CN1957701B - Insecticide of ivermectin - Google Patents

Insecticide of ivermectin Download PDF

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Publication number
CN1957701B
CN1957701B CN2006101048056A CN200610104805A CN1957701B CN 1957701 B CN1957701 B CN 1957701B CN 2006101048056 A CN2006101048056 A CN 2006101048056A CN 200610104805 A CN200610104805 A CN 200610104805A CN 1957701 B CN1957701 B CN 1957701B
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Prior art keywords
ivermectin
emulsifier
qualified
agent
deionized water
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CN1957701A (en
Inventor
郑敬敏
王同斌
刘健
毕标能
张崇斌
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Shaanxi Sunger Road Bio Science Co Ltd
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Shaanxi Sunger Road Bio Science Co Ltd
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Abstract

An agricultural insecticide for preventing and eliminating pests and mite of fruit tree and vegetables is prepared from ivermectin (0.5-50%), emulsifier, solvent, bag-forming monomer, wetting disperser, diluent, adhesive and deionized water.

Description

A kind of insecticide of ivermectin
Technical field
The present invention relates to a kind of crops pesticide, particularly a kind of agricultural insecticide that contains ivermectin.
Background technology
Ivermectin (english common name: ivermectin, chemical molecular formula C 48H 74O 14, C 47H 72O 14) be to be lead compound with the Avermectin, by two key hydrogenations, structure optimization and the novel synthetic pesticide succeeded in developing.Structure optimization product as agricultural antibiotic, compare with the parent Avermectin, its expelling parasite and acaricidal activity have not only been kept, and safety is higher, be difficult for to produce resistance, for the production of vegetables, fruit, cotton etc. provide efficient a, high security and with the good biological source insecticide of Environmental compatibility.
At present, ivermectin has only a kind of formulation of missible oil.Owing in the process of processing missible oil, need a large amount of organic solvents, as benzene,toluene,xylene etc.A large amount of uses of organic solvent not only cause the waste of industrial chemicals, simultaneously, return environment and human health and have brought very big threat.In recent years, proposed to forbid the part organic solvent in some developed countries.Therefore exploitation reduces or gets rid of the new dosage formulation of these organic solvents, has become a kind of imperative trend, and wherein water baseization of preparation is exactly one of important directions of formulations of pesticide development.
Summary of the invention
Purpose of the present invention is exactly in order to overcome the existing production and processing formulation of ivermectin, the environmental pollution that exists in the production use, is detrimental to health and shortcoming such as use cost height and develop new dosage formulation.Formulation involved in the present invention has: suspending agent, aqueous emulsion, microemulsion, water dispersible granules and microcapsule formulations.More than several formulations can both well solve numerous drawbacks related in the present production application of ivermectin.
Technical solution of the present invention is such: the active ingredient of insecticide of ivermectin is ivermectin, content range is 0.5~50% by weight percentage, is to add suspending agent, aqueous emulsion, microemulsion, micro emulsion wafer, the water dispersible granules that certain auxiliary agent is made by the former medicine of ivermectin.
Wherein, mainly contain according to the different auxiliary agents that each formulation was suitable for: emulsifier, solvent, encystation monomer, antifreezing agent, thickener, wetting dispersing agent, stabilizing agent, defoamer, disintegrant, thinner, binding agent and deionized water.Emulsifier can be the combination of any two or three among agricultural newborn 500#, 600#, 700#, 2201, Tween-60 #, the TX-10,1601; Solvent can be one or more the combination among toluene, DMF, carrene, the methyl alcohol etc.The encystation monomer can be a kind of of PPG, polyalcohol modified MDI series etc.Antifreezing agent can be one or more of ethylene glycol, propane diols, glycerine etc.; Thickener can be any a kind of in xanthans, polyvinyl alcohol, the bentonite; Wetting dispersing agent can be any composition of alkylphenol-polyethenoxy base ether formaldehyde condensation products phosphate (SOPA), alkylphenol-polyethenoxy base ether phosphate FLS, phenethyl phenol polyethenoxy base ether phosphate (2210), polyoxyethylene polyoxypropylene base ether block copolymers, alkylnaphthalene sulfonate (BX), alkylbenzenesulfonate, alkylsulfonate, Fluhyzon formaldehyde condensation products (NNO), sodium lignin sulfonate, polycarboxylate; Stabilizing agent can be a kind of of Sodium Benzoate, sodium sorbate; Defoamer is silicone based; Disintegrant can be a kind of of ammonium sulfate, white carbon; Thinner can be a kind of of kaolin, precipitated calcium carbonate, diatomite; Binding agent can be a kind of of carboxymethyl cellulose, polyvinyl alcohol.
Embodiment
Essence for a better understanding of the present invention describe technology contents of the present invention in detail with its theory of constitution and embodiment below, but content of the present invention is not limited to this.
In actual applications, according to different instructions for uses, the auxiliary agent that the former medicine of ivermectin and each formulation are suitable for can be processed into different dosage form proposed by the invention.
Be used for preparation method of the present invention and a series of specific embodiment be provided in order to make those of ordinary skill in the art understand the present invention better, to the invention provides:
Embodiment 1 0.5% ivermectin microcapsule formulations
Its each constituent content (by weight percentage) is an ivermectin 0.7%, emulsifier TX-10 4%, 22012%, solvent toluene 4%, DMF4%, the polyalcohol modified MDI 2.5% of encystation monomer, antifreeze glycol 4%, the yellow first glue 0.3% of thickener, wetting dispersing agent alkylphenol-polyethenoxy base ether phosphate 4%, stabilizing agent Sodium Benzoate 0.1% adds deionized water and supplies 100%.
With ivermectin with dissolution with solvents after, add encystation monomer and emulsifier evenly as oil phase, joining aqueous phase under high-speed shearing machine shears, make particle diameter to 1~3 micron of emulsion, then under suitable temperature and certain mixing speed, micro-capsule is solidified increase, the system for the treatment of stops the encystation reaction after being reacted to certain hour.Then wetting dispersing agent, thickener, stabilizing agent, antifreezing agent and deionized water are added, stir and promptly obtain 1.5% ivermectin microcapsule formulations.Through check ivermectin content 0.6%, suspensibility 98%, wet screening test (by 75 μ m testing sieves) 98%, low-temperature stability is qualified, and heat storage stability is qualified.
Embodiment 2 5% ivermectin microcapsule formulations
Its each constituent content (by weight percentage) is an ivermectin 5.3%, emulsifier 2,201 3%, Tween-60 3%, solvent DMF 4%, carrene 8%, encystation monomer PPG 5%, antifreezing agent propane diols 4%, the yellow first glue 0.3% of thickener, wetting dispersing agent phenethyl phenol polyethenoxy base ether phosphate 4%, stabilizing agent sodium sorbate 0.1% adds deionized water and supplies 100%.With ivermectin with dissolution with solvents after, add encystation monomer and emulsifier evenly as oil phase, joining aqueous phase under high-speed shearing machine shears, make particle diameter to 1~3 micron of emulsion, then under suitable temperature and certain mixing speed, micro-capsule is solidified increase, the system for the treatment of stops the encystation reaction after being reacted to certain hour.Then dispersant, thickener, stabilizing agent, antifreezing agent and deionized water are added, stir and promptly obtain 1.5% ivermectin micro-capsule suspension.Through check content 5.3%, suspensibility 97%, wet screening test (by 75 μ m testing sieves) 98%, low-temperature stability is qualified, and heat storage stability is qualified.
Embodiment 3 2.5% ivermectin aqueous emulsions
Its each constituent content (by weight percentage) is an ivermectin 2.8%, emulsifier 2,201 3%, 1,601 5%, and solvent DMF 4%, carrene 6%, antifreeze glycol 4% add deionized water and supply 100%.With ivermectin with dissolution with solvents after, add emulsifier evenly as oil phase, the mixture of antifreezing agent and water as water, is joined oil phase aqueous phase and shears certain hour under high-speed shearing machine, the particle diameter that makes emulsion promptly obtains 2.5% ivermectin aqueous emulsion less than 0.8 micron.Through check content 2.8%, pH6.8, stability of emulsion (diluting 200 times) is qualified, and low-temperature stability is qualified, and heat storage stability is qualified.
Embodiment 4 8% ivermectin aqueous emulsions
Its each constituent content (by weight percentage) is an ivermectin 8.3%, and emulsifier TX-10 6%, 2,201 4%, solvent toluene 6%, and carrene 10%, antifreeze glycol 4%, thickener polyvinyl alcohol 0.3% adds deionized water and supplies 100%.With ivermectin with dissolution with solvents after, add emulsifier evenly as oil phase, the mixture of antifreezing agent and water as water, is joined oil phase aqueous phase and shears certain hour under high-speed shearing machine, the particle diameter that makes emulsion promptly obtains 8% ivermectin aqueous emulsion less than 0.8 micron.Through check content 8.1%, pH6.6, stability of emulsion (diluting 200 times) is qualified, and low-temperature stability is qualified, and heat storage stability is qualified.
Embodiment 5 15% ivermectin suspending agents
Its each constituent content (by weight percentage) is the former medicine 15.3% of ivermectin, antifreezing agent glycerine 3%, the yellow first glue 0.3% of thickener, binding agent carboxymethyl cellulose 0.3%, wetting dispersing agent polyoxyethylene polyoxypropylene base ether block copolymers 3%, phenethyl phenol polyethenoxy base ether phosphate 2%, stabilizing agent sodium sorbate 0.3%, silicone defoaming agent 0.2% adds deionized water to 100%.Wetting dispersing agent, thickener, stabilizing agent, antifreezing agent, defoamer, deionized water are added, add the former medicine of ivermectin then while stirring, back sand milling 2~4 hours in sand mill stirs, make the particle diameter of former medicine reach 1~3 predetermined micron requirement, promptly obtain 15% ivermectin suspending agent.Through check content 15.2%, pH6.7, suspensibility 97%, wet screening test (by 75 μ m testing sieves) 98%, low-temperature stability is qualified, and heat storage stability is qualified.
Embodiment 6 50% ivermectin suspending agents
Its each constituent content (by weight percentage) is the former medicine 51% of ivermectin, antifreeze glycol 4%, the yellow first glue 0.3% of thickener, bentonite 0.3%, wetting dispersing agent alkylphenol-polyethenoxy base ether phosphate 6%, stabilizing agent Sodium Benzoate 0.3%, silicone defoaming agent 0.5% adds deionized water to 100%.Wetting dispersing agent, thickener, stabilizing agent, antifreezing agent, defoamer, deionized water are added, add the former medicine of ivermectin then while stirring, back sand milling 2~4 hours in sand mill stirs, make the particle diameter of former medicine reach 1~3 predetermined micron requirement, promptly obtain 50% ivermectin suspending agent.Through check content 50.8%, pH6.4, suspensibility 98%, wet screening test (by 75 μ m testing sieves) 99%, low-temperature stability is qualified, and heat storage stability is qualified.Qualified back packing gets final product.
Embodiment 7 20% ivermectin water dispersible granules (by weight percentage)
Take by weighing the former powder 20.5% of ivermectin, wetting dispersing agent alkylsulfonate 2%, sodium alkyl benzene sulfonate 2%, wetting dispersing agent polycarboxylate 4%, Fluhyzon formaldehyde condensation products 6%, the white carbon black 6% of disintegrant, thinner diatomite 15, precipitated calcium carbonate 39.5%.After it mixes, obtain female powder, female powder and 5% carboxymethyl cellulose binding agent are mixed through the airslide disintegrating mill pulverizing, granulation then, oven dry, sieving obtains about 98% 20% ivermectin water-dispersible granules.Active constituent content 20.2% after testing, moisture 1.8%, and wet screening test (by 75 μ m sieve) 98%, suspensibility 92%, lasting foaming characteristic (1min)≤10mL, wetability≤1min, heat storage stability is qualified.
Embodiment 8 30% ivermectin water dispersible granules
Take by weighing the former powder 30.5% of ivermectin, wetting dispersing agent alkylsulfonate 3%, wetting dispersing agent polycarboxylate 5%, sodium lignin sulfonate 5%, disintegrant ammonium sulfate 5%, thinner kaolin 10%, precipitated calcium carbonate 36.5%.After it mixes, obtain female powder, female powder and No. 3 binding agents of 5% modified polyvinyl alcohol are mixed through the airslide disintegrating mill pulverizing, granulation then, oven dry, sieving obtains about 96% 30% ivermectin water-dispersible granules.Active constituent content 30.4% after testing, moisture 1.9%, and wet screening screening (by 75 μ m sieve) 98%, suspensibility 90%, lasting foaming characteristic (1min)≤10mL, wetability≤1min,, heat storage stability is qualified.
Embodiment 9 2.5% ivermectin micro emulsions (by weight percentage)
Its each constituent content is an ivermectin 2.7%, emulsifier 2,201 8%, 600#5%, and TX-107%, solvent DMF 4%, toluene 6%, methyl alcohol 10% add deionized water and supply 100%.With ivermectin with dissolution with solvents after, add emulsifier evenly as oil phase, the aqueous phase of oil mixture being poured into deionized water stirs.Treat promptly to obtain 2.5% ivermectin micro emulsion after the system clarification.Through check content 2.6%, pH6.6, transparency temperature scope-3 ℃-47 ℃, stability of emulsion (diluting 200 times) is qualified, and low-temperature stability is qualified, and heat storage stability is qualified.
Embodiment 10 5% ivermectin micro emulsions (by weight percentage)
Its each constituent content is an ivermectin 5.3%, emulsifier farming newborn 500#8%, 700#5%, 1,601 8%, and solvent toluene 5%, carrene 10%, methyl alcohol 8% add deionized water and supply 100%.Ivermectin with toluene, cyclohexanone, dissolve with methanol, is added emulsifier evenly as oil phase, oil mixture is joined in the deionized water, stir, the system for the treatment of is recovered can obtain 5% ivermectin micro emulsion after the clarification.Through check content 5.3%, pH6.7, transparency temperature scope-3 ℃-45 ℃, stability of emulsion (diluting 200 times) is qualified, and low-temperature stability is qualified, and heat storage stability is qualified.
Its obvious advantage of dosage formulation involved in the present invention is:
(1) particle is thin, and particle is little, surface affinity is strong, opening up good penetrability, has improved drug effect;
(2) suspensibility height (more than the 90-95%);
(3) wetability, spread, tackness are good, resistance of rainwater washing against;
(4) biologically active is than the missible oil height, and it is long to compare the lasting period, and drug effect is higher than missible oil;
(5) reduced pollution in production, packing and the transportation, environmental pollution is few, and is safe;
(6) intermiscibility is preferably arranged, be convenient to mix with buckets such as other preparations, active component and auxiliary agents;
(7) replace organic solvent with water and done the pollution that solvent has reduced environment;
The insecticide of ivermectin that adopts prescription of the present invention to process, its implementation result shows, this product has intermiscibility preferably, working substance suspensibility height, and the height of adhesion rate in use, resistance of rainwater washing against lasting period are long, no dust, do not contain solvent, thereby produce, use relative with the storing condition better, environmental pollution is few, and is safe.The present invention has not only improved the availability of each active ingredient in production application, and has improved the biologically active of active ingredient.Through evidence, the insect pest of multiple fruit tree and vegetable, mite evil all there is the better prevention effect; And safety is good, and crops are not had poisoning.

Claims (2)

1. insecticide of ivermectin, its active ingredient is ivermectin, each composition weight percentage composition is as follows:
Ivermectin 8.3%
Emulsifier TX-10 6%
Emulsifier 2,201 4%
Solvent toluene 6%
Methylene chloride 10%
Antifreeze glycol 4%
Thickener polyvinyl alcohol 0.3%
Deionized water supplies 100%.
2. insecticide of ivermectin, its active ingredient is ivermectin, each composition weight percentage composition is as follows:
Ivermectin 2.8%
Emulsifier 2,201 3%
Emulsifier 1,601 5%
Solvent DMF 4%
Methylene chloride 6%
Antifreeze glycol 4%
Deionized water supplies 100%.
CN2006101048056A 2006-10-27 2006-10-27 Insecticide of ivermectin Expired - Fee Related CN1957701B (en)

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Application Number Priority Date Filing Date Title
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CN1957701B true CN1957701B (en) 2010-08-11

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Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9101131B2 (en) 2007-12-03 2015-08-11 Valent U.S.A., Corporation Seed treatment formulations
AU2008331802B2 (en) * 2007-12-03 2013-11-28 Sumitomo Chemical Company, Limited Seed treatment formulations and methods of use
CN102379297B (en) * 2011-09-13 2014-07-09 广西田园生化股份有限公司 Macrolide compound ultralow volume formulation
CN102440996B (en) * 2011-12-29 2013-04-24 郑国祥 Compound albendazole suspension containing ivermectin nanoemulsion and preparation method thereof
EP3362045B1 (en) * 2015-10-13 2019-10-09 Galderma S.A. A process for preparing a composition comprising a high concentration of one or more avermectins
CN109045058A (en) * 2018-09-28 2018-12-21 佛山市正典生物技术有限公司 A kind of albendazole ivermectin micro-capsule for animals and preparation method thereof
CN109874785A (en) * 2018-12-18 2019-06-14 北京化工大学 One-step shaping method is prepared using polyethers as the insecticide microcapsules and its continuous producing method of wall material
CN111195280A (en) * 2020-03-19 2020-05-26 潍坊富邦药业有限公司 Low-irritation ivermectin spray for pets and preparation method thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1775026A (en) * 2005-11-21 2006-05-24 河北威远生物化工股份有限公司 Disinsection emulsion in water containing avermectin
CN1788563A (en) * 2005-11-21 2006-06-21 河北威远生物化工股份有限公司 Insecticide microemulsion containing methylamino avermectin

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1775026A (en) * 2005-11-21 2006-05-24 河北威远生物化工股份有限公司 Disinsection emulsion in water containing avermectin
CN1788563A (en) * 2005-11-21 2006-06-21 河北威远生物化工股份有限公司 Insecticide microemulsion containing methylamino avermectin

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