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1、Agrochemical Formulation Trends农药制剂的开展趋势CCPIAGuilin, Guangxi, China中国 桂林Keith Parker, Ph.D.Syngenta Asia Pacific Pte. Ltd.Who is Syngenta 先正达引见Agrochemical Formulation Trends农业化学配方的开展趋势Contents 内容Our industry family tree 国际农化公司开展概略CibaSandozICIISK BiosciencesMonsantoDuPontShellCyanamidBASFBayerRhone
2、-PoulencHoechstScheringDowRohm & HaasMerck1992199319941995199619971998199920002001NovartisAHPAventis2002AgrevoZenecaExcellent complementary and leading product portfolio杰出全面、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 高价值商业种子排名第三First class research and developme
3、nt resources 一流的研发资源 Investment of around $800m annually 每年投入约八亿美圆Strong worldwide presence 业务遍及全球 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 agribusiness先正达全球领先的农业科技公司Syngenta a leading glob
4、al 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运用先正达植保产品Thats the equivalent of 20 billion T-Shirts这相当于200亿件T恤的用料4.4Syngenta a leading global agribusiness先正达全球领先的农业科技公司70% of Scotch Whisky is produced by Syngenta barley70% 苏格兰威士忌是用先正达大
5、麦制造的What We Do 我们从事哪些业务Crop Protection作物维护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 spend2006 研发投入 $ m1Syngenta 先正达2Bayer 拜尔4BASF 巴斯夫5DuPont 杜邦
6、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,研讨与开发的指点者 Source: Phillips McDougall, SyngentaMajor R&D sites located at theheart of scientific communitiesOther sitesMarker-assisted and seed breeding capabilitiesGlobal field station networkGlobal R&
7、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, Insecticides &Professional Products印度果阿GOAChemistrySyngenta in China 先正达在中国Crop Protect
8、ion作物维护Seeds 种子 Professional Products专业产品 R&D研发A history of more than 100 years 百多年协作历史 Associated investment US$ 200m 目前总投资达2亿美圆 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40Investment in China 先正达在中国的投资Syngenta (Suzhou) Crop Protection Co., Ltd.Syngenta Seeds Compan
9、y 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 one 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独一获此殊荣 “Top 10 environmen
10、tal 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为行业规范设定提供技术支持 Chinas sustainable agriculture development through innovative research and technology经过创新性的研讨和技术,中国农业的可继续性开展Improve crop productivit
11、y, quality and safety through integrated solutions经过完好的方案,提高和改善作物产量,质量和平安性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 先正达引见Agrochemical Formulation Trends农业化学配方的开展趋势Contents 内容Formulation Technology 制剂技术Agribusiness invest
12、s 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? 为什么要制成制剂运用?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运用 Our customers bu
13、y 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 没有运用过农药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 concentrat
14、e; 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)WPWG: Water Dispersible Granule 水分散粒剂 可湿性粉剂Requirements of a Formulation 制剂产品的要求Basic requirements 根本要求Easy & safe to handle 操作简单和平安Can be applied (sprayed, etc)
15、 方便运用 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) 适宜的消费本钱Added value from formulations 配成制剂的增值作用Attractive and easy to handle 能吸引人并容易操作Improved safety 提高其平安性Improved efficacy 提高其药效Wettable powder 可湿性粉剂application in Egypt circa 1980运用在埃及 大
16、约在1980Agricultural 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 / timeTriggered release触发释放Polymer layers聚合物层First generation第一代New surface properties新外表特性Anionic阴离子Cationic阳离子Liquid液体+-Improved handling改善操作Targeted activity 活性目的Different
17、iated products 产品多样化New markets 新市场Extended patent protection 扩展专利维护范围Zeon is a Reg. trademark触发剂割裂脆弱处在适宜的时间/地点释放Crop Protection Industry: a view from the West西方作物维护工业概览Approx $30 Billion per annum sales 每年销售额大约300亿美圆Market drivers 市场驱动Performance enhancement 加强药效Cost Reduction 降低本钱Environment/ regu
18、lations 环境/法规Environmental concerns 环境关注Fewer new actives / new modes of action 新原药较少/新作用方式Life cycle management 产品的生命周期管理How to enhance value of mature active ingredients? 怎样添加成熟原药的价值?What do Companies think? 公司在思索什么? “Product innovation using existing active ingredients “运用新技术对现有的原药进展创新 Combining
19、active ingredients in novel combination products drives innovation. 运用新技术,对产品重新配制,以推进创新。Novel formulation technology enables new products from existing compounds which have 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
20、于喷洒还是日益增长的种子处置剂,成为高效、平安、广谱的新产品。Bayer annual review: 拜尔年度回想Formulation know-how translates into competitive edge制剂技术成为竞争的优势Different technologies are used to formulate the 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正确运用性能的产品Syngenta Annual Review 2005 先正达2005
21、年度回想Formulation Trends 制剂的开展趋势 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)继续的法规压力环境cost pressures 本钱压力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
22、View 制剂技术研讨:历史回想1970s2000s1990s1980sECs and WPs乳油和可湿性粉剂SCs and EWs水悬浮剂&乳液o/wMicrocapsules微胶囊WGs 水分散颗粒Adjuvants 助剂Novel Physical Forms具有新性能的产品Oil Dispersions油分散产品Safety平安Safety, Environmental and Efficacy平安,环境和有效Convenience / Safety / Environmental方便/平安/环境Efficacy 有效Convenience方便Convenience / labile
23、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: 实例研讨Increased biological performance (adjuvants)加强生物性能助剂Improved handling and application characteristics 改善操作和运用特性Controlled release & enhanced safety 控制释放和加强平安性 Increased biological performance 加强生物活性The use of adjuvants may improve the pe
24、rformance or allow a reduced rate of many active ingredients 助剂的运用可以改善运用性能或可以降低运用原药的用量Adjuvants: Improved Efficacy 助剂:改善效果Example : Adjuvant can improve activity by : increasing droplet spreadincreasing leaf uptake例如:助剂可以经过以下方式改善活性添加液滴的分散添加植物叶片的吸收No adjuvant 没有助剂With adjuvant 有助剂Novel adjuvant新型助剂St
25、andard adjuvant 规范助剂No adjuvant无助剂时间Adjuvancy: the “on-off“ switch for pinoxaden当天运用未处置没有助剂有助剂未处置没有助剂有助剂运用20天以后Not Just Herbicides! 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 in
26、secticides 在杀虫剂中运用磷酸酯做助剂 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 改善操作和运用Formula M, a new technology in Seed Treatment配方M,在种子处置中的新技术Treated seeds 种子处置Ce
27、lest Extra (current) Celest Extra目前Celest Extra Formula M Celest Extra 配方MFormula M provides 配方M可以具有 Improved coverage (homogeneity of treatment) 改善覆盖层处置均匀性 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 较少零落 Faster processing of treated seed (faster d
28、rying) 加快种子处置过程 快速枯燥Less Dust-off : safer product 更少的零落:更平安的产品Dust-off filter, A8533F 200 mL/100kg on wheat, diluted with 400mL water ST22TA828/03粉尘滤膜,A8533F200ml/100kg,用于小麦。用400ml水稀释ST22TA828/03Dust-off filter, A8533G 200 mL/100kg on wheat, diluted with 400 mL water ST22TA828/09 滤膜A8533G 200 mL/100
29、kg,用于小麦。 用400ml水稀释ST22TA828/09Celest Extra (current)目前Celest Extra Formula M 配方M零落,克/100公斤小麦Higher productivity for treating companies种子处置公司有更高的消费才干Celest 025 FS (current)目前Celest 025 FS formula M配方MImprovement of bagging time by 15%!减少15的包装时间Controlled Release and Enhanced Safety 控制释放和加强平安性Karate a
30、nd Demand: microencapsulation provides many benefits功夫和大灭:微胶囊化可以提供很多益处Microencapsulation (1st Generation) 微胶囊化第一代polymericWall聚合物壁Water水Lambda in solvent高效氯氟氰菊脂在溶剂中 UV protectant 紫外线维护剂Demand High load capacity; safening; environmental高容量;平安;环保Robust - designed for slow release 可靠-设计为缓慢释放Micro-encap
31、sulation (2nd Generation) 微乳胶囊化第二代氯氟氰菊酯微胶囊剂 Improved safety 改善平安性Safer mammalian tox 对哺乳动物更平安Lower solvent levels 更低的溶剂量Improved performance 改善性能Efficacy EC by fast release 效果经过快速释放的ECUV protectant 防紫外线维护剂Lambda DemandParathion-methylLambda ZeonCapsule Suspensions 悬浮剂Capsules suspended in a liquid b
32、ase giving a flowable suspension concentrate. 胶囊悬浮在液体中,消费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) 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
33、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polymeric wall聚合物墙壁continuousPhase 延续相 Active Ingredient活性成分rrccConventional Microcapsules Release by Diffusion Control常规的微胶囊释放是由控制分散完成的释放速率外表积分散浓度墙壁厚度浸透性扩撒系数分配系数Applications Beyond Conventional Technology新技术的运用Reduce
34、d mammalian tox降低哺乳动物毒性Targeting against pest Pressure 将害虫作为目的的压力season long control from one application一次施药可长期有效Reduced antagonism降低抗性Hours / days / monthsTriggers;触发剂pH, light, temp,pH,光线,温度 Hours / days / monthsAI seenby target农药有效成份到达标靶EC浮油Microcap微胶囊Hrs / days / mthsExtended release for establ
35、ished benefits延伸有效成份释放到受药体research challenges ! 研讨挑战Beneficial insect protection 维护益虫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 在适宜的时间,触发剂被激活
36、,结合力较弱处断裂punctures reduce wall thickness (r-r) to zero, circumventing the normal diffusion process 浸透物使壁厚变小(r-r) 到0,突破常规的正常的分散过程triggerrupturesweak linkallowingfast releaseweak linkAIAI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 Vision: From a Wester
37、n perspective未来前景:西方展望 Further restrictions in the regulatory environment 环境法规更加严厉 Continued need for safer, more effective products 继续需求更平安,更有效的产品 Increased accessibility to useful triggered systems for targeted delivery 利用有用的触发机制,加强药物到达目的受体才干 Improved adjuvants offer reduced 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) 添加聚合系统的作用,更好地控制释放系统包括纳米技术,10-9 Greater understanding of crystallisation processes 更好
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