Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/58—Meliaceae (Chinaberry or Mahogany family), e.g. Azadirachta (neem)
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION 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
  • A01N65/00—Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION 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
  • A01N65/00—Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
  • A01N65/08—Magnoliopsida [dicotyledons]
  • A01N65/12—Asteraceae or Compositae [Aster or Sunflower family], e.g. daisy, pyrethrum, artichoke, lettuce, sunflower, wormwood or tarragon
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION 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
  • A01N65/00—Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
  • A01N65/08—Magnoliopsida [dicotyledons]
  • A01N65/22—Lamiaceae or Labiatae [Mint family], e.g. thyme, rosemary, skullcap, selfheal, lavender, perilla, pennyroyal, peppermint or spearmint
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION 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
  • A01N65/00—Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
  • A01N65/08—Magnoliopsida [dicotyledons]
  • A01N65/26—Meliaceae [Chinaberry or Mahogany family], e.g. mahogany, langsat or neem
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P33/00—Antiparasitic agents
  • A61P33/14—Ectoparasiticides, e.g. scabicides
• • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
  • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
  • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
  • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
  • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Definitions

• the present invention is in the field of combating arthropod pests.
• the invention relates to a composition of natural origin, based on plant pyrethrum.
• Pyrethrin is known to be a natural insecticidal molecule extracted from oleoresin plants, including chrysanthemum. This contact insecticide kills arthropods causing shock, affecting the nervous system, even at very low doses. Unfortunately, on the one hand, when pyrethrin is included in a formulation, it is very rapidly degraded by UV radiation and microorganisms to such an extent that its action is weakened or even destroyed; on the other hand, it is not stable during storage.
• Neem oil and margosa extract are both derived from the seed of the margosier, also called neem tree.
• the difference between neem oil and margosa extract lies in their extraction process used.
• Virgin neem oil is obtained by simple cold pressing of the seeds, while the margosa extract is obtained in the laboratory, according to various extraction processes of a chemical nature.
• One or more active molecules can then be selected from the extract.
• the main active ingredients of margosa extract are glyceride or free fatty acids, as well as limonoids such as nimbin, salanin and azadirachtin.
• margosa extract can be used to control many species of insects and arachnids, such as silverfish, flies, mosquitoes, ants, mites, etc.
• Margosa extract has a broad spectrum of action in arthropods due to the large number of active constituents that make it up; this results in a reduction of the risk of development of habituation in the said arthropods.
• margosa extract has a long-term mode of action that is to say that the insecticidal effect on targeted arthropods appears after a few hours. This mode of action with residual effect is very beneficial in the fight against certain arthropods for which, the shock effect paralyzes them only, without killing them.
• 3031006 discloses an insecticidal composition
• a plant extract of pyrethrum in the form of essential oil acting on the nervous system a macerate containing formic acid (nettle extract), an asphyxiating agent in the form of oil plant associated with saponin to clog the pores of the epidemic and citrus essential oil to destroy the cuticle of the body of the insect.
• European Patent No. 102540 proposes the addition of benzyl alcohol such as thymol or eugenol, the proportion by weight (pyrethrum / alcohol). is between 50/1 and 10/1.
• Other natural compounds are also used for this purpose, in particular sesame oil (US4983591), salts of specific fatty acids (US4983591), triglycerides and chrysanthemum extract (EP0761097).
• Vetobiol Vétobiol Pest Control Insecticide Habitat 100 mL discloses an insect lotion containing extracts of margosa, geraniol, lavandula hybrida, extract of plant pyrethrum in large quantities.
• WO2008 / 124882 discloses a composition comprising eucalyptus essential oil, 10 to 40% neem oil, lemongrass essential oil, pyrethrum, lavender essential oil.
• WO96 / 39034 discloses a pesticidal composition comprising 0.002 to 0.02% by weight of pyrethrum and neem oil.
• a first object of the present invention is to provide a composition comprising plant pyrethrum whose repulsive action against arthropods is not only improved and preserved, but also extended over time to ensure a residual insecticide effect.
• Another object of the present invention is to provide a plant pyrethrum composition capable of effectively repelling harmful arthropods, particularly ectoparasites, in a human and animal subject.
• Another object of the present invention is to provide a composition comprising plant pyrethrum capable of inducing a curative pesticidal effect when the subject is already infected with pests, as well as a preventive repellent effect to prevent re-infestation of a subject. by the said pests.
• Antephipods harmful means arachnids such as ticks, mites and insects such as flies, mosquitoes, fleas, bed bugs, lice and this, whatever their stage of development.
• Control of pests means the act of either repelling them or killing them, or both simultaneously.
• active agent is meant the synergistic mixture of the active ingredients with repellent and / or pesticidal action; said active agent may be combined with one or more suitable formulation additives during formulation of the composition.
• the present invention therefore has, as a first object, a composition for the control of arthropods that are harmful targets that may infect a human or animal subject to be treated, a composition containing an insecticide and / or insect repellent active agent whose diffusion ensures the control of said harmful arthropods, said composition further comprising a suitable topical application vehicle to allow distribution over at least a part of the body of said subject to be treated, the active agent being constituted by a synergistic mixture of plant pyrethrum, natural extract of margosa and at least one essential oil, characterized in that it comprises:
• the plant pyrethrum is selected from Caucasian pyrethrum, Dalmatian pyrethrum, pesticidal chrysanthemum, natural pyrethrum and pyrethrin.
• the essential oil is selected from the group consisting of cinnamon essential oil, spearmint essential oil, pennyroyal essential oil, mint essential oil, lemongrass essential oil, cedar essential oil, lemongrass essential oil, eucalyptus essential oil, lavandin essential oil, lavender essential oil, palmarosa essential oil or the mixture of these.
• the essential oil is lavandin essential oil or lavender essential oil.
• the essential oil can be replaced, in equal proportion, by their active constituents.
• Said majority constituents may be terpene alcohols such as geraniol, linalool, p-menthane-diol, menthol, terpene esters, aldehydes.
• the natural extract of margosa may be substituted, in equal proportion, by neem oil or its majority active constituents; it is the same with regard to the essential oil.
• the inventors have found that the combination of the three active ingredients, which are the plant pyrethrum, the natural extract of margosa and an essential oil constituting the active agent formulated in a composition makes it possible to obtain a synergistic effect on the skin. the desired effect on the species of parasitic arthropods.
• the ratio between these three ingredients it is possible either to obtain a repellent action or a pesticidal action.
• a high rate of pyrethrum and / or margosa confers a pesticidal effect to the composition while a high level of essential oil confers mainly a repellent effect.
• the active agent of the composition is formulated in liquid form.
• the vegetable pyridine / natural extract weight ratio of margosa / essential oil in the active agent is between 1/1/1 and 1/1/10.
• the composition comprises:
• active agent consisting of a synergistic mixture of vegetable pyrethrum, natural extract of margosa and an essential oil,
• the amount of constituents of the essential oil is between 0.15 and 10% by weight of the composition.
• composition of the present invention thanks to the active agent, has a preventive function coupled with a curative function for the control of arthropods harmful.
• the topical application vehicle may be a liquid, particularly water, a vegetable oil or a solid polymer matrix having been shaped, or in the form of a particular powder or in the form of granules, the active agent being incorporated in said polymer matrix.
• composition may comprise appropriate formulation additives depending on the state of the topical application vehicle used. Indeed, it is possible to incorporate the active agent into the topical application vehicle in the absence of formulation additive.
• the topical application vehicle is a liquid or a semi-liquid
• the active agent is formulated in lotion, spray, emulsion, suspension, liquid concentrate, emulsifiable concentrate, cream, foam, gel , ointment, paste.
• the topical application vehicle is a biodegradable or non-biodegradable solid polymer matrix
• the active agent is incorporated therein, in association or not with one or more formulation additives.
• the biodegradable polymers are chosen from the group formed by polymers of plant origin (agropolymers) based on polysaccharides, starch, celluloses and its derivatives, proteins; biopolyesters of the family of polyhydroxyalkanoates (PHA), polylactides (PLA), polcaprolactones (PCL), polyesteramides (PEA), aliphatic copolyesters (PBSA), aromatic copolyesters (PTAT).
• agropolymers based on polysaccharides, starch, celluloses and its derivatives, proteins
• said synthetic thermoplastic polymer matrix consists of a copolymer of ethylene and vinyl acetate (EVA), the vinyl acetate content of which is between 15 and 60% by weight. weight.
• the synthetic thermoplastic polymer matrix is chosen from the group formed by thermoplastic elastomers (TPE) such as copolyamides and polyamides (PA) of absorbent grades, absorbent grade polyamide amide blockers, starch grafted polyethylenes; polyvinyl chlorides; vulcanized thermoplastics; thermoplastic polyurethanes based on esters or ethers; styrenic polymers such as SIS, SEBS or a mixture of all these polymers.
• TPE thermoplastic elastomers
• PA copolyamides and polyamides
• PA polyamides
• styrenic polymers such as SIS, SEBS or a mixture of all these polymers.
• the solid polymer matrix is a particulate powder of mineral or synthetic origin.
• thermoplastic polymer matrix said matrix is shaped by plastics techniques well known to those skilled in the art, namely by extortion, by injection molding, by coating or by thermopressing.
• the polymer matrix is a thermoset which is a crosslinked polyurethane based on isocyanate and polyols or a polyurea based on isocyanate and polyamine.
• the crosslinked polyurethane is obtained from a liquid or liquid rendered polyol resin and a liquid or liquid isocyanate and then formed by casting.
• the crosslinked polyurea is obtained from a liquid polyamine resin or made liquid and a liquid isocyanate or made liquid and then shaped by casting.
• the isocyanate is chosen from the group formed by isocyanates with at least 2 functionalities, of aromatic or aliphatic structure.
• TDI toluene diisocyanate
• HDI hexamethylene diisocyanate
• MDI diphenylmethylene diisocyanate
• H12MDI dicyclohexylmethane diisocyanate
• IPDI isophorone diisocyanate
• NDI naphthalene diisocyanate
• TODI O-tolidine diisocyanate
• PPDI para-phenylene diisocyanate
• the polyol resin is chosen from that having at least 2 long-chain or short-chain hydroxyl functionalities, based on polyesters, polyethers, polythioethers, polyacetals, polycarbonates, polyesteramides, naturally hydroxylated or modified vegetable oils. or the mixture of these.
• the polyamines are those having at least 2 amino functional groups, chosen from polyetheramines, aliphatic or aromatic.
• additives for formulation of the composition is chosen as a function of the final dosage form (eg cream, lotion, gel, etc.) or of solid polymer matrix (eg necklace, bracelet, patch, medallion, etc.).
• the formulation additives may be chosen from water, vegetable oils, a surfactant, an emulsifier, an antioxidant, a stabilizer, a thickener, a foaming agent, a film-forming agent, a preservative, an anti-UV, inert fillers of mineral origin in the form of powder, a gelling agent, a colorant, a synthetic or natural fragrance or a mixture thereof.
• the present invention has, a second object, a method for the control of arthropods that are harmful targets that may infect a human or animal subject to be treated, a method according to which a composition is applied to at least a part of the body of said subject, said composition which contains an insecticidal and / or insect repellent active agent, furthermore comprises a suitable topical application vehicle, the active agent being constituted by a synergistic mixture of vegetable pyrethrum, natural extract of margosa and less an essential oil, characterized in that said composition comprises:
• the plant pyrethrum may be selected from Caucasian pyrethrum, Dalmatian pyrethrum, pesticidal chrysanthemum, natural pyrethrum and pyrethrin.
• the essential oil can be selected from the group consisting of cinnamon essential oil, spearmint essential oil, pennyroyal essential oil, essential mint of field mint lemongrass essential oil, cedar essential oil, lemongrass essential oil, eucalyptus essential oil, lavandin essential oil, lavender essential oil, palmarosa essential oil or the mixture thereof.
• the ratio of vegetable pyrethrum / natural extract of margosa / essential oil in the active agent is between 1/1 / 1 and 1/1/0.
• the topical application vehicle can be a liquid or a semi-liquid in which the active agent is formulated in lotion, spray, emulsion, suspension, liquid concentrate, emulsifiable concentrate, cream, foam, gel, ointment, paste.
• the topical application vehicle may be a solid matrix chosen from biodegradable polymers, synthetic thermoplastic polymers, cast polyuredian thermosets, particulate powder of mineral or synthetic origin.
• Example 1 Composition containing an active agent according to the invention for the control of fleas and ticks in a pet.
• Ingredients Function Ratio Active Ingredient Quantity (%) Composition containing an active agent according to the invention for the control of fleas and ticks in a pet.
• Table 1 formulation of a repellent anti-tick and anti-tick ticking composition
• Table 2 formulation of a repellent anti-flea and anti-tick composition whose vehicle is an EVA matrix
• the air bubbles through the pot filled with distilled water to be moistened then passes through the pot containing the composition to be tested or control before entering the olfactometer in the center of which it is sucked.
• About 20 chips are introduced in the center of the olfactometer, then every 30 seconds for 20 minutes, the number of chips in each arm is counted.
• the cumulative total number of chips for each of the two odors makes it possible to calculate a behavioral index according to the formula I- (TC) / (T + C) with T the cumulative total number of chips in both arm containing the odor test and C the cumulative total number of fleas in both arms containing the odor control.
• This index varies from -1 (repellent) to + / (attractive).
• the validity of the behavioral effect is statistically verified by a Mann-Whitney test through to software R. The manipulation is repeated six times by alternating the positions of the test pots and controls to cover all six different possible combinations.
• Table 3 Effect on the repellency of the lotion of Table 1 with respect to fleas
• the behavioral index measured was less than 0, giving a mean index significantly lower than this threshold value.
• the synergistic combination of the ingredients of the active agent constituted by the vegetable pyrethrum, the margosa extract and the lavandin essential oil of the composition of the present invention formulated in lotion significantly repels the fleas.
• nymphs of stage IV Ixodes nâmis (Linnaeus, 1758) (Acari: Ixodidae) are used.
• the study was conducted according to the protocol inspired by the publication of Dautel et al. (999).
• a filter paper with or without the lotion to be tested (Table 1: about 0.1 ml) is fixed on a balloon filled with hot water.
• a rod is placed horizontally about 1 to 2 mm in front of the filter paper and a tick is deposited about 2 cm from its end.
• Three behavioral steps are then noted: the tick walks to the end of the stem (walfi), clings to the filter paper (clinch) and moves on the filter paper without dropping (stay).
• Replicas are made for the control and lotion recorded in Table 1.
• the Chi square statistical test is applied via the R software, in order to compare the significance of the responses between the test and the control and thus statistically evaluate the response. repulsive efficacy of the composition according to the invention.
• composition according to the present invention formulated in lotion has demonstrated a good repulsive activity against ticks, hang (clin) and stay (stay) on the stimulus in the presence of the pipette lotion being significantly reduced compared to control (Table 4, Chi square test, ⁇ ⁇ 0.0 ⁇ ).
• composition according to the present invention has demonstrated a good repulsive action against fleas and ticks.
• Example 1 The protocol described in Example 1 was also used in this example to test the effect of each of the active ingredients on the chips.
• the evaluation test was performed according to the protocol described by Krober et al. (2013). To summarize the method, approximately 0.1 mL of solution (active ingredient dissolved in vegetable oil) to be tested is applied on a circle (diameter 13 cm) drawn on a sloped glass plate and heated. After 5 minutes, two ticks tested simultaneously are placed on a disk of aluminum (3 cm diameter) positioned in the center of the treated area. The behavior of each tick is then observed: if it rises the glass plate, the solution is considered ineffective whereas if it drops or drops the glass plate, the solution is considered repulsive. Twelve replicas for each solution and control are made and the average percentage of effective repulsion is then calculated.
• Table 5 below shows the results summarizing the tick repellent activity of each of the ingredients of the active agent of the composition of the present invention in solution.
• Table 6 summarizes the rate of the flea repellent effect of each ingredient of the active agent diluted to 5% in the same vegetable oil mentioned in Table 5.
• Table 6 Behavioral index (I) measured on chips against the atmospheric diffusion of the various ingredients of the active agent, diluted to 5% in vegetable oil.
• Example 3 Insecticidal effect of each of the ingredients of the active agent of the composition on fleas.
• the ingredients of the active agent tested for a volume of 500 ⁇ L each, are the vegetable pyrethrum, the essential oil of lavender, the extract of margosa and a lotion containing a mixture of 2.1 ⁇ , of pyrethrum vegetable, 7.7 ⁇ L of lavandin essential oil, 7.7 ⁇ of margosa extract and 482.5 of vegetable oil, ie a total volume of 500 jxL.
• Table 7 Percentage of surviving fleas after 24 hours and 96 hours of exposure.
• insecticidal effect of each of the ingredients of the active agent does not appear to be related to the sex of the fleas. While 92% ⁇ 1.2% of fleas survive after 24 hours (control), it is observed that less than 20% survive in the presence of one of the three ingredients of the active agent or lotion which is 25 times less concentrated. active agent.

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• 2017
  • 2017-03-15 FR FR1700271A patent/FR3063872B1/fr active Active
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