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1、Agrochemical Formulation Trends农药制剂的发展趋势,CCPIAGuilin, Guangxi, China中国 桂林Keith Parker, Ph.D.Syngenta Asia Pacific Pte. Ltd.,Who is Syngenta 先正达介绍Agrochemical Formulation Trends农业化学配方的发展趋势,Contents 内容,Our industry family tree 国际农化公司发展概况,Ciba,Sandoz,ICI,ISK Biosciences,Monsanto,DuPont,Shell,Cyanamid,B
2、ASF,Bayer,Rhone-Poulenc,Hoechst,Schering,Dow,Rohm & Haas,Merck,1992,1993,1994,1995,1996,1997,1998,1999,2000,2001,Novartis,AHP,Aventis,2002,Agrevo,Zeneca,Excellent complementary and leading product portfolio卓越全面、领先的产品线 A leader in crop protection 植保领域的领先者 Third in high-value commercial seeds 高价值商业种子排
3、名第三First class research and development resources 一流的研发资源 Investment of around $800m annually 每年投入约八亿美元Strong worldwide presence 业务遍布全球 Around 21,000 employees in over 90 countries 在90多个国家拥有2万1千名雇员Rich pipeline of Crop Protection and Seeds products丰富的植保和种子产品产销渠道,Syngenta a leading global agribusines
4、s先正达全球领先的农业科技公司,Syngenta a leading global agribusiness先正达全球领先的农业科技公司,million tonnes of cotton is grown using our crop protection products全球440万吨棉花种植过程中使用先正达植保产品Thats the equivalent of 20 billion T-Shirts这相当于200亿件T恤的用料,4.4,Syngenta a leading global agribusiness先正达全球领先的农业科技公司,70%,of Scotch Whisky is p
5、roduced by Syngenta barley70% 苏格兰威士忌是用先正达大麦制造的,What We Do 我们从事哪些业务,Crop Protection作物保护,Seeds种子,Professional Products专业产品,Bio-technology生物技术,Major product brands 主要的产品品牌,Herbicides 除草剂,Professional products 专业产品,Fungicides 杀菌剂,Insecticides 杀虫剂,Seeds 种子,阿克泰,金雷,世高,阿米西达,锐胜,泰草达,克无踪,功夫,千层红,Rank排名,2006 R&D
6、 spend2006 研发投入 $ m,1Syngenta 先正达,2Bayer 拜尔,4BASF 巴斯夫,5DuPont 杜邦,3Monsanto 孟山都,6Dow 陶氏,As % of Sales销售百分比,11%,10%,10%,14%,11%,10%,The leader in research and development 先正达，研究与开发的领导者,Source: Phillips McDougall, Syngenta,Major R&D sites located at theheart of scientific communities,Other sitesMarker-
7、assisted and seed breeding capabilitiesGlobal field station network,Global R&D capabilities 全球研发机构,美国格林斯博罗GREENSBOROFormulationEnvironmental Science,美国SBIBiotechnologyR&D,英国集能山JEALOTTS HILLChemical DiscoveryWeed ControlFormulationBioscienceEnvironmental Science,瑞士巴塞尔/斯坦恩BASEL/STEINFungicides, Insect
8、icides &Professional Products,印度果阿GOAChemistry,Syngenta in China 先正达在中国,Crop Protection作物保护,Seeds 种子,Professional Products专业产品,R&D研发,A history of more than 100 years 百多年合作历史 Associated investment US$ 200m 目前总投资达2亿美元 40% of the total direct foreign investment in CP section投资额占中国市场植保领域外商直接投资的40,Invest
9、ment in China 先正达在中国的投资,Syngenta (Suzhou) Crop Protection Co., Ltd.,Syngenta Seeds Company Ltd.,Syngenta Nantong Crop Protection Co., Ltd.,Environment Protection Responsibility in China先正达在中国环保社会责任,“Top 100 Environmental Friendly Projects” by State Environmental Protection Administration “the only o
10、ne of its kind in crop protection industry “国家环保局授予的“百佳环保工程”荣誉称号植保行业中唯一获此殊荣 “Top 10 environmental friendly enterprises” “江苏省十大环保企业”“High-tech enterprises” in Jiangsu province” “江苏省高新技术企业” Provide technical support for industry / national standards setup为行业标准设定提供技术支持,Chinas sustainable agriculture de
11、velopment through innovative research and technology通过创新性的研究和技术，中国农业的可持续性发展,Improve crop productivity, quality and safety through integrated solutions通过完整的方案，提高和改善作物产量，质量和安全性,Upgrade Chinese farmers income and the quality of life提升中国农民的收入和生活质量,Syngenta China is Committed To先正达中国忠于.,Who is Syngenta 先
12、正达介绍Agrochemical Formulation Trends农业化学配方的发展趋势,Contents 内容,Formulation Technology 制剂技术,Agribusiness invests heavily in Formulation Science 在制剂技术的上开发上，农化企业投入重金Both for first launch of new Active Ingredients and product life-cycle management对新开发的原药及老的原药在制剂技术上都会投入重金Why? 为什么？,Why Formulation? 为什么要制成制剂使用
13、？,Active Ingredients dont work. 原药本身没有药效.Until they are made into formulations 除非原药被做成制剂后使用 Our customers buy formulated products in packs我们的客户购买的是包装好的农药制剂产品,Solutions溶液,Emulsions乳液,Suspensions悬浮液,Solids固体,Capsules胶囊,Untreated 没有使用过农药,Un-Formulated Herbicide 未经制剂加工的除草剂,Formulated Herbicide 经过配制的除草剂,
14、Liquid Formulation SC SL, EC液体制剂 水悬浮剂、可溶性液剂、乳油,Concentrated Flowable具流动性的浓缩产品,On dilution稀释过程,(SC: suspension concentrate; SL: soluble concentrate; EC: Emulsifiable concentrate,Solid Formulations WP WG 固体制剂 可湿粉、水分散粒剂,WP: Wettable Powder可湿性粉剂,WG水分散粒剂,WG (Pepite),WP,WG: Water Dispersible Granule 水分散粒剂
15、,可湿性粉剂,Requirements of a Formulation 制剂产品的要求,Basic requirements 基本要求Easy & safe to handle 操作简单和安全Can be applied (sprayed, etc) 方便使用 （如喷洒等）Works biologically 具有生物活性Stable (physically and chemically) 稳定性（物理、化学稳定性）Can be manufactured (to cost) 合适的生产成本Added value from formulations 配成制剂的增值作用Attractive an
16、d easy to handle 能吸引人并容易操作Improved safety 提高其安全性Improved efficacy 提高其药效,Wettable powder 可湿性粉剂application in Egypt circa 1980应用在埃及 大约在1980,Agricultural formulations can be very sophisticated农药制剂具有悠久的历史,trigger ruptures weak linkfor fast release at right place / time,Triggered release触发释放,First genera
17、tion第一代,New surface properties新表面特性,Anionic阴离子,Cationic阳离子,Liquid液体,+,-,Improved handling改善操作Targeted activity 活性目标Differentiated products 产品多样化New markets 新市场Extended patent protection 扩大专利保护范围,Zeon is a Reg. trademark,触发剂割裂脆弱处在合适的时间/地点释放,Crop Protection Industry: a view from the West西方作物保护工业概览,App
18、rox $30 Billion per annum sales 每年销售额大约300亿美元Market drivers 市场驱动Performance enhancement 增强药效Cost Reduction 降低成本Environment/ regulations 环境/法规Environmental concerns 环境关注Fewer new actives / new modes of action 新原药较少/新作用模式Life cycle management 产品的生命周期管理How to enhance value of mature active ingredients?
19、 怎样增加成熟原药的价值？,What do Companies think? 公司在考虑什么？,“Product innovation using existing active ingredients” “运用新技术对现有的原药进行创新” Combining active ingredients in novel combination products drives innovation. 运用新技术，对产品重新配制，以推动创新。Novel formulation technology enables new products from existing compounds which h
20、ave new levels of activity, safety and spectrum, both as sprayed products and increasingly as seed treatments.利用新的制剂技术可以使现有的原药，无论是用于喷洒还是日益增长的种子处理剂，成为高效、安全、广谱的新产品。Bayer annual review: 拜尔年度回顾Formulation know-how translates into competitive edge制剂技术成为竞争的优势Different technologies are used to formulate th
21、e active ingredient into a product with optimal application properties采用的不同技术，将原药配制成具有最佳应用性能的产品,Syngenta Annual Review 2005 先正达2005年度回顾,Formulation Trends 制剂的发展趋势,Increasing complexity 日益复杂mixtures, AI properties, novel technology,混合制剂，原药的性能，新型技术Continued regulatory pressure (environment)持续的法规压力（环境）
22、cost pressures 成本压力Formulation differentiation increasingly important to agri business 制剂的多样性对农业行业日益重要,Formulation Research : Historic View 制剂技术研究：历史回顾,1970s,2000s,1990s,1980s,ECs and WPs乳油和可湿性粉剂,SCs and EWs水悬浮剂&乳液o/w,Microcapsules微胶囊,WGs 水分散颗粒,Adjuvants 助剂,Novel Physical Forms具有新性能的产品,Oil Dispersio
23、ns油分散产品,Safety安全,Safety, Environmental and Efficacy安全，环境和有效,Convenience / Safety / Environmental方便/安全/环境,Efficacy 有效,Convenience方便,Convenience / labile AIs方便/有效成份进入植物组织,Formulation Benefits 配制成制剂的益处,Case studies: 实例研究Increased biological performance (adjuvants)增强生物性能（助剂）Improved handling and applica
24、tion characteristics 改善操作和应用特性Controlled release & enhanced safety 控制释放和增强安全性,Increased biological performance 增强生物活性,The use of adjuvants may improve the performance or allow a reduced rate of many active ingredients 助剂的使用可以改善应用性能或可以降低使用原药的用量,Adjuvants: Improved Efficacy 助剂：改善功效,Example : Adjuvant
25、can improve activity by : increasing droplet spreadincreasing leaf uptake例如：助剂可以通过下列方式改善活性增加液滴的扩散增加植物叶片的吸收,No adjuvant 没有助剂,With adjuvant 有助剂,Novel adjuvant新型助剂,Standard adjuvant 标准助剂,No adjuvant无助剂,时间,Adjuvancy: the “on-off“ switch for pinoxaden,当天应用,未处理,没有助剂,有助剂,未处理,没有助剂,有助剂,应用20天以后,Not Just Herbi
26、cides! 不只是除草剂,Bayer WOO2098230-fatty alcohol alkoxylates with insecticides拜尔WOO2098230烷氧基脂肪醇与杀虫剂 WO 2003/099012A1 Syngenta 先正达2003/09912A1 Use of phosphonate adjuvants with insecticides 在杀虫剂中使用磷酸酯做助剂 Exemplified by bis(2-ethylhexyl)-2-ethylhexyl phosphonate (BEEP) 例如：双（2乙基己基）2乙基己基磷酸酯,吸收/转移,24小时后吸收/转
27、移48小时后吸收/转移,死亡率,多杀菌素,氯芬新,甲氨基阿维菌素苯甲酸盐,死亡率,死亡率,吸收/imidacloprid 的转移,Improved Handling and Application 改善操作和应用,Formula M, a new technology in Seed Treatment配方M，在种子处理中的新技术,Treated seeds 种子处理,Celest Extra (current) Celest Extra（目前）,Celest Extra Formula M Celest Extra 配方M,Formula M provides 配方M可以具有 Improve
28、d coverage (homogeneity of treatment) 改善覆盖层（处理均匀性） Improved appearance (stronger colour) 改善外观（较强的色泽） Reduced human exposure (less dust-off) 减少与人体接触 （较少脱落） Faster processing of treated seed (faster drying) 加快种子处理过程 （快速干燥）,Less Dust-off : safer product 更少的脱落：更安全的产品,Dust-off filter, A8533F 200 mL/100kg
29、 on wheat, diluted with 400mL water ST22TA828/03粉尘滤膜，A8533F200ml/100kg，用于小麦。用400ml水稀释ST22TA828/03,Dust-off filter, A8533G 200 mL/100kg on wheat, diluted with 400 mL water ST22TA828/09 滤膜A8533G 200 mL/100kg，用于小麦。 用400ml水稀释ST22TA828/09,Celest Extra (current)目前,Celest Extra Formula M 配方M,脱落，克/100公斤小麦,H
30、igher productivity for treating companies种子处理公司有更高的生产能力,Celest 025 FS (current)目前,Celest 025 FS formula M配方M,Improvement of bagging time by 15%!减少15的包装时间,Controlled Release and Enhanced Safety 控制释放和增强安全性,Karate and Demand: microencapsulation provides many benefits功夫和大灭：微胶囊化可以提供很多好处,Microencapsulatio
31、n (1st Generation) 微胶囊化（第一代）,Demand,High load capacity; safening; environmental高容量；安全；环保Robust - designed for slow release 可靠-设计为缓慢释放,Micro-encapsulation (2nd Generation) 微乳胶囊化（第二代）氯氟氰菊酯微胶囊剂,Improved safety 改善安全性Safer mammalian tox 对哺乳动物更安全Lower solvent levels 更低的溶剂量Improved performance 改善性能Efficacy
32、 EC by fast release 功效通过快速释放的ECUV protectant 防紫外线保护剂,Capsule Suspensions 悬浮剂,Capsules suspended in a liquid base giving a flowable suspension concentrate. 胶囊悬浮在液体中，生产出具有流动性的悬浮剂,Microcapsules 微胶囊,Typically 1-20 micron hollow spheres filled with AI通常活性成分被填入120微米的空心球中High load capacity 高容量Aqueous (CS)
33、or dry products水溶液（悬浮液）或固体产品,Reservoir储存囊,Matrix母体,Control of parameters to vary release rate: 控制参数以控制释放速率：particle size 颗粒大小monomer composition单体成分cross-link density铰链密度wall thickness壁厚,Stabiliser稳定剂,olymeric wall聚合物墙壁,continuousPhase 连续相,Active Ingredient活性成分,r,r”,c,c,Conventional Microcapsules Re
34、lease by Diffusion Control常规的微胶囊释放是由控制扩散完成的,释放速率,表面积,扩散浓度,墙壁厚度,渗透性,扩撒系数,分配系数,Applications Beyond Conventional Technology新技术的应用,Reduced mammalian tox降低哺乳动物毒性,Targeting against pest Pressure 将害虫作为目标的压力,season long control from one application一次施药可长期有效,Reduced antagonism降低抗性,Extended release for establ
35、ished benefits延长有效成份释放到受药体,research challenges ! 研究挑战,Beneficial insect protection 保护益虫,Chemically Triggered Release Strategy化学方法触发法,custom designed weak links are incorporated into the wall during polymerisation 在聚合过程中将结合力较弱的物质嵌入内壁trigger is activated at chosen moment - ruptures weak link 在合适的时间，触发
36、剂被激活，结合力较弱处断裂punctures reduce wall thickness (r-r”) to zero, circumventing the normal diffusion process 渗透物使壁厚变小(r-r”) 到0，打破常规的正常的扩散过程,triggerrupturesweak linkallowingfast release,weak link,AI,AI,触发剂,可以快速释放,结合力较弱处,裂开,释放率,结合力较弱的物质,Acid Triggered Capsules酸触发胶囊,Non-triggered没有被触发的,Triggered触发的,Future V
37、ision: From a Western perspective未来前景：西方展望,Further restrictions in the regulatory environment 环境法规更加严格 Continued need for safer, more effective products 持续需要更安全，更有效的产品 Increased accessibility to useful triggered systems for targeted delivery 利用有用的触发机制，增强（药物）达到目标受体能力 Improved adjuvants offer reduced
38、application rates 改善助剂以降低施用量 Increased role of polymeric systems to deliver better controlled release systems (including nanotechnologies) 增加聚合系统的作用，更好地控制释放系统（包括纳米技术，10-9） Greater understanding of crystallisation processes 更好地了解结晶过程 Changing pesticide chemistries will provide continually changing ch
39、allenges to the formulator不断变化的农药化学将会对制剂开发人员带来持续的挑战,Formulation Research : Future 制剂研究：未来,1990s,?,2010s,2000s,New ECs and solvents新型乳油及溶剂,SCs and EWs-more robust technology悬浮剂和乳液更多的完备技术,Controlled delivery 控制传递,New dry products technology 新型固体制剂技术,Adjuvants and uptake understanding 辅剂和吸收的认识,Novel Ph
40、ysical Forms 改变物理性能新技术,New delivery technology 新型传递技术,Formulation Failure? 配方会失败？,Risk factors: 风险因素- Development was too fast 发展太快- Poor raw materials 原料贫乏- Not tested in proper conditions 未在合适的条件进行测试Impact of failure: 失败带来的影响- Poor handling (sediment, blocked screens) 施用困难（沉淀，堵塞）- Crop injury (too
41、 much product applied)伤害作物（用药量太大）- Lack of efficacy (not enough product applied) 缺乏药效（产品的应用不充分）- Human exposure (cleaning up the mess!)人体暴露（处理废物）- Reduced crop yield (improper treatment) 降低作物产量（不恰当的使用）,Conclusions 结论,Formulations provide many benefits 制剂可以再来很多好处Improved efficacy 改善药效Improved applica
42、tion 改善应用Safer handling 更安全的操作Improved environmental profile 改善环境Etc. 等等Proper formulation development can take years of research in the laboratory 一个合适的制剂通常需要在实验室里经过数年的研究Do it right! Reduce the risk of failure 正确的方法可以降低失败的风险Added benefits & development time costs money! 增加产品的价值及花费的研发时间是需要投资的！,THANK YOU!谢谢,
