Animal pest control agent containing etofenprox and an insect growth regulator

Abstract

To provide a pest control agent for animals, particularly a pest control agent for animals suitable for direct application to animals.SOLUTION: A pest control agent for animals is prepared that comprises etofenprox of 20 mass% or more and less than 50 mass%, an insect growth control agent, and an ethylene glycol ether and / or a medium chain fatty acid triglyceride. Such a pest control agent for animals may further comprise an antioxidant. Here, pests typically include fleas, mites, mosquitoes or lice.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to an agent for controlling pests that infest animals such as pets and livestock. More specifically, the present invention relates to an animal pest control agent for controlling pests such as fleas, ticks, mosquitoes, and lice. [Background technology]

[0002] Pests that attach to animals that interact with humans, such as pets or livestock, can transmit diseases that cause serious symptoms in these animals, or can cause allergies or other harmful effects in humans. To combat these pests, pest control agents that are applied by dripping, spraying, or painting onto the body surfaces of pets and livestock are known.

[0003] As the active ingredient of such animal pest control agents, pyrethroid compounds and combinations of pyrethroid compounds with other compounds are widely used (Patent Document 1). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Publication No. 2020-007238 Summary of the Invention [Problem to be solved by the invention]

[0005] There is a need for further animal pest control agents that have good stability, good skin spreadability, and reliable pest control.

[0006] An object of the present invention is to provide an animal pest control agent that can be applied directly to animals that are the target of pest control and has a pest control effect. [Means for solving the problem]

[0007] As a result of extensive research to solve this problem, the inventors have discovered that an animal pest control agent that is stable even at low temperatures and has excellent skin diffusion properties can be prepared by incorporating specific concentrations of etofenprox, an insect growth regulator, and ethylene glycol ethers and / or medium-chain fatty acid triglycerides, and have thereby completed the present invention.

[0008] That is, the present invention provides the following animal pest control agents. Section 1. An animal pest control agent containing 20 w / v% or more but less than 50 w / v% etofenprox; an insect growth regulator; and ethylene glycol ethers and / or medium-chain fatty acid triglycerides. Section 2. Item 2. The animal pest control agent according to Item 1, wherein the insect growth regulator is pyriproxyfen and / or S-methoprene. Section 3. Item 3. The animal pest control agent according to Item 1 or 2, wherein the ethylene glycol ether is diethylene glycol monoethyl ether. Section 4. Item 3. The animal pest control agent according to Item 1 or 2, further comprising an antioxidant. Section 5. Item 5. The animal pest control agent according to any one of Items 1 to 4, wherein the pest is a flea, a tick, a mosquito, or a louse. Section 6. Item 6. The animal pest control agent according to any one of Items 1 to 5, comprising 0.001 to 1 part by mass of the insect growth regulator per 1 part by mass of the etofenprox.

[0009] Furthermore, the present invention provides the following stabilization methods. Section 7. A method for stabilizing a composition containing etofenprox and an insect growth regulator by setting the concentration of etofenprox to 20 w / v% or more and less than 50 w / v% and further allowing ethylene glycol ethers and / or medium-chain fatty acid triglycerides to be present.

[0010] Furthermore, the present invention provides the following method for enhancing skin diffusion. Section 8. A method for promoting the diffusion of etofenprox and an insect growth regulator in a composition on the skin by setting the concentration of etofenprox to 20 w / v% or more but less than 50 w / v% and further allowing ethylene glycol ethers and / or medium-chain fatty acid triglycerides to be present in the composition. [Effects of the Invention]

[0011] According to the present invention, it is possible to provide an animal pest control agent having excellent stability and excellent skin diffusion properties. [Brief explanation of the drawings]

[0012] [Figure 1] FIG. 1 is a diagram showing a method for testing the skin diffusibility of the composition of the present invention. DETAILED DESCRIPTION OF THE INVENTION

[0013] In this specification, the content unit "w / v%" is synonymous with "g / 100 ml."

[0014] [Animal pest control agents] The animal pest control agent of the present invention is an animal pest control agent containing etofenprox and an insect growth regulator as active ingredients.

[0015] (Etofenprox) Etofenprox means 2-(4-ethoxyphenyl)-2-methylpropyl 3-phenoxybenzyl ether. Any active stereoisomer or mixture of etofenprox can be used.

[0016] In the animal pest control agent of the present invention, the content of etofenprox relative to the total amount of the animal pest control agent is 20 w / v% or more and less than 50 w / v%, preferably 25 w / v% or more and 48 w / v% or less, more preferably 30 w / v% or more and 45 w / v% or less, even more preferably 35 w / v% or more and 42 w / v% or less, and particularly preferably 40 w / v%.

[0017] (insect growth regulator) Insect growth regulators are substances that inhibit insect molting and emergence by controlling the balance of hormones that regulate insect metamorphosis and molting. Examples of insect growth regulators include chitin synthesis inhibitors, such as benzoylurea compounds like chlorfluazuron, diflubenzuron, flufenoxuron, lufenuron, novaluron, and teflubenzuron; molting hormone-active compounds like ecdysteroids; and juvenile hormone-like substances selected from the group consisting of hydroprene, kinoprene, fenoxycarb, pyriproxyfen, diofenolan, epofenonane, triprene, methoprene (especially S-methoprene), and hydroprene. These insect growth regulators can be used alone or in combination. Any active stereoisomers or mixtures thereof can also be used as these compounds. Of these, juvenile hormone-like substances are preferably used, and pyriproxyfen and / or S-methoprene are more preferably used.

[0018] In order to achieve the effects of the present invention, the content of the insect growth regulator relative to the total amount of the animal pest control agent of the present invention is preferably 0.01 w / v% or more and 10 w / v% or less, more preferably 0.1 w / v% or more and 7 w / v% or less, and even more preferably 0.2 w / v% or more and 5 w / v% or less.

[0019] In particular, the content of pyriproxyfen and / or S-methoprene relative to the total amount of the animal pest control agent of the present invention is preferably 0.01 w / v% or more and 10 w / v% or less, more preferably 0.1 w / v% or more and 7 w / v% or less, and even more preferably 0.2 w / v% or more and 5 w / v% or less, from the viewpoint of exerting the effects of the present invention.

[0020] In the animal pest control agent of the present invention, the ratio of insect growth regulator to etofenprox is preferably 0.001 to 1 part by mass, more preferably 0.002 to 0.5 parts by mass, and even more preferably 0.004 to 0.2 parts by mass, per 1 part by mass of etofenprox.

[0021] In the animal pest control agent of the present invention, the ratio of pyriproxyfen and / or S-methoprene to etofenprox is preferably 0.001 parts by mass or more and 1 part by mass or less, more preferably 0.002 parts by mass or more and 0.5 parts by mass or less, and even more preferably 0.004 parts by mass or more and 0.2 parts by mass or less, per 1 part by mass of etofenprox.

[0022] (Ethylene glycol ethers) The animal pest control agent of the present invention may contain ethylene glycol ethers in addition to etofenprox and an insect growth regulator. By using ethylene glycol ethers, after the pest control agent containing etofenprox and an insect growth regulator is dropped onto an animal, the agent spreads across the entire body surface via the sebum on the animal's skin surface. The ethylene glycol ethers are not particularly limited as long as they are of a grade suitable for use as a component of topical skin preparations for animals or humans. Examples of ethylene glycol ethers include diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, diethylene glycol monoisobutyl ether, diethylene glycol dimethyl ether, ethylene glycol monobutyl ether, ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, triethylene glycol monobutyl ether, and tetraethylene glycol monobutyl ether. Among these, diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, diethylene glycol monopropyl ether, ethylene glycol monobutyl ether, triethylene glycol monobutyl ether, and tetraethylene glycol monobutyl ether are preferred, with diethylene glycol monoethyl ether being particularly preferred.

[0023] From the viewpoint of exerting the effects of the present invention, the content of ethylene glycol ethers relative to the total amount of the animal pest control agent of the present invention is preferably 10 w / v% or more and 80 w / v% or less, more preferably 20 w / v% or more and 75 w / v% or less, even more preferably 30 w / v% or more and 70 w / v% or less, and even more preferably 50 w / v% or more and 65 w / v% or less.

[0024] In particular, from the viewpoint of exerting the effects of the present invention, the content of diethylene glycol monoethyl ether relative to the total amount of the animal pest control agent of the present invention is preferably 10 w / v% or more and 80 w / v% or less, more preferably 20 w / v% or more and 75 w / v% or less, even more preferably 30 w / v% or more and 70 w / v% or less, and even more preferably 50 w / v% or more and 65 w / v% or less.

[0025] In the animal pest control agent of the present invention, the ratio of ethylene glycol ethers to etofenprox is preferably 0.3 parts by mass or more and 4 parts by mass or less, more preferably 0.5 parts by mass or more and 3 parts by mass or less, even more preferably 1 part by mass or more and 2 parts by mass or less, and even more preferably 1.2 parts by mass or more and 1.8 parts by mass or less, per 1 part by mass of etofenprox.

[0026] In the animal pest control agent of the present invention, the ratio of diethylene glycol monomethyl ether to etofenprox is preferably 0.3 parts by mass or more and 4 parts by mass or less, more preferably 0.5 parts by mass or more and 3 parts by mass or less, even more preferably 1 part by mass or more and 2 parts by mass or less, and even more preferably 1.2 parts by mass or more and 1.8 parts by mass or less, per 1 part by mass of etofenprox.

[0027] (medium-chain triglycerides) The animal pest control agent of the present invention may contain a medium-chain fatty acid triglyceride in addition to etofenprox and an insect growth regulator. By using a medium-chain fatty acid triglyceride, the pest control agent containing etofenprox and an insect growth regulator spreads across the entire body surface of the animal via sebum on the skin surface after being dropped onto the animal. The medium-chain fatty acid triglyceride is not particularly limited as long as it is of a grade suitable for use as a component of an animal or human skin preparation. The medium-chain fatty acid triglyceride is a fatty acid triglyceride having 6 to 10 carbon atoms. More specifically, it is an ester compound obtained by reacting an unsaturated fatty acid having 6 to 10 carbon atoms with glycerin, with the molar ratio of unsaturated fatty acid to glycerin being 3:1. Preferred examples of the medium-chain fatty acid triglyceride include tri(caprylic / capric)glyceryl, glyceryl tricaprylate, and glyceryl tricaprate. As the medium-chain fatty acid triglyceride, it is possible to use a compound extracted from a plant or the like, or a compound synthesized by a chemical method.

[0028] From the viewpoint of exerting the effects of the present invention, the content of medium-chain fatty acid triglycerides relative to the total amount of the animal pest control agent of the present invention is preferably 10 w / v% or more and 80 w / v% or less, more preferably 20 w / v% or more and 75 w / v% or less, even more preferably 30 w / v% or more and 70 w / v% or less, and even more preferably 50 w / v% or more and 65 w / v% or less.

[0029] In the animal pest control agent of the present invention, the ratio of medium-chain fatty acid triglyceride to etofenprox is preferably 0.3 parts by mass or more and 4 parts by mass or less, more preferably 0.5 parts by mass or more and 3 parts by mass or less, even more preferably 1 part by mass or more and 2 parts by mass or less, and even more preferably 1.2 parts by mass or more and 1.8 parts by mass or less, per 1 part by mass of etofenprox.

[0030] (antioxidant) The animal pest control agent of the present invention may contain an antioxidant in addition to etofenprox, an insect growth regulator, and an ethylene glycol ether and / or a medium-chain fatty acid triglyceride. Examples of antioxidants used in the present invention include dibutylhydroxytoluene (BHT), butylhydroxyanisole (BHA), and 4,4'-thiobis(3-methyl-6-t-butylphenol) (TBMTBP). Of these, BHT and BHA are particularly preferred.

[0031] The content of the antioxidant relative to the total amount of the animal pest control agent of the present invention is preferably 0.001 w / v% or more and 10.0 w / v% or less, more preferably 0.003 w / v% or more and 5.0 w / v% or less, even more preferably 0.005 w / v% or more and 1.5 w / v% or less, and even more preferably 0.01 w / v% or more and 1.0 w / v% or less.

[0032] In the animal pest control agent of the present invention, the ratio of antioxidant to etofenprox is preferably 0.00003 to 3 parts by mass, more preferably 0.000005 to 1.5 parts by mass, even more preferably 0.000008 to 1.0 part by mass, and even more preferably 0.00001 to 0.8 parts by mass, per part by mass of etofenprox.

[0033] In the animal pest control agent of the present invention, the ratio of the antioxidant to the ethylene glycol ethers and / or medium-chain fatty acid triglycerides is preferably 0.000001 to 3.0 parts by mass, more preferably 0.000005 to 2.0 parts by mass, even more preferably 0.000008 to 1.0 part by mass, and even more preferably 0.00001 to 0.5 parts by mass of the antioxidant per 1 part by mass of the ethylene glycol ethers and / or medium-chain fatty acid triglycerides.

[0034] (water) The animal pest control agent of the present invention can be formulated with water or can be in the form of a composition that does not contain any water. Examples of such water include purified water such as ion-exchanged water, ordinary tap water, and industrial water. The content of water relative to the total amount of the animal pest control agent is preferably 5 w / v % or less, more preferably 3 w / v % or less, and particularly preferably no water or substantially no water.

[0035] (pest) Pests as referred to in this specification are not limited to, but particularly include fleas (including fleas that parasitize dogs, cats, etc.), mites (including ticks, chiggers, oribatid mites, scabies mites, and animal chiggers), or parasitic or blood-sucking pests such as lice, mosquitoes, etc. Particularly preferred pests to be controlled are fleas, mites, mosquitoes, or lice.

[0036] The animals of the present invention include various animals such as pets, livestock, and poultry, particularly pets such as dogs, cats, rabbits, and hamsters, and livestock and poultry such as cows, horses, pigs, and chickens.

[0037] (pH) From the viewpoint of the stability or safety of the components, the animal pesticide of the present invention preferably has a liquid pH of 3 to 10. More preferably, the animal pesticide has a pH of 4 to 8. The pH of the animal pesticide can be measured at 20°C using a commercially available pH meter (for example, Model F-52 (registered trademark) manufactured by Horiba, Ltd.). When the animal pesticide does not contain water, the pH is determined by diluting the animal pesticide 20 times with purified water.

[0038] (viscosity) From the viewpoint of component stability, etc., the viscosity of the animal pest control agent of the present invention at 25°C, SPINDLE No. M1, 100 rpm is preferably about 0.5 to 1000 mPa·s, more preferably about 3 to 100 mPa·s. The viscosity of the animal pest control agent can be measured at 25°C using a commercially available viscometer (for example, TVB-10M model, manufactured by Toki Sangyo Co., Ltd.).

[0039] (Other ingredients) The animal pest control agent of the present invention may contain optional ingredients other than etofenprox and the insect growth regulator, as long as the effects of the present invention are not impaired. Examples of optional ingredients include pest control ingredients other than etofenprox and the insect growth regulator, pH adjusters, surfactants, silicone compounds, chelating agents, anti-redeposition agents, polymers, preservatives, antibacterial agents, disinfectants, natural product extracts, dispersants, antioxidants, thickeners, viscosity reducers, stabilizers, deodorizers, fragrances, and pigments.

[0040] Examples of pH adjusters include, but are not limited to, citric acid, sodium citrate, phosphoric acid, sodium bicarbonate, triethanolamine, ammonia, potassium hydroxide, sodium hydroxide, and the like.

[0041] (surfactant) Examples of surfactants include polyoxyethylene alkyl ethers, polyoxyethylene fatty acid alkyl esters, polyoxyethylene alkylamines, alkyl polyglucosides, and polyoxyethylene hydrogenated castor oil.

[0042] (Applications, etc.) The animal pest control agent of the present invention can be applied, but is not limited to, particularly by dropping it onto the back or the like of an animal.

[0043] The animal pest control agent of the present invention can be used once a week, once every two weeks, once a month, once every three months, or once every six months, depending on the intended use.

[0044] From the viewpoint of control effect, the amount of the animal pest control agent of the present invention to be used is, for example, preferably an amount that results in 10 mg or more of etofenprox per application, more preferably an amount that results in 50 mg or more, and even more preferably an amount that results in 150 mg or more. From the viewpoint of safety, the amount of the control agent of the present invention to be used is preferably an amount that results in 3000 mg or less of etofenprox per application, more preferably an amount that results in 2400 mg or less.

[0045] In terms of control effect, the amount of the animal pest control agent of the present invention to be used is, for example, preferably an amount such that the amount of insect growth inhibitor per application is 0.01 mg or more, more preferably an amount such that the amount is 0.2 mg or more, and even more preferably an amount such that the amount is 1.0 mg or more. In terms of safety, the amount of the control agent of the present invention to be used is preferably an amount such that the amount of the animal pest control agent per application is 500 mg or less, more preferably an amount such that the amount is 240 mg or less.

[0046] [Stabilization method] The present invention also relates to a method for stabilizing a composition by incorporating etofenprox and an insect growth regulator with ethylene glycol ethers and / or medium-chain fatty acid triglycerides into the composition. Here, "stabilization" refers to the absence of precipitation of etofenprox and / or the insect growth regulator, particularly after storage for 24 hours or more at room temperature or at temperatures ranging from about -5°C to room temperature. In the stabilization method of the present invention, the etofenprox and insect growth regulator, the ethylene glycol ethers and / or medium-chain fatty acid triglycerides, and their contents are as described above for the animal pest control agent. Furthermore, the pH, other optional ingredients, their contents, and other conditions are as described above for the animal pest control agent.

[0047] [Method for promoting skin diffusion] The present invention also relates to a method for promoting the diffusion of etofenprox and an insect growth regulator on the skin by incorporating etofenprox and an insect growth regulator with ethylene glycol ethers and / or medium-chain fatty acid triglycerides into the composition. The skin may be the skin of an animal other than humans. In the method for promoting skin diffusion of the present invention, the etofenprox and insect growth regulator, the ethylene glycol ethers and / or medium-chain fatty acid triglycerides, and their contents are the same as those described for the animal pest control agent. Furthermore, the pH, other optional ingredients, their contents, and other conditions are the same as those described for the animal pest control agent. [Example]

[0048] Next, the present invention will be described in detail with reference to examples, but the present invention is not limited to the following examples. The unit of the amount of each component in the tables is w / v % unless otherwise specified in the tables.

[0049] [1] Stability testing The compositions of the Examples and Comparative Examples shown in Table 1 were prepared by conventional methods, and the stability of these compositions was evaluated.

[0050] Specifically, the stability evaluation was carried out by transferring each composition to a 20 mL screw tube, sealing it, and leaving it to stand at −5° C. After 24 hours, the sample was taken out of the −5° C. storage cabinet and brought to room temperature, and the state of the solution at that time was visually observed. Those with crystal precipitation were rated as ×, and those without were rated as ◯.

[0051] The results are shown in Table 1.

[0052] [Table 1]

[0053] As a result of the stability test, the compositions of the examples showed remarkable stability at -5°C compared to the compositions of the comparative examples.

[0054] [2] Skin diffusion confirmation test The compositions of the Examples and Comparative Examples were evaluated for skin diffusion.

[0055] The evaluation for confirming skin diffusion was specifically carried out as follows. First, pigskin (suede) cut into a 5 cm wide x 12 cm long piece was left for 1 hour at a temperature of 25°C ± 2°C and a humidity of 75% RH ± 5% RH. In the same room, 0.5 mL of each composition from each Example or Comparative Example was dropped onto the center of the pigskin using a micropipette. As shown in Figure 1, the piece was left to stand for 24 hours after dropping. The piece was cut every 2 cm from the center and divided into three sections: (1) at a distance of 2 cm, (2) at a distance of 2-4 cm, and (3) at a distance of 4-6 cm. The amounts of etofenprox and pyriproxyfen contained in each section were analyzed. The abundance ratio (mass%) of each section was then calculated, assuming the initial amount of each composition to be 100%.

[0056] The results are shown in Table 2.

[0057] [Table 2]

[0058] As a result of the skin diffusion confirmation test, the compositions of the examples showed remarkable diffusion properties compared to the compositions of the comparative examples.

Claims

1. Etofenprox 25% w / v or more and 48% w / v or less; insect growth regulator 0.2 w / v % or more and 5 w / v % or less; antioxidants, 0.01 w / v% or more and 10 w / v% or less; and An animal pest control agent containing 50 w / v % or more and 70 w / v % or less of ethylene glycol ethers and / or medium-chain fatty acid triglycerides.

2. The animal pest control agent according to claim 1, wherein the insect growth regulator is pyriproxyfen and / or S-methoprene.

3. The animal pest control agent according to claim 1 or 2, wherein the ethylene glycol ether is diethylene glycol monoethyl ether.

4. The animal pest control agent according to any one of claims 1 to 3, wherein the pest is a flea, a tick, a mosquito, or a louse.

5. A method for stabilizing a composition containing etofenprox and an insect growth regulator by adjusting the concentration of the etofenprox to 25 w / v% or more and 48 w / v% or less, the concentration of the insect growth regulator to 0.2 w / v% or more and 5 w / v% or less, and further adding an antioxidant to the composition at 0.01 w / v% or more and 10 w / v% or less, and adding ethylene glycol ethers and / or medium-chain fatty acid triglycerides at 50 w / v% or more and 70 w / v% or less.

6. A method for promoting the diffusion of etofenprox and an insect growth regulator on the skin in a composition containing etofenprox and an insect growth regulator, by adjusting the concentration of the etofenprox to between 25 w / v% and 48 w / v%, the concentration of the insect growth regulator to between 0.2 w / v% and 5 w / v%, and further adding an antioxidant at between 0.01 w / v% and 10 w / v%, and adding ethylene glycol ethers and / or medium-chain fatty acid triglycerides at between 50 w / v% and 70 w / v%.

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