 不对称的acute 急性的administration 管理，（药的）服法availability 有效性，效力antagonize 拮抗aroma 芳香化合物anticancer 抗癌的a steady-state blood or tissue level稳定态的血液或组织水平B: benzene 苯bioavailability 生物利用度biotechnologic 生物技术的bioengineered 生物工程的C: Caffeine 咖啡因clinical 临床的capsule 胶囊chronic 慢性的chromogenic 发色的colorimetric 比色的coagulate 凝结chirality 手性的controlled release 控释D: dimeric 二聚的dosage 配药剂量digestion 消化力degradation 降解，退化degradation 退化，降级demineralize 去离子E: enzyme 酶extraction 萃取提取ether 醚excretion 排泄分泌efficacy 功效，效验expiration 截止enantiomer 对应异构体F: fermentation 发酵fractionation 分馏G: glucose 葡萄糖glycoside 苷，配糖类gastrointestinal 肠胃道的GMP 药品生产质量管理规范GI tract 肠胃系统H: hormone 激素hypotension 低血压heparin 肝素I: insulin 胰岛素interferon 干扰素intermediate 中间体interdependent 互相依赖的impurity 杂质intestinal 肠的interact 相互作用in vivo/in vitro environment在体内的/体外的环境L: lactone 内酯leach 滤取N: nitrate 硝酸盐nutrient 营养的M：Morphine 吗啡O: optimize 优化onset 开始反应P: pharmaceutical 制药的plasma 血浆pharmacokinetics 药物动力学penicillin 青霉素preclinical 潜伏期的prescription 处方，规定pharmacologically 药理的preservation 保存precipitation 沉淀phosphate 磷酸盐peroral 经口的preservative 防腐的；防腐剂pharmacognosist 生药学家pathology 病理学R: recrystallization 重结晶residue 渣滓racemate 外消旋体rational 理性的S: serum 血浆sterile 无细菌的syrup 糖浆suspension 悬浊液sustain 维持synergies 药的协同作用steroid 甾体化合物sedimentary 沉积的stoichiometric 化学计量的sustained release 缓释systemic effects 系统效应T: therapeutical 治疗学的Toluene 甲苯tumour 肿瘤topical （医）局部的tablet 药片，片剂turbidity 浊度V：valid expiration dates 有效截止日期W: World Health Organization世界卫生组织（WTO）X: xylene 二甲苯A: antibiotic 抗生的；抗生素antibody 抗体adverse 不利的相反的antitumour 抗癌的asymmetric 不对称的acute 急性的administration 管理，（药的）服法availability 有效性，效力antagonize 拮抗aroma 芳香化合物anticancer 抗癌的a steady-state blood or tissue level 稳定态的血液或组织水平B: benzene 苯bioavailability 生物利用度biotechnologic 生物技术的bioengineered 生物工程的C: Caffeine 咖啡因clinical 临床的capsule 胶囊chronic 慢性的chromogenic 发色的colorimetric 比色的coagulate 凝结chirality 手性的controlled release 控释D: dimeric 二聚的dosage 配药剂量digestion 消化力degradation 降解，退化degradation 退化，降级demineralize 去离子E: enzyme 酶extraction 萃取提取ether 醚excretion 排泄分泌efficacy 功效，效验expiration 截止enantiomer 对应异构体F: fermentation 发酵fractionation 分馏G: glucose 葡萄糖glycoside 苷，配糖类gastrointestinal 肠胃道的GMP 药品生产质量管理规范GI tract 肠胃系统H: hormone 激素hypotension 低血压heparin 肝素I: insulin 胰岛素interferon 干扰素intermediate 中间体interdependent 互相依赖的impurity 杂质intestinal 肠的interact 相互作用in vivo/in vitro environment在体内的/体外的环境L: lactone 内酯leach 滤取N: nitrate 硝酸盐nutrient 营养的M：Morphine 吗啡O: optimize 优化onset 开始反应P: pharmaceutical 制药的plasma 血浆pharmacokinetics 药物动力学penicillin 青霉素preclinical 潜伏期的prescription 处方，规定pharmacologically 药理的preservation 保存precipitation 沉淀phosphate 磷酸盐peroral 经口的preservative 防腐的；防腐剂pharmacognosist 生药学家pathology 病理学R: recrystallization 重结晶residue 渣滓racemate 外消旋体rational 理性的S: serum 血浆sterile 无细菌的syrup 糖浆suspension 悬浊液sustain 维持synergies 药的协同作用steroid 甾体化合物sedimentary 沉积的stoichiometric 化学计量的sustained release 缓释systemic effects 系统效应T: therapeutical 治疗学的Toluene 甲苯tumour 肿瘤topical （医）局部的tablet 药片，片剂turbidity 浊度V：valid expiration dates 有效截止日期W: World Health Organization世界卫生组织（WTO）X: xylene 二甲苯A: antibiotic 抗生的；抗生素antibody 抗体adverse 不利的相反的antitumour 抗癌的asymmetric 不对称的acute 急性的administration 管理，（药的）服法availability 有效性，效力antagonize 拮抗aroma 芳香化合物anticancer 抗癌的a steady-state blood or tissue level稳定态的血液或组织水平B: benzene 苯bioavailability 生物利用度biotechnologic 生物技术的bioengineered 生物工程的C: Caffeine 咖啡因clinical 临床的capsule 胶囊chronic 慢性的chromogenic 发色的colorimetric 比色的coagulate 凝结chirality 手性的controlled release 控释D: dimeric 二聚的dosage 配药剂量digestion 消化力degradation 降解，退化degradation 退化，降级demineralize 去离子E: enzyme 酶extraction 萃取提取ether 醚excretion 排泄分泌efficacy 功效，效验expiration 截止enantiomer 对应异构体F: fermentation 发酵fractionation 分馏G: glucose 葡萄糖glycoside 苷，配糖类gastrointestinal 肠胃道的GMP 药品生产质量管理规范GI tract 肠胃系统H: hormone 激素hypotension 低血压heparin 肝素I: insulin 胰岛素interferon 干扰素intermediate 中间体interdependent 互相依赖的impurity 杂质intestinal 肠的interact 相互作用in vivo/in vitro environment在体内的/体外的环境L: lactone 内酯leach 滤取N: nitrate 硝酸盐nutrient 营养的M：Morphine 吗啡O: optimize 优化onset 开始反应P: pharmaceutical 制药的plasma 血浆pharmacokinetics 药物动力学penicillin 青霉素preclinical 潜伏期的prescription 处方，规定pharmacologically 药理的preservation 保存precipitation 沉淀phosphate 磷酸盐peroral 经口的preservative 防腐的；防腐剂pharmacognosist 生药学家pathology 病理学R: recrystallization 重结晶residue 渣滓racemate 外消旋体rational 理性的S: serum 血浆sterile 无细菌的syrup 糖浆suspension 悬浊液sustain 维持synergies 药的协同作用steroid 甾体化合物sedimentary 沉积的stoichiometric 化学计量的sustained release 缓释systemic effects 系统效应T: therapeutical 治疗学的Toluene 甲苯tumour 肿瘤topical （医）局部的tablet 药片，片剂turbidity 浊度V：valid expiration dates 有效截止日期W: World Health Organization 世界卫生组织（WTO）X: xylene 二甲苯。