CN1448053A - Thiophanate methyl inclusion complex pesticide preparation - Google Patents
Thiophanate methyl inclusion complex pesticide preparation Download PDFInfo
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- CN1448053A CN1448053A CN 03114670 CN03114670A CN1448053A CN 1448053 A CN1448053 A CN 1448053A CN 03114670 CN03114670 CN 03114670 CN 03114670 A CN03114670 A CN 03114670A CN 1448053 A CN1448053 A CN 1448053A
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- cyclodextrin
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- thiophanate methyl
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Abstract
The farm chemical preparation of thiophanate-methyl clatherate features that thiophanate-methyl molecules are included inside cyclodextrin with cyclic molecular structure. The said cyclodextrin may be any one kind of cyclodextrins or derivatives or their mixture. Cylcodextrin has many hydroxyl groups distributed in the outer part and thus high hydrophilicity and water solability, so that including water insoluble thiophanate-methyl with cyclodextrin can raise the water solability, stabilization, emulsifying capacity and germicidal effect of the farm chemical.
Description
Technical field
The invention belongs to the chemistry of pesticide technical field, particularly relate to the improvement of thiophanate methyl pesticidal preparations.
Background technology
Thiophanate methyl (Thiophanate-methyl) is the agricultural fungi bactericide of a kind of hypotoxicity commonly used, belongs to the interior absorption sterilization pesticide of wide spectrum; Have prevention and therapeutic action, be widely used in preventing and treating the fungal disease of fruit, vegetables, cigarette, cotton, grain, oil, flowers and other crops.This material is water insoluble, is soluble in acetone, formaldehyde, chloroform, dissolves in methyl alcohol, ethanol equal solvent.Present commercially available commodity mostly are 70% wetting powder or are added with the dry powder doses and the colloidal suspending agent of auxiliary material, and in use owing to directly water dissolving, thereby causing using more dusts.So just cause that the medicament administration amount increases, crop is difficult for absorbing, utilization ratio is low, drug molecule exposed influence its chemical stability, reduction drug effect cycle easily in addition.
Cyclodextrin be a class by the cyclic compound that 6,7 or 8 glucose units constitute, be called α-, β-or gamma-cyclodextrin.Its inner chamber with hollow is tubular structure, can the multiple organic compound molecule of envelope or some group wherein.Many hydroxyls because the cyclodextrin outside is distributing, good hydrophilic property makes cyclodextrin can be dissolved in water.
Do not find the documents and materials of relevant thiophanate methyl cyclodextrin inclusion complex preparation according to the retrieval.
Summary of the invention
Purpose of the present invention proposes a kind of thiophanate methyl inclusion complex preparation exactly, to solve the above-mentioned existing problems of said preparation; And the preparation method of proposition said preparation.
Technical scheme of the present invention is to realize in the following manner, the characteristics of described thiophanate methyl inclusion complex are: the thiophanate methyl molecule is by cyclodextrin ring shaped molecule structure institute envelope, constitute thiophanate methyl cyclodextrin inclusion complex preparation, described cyclodextrin can be any or several mixing of various cyclodextrin and derivative thereof.Its characteristics also have: described preparation is water solube powder or the aqua of dissolving or the emulsion of emulsification altogether or the pulvis that emulsion is made.Selected various cyclodextrin of the present invention and derivative thereof comprise alpha-cyclodextrin, beta-schardinger dextrin-, gamma-cyclodextrin, with the alkylation of these cyclodextrin, hydroxyalkylation, collateralization, carboxyethylation, and sulfuric ester or sulphonic acid ester ether derivative, also comprise the polymer of above-mentioned various cyclodextrin.Aqua of the present invention is the aqueous solution of thiophanate methyl cyclodextrin inclusion complex, and water solube powder is the pulvis that this aqueous solution dusts and obtains; Described emulsion is thiophanate methyl, cyclodextrin and the emulsifier emulsion of emulsification altogether, and obtains emulsified powder through dusting with this emulsion.
Preparation method according to the above thiophanate methyl cyclodextrin inclusion complex preparation is, thiophanate methyl and chemical assistant are mixed with cyclodextrin aqueous solution, obtains formulation products after envelope is handled, and wherein the weight ratio of thiophanate methyl and cyclodextrin is 1: 2-10.Described envelope is handled can adopt arbitrary modes such as stirring, homogenate, grinding, ultrasonic, and concrete selection should look production cost and process conditions are taken all factors into consideration; Not strict to temperature requirement when envelope is handled, can finish under the room temperature, but under 60 ℃ of conditions, can make the envelope better effects if, so temperature condition is determined in room temperature-60 ℃.Because the performance (mainly referring to molten water-based) of various cyclodextrin and derivative thereof is widely different, makes that the amount ranges of cyclodextrin is very big, can't further dwindle again; And this performance has also caused the difference of price, directly has influence on production cost, so use cyclodextrin and the concrete selection of derivative thereof to consider comprehensively.
Characteristics of the present invention are that also described chemical assistant is an organic solvent, can select any one or two kinds of organic solvents such as acetone, formaldehyde, chloroform, methyl alcohol, ethanol, and concrete selection should be looked production cost and crop influenced and take all factors into consideration.Its concrete preparation process is: with the thiophanate methyl organic solvent dissolution, mix with cyclodextrin aqueous solution again, obtain liquid preparation after envelope is handled.The liquid preparation drying that obtains is dusted, can obtain water solube powder.
Characteristics of the present invention are that also described chemical assistant is an emulsifier.Its concrete preparation process is: thiophanate methyl and emulsifier are added water make the emulsification suspension, mix with cyclodextrin aqueous solution, obtain emulsion formulations through the envelope inorganic agent.With the emulsion formulations that obtains again drying dust and obtain the pulvis of emulsification among the Yi Zaishui.Emulsifier is that a class can promote two kinds of mutual insoluble materials that form emulsion mutually.Emulsifier commonly used can be divided into natural and synthetic; Synthetic emulsifier comprises hydrophilic macromolecule, pressed powder and surfactant etc.Synthetic emulsifier also can be divided into ionic emulsifying agent, as dodecyl sodium sulfate etc.; Nonionic emulsifier such as polyethylene glycol, tween etc.; And mixed emulsifier, as diatomite etc.Natural emulsifier such as spaonin powder etc.
Because organic solvent and emulsifier occupy the space of envelope equally, thus organic solvent satisfy dissolved substance, emulsifier is satisfying under the prerequisite of medicine emulsification, the consumption of the two should be few more good more.The material total concentration should be greater than 15% during machine on drying is dusted for various in addition solution (comprising emulsion).These all are general knowledge, repeat no more.
Thiophanate methyl with water-soluble high cyclodextrin or derivatives thereof (as HP-, DM-etc.) envelope after, can make aqua or make pulvis soluble in water.If consider production cost, also can with beta-schardinger dextrin-or hybrid ring dextrin (contain α-, β-and gamma-cyclodextrin) envelope, to improve the water-soluble of agricultural chemicals.Being used in combination emulsifier again makes stable emulsion or makes the pulvis of emulsification among the Yi Zaishui.List carries out emulsification with emulsifier to thiophanate methyl, and the fineness of its emulsion, suspensibility, plate-out ability all can not reach desirable requirement.Be wettable powder or colloidal suspending agent such as the thiophanate methyl that generally uses at present.All be added with emulsifier in its prescription.These preparations all can't resolve even, the stable emulsification problem of thiophanate methyl.Certainly when using, can not evenly spray, more difficultly crop be absorbed fully contact with fungi, can not give full play to drug effect, to cause the waste of medicine.Thiophanate methyl is with behind the cyclodextrin envelope, makes water miscible or emulsify well and stable emulsion, makes not only that medicament is fine and smooth to be sprayed evenly, be easy on crop, adhere to absorption, also be easy to contact, give full play to drug effect with germ, prolong the drug effect phase, save the agricultural chemicals usage amount.Many hydroxyls because the cyclodextrin outside is distributing, good hydrophilic property makes cyclodextrin can be dissolved in water.Therefore, can be increased its stability, water-soluble and emulsion stability by the compound of cyclodextrin envelope.Simultaneously can be delayed rate of release and play slow releasing function by the medicine of cyclodextrin envelope.And by the medicine of cyclodextrine derivatives envelope, in vivo can rapid release.Water-insoluble in a word thiophanate methyl agricultural chemicals with the cyclodextrin envelope after, water-soluble, stable, emulsibility, raising bactericidal effect and the prolongation drug effect phase that can improve agricultural chemicals.
Embodiment
Embodiment 1, preparation thiophanate methyl cyclodextrin inclusion complex aqua and pulvis.
1.1) take by weighing thiophanate methyl 100g, add 196ml acetone, it is fully dissolved; Other gets HP-500g, adds 1 liter of dissolving of water; Under 50 ℃ of stirring conditions, the thiophanate methyl acetone soln is added, continue to stir 3 hours, obtain agricultural chemicals inclusion complex water liquid.This solution drying dusted obtain pulvis.
1.2) take by weighing thiophanate methyl 100g, add 350ml ethanol, it is fully dissolved; Other gets DM-800g, adds 2 liters of dissolvings of water; Under 60 ℃ of stirring conditions, cyclodextrin aqueous solution is added, continue to stir 2 hours, medicine inclusion complex water liquid.This solution drying duster is obtained pulvis.
1.3) take by weighing thiophanate methyl 98g, fully dissolve with 200ml acetone; Other gets gamma-cyclodextrin 200g and separates with 800ml is water-soluble; The two mixes the back and uses 1.6 ten thousand rev/mins of homogenates of high-speed homogenization machine 5 minutes, obtains agricultural chemicals inclusion complex water liquid.This liquid can be obtained pulvis through the super-dry duster.
Embodiment 2.Preparation thiophanate methyl cyclodextrin inclusion complex emulsion and pulvis thereof.
2.1) take by weighing thiophanate methyl 68g and add water 800ml, add " Macrogol 600 " 1000g stirring and emulsifying again and made emulsion in 1 hour; Other gets beta-schardinger dextrin-200g and adds 1 liter of dissolving of water, under 60 ℃ of stirring conditions, thiophanate methyl emulsion is added, and continues to stir 3 hours, obtains the stable emulsion of agricultural chemicals inclusion complex.This liquid drying duster can be obtained pulvis.
2.2) take by weighing thiophanate methyl 30g and add water 500ml, add " Macrogol 2000 " 60g stirring and emulsifying again and made emulsion in 1 hour, other get 290g hybrid ring dextrin (contain α-, β-and gamma-cyclodextrin 50%, other contains maltodextrin 50%) add 1 liter of dissolving of water, under 50 ℃ of stirring conditions, add thiophanate methyl emulsion, continue to stir 2 hours, add the 2g dodecyl sodium sulfate again and continue to stir 1 hour, obtain the stable emulsion of agricultural chemicals inclusion complex.This liquid can be obtained pulvis through the super-dry duster.
2.3) take by weighing thiophanate methyl 60g and add water 500ml, adding Tween 80 g stirring and emulsifying and made emulsion in 1 hour, other gets 250g α-and the mixture of beta-schardinger dextrin-, add 1 liter of dissolving of water, the two is mixed the back under the 40KHz condition, handled 1 hour, obtain the stable emulsion of agricultural chemicals inclusion complex with ultrasonic.This liquid drying duster can be obtained pulvis.
Claims (8)
1, a kind of thiophanate methyl inclusion complex pesticidal preparations is characterized in that, the thiophanate methyl molecule is constituted by cyclodextrin ring shaped molecule structure envelope; Described cyclodextrin can be a kind of or several mixing of various cyclodextrin and derivative thereof.
2, pesticidal preparations according to claim 1 is characterized in that, preparation is water solube powder or the aqua of dissolving or the emulsion of emulsification altogether or the pulvis that emulsion is made.
3, according to the preparation method of the described thiophanate methyl cyclodextrin of claim 1 inclusion complex pesticidal preparations, it is characterized in that, thiophanate methyl and chemical assistant are mixed with cyclodextrin aqueous solution, obtain formulation products after envelope is handled, wherein the weight ratio of thiophanate methyl and cyclodextrin is 1: 2-10.
4, preparation method according to claim 3 is characterized in that, described chemical assistant is an organic solvent, and preparation process is: with the thiophanate methyl organic solvent dissolution, mix with cyclodextrin aqueous solution again, obtain liquid preparation after envelope is handled.
5, preparation method according to claim 4 is characterized in that, with the liquid preparation that obtains again drying dust and obtain water solube powder.
6, preparation method according to claim 3 is characterized in that, described chemical assistant is an emulsifier, and preparation process is: thiophanate methyl and emulsifier are added water make the emulsification suspension, mix with cyclodextrin aqueous solution, handle obtaining emulsion formulations through envelope.
7, preparation method according to claim 6 is characterized in that, with the emulsion formulations that obtains again drying dust and obtain the pulvis of emulsification among the Yi Zaishui.
According to described any preparation method of claim 3-7, it is characterized in that 8, described envelope is handled can adopt stirring, homogenate, grinding, the arbitrary mode of ultrasonic, its temperature condition is a room temperature-60 ℃.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03114670 CN1448053A (en) | 2003-04-22 | 2003-04-22 | Thiophanate methyl inclusion complex pesticide preparation |
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| CN 03114670 CN1448053A (en) | 2003-04-22 | 2003-04-22 | Thiophanate methyl inclusion complex pesticide preparation |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104222121A (en) * | 2014-08-26 | 2014-12-24 | 中农立华生物科技股份有限公司 | Sterilization composition, preparation and application of preparation |
| WO2018151177A1 (en) * | 2017-02-15 | 2018-08-23 | 大鵬薬品工業株式会社 | Pharmaceutical composition |
-
2003
- 2003-04-22 CN CN 03114670 patent/CN1448053A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104222121A (en) * | 2014-08-26 | 2014-12-24 | 中农立华生物科技股份有限公司 | Sterilization composition, preparation and application of preparation |
| CN104222121B (en) * | 2014-08-26 | 2016-08-24 | 中农立华生物科技股份有限公司 | A kind of bactericidal composition and preparation and application thereof |
| WO2018151177A1 (en) * | 2017-02-15 | 2018-08-23 | 大鵬薬品工業株式会社 | Pharmaceutical composition |
| JPWO2018151177A1 (en) * | 2017-02-15 | 2019-11-07 | 大鵬薬品工業株式会社 | Pharmaceutical composition |
| AU2018222163B2 (en) * | 2017-02-15 | 2021-01-28 | Taiho Pharmaceutical Co., Ltd. | Pharmaceutical composition |
| AU2018222163C1 (en) * | 2017-02-15 | 2021-08-12 | Taiho Pharmaceutical Co., Ltd. | Pharmaceutical composition |
| US11110062B2 (en) | 2017-02-15 | 2021-09-07 | Taiho Pharmaceutical Co., Ltd. | Pharmaceutical composition |
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