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1、Agrochemical Formulation Trends農(nóng)藥制劑的開展趨勢(shì)CCPIAGuilin, Guangxi, China中國(guó) 桂林Keith Parker, Ph.D.Syngenta Asia Pacific Pte. Ltd.Who is Syngenta 先正達(dá)引見Agrochemical Formulation Trends農(nóng)業(yè)化學(xué)配方的開展趨勢(shì)Contents 內(nèi)容Our industry family tree 國(guó)際農(nóng)化公司開展概略CibaSandozICIISK BiosciencesMonsantoDuPontShellCyanamidBASFBayerRhone
2、-PoulencHoechstScheringDowRohm & HaasMerck1992199319941995199619971998199920002001NovartisAHPAventis2002AgrevoZenecaExcellent complementary and leading product portfolio杰出全面、領(lǐng)先的產(chǎn)品線 A leader in crop protection 植保領(lǐng)域的領(lǐng)先者 Third in high-value commercial seeds 高價(jià)值商業(yè)種子排名第三First class research and developme
3、nt resources 一流的研發(fā)資源 Investment of around $800m annually 每年投入約八億美圓Strong worldwide presence 業(yè)務(wù)遍及全球 Around 21,000 employees in over 90 countries 在90多個(gè)國(guó)家擁有2萬(wàn)1千名雇員Rich pipeline of Crop Protection and Seeds products豐富的植保和種子產(chǎn)品產(chǎn)銷渠道Syngenta a leading global agribusiness先正達(dá)全球領(lǐng)先的農(nóng)業(yè)科技公司Syngenta a leading glob
4、al agribusiness先正達(dá)全球領(lǐng)先的農(nóng)業(yè)科技公司 million tonnes of cotton is grown using our crop protection products全球440萬(wàn)噸棉花種植過(guò)程中運(yùn)用先正達(dá)植保產(chǎn)品Thats the equivalent of 20 billion T-Shirts這相當(dāng)于200億件T恤的用料4.4Syngenta a leading global agribusiness先正達(dá)全球領(lǐng)先的農(nóng)業(yè)科技公司70% of Scotch Whisky is produced by Syngenta barley70% 蘇格蘭威士忌是用先正達(dá)大
5、麥制造的What We Do 我們從事哪些業(yè)務(wù)Crop Protection作物維護(hù)Seeds種子 Professional Products專業(yè)產(chǎn)品 Bio-technology生物技術(shù) Major product brands 主要的產(chǎn)品品牌Herbicides 除草劑Professional products 專業(yè)產(chǎn)品Fungicides 殺菌劑Insecticides 殺蟲劑Seeds 種子 阿克泰金雷世高阿米西達(dá)銳勝泰草達(dá)克無(wú)蹤功夫千層紅Rank排名2006 R&D spend2006 研發(fā)投入 $ m1Syngenta 先正達(dá)2Bayer 拜爾4BASF 巴斯夫5DuPont 杜邦
6、3Monsanto 孟山都6Dow 陶氏As % of Sales銷售百分比11%10%10%14%11%10%The leader in research and development 先正達(dá),研討與開發(fā)的指點(diǎn)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 全球研發(fā)機(jī)構(gòu)美國(guó)格林斯博羅GREENSBOROFormulationEnvironmental Science美國(guó)SBIBiotechnologyR&D英國(guó)集能山JEALOTTS HILLChemical DiscoveryWeed ControlFormulationBioscienceEnvironmental Science瑞士巴塞爾/斯坦恩BASEL/STEINFungicides, Insecticides &Professional Products印度果阿GOAChemistrySyngenta in China 先正達(dá)在中國(guó)Crop Protect
8、ion作物維護(hù)Seeds 種子 Professional Products專業(yè)產(chǎn)品 R&D研發(fā)A history of more than 100 years 百多年協(xié)作歷史 Associated investment US$ 200m 目前總投資達(dá)2億美圓 40% of the total direct foreign investment in CP section投資額占中國(guó)市場(chǎng)植保領(lǐng)域外商直接投資的40Investment in China 先正達(dá)在中國(guó)的投資Syngenta (Suzhou) Crop Protection Co., Ltd.Syngenta Seeds Compan
9、y Ltd.Syngenta Nantong Crop Protection Co., Ltd.Environment Protection Responsibility in China先正達(dá)在中國(guó)環(huán)保社會(huì)責(zé)任“Top 100 Environmental Friendly Projects by State Environmental Protection Administration “the only one of its kind in crop protection industry “國(guó)家環(huán)保局授予的“百佳環(huán)保工程榮譽(yù)稱號(hào)植保行業(yè)中獨(dú)一獲此殊榮 “Top 10 environmen
10、tal friendly enterprises “江蘇省十大環(huán)保企業(yè)“High-tech enterprises in Jiangsu province “江蘇省高新技術(shù)企業(yè) Provide technical support for industry / national standards setup為行業(yè)規(guī)范設(shè)定提供技術(shù)支持 Chinas sustainable agriculture development through innovative research and technology經(jīng)過(guò)創(chuàng)新性的研討和技術(shù),中國(guó)農(nóng)業(yè)的可繼續(xù)性開展Improve crop productivit
11、y, quality and safety through integrated solutions經(jīng)過(guò)完好的方案,提高和改善作物產(chǎn)量,質(zhì)量和平安性Upgrade Chinese farmers income and the quality of life提升中國(guó)農(nóng)民的收入和生活質(zhì)量Syngenta China is Committed To先正達(dá)中國(guó)忠于.Who is Syngenta 先正達(dá)引見Agrochemical Formulation Trends農(nóng)業(yè)化學(xué)配方的開展趨勢(shì)Contents 內(nèi)容Formulation Technology 制劑技術(shù)Agribusiness invest
12、s heavily in Formulation Science 在制劑技術(shù)的上開發(fā)上,農(nóng)化企業(yè)投入重金B(yǎng)oth for first launch of new Active Ingredients and product life-cycle management對(duì)新開發(fā)的原藥及老的原藥在制劑技術(shù)上都會(huì)投入重金Why? 為什么?Why Formulation? 為什么要制成制劑運(yùn)用?Active Ingredients dont work. 原藥本身沒(méi)有藥效.Until they are made into formulations 除非原藥被做成制劑后運(yùn)用 Our customers bu
13、y formulated products in packs我們的客戶購(gòu)買的是包裝好的農(nóng)藥制劑產(chǎn)品Solutions溶液Emulsions乳液Suspensions懸浮液Solids固體Capsules膠囊Untreated 沒(méi)有運(yùn)用過(guò)農(nóng)藥Un-Formulated Herbicide 未經(jīng)制劑加工的除草劑Formulated Herbicide 經(jīng)過(guò)配制的除草劑Liquid Formulation SC SL, EC液體制劑 水懸浮劑、可溶性液劑、乳油Concentrated Flowable具流動(dòng)性的濃縮產(chǎn)品On dilution稀釋過(guò)程(SC: suspension concentrat
14、e; SL: soluble concentrate; EC: Emulsifiable concentrate Solid Formulations WP WG 固體制劑 可濕粉、水分散粒劑WP: Wettable Powder可濕性粉劑WG水分散粒劑 WG (Pepite)WPWG: Water Dispersible Granule 水分散粒劑 可濕性粉劑Requirements of a Formulation 制劑產(chǎn)品的要求Basic requirements 根本要求Easy & safe to handle 操作簡(jiǎn)單和平安Can be applied (sprayed, etc)
15、 方便運(yùn)用 如噴灑等Works biologically 具有生物活性Stable (physically and chemically) 穩(wěn)定性物理、化學(xué)穩(wěn)定性Can be manufactured (to cost) 適宜的消費(fèi)本錢Added value from formulations 配成制劑的增值作用Attractive and easy to handle 能吸引人并容易操作Improved safety 提高其平安性Improved efficacy 提高其藥效Wettable powder 可濕性粉劑application in Egypt circa 1980運(yùn)用在埃及 大
16、約在1980Agricultural formulations can be very sophisticated農(nóng)藥制劑具有悠久的歷史trigger ruptures weak linkfor fast release at right place / timeTriggered release觸發(fā)釋放Polymer layers聚合物層First generation第一代New surface properties新外表特性Anionic陰離子Cationic陽(yáng)離子Liquid液體+-Improved handling改善操作Targeted activity 活性目的Different
17、iated products 產(chǎn)品多樣化New markets 新市場(chǎng)Extended patent protection 擴(kuò)展專利維護(hù)范圍Zeon is a Reg. trademark觸發(fā)劑割裂脆弱處在適宜的時(shí)間/地點(diǎn)釋放Crop Protection Industry: a view from the West西方作物維護(hù)工業(yè)概覽Approx $30 Billion per annum sales 每年銷售額大約300億美圓Market drivers 市場(chǎng)驅(qū)動(dòng)Performance enhancement 加強(qiáng)藥效Cost Reduction 降低本錢Environment/ regu
18、lations 環(huán)境/法規(guī)Environmental concerns 環(huán)境關(guān)注Fewer new actives / new modes of action 新原藥較少/新作用方式Life cycle management 產(chǎn)品的生命周期管理How to enhance value of mature active ingredients? 怎樣添加成熟原藥的價(jià)值?What do Companies think? 公司在思索什么? “Product innovation using existing active ingredients “運(yùn)用新技術(shù)對(duì)現(xiàn)有的原藥進(jìn)展創(chuàng)新 Combining
19、active ingredients in novel combination products drives innovation. 運(yùn)用新技術(shù),對(duì)產(chǎn)品重新配制,以推進(jìn)創(chuàng)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.利用新的制劑技術(shù)可以使現(xiàn)有的原藥,無(wú)論是用
20、于噴灑還是日益增長(zhǎng)的種子處置劑,成為高效、平安、廣譜的新產(chǎn)品。Bayer annual review: 拜爾年度回想Formulation know-how translates into competitive edge制劑技術(shù)成為競(jìng)爭(zhēng)的優(yōu)勢(shì)Different technologies are used to formulate the active ingredient into a product with optimal application properties采用的不同技術(shù),將原藥配制成具有最正確運(yùn)用性能的產(chǎn)品Syngenta Annual Review 2005 先正達(dá)2005
21、年度回想Formulation Trends 制劑的開展趨勢(shì) Increasing complexity 日益復(fù)雜mixtures, AI properties, novel technology,混合制劑,原藥的性能,新型技術(shù)Continued regulatory pressure (environment)繼續(xù)的法規(guī)壓力環(huán)境cost pressures 本錢壓力Formulation differentiation increasingly important to agri business 制劑的多樣性對(duì)農(nóng)業(yè)行業(yè)日益重要Formulation Research : Historic
22、View 制劑技術(shù)研討:歷史回想1970s2000s1990s1980sECs and WPs乳油和可濕性粉劑SCs and EWs水懸浮劑&乳液o/wMicrocapsules微膠囊WGs 水分散顆粒Adjuvants 助劑Novel Physical Forms具有新性能的產(chǎn)品Oil Dispersions油分散產(chǎn)品Safety平安Safety, Environmental and Efficacy平安,環(huán)境和有效Convenience / Safety / Environmental方便/平安/環(huán)境Efficacy 有效Convenience方便Convenience / labile
23、AIs方便/有效成份進(jìn)入植物組織Formulation Benefits 配制成制劑的益處Case studies: 實(shí)例研討Increased biological performance (adjuvants)加強(qiáng)生物性能助劑Improved handling and application characteristics 改善操作和運(yùn)用特性Controlled release & enhanced safety 控制釋放和加強(qiáng)平安性 Increased biological performance 加強(qiáng)生物活性The use of adjuvants may improve the pe
24、rformance or allow a reduced rate of many active ingredients 助劑的運(yùn)用可以改善運(yùn)用性能或可以降低運(yùn)用原藥的用量Adjuvants: Improved Efficacy 助劑:改善效果Example : Adjuvant can improve activity by : increasing droplet spreadincreasing leaf uptake例如:助劑可以經(jīng)過(guò)以下方式改善活性添加液滴的分散添加植物葉片的吸收No adjuvant 沒(méi)有助劑With adjuvant 有助劑Novel adjuvant新型助劑St
25、andard adjuvant 規(guī)范助劑No adjuvant無(wú)助劑時(shí)間Adjuvancy: the “on-off“ switch for pinoxaden當(dāng)天運(yùn)用未處置沒(méi)有助劑有助劑未處置沒(méi)有助劑有助劑運(yùn)用20天以后Not Just Herbicides! 不只是除草劑 Bayer WOO2098230-fatty alcohol alkoxylates with insecticides拜爾WOO2098230烷氧基脂肪醇與殺蟲劑 WO 2003/099012A1 Syngenta 先正達(dá)2003/09912A1 Use of phosphonate adjuvants with in
26、secticides 在殺蟲劑中運(yùn)用磷酸酯做助劑 Exemplified by bis(2-ethylhexyl)-2-ethylhexyl phosphonate (BEEP) 例如:雙2乙基己基2乙基己基磷酸酯吸收/轉(zhuǎn)移24小時(shí)后吸收/轉(zhuǎn)移48小時(shí)后吸收/轉(zhuǎn)移死亡率多殺菌素氯芬新 甲氨基阿維菌素苯甲酸鹽 死亡率死亡率吸收/imidacloprid 的轉(zhuǎn)移Improved Handling and Application 改善操作和運(yùn)用Formula M, a new technology in Seed Treatment配方M,在種子處置中的新技術(shù)Treated seeds 種子處置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) 改善覆蓋層處置均勻性 Improved appearance (stronger colour) 改善外觀較強(qiáng)的色澤 Reduced human exposure (less dust-off) 減少與人體接觸 較少零落 Faster processing of treated seed (faster d
28、rying) 加快種子處置過(guò)程 快速枯燥L(fēng)ess Dust-off : safer product 更少的零落:更平安的產(chǎn)品Dust-off filter, A8533F 200 mL/100kg on wheat, diluted with 400mL water ST22TA828/03粉塵濾膜,A8533F200ml/100kg,用于小麥。用400ml水稀釋ST22TA828/03Dust-off filter, A8533G 200 mL/100kg on wheat, diluted with 400 mL water ST22TA828/09 濾膜A8533G 200 mL/100
29、kg,用于小麥。 用400ml水稀釋ST22TA828/09Celest Extra (current)目前Celest Extra Formula M 配方M零落,克/100公斤小麥Higher productivity for treating companies種子處置公司有更高的消費(fèi)才干Celest 025 FS (current)目前Celest 025 FS formula M配方MImprovement of bagging time by 15%!減少15的包裝時(shí)間Controlled Release and Enhanced Safety 控制釋放和加強(qiáng)平安性Karate a
30、nd Demand: microencapsulation provides many benefits功夫和大滅:微膠囊化可以提供很多益處Microencapsulation (1st Generation) 微膠囊化第一代polymericWall聚合物壁Water水Lambda in solvent高效氯氟氰菊脂在溶劑中 UV protectant 紫外線維護(hù)劑Demand High load capacity; safening; environmental高容量;平安;環(huán)保Robust - designed for slow release 可靠-設(shè)計(jì)為緩慢釋放Micro-encap
31、sulation (2nd Generation) 微乳膠囊化第二代氯氟氰菊酯微膠囊劑 Improved safety 改善平安性Safer mammalian tox 對(duì)哺乳動(dòng)物更平安Lower solvent levels 更低的溶劑量Improved performance 改善性能Efficacy EC by fast release 效果經(jīng)過(guò)快速釋放的ECUV protectant 防紫外線維護(hù)劑Lambda DemandParathion-methylLambda ZeonCapsule Suspensions 懸浮劑Capsules suspended in a liquid b
32、ase giving a flowable suspension concentrate. 膠囊懸浮在液體中,消費(fèi)出具有流動(dòng)性的懸浮劑Microcapsules 微膠囊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水溶液懸浮液或固體產(chǎn)品Reservoir儲(chǔ)存囊Matrix母體Control of parameters to vary release rate: 控制參數(shù)以控制釋放速率:particle
33、size 顆粒大小monomer composition單體成分cross-link density鉸鏈密度wall thickness壁厚Stabiliser穩(wěn)定劑polymeric wall聚合物墻壁continuousPhase 延續(xù)相 Active Ingredient活性成分rrccConventional Microcapsules Release by Diffusion Control常規(guī)的微膠囊釋放是由控制分散完成的釋放速率外表積分散濃度墻壁厚度浸透性擴(kuò)撒系數(shù)分配系數(shù)Applications Beyond Conventional Technology新技術(shù)的運(yùn)用Reduce
34、d mammalian tox降低哺乳動(dòng)物毒性Targeting against pest Pressure 將害蟲作為目的的壓力season long control from one application一次施藥可長(zhǎng)期有效Reduced antagonism降低抗性Hours / days / monthsTriggers;觸發(fā)劑pH, light, temp,pH,光線,溫度 Hours / days / monthsAI seenby target農(nóng)藥有效成份到達(dá)標(biāo)靶EC浮油Microcap微膠囊Hrs / days / mthsExtended release for establ
35、ished benefits延伸有效成份釋放到受藥體research challenges ! 研討挑戰(zhàn)Beneficial insect protection 維護(hù)益蟲Chemically Triggered Release Strategy化學(xué)方法觸發(fā)法custom designed weak links are incorporated into the wall during polymerisation 在聚合過(guò)程中將結(jié)合力較弱的物質(zhì)嵌入內(nèi)壁trigger is activated at chosen moment - ruptures weak link 在適宜的時(shí)間,觸發(fā)劑被激活
36、,結(jié)合力較弱處斷裂punctures reduce wall thickness (r-r) to zero, circumventing the normal diffusion process 浸透物使壁厚變小(r-r) 到0,突破常規(guī)的正常的分散過(guò)程triggerrupturesweak linkallowingfast releaseweak linkAIAI觸發(fā)劑可以快速釋放結(jié)合力較弱處裂開釋放率結(jié)合力較弱的物質(zhì)Acid Triggered Capsules酸觸發(fā)膠囊Non-triggered沒(méi)有被觸發(fā)的Triggered觸發(fā)的Future Vision: From a Wester
37、n perspective未來(lái)前景:西方展望 Further restrictions in the regulatory environment 環(huán)境法規(guī)更加嚴(yán)厲 Continued need for safer, more effective products 繼續(xù)需求更平安,更有效的產(chǎn)品 Increased accessibility to useful triggered systems for targeted delivery 利用有用的觸發(fā)機(jī)制,加強(qiáng)藥物到達(dá)目的受體才干 Improved adjuvants offer reduced application rates 改善助劑以降低施用量 Increased role of polymeric systems to deliver better controlled release systems (including nanotechnologies) 添加聚合系統(tǒng)的作用,更好地控制釋放系統(tǒng)包括納米技術(shù),10-9 Greater understanding of crystallisation processes 更好
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