WO2010048891A1

WO2010048891A1 - Method of preventing and killing ectoparasites of endotherm by combined application of amitraz and bifenthrin

Info

Publication number: WO2010048891A1
Application number: PCT/CN2009/074683
Authority: WO
Inventors: 布里斯托·詹姆斯·T
Original assignee: 龙灯农业化工国际有限公司
Priority date: 2008-10-30
Filing date: 2009-10-29
Publication date: 2010-05-06
Also published as: UA101073C2; AP2969A; CN101380017A; AP2011005723A0; ZA201103843B; CN101380017B

Abstract

The present invention provides a method of preventing and killing parasites (specially ticks and tsetse fly) by combined application of amitraz and bifenthrin. The method provides a medicinal composition comprising amitraz and bifenthrin, and applying the medicinal composition for preventing and killing parasites in animals easily injured by parasites.

Description

Method for controlling ectoparasites of warm-temperature animals by using a combination of amitraz and bifenthrin

[01] The present invention relates to a method for controlling parasites (especially mites and tsetse flies) by the combination of Amitraz and bifenthrin.

Background technique

[02] Acarids are important blood-sucking arthropod parasites, both of which belong to the Acarina parasite (parasitic parasite). Tsetse flies are one of the genus of the genus Diptera in the Diptera parasite (double-winged parasite). The veterinary community faces the problem of resistance to sputum, organophosphorous, op and synthetic pyrethroid (sp) insecticides. Now we have found that the blue tick is resistant to the scorpion, and in some parts of the world it is impossible to kill the cockroach. In the case of brown cockroaches, we found that cockroaches could not be killed by sp on the market. For op, we found that both of these cockroaches are gaining resistance to them. Therefore, farmers are now using a one-week spin-spray method using sp-types and three-week double-twisting to remove these two main types of plutonium.

[03] However, in the veterinary world, we have not seen major companies giving new molecules for the control of animal mites and tsetse flies, and we are seeing this resistance problem becoming more and more serious worldwide.

[04] Chemical pesticides are non-renewable resources that are permanently ineffective due to the development of resistance, a phenomenon that cannot be changed. The proposed strategy is to use ew and improved intervention methods (COMMUNICABLE DISEASES CLUSTER WHO, 2003). In this treatment, the moss is exposed to more than one active agent. A necessary condition for effective drug combination is that there is no cross-resistance between the active agents. However, it is very difficult to obtain a killing composition with the following conditions: Does not show cross-resistance with existing insecticides and acaricides Sex, no toxicity problems and little negative impact on the environment. Therefore, methods for delaying or preventing the production of resistant strains of pest species have been sought. In order to apply the effective agent as long as possible, it is necessary to apply an agent having a different action mechanism in rotation to carry out a good pest control specification. However, this method does not necessarily satisfactorily control pests. Therefore, after the emergence of resistance problems, measures to cope with resistance by combining insecticides and acaricides were studied. However, significant synergies have not been found to date.

Accordingly, it is an object of the present invention to provide a novel method of controlling mites and tsetse flies. Another object of the present invention is to provide acaricidal compositions for controlling mites and tsetse flies (especially blue and brown mites) which are resistant to bismuth, op and sp compounds. The mites show a strong control effect. These and other objects of the present invention are fully or partially achieved by the method of the present invention.

Summary of the invention

The present invention relates to a method for controlling parasites (especially mites and tsetse flies) by the use of biguanide and bifenthrin.

The present invention provides a method of controlling parasites (especially mites and tsetse flies) of animals, the method comprising

(a) providing a composition comprising a synergistically effective amount of biguanide and bifenthrin, and

(b) applying the composition to an animal susceptible to parasite damage.

(b) applying the composition to an animal susceptible to parasite damage,

(c) applying the composition to the animal by swarm spraying.

The present invention provides compositions comprising biguanides and bifenthrins which are useful for controlling parasites, particularly mites and tsetse flies. In some embodiments, the inventive group The biguanide and bifenthrin are synergistically effective amounts. In still other embodiments, the amount of biguanide in the composition of the invention is preferably from 0.0001% by weight to 95% by weight, preferably from 0.001% by weight to 90% by weight, more preferably from 0.01% by weight to 85% by weight, still more preferably 0.1% From wt to 80% by weight, particularly preferably from 5% by weight to 60% by weight, most preferably from 7.5% by weight to 50% by weight. In other embodiments, the amount of bifenthrin in the composition of the invention is preferably from 0.0001% by weight to 50% by weight, preferably from 0.001% by weight to 40% by weight, more preferably from 0.01% by weight to 30% by weight, still more preferably 0.1% % wt to 20% wt, particularly preferably 0.2% wt to 12.5% wt, most preferably 1% wt to 10% wt. In some embodiments, the weight ratio of biguanide to bifenthrin in the composition of the invention is from 1000:1 to 0.001:1, preferably from 200:1 to 0.05:1, more preferably from 50:1 to 0.75:1, Most preferred is 5:1 to 1.5:1.

[10] The present invention also provides a composition comprising a synergistically effective amount of biguanide and bifenthrin for controlling parasites which have obtained resistance to biguanides, op compounds and sp compounds ( Especially mites and tsetse flies).

The invention also provides a product for controlling mites and tsetse flies comprising separate, sequential or simultaneous administration of biguanide and bifenthrin.

[12] In some aspects of the invention, the parasite of the animal is an ectoparasite of an animal (especially a warm-blooded animal such as a mammal, such as sheep, cattle, etc.), particularly a mites and a picking rope.

[13] The present invention also provides the use of a composition comprising biguanide and bifenthrin for the preparation of a medicament for controlling parasites in animals. Preferably, the parasite is an ectoparasite. In some embodiments, the biguanide and bifenthrin in the compositions of the invention are synergistically effective amounts. In still other embodiments, the amount of biguanide in the composition of the invention is preferably from 0.0001% by weight to 95% by weight, preferably from 0.001% by weight to 90% by weight, more preferably from 0.01% by weight to 85% by weight, still more preferably 0.1% From wt to 80% by weight, particularly preferably from 5% by weight to 60% by weight, most preferably from 7.5% by weight to 50% by weight. In other embodiments, the amount of bifenthrin in the composition of the invention is preferably from 0.0001% by weight to 50% by weight, preferably from 0.001% by weight to 40% by weight, more preferably from 0.01% by weight to 30% by weight, still more preferably 0.1% % wt to 20% wt, particularly preferably 0.2% wt to 12.5% wt, most preferably 1% wt to 10% wt. In some embodiments, the weight ratio of biguanide to bifenthrin in the composition of the invention is from 1000:1 to 0.001:1, preferably from 200:1 to 0.05:1, more preferably from 50:1 to 0.75:1, Optimal [14] As is well known to those skilled in the art, the term "synergistic" as used herein means that the combined effect of two or more substances is significantly greater than the sum of the two. detailed description

[15] Biguanide is the common name for N,N-bis(2,4-diphenylphenyliminoindenyl)guanamine. Double mites are used for pests in anti-mammal domesticated pets, where they are used to control mites and mites. Also, it is used to control lice on cattle and pigs. These insecticidal formulations contain, as an essential component, biguanide and at least one specific insecticidal active pyrethroid compound. It has been found that these α-cyanobenzylphenyl acetate pyrethroids and biguanides have synergistic activity against mites (i.e., the combination exhibits activity compared to the two insecticide components). Higher insecticidal activity is expected).

[16] The pyrethroids expected to contain a halogen atom (preferably a chlorine atom) having an atomic number of 9 to 35 inclusive, or an alkoxy group having 1 to 4 carbon atoms. An example is bifenthrin or (2-mercapto[1,1-biphenyl]-3-yl)-indolyl-3-(2-chloro-3,3,3-trifluoro-1-propene -2,2-Dimercaptocyclopropanecarboxylate.

[17] Bifenthrin is a synthetic pyrethroid with insecticidal and acaricidal activity. The chemical name is (2-mercapto[1,1-biphenyl]-3-yl)-indolyl-3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2. 2-Dimercaptocyclopropanecarboxylate. Bifenthrin acts through contact and stomach toxicity, which paralyzes the nervous system of insects and ticks.

[18] In order to prepare the composition of the present invention, the composition is formulated into a wettable powder, an aqueous concentrate, an emulsifiable concentrate (EC), a liquid concentrate, etc. by a conventional method. The conventional methods are, for example, admixing the active compound with suitable carriers and adjuvants such as emulsifying agents, dispersing agents, stabilizing agents, suspending agents, penetrating agents and the like. The invention is preferably formulated as an emulsifiable concentrate.

The composition according to the invention is especially suitable for controlling ectoparasites (preferably mites) of animals, especially warm-blooded animals such as mammals. The composition according to the invention is preferably used in pets. Here, pets should be understood to include especially sheep, cattle and other temperatures. Blood animals.

The amount of active ingredient in the compositions of the present invention may vary widely, but will generally be from about 0.1% to about 95% of the active ingredient (the percentages in the specification and claims of the present application are usually by weight unless otherwise indicated) . Preferably, the ratio of the amount of bifenthrin to the amount of bismuth is from about 1:5 to about 4:6. The amount of biguanide in the composition according to the invention may vary widely from 0.1% to about 80%. Amounts of from 5 to 60% are preferred, and more preferably, the composition according to the invention comprises biguanides in the range of from 7.5 to 50%. Also, the amount of bifenthrin can vary widely from 0.2% to 12.5%. An amount of from 1 to 10% is preferred, and more preferably, the amount of bifenthrin used in the composition according to the present invention is from 2 to 8%.

[21] Residues that bring the composition to 100% include a carrier and various additives. "Carrier, as used herein, means an organic substance which may be natural or synthetic and which is associated with the active ingredient and which facilitates its administration to an animal. Thus, the carrier is generally inert and should be achievable by an animal Acceptable (especially for cattle or sheep). The carrier can be solid (eg clay, silicate, silica, resin, wax, fertilizer, etc.) or liquid (eg water, alcohols, ketones, oil solvents, saturated) Or unsaturated hydrocarbons, chlorinated hydrocarbons, liquefied petroleum gas, etc.).

[22] Among a wide variety of adjuvants, the compositions of the present invention may comprise surfactants as well as other ingredients such as dispersants, stickers, antifoaming agents, antifreeze agents, dyes, thickeners, binders, protections. Colloids, penetrants, stabilizers, chelating agents, anti-flocculants, corrosion inhibitors, pigments and polymers.

More generally, the compositions of the present invention may comprise all types of solid or liquid additives well known in the art of insecticides and insecticidal treatments.

[24] Surfactants may be emulsified or wetted, ionic or nonionic. Nonionic surfactants such as: polyethoxylated castor oil, polysorbated sorbitan monooleate, sorbitan monostearate, glyceryl monostearate, polyoxyethylene Stearic acid ester, alkylphenol polyglycol ether. Anionic surfactants such as sodium lauryl sulfate, fatty alcohol ether sulfates, mono/dialkyl polyethylene glycol ether orthophosphate monoethanolamine salts. The composition according to the present invention can be prepared by a conventional method of mixing the active compound and preparing a solution, for example, by stirring with other ingredients.

The formulation according to the invention is characterized in that it has a good storage stability of at least 3 years in all climatic zones. Due to its high potency, the application volume can be small. The preferred administration volume is 0.075-0.25 ml/kg [weight of the pet to be treated], preferably 0.1-0.15 ml/1.0 kg [weight of the pet to be treated].

Further, the composition according to the present invention is non-irritating to the skin and low in toxicity to animals.

[28] Finally, they are environmentally friendly due to their biodegradability. The following examples further illustrate details for making and using the compositions of the present invention. The spirit or scope of the invention as set forth in the foregoing disclosure is not limited by the embodiments. Those skilled in the art will appreciate that known variations in the conditions and procedures of the following preparative methods can be used to prepare these compositions. EXAMPLES [30] Example 1 :

100 composition bismuth original drug 10.00g bifenthrin original drug 2.50g

Solvesso 150 72.9g butyl hydroxy benzene. ig ethoxylated soybean oil ll.OOg

[31] Example 2: lOO composition

Amitraz and the original drug lO.OOg bifenthrin original drug 2.50g

Solvesso 150 72.9g Butyl Hydroxyphenylene O.lg Polyoxyethyl Stearate ll.OOg Sodium Lauryl Sulfate 3.50g

[32] Example 3:

100 composition

Double bismuth original drug 10.00g bifenthrin original drug 2.50g

Solvesso 150 72.9g Butylhydroxyindole Benzene O.lg Polyethoxylated Sorbitan Monooleate ll.OOg Sodium Lauryl Sulfate 3.50g

[33] Example 4:

100 composition

Bismuth drug 10.00g bifenthrin original drug 2.50g N-methylpyrrolidone 72.9g butyl hydroxy benzene benzene O.lg Polyethoxylated sorbitan monooleate ll.OOg sodium lauryl sulfate 3.50g

[34] Example 5:

100 composition

Amitraz and the original drug lO.OOg bifenthrin original drug 2.50g

N-methylpyrrolidone 68.9g water 4.0g butylhydroxytoluene O.lg polyethoxylated sorbitan monooleate ll ll.OOg sodium lauryl sulfate 3.50g

[35] Example 6:

100 composition

Biguanide original drug lO.OOg bifenthrin original drug 2.50g N-mercaptopyrrolidone 68.9g water 4.0g butylhydroxyindole benzene O.lg ethoxylated soybean oil ll.OOg calcium benzenesulfonate 3.50g

[36] Example 7: lOO composition

Shuangzhi original drug 12.5 _g bifenthrin original drug 5.00g

Solvesso 150 67.9g Butylhydroxyindole Benzene .ig Ethoxylated Soybean Oil ll.OOg Calcium Benzosulfonate 3.50g

[37] Example 8:

100 composition

Bismuth drug 12.5g bifenthrin original drug 5.00g

Solvesso 150 67.9g butyl hydroxy benzene o.ig polyoxyethyl stearate ll.OOg sodium lauryl sulfate 3.50g

[38] Example 9:

100 composition

Biguanide original drug 12.50g bifenthrin original drug 5.00g Solvesso 150 67.9g butyl hydroxy phenyl benzene. ig Polyethoxylated sorbitan monooleate ll.OOg sodium lauryl sulfate 3.50g

[39] Example 10:

100g composition

Biguanide original drug 12.50g bifenthrin original drug 5.00g N-mercaptopyrrolidone 67.9g butylhydroxyindole benzene.ig polyethoxylated sorbitan monooleate ll.OOg dodecyl sulfate Sodium 3.50g

[40] Example 11:

100 composition

Biguanide original drug 12.50g bifenthrin original drug 5.00g N-mercaptopyrrolidone 64.0g water 4.0g butylhydroxyindole benzene o.ig polyethoxylated sorbitan monooleate ll.OOg Sodium dialkyl sulfate 3.50g

[41] Example 12:

100 composition Double bismuth original drug lO.OOg bifenthrin original drug 2.50g

N-decylpyrrolidone 68.9 g water 4.0 g butylhydroxyindole benzene O.lg ethoxylated soybean oil ll.OOg calcium benzenesulfonate 3.50 g [42] Example 13

[43] The following experiment was performed to show that bismuth and bifenthrin were combined with cockroaches (Dopper Sheep) in Nakura, Kenya (mainly / 3⁄4> 3⁄4 head) ( Rhipicephalus appendiculatus ) ^ L force.

[44] The test was carried out using the following compositions according to Examples 1-12 compared to the untreated control: a. Composition A: According to Example 1 containing 12.5% biguanide + 5% bifenthrin 6 The composition was prepared to provide 250 ppm of biguanide and 100 ppm of bifenthrin. b. Composition B: This composition was prepared according to Examples 7-12 containing 10.0% biguanide + 2.5% bifenthrin to provide 250 ppm biguanide and 62.25 ppm bifenthrin. c Composition C: The composition was prepared according to a registered hydrazine based on biguanide to provide 250 ppm biguanide. [45] Identify a group of 60 sheep aged 1-2 years, mark them and freely stock them for 28 days at Sunset Farm in Nakuru. The mites on these sheep were counted. Sixteen candidates were selected for the experiment, and the following Table 1 was systematically randomized to make the average count around the flocks and to be divided into four groups. A unique ear tag ( Eartag ) was used for each group, and each individual in the group was marked to identify the animal. The treatment groups were sprayed with various preparations, and the treatment was carried out four times in order of seven days. Processed The first day is designated as day 0. The mites were counted and recorded after treatment on days 1, 3, 5 and 7. Table 1 Experimental group and processing

[46] The sheep are appropriately imprisoned to count the face (including the ears) and the mites on the perineum. Identify, count, and record all adult monuments that are parasitic on the animal in each region.

[47] 10 liters of dip wash was prepared freshly for each group on each spray day. Each test preparation was uniformly emulsified in water to give a white mixture. Each animal was sprayed with a Hobra rocker double suction pump equipped with a double hose and an adjustable double cone nozzle. The entire batt of each sheep was thoroughly wetted with 2.5 liters of acaricide formulated for each treatment group.

[48] Use the improved formula according to Abbott's formula: Effectiveness % = [1- (Process / Control) ] χ 100%

[49] The efficacy of the compositions of the invention was evaluated by comparing the counts of treated mites on treated sheep to the counts of untreated sheep.

[50] The combined weekly total mites and the total counts for the 28-day period are shown in Table 2. Table 2 Summary of axillary counts Weekly total

Group effectiveness

Day 1 2 3 4 Total % 0 22 22

Y 1 21 25 23 21 90

3 24 22 24 22 92

5 21 20 23 24 88

7 22 22 22 24 90

0 22 22

B 1 7 1 0 0 8

3 1 0 0 0 1 98.91

5 1 1 0 0 2 97.73

7 2 1 0 0 3 96.67

0 23 23

G 1 5 0 0 0 5

3 1 0 0 0 1 98.91

5 1 1 0 0 2 97.73

7 2 2 0 0 4 95.56

0 22 22

R 1 5 2 0 0 7

3 1 1 0 0 2 97.82

5 2 1 1 0 4 95.45

7 3 1 1 1 6 93.33

[51] The results showed that Composition A reached 98.91%, 97.73%, and 96.67% on days 3, 5, and 7, and Composition B reached 98.91%, 97.73%, and 95.56% on days 3, 5, and 7. Composition C reached 97.82%, 95.45%, and 93.33% on days 3, 5, and 7. The results also show the sheep body treated by Composition A and Composition B after 2 weeks (14 days). The mites on the count were 0, while the mites were present on the sheep treated with Composition C. Therefore, composition C was used to cause resistance to blue sputum based on the efficacy data on day 7 and the sputum count data after 2 weeks (14 days). This phenomenon corresponds to the practical application of a three-week rotation spray method applied by farmers to remove mites (especially blue sputum and brown sputum). However, Composition A and Composition B according to the present invention showed no resistance.

Further, in the present invention, the combination of bismuth-bifenthrin forms a stable emulsion which can be effectively used as an acaricide. This combination is also safe for livestock. No adverse effects associated with the use of the formulation were observed on the test sheep.

In addition, it has been found that the biguanide-bifenthrin combination of the present invention is better against flies which cause sleep disorders which cannot be killed by the biguanide.

Claims

Rights request

A composition comprising a synergistically effective amount of biguanide and bifenthrin and optionally a solid or liquid carrier, wherein the composition is useful for controlling parasites, preferably ectoparasites, especially Apes or tsetse flies.

2. The composition of claim 1 wherein the weight ratio of biguanide to bifenthrin is

1000:1 to 0.001:1, preferably 200:1 to 0.05:1, more preferably 50:1 to 0.75:1, most preferably

3. The composition of claim 1 or 2, wherein the amount of biguanide is from 0.0001% by weight to 95% by weight, preferably from 0.001% by weight to 90% by weight, more preferably from 0.01% by weight to 85% by weight, still more preferably 0.1% by weight Up to 80% by weight, particularly preferably 5% by weight to 60% by weight, most preferably 7.5% by weight to 50% by weight.

4. The composition of claim 1 or 2 wherein the amount of bifenthrin is from 0.0001% by weight to 50% by weight, preferably from 0.001% by weight to 40% by weight, more preferably from 0.01% by weight to 30% by weight, still more preferably 0.1% From wt to 20% by weight, particularly preferably from 0.2% by weight to 12.5% by weight, most preferably from 1% by weight to 10% by weight.

5. A method of controlling parasites (especially mites or tsetse flies) of an animal, the method comprising

(a) providing a composition according to any one of claims 1-4, and

(b) applying the composition to an animal susceptible to parasite damage.

6. The method of claim 5, wherein the animal is a warm-blooded animal, such as a mammal, such as sheep, cattle, and the like.

7. Use of a composition according to any of claims 1-4 for the preparation of a medicament for controlling parasites in animals, preferably ectoparasites, in particular ticks or tsetse flies.

8. The use of claim 7, wherein the biguanide and the bifenthrin are synergistically effective amounts.

9. Use according to claim 7 or 8, wherein the animal is a warm-blooded animal, such as a mammal, such as sheep, cattle, and the like.

The use according to any one of claims 7 to 9, wherein the weight ratio of biguanide to bifenthrin is from 1000:1 to 0.001:1, preferably from 200:1 to 0.05:1, more preferably 50:1. 0.75:1, most preferably 5:1-1.5:1.

The use according to any one of claims 7 to 9, wherein the amount of biguanide is

0.0001% wt to 95% wt, preferably 0.001% wt to 90% wt, more preferably 0.01% wt to 85% wt, still more preferably 0.1% wt to 80% wt, particularly preferably 5% wt to 60% wt, most preferably 7.5 %wt to 50%wt.

The use according to any one of claims 7 to 9, wherein the amount of bifenthrin is 0.0001% by weight to 50% by weight, preferably 0.001% by weight to 40% by weight, more preferably 0.01% by weight to 30% by weight, and further It is preferably from 0.1% by weight to 20% by weight, particularly preferably from 0.2% by weight to

12.5% wt, most preferably from 1% wt to 10% wt.