Composition for dissolving oily compound in water

Abstract

The present invention relates to the use of a composition for dissolving a water-insoluble active compound, comprising an alcohol, a surfactant (quaternary ammonium salt according to formula I) and water, where R3 of formula I is a C1-18 alkyl or alkenyl group. The invention also relates to the use of a composition comprising an active ingredient. The invention also relates to the use of a composition containing an active ingredient as an insecticide, an antimicrobial composition, an antibacterial composition, a perfume or a fungicide. Furthermore, the present invention relates to a method for exterminating insects, and the present invention relates to a method for dissolving water-insoluble active compounds. The invention also relates to the use of such compositions to store active compounds under extreme conditions.

Description

Technical Field

[0001] The present invention relates to a composition for dissolving a water-insoluble active compound. The present invention also relates to a composition comprising the active ingredient. The present invention also relates to the use of the composition comprising the active ingredient as an insect repellent. Background Art

[0002] Insect repellents can prevent and control outbreaks of insect-borne and other arthropod diseases, such as malaria, Lyme disease, dengue fever, bubonic plague, river blindness, and West Nile fever. Most repellents are insecticides (insect killers), but some deter insects, causing them to fly or crawl away. Common repellents include DEET (N,N-diethyl-m-toluamide), permethrin, and icaridin (also known as picaridin or Saltidin). Icaridin is effective against most insects, and the chemical is a synthetic version of piperine, an insect repellent found in pepper plants. Icaridin also has minimal odor and is non-destructive to plastics and other synthetic materials, meeting all the requirements for safe and effective use by humans and the environment. As a result, along with DEET, icaridin is one of the most popular repellents.

[0003] Icaridin is commonly sold under its product name Picaridin. The product is icaridin dissolved in pure oil. Pure oil is a mineral or vegetable oil that is not diluted with water and mixed with certain additives to produce certain beneficial properties. Picaridin can be further diluted in organic solvents such as ethanol, dimethyl sulfoxide (DMSO) and dimethylformamide (DMF).

[0004] Due to its hydrophobicity, an effective amount of icaridin cannot be dissolved in water. Therefore, it is impossible to prepare an aqueous solution containing icaridin that can be used as an insect repellent. Therefore, icaridin cannot be used in sprayable non-hazardous and harmless insect repellents, such as active wall sprays, clothing sprays and topical skin preparations. The lack of safe sprayable formulations containing icaridin seriously hinders the effectiveness of this compound. In addition, on the surface, the compound evaporates faster, thereby limiting the duration of action. Currently available icaridin products are based on alcohol, which makes the product flammable. This causes logistics limitations and more implementation problems.

[0005] Another method of dissolving compounds with hydrophobic properties in water is by using co-solvents to dissolve these compounds. However, co-solvent technology has only been used to dissolve solid or hydrophobic compounds and is not applicable to water-insoluble compounds such as oily compounds. Furthermore, as another option, surfactants are often applied to dissolve oily compounds, however the addition of surfactants only provides solubility for oily compounds at (very) low concentrations. Summary of the invention

[0006] It is therefore an object of the present invention to provide a composition for dissolving hydrophobic compounds in water.

[0007] Surprisingly it has been found that a composition comprising an alcohol which is liquid at room temperature and a surfactant which is a quaternary ammonium salt can be used to dissolve water-insoluble active compounds in water.

[0008] The alcohol in the composition is a cosolvent. Cosolvents are added to the composition to increase the solubility of poorly soluble compounds. Cosolvents are used to dissolve solid or hydrophobic compounds in aqueous systems rather than in oily solvents.

[0009] The term surfactant is derived from the term surface-active agent. This means that the compound can reduce the surface tension of a liquid or the interfacial tension between two liquids, between a gas and a liquid, or between a solid and a liquid. Thus, a surfactant can act as a detergent, a wetting agent, an emulsifier, a foaming agent or a dispersant. In the context of the present invention, a surfactant acts as an emulsifier, which means that the surfactant will form micelles or micelle-like structures around the water-insoluble active compound.

[0010] Therefore, the present invention relates to the use of a composition for dissolving a water-insoluble active compound, the composition comprising:

[0011] - an alcohol selected from the group consisting of methanol, ethanol, propanol, propanol derivatives, butanol and butanol derivatives,

[0012] - a surfactant which is a quaternary ammonium salt according to formula I, and

[0013] -water,

[0014]

[0015] Wherein R3 is C1-18 alkyl or alkenyl.

[0016] Thus, the composition comprising the surfactant and co-solvent combination is capable of solubilizing water-insoluble compounds in water.

[0017] The surfactant of the composition of the invention is a quaternary ammonium salt according to formula I. The surfactant forms a corona structure with its hydrophobic side turned toward the water-insoluble compound and its hydrophilic side turned toward the water molecule. This type of surfactant allows oily substances to form a stable mixture with aqueous solutions.

[0018] The present invention provides a system capable of dissolving water-insoluble active compounds. Therefore, the present invention also relates to the use of the above composition, wherein the composition further comprises an effective amount of a water-insoluble active compound, preferably an oily active compound.

[0019] The active compound of the composition of the present invention may be a natural or synthetic insect repellent, pesticide, antimicrobial compound, antibacterial compound or fungicide, anilino-based molecule such as a dye, fragrance or odorant.

[0020] According to the present invention, the active compound can be selected from the group consisting of: icaridin, DEET (N,N-diethyl-m-toluamide), citronellal, citronellol, eucalyptol, nepetalactone, azadirachtin, A-terpineol, carvacrol, thymol, cinnamaldehyde, rosemary oil, cedarwood oil, myrcene, citral, geranyl acetate, nerol, geraniol, limonene, permethrin, zinc pyrithione, or derivatives thereof, preferably icaridin and its derivatives.

[0021] Based on the definition of the R-group, the surfactants of the composition of the present invention can be divided into four embodiments. The first embodiment also defines R4.

[0022] Therefore, the present invention also relates to the use of the above composition, wherein R4 of formula I is methyl, an alkyl group shorter than the alkyl groups in R1, R2 and R3, or wherein R4 of formula I is one to three carbon containing carboxylic acid group, hydroxyl group, sulfonate group, quaternary silane group or phenyl group.

[0023] A second embodiment relates to the use of a composition according to the invention, wherein R1, R2 and R3 are identical.

[0024] In addition, in the third embodiment, all R-groups are defined. Therefore, the present invention also relates to the use of the above composition, wherein R1, R2 are methyl, R3 is C n H 2n+1 , wherein n=1-18, and R4 is an alkyl group shorter than the alkyl groups in R1, R2 and R3, or R4 is one to three carbon atoms having a carboxylic acid group, a hydroxyl group, a sulfonate group or a phenyl group.

[0025] Finally, in a fourth embodiment, the present invention relates to the use of the above composition, wherein each of R1, R2, R3 and R4 are the same.

[0026] Therefore, the present invention also relates to the use of the above composition, wherein the counterion of the quaternary ammonium salt is a halogen anion, preferably a chloride ion or a bromide ion.

[0027] The surfactant of the composition of the present invention can be a compound selected from the list consisting of trimethyloctadecyl ammonium chloride, stearyl trimethyl ammonium chloride, hexadecyl trimethyl ammonium chloride, cetyl trimethyl ammonium chloride, tetradecyl trimethyl ammonium bromide, myristyl trimethyl ammonium bromide, tetradecyl trimethyl ammonium chloride, dodecyl trimethyl ammonium bromide, dodecyl trimethyl ammonium chloride, trimethylacetyl ammonium chloride, tetramethyl ammonium chloride, dimethyloctadecyl [3- (trimethoxysilyl) propyl] ammonium chloride, cetyl dimethyl betaine, benzalkonium chloride, 3- (dimethyl (octadecyl) ammonium) propane-1-sulfonate, N-dodecyl-N, N- (dimethylammonium) butyrate (DDMAB), benzyl dimethyl dodecyl ammonium chloride, benzalkonium chloride (zephirol), N-dodecyl-N, N-dimethyl-3-ammonium-1-propanesulfonate, domiphen bromide (domiphen ammonium bromide), (dodecyl) dimethylammonium) acetate, didecyl dimethylammonium bromide, bis (dodecyl) dimethylammonium bromide, methyl trioctyl ammonium chloride, tri (dodecyl) methyl ammonium chloride, tetraoctyl ammonium bromide, tetra (dodecyl) ammonium bromide, preferably trimethyl octadecyl ammonium chloride.

[0028] Alcohol is an organic compound containing at least one hydroxyl group. In the context of the present invention, alcohol acts as a cosolvent. The alcohol present in the composition of the present invention can be divided into four main categories, which work on the cosolvent principle. The first category is straight-chain alcohols, which are hydrocarbons with one hydroxyl group. The carbon chain lengths of straight-chain alcohols are different, but these straight-chain alcohols do not have branches. The second category is branched alcohols, which are hydrocarbon chains with at least one branch, and the branch has a length of at least methyl. The third category is described as formula II. Each compound of formula II of this type contains a 1-butanol backbone with two methyl groups and an R-group at the 3-position.

[0029]

[0030] The final category involves the same alcohols as the first three, but these alcohols contain at least two hydroxyl groups instead of just one.

[0031] The present invention also relates to the use of the above composition, wherein the alcohol is liquid at room temperature, and wherein the alcohol is methanol, ethanol, propanol, a propanol derivative, butanol or a butanol derivative.

[0032] In other embodiments, the propanol derivative of the composition of the present invention is 2-propanol or isopropyl ether-ethanol.

[0033] In another embodiment, the butanol derivative of the composition of the present invention is selected from the list consisting of tert-butanol, isobutanol, 2-methoxy-3-methyl-1-butanol (MMB), 3-ethoxy-3-methyl-1-butanol, 3-benzyloxy-3-methyl-1-butanol, 3-methyl-3-methyl-1-butanol, 3-methyl-1,3-butanediol, preferably 2-methoxy-3-methyl-1-butanol (MMB).

[0034] According to the present invention, the active compound is present in the composition at about 0.1 wt.% to about 44.9 wt.%, preferably about 0.1 wt.% to about 20 wt.%, more preferably about 0.1 wt.% to about 10 wt.%, even more preferably about 0.5 wt.% to about 7 wt.%, most preferably about 1 wt.% to about 5 wt.%, and most preferably about 2 wt.% to about 3 wt.%, relative to the total weight of the composition.

[0035] The surfactant may be present in the composition of the present invention at about 0.1 wt.% to 6 wt.%, preferably about 0.5 wt.% to 4 wt.%, more preferably about 0.75 wt.% to 3 wt.%, most preferably about 1 wt.% to 2 wt.%, relative to the total weight of the composition.

[0036] The alcohol may be present in the composition at about 5 wt.% to 49.9 wt.%, preferably about 7 wt.% to 40 wt.%, more preferably about 9 wt.% to 30 wt.%, more preferably about 10 wt.% to 25 wt.%, even more preferably about 12 wt.% to 16 wt.%, most preferably about 12.5 wt.%, relative to the total weight of the composition, provided that the wt.% of water present in the composition is higher than the respective wt.% of any other component in the composition.

[0037] In the context of the present invention, a solution is defined as a solute dissolved in a solvent, producing a homogeneous mixture that is stable over time and will remain a homogeneous and stable mixture when passed through a filter.

[0038] Furthermore, in the context of the present invention, the solvent in an aqueous solution is always liquid water. Thus, a composition having multiple components is considered to be an aqueous solution when the wt.% of water present in the composition is higher than the respective wt.% of any other component in the composition.

[0039] Thus, in another embodiment, the present invention relates to a composition of the present invention, wherein the wt.% of water present in the composition is higher than the respective wt.% of any other component in the composition.

[0040] Furthermore, in one embodiment of the present invention, the water is deionized water.

[0041] In further embodiments of the invention, water is present in the composition at a higher wt. % than the other components of the composition combined.

[0042] According to a preferred embodiment of the present invention, water is present in the composition at more than 50 wt.%, preferably more than 60 wt.%, more preferably more than 70 wt.%, most preferably more than 80 wt.%, relative to the total weight of the composition, or wherein water is present at about 80 wt.% relative to the total weight of the composition.

[0043] In a preferred embodiment, the present invention relates to the above composition, wherein the composition comprises 2-methoxy-3-methyl-1-butanol, trimethyloctadecyl ammonium chloride, icaridin and water.

[0044] In this more preferred embodiment, the composition of the present invention may comprise at least 12.5 wt.% of methoxy-3-methyl-1-butanol and at least 1 wt.% of trimethyloctadecyl ammonium chloride, relative to the total weight of the composition.

[0045] The composition of the present invention may contain an active compound, however the present invention also relates to the use of a composition in which no active compound is present, i.e. in which the composition consists only of a system for dissolving an oily compound. The latter composition comprises a different wt.% of alcohol than the composition comprising the active compound. Thus, the composition of the present invention in which no active compound is present may comprise at least 12.5 wt.%, preferably 12.5 wt.% to 50 wt.%, more preferably 15 wt.% to 40 wt.%, even more preferably 15 wt.% to 25 wt.%, most preferably about 20 wt.% of alcohol relative to the total weight of the composition.

[0046] In embodiments where the composition of the present invention does not include an active compound, the composition may also include a different wt.% surfactant than the composition without the active compound. Relative to the total weight of the composition, the composition of the present invention in which the active compound is not present may include about 0.1 wt.% to 12 wt.%, preferably about 0.5 wt.% to 8 wt.%, more preferably about 0.75 wt.% to 4 wt.%, most preferably about 1 wt.% to 2 wt.% surfactant.

[0047] The compositions of the invention comprising the active compound are stable under extreme conditions, such as in a refrigerator, freezer or at 50°C overnight. Therefore, the present invention also relates to the use of the above-mentioned composition to store the active compound under such extreme conditions. The present invention also relates to the use of the present invention as described herein for storing the active compound as described herein at a temperature of -20°C to 20°C, in particular -20°C to 4°C, more particularly -20°C to 0°C. The present invention also relates to the use of the compositions of the invention as described herein for storing the active compound at a temperature of 20°C to 60°C, in particular 30°C to 55°C, more particularly 40°C to 50°C.

[0048] The present invention further relates to the use of the composition according to the invention for storing active compounds at temperatures from -20°C to 0°C and / or from 30°C to 55°C.

[0049] In addition, the composition of the invention comprising the active compound remains homogeneous, translucent and colorless after storage for 3.5 months. Therefore, the present invention also relates to the use of the above-mentioned composition of the present invention for storing the active compound for at least 1 week, in particular at least 1 month, more particularly at least 2 months, and most particularly at least 3.5 months.

[0050] In addition, the compositions of the present invention comprising the active compound can be used as insect repellents, insecticides, antimicrobial compositions, antibacterial compositions, fragrances or fungicides. In particular, the compositions of the present invention can be used to repel insects, especially insects with the potential to carry infectious diseases, especially mosquitoes, ticks, cockroaches, bedbugs, ants, biting flies, fleas and chiggers.

[0051] In another embodiment, the present invention relates to the use of the above composition on a building, a part of a building, a building material such as concrete, plastic, brick, foam or polyester. Applying the composition of the present invention to a home or home building material allows for convenient application of the active compound present in the composition of the present invention. When the active compound is in an aqueous solution, such compound can be better implemented in a home or home building material.

[0052] In a further embodiment, the present invention relates to the use of the above composition in coatings, paints, epoxy resins, wood, bricks, fibers, composites or textiles.

[0053] In addition, in another embodiment, the composition of the present invention can be used on the skin of humans or animals. The composition applied is an aqueous solution, so it is non-flammable and less dangerous. Therefore, it is more convenient and safe to apply the composition of the present invention on human skin or animal skin.

[0054] Furthermore, it is a further embodiment of the present invention that the composition can be used as a topical skin composition, in particular a cosmetic emulsion, spray or cream, or as a part of a topical skin composition such as an emulsion, spray or cream.

[0055] The present invention also relates to a method for repelling insects, comprising:

[0056] - applying the composition according to the invention to a surface, wherein the surface is preferably human or animal skin, the surface of a building or a part of a building, a building material or a coating.

[0057] The present invention also relates to a method for preparing a composition of the present invention which does not contain an active compound, comprising:

[0058] - Dissolve the alcohol and surfactant as described above in water to obtain a solution.

[0059] The present invention also relates to a method for dissolving a water-insoluble active compound in water, comprising:

[0060] - dissolving the alcohol and the surfactant as described above in water to obtain a solution,

[0061] - Adding the water-insoluble active compound as described above to the solution.

[0062] The present invention also relates to the use of the composition of the present invention as an insect repellent, insecticide, antimicrobial composition, antibacterial composition or fungicide.

[0063] The invention will now be illustrated by the following examples, which are not intended to limit the scope of the invention in any way. BRIEF DESCRIPTION OF THE DRAWINGS

[0064] Figure 1 :MMB and trimethyloctadecyl ammonium chloride

[0065] Figure 2 : MMB and dimethyloctadecyl[3-trimethoxysilyl]propyl]ammonium chloride

[0066] Figure 3 :MMB and tetradecyltrimethylammonium chloride

[0067] Figure 4 :MMB and 3-(dimethyl(octadecyl)ammonium)propane-1-sulfonate

[0068] Figure 5 :MMB and domiphene bromide

[0069] Figure 6 :MMB and bis(dodecyl)dimethylammonium bromide

[0070] Figure 7 :IPA and trimethyloctadecyl ammonium chloride

[0071] Figure 8 :Methanol and trimethyloctadecyl ammonium chloride

[0072] Fig. 9 :Ethanol and trimethyloctadecyl ammonium chloride

[0073] Fig.10 : Icaridin in the Water

[0074] Fig.11 : Icaridin in a mixture of water and MMB (45%)

[0075] Fig.12 : Icaridin in a mixture of water and MMB (25%)

[0076] Fig.13 : Icaridin in a mixture of water and MMB (12.5%)

[0077] Fig.14 :Icaridin and surfactant in water

[0078] Fig.15 :MMB and tetra(dodecyl)ammonium bromide

[0079] Fig.16 : Converting Icaridin to DEET

[0080] Fig.17 : Mosquito Method (Modular Testing System)

[0081] Fig.18 : Mosquito Method (Modular Testing System)

[0082] Fig.19 :Tetradecyltrimethylammonium chloride + MMB + Saltidin

[0083] Fig. 20 :3-(dimethyl(octadecyl)ammonium)propane-1-sulfonate+MMB+Saltidin

[0084] Fig.21 :Domiphene bromide + MMB + Saltitin

[0085] Fig. 22 :Bis(dodecyl)dimethylammonium bromide+MMB+Saltidin

[0086] Fig.23 :SiQ(DTSACl)+MMB+Saltidin

[0087] Fig.24:Isopropyl alcohol+IPA+Saltidin

[0088] Fig.25 :Methanol+IPA+Saltidin

[0089] Fig.26 :Ethanol+IPA+Saltidin

[0090] Fig. 27 :Trimethyloctadecyl ammonium chloride + MMB + dimethyl phthalate

[0091] Fig.28 :Trimethyloctadecyl ammonium chloride + MMB + 1,8-cineole

[0092] Fig.29 :Trimethyloctadecyl ammonium chloride + MMB + geraniol

[0093] Fig.30 :Trimethyloctadecyl ammonium chloride + MMB + eugenol

[0094] Fig.31 :Trimethyloctadecyl ammonium chloride + MMB + 2,5-dimethyl-2,5-hexanediol

[0095] Fig.32 : Trimethyloctadecyl ammonium chloride + MMB + lemongrass oil

[0096] Fig.33 : TEM examination: MMB + Domiphene Bromide + Saltidin

[0097] Fig.34 :TEM inspection:MMB+Saltidin DETAILED DESCRIPTION

[0098] Example

[0099] Example 1

[0100] The general procedure for preparing solutions of active compounds and compositions of the present invention is carried out as follows:

[0101] Deionized water was placed in a beaker equipped with a stirring bar and placed on a stirring plate. The co-solvent was added to the solution while stirring. Subsequently, the surfactant was added and before the surfactant was dissolved, the icaridin was also added. When all components of the composition were dissolved, the stirring was stopped.

[0102] The experiments are summarized in Table 1 below. The first column lists the cosolvents and surfactants used. The second column describes the results and the third column provides the weight percentages of the various components.

[0103] Table 1

[0104]

[0105]

[0106] Example 2

[0107] In this experiment, it was tested whether a cosolvent and surfactant combination was required to dissolve icaridin or whether the individual components were also able to dissolve icaridin in water.

[0108] Place deionized water in a beaker equipped with a stir bar and place on a stir plate. Add co-solvent (when applicable) to the solution while stirring. Add surfactant (when applicable) subsequently and icaridin (when applicable) before dissolution. Stop stirring when everything is dissolved.

[0109] Table 2

[0110]

[0111]

[0112] From Table 2 it can be concluded that icaridin is soluble in water only when a combination of cosolvent and surfactant is used.

[0113] Example 3

[0114] The same test was performed to determine whether the compositions of the present invention were also able to dissolve alternative water-insoluble compounds. In this experiment, icaridin was converted to DEET and the general procedure was performed.

[0115] Table 3

[0116]

[0117] In Table 3, it is demonstrated that the composition of the present invention is also able to dissolve 5 wt. % DEET in water.

[0118] Example 4

[0119] General procedure for testing various co-solvents and surfactants for dissolving Saltidin under extreme conditions: Deionized water (8.15 g, 81.50 wt%) was placed in a beaker equipped with a stir bar and placed on a stir plate. Co-solvent (1.25 g, 12.50 wt%) was added to the solution while stirring. Subsequently, surfactant (0.10 g, 1.00 wt%) was added, and before dissolution, Saltidin (0.5 g, 5.00 wt%) was also added. When everything was dissolved, stirring was stopped.

[0120]

[0121]

[0122] Example 5. Dissolution of various active compounds using a system comprising a cosolvent and a surfactant.

[0123] General procedure:

[0124] Deionized water (8.15 g, 81.50 wt%) was placed in a beaker equipped with a stirring rod and placed on a stirring plate. A cosolvent (1.25 g, 12.50 wt%) was added to the solution while stirring. Subsequently, a surfactant (0.10 g, 1.00 wt%) was added and before this dissolved, the active compound (0.5 g, 5.00 wt%) was also added. When everything was dissolved, stirring was stopped.

[0125]

[0126]

[0127] Example 6. GC-method and NMR-method

[0128] A GC-method was performed to demonstrate that the active compound was present in solution. The GC-method experiment was performed according to the following steps:

[0129] 1. Prepare an internal standard solution (IS) by diluting EBAP (ethyl butylacetamidopropionate, cas#52304-36-6) with IPA (2-propanol, cas#67-63-0) to obtain a 1% EBAP solution in IPA.

[0130] 2. Prepare the flushing solution. Dilute the IS solution 100-fold with IPA to 0.01% EBAP.

[0131] 3. Cut Whatman No. 1 paper into multiple pieces (25mm×40mm+10mm(10cm 2 +2.5cm 2 )).

[0132] 4.100% cotton shirt cut into multiple pieces (25mm×40mm+10mm(10cm 2 +2.5cm 2 ))

[0133] 5. Prepare the test solution as described in Section 3.1.

[0134] 6. Use a micropipette to apply 20 μL of the test solution in the form of dots on five pieces of paper and five pieces of fabric, with ~2 μL per dot.

[0135] 7. Before sampling, prepare 10 sample bottles (25 mL) and fill each sample bottle with 10 mL of flushing solution.

[0136] 8. Transfer the paper / fabric pieces to the corresponding sample bottles and make sure they are completely soaked in the solution.

[0137] 9. Once all paper and textiles are in the sample vials, allow to sit for at least 8 hours. Next, transfer 1 mL of each solution to a GC vial and measure the GC as specified in the table below.

[0138] 10. Check for the presence of compound peaks at the expected retention time.

[0139] Table 4 GC-Chromatography Equipment and Information.

[0140]

[0141] NMR methods were also performed to prove that the active compound was present in the solution. The NMR method experiments were performed according to the following steps:

[0142] Depending on the active compound, 25 μg of the solution was dissolved in 0.7 mL of DMSO-d6 or CDCl3 and NMR was measured on at least a 500 MHz machine. Make sure that the active compound and other compounds are predicted and the signals are identified.

[0143] Example 7. Transmission electron microscopy

[0144]

[0145] Example 8. Mosquito Method

[0146] The following mosquito method was performed to demonstrate that the active compound was still active in the formulation of the repellent compound.

[0147] In the absence of an official standard method, the procedure was based on the World Health Organization's "Guidelines for efficacy testing of spatial repellents" (World Health Organization, 2013, ISBN 978 924 150 502 4).

[0148] To prepare the test samples, aliquots (3.0 mL) of IRL (insect repellent liquid) were evenly applied to a 20.0 × 27.5 cm (550 cm 2) paper (Type: Whitman No 1). The samples were dried under ambient conditions (20-25°C) without any forced heating. All IRLs were kept in their original packaging at 15°C to 25°C before the start of the test.

[0149] Female mosquitoes of the genus Anopheles Arabiensis KGB were raised according to standard protocols. Mosquitoes were raised at a temperature of 27 ± 2 ° C, a relative humidity of 80 ± 10%, and a light period of 11.5 hours of light: 45 minutes of dusk: 11.15 hours of darkness: 45 minutes of dusk. Pupae were collected and transferred to a mesh cage, where they were enclosed as adults. Adults were raised in mesh cages using a 10% sucrose solution as an energy source. Before testing, 5 to 8-day-old female sterile mosquitoes that did not suck blood were starved (only water was provided) for 24 hours. Female mosquitoes that actively sought hosts were selected from the general population to ensure maximum behavioral responses. This was done with an aspirator or appropriate airflow device, while the hand was close to (but not touching) the cage and those mosquitoes that actively explored were collected. All repellent tests were observed in female mosquitoes that had been starved for 12 hours. Mosquitoes were carefully transferred to a holding container to avoid physical damage to them.

[0150] A modular test system was used based on the World Health Organization guidelines (Guidelines for testing the efficacy of spatial repellents, World Health Organization, 2013, ISBN 97892 4 150 502 4). The spatial repellency assay allows the examination of both spatial repulsion and contact stimulus responses. The main components of the modular system are Fig.17 The actual modular test system used is shown in Figure 1 and numbered. Fig.18 The total length of the test system used was 80 cm.

[0151] Each processing cylinder ( Fig.17 ) is constructed of a Plexiglas tube (9.0 cm OD, 0.3 cm thick, 28.5 cm long, 25 cm long capture area) and is mounted with a butterfly valve on one side and an end cap on the other side. The end cap is constructed of a Plexiglas cylinder (9.8 cm OD, 0.4 cm thick, 2.6 cm long) and is covered with a membrane that allows air to enter and exit the modular system. The transparent middle cylinder ( Fig.18 ) consisted of a Plexiglas tube with the same outer diameter and thickness as the treatment cylinder (outer diameter 9.8 cm at both ends, thickness 0.4 cm, length 3.4 cm), but with a length of 25.8 cm and a capture area of ​​16.4 cm. In the middle of the length of the transparent cylinder, there was a hole covered with a cork to transfer mosquitoes.

[0152] Treated filter paper (Whitman No. 1 or similar) was cut to 10 x 27.5 cm to match the capture area of ​​the treated cylinder (two pieces) and secured in place with scotch tape. The room temperature for all repellency tests was maintained at 27 ± 2 °C and relative humidity at 80 ± 10%.

[0153] The spatial repellency assay was performed in a closed temperature and humidity controlled room, without windows and with lights. Twenty female mosquitoes per group were introduced from a holding tube into a transparent cylinder (with an aspirator) and allowed to acclimate to the test environment for 30 seconds. The number of mosquitoes with body damage and unable to fly or walk was recorded to correct the total amount of mosquito samples available to respond to repeated test samples. Fig.17 As shown by the grey arrows in the figure, all butterfly valves were opened simultaneously for 4 minutes to allow the chemical vapor to flow through the test cell and also allow the mosquitoes to move freely throughout the cell. After 4 minutes, the butterfly valves were closed and the number of mosquitoes in each cylinder was recorded. The number of mosquitoes knocked down in each cylinder was also recorded.

[0154] The treatment cylinders were removed from the central transparent cylinder, the end caps were removed from both treatment cylinders, and the mosquitoes were blown into the mosquito collection cage. Likewise, mosquitoes from the central transparent cylinder were blown into the mosquito collection cage. All treated substrates remained in place between replicates. Consecutive replicates were performed without delay.

[0155] The test was repeated for each test sample. At the end of the test, the proportion of mosquitoes repelled by the treatment was determined. Spatial repellency was expressed as the proportion of mosquitoes prevented from entering the treatment space relative to all mosquitoes moving within the system and was calculated by the 'spatial activity index':

[0156]

[0157] where SAI is the spatial activity index, Nc is the number of mosquitoes in the control metal chamber, Nt is the number of mosquitoes in the treatment metal chamber, Nm is the total number of mosquitoes in both metal chambers, and N is the total number of mosquitoes in the test unit.

[0158] The spatial activity index ranges from -1 to 1: zero indicates no response; -1 indicates that all mosquitoes entered the treatment chamber, resulting in an attractant response; and 1 indicates that all mosquitoes moved to the control chamber (away from the treatment source), resulting in a spatial repulsion response. t =0, Nc=0), the test is valid, but the spatial activity index is 0.

[0159] Calculate the spatial activity index for each replicate. Report the number of replicates, total number of mosquitoes, and spatial activity index for each test sample.

Claims

1. Use of a composition for dissolving a water-insoluble active compound, the composition comprising: - an alcohol selected from the group consisting of methanol, ethanol, propanol, propanol derivatives, butanol and butanol derivatives, - a surfactant which is a quaternary ammonium salt according to formula I, and -water, Wherein R3 is C1-18 alkyl or alkenyl.

2. The use according to claim 1, wherein the composition further comprises an effective amount of a water-insoluble active compound, preferably an oily active compound.

3. The use according to claim 1 or 2, wherein the active compound is selected from the group consisting of icaridin, DEET, N,N-diethyl-m-toluamide, citronellal, citronellol, eucalyptol, nepetalactone, azadirachtin, A-terpineol, carvacrol, thymol, cinnamaldehyde, rosemary oil, cedarwood oil, myrcene, citral, geranyl acetate, nerol, geraniol, limonene, permethrin, zinc pyrithione, or a derivative thereof, preferably icaridin or a derivative thereof.

4. The method according to claim 1, wherein R4 of formula I is a methyl group, an alkyl group shorter than the alkyl groups in R1, R2 and R3, or R4 is one to three carbon groups containing a carboxylic acid group, a hydroxyl group, a sulfonate group or a phenyl group.

5. The use according to any one of claims 1 to 3, wherein R1, R2 and R3 are the same.

6. The use according to any one of claims 1 to 3, wherein R1, R2 are methyl, R3 is C n H 2n+1 , wherein n=1-18, and R4 is an alkyl group shorter than the alkyl groups in R1, R2 and R3, or R4 is one to three carbons containing a carboxylic acid group, a hydroxyl group, a sulfonate group or a phenyl group.

7. The use according to any one of claims 1 to 3, wherein R1, R2, R3 and R4 are the same.

8. The method according to any one of claims 1 to 7, wherein the counterion of the quaternary ammonium salt is a halogen anion, preferably a chloride ion or a bromide ion.

9. The use according to any one of claims 1 to 8, wherein the surfactant is a compound selected from the list consisting of trimethyloctadecyl ammonium chloride (SQ), stearyl trimethyl ammonium chloride, hexadecyl trimethyl ammonium chloride, cetyl trimethyl ammonium chloride, tetradecyl trimethyl ammonium bromide, myristyl trimethyl ammonium bromide, tetradecyl trimethyl ammonium chloride, dodecyl trimethyl ammonium bromide, dodecyl trimethyl ammonium chloride, trimethylacetyl ammonium chloride, tetramethyl ammonium chloride, dimethyloctadecyl [3- (trimethoxysilyl) propyl] ammonium chloride, cetyl trimethyl ammonium chloride. Dimethyl betaine, benzalkonium chloride, 3-(dimethyl(octadecyl)ammonium)propane-1-sulfonate, N-dodecyl-N,N-(dimethylammonium)butyrate (DDMAB), benzyldimethyldodecylammonium chloride, benzalkonium chloride, N-dodecyl-N,N-dimethyl-3-ammonium-1-propanesulfonate, domiphen bromide, (dodecyl)dimethylammonium) acetate, didecyldimethylammonium bromide, di(dodecyl)dimethylammonium bromide, methyltrioctylammonium chloride, tri(dodecyl)methylammonium chloride, tetraoctylammonium bromide, tetra(dodecyl)ammonium bromide.

10. The use according to any one of claims 1 to 9, wherein the surfactant is trimethyloctadecyl ammonium chloride (SQ).

11. The use according to any one of claims 1 to 10, wherein the alcohol is propanol, a propanol derivative, butanol or a butanol derivative.

12. The use according to claim 11, wherein the propanol derivative is 2-propanol or isopropyl ether-ethanol.

13. The use according to claim 11, wherein the butanol derivative is selected from the list consisting of tert-butanol, isobutanol, 2-methoxy-3-methyl-1-butanol (MMB), 3-ethoxy-3-methyl-1-butanol, 3-benzyloxy-3-methyl-1-butanol, 3-methyl-3-methyl-1-butanol, 3-methyl-1,3-butanediol, preferably 2-methoxy-3-methyl-1-butanol (MMB).

14. The use according to any one of claims 2 to 13, wherein the water-insoluble active compound is present in the composition at about 0.01 wt.% to about 44.9 wt.%, preferably about 0.1 wt.% to about 20 wt.%, more preferably about 0.1 wt.% to about 10 wt.%, even more preferably about 0.5 wt.% to about 7 wt.%, even more preferably about 1 wt.% to about 5 wt.%, most preferably about 2 wt.% to about 3 wt.%, relative to the total weight of the composition.

15. The use according to any one of claims 1 to 14, wherein the surfactant is present in the composition at about 0.1 wt.% to 6 wt.%, preferably about 0.5 wt.% to 4 wt.%, more preferably about 0.75 wt.% to 3 wt.%, most preferably about 1 wt.% to 2 wt.%, relative to the total weight of the composition.

16. Use according to any one of claims 1 to 15, wherein the alcohol is present in the composition at about 5 wt.% to 49.9 wt.%, preferably about 7 wt.% to 40 wt.%, more preferably about 9 wt.% to 30 wt.%, more preferably about 10 wt.% to 25 wt.%, even more preferably about 12 wt.% to 16 wt.%, most preferably about 12.5 wt.%, relative to the total weight of the composition, provided that the wt.% of water present in the composition is higher than the respective wt.% of any other component in the composition.

17. Use according to any one of claims 1 to 16, wherein the wt.% of water present in the composition is higher than the respective wt.% of any other component in the composition.

18. Use according to any one of claims 1 to 17, wherein the water is deionized water.

19. Use according to any one of claims 1 to 18, wherein the wt.% of water present in the composition is higher than the wt.% of the other components of the composition taken together.

20. The use according to any one of claims 1 to 19, wherein water is present in the composition at more than 50 wt.%, preferably more than 60 wt.%, more preferably more than 70 wt.%, most preferably more than 80 wt.%, relative to the total weight of the composition, or wherein the water is present at about 80 wt.%, relative to the total weight of the composition.

21. The use according to any one of claims 2 to 20, wherein the composition comprises 2-methoxy-3-methyl-1-butanol, trimethyloctadecyl ammonium chloride, icaridin and water.

22. Use according to claim 21, wherein the composition comprises at least 12.5 wt.% of methoxy-3-methyl-1-butanol and at least 1 wt.% of trimethyloctadecyl ammonium chloride, relative to the total weight of the composition.

23. Use according to claim 1, wherein the alcohol is present in the composition at at least 12.5 wt.%, preferably 12.5 wt.% to 50 wt.%, more preferably 15 wt.% to 40 wt.%, even more preferably 15 wt.% to 25 wt.%, most preferably about 20 wt.%, relative to the total weight of the composition.

24. The use according to claim 1, wherein the surfactant is present in the composition at about 0.1 wt.% to 12 wt.%, preferably about 0.5 wt.% to 8 wt.%, more preferably about 0.75 wt.% to 4 wt.%, most preferably about 1 wt.% to 2 wt.%, relative to the total weight of the composition.

25. Use of a composition as defined in any one of claims 2 to 22 as an insect repellent, insecticide, antimicrobial composition, antibacterial composition, fragrance or fungicide.

26. Use of a composition as defined in any one of claims 2 to 22 on a building, a part of a building, a building material such as concrete, plastic, brick, foam or polyester.

27. Use of a composition as defined in any one of claims 2 to 22 in coatings, paints, epoxy resins, wood, bricks, fibers, composites or textiles.

28. Use of a composition as defined in any one of claims 2 to 22 on the human or animal skin.

29. Use of a composition as defined in any one of claims 2 to 22 as or as part of a topical dermatological or cosmetic lotion, spray or cream.

30. A method for repelling insects comprising: - Applying a composition as defined in any one of claims 2 to 22 to a surface, wherein the surface is preferably human or animal skin, or the surface of a building, a part of a building, a building material or a coating.

31. A method for preparing a composition as defined in any one of claims 1 to 24, comprising: - Dissolving an alcohol as defined in any one of claims 1 to 24 and a surfactant in water to obtain a solution.

32. A method for dissolving a water-insoluble active compound as defined in any one of claims 2 to 22 in water, comprising: - dissolving an alcohol as defined in any one of claims 1 to 24 and a surfactant in water to obtain a solution, - adding a water-insoluble active compound as defined in any one of claims 2 to 22 to said solution.

33. Use of a composition as defined in any one of claims 2 to 22 for storing active compounds under extreme conditions, wherein the extreme conditions are temperatures of -20°C to 20°C, particularly -20°C to 4°C, especially -20°C to 0°C.

34. Use of a composition as defined in any one of claims 2 to 22 for storing active compounds under extreme conditions, wherein the extreme conditions are temperatures of 20°C to 60°C, particularly 30°C to 55°C, especially 40°C to 50°C.

35. Use of a composition as defined in any one of claims 2 to 22 for storing the active compound for at least 1 week, in particular at least 1 month, especially at least 2 months, and also in particular at least 3.5 months.

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