CN102651967A - Insecticide composition and method of controlling insects using the same - Google Patents

Insecticide composition and method of controlling insects using the same Download PDF

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Publication number
CN102651967A
CN102651967A CN2011800048560A CN201180004856A CN102651967A CN 102651967 A CN102651967 A CN 102651967A CN 2011800048560 A CN2011800048560 A CN 2011800048560A CN 201180004856 A CN201180004856 A CN 201180004856A CN 102651967 A CN102651967 A CN 102651967A
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ether
preparation
animal
glycol
formula
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CN102651967B (en
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詹姆斯·蒂莫西·布里斯托
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Rotam Agrochem International Co Ltd
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Rotam Agrochem International Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A61K9/0017—Non-human animal skin, e.g. pour-on, spot-on
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/02—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system

Abstract

A pour-on formulation for control of an external parasite on an animal is provided, the formulation comprises an effective amount of an ectoparasiticidally active ingredient and at least one C2-C4 dialkylene glycol mono/di - C1-C4 alkyl ether as a carrier. The ectoparasiticidally active ingredient is preferably an insect growth regulator (IGR). There is further provided the use of a C2-C4 dialkylene glycol mono/di - C1-C4 alkyl ether for improving the properties of a pour-on formulation, in particular the properties of stability, efficacy and water-resistance.

Description

Insecticides and with its control insect method
Technical field
The present invention relates to be used to prevent and treat the composition of insect; Relate in particular to and kill the epizoa activating agent (like insect growth regulator, IGR (Insect Growth Regulator; And the formula that pours (pour-on) composition of insecticide, and relate to the method for using said compositions-treated or control insect and parasite (especially preventing and treating insect or parasite on the animal) IGR)).Particularly, the present invention relates to the pour formula composition of water-fast IGR in a kind of or more kinds of nonaqueous solvents.
Background technology
For animal doctor and poultry raiser, infecting of parasite on the domestic animal (like flea) still represented as yet not by the satisfied problem that solves.
In the past, handle animal through multiple different measures, with control insect and interior and epizoa.Also knownly will be used to handle the composition that is infected animal and be mixed with and be applied to zoodermic powder.Use this dusting and can not accepted by animal passivity ground usually, because need a few minutes to handle whole skin surface equably, and dust can arrive mouthful inevitably, nose and eye, causes animal discomfort or pain.Even in the process of using carefully, can not get rid of the possibility that animal and poultry raiser suck powder.Usually, the people who handles animal also can touch said composition in large quantities, and this is being actually inevitably, and this contact can only be got rid of or eliminates through time-consuming and difficult measure.
Also knownly will be used to handle the reagent that is infected animal and be mixed with fluid composition.Can in many ways these fluid compositions be used for animal.For example,, whole animal contains in the said fluid composition bath of (comprising effective parasiticidal medicament), perhaps through whole body surface with said composition spray animal through being immersed in.In some cases, can not successfully use suitable fluid composition (like the active shampoo of flea), because many animals (especially cat and many dogs) do not let its poultry raiser have a bath to them or can only force to carry out.In addition, the effect that this bathing is handled only continues limited a period of time (a for example maximum about week), and the process of this whole trouble of having to repeat with the frequent time interval.When using dipping or rinsing, identical or similar problem appears.
For many people, use spray to have offending accident, because hearing the sound of spray, most of animal (especially cat) will make fight or aggressive reactions.In addition, spray also has all shortcomings of being mentioned in the solid composite (especially powder).In addition, the fluid composition of using as spray more fine disperses in atmosphere than powder usually, and is therefore more easily sucked by people who uses them and handled animal.
Also usually use the necklace or the band (for example so-called flea necklace) that soak into suitable parasitocidal activity agent to prevent and treat multiple parasite (for example flea).This has guaranteed the good validity of short-term.Certain weakness of this processing method is that especially local application is very restricted.Usually, necklace or band neck and chest to kill activity very high, even possibly reach 100%.Yet farther body part more is difficult to handle, and almost can not be affected in some cases.In addition, the active free restriction of these necklaces.In addition, many attractions that do not have are arranged in these necklaces, and when wearing, can disturb animal.
As other alternative, also can obtain the disk that hangs on the conventional necklace and comprise active component.These have attractive outward appearance usually, but usually it is active and unsatisfactory, because contacting between disk and the animal skin is inadequate.
Recently, found and can use multiple antiparasitic active principle through local application (so-called " pouring formula " uses).Although the antiparasitic active principle provides through local application, activating agent can move the whole outer surface to watch for animals." local application " means the sub-fraction that active component only is applied to the animal outer surface, is generally line or point on animal back.
The local surfaces (topical) of the location through pouring the formula preparation is used the epizoon of preventing and treating on sheep, cat, dog, ox and other animal (comprising goat, pig and horse) has become conventional way for a long time.Pour the formula preparation and all existing water-insoluble IGR pour in the formula preparation at the great majority that the inventor knew, activating agent is dissolved in the non-aqueous solvent systems to produce the suitable formula that pours preparation.Preparation is present in these and pours solvent in the formula preparation to be implemented in fine dispersion and/or the infiltration of epidermis around the animal skin.So far, the commercially available formula that pours preparation is suspension, missible oil (emulsificable concentrate) or solution, and usually comprises at least a organic solvent.Usually these pour the solvent that is used as carrier in the formula preparation comprise propane diols, paraffin, isoparaffin, aromatic compound (aromatic), isopropyl myristate (isopropyl myristate, IPM), glycol ether and alcohol (like normal propyl alcohol).US 4,672, and 072 discloses the preferred solvent systems that comprises 30% to 70% xylol, 20% to 40% cyclohexanone and 5% to 25% vegetable oil.
Regrettably, when with the commercially available solvent system that is used as carrier/supporting agent in the formula preparation that pours when being applied to animal skin, it can cause the tissue reaction of some forms; This so cause animal uncomfortable; And in many cases, cause the infringement of animal skin, sheepskin or wool, thereby produce economic loss.Especially, some animal has highstrung skin, and itself and some commercially available solvent systems that pour in the formula preparation react.For example, aromatic compound (for example xylol and paraffin) produces tissue reaction dry, rubescent like skin and that chap.
European patent No.0137627B1 discloses a kind of formula preparation that pours; Wherein active component is interior insecticide; And that carrier comprises is single-or gather-at least a polyunsaturated fatty acid ester of the monoalky lether of aklylene glycol, like acetate 1-ethoxy-c-2-base ester and butyric acid 2-(n-butoxy) ethyl ester.In sheep of handling or ox, do not have disadvantageous skin reaction though this specification is claimed this preparation, should be noted that in some animals, (especially to have in the sensitive-skinned sheep) still to can be observed disadvantageous epidermis reaction.
In addition, when using the conventional formula that pours preparation, 95% to 98% the active component of being used is stayed site of administration and is combined with fur or the hair of animal.This so cause lack rendeing a service.Therefore, must use more substantial active component, infect to prevent and treat effectively to animal.
In addition, when multiple known formulations is contacted with water, find that active component can be precipitated out from solvent formulation.Therefore, if be applied to wet animal, if perhaps after using, soon and before handling drying animal is exposed in the water (like heavy rain), it is so ineffective that then solvent IGR pours the formula preparation.When making the multiple formula preparation that pours when contacting with water, active component is precipitated out from said preparation rapidly.If said preparation is applied to wet animal, if before the processing drying perhaps on animal this animal is exposed in the rain, then active component is precipitated out from solution, and deposits along the back of this animal, and solvent is also washed away by rain.This obstruction or stoped the distribution of active component around whole animal.This phenomenon is even more important for those zones of animal downside.This phenomenon has reduced in following validity based on the preparation of solvent of these conditions.
Therefore, the current safety barrier that needs searching to be used to pour the formula preparation, it is not only to the animal nonirritant, and the permission end-product becomes effective, stable, water-fast preparation to the mammal low toxicity.Preferably, said carrier has gratifying freezing point, suitable denseness and cost-effective advantage.In addition, preferably, said carrier can easily be prepared with active component, for example, can easily dissolve any activating agent, is easy to use and provide superior processing safety.
In the present invention, have been found that through in pouring the formula preparation, using above-mentioned some or all shortcoming that can reduce or overcome the formula that the pours preparation of prior art as C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether of solvent or carrier.End-product based on new support is effective, stable, water-fast preparation to the mammal low toxicity, and it is to the animal nonirritant.
Summary of the invention
The present invention relates to a kind of or more kinds of C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether purposes as solvent or carrier in the formula that the pours preparation of parasitocidal activity agent.Said preparation can effectively reduce the excitant to animal.In addition, use aforementioned ether as also providing of solvent or carrier effective, stable, water-fast and to the preparation of mammal low toxicity.
In aspect first; The invention provides the nonirritant that is suitable for being locally applied to animal and pour the formula preparation, said preparation comprise effective dose kill epizoa active component (being preferably insect growth regulator, IGR (IGR)) and as at least a C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether of carrier.
Have been found that said C2-C4 two aklylene glycols two-/list-C1-C4 alkyl ether chemically and physically stable, nonflammable, to the mammal low toxicity and to the animal nonirritant.Have been found that in the multiple parasite infestation of the formula that pours preparation on handling animal (for example tick, flea etc.) that comprises a kind of or more kinds of aforementioned ether and kill epizoa active component (especially IGR) be effective.
Preparation of the present invention comprises C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether.Can use the combination of any appropriate C 2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether or two kinds or more kinds of this ethers.More preferably, said C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether is selected from: diethylene glycol dimethyl ether, diethylene glycol dimethyl ether, DPG dimethyl ether, dipropylene glycol methyl ether, dibutylene glycol dimethyl ether, dibutylene glycol methyl ether, diethylene glycol diethyl ether, diethylene glycol ether, DPG diethyl ether, DPG ether, dibutylene glycol diethyl ether, dibutylene glycol ether, diethylene glycol dipropyl ether, diethylene glycol propyl ether, DPG dipropyl ether, DPG propyl ether, dibutylene glycol dipropyl ether, dibutylene glycol propyl ether, dibutyl ethylene glycol ether, diethylene glycol butyl ether, DPG butyl oxide, DPG butyl ether, dibutylene glycol butyl oxide, dibutylene glycol butyl ether and composition thereof.
In said preparation, said C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether can exist with a kind of or more kinds of other solvent, thereby forms the carrier of said active component.More preferably, said preparation comprise by a kind of or more kinds of C2-C4 two aklylene glycols two-/carrier that list-C1-C4 alkyl ether is formed.
Preparation of the present invention comprises epizoa active component extremely, and it effectively prevents and treats the epizoa of infecting target animal.The suitable epizoa activating agent that kills comprises insecticide and miticide.In one embodiment; The said epizoa activating agent that kills is preferably influence, control or regulates the activating agent that parasite grows; For example be that chitin synthetic inhibitor or hormone are intended like thing, such reagent is commonly called and is called insect growth regulator, IGR (IGR) in this article.Said preparation can comprise the single mixture that kills epizoa activating agent or two kinds or more kinds of this medicaments, the mixture of for example single IGR or two kinds or more kinds of IGR.In preparation of the present invention, can use any water-fast epizoa activating agent that kills.
Be known in the art and can be purchased suitable epizoa activating agent extremely.For example, the known in the art suitable IGR that is contained in the preparation of the present invention comprises diflubenzuron (diflubenzuron), kills bell urea (triflumuron), fluazuron (fluazuron), Acarus tritici urea (lufenuron), fluorine uride (novaluron), fluorine bell urea (hexaflumuron), fluorobenzene urea (teflubenuron), fluorine pyridine urea (chlorfluazuron), flufenoxuron (flufenoxuron), noviflumuron (noviflumuron) and methoprene (methoprene).These IGR are available commercially.
As as known in the art, preparation of the present invention can comprise routine and be included in a kind of or more kinds of other component that pours in the formula preparation.The instance of other suitable composition is stabilizing agent (for example antioxidant), spreading agent, preservative, adhesion promotor, active solubilizer (for example oleic acid), viscosity modifier, ultraviolet isolating agent or absorbent and colouring agent.Also can comprise surfactant said pouring in the formula preparation, said surfactant comprises anion surfactant, cationic surfactant, non-ionic surface active agent and amphoteric surfactant.
As stated, preparation of the present invention can be used for preventing and treating infecting in the animal.Therefore, aspect second in, the invention provides insect or the parasitic method of control on the animal, this method comprises that appearance uses the formula that the pours preparation of first aspect according to the present invention of epizoa effective dose (like volume) extremely.
Can said preparation be applied to some of animal appearance or all.Said method preferably includes the regional area administration such formulations to the animal outer surface.In aspect this, term " regional area " is meant the outer table section of said animal, and it is the sub-fraction in the total surface zone of said animal.Particularly, said regional area is 0.1% to 10% animal surf zone, more specifically 0.5% to 5% animal outer surface.A special advantage of preparation of the present invention is only to apply it to very little zone, animal surface, and the effective processing that still provides antagonism to infect.
Can be to the single regional area administration such formulations of animal.Perhaps, can be through handling animal to a plurality of different regional area administration such formulations, said zone is spaced apart fully.
Said method can comprise any appropriate area administration such formulations to animal.Preferred zone is the neck and the back of the body of animal.
Another aspect of the present invention relates to C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether and pours in the formula preparation as the purposes of carrier in the ectozoic nonirritant that is used for preventing and treating animal, and what wherein said preparation also comprised effective dose kills the epizoa agent.
Detailed Description Of The Invention
As stated; Find unexpectedly in the present invention; C2-C4 two aklylene glycols two-/list-C1-C4 alkyl ether is not only and can be used for preparing the improved avirulence nonirritant carrier that epizoa pours the formula preparation that kills; But also can improve the said formula preparation that pours, make it more effective, stable and water-fast.
For example, find that IGR preparation prepared in accordance with the present invention has killed most of ticks (＞96%) in 4 to 5 hours of the regional area that is applied to animal.
In addition, find that preparation of the present invention can tolerate by volume the water up to 10% before water-fast IGR begins from carrier solvent, to be precipitated out lentamente.This and compatibility water means that if said preparation is added into wet animal, then active component will continue on animal skin, to sprawl, and can not break away from animal.The water tolerance of this increase helps to increase the effectiveness of preparation.Similarly, if after using preparation of the present invention, rain soon, then said rainfall will help said preparation on animal skin, to sprawl and can it not washed out.This will help to increase the effectiveness of preparation once more.
In addition, when being applied to animal and not raining for weeks on end, said preparation also is effective.Under all these situation, believe that said carrier has promoted active component to sprawl in that animal is lip-deep.When using conventional or known preparation based on solvent, can not obtain these useful effects.
In addition, the present invention also provides and can be used for preparing the improved avirulence nonirritant carrier that pours the formula preparation.The present invention also provides these improved useful especially preparations, because the animal that can they be locally applied to agronomical value is with the control epizoa, and can in animal, not cause disadvantageous epidermis reaction.
As stated, the present invention also provides a kind of and is applied to animal and prevents and treats the ectozoic method in the animal of agronomical value through the said nonirritant formula of pouring being killed the epizoa preparation.
Said preparation can comprise a kind of or more kinds of epizoa active component that kills, and comprises miticide and insecticide.These active components are as known in the art and comprise usually through pouring those active components that the formula preparation is used.Said active component is preferably insect growth regulator, IGR (IGR).Said active component can be present in the said preparation with any suitable amount.Particularly, the amount of said active component can for composition by weight 0.05% to 60%, more preferably, for by weight 0.1% to 50%, also more preferably be by weight 0.1% to 40%.
The said epizoa active component that kills can be any water-fast medicament.Particularly, any water-fast IGR can use in preparation.Suitable IGR is as known in the art, and comprise diflubenzuron, kill the bell urea, fluazuron, Acarus tritici urea, fluorine uride, fluorine bell urea, fluorobenzene urea, fluorine pyridine urea, flufenoxuron, noviflumuron and methoprene.These IGR can be commercially available.
Pour in the formula preparation of the present invention, said activating agent can be single epizoa compound extremely or two kinds or more kinds of epizoa combination of compounds of killing.
Preparation of the present invention comprises the carrier that contains C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether.Said composition can comprise single C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether or two kinds or more kinds of C2-C4 two aklylene glycols two-/combination of list-C1-C4 alkyl ether.
More specifically; The carrier of said preparation comprises ether; Said ether be selected from C2-C4 two aklylene glycols two-/list-C1-C4 alkyl ether, said C2-C4 two aklylene glycols two-/list-C1-C4 alkyl ether comprises diethylene glycol dimethyl ether, diethylene glycol dimethyl ether, DPG dimethyl ether, dipropylene glycol methyl ether, dibutylene glycol dimethyl ether, dibutylene glycol methyl ether, diethylene glycol diethyl ether, diethylene glycol ether, DPG diethyl ether, DPG ether, dibutylene glycol diethyl ether, dibutylene glycol ether, diethylene glycol dipropyl ether, diethylene glycol propyl ether, DPG dipropyl ether, DPG propyl ether, dibutylene glycol dipropyl ether, dibutylene glycol propyl ether, dibutyl ethylene glycol ether, diethylene glycol butyl ether, DPG butyl oxide, DPG butyl ether, dibutylene glycol butyl oxide, dibutylene glycol butyl ether and composition thereof.
Said preparation can comprise a kind of or more kinds of C2-C4 two aklylene glycols two-/list-C1-C4 alkyl ether; Its amount is 40% to 99.95% of said composition by weight; More preferably by weight 50% to 99.9%, also more preferably by weight 60% to 99%.
In the embodiment of the present invention aspect first, it is to comprise by weight 0.1% to 40% at least a activating agent that is selected from insect growth regulator, IGR and the preparation of C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether of 40% to 99.9% by weight that animal ectozoic that is used for preventing and treating agronomical value pours the formula preparation.
Can the formula preparation that pour of the present invention be provided with any suitable form.Particularly, said preparation can be following form: liquid, powder, emulsion, foam, paste, aerosol, ointment, ointment (salve) or gel.Usually, the said formula preparation that pours is a liquid.The carrier of preparation of the present invention is nonaqueous.Said activating agent can be combined with carrier in any suitable manner.For example, said active component can suspend in said carrier, dissolves or disperse.As stated, the carrier in the preparation of the present invention has promoted infiltration and activating agent the sprawling on animal skin of activating agent through animal skin.
Except that said carrier and said activating agent, the formula preparation that pours of the present invention also can comprise a kind of or more kinds of other composition.The instance of other suitable composition is stabilizing agent (like antioxidant), dispersant, preservative, adhesion promotor, active solubilizer (like oleic acid), viscosity modifier, ultraviolet isolating agent or absorbent and colouring agent.In these preparations, also can comprise surfactant, it comprises anion surfactant, cationic surfactant, non-ionic surface active agent and amphoteric surfactant.
Preparation of the present invention comprises antioxidant usually.Suitable antioxidant is as known in the art, and can be commercially available.A kind of suitable antioxidant is BHT (butylated hydroxytoluene).The amount of said antioxidant is generally 0.05% to 10% of composition by weight, more preferably be by weight 0.1% to 5%.
The suitable spreading agent that is comprised in the said preparation is as known in the art, and can be commercially available.The suitable spreading agent that is used for pouring the formula preparation comprises isopropyl myristate (IPM), isopropyl palmitate (IPP), C 12-C 18Caprylate/the decylate of saturated fatty alcohol, oleic acid, oleyl ester oil acid methyl esters (oleyl ester methyl oleate), triglycerides, silicone oil.Said dispersant amount by weight can be 0.05% to 10% of said composition, more preferably by weight 0.1% to 5%.
Can prepare the formula preparation that pours of the present invention according to known technology.For example, when said preparation is the solution of active component in said carrier, sharp said activating agent is mixed with said carrier, utilize when needed and heat and stirring.Can in the mixture of activating agent and carrier, add auxiliary element or other composition, perhaps, can before adding carrier, it be mixed with activating agent.If the said formula preparation that pours is emulsion or suspension, then use known technology to come to prepare similarly these preparations.
The universal method that is used to prepare said preparation comprises these steps: the activating agent (technical active agent) that 1) weighs up desired amount; 2) add suitable antioxidant (if existence); 3) add solubilizer (if existence), and dissolve through stirring; 4) reach desired volume through adding carrier; 5) mix through stirring with heating (, for example being heated to 50 ℃) leniently if be necessary; 6) divide in the impermeability container of packing into and lucifuge.
The present invention also provides the ectozoic method of control in the animal of agronomical value is arranged, and said method comprises that the present invention who kills the epizoa effective volume to said animal surface applied pours the formula preparation, especially uses to the regional area of said animal outer surface.
Utilize active to the target parasite and active component that select, preparation of the present invention can be used for control or handles diversified epizoa.The target epizoa comprises lice, tick, mite, dipteron winged insect (biting flies), food meat winged insect and flea.Said preparation can be used for diversified animal, and the animal of agronomical value is especially arranged.There is the animal of agronomical value to comprise ox, sheep, goat, pig, horse, cat, dog.
The formula preparation that pours of the present invention can be used in any suitable manner.Suitable application technique is as known in the art.For example, usually come administration such formulations through on the chi chung line (back of the body) of animal or shoulder, perhaps toppling over by point by one or several line.More preferably, topple over and come administration such formulations through said preparation is followed spine along the back of the body of said animal.Said preparation also can be used to animal through other conventional method; Be included in the material that brush soaked at least one pocket of animal, perhaps use commercially available giver it to be used (as by syringe, through spraying or through the use hurdle (spay race) of spraying).
The effective dose that is used for the formula that the pours preparation of surface applied will depend on Several Factors, activating agent in for example handled animal, the preparation and employed concrete preparation.In general, the amount of institute's administered formulation provides about 0.1mg to 2000mg activating agent/kg the weight of animals.
As stated, find, can improve C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether and pour the application of formula preparation (especially comprise and be used for handling or preventing and treating upward ectozoic formulations of active ingredients of animal) as carrier.Particularly, find to use C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether to improve the characteristic of effectiveness, stability and the water proofing property of preparation as carrier.In addition, find C2-C4 two aklylene glycols two-/list-C1-C4 alkyl ether causes the excitant reduction to animal.
Therefore, in another aspect, the invention provides C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether and in pouring the formula preparation, be used for reducing the irritating purposes of animal as carrier.
In aspect another, the invention provides C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether is used to improve effectiveness, stability and the resistance to water of said preparation as carrier in pouring the formula preparation purposes.
The present invention also provides effectiveness, stability and/or resistance to water that a kind of raising pours the formula preparation and/or the said preparation that reduces surface applied to the irritating method of animal, and said method comprises C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether is included in the said preparation as carrier.
In aspect another, the invention provides a kind of ectozoic method of preventing and treating on the animal, said method comprises the preparation that surface applied is as noted before.
The present invention also provides the purposes in the preparation as noted before epizoa on the control animal.
The following example further illustrates the preparation of the present composition and the details of purposes.The present invention who in aforementioned disclosure, proposes does not receive the restriction of these embodiment on spirit or scope.Those skilled in the art will easily understand, and the known variant mode of following preparation method's condition and process can be used for preparing these compositions.
Embodiment
The conventional method that is used to prepare said preparation relates to following these steps:
1) weighs the activating agent of desired amount;
2) add suitable antioxidant (if existence);
3) add solubilizer (if existence), and dissolve through stirring;
4) through adding carrier to reach the volume of expectation;
5) mix through stirring with heating (if necessary, for example being heated to 50 ℃) leniently;
6) divide in the impermeability container of packing into and lucifuge.
The dashing agent that has prepared embodiment 1 to 12 according to above-mentioned conventional method.
Embodiment 1
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900101
Embodiment 2
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900102
Embodiment 3
Prepared the formula that pours preparation with following composition:
Embodiment 4
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900111
Embodiment 5
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900112
Embodiment 6
Prepared the formula that pours preparation with following composition:
Embodiment 7
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900114
Figure BDA00001737764900121
Embodiment 8
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900122
Embodiment 9
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900123
Embodiment 10
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900124
Embodiment 11
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900132
Embodiment 12
Prepared the formula that pours preparation with following composition:
Figure BDA00001737764900133
Result of the test
Test, compare with the commercially available formula preparation that pours, relative efficiency and any unfavorable effect of formula preparation aspect control epizoa (like tick in the ox and flea) that pour more of the present invention to estimate.
Compare with the commercially available formula preparation that pours with untreated contrast, use the combination thing to test:
Composition (1): according to the preparation of embodiment 1 preparation;
Composition (2): according to the preparation of embodiment 5 preparations;
Composition (3): based on the pour formula commercial product (Stampede coopers, Farm Service NSW) of N-N-methyl-2-2-pyrrolidone N-as 2% diflubenzuron of carrier.
Composition (1) to (3) is tested as follows:
Tested object is the adult ox on Isaiah Pole Ntauiti farm.This farm is at the Ilmugush of the Mashuru portion in the card many areas of merchant (Kajiado district), (Nairobo) 76km apart from Nairobi.This specific region 3000 feet locate and annual rainfall less than 500mm.For domestic animal shepherd (mainly be Marseille (Masai) people, it is the neatherd), this zone is extremely important.There is important wildlife population in this zone, comprises gnu, zebra and antelope, and itself and Niu Yiqi herd, because farm hedge of no use surrounds, and the wildlife refuge is adjoined in this zone.Therefore, in this zone the challenge of tick high, and be to be used to test acaricidal appropriate area.
By the group test animal, be summarized in the table 1.
Table 1
Group Size of animal Handle
Y 5 Composition (1)
B 5 Composition (2)
G 5 Be untreated
R 5 Composition (3)
Experimental group and processing
The ox that will grow up is divided into four groups at random, and every group has based on five animals from the herd of average weight 350kg, selecting, with its mark and processing and allow it normally freely to herd.
With handle each selected group like preparation specified in the table 1 (composition 1, composition 2 and composition 3).
Use suitable applicator, spinally evenly applies from the end (initiating terminal of duster) of base portion to the tail at angle and makes every animals received 40ml (or recommending by manufacturer) pour the formula preparation.
Continuously, all animals are repeated single treatment weekly.All processing are separated by and were carried out in 7 days, and wherein handling first day is the 0th day, and processing subsequently was at the 7th, 14,21 and 28 day.When each the processing, respectively pour every animal of formula treated with 40ml.
Suitably retrain ox to allow absolute tick counting and to pour using of formula preparation.The the 1st, 3,5, the 7 day tick counting to all animals weekly carries out record.
The effectiveness of every kind of preparation is calculated in use according to the correction formula of Abbot (Abbott):
Figure BDA00001737764900151
Through will be after the processing of handling on the ox tick counting compare with the counting of the group of the ox of being untreated and estimate the effectiveness of the present composition.
In table 2, shown and merged tick counting total and the total of the merging during 28 days weekly.
Figure BDA00001737764900161
Table 2
Result and observation
1. composition 1 and initially sprawling of composition 2 are similar.Two kinds of compositions are all well sprawled on the skin of said animal.Yet composition 3 is sprawled slower.All three kinds of compositions are all sprawled in being applied to 4 to 5 hours of animal, especially reduce to the center line of animal along the spine line.Tick on center line, tsetse fly and flea are killed off.
2. composition 3 causes that in site of administration hair excessively takes off gloss, and excitant increases when causing being exposed to sunlight, makes ox seek the cool place and sentences and avoid pain.Composition 1 and composition 2 cause that seldom hair takes off gloss to not causing that hair takes off gloss and to the animal skin nonirritant.
3. the rainfall in the 15th day from testing.Rainfall does not influence the effectiveness of composition 1 and composition 2.On the contrary, composition 3 is not water-fast, and rainfall causes tick and the increase of flea population before the subsequent treatment.
4. at duration of test, composition 1 has been prevented and treated tick effectively with composition 2.
5. composition 1 has been beaten back tsetse fly (Tsetse) with composition 2, and the effect of knocking down fly is arranged.
6. based on these observed results, along animal center line fine dispersion, do not cause skin irritatin, especially reach 7 days and kill tick and beat back fly according to composition of the present invention (composition 1 and 2).Product of the present invention can use once in per two weeks.Exist (especially during the raining and after raining) of water do not reduced the validity of the present composition.

Claims (12)

1. one kind is used to prevent and treat animal and goes up the ectozoic formula preparation that pours, its comprise effective dose kill the epizoa active component and as at least a C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether of carrier.
2. preparation according to claim 1, the wherein said epizoa active component that kills comprises insect growth regulator, IGR (IGR).
3. preparation according to claim 2, wherein said insect growth regulator, IGR (IGR) comprise be selected from following compound with and composition thereof: diflubenzuron, kill bell urea, fluazuron, Acarus tritici urea, fluorine uride, fluorine bell urea, fluorobenzene urea, fluorine pyridine urea, flufenoxuron, noviflumuron and methoprene.
4. according to each described preparation in the aforementioned claim, it comprises by weight 0.1% to 40% said epizoa active component and 40% to 99.9% at least a C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether by weight of killing.
5. according to each described preparation in the aforementioned claim, wherein there are two kinds or more kinds of epizoa active component that kills.
6. according to each described preparation in the aforementioned claim, wherein there are two kinds or more kinds of C2-C4 two aklylene glycols two/list-C1-C4 alkyl ether.
7. according to each described preparation in the aforementioned claim, wherein said C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether is diethylene glycol dimethyl ether, diethylene glycol dimethyl ether, DPG dimethyl ether, dipropylene glycol methyl ether, dibutylene glycol dimethyl ether, dibutylene glycol methyl ether, diethylene glycol diethyl ether, diethylene glycol ether, DPG diethyl ether, DPG ether, dibutylene glycol diethyl ether, dibutylene glycol ether, diethylene glycol dipropyl ether, diethylene glycol propyl ether, DPG dipropyl ether, DPG propyl ether, dibutylene glycol dipropyl ether, dibutylene glycol propyl ether, dibutyl ethylene glycol ether, diethylene glycol butyl ether, DPG butyl oxide, DPG butyl ether, dibutylene glycol butyl oxide, dibutylene glycol butyl ether or its mixture.
8.C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether is used for reducing the irritating purposes of animal as carrier in pouring the formula preparation.
9.C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether is used to improve the purposes of effectiveness, stability and the resistance to water of said preparation as carrier in pouring the formula preparation.
10. effectiveness, stability and/or a resistance to water that is used to improve pour the formula preparation and/or reduce the irritating method of the said preparation of surface applied to animal, said method comprise C2-C4 two alkylene glycol monos/two-C1-C4 alkyl ether are included in the said preparation as carrier.
11. a control animal goes up ectozoic method, said method comprises that surface applied is according to each preparation in the claim 1 to 7.
12. according to each preparation purposes in the epizoa on the control animal in the claim 1 to 7.
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