WO2009012415A1 - Insect repellent composition - Google Patents

Insect repellent composition Download PDF

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Publication number
WO2009012415A1
WO2009012415A1 PCT/US2008/070378 US2008070378W WO2009012415A1 WO 2009012415 A1 WO2009012415 A1 WO 2009012415A1 US 2008070378 W US2008070378 W US 2008070378W WO 2009012415 A1 WO2009012415 A1 WO 2009012415A1
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WO
WIPO (PCT)
Prior art keywords
concentration
insect control
control composition
limonene
oil
Prior art date
Application number
PCT/US2008/070378
Other languages
French (fr)
Inventor
Esam Enan
Krishna Prasad Sudhir
Original Assignee
Tyratech, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tyratech, Inc. filed Critical Tyratech, Inc.
Publication of WO2009012415A1 publication Critical patent/WO2009012415A1/en

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Classifications

    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/36Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a singly bound oxygen or sulfur atom attached to the same carbon skeleton, this oxygen or sulfur atom not being a member of a carboxylic group or of a thio analogue, or of a derivative thereof, e.g. hydroxy-carboxylic acids
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N49/00Biocides, pest repellants or attractants, or plant growth regulators, containing compounds containing the group, wherein m+n>=1, both X together may also mean —Y— or a direct carbon-to-carbon bond, and the carbon atoms marked with an asterisk are not part of any ring system other than that which may be formed by the atoms X, the carbon atoms in square brackets being part of any acyclic or cyclic structure, or the group, wherein A means a carbon atom or Y, n>=0, and not more than one of these carbon atoms being a member of the same ring system, e.g. juvenile insect hormones or mimics thereof
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N65/00Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N65/00Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
    • A01N65/08Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N65/00Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
    • A01N65/08Magnoliopsida [dicotyledons]
    • A01N65/22Lamiaceae or Labiatae [Mint family], e.g. thyme, rosemary, skullcap, selfheal, lavender, perilla, pennyroyal, peppermint or spearmint
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N65/00Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
    • A01N65/08Magnoliopsida [dicotyledons]
    • A01N65/36Rutaceae [Rue family], e.g. lime, orange, lemon, corktree or pricklyash
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N65/00Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
    • A01N65/40Liliopsida [monocotyledons]
    • A01N65/44Poaceae or Gramineae [Grass family], e.g. bamboo, lemon grass or citronella grass
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/02Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings containing insect repellants

Definitions

  • the present invention relates to compositions and methods for controlling insects.
  • insects have long sought protection against insects, and various chemicals and mixtures have been studied for insect repellent activity. Probing and blood engorgement from insects can be annoying and painful, and can often result in allergic reactions. More importantly, insects can act as vectors of diseases such as West Nile virus and Malaria.
  • compositions with insect repellent properties have been developed to provide protection against insect bites, however many of these compositions lose effectiveness as ambient temperatures rise. This problem is especially acute in regions of the world that are prone to higher temperatures, such as the tropics. In addition to poor heat tolerance, many current compositions having insect repellent properties impart an unpleasant odor, or leave an oily residue after application.
  • Embodiments of the invention include an insect control composition comprising at least two active ingredients and at least three of the following ingredients: lilac flower oil, tetrahydrolinalool, triethyl citrate, limonene, heliotropine, ⁇ -pinene, camphene, ⁇ -terpinene, carvacrol, thyme oil, paraffin, and petroleum jelly.
  • the composition can include tetrahydrolinalool, limonene, camphene, paraffin, and petroleum jelly., for example tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and camphene at a concentration of 0.1 %-1.0%.
  • the composition can include tetrahydrolinalool, limonene, thyme oil, paraffin, and petroleum jelly, with tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and thyme oil at a concentration of 0.1 %-1 .0%.
  • the composition can include lilac flower oil, limonene, ⁇ -pinene, paraffin, and petroleum jelly, with lilac flower oil at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and ⁇ - pinene at a concentration of 0.1 %-1 .0%.
  • the composition can include triethyl citrate, limonene, thyme oil, paraffin, and petroleum jelly, with triethyl citrate at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and thyme oil at a concentration of 0.1 %-1.0%.
  • the composition can include tetrahydrolinalool, limonene, ⁇ -terpinene, paraffin, and petroleum jelly, with tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and ⁇ -terpinene at a concentration of 0.1 %-1.0%.
  • the composition can include heliotropine, limonene, thyme oil, paraffin, and petroleum jelly, with heliotropine at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and thyme oil at a concentration of 0.1 %-1.0%.
  • the composition can include lilac flower oil, limonene, thyme oil, paraffin, and petroleum jelly, with lilac flower oil at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and thyme oil at a concentration of 0.1 %-1.0%.
  • the composition can include heliotropine, limonene, ⁇ -pinene, paraffin, and petroleum jelly, with heliotropine at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and ⁇ -pinene at a concentration of 0.1 %-1.0%.
  • the composition can include triethyl citrate, limonene, carvacrol, paraffin, and petroleum jelly, with triethyl citrate at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and carvacrol at a concentration of 0.1 %-1.0%.
  • the composition can include tetrahydrolinalool, limonene, ⁇ -terpinene, paraffin, and petroleum jelly, with tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and ⁇ -terpinene at a concentration of 0.1 %-1.0%.
  • insect refers, not only to insects, but also to, for example, arachnids and like invertebrates.
  • insect control means the presence of a repellent effect, a pesticidal effect, or both, that is attributable to the presence of an active ingredient.
  • a repellent effect is an effect, wherein more insects are repelled away from a host or area that has been treated with the composition than a control host or area that has not been treated with the composition.
  • a repellent effect is an effect wherein at least about 15% of insects are repelled away from a host or area that has been treated with the composition.
  • a repellent effect is an effect wherein at least about 50% of insects are repelled away from a host or area that has been treated with the composition.
  • a repellent effect is an effect wherein at least about 90% of insects are repelled away from a host or area that has been treated with the composition.
  • a "pesticidal effect” is an effect, wherein treatment with a composition causes at least about 1 % of the insects to die.
  • an LCi to LC 1 00 (lethal concentration) or an LD 1 to LD 10 O (lethal dose) of a composition will cause a pesticidal effect.
  • Embodiments of the invention include compositions for controlling insects, and methods for making these compositions. Certain embodiments of the invention can include one or more plant essential oils. Additionally, it is contemplated that these compositions can be made up of generally regarded as safe (GRAS) compounds.
  • GRAS generally regarded as safe
  • Embodiments of the invention can protect against insects in warm environments by use of a composition that resists the effects of high temperature and thus maintains its effectiveness for longer periods of time.
  • "warm environments” can include an environment with an air temperature over about 15 0 C, or over 2O 0 C, or over 3O 0 C, or over 4O 0 C, or higher.
  • Embodiments of the present invention can be used to control insects by treating a host directly.
  • the host can be treated by using a cream formulation, which can be taken internally or applied topically, e.g., to the skin of a human.
  • Compositions could be applied to the host, for example, in the case of a human, using formulations of a variety of personal products or cosmetics.
  • any of the following could be used: skin creams, skin lotions, hair conditioners and styling agents.
  • stabilizers, fragrances, and other substances can comprise compositions of the invention.
  • insect control compositions according to the invention include at least one of lilac flower oil, wintergreen oil, thyme oil, and citronella. In other embodiments, insect control compositions of embodiments of the invention include at least two of lilac flower oil, wintergreen oil, thyme oil, and citronella.
  • insect control compositions according to the invention can include at least one of light liquid paraffin, white soft paraffin, cetomacragol emulsifying wax, and white bees wax.
  • insect control compositions of embodiments of the invention can include at least two of light liquid paraffin, white soft paraffin, cetomacragol emulsifying wax, and white bees wax.
  • insect control compositions include light liquid paraffin, white soft paraffin, cetomacragol emulsifying wax, and white bees wax.
  • the paraffin is a micro paraffin wax.
  • LFO or lilac flower oil
  • IFF International Flavors & Fragrance
  • LFO can be replaced by any combination of ingredients having the major ingredients of LFO, such as, for example, various combinations of linalool asphalt, tetrahydrolinalool, vanillin, isopropyl myristate, piperonal (aldehyde), geraniol 60, and triethyl citrate.
  • the manufacturing process is performed in a cooled environment, such as in a refrigerated facility. In some embodiments, the manufacturing process is performed in a significantly cooled environment, such as, for example, in a coldroom. In some embodiments, the process can be performed at a constant temperature of, for example, 1 O 0 C, O 0 C,- 1 O 0 C, -2O 0 C, -3O 0 C, -4O 0 C, -6O 0 C, -8O 0 C, or the like. In some embodiments, the manufacturing process can utilize a dynamic temperature curve, such as, increasing the temperature during the process, decreasing the temperature during the process, a combination thereof, and the like.
  • compositions according to embodiments of the invention can be applied as liquids, suspension, emulsions, or solids by conventional application techniques for each.
  • the insect-control composition can be, for example, a composition including one or more plant essential oils, such as, for example, the compositions listed in Table 1 :
  • Embodiments of the invention comprise compositions for controlling insects and methods for using these compositions.
  • the compositions of the present invention can include any of the following oils listed in Table 2, or mixtures thereof:
  • compositions of the present invention may also include any of the following oils listed in Table 3, or mixtures thereof: TABLE 3
  • each oil can make up between about 1 % to about 99%, by weight, of the composition mixture.
  • one composition of the present invention comprises about 1 % thymol and about 99% geraniol.
  • the compositions can additionally comprise a fixed oil, which is a non-volatile non-scented plant oil.
  • the composition could include one or more of the following fixed oils listed in Table 4:
  • one composition of the present invention includes about 1 % thymol, about 50% geraniol and about 49% mineral oil.
  • embodiments are specifically contemplated in which any of the ingredients of the above tables are combined.
  • composition includes Lilac Flower Oil (LFO)
  • LFO Lilac Flower Oil
  • Tetrahydrolinalool Tetrahydrolinalool
  • Ethyl Linalool Heliotropine
  • Hedion Hercolyn D
  • Triethyl Citrate Triethyl Citrate
  • a blend of the following compounds can be substituted for the LFO: lsopropyl myhstate, Tetrahydrolinalool FCC, Linalool, Geraniol Fine FCC, Piperonal (aldehyde), and Vanillin.
  • composition includes LFO
  • a blend of the following compounds can be substituted for the LFO: lsopropyl myristate, Tetrahydrolinalool, Linalool, Geraniol, Piperonal (aldehyde), Vanillin, Methyl Salicylate, and D-limonene.
  • composition includes Black Seed Oil (BSO)
  • BSO Black Seed Oil
  • compositions include Thyme Oil
  • one or more of the following compounds can be substituted for the Thyme Oil: thymol, ⁇ -thujone; ⁇ -pinene, camphene, ⁇ -pinene, p-cymene, ⁇ - terpinene, linalool, borneol, ⁇ -caryophyllene, and carvacrol.
  • Compounds used to prepare the exemplary compositions of the present invention can be obtained, for example, from the following sources: Millennium Chemicals, Inc. (Jacksonville, FL), Ungerer Company (Lincoln Park, NJ), SAFC (Milwaukee, Wl), and IFF Inc. (Hazlet, NJ).
  • compositions it can be desirable to include compounds each having a purity of about 60%, 65%, 70%, 75%, 80%, 85%, 90%, or 95%.
  • geraniol it can be desirable to include a geraniol that is at least about 60%, 85% or 95% pure.
  • the compositions can include: geraniol 60, geraniol 85, or geraniol 95.
  • Nerol is a monoterpene (C10H18O), that can be extracted from attar of roses, oil of orange blossoms and oil of lavender.
  • Embodiments of the present invention can include art-recognized ingredients normally used in such formulations.
  • ingredients can include, for example, antifoaming agents, antimicrobial agents, anti-oxidants, anti-redeposition agents, bleaches, colorants, emulsifiers, enzymes, fats, fluorescent materials, fungicides, hydrotropes, moisturisers, optical bhghteners, perfume carriers, perfume, preservatives, proteins, silicones, soil release agents, solubilisers, sugar derivatives, sun screens, surfactants, vitamins waxes, and the like.
  • antifoaming agents for example, antifoaming agents, antimicrobial agents, anti-oxidants, anti-redeposition agents, bleaches, colorants, emulsifiers, enzymes, fats, fluorescent materials, fungicides, hydrotropes, moisturisers, optical bhghteners, perfume carriers, perfume, preservatives, proteins, silicones, soil release agents, solubilisers, sugar derivatives, sun screens, surfactants, vitamins waxes, and the like.
  • embodiments of the present invention can also contain other adjuvants or modifiers such as one or more therapeutically or cosmetically active ingredients.
  • exemplary therapeutic or cosmetically active ingredients useful in the compositions of the invention can include, for example, fungicides, sunscreening agents, sunblocking agents, vitamins, tanning agents, plant extracts, anti-inflammatory agents, anti-oxidants, radical scavenging agents, retinoids, alpha-hydroxy acids, emollients, antiseptics, antibiotics, antibacterial agents, antihistamines, and the like, and can be present in an amount effective for achieving the therapeutic or cosmetic result desired.
  • compositions of this invention can include one or more materials that can function as an antioxidant, such as reducing agents and free radical scavengers.
  • suitable materials that can function as antioxidants can include, for example: acetyl cysteine, ascorbic acid, t-butyl hydroquinone, cysteine, diamylhydroquinone, erythorbic acid, ferulic acid, hydroquinone, p-hydroxyanisole, hydroxylamine sulfate, magnesium ascorbate, magnesium ascorbyl phosphate, octocrylene, phloroglucinol, potassium ascorbyl tocopheryl phosphate, potassium sulfite, rutin, sodium ascorbate, sodium sulfite, sodium thloglycolate, thiodiglycol, thiodiglycolamide, thioglycolic acid, thiosalicylic acid, tocopherol, tocopheryl acetate, to
  • Embodiments of the invention can also include one or more materials that can function as a chelating agent to complex with metallic ions. This action can help to inactivate the metallic ions for the purpose of preventing their adverse effects on the stability or appearance of a formulated composition.
  • Chelating agents suitable for use in an embodiment of this invention can include, for example, aminothmethylene phosphonic acid, beta-alanine diacetic acid, calcium disodium EDTA, citric acid, cyclodexthn, cyclohexanediamine tetraacetic acid, diammonium citrate, diammonium EDTA, dipotassium EDTA, disodium azacycloheptane diphosphonate, disodium EDTA, disodium pyrophosphate, EDTA (ethylene diamine tetra acetic acid), gluconic acid, HEDTA (hydroxyethyl ethylene diamine triacetic acid), methyl cyclodextrin, pentapotassium triphosphate, pentasodium aminothmethylene phosphonate, pentasodium triphosphate, pentetic acid, phytic acid, potassium citrate, potassium gluconate, sodium citrate, sodium diethylenetriamine pentamethylene phosphonate, sodium di
  • each compound can make up between about 1 % to about 99%, by weight (wt/wt %) or by volume (vol/vol %), of the composition.
  • one composition of the present invention comprises about 2% ⁇ -Pinene and about 98% D-limonene.
  • percent amounts, by weight or by volume, of compounds are to be understood as referring to relative amounts of the compounds.
  • a composition including 7% linalool, 35% thymol, 4% alpha-pinene, 30% para-cymene, and 24% soy bean oil can be said to include a ratio of 7 to 35 to 4 to 30 to 24 linalool, thymol, alpha-pinene, para-cymene, and soy bean oil, respectively (by volume).
  • the resulting composition would include 7 to 35 to 4 to 40 linalool, thymol, ⁇ -pinene, and para-cymene, respectively (by volume).
  • This resulting composition would include 9.21 % linalool, 46.05% thymol, 5.26% ⁇ -pinene, and 39.48% para-cymene (vol/vol %).
  • the resulting composition would include 4.2% linalool, 21 % thymol, 2.4% ⁇ -pinene, 18% para-cymene, 14.4% soy bean oil, and 40% safflower oil (vol/vol %).
  • volume percentages are easily converted to weight percentages based the known or measured specific gravity of the substance.
  • Blend 61 a synthetic lime oil that can be obtained, for example, from Millennium Chemicals, Inc.
  • FCC Food Chemical Codex
  • Geraniol Fine FCC Geraniol Fine FCC or Tetrahydrolinalool FCC, which compounds can be obtained, for example, from Millennium Chemicals, Inc.
  • the compounds of plant origin can be tested for their precise chemical composition using, for example, High-Pressure Liquid Chromatography (HPLC), Mass Spectrometry (MS), gas chromatography, or the like.
  • HPLC High-Pressure Liquid Chromatography
  • MS Mass Spectrometry
  • gas chromatography or the like.
  • the term "about” or “approximately” means within an acceptable error range for the particular value as determined by one of ordinary skill in the art, which will depend in part on how the value is measured or determined, i.e., the limitations of the measurement system, i.e., the degree of precision required for a particular purpose, such as a pharmaceutical formulation.
  • “about” can mean within 1 or more than 1 standard deviations, per the practice in the art.
  • “about” can mean a range of up to 20%, preferably up to 10%, more preferably up to 5%, and more preferably still up to 1 % of a given value.
  • the term can mean within an order of magnitude, preferably within 5-fold, and more preferably within 2-fold, of a value.
  • the term "substantially,” as used herein, means at least about 80%, preferably at least about 90%, more preferably at least about 99%, for example at least about 99.9%. In some embodiments, the term “substantially” can mean completely, or about 100%.
  • Embodiments of the invention can include at least one oil, such as, for example, "Superior oil,” highly-refined oils, and the like.
  • the host can also be treated directly by using a formulation of a composition that is delivered orally.
  • a composition can be enclosed within a liquid capsule and ingested.
  • compositions containing plant essential oils have been prepared and tested for efficacy against different targets.
  • the following examples provide details of exemplary compositions. As disclosed herein, it is within the scope of the present invention to vary the concentrations of components of each composition within useful ranges. Accordingly, these specific compositions are merely representative of certain embodiments of the invention.
  • This embodiment of the invention is prepared at 15°C.
  • This embodiment of the invention was prepared at a temperature significantly reduced relative to the ambient temperature.
  • Citronella Oil 0.4g
  • This embodiment of the invention is prepared at 10 0 C.
  • Hairless or shaved mice and guinea pigs are used to test the repellent effect of compositions delivered orally.
  • the test composition is administered orally to about 10 rodents.
  • a control substance such as mineral oil, is administered orally to about 10 rodents.
  • each rodent is placed in an enclosed container.
  • About 20 mosquitoes are introduced to each container. Each container is observed for approximately 1 hour.
  • the time that each insect spends on the rodent is recorded and number of lesions caused by the insect on the skin of the rodent is recorded.
  • the insects spend less time on rodents receiving the test compositions than on the rodents receiving the control substance.
  • the rodents receiving the test compositions receive fewer lesions than the rodents receiving the control substances.
  • Hairless or shaved mice and guinea pigs are used to test the repellent effect of test compositions delivered topically.
  • the test compositions are administered topically to the skin of about 10 rodents.
  • a control substance such as mineral oil, is administered topically to the skin of about 10 rodents.
  • each rodent is placed in an enclosed container.
  • About 20 mosquitoes are introduced to each container. Each container is observed for approximately 1 hour.
  • the time that each insect spends on the rodent is recorded and number of lesions caused by the insect on the skin of the rodent is recorded.
  • the insects spend less time on rodents receiving the test compositions than on the rodents receiving the control substance.
  • the rodents receiving the test compositions receive fewer lesions than the rodents receiving the control substances.
  • Each cage is stocked with about 100 southern house mosquitoes (culex quinquefasciatus), which are about 7 to 10 days-old. The mosquitoes are starved for about 12 hours. Each cage is supplied with four containers, each filled with cotton that has been soaked with sugar water.
  • Three of the four containers are treated randomly with about 1 ml_ of the composition being tested, while the remaining container serves as an untreated control.
  • the containers are positioned in the four opposing corners of each cage and landing counts are conducted at about 0, 1 , 2, 4, and 6 hour intervals following addition of the compositions being tested to the respective containers.
  • the containers are removed from the cage between exposure intervals. Each exposure interval lasts for about 5 minutes.
  • Pesticidal effect of test compositions containing plant essential oils on red ants is tested in the following manner.
  • a paper disk is treated with about 20 uL of each of the composition being tested and the treated disks are each placed in a vial.
  • An untreated paper disk is placed in a control vial.
  • a paper disk is treated with about 20 uL 100% DEET and placed in a vial to compare the pesticidal effect of the test compositions to that of DEET, a known commercial insect control agent.
  • About three red ants are introduced into each vial and the openings to the vials are closed with cotton to prevent the insects from escaping. The insects are exposed to the compositions for about one hour or less and mortality is recorded.
  • Repellent effect of test compositions containing plant essential oils on red ants is tested in the following manner.
  • a paper disk is treated with about 200 uL of each composition and placed in a dish.
  • An untreated paper disk is placed in a control dish.
  • a paper disk is treated with about 200 uL 100% DEET and placed in a dish to compare the repellent effect of the compositions to that of DEET.
  • Red ants are introduced into each dish. Insect behavior and number of visits to the treated paper disk are monitored for about 5 minutes. The number of visits by a red ant to the paper disk is recorded.
  • Residuality with regard to pesticidal effect and repellent effect, is tested by treating a paper disk with the composition being tested, keeping the treated paper disk under laboratory conditions for a predetermined period of time (e.g., 0 min, 6 hours, 1 day, 3 days, 5 days, 7 days), and exposing red ants to the treated paper disk in the above described manners.
  • a predetermined period of time e.g., 0 min, 6 hours, 1 day, 3 days, 5 days, 7 days

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Abstract

Insect control compositions are disclosed that maintain their effectiveness under elevated ambient temperatures. Methods of preparation of the compositions can include maintaining specific temperature(s) during manufacturing steps.

Description

INSECT REPELLENT COMPOSITION
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority from U.S. Provisional Application Serial No. 60/961 ,066 filed on July 17, 2007, which is incorporated herein by reference in its entirety.
FIELD OF THE INVENTION
[0002] The present invention relates to compositions and methods for controlling insects.
BACKGROUND
[0003] Humans have long sought protection against insects, and various chemicals and mixtures have been studied for insect repellent activity. Probing and blood engorgement from insects can be annoying and painful, and can often result in allergic reactions. More importantly, insects can act as vectors of diseases such as West Nile virus and Malaria.
[0004] Compositions with insect repellent properties have been developed to provide protection against insect bites, however many of these compositions lose effectiveness as ambient temperatures rise. This problem is especially acute in regions of the world that are prone to higher temperatures, such as the tropics. In addition to poor heat tolerance, many current compositions having insect repellent properties impart an unpleasant odor, or leave an oily residue after application. SUMMARY
[0005] Embodiments of the invention include an insect control composition comprising at least two active ingredients and at least three of the following ingredients: lilac flower oil, tetrahydrolinalool, triethyl citrate, limonene, heliotropine, α-pinene, camphene, α-terpinene, carvacrol, thyme oil, paraffin, and petroleum jelly.
[0006] Some embodiments utilize at least one essential oil as an active ingredient. In some embodiments the composition can include tetrahydrolinalool, limonene, camphene, paraffin, and petroleum jelly., for example tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and camphene at a concentration of 0.1 %-1.0%.
[0007] In some embodiments the composition can include tetrahydrolinalool, limonene, thyme oil, paraffin, and petroleum jelly, with tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and thyme oil at a concentration of 0.1 %-1 .0%.
[0008] In some embodiments the composition can include lilac flower oil, limonene, α-pinene, paraffin, and petroleum jelly, with lilac flower oil at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and α- pinene at a concentration of 0.1 %-1 .0%.
[0009] In some embodiments the composition can include triethyl citrate, limonene, thyme oil, paraffin, and petroleum jelly, with triethyl citrate at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and thyme oil at a concentration of 0.1 %-1.0%.
[0010] In some embodiments the composition can include tetrahydrolinalool, limonene, α-terpinene, paraffin, and petroleum jelly, with tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and α-terpinene at a concentration of 0.1 %-1.0%.
[0011] In some embodiments the composition can include heliotropine, limonene, thyme oil, paraffin, and petroleum jelly, with heliotropine at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and thyme oil at a concentration of 0.1 %-1.0%.
[0012] In some embodiments the composition can include lilac flower oil, limonene, thyme oil, paraffin, and petroleum jelly, with lilac flower oil at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and thyme oil at a concentration of 0.1 %-1.0%.
[0013] In some embodiments the composition can include heliotropine, limonene, α-pinene, paraffin, and petroleum jelly, with heliotropine at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and α-pinene at a concentration of 0.1 %-1.0%.
[0014] In some embodiments the composition can include triethyl citrate, limonene, carvacrol, paraffin, and petroleum jelly, with triethyl citrate at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1 .0%, and carvacrol at a concentration of 0.1 %-1.0%. [0015] In some embodiments the composition can include tetrahydrolinalool, limonene, α-terpinene, paraffin, and petroleum jelly, with tetrahydrolinalool at a concentration of 0.1 %-1.0%, and limonene at a concentration of 0.1 %-1.0%, and α-terpinene at a concentration of 0.1 %-1.0%.
DETAILED DESCRIPTION OF THE INVENTION
[0016] For purposes of simplicity, the term "insect" shall be used throughout this application; however, it should be understood that the term "insect" refers, not only to insects, but also to, for example, arachnids and like invertebrates.
[0017] As used herein, the term "insect control" means the presence of a repellent effect, a pesticidal effect, or both, that is attributable to the presence of an active ingredient.
[0018] As used herein, a "repellent effect" is an effect, wherein more insects are repelled away from a host or area that has been treated with the composition than a control host or area that has not been treated with the composition. In some embodiments, a repellent effect is an effect wherein at least about 15% of insects are repelled away from a host or area that has been treated with the composition. In some embodiments, a repellent effect is an effect wherein at least about 50% of insects are repelled away from a host or area that has been treated with the composition. In some embodiments, a repellent effect is an effect wherein at least about 90% of insects are repelled away from a host or area that has been treated with the composition. [0019] As used herein, a "pesticidal effect" is an effect, wherein treatment with a composition causes at least about 1 % of the insects to die. In this regard, an LCi to LC100 (lethal concentration) or an LD1 to LD10O (lethal dose) of a composition will cause a pesticidal effect.
[0020] Embodiments of the invention include compositions for controlling insects, and methods for making these compositions. Certain embodiments of the invention can include one or more plant essential oils. Additionally, it is contemplated that these compositions can be made up of generally regarded as safe (GRAS) compounds.
[0021] Embodiments of the invention can protect against insects in warm environments by use of a composition that resists the effects of high temperature and thus maintains its effectiveness for longer periods of time. In some embodiments, "warm environments" can include an environment with an air temperature over about 150C, or over 2O0C, or over 3O0C, or over 4O0C, or higher.
[0022] Embodiments of the present invention can be used to control insects by treating a host directly. For example, the host can be treated by using a cream formulation, which can be taken internally or applied topically, e.g., to the skin of a human. Compositions could be applied to the host, for example, in the case of a human, using formulations of a variety of personal products or cosmetics. For example, any of the following could be used: skin creams, skin lotions, hair conditioners and styling agents.
[0023] In certain embodiments, stabilizers, fragrances, and other substances can comprise compositions of the invention. [0024] In certain embodiments, insect control compositions according to the invention include at least one of lilac flower oil, wintergreen oil, thyme oil, and citronella. In other embodiments, insect control compositions of embodiments of the invention include at least two of lilac flower oil, wintergreen oil, thyme oil, and citronella.
[0025] Likewise, insect control compositions according to the invention can include at least one of light liquid paraffin, white soft paraffin, cetomacragol emulsifying wax, and white bees wax. In some embodiments, insect control compositions of embodiments of the invention can include at least two of light liquid paraffin, white soft paraffin, cetomacragol emulsifying wax, and white bees wax. In other exemplary embodiments, insect control compositions include light liquid paraffin, white soft paraffin, cetomacragol emulsifying wax, and white bees wax. In some embodiments, the paraffin is a micro paraffin wax.
[0026] In some embodiments of the invention, LFO, or lilac flower oil, can be replaced by International Flavors & Fragrance (IFF) luscious lilac. Likewise, LFO can be replaced by any combination of ingredients having the major ingredients of LFO, such as, for example, various combinations of linalool coeur, tetrahydrolinalool, vanillin, isopropyl myristate, piperonal (aldehyde), geraniol 60, and triethyl citrate.
[0027] In some embodiments of the invention, the manufacturing process is performed in a cooled environment, such as in a refrigerated facility. In some embodiments, the manufacturing process is performed in a significantly cooled environment, such as, for example, in a coldroom. In some embodiments, the process can be performed at a constant temperature of, for example, 1 O0C, O0C,- 1 O0C, -2O0C, -3O0C, -4O0C, -6O0C, -8O0C, or the like. In some embodiments, the manufacturing process can utilize a dynamic temperature curve, such as, increasing the temperature during the process, decreasing the temperature during the process, a combination thereof, and the like.
[0028] Compositions according to embodiments of the invention can be applied as liquids, suspension, emulsions, or solids by conventional application techniques for each.
[0029] In some embodiments of the present invention, the insect-control composition can be, for example, a composition including one or more plant essential oils, such as, for example, the compositions listed in Table 1 :
TABLE 1
Figure imgf000009_0001
Figure imgf000010_0001
Figure imgf000011_0001
Figure imgf000012_0001
Figure imgf000013_0001
Figure imgf000014_0001
Figure imgf000015_0001
Figure imgf000016_0001
Figure imgf000017_0001
Figure imgf000018_0001
[0030] Embodiments of the invention comprise compositions for controlling insects and methods for using these compositions. The compositions of the present invention can include any of the following oils listed in Table 2, or mixtures thereof:
TABLE 2 trans-anethole lime oil piperonyl
Black seed oil (BSO) d-limonene piperonyl acetate camphene linalyl anthranilate piperonyl alcohol carvacrol linalool piperonyl amine quinone d-carvone lindenol sabinene l-carvone methyl citrate α-terpinene
1 ,8-cineole methyl di-hydrojasmonate terpinene 900 p-cymene myrcene α-terpineol diethyl phthalate perillyl alcohol gamma-terpineol eugenol phenyl acetaldehyde 2-tert-butyl-p-quinone geraniol phenylethyl alcohol α-thujone isopropyl citrate phenylethyl propionate thyme oil lemon grass oil α-pinene thymol lilac flower oil (LFO) β-pinene piperonal
[0031] The compositions of the present invention may also include any of the following oils listed in Table 3, or mixtures thereof: TABLE 3
AIIyI sulfide β-elemene Menthyl salicylate
AIIyI trisulfide gamma-elemene Myrtenal
Allyl-disulfide Elmol Neraldimethyl acetate
Anethole Estragole Nerolidol
Artemisia alcohol 2-ethyl-2-hexen-1-ol Nonanone acetate Eugenol acetate 1-octanol
Benzyl acetate α-farnesene E ocimenone
Benzyl alcohol (Z1E)- α-farnesene Z ocimenone
Bergamotene E-β-farnesene 3-octanone β-bisabolene Fenchone Ocimene
Bisabolene oxide Forskolin Octyl acetate α-bisabolol Furanodiene PD 98059
Bisabolol oxide Furanoeudesma-1 ,3-diene Peppermint oil
Bisobolol oxide β Furanoeudesma-1 ,4-diene Permethhn
Bornyl acetate Furano germacra 1 ,10(15)- α-phellandrene β-bourbonene diene-6-one β -phellandrene α-cadinol Furanosesquiterpene piperonal
Camphene Geraniol Prenal α-campholene Geraniol acetate Propargite α-campholene aldehyde Germacrene D Pulegone camphor Germacrene B Pyrethrum carbaryl α-gurjunene Sabinene
Caryophyllene oxide α-humulene Sabinyl acetate
Chamazulene α-ionone D-santalene
Chrysanthemate ester β-ionone Santalol
Chrysanthemic acid lsoborneol Sativen
Chrysanthemyl alcohol lsofuranogermacrene δ-selinene
Cinnamaldehyde Iso-menthone β-sesquphelandrene
Cis-verbenol Iso-pulegone Spathulenol
Citral A Jasmone Tagetone
Citral B cis-jasmone Tamoxifen
Citronellal Lavandustin A Tebufenozide
Citronellol Lilac flower oil α-terpinene
Citronellyl acetate Limonene 4-terpineol
Citronellyl formate Linalool α-terpinolene α-copaene Linalyl acetate α-terpinyl acetate cornmint oil Lindestrene tetrahydrofurfuryl alcohol. β-costol Methyl-allyl-trisulfide D-thujene
Cryptone Menthol Thymyl methyl ether
Curzerenone 2-methoxy furanodiene Trans-caryophyllene d-Carvone menthone Trans-pinocarveol
/-Carvone Menthyl acetate Trans-verbenol
Davanone Menthyl salicylate Verbenone
Diallyl tetrasulfide Methyl cinnamate Yomogi alcohol dihydropyrocurzerenone Zingiberene Dihydrotagentone
[0032] In those compositions including more than one oil, each oil can make up between about 1 % to about 99%, by weight, of the composition mixture. For example, one composition of the present invention comprises about 1 % thymol and about 99% geraniol. Optionally, the compositions can additionally comprise a fixed oil, which is a non-volatile non-scented plant oil. For example, the composition could include one or more of the following fixed oils listed in Table 4:
TABLE 4 castor oil mineral oil saff lower oil corn oil olive oil sesame oil cumin oil peanut oil soy bean oil canola oil
[0033] For example, one composition of the present invention includes about 1 % thymol, about 50% geraniol and about 49% mineral oil. In addition, embodiments are specifically contemplated in which any of the ingredients of the above tables are combined.
[0034] In certain embodiments wherein the composition includes Lilac Flower Oil (LFO), one or more of the following compounds can be substituted for the LFO: Tetrahydrolinalool, Ethyl Linalool, Heliotropine, Hedion, Hercolyn D, and Triethyl Citrate. In certain embodiments wherein the composition includes LFO, a blend of the following compounds can be substituted for the LFO: lsopropyl myhstate, Tetrahydrolinalool FCC, Linalool, Geraniol Fine FCC, Piperonal (aldehyde), and Vanillin. In certain embodiments wherein the composition includes LFO, a blend of the following compounds can be substituted for the LFO: lsopropyl myristate, Tetrahydrolinalool, Linalool, Geraniol, Piperonal (aldehyde), Vanillin, Methyl Salicylate, and D-limonene.
[0035] In certain embodiments wherein the composition includes Black Seed Oil (BSO), one or more of the following compounds can be substituted for the BSO: α -thujene: α -pinene; β -pinene; p-cymene; limonene; and tert-butyl-p- benzoquinone.
[0036] In certain exemplary embodiments wherein the composition includes Thyme Oil, one or more of the following compounds can be substituted for the Thyme Oil: thymol, α-thujone; α-pinene, camphene, β-pinene, p-cymene, α- terpinene, linalool, borneol, β-caryophyllene, and carvacrol. Compounds used to prepare the exemplary compositions of the present invention can be obtained, for example, from the following sources: Millennium Chemicals, Inc. (Jacksonville, FL), Ungerer Company (Lincoln Park, NJ), SAFC (Milwaukee, Wl), and IFF Inc. (Hazlet, NJ).
[0037] In some embodiments of the compositions, it can be desirable to include compounds each having a purity of about 60%, 65%, 70%, 75%, 80%, 85%, 90%, or 95%. For example, in some embodiments of the compositions that include geraniol, it can be desirable to include a geraniol that is at least about 60%, 85% or 95% pure. In some embodiments, it can be desirable to include a specific type of geraniol. For example, in some embodiments, the compositions can include: geraniol 60, geraniol 85, or geraniol 95. When geraniol is obtained as geraniol 60, geraniol 85, or geraniol 95, then forty percent, fifteen percent, or five percent of the oil can be Nerol. Nerol is a monoterpene (C10H18O), that can be extracted from attar of roses, oil of orange blossoms and oil of lavender. Embodiments of the present invention can include art-recognized ingredients normally used in such formulations. These ingredients can include, for example, antifoaming agents, antimicrobial agents, anti-oxidants, anti-redeposition agents, bleaches, colorants, emulsifiers, enzymes, fats, fluorescent materials, fungicides, hydrotropes, moisturisers, optical bhghteners, perfume carriers, perfume, preservatives, proteins, silicones, soil release agents, solubilisers, sugar derivatives, sun screens, surfactants, vitamins waxes, and the like.
[0038] In certain embodiments, embodiments of the present invention can also contain other adjuvants or modifiers such as one or more therapeutically or cosmetically active ingredients. Exemplary therapeutic or cosmetically active ingredients useful in the compositions of the invention can include, for example, fungicides, sunscreening agents, sunblocking agents, vitamins, tanning agents, plant extracts, anti-inflammatory agents, anti-oxidants, radical scavenging agents, retinoids, alpha-hydroxy acids, emollients, antiseptics, antibiotics, antibacterial agents, antihistamines, and the like, and can be present in an amount effective for achieving the therapeutic or cosmetic result desired. [0039] In some embodiments, compositions of this invention can include one or more materials that can function as an antioxidant, such as reducing agents and free radical scavengers. Suitable materials that can function as antioxidants can include, for example: acetyl cysteine, ascorbic acid, t-butyl hydroquinone, cysteine, diamylhydroquinone, erythorbic acid, ferulic acid, hydroquinone, p-hydroxyanisole, hydroxylamine sulfate, magnesium ascorbate, magnesium ascorbyl phosphate, octocrylene, phloroglucinol, potassium ascorbyl tocopheryl phosphate, potassium sulfite, rutin, sodium ascorbate, sodium sulfite, sodium thloglycolate, thiodiglycol, thiodiglycolamide, thioglycolic acid, thiosalicylic acid, tocopherol, tocopheryl acetate, tocopheryl linoleate, ths(nonylpheny)phosphite, and the like.
[0040] Embodiments of the invention can also include one or more materials that can function as a chelating agent to complex with metallic ions. This action can help to inactivate the metallic ions for the purpose of preventing their adverse effects on the stability or appearance of a formulated composition. Chelating agents suitable for use in an embodiment of this invention can include, for example, aminothmethylene phosphonic acid, beta-alanine diacetic acid, calcium disodium EDTA, citric acid, cyclodexthn, cyclohexanediamine tetraacetic acid, diammonium citrate, diammonium EDTA, dipotassium EDTA, disodium azacycloheptane diphosphonate, disodium EDTA, disodium pyrophosphate, EDTA (ethylene diamine tetra acetic acid), gluconic acid, HEDTA (hydroxyethyl ethylene diamine triacetic acid), methyl cyclodextrin, pentapotassium triphosphate, pentasodium aminothmethylene phosphonate, pentasodium triphosphate, pentetic acid, phytic acid, potassium citrate, potassium gluconate, sodium citrate, sodium diethylenetriamine pentamethylene phosphonate, sodium dihydroxyethylglycinate, sodium gluconate, sodium metaphosphate, sodium metasilicate, sodium phytate, triethanolamine ("TEA")-EDTA, TEA-polyphosphate, tetrahydroxypropyl ethylenediamine, tetrapotassium pyrophosphate, tetrasodium EDTA, tetrasodium pyrophosphate, tripotassium EDTA, trisodium EDTA, trisodium HEDTA, trisodium phosphate, and the like.
[0041] In some embodiments, each compound can make up between about 1 % to about 99%, by weight (wt/wt %) or by volume (vol/vol %), of the composition. For example, one composition of the present invention comprises about 2% α-Pinene and about 98% D-limonene. As used herein, percent amounts, by weight or by volume, of compounds are to be understood as referring to relative amounts of the compounds. As such, for example, a composition including 7% linalool, 35% thymol, 4% alpha-pinene, 30% para-cymene, and 24% soy bean oil (vol/vol %) can be said to include a ratio of 7 to 35 to 4 to 30 to 24 linalool, thymol, alpha-pinene, para-cymene, and soy bean oil, respectively (by volume). As such, if one compound is removed from the composition, or additional compounds or other ingredients are added to the composition, it is contemplated that the remaining compounds can be provided in the same relative amounts. For example, if soy bean oil were removed from the exemplary composition, the resulting composition would include 7 to 35 to 4 to 40 linalool, thymol, α-pinene, and para-cymene, respectively (by volume). This resulting composition would include 9.21 % linalool, 46.05% thymol, 5.26% α-pinene, and 39.48% para-cymene (vol/vol %). For another example, if safflower oil were added to the original composition to yield a final composition containing 40% (vol/vol) safflower oil, then the resulting composition would include 4.2% linalool, 21 % thymol, 2.4% α-pinene, 18% para-cymene, 14.4% soy bean oil, and 40% safflower oil (vol/vol %). One having ordinary skill in the art would understand that volume percentages are easily converted to weight percentages based the known or measured specific gravity of the substance.
[0042] In certain embodiments, it can be desirable to include a naturally- occurring version or a synthetic version of a compound. For example, in certain embodiments it can be desirable to include Blend 61 , a synthetic lime oil that can be obtained, for example, from Millennium Chemicals, Inc. In certain exemplary embodiments, it can be desirable to include a compound that is designated as meeting Food Chemical Codex (FCC), for example, Geraniol Fine FCC or Tetrahydrolinalool FCC, which compounds can be obtained, for example, from Millennium Chemicals, Inc.
[0043] In embodiments of the invention that include at least one blend of compounds of a plant origin, the compounds of plant origin can be tested for their precise chemical composition using, for example, High-Pressure Liquid Chromatography (HPLC), Mass Spectrometry (MS), gas chromatography, or the like.
[0044] The term "about" or "approximately" means within an acceptable error range for the particular value as determined by one of ordinary skill in the art, which will depend in part on how the value is measured or determined, i.e., the limitations of the measurement system, i.e., the degree of precision required for a particular purpose, such as a pharmaceutical formulation. For example, "about" can mean within 1 or more than 1 standard deviations, per the practice in the art. [0045] Alternatively, "about" can mean a range of up to 20%, preferably up to 10%, more preferably up to 5%, and more preferably still up to 1 % of a given value. Alternatively, particularly with respect to biological systems or processes, the term can mean within an order of magnitude, preferably within 5-fold, and more preferably within 2-fold, of a value. Where particular values are described in the application and claims, unless otherwise stated the term "about" meaning within an acceptable error range for the particular value should be assumed.
[0046] The term "substantially," as used herein, means at least about 80%, preferably at least about 90%, more preferably at least about 99%, for example at least about 99.9%. In some embodiments, the term "substantially" can mean completely, or about 100%.
[0047] Embodiments of the invention can include at least one oil, such as, for example, "Superior oil," highly-refined oils, and the like.
[0048] In the case of an animal, human or non-human, the host can also be treated directly by using a formulation of a composition that is delivered orally. For example, a composition can be enclosed within a liquid capsule and ingested.
[0049] Having described the invention in detail, it will be apparent that modifications, variations, and equivalent embodiments are possible without departing the scope of the invention defined in the appended claims. Furthermore, it should be appreciated that all examples in the present disclosure are provided as non-limiting examples. EXAMPLES
[0050] The following non-limiting examples are provided to further illustrate the present invention. It should be appreciated by those of skill in the art that the techniques disclosed in the examples that follow represent approaches the inventors have found function well in the practice of the invention, and thus can be considered to constitute examples of modes for its practice. However, those of skill in the art should, in light of the present disclosure, appreciate that many changes can be made in the specific embodiments that are disclosed and still obtain a like or similar result without departing from the spirit and scope of the invention.
[0051] Various exemplary compositions containing plant essential oils have been prepared and tested for efficacy against different targets. The following examples provide details of exemplary compositions. As disclosed herein, it is within the scope of the present invention to vary the concentrations of components of each composition within useful ranges. Accordingly, these specific compositions are merely representative of certain embodiments of the invention.
EXAMPLE 1
[0052] Preparation of Test Composition.
[0053] The following amounts were used to make 20Og of this embodiment (Example Formulation 1 of Table 1 ) of the invention:
Ingredients Qty.
Citronella Oil 0.2g Light Liquid Paraffin 6.Og
Cetomacragol Emulsifying Wax 20.Og
Butylated hydroxy Tulune 0.2g
White Soft Paraffin 12.Og
White Bees Wax 6.Og
Propylene Glycol 4.Og
Methyl Paraben 0.3g
Propyl Paraben 0.10g Cresmer RH 40 (Hydrogenated
Castor Oil) 10.0g
Carbopol Altraz-21 0.4g
Thethanolamine 0.2g
Vitamin E Acetate 0.04g
Disodium EDTA 0.02g
Tetrahydrolinalool 1 .3Og
D-limonene 0.88g
Camphene 0.96g
Lime Oil 410 6.8g
Purified Water 130.5g
[0054] This embodiment of the invention is prepared at 15°C.
EXAMPLE 2
[0055] Preparation of Test Composition.
[0056] The following amounts were used to make 20Og of this embodiment (Example Formulation 19 of Table 1 ) of the invention:
Ingredients Qty.
Citronella Oil 0.2g
Light Liquid Paraffin 6.Og
Cetomacragol Emulsifying Wax 20.Og
Butylated hydroxy Tulune 0.2g
White Soft Paraffin 12.Og
White Bees Wax 6.Og Propylene Glycol 4.Og
Methyl Paraben 0.3g
Propyl Paraben 0.1 Og Cresmer RH 40 (Hydrogenated
Castor Oil) 10.0g
Carbopol Altraz-21 0.4g
Thethanolamine 0.2g
Vitamin E Acetate 0.04g
Disodium EDTA 0.02g
LFO 1.3Og
D-limonene 0.88g
Thyme Oil White 0.96g
Lime Oil 410 6.8g
Purified Water 130.5g
[0057] This embodiment of the invention was prepared at a temperature significantly reduced relative to the ambient temperature.
EXAMPLE 3
[0058] Preparation of Test Composition.
[0059] The following amounts are used to make 20Og of this embodiment (Example Formulation 26 of Table 1 ) of the invention:
Ingredients Qty.
Citronella Oil 0.4g
Light Liquid Paraffin 6.Og
Cetomacragol Emulsifying Wax 20.Og
Butylated hydroxy Tulune 0.2g
White Soft Paraffin 12.Og
White Bees Wax 6.Og
Propylene Glycol 4.Og
Methyl Paraben 0.3g
Propyl Paraben 0.10g
Cresmer RH 40 (Hydrogenated 10.0g Castor Oil)
Carbopol Altraz-21 0.4g
Triethanolamine 0.2g
Vitamin E Acetate 0.04g
Disodium EDTA 0.02g
Triethyl citrate 2.6Og
D-limonene 1 -72g
Carvacrol 1 .92g
Lime Oil 410 13.6g
Purified Water 120.5g
[0060] This embodiment of the invention is prepared at 100C.
EXAMPLE 4
[0061] Repellent Effect of Test Compositions on Mosquitoes.
[0062] Oral Delivery
[0063] Hairless or shaved mice and guinea pigs are used to test the repellent effect of compositions delivered orally. The test composition is administered orally to about 10 rodents. A control substance, such as mineral oil, is administered orally to about 10 rodents. After approximately 30 minutes, each rodent is placed in an enclosed container. About 20 mosquitoes are introduced to each container. Each container is observed for approximately 1 hour. The time that each insect spends on the rodent is recorded and number of lesions caused by the insect on the skin of the rodent is recorded. The insects spend less time on rodents receiving the test compositions than on the rodents receiving the control substance. The rodents receiving the test compositions receive fewer lesions than the rodents receiving the control substances. [0064] Topical Delivery
[0065] Hairless or shaved mice and guinea pigs are used to test the repellent effect of test compositions delivered topically. The test compositions are administered topically to the skin of about 10 rodents. A control substance, such as mineral oil, is administered topically to the skin of about 10 rodents. After approximately 30 minutes, each rodent is placed in an enclosed container. About 20 mosquitoes are introduced to each container. Each container is observed for approximately 1 hour. The time that each insect spends on the rodent is recorded and number of lesions caused by the insect on the skin of the rodent is recorded. The insects spend less time on rodents receiving the test compositions than on the rodents receiving the control substance. The rodents receiving the test compositions receive fewer lesions than the rodents receiving the control substances.
EXAMPLE 5
[0066] Repellent Effect of Test Compositions on Mosquitoes.
[0067] About three cages are each stocked with about 100 southern house mosquitoes (culex quinquefasciatus), which are about 7 to 10 days-old. The mosquitoes are starved for about 12 hours. Each cage is supplied with four containers, each filled with cotton that has been soaked with sugar water.
[0068] Three of the four containers are treated randomly with about 1 ml_ of the composition being tested, while the remaining container serves as an untreated control. The containers are positioned in the four opposing corners of each cage and landing counts are conducted at about 0, 1 , 2, 4, and 6 hour intervals following addition of the compositions being tested to the respective containers. The containers are removed from the cage between exposure intervals. Each exposure interval lasts for about 5 minutes.
EXAMPLE 6
[0069] Methods of Testing Repellent Effect and Pesticidal Effect of Compositions Containing Plant Essential Oils on Red Ants.
[0070] Pesticidal effect of test compositions containing plant essential oils on red ants is tested in the following manner. A paper disk is treated with about 20 uL of each of the composition being tested and the treated disks are each placed in a vial. An untreated paper disk is placed in a control vial. Also, a paper disk is treated with about 20 uL 100% DEET and placed in a vial to compare the pesticidal effect of the test compositions to that of DEET, a known commercial insect control agent. About three red ants are introduced into each vial and the openings to the vials are closed with cotton to prevent the insects from escaping. The insects are exposed to the compositions for about one hour or less and mortality is recorded.
[0071] Repellent effect of test compositions containing plant essential oils on red ants is tested in the following manner. A paper disk is treated with about 200 uL of each composition and placed in a dish. An untreated paper disk is placed in a control dish. Also, a paper disk is treated with about 200 uL 100% DEET and placed in a dish to compare the repellent effect of the compositions to that of DEET. Red ants are introduced into each dish. Insect behavior and number of visits to the treated paper disk are monitored for about 5 minutes. The number of visits by a red ant to the paper disk is recorded.
[0072] Residuality, with regard to pesticidal effect and repellent effect, is tested by treating a paper disk with the composition being tested, keeping the treated paper disk under laboratory conditions for a predetermined period of time (e.g., 0 min, 6 hours, 1 day, 3 days, 5 days, 7 days), and exposing red ants to the treated paper disk in the above described manners.

Claims

CLAIMSWHAT IS CLAIMED IS:
1. An insect control composition comprising at least two active ingredients and at least three of the following ingredients: lilac flower oil, tetrahydrolinalool, triethyl citrate, limonene, heliotropine, α-pinene, camphene, α-terpinene, carvacrol, thyme oil, paraffin, and petroleum jelly.
2. The composition of claim 1 , comprising at least one essential oil as an active ingredient.
3. The insect control composition of claim 1 , comprising tetrahydrolinalool, limonene, camphene, paraffin, and petroleum jelly.
4. The insect control composition of claim 3, which comprises tetrahydrolinalool at a concentration of 0.1 %-1.0%.
5. The insect control composition of claim 3, which comprises limonene at a concentration of 0.1 %-1.0%.
6. The insect control composition of claim 3, which comprises camphene at a concentration of 0.1 %-1.0%.
7. The insect control composition of claim 1 , comprising tetrahydrolinalool, limonene, thyme oil, paraffin, and petroleum jelly.
8. The insect control composition of claim 7, which comprises tetrahydrolinalool at a concentration of 0.1 %-1.0%.
9. The insect control composition of claim 7, which comprises limonene at a concentration of 0.1 %-1.0%.
10. The insect control composition of claim 7, which comprises thyme oil at a concentration of 0.1 %-1.0%.
1 1. The insect control composition of claim 1 , comprising lilac flower oil, limonene, α-pinene, paraffin, and petroleum jelly.
12. The insect control composition of claim 1 1 , which comprises lilac flower oil at a concentration of 0.1 %-1.0%.
13. The insect control composition of claim 1 1 , which comprises limonene at a concentration of 0.1 %-1.0%.
14. The insect control composition of claim 1 1 , which comprises α-pinene at a concentration of 0.1 %-1.0%.
15. The insect control composition of claim 1 , comprising triethyl citrate, limonene, thyme oil, paraffin, and petroleum jelly.
16. The insect control composition of claim 15, which comprises triethyl citrate at a concentration of 0.1 %-1.0%.
17. The insect control composition of claim 15, which comprises limonene at a concentration of 0.1 %-1.0%.
18. The insect control composition of claim 15, which comprises thyme oil at a concentration of 0.1 %-1.0%.
19. The insect control composition of claim 1 , comprising tetrahydrolinalool, limonene, α-terpinene, paraffin, and petroleum jelly.
20. The insect control composition of claim 19, which comprises tetrahydrolinalool at a concentration of 0.1 %-1.0%.
21. The insect control composition of claim 19, which comprises limonene at a concentration of 0.1 %-1.0%.
22. The insect control composition of claim 19, which comprises α-terpinene at a concentration of 0.1 %-1.0%.
23. The insect control composition of claim 1 , comprising heliotropine, limonene, thyme oil, paraffin, and petroleum jelly.
24. The insect control composition of claim 23, which comprises heliotropine at a concentration of 0.1 %-1.0%.
25. The insect control composition of claim 23, which comprises limonene at a concentration of 0.1 %-1.0%.
26. The insect control composition of claim 23, which comprises thyme oil at a concentration of 0.1 %-1.0%.
27. The insect control composition of claim 1 , comprising lilac flower oil, limonene, thyme oil, paraffin, and petroleum jelly.
28. The insect control composition of claim 27, which comprises lilac flower oil at a concentration of 0.1 %-1.0%.
29. The insect control composition of claim 27, which comprises limonene at a concentration of 0.1 %-1.0%.
30. The insect control composition of claim 27, which comprises thyme oil at a concentration of 0.1 %-1.0%.
31. The insect control composition of claim 1 , comprising heliotropine, limonene, α-pinene, paraffin, and petroleum jelly.
32. The insect control composition of claim 31 , which comprises heliotropine at a concentration of 0.1 %-1.0%.
33. The insect control composition of claim 31 , which comprises limonene at a concentration of 0.1 %-1.0%.
34. The insect control composition of claim 31 , which comprises α-pinene at a concentration of 0.1 %-1.0%.
35. The insect control composition of claim 1 , comprising triethyl citrate, limonene, carvacrol, paraffin, and petroleum jelly.
36. The insect control composition of claim 35, which comprises triethyl citrate at a concentration of 0.1 %-1.0%.
37. The insect control composition of claim 35, which comprises limonene at a concentration of 0.1 %-1.0%.
38. The insect control composition of claim 35, which comprises carvacrol at a concentration of 0.1 %-1.0%.
39. The insect control composition of claim 1 , comprising tetrahydrolinalool, limonene, α-terpinene, paraffin, and petroleum jelly.
40. The insect control composition of claim 39, which comprises tetrahydrolinalool at a concentration of 0.1 %-1.0%.
41. The insect control composition of claim 39, which comprises limonene at a concentration of 0.1 %-1.0%.
42. The insect control composition of claim 39, which comprises α-terpinene at a concentration of 0.1 %-1.0%.
PCT/US2008/070378 2007-07-17 2008-07-17 Insect repellent composition WO2009012415A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US96106607P 2007-07-17 2007-07-17
US60/961,066 2007-07-17

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8231887B2 (en) 2008-04-11 2012-07-31 Basf Corporation Pesticidal compositions
JP2014161279A (en) * 2013-02-26 2014-09-08 Shiono Koryo Kk Bird repellent

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030091531A1 (en) * 2001-04-11 2003-05-15 Lon Kensek Method and composition for insect and animal control
US20030194454A1 (en) * 1998-07-28 2003-10-16 Bessette Steven M. Pesticidal compositions containing rosemary oil and wintergreen oil
US20050008714A1 (en) * 2003-04-24 2005-01-13 Essam Enan Compositions and methods for controlling insects

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030194454A1 (en) * 1998-07-28 2003-10-16 Bessette Steven M. Pesticidal compositions containing rosemary oil and wintergreen oil
US20030091531A1 (en) * 2001-04-11 2003-05-15 Lon Kensek Method and composition for insect and animal control
US20050008714A1 (en) * 2003-04-24 2005-01-13 Essam Enan Compositions and methods for controlling insects

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8231887B2 (en) 2008-04-11 2012-07-31 Basf Corporation Pesticidal compositions
US8591927B2 (en) 2008-04-11 2013-11-26 Basf Corporation Pesticidal compositions
US9005644B2 (en) 2008-04-11 2015-04-14 Basf Corporation Pesticidal compositions
JP2014161279A (en) * 2013-02-26 2014-09-08 Shiono Koryo Kk Bird repellent

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