Ready-to-use liquid pest control composition
A stable, ready-to-use pest control composition using polyether modified trisiloxane surfactants with bulky bases and tocopherol maintains stability and efficacy for prolonged periods, addressing safety and convenience issues of existing formulations.
Patent Information
- Application Number
- PCT/EP2025/051863
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-04-23
- Filing Date
- 2025-01-24
- Publication Date
- 2025-07-31
AI Technical Summary
Existing pest control compositions using pyrethroids are harmful to humans and pets, and require inconvenient dilution before use, with trisiloxane-based formulations experiencing stability issues due to hydrolysis, especially at pH levels outside the neutral range.
A ready-to-use liquid pest control composition comprising polyether modified trisiloxane surfactants stabilized by bulky bases with steric hindrance and tocopherol, maintaining a pH of at least 7, which prevents hydrolysis and ensures stability for prolonged periods without the need for dilution.
The composition effectively immobilizes and kills pests, remaining stable for at least two years without phase separation, and is safe for domestic use, offering improved safety and convenience.
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Figure EP2025051863_31072025_PF_FP_ABST
Abstract
Description
[0001] Ready-to-use liquid pest control composition
[0002] The present invention relates to a ready-to-use liquid pest control composition, to a method of immobilizing and / or killing insects, and to a pest control product.
[0003] Background
[0004] Pesticides are used to kill insects, such as cockroaches, flies, ants, and spiders. Normally these pesticides contain toxic substances, which are well-known in the art; for example, pyrethroids, which kill insects through a neuro-toxicant mechanism.
[0005] Some drawbacks of pyrethroids when used by domestic consumers inside the home are that these may be harmful to domestic pets, to the environment and these should not be used around food preparation areas.
[0006] Some attempts have been made of providing formulations in which a pest is trapped in a network. For example, patent application WO2016 / 061259 to ICB Pharma describes pesticidal compositions for controlling pests and pathogens with a physical mode of action. The compositions comprise trisiloxane surfactants and matrix-forming agents. Because of the ingredients in the compositions, these are safe to humans and domestic pets, and environmentally benign. However, WO2016 / 061259 has its predominant focus on use in the industrial setting (e.g. agriculture and animal husbandry). It makes the formulations initially as one of various types of format such as a powder, emulsifiable concentrate or solvent dispersion, which are then diluted in water before use to control the pests. The present inventors recognise that when such formulations are mixed with water, the compositions are not stable. The lack of stability is not such an issue in the context of WO2016 / 061259, since the formulations need not be stored for prolonged periods in the aqueous state; they can be made up into aqueous liquids just prior to use. For the domestic consumer, on the other hand, it is inconvenient to have to carry out the extra dilution step. In order to be able to sell a pest control composition to a consumer in a prediluted format for them to use as is, longer term water stability of that composition is obviously critical.
[0007] Other examples of disclosures of water dispersible granules containing trisiloxanes for agricultural pesticidal use include CN105325415A (Jiangsu Rotam) and CN107136063B (Guilin Jiqi Biochemistry). CN104996418A (Guangzhou Fangzhong) discloses synergist compositions comprising silicones, which are intended to be mixed with other pesticides prior to application, but does not discuss the hydrolysis stability issue or the pH of the diluted formulation.
[0008] CN 109810131 A (Fujian Taxi New Material) discusses that polyether trisiloxane surfactants are used in water-based paints, pesticides, water-based inks and detergents, but have poor resistance to hydrolysis. It notes the problem exists at all pHs, but even more so at pH less than 5 or more than 9, where it will fail in about a week. Its approach to addressing this problem is to modify the structure of the polyether trisiloxane to lengthen the linking group between the O-Si-O structure and the polyether to the unit -CH2CH2CH2-S-CH2CH2CH2-. The new compound is synthesised via a mercaptopropyl intermediate compound. Data is provided to show surface tension and improved hydrolytic stability (more than 1 month in acidic and alkaline environments). However, there is still room for improvement on the stability, and efficacy of the new compounds in pest control compositions is not tested. In addition, such modified trisiloxane compounds are rather specialist and not so widely available at a good price due to their complex synthetic process of manufacture.
[0009] Therefore, there is a need of a ready-to-use liquid pest control composition which is easy to manufacture and remains stable for a prolonged period, preferably at least two years. The ready-to-use formulation should be capable of immobilising and / or killing a pest, ideally without the need of using substances which might be toxic to humans and domestic pets.
[0010] It would be desirable to have a ready-to-use liquid pest control composition comprising water, which immobilises and / or kills a pest and remains stable for a prolonged period, preferably at least 2 years. Because the composition comprises water and is ready-to- use it can be sold “as is”, meaning that it is shelf stable.
[0011] Summary of the invention
[0012] In a first aspect of the invention, there is provided a ready-to-use liquid pest control composition comprising: at least one polyether modified trisiloxane surfactant of Formula (I), at least 40 wt% water, and at least one hydrolysis-preventing compound selected from at least one bulky base with steric hindrance, tocopherol, and combinations thereof, wherein the bulky base with steric hindrance is selected from the group consisting of alkali metal bicarbonates, trialkylamines, trialkanolamines, 2-tert-butyl-1 ,1 ,3,3- tetramethylguanidine, lithium diisopropylamine, alkali metal tert-butoxide, and combinations thereof; wherein the composition has a pH of at least 7, measured at 20°C.
[0013] Formula (I) is as follows: wherein: R is -(CH2)3-(OCH2CH2)nR1; R1is -CH3, -OH, or -O(O)CCH3, and n is 2 to 25, preferably 5 to 20, more preferably 5 to 15, even more preferably 7 to 11.
[0014] In an embodiment, the composition has a pH of between 7 and 9.5, measured at 20 °C.
[0015] In another embodiment, the at least one bulky base with steric hindrance is selected from the group consisting of alkali metal bicarbonates, trialkylamines, trialkanolamines, and combinations thereof.
[0016] In another embodiment, the at least one bulky base with steric hindrance is selected from the group consisting of sodium bicarbonate, triethanolamine, diisopropylethylamine, 2-tert-Butyl-1 ,1 ,3,3-tetramethylguanidine, potassium tert-butoxide, and combinations thereof.
[0017] In another embodiment, the at least one bulky base with steric hindrance is selected from the group consisting of sodium bicarbonate, triethanolamine, and combinations thereof.
[0018] In a preferred embodiment, the at least one bulky base with steric hindrance is sodium bicarbonate.
[0019] In another preferred embodiment, the at least one hydrolysis-preventing compound is at least one bulky base with steric hindrance and the composition has a pH of between 7.5 and 9.5, measured at 20°C, preferably between 8.0 and 9.0, more preferably between 8.0 and 8.5.
[0020] In another preferred embodiment, the at least one hydrolysis-preventing compound is tocopherol, and the composition has a pH of between 7.1 and 9.0, measured at 20°C. In another preferred embodiment, R is -(CH2)3-(OCH2CH2)nOH or -(CH2)3- (OCH2CH2)nCH3.
[0021] In an embodiment, the composition is substantially free of matrix-forming agents selected from a chitosan salt, a sol-gel precursor and combinations thereof, wherein the sol-gel precursor is selected from the group consisting of tetraethyl orthosilicate, tetramethyl orthosilicate, and combinations thereof.
[0022] In another embodiment, the composition comprises between 0.1 wt.% and 20 wt.% of the trisiloxane surfactant, based on the total weight of the composition, preferably between 0.25 wt.% and 15 wt.%, more preferably between 0.5 wt.% and 10 wt.%, even more preferably between 0.75 wt.% and 7.5 wt.%, most preferably between 1 wt.% and 5 wt.% or between 1.25 wt.% and 3 wt.% or between 1.5 wt.% and 2.5 wt.%.
[0023] In another embodiment, the composition comprises at least 50 wt.% water, based on the total weight of the composition, preferably between 55 wt.% and 95 wt.%, or between 60 wt.% and 90 wt.%, or between 65 wt.% and 85 wt.%, or between 70 wt.% and 80 wt.%.
[0024] In a further embodiment, the composition comprises between 0.001 wt.% and 10 wt.% of the at least one hydrolysis-preventing compound, based on the total weight of the composition, preferably between 0.0025 wt.% and 7.5 wt.%, more preferably between 0.005 wt.% and 5 wt.%, even more preferably between 0.0075 wt.% and 2.5 wt.%, most preferably between 0.009 wt.% and 1 wt.% or between 0.009 wt.% and 0.5 wt.%.
[0025] In a preferred embodiment, the composition further comprises at least one alcohol selected from the group consisting of primary, secondary and tertiary alcohols having between 2 and 10 carbon atoms.
[0026] In another embodiment, the at least one alcohol is selected from the group consisting of ethanol, isopropanol, and mixtures thereof, preferably the alcohol is ethanol.
[0027] In a further embodiment, the composition comprises between 1 wt.% and 50 wt.% of the at least one alcohol, based on the total weight of the composition, preferably between 10 wt.% and 40 wt.%, more preferably between 15 wt.% and 35 wt.%, most preferably between 20 wt.% and 30 wt.%.
[0028] In another embodiment, the composition further comprises at least one active agent selected from the group consisting of pyrethroids, essential oils, and combinations thereof.
[0029] In a preferred embodiment, the composition is substantially free of active agents selected from the group consisting of pyrethroids. In another preferred embodiment, the composition is substantially free of active agents selected from the group consisting of pyrethroids, essential oils, and combinations thereof.
[0030] In a second aspect, the invention relates to a method of immobilising and / or killing insects, comprising contacting the insects with the ready-to-use liquid pest control composition according to first aspect of the invention, preferably wherein the insects are crawling insects and / or flying insects, preferably wherein the insects comprise cockroaches.
[0031] In an embodiment, the method comprises contacting the insects with from 1 g to 20 g of the composition according to the first aspect of the invention.
[0032] In another embodiment of the second aspect of the invention, the insects are crawling insects and the method comprises contacting the crawling insects with from 2 g to 20 g of the ready-to-use pest control composition, preferably with from 5 g to 15 g.
[0033] In another embodiment of the second aspect of the invention, the insects are flying insects and the method comprises contacting the flying insects with 1 g to 20 g or 2 g to 20 g of the ready-to-use pest control composition, preferably with 1.5 g to 15 g, more preferably with from 2 g to 10 g, even more preferably with from 2.5 to 5 g.
[0034] In a third aspect, the invention relates to a pest control product comprising the ready-to- use liquid control composition according to the first aspect of the invention and a container, wherein the ready-to-use liquid control composition is contained in said container, and preferably, the container is in the form of a pump spray or an aerosol can.
[0035] Definitions
[0036] The following definitions are used in the present application.
[0037] “Pest control composition” as used in the present patent application means a composition comprising at least one active ingredient, which is used as a means for directly or indirectly controlling, destroying, attracting or repelling a pest, for example, insects.
[0038] “Pest control product”, as used in the present application means a product comprising a pest control composition, which is used as a means for directly or indirectly controlling, destroying, attracting or repelling a pest, for example, insects. “Glass ring study” as used in the present application means a method for determining the bio-efficacy of a pest control composition or a pest control product. Using glass rings of about 15.5 cm of diameter and 8.5 cm height a thin layer of Vaseline is applied to the extremes of the ring. Subsequently 10 insects, e.g. German cockroaches or American cockroaches, are placed in the ring and the formulation to be tested is applied to the insects. The KT50 and KT90 are recorded immediately after spraying. Post recording the knockdown (KD), the test pests are transferred to clean rings covered with a meshed sieve containing food and water and observed for 24, 48, 72 hours mortality. This type of studies is performed at about 25°C and about 60% relative humidity.
[0039] “Metal ring study” as used in the present application means a method for determining the bio-efficacy of a pest control composition or a pest control product. The metal ring study can be performed using a large metal ring or a small metal ring.
[0040] The large metal ring study is performed using a top ring of about 15.0 cm height and 15.0 cm diameter attached to a base ring of about 10.0 cm height and 15.0 cm diameter. A meshed sieve separates the top ring and the base ring.
[0041] The small metal ring study is performed using a top ring of about 15.0 cm height and 10.0 cm diameter attached to a base ring of about 10.0 cm height and 10.0 cm diameter. A meshed sieve separates the top ring and the base ring.
[0042] When the metal ring study is used to determine the bio-efficacy of a pest control composition or a pest control product on flying insects, the top ring is also covered with a meshed sieve after a population of the flying insects has been introduced in the top ring. Therefore, the flying insects remain between the meshed sieve that separates the top ring and the base ring and the meshed sieve on the top ring.
[0043] A thin layer of Vaseline is applied to the extremes of the top ring. Subsequently 10 insects, are placed in the top ring and the formulation to be tested is applied to the insects. The KT50 and KT90 are recorded immediately after spraying. Post recording the knockdown (KD), the test pests are transferred to clean rings covered with a meshed sieve containing food and water and observed for 24, 48, 72 hours mortality. This type of studies is performed at about 25°C and about 60% relative humidity.
[0044] “KT50 or KT50” as used in the present application means, the time, in seconds, needed to paralyse or knock-down 50% of the insects in a test. For example, if the sample size in a test is of 10 insects, then the KT50 or KT50 is the time, in seconds, needed to paralyse 5 insects. By paralyse or knock-down is meant that the insects cannot move, take off or stand.
[0045] “KT90 or KT90” as used in the present application means, the time, in seconds, needed to paralyse or knock-down 90% of the insects in a test. For example, if the sample size in a test is of 10 insects, then the KT90 or KT90 is the time, in seconds, needed to paralyse 9 insects. By paralyse or knock-down is meant that the insects cannot move, take off or stand.
[0046] Detailed description of the invention
[0047] In a first aspect, the present invention relates to a ready-to-use liquid pest control composition as described in the summary of the invention above.
[0048] The pest control composition is in liquid form, and it will be understood that it does not show phase separation and, macroscopically, it is a homogeneous liquid.
[0049] The present inventors have observed that by adding a bulky base that acts as a poor nucleophile due to its steric hindrance, hydrolysis of the trisiloxane surfactant is reduced or avoided. This makes it possible to have a pest control composition that is ready to use, in other words, the pest control composition does not need to be dissolved and can be directly applied to the pest of interest.
[0050] Furthermore, the present inventors have observed that tocopherol acts as a proton scavenger and therefore, it also reduces or prevents hydrolysis of the trisiloxane surfactant.
[0051] In short, the present inventors have observed that a hydrolysis-preventing compound selected from at least one bulky base with steric hindrance and tocopherol provides a ready-to-use composition comprising water and a trisiloxane surfactant that is ready to use. It will be understood that by preventing hydrolysis of the trisiloxane surfactant the composition remains stable and the amount of active, i.e. trisiloxane surfactant, does not significantly change in time.
[0052] One parameter of paramount importance in the compositions according to the invention is the pH. When a composition comprising only water and a trisiloxane surfactant is prepared, its pH is of less than 7. However, when a hydrolysis-preventing compound selected from at least one bulky base with steric hindrance and tocopherol is added to the composition, its pH increases. The present inventors have observed that a pH of at least 7, measured at 20°C allows for the preparation of a composition that is stable, i.e. hydrolysis of the trisiloxane surfactant is reduced or avoided. Preferably the pH of the composition is between 7 and 9.5, measured at 20 °C.
[0053] Depending on the type of hydrolysis-preventing compound present in the composition the optimum pH to avoid or reduce hydrolysis of the trisiloxane may vary. For example, when the at least one hydrolysis-preventing compound is tocopherol, the composition preferably has a pH of between 7.1 and 9.0, measured at 20°C. Conversely, when the at least one hydrolysis-preventing compound is at least one bulky base with steric hindrance, the composition preferably has a pH of between 7.5 and 9.5, measured at 20°C, more preferably between 8.0 and 9.0, even more preferably between 8.0 and 8.5.
[0054] It should be noted that if a base without steric hindrance is added to the composition, e.g. sodium hydroxide, hydrolysis is not avoided; actually, the present inventors have observed that bases without steric hindrance, e.g. NaOH, accelerate hydrolysis of the trisiloxane surfactant.
[0055] The composition may comprise between 0.001 wt.% and 10 wt.% of the at least one hydrolysis-preventing compound, based on the total weight of the composition, preferably between 0.0025 wt.% and 7.5 wt.%, more preferably between 0.005 wt.% and 5 wt.%, even more preferably between 0.0075 wt.% and 2.5 wt.%, most preferably between 0.009 wt.% and 1 wt.% or between 0.009 wt.% and 0.5 wt.%.
[0056] The at least one bulky base with steric hindrance may be selected from the group consisting of alkali metal bicarbonates, trialkylamines, trialkanolamines, and combinations thereof; preferably selected from the group consisting of sodium bicarbonate, triethanolamine, di-isopropylethylamine, 2-tert-Butyl-1 , 1 ,3,3- tetramethylguanidine, potassium tert-butoxide, and combinations thereof; more preferably selected from the group consisting of sodium bicarbonate, triethanolamine, and combinations thereof; even more preferably the at least one bulky base with steric hindrance is sodium bicarbonate.
[0057] The trisiloxane surfactant is a polyether modified trisiloxane, which has Formula (I) wherein: R is -(CH2)3-(OCH2CH2)nR1; R1is -CH3, -OH, or -O(O)CCH3, and n is 2 to 25, preferably 5 to 20, more preferably 5 to 15, even more preferably 7 to 11.
[0058] In a preferred embodiment, R is -(CH2)3-(OCH2CH2)nOH or -(CH2)3-(OCH2CH2)nCH3.
[0059] Examples of trisiloxane surfactants in which R is -(CH2)3-(OCH2CH2)nOH are Silibase 2848, Coatosil 7608, and Silwet 408.
[0060] Examples of trisiloxane surfactants in which R is-(CH2)3-(OCH2CH2)nCH3are Silibase 2877, and Coatosil 77.
[0061] Polyether modified trisiloxanes having formula (I) in which R is -(CH2)3-(OCH2CH2)nOH or -(CH2)3-(OCH2CH2)nCH3and n is 2 to 25, preferably 5 to 20, more preferably 5 to 15, even more preferably 7 to 11 , are considered superspreaders. When a composition comprising water and this type of surfactants is applied to a pest, it affects the insects’ body, particularly the jointed appendages, causing immobilisation and death.
[0062] It should be noted that the composition according to the invention is in liquid form and, when applied, it does not form any type of 3D network as provided in patent application WO 2016 / 061259 to ICB Pharma. In WO 2016 / 061259 to ICB Pharma a 3D network is formed thanks to the combination of a trixilosane surfactant and a matrix forming agent; this 3D network immobilises the pest and this leads to its death.
[0063] The mode of action of the composition according to the invention and that of WO 2016 / 061259 to ICB Pharma is different. In the present application the pest is immobilized via interaction with jointed appendages whilst in WO 2016 / 061259 the pest is immobilised with a 3D polymer network. In an embodiment of the present invention, the composition is substantially free of at least one matrix-forming agent selected from a chitosan salt, a sol-gel precursor and combinations thereof, wherein the sol-gel precursor is selected from the group consisting of tetraethyl orthosilicate, tetramethyl orthosilicate, and combinations thereof.
[0064] By substantially free it is meant that an ingredient has not been deliberately added to the composition. Therefore, in an embodiment the composition comprises less than 5 wt.% of at least one matrix-forming agent selected from a chitosan salt, a sol-gel precursor and combinations thereof, wherein the sol-gel precursor is selected from the group consisting of tetraethyl orthosilicate, tetramethyl orthosilicate, and combinations thereof, based on the total weight of the composition, preferably less than 2 wt.%, or less than 1 wt.%, or less than 0.5 wt.%, or less than 0.1 wt.% or 0 wt.%.
[0065] The composition may comprise between 0.1 wt.% and 20 wt.% of the trisiloxane surfactant, based on the total weight of the composition, preferably between 0.25 wt.% and 15 wt.%, more preferably between 0.5 wt.% and 10 wt.%, even more preferably between 0.75 wt.% and 7.5 wt.%, most preferably between 1 wt.% and 5 wt.% or between 1.25 wt.% and 3 wt.% or between 1.5 wt.% and 2.5 wt.%.
[0066] The composition is in liquid form and it comprises at least 50 wt.% water, based on the total weight of the composition, most preferably between 55 wt.% and 95 wt.%, or between 60 wt.% and 90 wt.%, or between 65 wt.% and 85 wt.%, or between 70 wt.% and 80 wt.%.
[0067] As the composition is a ready-to-use composition at least one alcohol may be added to help solubilise the trisiloxane surfactant in water. Therefore, in an embodiment, the composition further comprises at least one alcohol selected from the group consisting of primary, secondary and tertiary alcohols having between 2 and 10 carbon atoms; preferably selected from the group consisting of ethanol, isopropanol, and mixtures thereof, more preferably the alcohol is ethanol.
[0068] The composition may comprise between 1 wt.% and 50 wt.% of the at least one alcohol, based on the total weight of the composition, preferably between 10 wt.% and 40 wt.%, more preferably between 15 wt.% and 35 wt.%, most preferably between 20 wt.% and 30 wt.%.
[0069] Although the main mode of action of the composition according to the invention is interaction with parts of the insect’s body, particularly the jointed appendages, the composition may further comprise at least one active agent selected from the group consisting of pyrethroids, essential oils, and combinations thereof. However, pyrethroids tend to be stable only in acidic pHs. In an embodiment, the composition is substantially free of pyrethroids. As for essential oils, these may experience solubility challenges in the formulation ultimately risking phase separation, depending on the concentration, presence of alcohol etc. as the trisiloxane does not emulsify them. In a preferred embodiment, the composition is substantially free of active agents selected from the group consisting of pyrethroids, essential oils, and combinations thereof.
[0070] By substantially free it is meant that an ingredient has not been deliberately added to the composition. Therefore, in an embodiment the composition comprises less than 5 wt.% of active agents selected from the group consisting of pyrethroids, essential oils, and combinations thereof, based on the total weight of the composition, preferably less than 2 wt.%, or less than 1 wt.%, or less than 0.5 wt.%, or less than 0.1 wt.% or 0 wt.%. In another embodiment the composition comprises less than 5 wt.% of pyrethroids based on the total weight of the composition, preferably less than 2 wt.%, or less than 1 wt.%, or less than 0.5 wt.%, or less than 0.1 wt.% or 0 wt.% pyrethroids.
[0071] The composition may further be electrolytic. In an embodiment, it comprises a water- soluble ionic salt, preferably a water-soluble ionic salt having a pH of 7 or above. In an embodiment, the composition comprises a water-soluble chloride salt, such as sodium chloride, potassium chloride or ammonium chloride. Without wishing to be bound by theory, it is believed that such salts, particularly those with high ionic strength, may disrupt the structural integrity of the chitin layer of insects and enhance penetration of the trisiloxane through the exoskeleton. A particularly strong effect has been observed with crawling insects, which are easier to get sufficiently wet with the composition of the invention, and especially cockroaches, which do not have hairs impacting how the salt interacts with the chitin layer. Sodium chloride is an excellent choice for the salt from a pH and formulation stability point of view.
[0072] Preferably, the salt (preferably sodium chloride) is present in an amount of up to 5 wt%, based on the total weight of the composition, preferably: at least 0.1 wt%, at least 0.3 wt%, at least 0.5 wt%, at least 0.7 wt%, or at least 1.0 wt%; and / or up to 4 wt%, up to 3 wt %, up to 2 wt%, or up to 1.5 wt%.
[0073] In a second aspect, the invention relates to a method of immobilising and / or killing insects, comprising contacting the insects with the ready-to-use liquid pest control composition according to the first aspect of the invention, preferably wherein the insects are crawling insects and / or flying insects. In an embodiment, the insects comprise crawling insects, preferably cockroaches.
[0074] The method according to the second aspect of the invention may comprise contacting the insects with from 1 g to 20 g of the composition of the first aspect of the invention.
[0075] The amount of the composition to be applied to the insect of interest would depend on the type of insects. Therefore, in an embodiment, the insects are crawling insects, and the method comprises contacting the crawling insects with from 2 g to 20 g of the ready- to-use pest control composition, preferably with from 5 g to 15 g. In another embodiment, the insects are flying insects, and the method comprises contacting the flying insects with 1 g to 20 g or 2 g to 20 g of the ready-to-use pest control composition, preferably with 1.5 g to 15 g, more preferably with from 2 g to 10 g, even more preferably with from 2.5 to 5 g. In a third aspect, the invention relates to a pest control product comprising the ready-to- use liquid control composition according to the first aspect of the invention and a container, wherein the ready-to-use liquid control composition is contained in said container, and preferably, the container is in the form of a pump spray or an aerosol can.
[0076] As the composition according to the first aspect of the invention is a ready-to-use one, a wide range of pump type sprays known in the art may be used. For example, the container for the composition may comprise a high-density polyethylene or PET bottle and a pump assembly formed of a polypropylene and / or polyethylene housing and dip tube and actuator, the pump dispensing a volume of 30 - 300 microlitres per stroke.
[0077] In the case of an aerosol the composition may comprise between 10 % and 90 % of a propellant, such as butane or butane / propane mixtures. Preferably the propellant is in a concentration of 15-80% w / v, most preferably 20-70% w / v. Particularly preferred is a concentration of about 40% w / v of propellant.
[0078] A typical aerosol can comprise a 52-67 mm diameter tinplate can with a 159 - 241mm length and a 250 - 600mL nominal fill capacity. The valving arrangement comprising a standard diameter valve, sleeved gasket with a tinplate valve cup and a polyethylene dip tube. The stem should have a single or multiple orifices ranging from 0.4 - 0.7mm and an output of 1.0 - 3.0 g / sec.
[0079] The foregoing aspects may be freely combined with any of the foregoing aspects disclosed herein.
[0080] The invention will be further described, by way of example, with the reference to the following non-limiting embodiments.
[0081] Examples
[0082] Formulations according to the invention and comparative formulations were prepared by: i. Mixing water and ethanol, ii. Adding the trisiloxane surfactant to the mixture of water and ethanol and stirring until the trisiloxane surfactant has been fully dissolved, iii. For the formulations according to the invention, adding the hydrolysispreventing compound to the solution of water, ethanol, and the trisiloxane surfactant to achieve the desired pH. Stability tests
[0083] The formulations shown in Table 1 were prepared following the procedure shown above. In this table formulations represented by a letter are comparative formulations, whilst those represented by a number are formulations according to the invention. Table 1. Comparative formulations and formulations according to the invention used in the stability tests.
[0084] In table 1 : all formulations contain 25 wt.% of ethanol and the rest of water, - TEOA means triethanolamine,
[0085] Tocoph. Means tocopherol,
[0086] NaHCOs + TEOA is a mixture of 50 wt.% NaHCO3and 50 wt. % triethanolamine, all trisiloxane surfactants (Tris. 1 , tris. 2, tris. 3, and tris. 4) have formula (I): o In tris. 1 (OH): R is -(CH2)3-(OCH2CH2)nOH, which is commercially available under Silibase 2848. o In tris. 2 (CH3): R is -(CH2)3-(OCH2CH2)nCH3, which is commercially available under Silibase 2877. o In tris 3 (CH3): R is -(CH2)3-(OCH2CH2)nCH3, which is commercially available under Coatosil 77. o In tris. 4 (OH): R is -(CH2)3-(OCH2CH2)nOH, which is commercially available under Coatosil 7608.
[0087] The formulation to be tested was placed in a PET bottle or a Glass bottle, subsequently the formulation in the bottle was kept at a temperature of about 55 °C and the following values were measured at the beginning of the test, after 1 week and after 2 weeks: - pH appearance, and active content, i.e. trisiloxane surfactant content
[0088] These tests in which the formulations were kept at a temperature of about 55°C for 2 weeks are equivalent to 2 years on shelf. The active content (i.e. % of trisiloxane) was measured using High Performance Liquid Chromatography. It should be noted that due to the temperature used in the tests, i.e. 55 °C, the lid of the bottle could have expanded, and some evaporation occurred. The results of the stability tests are shown in Table 2.
[0089] Table 2. Stability results of the formulations in table 1.
[0090] In table 2, with appearance the following scale is used:
[0091] • 4: clear transparent solution
[0092] • 3: slightly hazy solution
[0093] • 2: slightly hazy solution with fine precipitate in the bottom • 1 : hazy solution.
[0094] The results in Table 2 clearly demonstrate that by adding a hydrolysis-preventing compound to the composition hydrolysis of the trisiloxane surfactant is highly reduced. This is evidenced by the %-age of trisiloxane measured after 2 weeks using HPLC.
[0095] Bio-efficacy tests The formulations shown in Table 3 were prepared following the procedure previously shown. In all the formulations shown in Table 3 NaHCCh was added to the formulations until a pH of between 8 and 8.5 was achieved. Furthermore, all formulations in Table 3 contained 25 wt.% of ethanol and the rest of water.
[0096] The formulations were tested using American cockroaches. Table 3. Formulations for bio-efficacy tests
[0097] In Table 3: trisiloxane surfactants tris. 2 and tris. 4 have formula (I): o In tris. 2: R is -(CH2)3-(OCH2CH2)nCH3, which is commercially available under Silibase 2877. o In tris. 4: R is -(CH2)3-(OCH2CH2)nOH, which is commercially available under Coatosil 7608.
[0098] The mortality after 24 hours using the formulations shown in table 3 was of 100%.
[0099] The formulations shown in Table 4 were prepared following the procedure previously shown. In all the formulations shown in Table 4 NaHCCh was added to the formulations until a pH of between 8 and 8.5 was achieved. The amount of trisiloxane surfactant was varied and the content of ethanol in all formulations was 25 wt.%, with the rest of the formulation being water.
[0100] The formulations were tested using American cockroaches.
[0101] Table 4. Formulations for bio-efficacy tests
[0102] In Table 4:
[0103] The trisiloxane surfactant tris. 1 has formula (I):
[0104] Wherein R is -(CH2)3-(OCH2CH2)nOH, which is commercially available under Silibase 2848. The mortality after 24 hours using the formulations shown in table 4 was of 100%.
[0105] The formulations shown in Table 5 were prepared following the procedure previously shown. In all the formulations shown in Table 5 NaHCCh was added to the formulations until a pH of about 8.5 was achieved. The type of trisiloxane surfactant was varied and the content of ethanol in all formulations was 25 wt.%, with the rest of the formulation being water.
[0106] The formulations were tested using American cockroaches.
[0107] Table 5. Formulations for bio-efficacy tests
[0108] In Table 5:
[0109] The trisiloxane surfactant tris. 1 has formula (I): o In tris. 1 : R is -(CH2)3-(OCH2CH2)nOH, which is commercially available under Silibase 2848. o In tris. 2: R is -(CH2)3-(OCH2CH2)nCH3, which is commercially available under Silibase 2877. o In tris 3: R is -(CH2)3-(OCH2CH2)nCH3, which is commercially available under Coatosil 77. o In tris. 4: R is -(CH2)3-(OCH2CH2)nOH, which is commercially available under Coatosil 7608.
[0110] The results in Tables 3-5 show that the compositions according to the invention effectively immobilise and kill a pest.
[0111] Further formulations were tested which incorporate 1 wt% sodium chloride into a composition of the invention comprising sodium bicarbonate, 2.5 wt% of a trisiloxane surfactant of formula I in which R is -(CH2)3-(OCH2CH2)nOH, 25 wt% ethanol, > 70 wt% water and minor fragrances. The quantity of sodium bicarbonate used was chosen to adjust the pH to within the range 8-8.5. An American cockroach was released in a glass ring and sprayed with 5 consecutive sprays of the composition corresponding to a total quantity of 5g. Immediately after spraying, the glass ring was removed and the cockroach was allowed to move freely. The total run distance and knockdown time was recorded. The test was repeated and compared with an identical composition without the sodium chloride, the balance being made up with water. Results were as follows:
[0112] These results show that addition of sodium chloride to the inventive compositions improves the efficacy, seen particularly via the reduction in the distance travelled by the cockroaches before they are killed. Hence one or more objects of the present invention are achieved by the compositions according to the invention which is further elucidated in the appended claims.
Claims
CLAIMS1. A ready-to-use liquid pest control composition comprising: at least one trisiloxane surfactant, at least 40 wt.% water, and at least one hydrolysis-preventing compound selected from at least one bulky base with steric hindrance, tocopherol, and combinations thereof, wherein the bulky base with steric hindrance is selected from the group consisting of alkali metal bicarbonates, trialkylamines, trialkanolamines, 2-tert-Butyl-1 , 1 ,3,3- tetramethylguanidine, lithium diisopropylamine, alkali metal tert-butoxide, and combinations thereof; wherein the composition has a pH of at least 7, measured at 20°C; and wherein the trisiloxane surfactant is a polyether modified trisiloxane of Formula (I):wherein: R is -(CH2)3-(OCH2CH2)nR1; R1is -CH3, -OH, or -O(O)CCH3(preferably CH3or OH), and n is 2 to 25, preferably 5 to 20, more preferably 5 to 15, even more preferably 7 to 11.
2. The composition according to claim 1 , wherein the composition has a pH of between 7 and 9.5, measured at 20 °C.
3. The composition according to claim 1 or 2, wherein the at least one bulky base with steric hindrance is selected from the group consisting of alkali metal bicarbonates, trialkylamines, trialkanolamines, 2-tert-Butyl-1 ,1 ,3,3-tetramethylguanidine, potassium tert-butoxide, and combinations thereof; preferably wherein the at least one bulky base with steric hindrance is selected from the group consisting of sodium bicarbonate, triethanolamine, di-isopropylethylamine, 2-tert- Butyl- 1 ,1 ,3,3-tetramethylguanidine, potassium tert-butoxide, and combinations thereof; preferably wherein the at least one bulky base with steric hindrance is selected from the group consisting of sodiumbicarbonate, triethanolamine, and combinations thereof; preferably wherein the at least one bulky base with steric hindrance is sodium bicarbonate.
4. The composition according to any of the preceding claims, wherein the at least one hydrolysis-preventing compound is at least one bulky base with steric hindrance and the composition has a pH of between 7.5 and 9.5, measured at 20°C, preferably between 8.0 and 9.0, more preferably between 8.0 and 8.5.
5. The composition according to claim 2, wherein the at least one hydrolysispreventing compound is tocopherol, and the composition has a pH of between 7.1 and 9.0, measured at 20°C.
6. The composition according to any of the preceding claims, wherein the composition is substantially free of matrix-forming agents selected from a chitosan salt, a sol-gel precursor and combinations thereof, wherein the sol-gel precursor is selected from the group consisting of tetraethyl orthosilicate, tetramethyl orthosilicate, and combinations thereof.
7. The composition according to any of the preceding claims, wherein the composition comprises between 0.1 wt.% and 20 wt.% of the trisiloxane surfactant, based on the total weight of the composition, preferably between 0.25 wt.% and 15 wt.%, more preferably between 0.5 wt.% and 10 wt.%, even more preferably between 0.75 wt.% and 7.5 wt.%, most preferably between 1 wt.% and 5 wt.% or between 1.25 wt.% and 3 wt.% or between 1.5 wt.% and 2.5 wt.%.
8. The composition according to any of the preceding claims, wherein the composition comprises at least 50 wt.% water, based on the total weight of the composition, preferably between 55 wt.% and 95 wt.%, or between 60 wt.% and 90 wt.%, or between 65 wt.% and 85 wt.%, or between 70 wt.% and 80 wt.%, water based on the total weight of the composition.
9. The composition according to any of the preceding claims, wherein the composition comprises between 0.001 wt.% and 10 wt.% of the at least one hydrolysispreventing compound, based on the total weight of the composition, preferably between 0.0025 wt.% and 7.5 wt.%, more preferably between 0.005 wt.% and 5 wt.%, even more preferably between 0.0075 wt.% and 2.5 wt.%, most preferably between 0.009 wt.% and 1 wt.% or between 0.009 wt.% and 0.5 wt.%.
10. The composition according to any of the preceding claims, wherein the composition further comprises at least one alcohol selected from the group consisting of primary, secondary and tertiary alcohols having between 2 and 10 carbon atoms; preferably: a) wherein the at least one alcohol is selected from the group consisting of ethanol, isopropanol, and mixtures thereof, preferably wherein the alcohol is ethanol; and / or b) wherein the composition comprises between 1 wt.% and 50 wt.% of the at least one alcohol, based on the total weight of the composition, preferably between 10 wt.% and 40 wt.%, more preferably between 15 wt.% and 35 wt.%, most preferably between 20 wt.% and 30 wt.%.
11. The composition according to any of the preceding claims, wherein the composition: a) comprises less than 5 wt.% of pyrethroids, based on the total weight of the composition, preferably less than 2 wt.%, or less than 1 wt.%, or less than 0.5 wt.%, or less than 0.1 wt.% or 0 wt.% of pyrethroids, based on the total weight of the composition; or b) is substantially free of active agents selected from the group consisting of pyrethroids, essential oils, and combinations thereof.
12. The composition according to any of the preceding claims, which further comprises a water-soluble ionic salt, preferably: a water-soluble ionic salt having a pH of 7 or above; and / or a water-soluble chloride salt (preferably sodium, potassium or ammonium chloride, preferably sodium chloride); preferably in an amount of up to 5 wt%, based on the total weight of the composition, preferably: at least 0.1 wt%, at least 0.3 wt%, at least 0.5 wt%, at least 0.7 wt%, or at least 1.0 wt%; and / or up to 4 wt%, up to 3 wt %, up to 2 wt%, or up to 1.5 wt%.
13. A method of immobilising and / or killing insects, comprising contacting the insects with a ready-to-use liquid pest control composition according to any of the preceding claims, preferably wherein the insects are crawling insects and / or flying insects,preferably wherein the insects comprise crawling insects, preferably wherein the insects comprise cockroaches.
14. The method according to claim 13, wherein the method comprises contacting the insects with from 1 g to 20 g of the composition according to any of claims 1-12; preferably wherein: a) the insects are crawling insects and the method comprises contacting the crawling insects with from 2 g to 20 g of the ready-to-use pest control composition, preferably with from 5 g to 15 g; or b) the insects are flying insects and the method comprises contacting the flying insects with 2 g to 20 g or 1.5 g to 15 g of the ready-to-use pest control composition, preferably with from 2 g to 10 g, even more preferably with from 2.5 to 5 g.
15. A pest control product comprising the ready-to-use liquid control composition according to any of the claims 1-12 and a container, wherein the ready-to-use liquid control composition is contained in said container, and preferably, the container is in the form of a pump spray or an aerosol can.
Citation Information
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