Powder formulations comprising a carrier to which the active ingredient is applied via a solvent

Abstract

The present disclosure provides insecticidal compositions capable of controlling insects, including bed bugs. The present disclosure further provides methods of applying the insecticidal compositions described herein to control insects, including bed bug infestations. The present disclosure further provides methods of preparing insecticidal compositions useful for controlling insects, including bed bugs.

Description

Technical Field

[0001] The present disclosure provides insecticidal compositions capable of controlling insects, including bed bugs. The present disclosure further provides methods of applying the insecticidal compositions described herein to control insects, including bed bug infestations. The present disclosure further provides methods of preparing insecticidal compositions useful for controlling insects, including bed bugs. Background Art

[0002] There is a continuing need for compositions and methods that are effective in controlling bed bugs.

[0003] Bed bugs have been known parasites for thousands of years and feed on blood. Treatment of bed bug bites is aimed at controlling symptoms. Patient response to the bites varies, ranging from no visible effects to small yellow spots to noticeable wheals and bullae formation, accompanied by intense itching that may last for several days.

[0004] Central bleeding spots may also occur due to the release of anticoagulants in the insect's saliva. Symptoms may not develop until several days after the bite, and reactions usually occur immediately after exposure after multiple bites, probably due to sensitivity to the bed bug's anticoagulant salivary proteins. Skin reactions usually occur in the area of ​​the bite, most commonly on the arms, shoulders, and legs. Multiple bites may result in an erythematous rash or urticaria.

[0005] More severe bed bug infestations and chronic bites are known to cause anxiety, stress, and insomnia in some patients. The development of persistent delusional parasitosis is possible because the patient develops a great obsession with bed bugs. Therefore, there is a need for improved methods and compositions for controlling bed bugs in homes and hotels.

[0006] It is often difficult to remove bed bugs from homes, in part because bed bugs can survive for up to a year without feeding. Repeated treatments of infested areas may be necessary. Traditionally, such treatments can include heating the room to 57°C (or 135°F) or 60°C (140°F) for 6-8 hours, frequent vacuuming, drying / washing clothing at high temperatures, and the use of various insecticides.

[0007] Bed bug infestations are a global problem, occurring in all habitable areas and especially in densely populated areas. Bed bug infestations are relatively common, especially since the 1990s. Possible contributing factors include significant increases in human travel and relocation rates, increased exchange of second-hand furniture such as mattresses and sofas, greater focus on controlling other more harmful pests, and increasing resistance to insecticides.

[0008] Bed bug control is critical to the hotel industry. According to a 2017 survey, 80% of hotels had treated for bed bugs in the previous year, and approximately 40% had treated for bed bugs in the previous month. Ongoing monitoring and treatment for bed bugs is routine and expensive. Hotels spend an average of $6,383 per bed bug incident. Common costs associated with bed bug infestations include replacement of soft goods, treatments, and lost business.

[0009] Additionally, almost half of all hotels have experienced litigation due to bed bug infestations, with the average cost per incident exceeding $17,000, and litigation and remediation costs for a single bed bug incident totaling approximately $240,000. Additionally, hotels treat bed bugs approximately seven times every five years on average.

[0010] While bed bug resistance to active ingredients is not a new phenomenon, reports of resistance to bed bug spray formulations are a disturbing development. The increasing number of reports of bed bug resistance to modern insecticide solutions only highlights the fact that products that can break bed bug resistance are urgently needed.

[0011] A variety of suspension concentrate products have been developed to control bed bugs, including MIKRON TM and These formulations have limited effectiveness against highly resistant strains of bed bugs.While active ingredient combination products have had varying degrees of success in the past, bed bugs have an inherent tendency to develop resistance to the active ingredients, even when used in combination.

[0012] The inventors have discovered that the methods and formulations described herein exhibit unexpected efficacy in controlling insects, including bed bugs that have become resistant to many existing treatments. Summary of the invention

[0013] The inventors of the present disclosure have discovered that the compositions and methods described herein exhibit surprising control of insects, including bed bugs.

[0014] In some embodiments, the present disclosure provides pesticidal compositions comprising:

[0015] (a) at least one active insecticidal ingredient and

[0016] (b) at least one carrier.

[0017] In some embodiments, the composition further comprises:

[0018] (c) at least one solvent and

[0019] (d) at least one surfactant.

[0020] In some embodiments, the present disclosure provides a method of controlling insects comprising applying to the insects, surface, or object to be treated a spreadable insecticidal composition comprising a composition disclosed herein.

[0021] In some embodiments, the present disclosure provides a method of controlling insects comprising applying a sprayable powder insecticidal composition comprising a composition disclosed herein diluted with water to the insects, surface or object to be treated.

[0022] In some embodiments, the present disclosure provides a method for preparing a sprayable insecticidal composition, the method comprising the following:

[0023] In the first step, an emulsifiable concentrate is prepared, the emulsifiable concentrate comprising:

[0024] (a) at least one surfactant;

[0025] (b) at least one solvent; and

[0026] (c) at least one active insecticidal ingredient; and

[0027] In the second step, at least one carrier is added to the emulsifiable concentrate and the carrier is suspended in the emulsifiable concentrate.

[0028] In some embodiments, the present disclosure provides a method for preparing a sprayable powder insecticide composition, the method comprising the following:

[0029] In the first step, an emulsifiable concentrate is prepared, the emulsifiable concentrate comprising:

[0030] (a) at least one surfactant;

[0031] (b) at least one solvent; and

[0032] (c) at least one active insecticidal ingredient; and

[0033] In a second step, at least one carrier is added to the emulsifiable concentrate and the carrier is suspended in the emulsifiable concentrate; and

[0034] In a third step, the emulsifiable concentrate is diluted in water or other solvent.

[0035] In some embodiments, the active ingredient is a sodium channel blocker.

[0036] In some embodiments, the active ingredient is a nicotinic receptor agonist.

[0037] In some embodiments, the pesticidal compositions include a combination of one or more sodium channel blockers.

[0038] In some embodiments, the pesticidal compositions include a combination of one or more nicotinic receptor agonists.

[0039] In some embodiments, pesticidal compositions include a combination of one or more sodium channel blockers and one or more nicotinic receptor agonists.

[0040] In some embodiments, the carrier is an inert carrier that has been shown to have insecticidal activity, ie, dry properties, abrasive properties, thermal properties, etc.

[0041] In some embodiments, the pesticidal composition is micronized or solubilized onto carrier particles. DETAILED DESCRIPTION

[0042] The inventors of the present disclosure have discovered that the compositions and methods described herein exhibit surprising control of insects, including bed bugs.

[0043] Bed bugs have an inherent tendency to develop resistance to active ingredients (ai), even when used in combination. However, bed bugs have not yet developed significant resistance to physical modes of action such as heat, drying and / or abrasion. Therefore, the present invention represents a positive response to the growing threat of bed bug resistance in the pest control industry.

[0044] The industry has also developed spreadable formulations to combat resistant bed bugs through various modes of action, such as the drying properties of silica aerogels (e.g., CimeXa) or the abrasive properties of diatomaceous earth. These currently available spreadable formulations have some efficacy against resistant bed bugs due to their alternative modes of action (e.g., disrupting the bed bug cuticle by physical means rather than physiological effects on the nervous system), but lack the "kill speed" desired with traditional suspension concentrate formulations.

[0045] For example, the inventors of the present disclosure have discovered that dustable powder insecticide formulations differ in bioavailability, and therefore in efficacy, from conventional insecticidal suspension concentrate formulations. In addition, while insecticidal powders are generally highly effective against insects, the application of such powders has traditionally been a labor-intensive process involving hand sprayers that require pest control operators to crawl under hard-to-reach areas to apply the product. Conventional spray products, on the other hand, are easy to apply but lack the bioavailability and residual properties of conventional powder products.

[0046] The inventors of the present disclosure have discovered that, in certain embodiments, combining a dustable powder with a suspension concentrate can achieve improved bed bug control relative to existing compositions and methods. Incorporating an insecticidal powder into an emulsifiable concentrate sprayable product increases the accessibility of the powder application over traditional spray services. The present invention also allows for liquid spray application of the insecticidal powder, which is significantly less labor intensive than traditional powder application. Additionally, liquid spray deposition allows for uniform distribution of the product on a surface relative to the distribution of a powder on a surface.

[0047] Thus, the inventors have discovered that the dustable powder compositions described herein and methods of using and applying the powder compositions exhibit surprisingly improved control of insects including bed bugs relative to existing compositions and methods. The described invention bridges the gap between traditional spray products and traditional powder products.

[0048] The compositions and methods of the invention described herein have multiple modes of action to overcome the resistance exhibited by certain strains of particular pests, such as bed bugs.

[0049] In some embodiments, the present disclosure provides pesticidal compositions comprising: (a) at least one active pesticidal ingredient and (b) at least one carrier.

[0050] In some embodiments, the composition further comprises: (c) at least one solvent and (d) at least one surfactant.

[0051] In certain embodiments, the compositions of the present invention include a solubilized active ingredient incorporated into a micronized carrier.

[0052] In one aspect, one or more insecticidal powders are incorporated into the compositions of the present invention to increase the bioavailability of the carrier on the microporous substrate and to provide prolonged residual efficacy since any insect that passes through the insecticidal powder is exposed to both the insecticidal carrier and the solubilized or suspended active ingredient.

[0053] In addition, in one aspect, the carrier may also increase efficacy because the carrier itself possesses insecticidal properties with different modes of action, such as drying properties that dry out the insects by absorbing the waxy cuticle, or abrasive properties, or thermal properties. It has been surprisingly found that active ingredients that have insecticidal properties themselves can overcome bed bug resistance when used with such carriers. In one aspect, the active ingredient is micronized or solubilized onto carrier particles.

[0054] Furthermore, in one aspect, the compositions described herein exhibit enhanced persistence, surface compatibility, and surface bioavailability for all active ingredients included therein.

[0055] When combined, the carrier and active ingredient can have unexpected effects, such as the carrier absorbing the insect's waxy cuticle (which normally acts as a barrier to entry of sprayed active ingredients), thereby allowing the active ingredient to more easily penetrate the insect's hemolymph, etc. The combined effect is twofold: degradation of the insect's cuticle and penetration of the active ingredient into the body.

[0056] On the one hand, simple aqueous tank mixing of carrier and active ingredient is not enough for simultaneous degradation and penetration. In the present invention, the active ingredient is micronized or solubilized on the carrier particles, so as to achieve simultaneous degradation and penetration of the carrier and active ingredient into insects at each contact point. By combining one or more active ingredients with a carrier so that the active ingredient is micronized or solubilized on the carrier particles such as silica carriers, improved insecticidal efficacy is achieved. In contrast, formulations in which both active ingredient and silica are micronized into traditional suspension concentrates will not deliver the same efficacy, because silica will no longer be used as a carrier for active ingredients; bed bugs or other insects / pests will interact with silica and active substances at different contact points in such traditional suspension concentrates. However, the composition of the present invention achieves a true combination, so that silica and active ingredients are contacted with target pests at the same time.

[0057] In certain embodiments, the compositions of the present invention include a solid carrier that does not contain a liquid component. On the one hand, such embodiments can be spread or otherwise dispersed without the use of a spray, thereby eliminating the need for incorporation into a liquid. In certain embodiments, the compositions described herein are powder formulations.

[0058] The composition can be a concentrate or a ready-to-use composition. A concentrate refers to a composition that is diluted to form a ready-to-use composition. A ready-to-use composition refers to a composition that is applied to a target. A concentrated composition can be diluted prior to use, for example, in a ratio of 1:2, 1:3, 1:4, 1:5, 1:10, 1:20, 1:50, 1:99 or any other ratio that produces an effective amount of the active ingredient (pheromone ingredient and / or insecticide) in the diluted solution.

[0059] In certain embodiments, the compositions of the present invention are formulated as aqueous silica suspension formulations.

[0060] In certain embodiments, the composition of the present invention includes a solid carrier incorporated into a liquid that can be sprayed. Incorporation into a liquid will retain the beneficial properties of the composition described herein (i.e., improved surface bioavailability, surface compatibility, and residual properties). Incorporation into a sprayable liquid formulation will further allow for more modes of use, more specific dosages, and support a wider range of application ratios.

[0061] In certain embodiments, the compositions described herein are suspension concentrate formulations.

[0062] In certain embodiments, the compositions described herein are carrier-based suspension concentrate formulations.

[0063] In one aspect, the inert carrier is selected to be insecticidal due to drying, grinding or heating.

[0064] In certain embodiments, the support is silica or any silica-based or silica-derived support.

[0065] Suitable solid carriers are, for example, ground natural minerals such as kaolin, clay, talc, chalk, quartz, attapulgite, montmorillonite or diatomaceous earth; and ground synthetic minerals such as finely divided silicon dioxide, alumina and silicates. Suitable fine-grained solid carriers are, for example, crushed and fractionated natural rocks such as calcite, pumice, marble, sepiolite and dolomite; and synthetic fine particles of inorganic and organic diets; and fine particles of organic materials such as sawdust, coconut shells, corn cobs and tobacco stalks.

[0066] In certain embodiments, whether or not the carrier is incorporated into the liquid component, the carrier is silica aerogel, amorphous silica, microporous silica, talc, diatomaceous earth, clay, defatted or dehydrated corn grits, calcium carbonate, hydrated aluminum silicate (kaolinite), and / or gypsum.

[0067] In one aspect, any solvent and surfactant can be used to prepare the composition according to the present invention.

[0068] In one aspect, any solvent may be used to incorporate the solid components into the sprayable formulation.

[0069] In certain embodiments, the solvent is a low volatility organic solvent that is immiscible with water.

[0070] In certain embodiments, the solvent is N,N-dimethyl(octanamide / decanamide).

[0071] In other embodiments, the solvent is 1-octyl-2-pyrrolidone, benzyl acetate, benzyl benzoate, 2-ethylhexyl lactate, dibutyl isosorbide, cyclohexanone, propylene glycol phenyl ether, and combinations and / or derivatives thereof.

[0072] In certain embodiments, the solvent is a nonionic and anionic emulsifier, such as polyoxyethylene fatty acid esters, polyoxyethylene fatty alcohol ethers, such as alkyl aryl polyglycol ethers, alkyl sulfonates, alkyl sulfates, aryl sulfonates and protein hydrolysates. As dispersants, for example, lignin sulfite waste liquor and methylcellulose are suitable.

[0073] On the one hand, surfactants can be used to help the solubility of the composition or composition components, and improve the uniformity of the composition. Surfactants can also be used to reduce surface tension and help the application of the composition, such as by spraying. Suitable surfactants include, for example, nonionic, cationic, anionic, zwitterionic (amphoteric) or semi-polar nonionic surfactants and combinations thereof. Exemplary emulsifiers include esters of fatty carboxylic acids, fatty carboxylates and fatty carboxylic acids, such as polyglycerol oleate, polyglycerol stearate or lecithin. Surfactants can be selected based on the intended use of the composition. For example, surfactants can be incorporated into the composition to improve the solubility of active ingredients, form emulsions, improve wettability or other similar purposes. The composition can include about 0-20wt-% of surfactants or about 0.5-15wt-% of surfactants. For example, suitable surfactants include, but are not limited to, polyoxyethylene and / or polyoxypropylene of sorbitol oleate, block copolymers of polyoxyethylene and polyoxypropylene, ethoxylated tristyrylphenol / propoxylated tristyrylphenol, polyoxyethylene castor oil, alkoxylated phosphates and combinations and / or derivatives thereof.

[0074] In one aspect, any insecticidal active ingredient can be used according to the present invention. Suitable active ingredients include:

[0075] Pyrethroid compounds, such as dd-T-cypermethrin, acralthrin, permethrin, phenothrin, d-phenothrin, allethrin, d-allethrin, dd-allethrin, pyrethrin, prallethrin, cypermethrin, flucythrin, beta-cypermethrin, bifenthrin, cypermethrin, flucythrin, lambda-cypermethrin, gamma-cypermethrin, cypermethrin, sigma-cypermethrin, alpha-cypermethrin, zeta-cypermethrin, fenfluthrin, fenthrin, deltamethrin, cypermethrin, tefluthrin, cypermethrin, esfenvalerate, flucythrinate, trifluthrin, flumethrin, fluvalinate, t-fluvalinate, profluthrin, benzylthrin, imiprothrin, transfluthrin, resmethrin, d-resmethrin, silafluthrin, tralomethrin, tetramethrin, d-tetramethrin, ethynethrin, metofluthrin, cypermethrin, transfluthrin or etofenprox;

[0076] Organophosphorus compounds, such as acephate, butathiofos, chlorethoxyfos, chlorfenvinphos, chlorpyrifos, chlorpyrifos-methyl, cyanophos, diazinon, bis(2-chloroisopropyl) ether (DCIP), dichlofenthion, dichlorvos, dimethoate, dimethylvinphos, disulfoton, o-ethyl-o-(4-nitrophenyl)phenyl thiophosphate (EPN), ethion, ethoprophos, etrimfos, fenthion, fenitrothion, fosthiazate, formothion, isoflavone sofenphos), isoxathion, malathion, mesulfenfos, methidathion, monocrotophos, naled, parathion, phosalone, phosmet, pirimiphos-methyl, pyridaphenthion, quinalphos, phenthoate, profenofos, propaphos, prothiofos, pyraclofos, salithion, sulprofos, temefos, terbufos, trichlorfon or cadusafos;

[0077] N-phenylpyrazole compounds, such as fipronil;

[0078] Carbamate compounds, such as propoxur, alanycarb, benfuracarb, Bassa (BPMC), carbaryl, carbofuran, carbosulfan, cloethocarb, ethiofencarb, fenobucarb, methomyl, methiocarb, carbaryl (NAC), oxamyl, pirimicarb, xylyl 3,5-methylcarbamate (XMC), thiodicarb, xylycarb or aldicarb;

[0079] Oxadiazole compounds, such as metoxadiazone;

[0080] Neonicotinoid compounds, such as imidacloprid, clothianidin, thiamethoxam, dinotefuran, acetamiprid, nitenpyram or thiacloprid;

[0081] insect growth regulators, such as pyriproxyfen, methoprene, hydroplane, fenoxycarb, etoxazole, chlorfluazuron, triazuron, novaluron, hexaflumuron, difhibenzuron, cyromazine, flufenoxuron, teflubenzuron, triflumuron or lufenuron;

[0082] Macrolide compounds, such as milbemycin, abamectin or ivermectin; and

[0083] Diamide compounds, such as chlorantraniliprole, cyantraniliprole, cyclaniliprole, tetraniliprole, flubendiamide or cyhalodiamide.

[0084] In certain embodiments, the active ingredient is a sodium channel blocker.

[0085] In certain embodiments, the active ingredient is a pyrethroid.

[0086] In certain embodiments, the active ingredient is alpha-cypermethrin, cyhalothrin, beta-cyhalothrin, esfenvalerate, phenothrin, cyhalothrin, gamma-cyhalothrin, lambda-cyhalothrin, bifenthrin, or a combination thereof.

[0087] In certain embodiments, the active ingredient is a nicotinic receptor agonist.

[0088] In certain embodiments, the active ingredient is a neonicotinoid such as imidacloprid, thiamethoxam, acetamiprid, nitenpyram, thiacloprid, flupyralidone, dinotefuran, clothianidin, or a combination thereof.

[0089] In certain embodiments, the compositions described herein include a combination of two or more active ingredients.

[0090] In certain embodiments, the composition of the present invention includes sodium channel blockers and nicotinic receptor agonists as active ingredients. On the one hand, the sodium channel blocker is a pyrethroid, and the nicotinic receptor agonist is a neonicotinoid. In certain embodiments, the sodium channel blocker is alpha-cypermethrin, cyhalothrin, beta-cyhalothrin, esfenvalerate, phenothrin, cyhalothrin, gamma-cyhalothrin, lambda-cyhalothrin, bifenthrin or its combination. In certain embodiments, the nicotinic receptor agonist is imidacloprid, thiamethoxam, flupyr, dinotefuran, clothianidin or its combination.

[0091] On the one hand, the amount, concentration and application rate of sodium channel blocker or nicotinic receptor agonist and the total amount of the composition to be used depend on the specific insect pest strain and the occurrence of the pest. The optimal ratio and total ratio used can be determined for each application through a test series.

[0092] In one aspect, the composition of the present invention comprises a concentration of 0.0001 mg / m 2 To 1000mg / m 2 , or 0.0005mg / m 2 Up to 500 mg / m 2, or 0.001mg / m 2 Up to 250 mg / m 2 , or 0.005 mg / m 2 Up to 100 mg / m 2 Sodium channel blockers.

[0093] In one aspect, the composition of the present invention comprises a concentration of 0.0001 mg / m 2 To 1000mg / m 2 , or 0.0005mg / m 2 Up to 500 mg / m 2 , or 0.001mg / m 2 Up to 250 mg / m 2 , or 0.005 mg / m 2 Up to 100 mg / m 2 Nicotinic receptor agonists.

[0094] In one aspect, the compositions of the invention comprising a sodium channel blocker ("SCB") and a nicotinic receptor agonist ("NRA") comprise the SCB and NRA in a ratio of 1:200 to 200:1, or 1:100 to 100:1, or 1:50 to 50:1, or 1:25 to 25:1, or 1:10 to 10:1.

[0095] In one aspect, the present disclosure provides a method of preventing or controlling insects or pests, the method comprising applying a composition as discussed herein to the insect, surface or object to be treated.

[0096] In one aspect, according to the methods of the present invention, the composition described herein is administered at 0.0001 mg / m 2 To 1000mg / m 2 , or 0.0005mg / m 2 Up to 500 mg / m 2 , or 0.001mg / m 2 Up to 250 mg / m 2 , or 0.005 mg / m 2 Up to 100 mg / m 2 The application rate is applied to a surface or other area.

[0097] The combination of pyrethroids and nicotinic receptor agonists achieves effective insecticidal activity because nicotinic receptor agonists increase sodium channel opening, thereby increasing the uptake of molecules that act on sodium channels. Previous products combined pyrethroid and neonicotinoid active ingredients in formulations that suspended micronized active ingredients. However, these combination products did not overcome all forms of resistance seen in selected bed bug strains. The compositions of the present invention differ in that, in certain embodiments, one or more solubilized active ingredients are combined with an inert carrier.

[0098] The formulations described herein can be sprinkled or sprayed onto surfaces. If sprayed, the liquid application dries, leaving behind an insecticide powder residue. Insecticide powders are known for their excellent residual efficacy.

[0099] Heretofore, the incorporation of dusts into spray products has not been seen in the pest control industry for the control of insects such as bed bugs. Furthermore, specific combinations of carrier dusts such as silica dusts and active ingredients can result in resistance breaking behavior not otherwise seen from dusts or AIs alone.

[0100] In certain embodiments, the compositions of the invention include active ingredients in addition to the sodium channel blocker and / or nicotinic receptor agonist.In one aspect, any additional insecticidal or biocidal active ingredients may be present in the composition.

[0101] In certain embodiments, the composition of the present invention further comprises one or more active ingredients as active ingredients, and the one or more active ingredients are selected from diamide / pyridylpyrazole, bromofenac, chlorantraniliprole, cyantraniliprole, flucyantraniliprole, isoxazoline, afoxalaner, fluralaner, fluxametamide, oxadiazine / semicarbazone, indoxacarb and metaflumizone.

[0102] In certain embodiments, the composition of the present invention may be formulated as a suspoemulsion together with an emulsifier.

[0103] The present disclosure further provides a method of preparing a sprayable powder formulation of the composition described herein.The order and method of combination are important to the performance of the final product.

[0104] In one aspect, to prepare certain embodiments of the present invention, a conventional emulsifiable concentrate is first prepared, which includes a solvent, a surfactant, and an active ingredient. In one aspect, a mixer can be used.

[0105] Next, the carrier is added and incorporated into the emulsifiable concentrate under moderate to high shear. Over time, the emulsifiable concentrate is completely absorbed into the carrier. In one aspect, a high shear mixer can be used.

[0106] Next, the carrier is suspended into the emulsifiable concentrate. In one aspect, a high shear mixer can be used.

[0107] In one aspect, the support particles used to prepare the compositions of the present invention, such as silica particles, can have any particle size and any pore diameter.

[0108] In one aspect, conventional production methods can be used to prepare the emulsifiable concentrates, which conventional production methods include mixing one or more solvents, one or more surfactants, and one or more active ingredients.

[0109] To prepare a sprayable formulation, a final dilution is carried out in water or other sprayable solvent. After dilution with water into the spray tank, the emulsifiable concentrate forms an emulsion in water. Since the adsorption / desorption kinetics take a long time, the carrier remains suspended into the spray tank and almost no emulsifiable concentrate is desorbed from the silica aerogel. Such adsorption / desorption times depend on properties such as the pore size of the carrier, the steric volume of the surfactant used and the binding coefficient between the emulsifiable concentrate solvent and the carrier.

[0110] In one aspect, any pest or insect can be controlled by the compositions and / or methods taught herein.Some embodiments of the present invention can be used to control pests such as arthropods, including insects and arachnids.Exemplary pests include arthropods such as insects, spiders, lipopods and millipedes, bed bugs, German cockroaches (Blattella germanica), smoke cockroaches (Periplaneta fuliginosa), American cockroaches (Periplaneta americana), cat fleas (Ctenocephalides felis), fire ants (Solenopsis Invicta), black carpenter ants (Camponotus pennsylvanicus), pavement ants (Tetramorium caespitum), field ants (Formica sp.), moisture ants (Lasius sp.), wood ants (Formica rufa), common housefly (Musca domestica), vomiting blowfly (Lucilia sericata), sericata), silverfish (Ctenolepisma longicaudata), house silverfish (Thermobia domestica), bean aphid (Aphis fabae), pea aphid (Acyrthosiphon pisum), termites (Reticulitermes flavipes), grain weevils (Sitophilus granarius), corn weevils (Sitophilus zeamais), flour beetles (Tribolium confusum), rusty flour beetles (Cryptolestes ferrugineus), dust mites (Dermatophagoides farinae), millipedes (Cylindroiulus caeruleocinctus), lipped centipedes (Strigamia aluminata), woodlice (Oniscusasellus), oribatid mites (Haplozetes sp.), house crickets (Acheta domestica), black widow spiders (Latrodectus mactans), brown recluse spiders (Loxoscelesreclusa), and pharaoh ants (Monomorium pharaonis). Exemplary pests include arthropod eggs, including bed bug eggs and cockroach eggs.Other exemplary pests may include but are not limited to whiteflies, mosquitoes, flies of other kinds, aphids of other kinds, borers of other kinds, lice, stink bugs, moths, beetles, web bugs, whiteflies, peach aphids, western flower thrips, diamondback moths, leaf miners, grasshoppers, crickets, locusts, leafhoppers, rice planthoppers, psyllids, scale insects, chironomids, fruit flies, earworms, borers, armyworms, heartworms, hawk moth larvae, milkweed stink bugs, mealybugs, weevils, horseflies, gadflies, sawflies, rice bugs, stink bugs with spotted shields, vegetable worms, corn borers, horn flies, green-headed flies, pillbugs, dung bugs, dust mites, lippedias and millipedes. Exemplary pests also include arachnids, which include cellar spiders, ticks, black widow spiders and brown recluse spiders. Possible pests also include but are not limited to scorpions and spiders of other kinds. The present disclosure is intended to encompass uses against all of the foregoing, as well as uses against other pests, including other insects and arachnids, and other organisms including fungi, bacteria, viruses, and nematodes.

[0111] In some embodiments, the pesticidal compositions described herein effectively kill and / or control pests and / or prevent or reduce egg laying and / or prevent or reduce the emergence of pest eggs. In some embodiments, the pesticidal compositions described herein exhibit effective knockdown insecticidal activity, exhibit effective dry residual insecticidal activity, and / or exhibit effective extended residual insecticidal activity.

[0112] Some embodiments of the present invention can be used to control pests that affect humans and non-human mammals, including bed bugs, cockroaches, lice, fleas, ticks, mites, and scabies. Some embodiments of the present invention can be used to control pests that affect plants or agriculture, such as aphids or nematodes.

[0113] In certain embodiments, the insects controlled by the compositions and / or methods taught herein are bed bugs.

[0114] As used herein with respect to insects, and particularly with respect to bed bugs, the term "control" refers to the ability to kill and / or repel insects and / or bed bugs.

[0115] In another aspect, bed bugs controlled by the compositions and / or methods taught herein include, but are not limited to, insects belonging to the Cimex genus.

[0116] In yet another aspect, bed bugs controlled by the compositions and / or methods taught herein include, but are not limited to, Cimex lectularius and Cimex hemipterus species.

[0117] The active compound combinations according to the invention may comprise further components, for example further active compounds of different types (e.g. other insecticides, antimicrobial compounds, fungicides, herbicides, etc.) and / or additives and / or formulation auxiliaries customary in crop protection, or may be used together with these compounds.

[0118] In one aspect, the compositions according to the present invention may include one or more biocides. In one aspect, any commercially available biocide may be used. For example, PROXEL provided by Arch Chemical TM GXL (20%) (see excelind.co.in / Excel_Chemical / download / Proxel_GXL_literature.pdf), and KATHON TM CG / ICP is provided by DuPont (see dupont.com / products / kathoncgicp.html).

[0119] The formulations disclosed herein may optionally include one or more additional compounds that provide additional beneficial or otherwise useful effects. Such compounds include, but are not limited to, binders, surfactants, solvents, wetting agents, emulsifiers, carriers, adjuvants, diluents, dispersants, insecticides, pesticides, fungicides, fertilizers with micronutrient or macronutrient properties, herbicides, feeding inhibitors, insect molting inhibitors, insect mating inhibitors, insect maturation inhibitors, nematicides, nutritional or horticultural supplements, or any combination thereof.

[0120] In one aspect, the suspension formulation according to the present invention may include one or more wetting agents or dispersants. In one aspect, any commercially available wetting agent or dispersant may be used.

[0121] The present disclosure further provides methods of making and using the sprinkleable formulations of the present invention.

[0122] The present disclosure further provides methods of making and using the suspension formulations of the present invention.

[0123] In certain embodiments, the active ingredient is micronized or solubilized in a carrier.

[0124] In certain embodiments, the active ingredient is micronized or solubilized in a liquid solution.

[0125] In certain embodiments, the active ingredient is micronized or solubilized in a carrier and a liquid solution.

[0126] In one aspect, the compositions of the present invention may further include or otherwise incorporate other powders. In another aspect, such additional powders may be incorporated or otherwise incorporated in the form of free micronized active ingredients, with or without carrier solubilization. In yet another aspect, other embodiments may comprise a combination of micronized and solubilized active ingredients and carriers.

[0127] These formulations are produced in any desired or known manner, for example by mixing the active compound with extenders such as liquid solvents, pressurized liquefied gas and / or solid carriers, optionally using surfactants such as emulsifiers and / or dispersants and / or foam forming agents. If the extender used is water, it is also useful to use, for example, an organic solvent as a cosolvent. Suitable liquid solvents include, but are not limited to: aromatic hydrocarbons such as xylene, toluene or alkylnaphthalene, chlorinated aromatic hydrocarbons or chlorinated aliphatic hydrocarbons such as chlorobenzene, vinyl chloride or methylene dichloride, aliphatic hydrocarbons such as cyclohexane or paraffin, for example mineral oil fractions, alcohols such as butanols or ethylene glycol and their ethers and esters, ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone, strong polar solvents such as dimethyl formamide and dimethyl sulfoxide and water. Liquefied gaseous extenders or carriers are included in those liquids that are gaseous at ambient temperature and atmospheric pressure, for example aerosol propellants such as halogenated hydrocarbons and butane, propane, nitrogen and carbonic acid gas. As solid carrier, there are suitable: for example, natural minerals such as kaolin, clay, talc, chalk, quartz, attapulgite, montmorillonite or diatomaceous earth ground; and synthetic minerals such as finely divided silicon dioxide, alumina and silicate ground. As fine-grained solid carrier, there are suitable: for example, natural rocks such as calcite, pumice, marble, sepiolite and dolomite crushed and fractionated; and synthetic fine particles of inorganic and organic diets; and fine particles of organic materials such as sawdust, coconut shells, corn cobs and tobacco rods. As emulsifiers and / or foam formers, there are suitable: for example, nonionic and anionic emulsifiers, such as polyoxyethylene fatty acid esters, polyoxyethylene fatty alcohol ethers, such as alkylaryl polyglycol ethers, alkyl sulfonates, alkyl sulfates, aryl sulfonates and protein hydrolyzates. As dispersants, for example, lignin sulfite waste liquor and methylcellulose are suitable.

[0128] Viscosifiers such as carboxymethylcellulose and natural and synthetic polymers in the form of powders, granules or latexes, such as gum arabic, polyvinyl alcohol and polyvinyl acetate, and natural phospholipids such as cephalin and lecithin and synthetic phospholipids can be used in the formulation. Other possible additives are mineral oils and vegetable oils.

[0129] Colorants such as inorganic pigments, for example, iron oxide, titanium oxide and Prussian blue, and organic dyes such as alizarin dyes, azo dyes and metal phthalocyanine dyes, and trace nutrients such as iron salts, manganese salts, boron salts, copper salts, cobalt salts, molybdenum salts and zinc salts can also be used.

[0130] The active compound combination according to the invention may comprise further components, for example further active compounds of different types (e.g. other insecticides, antimicrobial compounds, fungicides, herbicides, etc.) and / or additives and / or formulation auxiliaries customary in crop protection, or may be used together with these compounds. However, the active compound combination according to the invention does not include piperonyl butoxide (PBO).

[0131] These formulations are produced in a known manner, for example by mixing the active compound / active compound combination with extenders, i.e. liquid solvents and / or solid carriers, optionally using surfactants, i.e. emulsifiers and / or dispersants, auxiliaries, i.e. substances which improve the biological properties without having their own biological activity, defoamers, preservatives, antioxidants, colorants, antifreeze agents, pH stabilizers, thickeners and / or foam formers.

[0132] Alternatively, in another embodiment of the invention, the active compound combination is used to control bed bugs by ovicidal activity. For this purpose, the active compound combination of the invention is applied (e.g., sprayed or sprinkled) directly on the bed bugs and eggs (e.g., on the box spring, box spring mattress, and the inside of the bed frame or headboard, including all cracks and joints).

[0133] Also suitable as optional auxiliaries are substances which are suitable for imparting specific properties, such as certain technical properties and / or specific biological properties, to the active compound / active compound combination itself and / or to preparations derived therefrom (e.g. spray liquors, seed dressings). Typical suitable auxiliaries are: extenders, solvents and carriers.

[0134] Suitable extenders are, for example, water, polar and nonpolar organic chemical liquids, for example from the following classes: aromatic and nonaromatic hydrocarbons (such as paraffins, alkylbenzenes, alkylnaphthalenes, chlorobenzenes), alcohols and polyols (which, if appropriate, may also be substituted, etherified and / or esterified), ketones (such as acetone, cyclohexanone), esters (including fats and oils) and (poly)ethers, unsubstituted and substituted amines, amides, lactams (such as N-alkylpyrrolidones) and lactones, sulfones and sulfoxides (such as dimethyl sulfoxide).

[0135] If the extender used is water, it is also possible to use, for example, organic solvents as auxiliary solvents. Suitable liquid solvents are, in essence, aromatic hydrocarbons such as xylene, toluene or alkylnaphthalenes, chlorinated aromatic hydrocarbons and chlorinated aliphatic hydrocarbons such as chlorobenzene, vinyl chloride or methylene chloride, aliphatic hydrocarbons such as cyclohexane or paraffins, for example petroleum fractions, mineral oils and vegetable oils, alcohols such as butanol or ethylene glycol and their ethers and esters, ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone, strongly polar solvents such as dimethylformamide and dimethyl sulfoxide and water.

[0136] Suitable solid carriers are: for example, ammonium salts and ground natural minerals such as kaolin, clay, talc, chalk, quartz, attapulgite, montmorillonite or diatomaceous earth; and ground synthetic minerals such as finely divided silicon dioxide, aluminum oxide and silicates; suitable solid carriers of fine particles are: for example, crushed and fractionated natural rocks such as calcite, marble, pumice, sepiolite and dolomite; and synthetic fine particles of inorganic and organic diets; and fine particles of organic materials such as paper, sawdust, coconut shells, corn cobs and tobacco stems; suitable emulsifiers and / or foaming agents are: for example, nonionic and anionic emulsifiers, such as polyoxyethylene fatty acid esters, polyoxyethylene Alkenyl fatty alcohol ethers, such as alkylaryl polyglycol ethers, alkyl sulfonates, alkyl sulfates, aryl sulfonates and protein hydrolysates; Suitable dispersants are nonionic and / or ionic substances, for example from the following categories: alcohol-POE- and / or-POP-ethers, acids and / or POP-POE esters, alkylaryl and / or POP-POE ethers, fat- and / or POP-POE adducts, POE- and / or POP-polyol derivatives, POE- and / or POP-sorbitol or sugar adducts, alkyl or aryl sulfates, alkyl or aryl sulfonates and alkyl or aryl phosphates or corresponding PO-ether adducts. In addition, suitable oligomers or polymers, such as those derived from vinyl monomers, acrylic acid, EO and / or PO alone or in combination with, for example, (poly) alcohols or (poly) amines. Lignin and its sulfonic acid derivatives, unmodified and modified cellulose, aromatic and / or aliphatic sulfonic acids and their adducts with formaldehyde can also be used.

[0137] The compositions described herein can be applied directly to the site of insect infestation or directly to the insects themselves.

[0138] The compositions described herein can be applied directly to a site or area as a preventative treatment. For example, the compositions described herein can be applied to kill insects that cross or otherwise pass through the treated area.

[0139] The disclosed compositions can be used on a variety of surfaces and in a variety of locations. In one aspect, the formulations described herein can be applied directly to walls, surfaces, floors, carpets, mattresses, clothing, luggage or to sheets, pillows, and other bedding. For example, the disclosed compositions can be used to treat surfaces, textiles, furniture, and structures, including mattresses, box springs, beds, bed frames, cushions, chairs, sofas, seats, and other upholstered furniture, compartments; textiles, carpets, blankets, clothing, and toys; closets, dressers, cabinets, drawers, tables, etc.; personal items, books, electronic products, photo frames, etc.; cracks and crevices between floors, behind baseboards, headboards, furniture, and wallpaper. For example, the composition can be used in residential and lodging structures (e.g., homes, multi-family dwellings, dormitories, hotels, motels, hostels, etc.), food service facilities (e.g., restaurants, cafes, cafeterias, canteens, etc.), offices, government buildings, military installations, vehicles (e.g., buses, trains, airplanes, automobiles, etc.), vessels (e.g., boats, submarines, cruise ships, ships, ferries, etc.), shelters, recreational facilities (e.g., theaters, movie theaters, casinos, etc.), or in patient rooms and common areas of healthcare and long-term care facilities. The composition can be used to treat the entrance of a building, around a drive-in window, pavement near a drive-in window, or concrete or trash cans outside a building. In general, the composition can be used in any location where people live, or where items can be placed and where bed bugs may have an opportunity to transfer from a person or his / her items to the surrounding environment.

[0140] In one aspect, the compositions described herein can be applied in a single application step. In another aspect, the compositions described herein can be applied in multiple application steps, e.g., two, three, four, five or more application steps. In another aspect, the second, third, fourth or fifth or more application steps can use the same or different formulations. The methods described herein also provide aspects that exclude multiple application steps.

[0141] The formulations described herein can be applied to the insect or part or object to be treated at one or more application intervals of about 15 minutes, 30 minutes, about 1 hour, about 2 hours, about 6 hours, about 8 hours, about 12 hours, about 1 day, about 5 days, about 7 days, about 10 days, about 12 days, about 14 days, about 21 days, about 28 days, about 35 days, about 40 days, about 45 days, about 50 days, or about 56 days.

[0142] After the insects are observed to be killed, repelled or otherwise controlled, the formulations described herein can be applied to the insects or parts or objects to be treated. Alternatively, the compositions described herein are applied to the parts or objects to be treated before any insects are observed as a preventive measure to kill, repel or otherwise control insects that have not yet been identified.

[0143] Further embodiments of the invention relate to the use of the compositions and / or materials described above to control animal pests, preferably arthropods, preferably insects, and more preferably bed bugs, including insecticide-resistant bed bugs and bed bugs resistant to target sites and / or metabolism. In another preferred embodiment, the invention relates to the use of such materials to control pyrethroid and / or carbamate-resistant mosquitoes, preferably pyrethroid and / or carbamate-resistant Anopheles gambiae and / or Anopheles funestus mosquitos. In one aspect, the compositions and materials of the invention are used to control pyrethroid-resistant insects. Another preferred embodiment of the invention relates to the use of such materials to control multi-resistant mosquitoes.

[0144] In another embodiment of the invention, the active compound composition of the invention is used to control insecticide-resistant insects, in one aspect insecticide-resistant bed bugs. The term "insecticide resistance" is a term used to describe target insects or bed bugs that are no longer killed by standard doses of insecticides (i.e., they are no longer sensitive to the insecticide and try to avoid contact with the insecticide). (See 1.2.; page 27; "Global Plan for Insecticide Resistance Management", WHO 2012).

[0145] In one aspect, certain embodiments of the present invention also relate to using the compositions and / or materials described above to control pyrethroid-resistant bed bugs. In one embodiment, the materials are used to control pyrethroid-resistant bed bugs, wherein the bed bugs have a valine to leucine mutation (V419L) and / or a leucine to isoleucine mutation (L925I) in the voltage-gated sodium channel α-subunit gene.

[0146] On the one hand, the formulations described herein are combined with talc and / or graphite. On the one hand, the compositions or methods described herein do not include talc. On the other hand, the formulations or methods described herein do not include graphite or graphite blends. On the other hand, the formulations or methods described herein do not include a blend of graphite and / or talc. On the other hand, the formulations or methods described herein contain trace amounts of talc or graphite. On the other hand, the formulations or methods described herein contain less than about 5% by weight, less than about 10% by weight, less than about 20% by weight, less than about 20% by weight, less than about 30% by weight, less than about 40% by weight, or less than about 50% by weight of talc, graphite, or a combination of talc or graphite.

[0147] In yet another aspect, the formulations described herein can be blended with inert materials to improve handling or packaging, such as silicon dioxide, starches (natural and derived), clays, and other minerals.

[0148] Examples

[0149] The following examples are used to illustrate certain aspects of the present disclosure and are not intended to limit the present disclosure.

[0150] Example 1: Testing on cockroaches

[0151] An emulsifiable concentrate (EC) was used as a template to illustrate the improvements of the present invention. A comparative EC (hereinafter referred to as "powder-free") was created in a standard manner, where solvent, surfactant, active ingredient and other inert materials were added to a container and homogenized by simple mixing.

[0152] A second EC was also formulated that mirrored the creation of the first EC. However this EC had amorphous silicon dioxide and a suspending agent added in a final step to obtain a liquid powder formulation according to the invention.

[0153] Table 1.

[0154]

[0155]

[0156] Figure 1 The residual insecticidal activity difference of the liquid powder formulation and the comparative formulation not containing the powder as described in Table 1 is shown. 2 ) was sprayed on the wood surface, allowed to dry completely, and then German cockroaches were placed on the surface for 4 hours, after which they were removed from the treated surface and placed in a clean container for monitoring. It was seen that the liquid powder formulation according to the present invention generally maintained its advantage over the control formulation containing no powder at 1 day after application (daa) and 7 and 14 days after application.

[0157] Experiment 2: (Testing on bed bugs)

[0158] There is no pre-existing formulation type to which the present invention will belong. In one container, flupyralidone, beta-cyfluthrin and citric acid are dissolved in benzyl acetate. This solution is then adsorbed into amorphous silica. To this silica, polyalkylene oxide-modified heptamethyl trisiloxane is added. In a separate container, the total amount of water is added. Then surfactants, biocides and defoamers are added thereto, just as the SC is constructed. Then silica is added to this mixture using a homogenizer with medium shear. Once fully dispersed, glycerol and xanthan gum are added to stabilize the solution. The weight ratios (% w / w) used are described in Table 2.

[0159] Table 2.

[0160]

[0161]

[0162] like Figure 2 As shown, liquid powder formulation (30 mg ai / m 2 , β-cyfluthrin + imidacloprid) were sprayed directly against a susceptible bed bug strain (referred to as the MANDA strain) and then the mortality was monitored over time. Including the powder in the formulation increased the killing rate of the formulation relative to the control. As a comparative example, the commercially available product " FX" (Bayer CropScience LP) (known as Both formulations have the same concentration of active ingredient, the only difference being the inclusion of powder in the liquid powder formulation (called KTD-1C).

[0163] exist Figure 3 In the present invention, the liquid powder formulation (30 mg ai / m 2 , β-cyfluthrin + imidacloprid) were directly sprayed on the resistant strain of bed bugs (called ALBUQUERQUE strain). The inclusion of a dust in a liquid formulation (called KTD-1C) increased the kill rate of the insecticide formulation compared to the inclusion of a dust in a liquid formulation (called KTD-1C). The active ingredient levels of both sprays were the same, the only difference being the inclusion of a dust in a liquid powder formulation (called KTD-1C).

Claims

1. A liquid powder formulation, Includes the following components: Flupyralidone in an amount of 3.00% w / w; β-cyfluthrin in an amount of 1.50% w / w; Piperonyl butoxide in an amount of 3.00% w / w; Benzyl acetate in an amount of 73.00% w / w; Ethoxylated castor oil containing 30EO in an amount of 4.00% w / w; Polyoxyethylene-polyoxypropylene block copolymer in an amount of 2.00% w / w; Ethoxylated (16EO) tristyrylphenol phosphate, potassium salt, in an amount of 4.00% w / w; Polydimethylsiloxane aqueous emulsion, Y-17259, in an amount of 0.10% w / w; Amorphous silicon dioxide in an amount of 9.00% w / w; A polyester block copolymer in an amount of 0.35% w / w; Citric acid in an amount of 0.05% w / w.

2. A liquid powder formulation comprising the following components: Imidacloprid (98%), in an amount of 1.01% w / w; β-cyfluthrin (98%) in an amount of 0.50% w / w; Citric acid in an amount of 0.00% w / w; Benzyl acetate in an amount of 8.10% w / w; Highly dispersed amorphous silicon dioxide in an amount of 9.88% w / w; Polyalkylene oxide-modified heptamethyltrisiloxane in an amount of 0.30% w / w; Sodium naphthalenesulfonate formaldehyde concentrate in an amount of 1.00% w / w; Sodium polycarboxylate anion, in an amount of 1.00% Polydimethylsiloxane aqueous emulsion, in an amount of 0.15% w / w; 20% 1,2-benzisothiazolin-3-one (BIT) sodium salt, in an amount of 0.18% w / w; An isothiazolone-based microbicide in an amount of 0.08% w / w; Citric acid in an amount of 0.02% w / w; Glycerol in an amount of 8.00% w / w; Sanxian gum, the amount of which is 0.30% w / w; Water in an amount of 69.48% w / w.

3. The liquid powder formulation according to claim 1 or 2, wherein the liquid powder formulation is a sprayable powder insecticidal composition.

4. A method of controlling insects, the method comprising applying the liquid powder formulation of any one of claims 1 to 3 to insects, insect eggs, surfaces or objects, or any combination thereof.

5. The method of claim 4, wherein the liquid powder formulation is at 0.001 mg ai / m 2 To 1000mgai / m 2 ratio is applied.

6. The method of claim 4, wherein the liquid powder formulation is at 0.01 mg ai / m 2 Up to 500mg ai / m 2 ratio is applied.

7. The method of claim 4, wherein the liquid powder formulation is at 0.10 mg ai / m 2 Up to 250mg ai / m 2 ratio is applied.

8. The method of claim 4, wherein the liquid powder formulation is at 0.50 mg ai / m 2 Up to 150mg ai / m 2 ratio is applied.

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