EP3681462A1 - Oil solution of benzyl alcohol, and use in the prevention and treatment of parasitoses - Google Patents

Oil solution of benzyl alcohol, and use in the prevention and treatment of parasitoses

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Publication number
EP3681462A1
EP3681462A1 EP18782315.8A EP18782315A EP3681462A1 EP 3681462 A1 EP3681462 A1 EP 3681462A1 EP 18782315 A EP18782315 A EP 18782315A EP 3681462 A1 EP3681462 A1 EP 3681462A1
Authority
EP
European Patent Office
Prior art keywords
composition according
composition
benzyl alcohol
esters
oily
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
EP18782315.8A
Other languages
German (de)
French (fr)
Inventor
Nadine Pagnotta
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Invictus
Original Assignee
Invictus
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 Invictus filed Critical Invictus
Publication of EP3681462A1 publication Critical patent/EP3681462A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • 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
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • A61K9/0017Non-human animal skin, e.g. pour-on, spot-on
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/02Preparations for cleaning the hair

Definitions

  • the present invention relates to the prevention and treatment of parasitosis, in particular the fight against head lice, nits, fleas, demodex, chiggers and scabies.
  • the invention relates in particular to a particular oily solution very effective in the fight against these parasites.
  • Parasitic diseases are a real public health problem that can affect everyone. Often non-serious for health, external parasites can nevertheless be very disabling for humans or animals that are affected. This is particularly the case with fleas, demodex, gall, chiggers and lice.
  • the demodex is a genus of mites of the family Demodicidae. Some species are naturally part of the microflora of human skin or live associated with hair, eyelashes and / or eyebrows. They live in or near the hair follicles of mammals. Although the presence of Demodex is generally benign, it can cause some skin diseases. The researchers explain that Demodex accumulate waste throughout their lives in their abdomen. This waste, which they release at their death, can cause, if the mites are very numerous, redness and inflammation of the skin, eyelids and eyelashes. This disease affects between 5 and 20% of the population. Current treatments involve the application of mercury salt cream increasingly proscribed by health authorities or by corticosteroid preparations to relieve inflammation but no effect on the parasite. There is therefore a need for safe and effective new treatment against this parasitosis acting physically by stifling these parasites.
  • Fleas form the order of the siphonaptera (Siphonaptera, from the Latin sipho "tube"), formerly called Aphaniptera (Aphaniptera). They are holometabolic pterygotic insects, characterized by, among other things, their mouthparts shaped like a piercing-sucking apparatus. They are ectoparasites: current fleas infest mammals (of which the man) and some birds, and live from the blood of their bearers. As it passes easily from one animal to another, it can carry various animal diseases, human or zoonotic. They are also a possible source of allergies.
  • insecticidal shampoos such as organophosphorus compounds such as malathion, permethrins or pyrethrins, combined with a synergistic agent such as piperonyl butoxide, fipronil.
  • Scabies (gall, "gall”, or scabies, “scabies”) is an infectious skin disease caused by a microscopic mite-like parasite (Sarcoptes scabiei). According to the subtype of this parasite, human scabies, specific for humans, and specific scales of other mammals are distinguished. It is a benign contagious disease, which is transmitted by contact and whose main symptom in humans is itching. The lesional profile is that of perivascular dermatitis. Depending on the case, the diagnosis may be made on clinical examination or may require a sample. The treatment uses drugs used orally or cutaneously.
  • the reference product is ivermectin administered orally, which can cause side effects, particularly neurotoxic effects.
  • the chickens designate the larvae of a species of small mite of the Trombiculidae family: Trombicula autumnalis, also called red mullet, harvest or pickle.
  • the larva of this arthropod mite temporarily parasitizes the warm-blooded organisms and causes by its bites itching sometimes important in its host.
  • the itching can be calmed by taking an antihistamine, the need for a topical steroid is more rare and possibly an antibiotic cream in case of risk of superinfection.
  • dogs and cats or other domestic animals are affected, they must also be treated (the veterinarian prescribes, for example, a fipronil-based anti-parasite (0.25%), an oral antihistamine and a local pyrethrum treatment). , permethrin or phosphoric ester).
  • Lice are hematophagous insects that can be responsible for frequent and contagious parasitic diseases called pediculosis or phitiriasis. Three types of lice in particular are responsible for these ectoparasitoses:
  • Pediculus humanus capitis the head lice, responsible for pediculosis of the scalp and pediculosis of the head.
  • the pediculosis of the head is the most widespread. It is a very common endemic condition affecting all countries and all socio-economic backgrounds. It mainly affects children between 5 and 11 years old.
  • the head louse is a small greyish-colored insect that feeds on the host's blood three to five times a day. Their eggs or nits, oval shaped, attach themselves very securely to the hair thanks to the sticky material spumaline secreted by the nits. Each slow is usually glued to a hair, mostly close to the skin.
  • Head lice can not jump or fly and are mostly transmitted by face-to-face contact. They may be present for several months on the scalp without the wearer noticing it, which hampers the implementation of adequate prophylactic measures and promotes transmission.
  • the infestation is usually symptomless for the first three to four weeks, and then itching usually occurs due to the presence of allergenic substances in the saliva of the parasites.
  • the first local treatments that have been developed are insecticide-based products, such as organophosphorus compounds such as malathion, permethrins or pyrethrins, combined with a synergistic agent such as piperonyl butoxide. These treatments, particularly those based on malathion, were considered effective. However, these are very irritating products for the scalp, which also have a strong unpleasant odor and are considered toxic and polluting the environment. In addition their effectiveness decreases with time due to an enzymatic adaptation, so that this type of product is neglected.
  • organophosphorus compounds such as malathion, permethrins or pyrethrins
  • a synergistic agent such as piperonyl butoxide
  • the silicones used are not biodegradable, which is harmful for the environment.
  • Insecticidal products based on siloxanes and fatty acid esters such as those described in patent application EP-1,499,184, are also known. These products work by dissolving the chitin that covers the exoskeleton of the louse, causing it to dehydrate and then die. They are known under the trade name ® Resultz constituted 50% by the Cyclomethicone, highly flammable, and 50% of isopropyl myristate.
  • the object of the invention is to overcome the drawbacks of the prior art, by proposing an easy-to-use solution, inexpensive, without toxic insecticide, non-flammable very effective both against head lice, nits, fleas, chiggers, scarpotes and demodex and also exhibiting preventive properties by exerting a repulsive power.
  • the invention proposes an oily solution constituted at least by an oily dispersing phase in which benzyl alcohol is dispersed.
  • Benzyl alcohol is particularly known for its use as a versatile solvent in the manufacture of inks, paints, lacquers, and epoxy coatings. It is also a precursor of several esters, used in photography (as developer), in the manufacture of soaps, perfumes and as a flavoring agent.
  • Benzyl alcohol at low concentration (about 1%), is also used as a preservative to prevent microbial growth of therapeutic or cosmetic formulations.
  • the present invention proposes the use of benzyl alcohol dispersed in an oil, which avoids all these problems and makes it possible to obtain a very important efficacy pediculicide, lenticide and reinforced repellent, in a single application with great ease of use. especially for children.
  • the composition according to the invention is also effective against fleas, demodex, chiggers and scabies.
  • the subject of the invention is therefore also the use of an oily solution consisting at least of an oily dispersing phase in which benzyl alcohol is dispersed, for topical application to the skin, superficial body growths, mucous membranes or scalp. , in the prevention and treatment of parasitosis in humans or animals.
  • colloidal particles in the sense of the invention means suspended particles whose size is between one nanometer (10-9 m) and ten micrometers.
  • oil or “oily component” or “oily phase” means an oil in which at least one molecule is dispersed.
  • the term "rinse” means the action of rinsing the composition according to the invention present on the hair or the skin without having to add an additional soap or shampoo in addition to the composition.
  • the subject of the invention is therefore a composition in the form of an oily solution constituted at least by an oily dispersing phase in which benzyl alcohol is dispersed.
  • the oily dispersing phase preferably represents between 5 and 95.5% by weight relative to the total weight of the composition.
  • the benzyl alcohol in the composition is preferably present at least 0.5% by weight relative to the total weight of the composition, in particular at least 1%. Even more preferentially, it is between 0.5 and 20% by weight relative to the total weight of the composition, in particular between 1 and 20%.
  • the oily dispersing phase may be any oil suitable for use on the skin and scalp.
  • the oily dispersant phase may be composed of isopropyl myristate and / or a mixture of glycerides of polyethylene glycol esters and / or one or more caprylocapous triglyceride (s) and / or one or more silicone (s) and / or one or more vegetable oil (s) such as olive oil and / or one or more mineral oils such as paraffin.
  • oils such as isopropyl myristate and benzyl alcohol are able to dissolve the chitin of the exoskeleton parasites (lice, fleas, demodex) and nits, which further enhances the effectiveness of the composition.
  • composition according to the invention in addition to the oily dispersing phase and benzyl alcohol, may also contain less surfactant also called surfactant.
  • surfactant also called surfactant.
  • the presence of the surfactant makes it possible to reduce the surface tension of the medium, which facilitates the penetration of the formulation into the parasites, in particular lice and nits, thus contributing to reinforcing the effectiveness of the composition. In addition, it facilitates the rinsability of the composition according to the invention.
  • composition according to the invention is preferably rinsable and the presence of one or more agent (s) surfactant (s) improves the rinsing step of the composition after application.
  • agent (s) surfactant (s) improves the rinsing step of the composition after application.
  • the agent (s) surfactant (s) present in the composition according to the invention may be chosen from anionic surfactants, cationic surfactants, amphoteric surfactants and nonionic surfactants. It may be in particular one or more of the following surfactant (s): carboxylates, sulfuric esters of primary alcohols, sulfonates, cetrimide bromide, lecithin, esters of polyol fatty acids, sucrose esters, polyoxyethylenated fatty acid esters, sorbitan esters, polyoxyethylenesorbitan esters, polyoxyethylenated fatty acid esters, poloxamers, polyethylene glycol ester mixtures and glycerides.
  • the composition comprises as surfactant a mixture of polyethylene glycol esters and glycerides such as PEG-8 caprylic / capric GLYCERIDES (Labrasol ®) or propylene glycol LAURATE (Lauroglycol ®) alone or in combination.
  • PEG-8 caprylic / capric GLYCERIDES Labrasol ®
  • propylene glycol LAURATE Liauroglycol ®
  • these surfactants are liquid, very fluid, and weakly or non-irritating.
  • the surfactants present in the compositions according to the invention are between 10 and 50% by weight relative to the total weight of the composition.
  • the composition comprises:
  • composition according to the invention may also comprise colloidal particles.
  • colloidal particles present in the composition according to the invention have a diameter of between 5 and 100 nm.
  • They may consist of particles of alumina silicon dioxide, clays, silica beads, glass beads, iron oxide, iron silicate, magnesium silicate or titanium dioxide. , alone or in mixtures.
  • the colloidal particles when they are present in the composition according to the invention are preferably in a proportion of 0.1 to 20% by weight relative to the total weight of the composition, in particular between 0.1 and 5%.
  • the colloidal particles further improve the effectiveness of the composition according to the invention, in particular against nits and lice. They agglomerate at the level of spiracles, breathing holes of the nits thus causing their asphyxiation.
  • silica particles because of their negative charge, they have a particular affinity for the components of the chitin of the insects which is positively charged, which explains the particular tropism of the silica particles for the shell of the parasites.
  • the chitin of the carapace of arthropods and thus lice and nits is a polymer of N-acetylglucosamine which has positive charges due to the presence of the amine function.
  • Negatively charged silica particles bind electrostatically to the chitin of arthropods and thus lice and nits obstruct parasite spiracles preventing their breathing thus causing their death.
  • the obstruction of the spiracles of the lice and the nits also inhibits the excretion of the water of the parasites creating an osmotic shock favorable to their death.
  • composition according to the invention may also comprise at least one antioxidant agent such as butylhydroxytoluene, butylhydroxyanisol or ascorbyl palmitate, and / or one or more pediculicidal compounds such as malathion, permethrines and pediculicidal or repulsive plant essences.
  • antioxidant agent such as butylhydroxytoluene, butylhydroxyanisol or ascorbyl palmitate
  • pediculicidal compounds such as malathion, permethrines and pediculicidal or repulsive plant essences.
  • These species can be, for example, aniseed oil, tea tree oil, myrtle oil, lavender oil, neem oil and substances described as growth inhibitors. nits such as Farnesol and Nerolidol.
  • the viscosity of the solution can be adapted to correspond to different forms of application and galenic presentations.
  • the solution may in particular be applied in the form of a lotion or spray.
  • Its viscosity is preferably between 1.00 ⁇ 10 ⁇ 3 and 1.0 mPa.s. (Brookfield LVT viscometer, Cylinder 3, Speed 12 at 20 ° C).
  • the viscosity can reach a gel texture that extends like a styling gel and does not flow into the eyes.
  • the viscosity is preferably between 1.0 and 100 mPa.s. (Brookfield LVT viscometer, Cylinder 3, Speed 12 at 20 ° C).
  • the oil solution of the invention can be gelled, for example by adding siloxane copolymer type components and / or polyamides, such as those sold by the company Croda under the trade name LP20 Oléocraft ®.
  • the oily solution consists of:
  • colloidal particles in particular of colloidal silica
  • the composition according to the invention is stable, transparent, washable with water and very little or no irritant. It is very effective against both head lice, especially head lice, and against nits. It also acts faster than the products of the prior art.
  • composition according to the invention does not require the addition of a complementary preservative, benzyl alcohol also plays this role.
  • the oily solution according to the invention can be obtained by carrying out a process comprising the following steps, preferably at ambient temperature:
  • the process may also comprise a further step, preferably after the other steps, which consists in heating the oily solution to about 50 ° C. and dispersing a gelling agent such as a polysiloxane copolymer and of polyamide, then to cool the preparation.
  • a gelling agent such as a polysiloxane copolymer and of polyamide
  • composition according to the invention may be in different galenical forms such as a lotion, a gel or a shampoo. It may also be incorporated into another composition, in particular in the form of a lotion, gel, shampoo or hair mousse intended to be applied to the scalp and human hair or to the coat of animals.
  • the subject of the invention is also a composition in the form of a lotion, a gel, a shampoo or a hair mousse intended to be applied to the scalp and human hair or to the animal's coat, comprising an oily solution according to the invention.
  • compositions according to the invention alone or incorporated in lotions, gels, shampoos, foams, etc. can be applied to human skin, scalp and human hair, but also to animal fur, especially domestic animals. These include horses, donkeys, poultry, cats, dogs, etc.
  • the oily solutions according to the invention or the compositions containing them may be applied to hair (or hair), dry or moist. They are rinsable with water.
  • the invention makes it possible to combine within the same formulation a pediculicidal product when an infestation is diagnosed by applying the product to dry hair, and a preventive repellent product when an infestation is declared in the environment of the subjects in question. applying in this case the product on wet hair and using shampoo.
  • One method of application is to impregnate the dry hair with an oily solution and rinse the hair simply with water between five minutes and one hour after application.
  • One of the properties of the present invention is to leave a silky hair combable and aesthetically perfect unlike competing products that leave hair rough, greasy and difficult to style.
  • compositions according to the invention have a high dissolution capacity especially vis-à-vis the spumaline, natural glue and strong secreted by the nits that makes it difficult to unhook.
  • the application of the formulations allows easy removal of the nits with the aid of a suitable comb which is an additional advantage over other anti-lice products that make the hair rough and poorly combable.
  • the invention therefore also relates to a composition according to the invention (or any composition including it) for use in topical application to the skin, superficial body growths, mucous membranes, fur or scalp, in the prevention and control of treatment of parasitosis in humans or animals.
  • the invention relates to the use of the composition in the treatment of pediculosis of the head (control and prevention against head lice and nits), but also for the prevention and treatment of demodex, gall and parasitic diseases caused by fleas and chiggers.
  • compositions according to the invention are presented in the tables below.
  • Table 1 Examples of compositions according to the invention.
  • Al A2 A3 formulations are gelled and contain Oléocraft LP20.
  • A4 A5 A6 formulations are liquid.
  • Al A2 A3 A5 A6 formulations contain colloidal silica.
  • Table 2 Examples of compositions according to the invention.
  • the formulations BIL B2 B3 are gelled and contain Oleocraft LP20.
  • the formulations B4 B5 B6 are liquid.
  • Formulations B1 B2 B4 B5 B6 contain colloidal silica.
  • Table 3 Examples of compositions according to the invention.
  • G 1 G 2 G 3 formulations are gelled and contain Oleocraft LP20.
  • Gl G2 L1 L2 formulations contain colloidal silica.
  • Gl G3 L1 L3 formulations contain 1% benzyl alcohol.
  • G2 L2 formulations contain 5% benzyl alcohol.
  • compositions are obtained by the implementation of the following process:
  • the objective is to evaluate the pediculicidal efficacy of Gl G2 G3 L1 L3 L3 samples against a distilled water control and in comparison with the Ulsefia ® product.
  • Gl G2 L1 L2 formulations which contain colloidal particles have also been found to have improved performances compared with formulations G3 and L3 which do not contain them.
  • a 1.5 cm square of fabric carrying a hundred nits is placed in the lid of a petri dish (5.5 cm in diameter).
  • 300 ⁇ l of distilled water or Gl G2 G3 L1 L3 L3 products, the Ulsefia ® product are poured onto the nits so that they are completely covered and the poured compositions diffuse rapidly on the nerve-bearing tissue.
  • tissue squares and their nits are then placed on a washer of filter paper, moistened with ⁇ of distilled water, lining the bottom of the petri dish.
  • the petri dishes are placed in an oven at 28 ° C and 60% relative humidity for 5 and 15 minutes, then washed and rinsed with distilled water before being deposited on a new filter paper washer.
  • Petri dishes are placed in an oven at 28 ° C and 60% relative humidity for a fortnight (until hatching nits).
  • Nits are observed from the 6th day until I5 th day to note outbreaks and accounted for. Whenever possible, the hatched lice are recovered and fed.
  • the products of the present invention show a remarkable activity for all the formulations G1 G2 G3 L1 L2 L3.

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  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
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  • Dermatology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Pest Control & Pesticides (AREA)
  • Engineering & Computer Science (AREA)
  • Dispersion Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

The invention relates to a composition in the form of an oil solution which consists, at least, of an oil dispersion phase with benzyl alcohol dispersed therein, and to the use thereof in topical application to the skin, cutaneous appendages, fur, mucous membranes or scalp, in the prevention and treatment of parasitoses in humans or animals.

Description

SOLUTION HUILEUSE D'ALCOOL BENZYLIQUE ET UTILISATION DANS LA PREVENTION ET  OIL SOLUTION OF BENZYL ALCOHOL AND USE IN THE PREVENTION AND
LE TRAITEMENT DES PARASITOSES  TREATMENT OF PARASITOSES
La présente invention concerne la prévention et le traitement des parasitoses, en particulier la lutte contre les poux de tête, les lentes, les puces, les demodex, les aoûtats et la gale. L'invention se rapporte en particulier à une solution huileuse particulière très efficace dans la lutte contre ces parasites. The present invention relates to the prevention and treatment of parasitosis, in particular the fight against head lice, nits, fleas, demodex, chiggers and scabies. The invention relates in particular to a particular oily solution very effective in the fight against these parasites.
Les parasitoses sont un vrai problème de santé publique pouvant concerner tout le monde. Souvent sans gravité pour la santé, les parasitoses externes peuvent néanmoins être très invalidantes pour les êtres humains ou les animaux qui sont touchés. C'est le cas en particulier des puces, du demodex, de la galle, des aoûtats et des poux. Parasitic diseases are a real public health problem that can affect everyone. Often non-serious for health, external parasites can nevertheless be very disabling for humans or animals that are affected. This is particularly the case with fleas, demodex, gall, chiggers and lice.
Le demodex est un genre d'acariens de la famille des Demodicidae. Certaines espèces font naturellement partie de la microflore de la peau humaine ou vivent associées aux cheveux, cils et/ou sourcils. Ils vivent dans ou à proximité des follicules pileux des mammifères. Si la présence du Demodex est généralement bénigne, elle peut toutefois être à l'origine de certaines maladies de peau. Les chercheurs expliquent que les Demodex accumulent, tout au long de leur vie, des déchets dans leur abdomen. Ces déchets, qu'ils libèrent à leur mort, peuvent provoquer, si les acariens sont très nombreux, des rougeurs et des inflammations de la peau, des paupières et des cils. Cette maladie touche entre 5 et 20% de la population. Les traitements actuels font appel à l'application de crème à base de sels de mercure de plus en plus proscrits par les autorités sanitaires ou par des préparations à base de corticoïdes pour soulager l'inflammation mais sans effet sur le parasite. Il existe donc un besoin de nouveau traitement sûr et efficace contre cette parasitose agissant physiquement en étouffant ces parasites.  The demodex is a genus of mites of the family Demodicidae. Some species are naturally part of the microflora of human skin or live associated with hair, eyelashes and / or eyebrows. They live in or near the hair follicles of mammals. Although the presence of Demodex is generally benign, it can cause some skin diseases. The researchers explain that Demodex accumulate waste throughout their lives in their abdomen. This waste, which they release at their death, can cause, if the mites are very numerous, redness and inflammation of the skin, eyelids and eyelashes. This disease affects between 5 and 20% of the population. Current treatments involve the application of mercury salt cream increasingly proscribed by health authorities or by corticosteroid preparations to relieve inflammation but no effect on the parasite. There is therefore a need for safe and effective new treatment against this parasitosis acting physically by stifling these parasites.
Les puces forment l'ordre des siphonaptères (Siphonaptera, du latin sipho « tube »), anciennement dénommés aphaniptères (Aphaniptera). Ce sont des insectes ptérygotes holométaboles, caractérisés entre autres par leurs pièces buccales conformées en un appareil piqueur-suceur. Elles sont ectoparasites : les puces actuelles infestent les mammifères (dont l'homme) et quelques oiseaux, et vivent du sang de leurs porteurs. Comme elle passe facilement d'un animal à l'autre, elle peut véhiculer diverses maladies animales, humaines ou zoonotiques. Elles sont aussi une source possible d'allergies. Fleas form the order of the siphonaptera (Siphonaptera, from the Latin sipho "tube"), formerly called Aphaniptera (Aphaniptera). They are holometabolic pterygotic insects, characterized by, among other things, their mouthparts shaped like a piercing-sucking apparatus. They are ectoparasites: current fleas infest mammals (of which the man) and some birds, and live from the blood of their bearers. As it passes easily from one animal to another, it can carry various animal diseases, human or zoonotic. They are also a possible source of allergies.
Les traitements actuels font appel à des shampoing à base d'insecticides tels que des organophosphorés comme le malathion, des perméthrines ou des pyréthrines, associés à un agent synergique tel que le butoxyde de pipéronyle, le fipronil.  Current treatments use insecticidal shampoos such as organophosphorus compounds such as malathion, permethrins or pyrethrins, combined with a synergistic agent such as piperonyl butoxide, fipronil.
Toutefois, il s'agit de produits qui sont considérés comme toxiques et polluants pour l'environnement. Certains d'entre eux notamment le fipronil entraînent chez les animaux de compagnie des troubles comportementaux.  However, these are products that are considered toxic and polluting the environment. Some of them, including fipronil, cause behavioral problems in pets.
La gale ou scabiose (de galla, « galle », ou de scabies, « gale ») est une maladie infectieuse de la peau causée par un parasite de type acarien microscopique, le sarcopte (Sarcoptes scabiei). Selon le sous-type de ce parasite, on distingue la gale humaine, spécifique de l'Homme, et les gales spécifiques d'autres mammifères. Il s'agit d'une affection contagieuse bénigne , qui se transmet par le contact et dont le principal symptôme chez l'Homme est la démangeaison. Le profil lésionnel est celui d'une dermatite périvasculaire. Le diagnostic peut selon les cas être établi à l'examen clinique ou nécessiter un prélèvement. Le traitement fait appel à des médicaments utilisés par voie orale ou cutanée. Scabies (gall, "gall", or scabies, "scabies") is an infectious skin disease caused by a microscopic mite-like parasite (Sarcoptes scabiei). According to the subtype of this parasite, human scabies, specific for humans, and specific scales of other mammals are distinguished. It is a benign contagious disease, which is transmitted by contact and whose main symptom in humans is itching. The lesional profile is that of perivascular dermatitis. Depending on the case, the diagnosis may be made on clinical examination or may require a sample. The treatment uses drugs used orally or cutaneously.
Ces traitements sont à base de molécules pharmacologiquement actives et non dépourvues d'effets secondaires ce qui démontre l'intérêt d'un traitement agissant de façon physique sur le parasite. Le produit de référence est l'ivermectine administré par voie orale qui peut entraîner des effets secondaires notamment neurotoxiques.  These treatments are based on pharmacologically active molecules and not devoid of side effects which demonstrates the interest of a treatment acting physically on the parasite. The reference product is ivermectin administered orally, which can cause side effects, particularly neurotoxic effects.
Les aoûtats désignent la larve d'une espèce de petit acarien de la famille des Trombiculidés : Trombicula autumnalis, appelé aussi rouget, vendangeon ou vendangeron.  The chickens designate the larvae of a species of small mite of the Trombiculidae family: Trombicula autumnalis, also called red mullet, harvest or pickle.
La larve de cet arthropode acarien parasite temporairement les organismes à sang chaud et occasionne par ses piqûres des démangeaisons parfois importantes chez son hôte. The larva of this arthropod mite temporarily parasitizes the warm-blooded organisms and causes by its bites itching sometimes important in its host.
Il est vecteur de plusieurs maladies, et de nombreuses espèces animales sauvages ou domestiques, dont le chat, le chien, le lapin, la vache et le cheval, semblent pouvoir servir de réservoir à ce parasite.  It is a vector of several diseases, and many wild or domestic animal species, including the cat, the dog, the rabbit, the cow and the horse, seem to be able to serve as a reservoir for this parasite.
Les démangeaisons (sur l'homme) peuvent être calmées par la prise d'un antihistaminique, la nécessité d'un stéroïde topique est plus rare et éventuellement une crème antibiotique en cas de risque de surinfection. Si des chiens et chats ou autres animaux domestiques sont touchés, ils doivent aussi être soignés (le vétérinaire prescrit par exemple un anti-parasitaire à base de fipronil (à 0,25 %), un antihistaminique oral et un traitement local à base de pyrèthre, perméthrine ou d'ester phosphorique). Toutefois, il s'agit de produits qui sont considérés comme toxiques et polluants pour l'environnement. Certains d'entre eux notamment le fipronil entraînent chez les animaux de compagnie des troubles comportementaux. The itching (on the man) can be calmed by taking an antihistamine, the need for a topical steroid is more rare and possibly an antibiotic cream in case of risk of superinfection. If dogs and cats or other domestic animals are affected, they must also be treated (the veterinarian prescribes, for example, a fipronil-based anti-parasite (0.25%), an oral antihistamine and a local pyrethrum treatment). , permethrin or phosphoric ester). However, these are products that are considered toxic and polluting the environment. Some of them, including fipronil, cause behavioral problems in pets.
Il existe par conséquent également un besoin pour des produits capables d'agir physiquement sur les scarpotes, les aoûtats et les puces et sans effets néfastes tant pour les sujets traités que pour l'environnement.  There is therefore also a need for products capable of acting physically on scarpotes, chiggers and fleas and without any adverse effects for both the treated subjects and the environment.
Les poux sont des insectes hématophages pouvant être responsables de maladies parasitaires fréquentes et contagieuses appelées pédiculoses ou phitiriases. Trois types de poux en particulier sont responsables de ces ectoparasitoses : Lice are hematophagous insects that can be responsible for frequent and contagious parasitic diseases called pediculosis or phitiriasis. Three types of lice in particular are responsible for these ectoparasitoses:
- Pediculus humanus corporis, le pou de corps, vivant dans les coutures et les plis de vêtements, ne passant sur la peau que pour se nourrir, responsable de pédiculoses corporelles,  - Pediculus humanus corporis, the body louse, living in the seams and folds of clothing, passing on the skin only for food, responsible for body pediculosis,
- Phtirius pubis, le pou du pubis et des autres régions du corps couvertes de poils grossiers ou morpion, responsable de phitiriases pubiennes, et  - Phtirius pubis, pubic louse and other areas of the body covered with coarse hairs or tinea, responsible for pubic phitiriasis, and
- Pediculus humanus capitis : le pou de tête, responsable de pédiculoses du cuir chevelu et ou pédiculose de la tête.  - Pediculus humanus capitis: the head lice, responsible for pediculosis of the scalp and pediculosis of the head.
La pédiculose de la tête est la plus répandue. C'est une affection endémique très fréquente touchant tous les pays et tous les milieux socio-économiques. Elle affecte surtout les enfants entre 5 et 11 ans. The pediculosis of the head is the most widespread. It is a very common endemic condition affecting all countries and all socio-economic backgrounds. It mainly affects children between 5 and 11 years old.
Le pou de tête est un petit insecte de couleur grisâtre qui se nourrit du sang de son hôte trois à cinq fois par jour. Leurs œufs ou lentes, de forme ovale, se fixent très solidement aux cheveux grâce à la spumaline matière collante sécrétée par les lentes. Chaque lente est généralement collée à un cheveu, la plupart du temps tout près de la peau.  The head louse is a small greyish-colored insect that feeds on the host's blood three to five times a day. Their eggs or nits, oval shaped, attach themselves very securely to the hair thanks to the sticky material spumaline secreted by the nits. Each slow is usually glued to a hair, mostly close to the skin.
Les poux de tête ne peuvent ni sauter, ni voler et se transmettent surtout par un contact tête à tête. Ils peuvent être présents pendant plusieurs mois sur le cuir chevelu sans que le porteur ne s'en rende compte, ce qui nuit à la mise en place de mesures prophylactiques adéquates et favorise la transmission. L'infestation est habituellement sans symptôme durant les trois à quatre premières semaines, puis des démangeaisons apparaissent généralement, dues à la présence de substances allergènes dans la salive des parasites. Head lice can not jump or fly and are mostly transmitted by face-to-face contact. They may be present for several months on the scalp without the wearer noticing it, which hampers the implementation of adequate prophylactic measures and promotes transmission. The infestation is usually symptomless for the first three to four weeks, and then itching usually occurs due to the presence of allergenic substances in the saliva of the parasites.
Dans le traitement des pédiculoses de la tête plusieurs approches peuvent être utilisées. II est notamment possible de peigner les cheveux pour éliminer les poux qui meurent rapidement une fois qu'ils sont séparés de leur hôte, mais cette solution ne permet d'éliminer qu'une partie des poux et ne peut aucunement être utilisée seule, sauf pour les enfants en très bas âge.  In the treatment of pediculosis of the head several approaches can be used. It is particularly possible to comb the hair to eliminate lice that die quickly once they are separated from their host, but this solution eliminates only part of the lice and can not be used alone, except for children at a very young age.
L'approche la plus courante consiste à appliquer un insecticide sur le cuir chevelu.  The most common approach is to apply an insecticide to the scalp.
Les premiers traitements locaux qui ont été développés sont des produits à base d'insecticides, tels que des organophosphorés comme le malathion, des perméthrines ou des pyréthrines, associés à un agent synergique tel que le butoxyde de pipéronyle. Ces traitements, notamment ceux à base de malathion étaient considérés efficaces. Toutefois, il s'agit de produits très irritants pour le cuir chevelu, qui présentent en outre une odeur forte désagréable et qui sont considérés comme toxiques et polluants pour l'environnement. En outre leur efficacité diminue avec le temps du fait d'une adaptation enzymatique, si bien que ce type de produit est délaissé. The first local treatments that have been developed are insecticide-based products, such as organophosphorus compounds such as malathion, permethrins or pyrethrins, combined with a synergistic agent such as piperonyl butoxide. These treatments, particularly those based on malathion, were considered effective. However, these are very irritating products for the scalp, which also have a strong unpleasant odor and are considered toxic and polluting the environment. In addition their effectiveness decreases with time due to an enzymatic adaptation, so that this type of product is neglected.
Il existe également des traitements locaux à base de siloxanes notamment à base de diméticone, comme ceux décrit dans la demande WO-01/19190. Ces produits agissent en noyant les poux dans une phase huileuse, qui meurent par asphyxie.  There are also local treatments based on siloxanes including dimeticone-based, such as those described in the application WO-01/19190. These products act by drowning the lice in an oily phase, which die by asphyxiation.
Néanmoins, ces produits ne sont pas suffisamment efficaces en particulier contre les lentes et nécessitent plusieurs applications répétées. En outre ils rendent les cheveux gras, et sont très inflammables.  Nevertheless, these products are not sufficiently effective especially against nits and require several repeated applications. In addition they make the hair greasy, and are very flammable.
Par ailleurs les silicones utilisées ne sont pas biodégradables ce qui est dommageable pour l'environnement.  In addition, the silicones used are not biodegradable, which is harmful for the environment.
On connaît encore des produits insecticides à base de siloxanes et d'esters d'acides gras, tels que ceux décrits dans la demande EP-1.499.184. Ces produits agissent en dissolvant la chitine qui recouvre l'exosquelette du pou, provoquant sa déshydratation puis sa mort. Ils sont connus sous le nom commercial Resultz® constitués à 50% par de la Cyclométhicone, très inflammable, et à 50% par le Myristate d'isopropyle. Insecticidal products based on siloxanes and fatty acid esters, such as those described in patent application EP-1,499,184, are also known. These products work by dissolving the chitin that covers the exoskeleton of the louse, causing it to dehydrate and then die. They are known under the trade name ® Resultz constituted 50% by the Cyclomethicone, highly flammable, and 50% of isopropyl myristate.
Néanmoins, leur efficacité sur les poux adultes est très variable et leur pouvoir sur les lentes n'a pas été établi. En outre, ces produits ne peuvent pas être appliqués chez les enfants de moins de 4 ans et leur utilisation est fastidieuse puisqu'elle nécessite une application sur cheveux secs, un temps de pose d'au moins 8 heures et plusieurs shampoings des cheveux et du cuir chevelu pour être éliminé et diminuer le côté gras de la chevelure. Une nouvelle application, voire deux applications supplémentaires sont nécessaires pour éliminer les lentes écloses après un intervalle de 7 jours. Nevertheless, their effectiveness on adult lice is very variable and their power on nits has not been established. In addition, these products can not be applied in children of less than 4 years and their use is tedious since it requires an application on dry hair, a time of exposure of at least 8 hours and several hair shampoos and scalp to be eliminated and reduce the fat side of the hair. A new application, or two additional applications are needed to eliminate nits that are hatched after an interval of 7 days.
Ces produits rendent également les cheveux gras et sont inflammables.  These products also make the hair greasy and flammable.
Il existe également des formulations de types microémulsion décrites dans la demande FR0955753, cependant ces formulations ne sont totalement efficaces sur les poux qu'après un temps d'une heure ce qui est long par rapport aux demandes actuelles des consommateurs et l'efficacité sur les lentes n'est pas complète. There are also formulations of the microemulsion type described in the application FR0955753, however these formulations are totally effective on lice after a time of one hour which is long compared to current consumer demands and efficiency on slow is not complete.
L'objectif de l'invention est de pallier les inconvénients de l'art antérieur, en proposant une solution facile d'utilisation, peu coûteuse, sans insecticide toxique, non inflammable très efficace à la fois contre les poux de tête, les lentes, les puces, les aoûtats, les scarpotes et les demodex et présentant également des propriétés de prévention en exerçant un pouvoir répulsif.  The object of the invention is to overcome the drawbacks of the prior art, by proposing an easy-to-use solution, inexpensive, without toxic insecticide, non-flammable very effective both against head lice, nits, fleas, chiggers, scarpotes and demodex and also exhibiting preventive properties by exerting a repulsive power.
Pour y répondre, l'invention propose une solution huileuse constituée au moins par une phase dispersante huileuse dans laquelle est dispersée de l'alcool benzylique.  In order to meet them, the invention proposes an oily solution constituted at least by an oily dispersing phase in which benzyl alcohol is dispersed.
L'alcool benzylique est connu en particulier pour son utilisation comme solvant polyvalent dans la fabrication des encres, des peintures, des laques, et des revêtements en résine époxy. C'est aussi un précurseur de plusieurs esters, employé en photographie (comme révélateur), dans la fabrication des savons, des parfums et comme agent de sapidité. Benzyl alcohol is particularly known for its use as a versatile solvent in the manufacture of inks, paints, lacquers, and epoxy coatings. It is also a precursor of several esters, used in photography (as developer), in the manufacture of soaps, perfumes and as a flavoring agent.
L'alcool benzylique, à faible concentration (1% environ), est également utilisé comme un agent conservateur pour prévenir les croissances microbiennes des formulations thérapeutiques ou cosmétiques. Benzyl alcohol, at low concentration (about 1%), is also used as a preservative to prevent microbial growth of therapeutic or cosmetic formulations.
Par ailleurs, l'utilisation de l'alcool benzylique en solution aqueuse à 5% pour la lutte contre les poux chez les enfants de plus de 6 mois et les adultes a déjà été décrite. C'est le cas en particulier du brevet US6793931 qui décrit des formulations aqueuses à base d'alcool benzylique. Cependant ces formulations, commercialisées entre autres sous le nom d'Ulfesia® aux Etats Unis, ne sont pas efficaces sur les lentes et une deuxième application est nécessaire. De plus, l'alcool benzylique est peu soluble dans l'eau (solubilité à 40g/L à 20°C) ce qui signifie que les formulations existantes sont des émulsions dont la stabilité dans le temps est restreinte et dont le procédé de fabrication est complexe. Avantageusement, la présente invention propose d'utiliser de l'alcool benzylique dispersé dans une huile, ce qui évite toutes ces problématiques et permet d'obtenir une efficacité très importante pédiculicide, lenticide et répulsive renforcée, en une seule application avec une grande facilité d'utilisation en particulier pour les enfants. La composition selon l'invention est également efficace contre les puces, les demodex, les aoûtats et la gale. In addition, the use of benzyl alcohol in 5% aqueous solution for the control of lice in children over 6 months and adults has already been described. This is the case in particular of patent US 6793931 which describes aqueous formulations based on benzyl alcohol. However, these formulations, sold inter alia under the name of Ulfesia ® in the United States, are not effective on nits and a second application is necessary. In addition, benzyl alcohol is poorly soluble in water (solubility at 40 g / L at 20 ° C) which means that existing formulations are emulsions whose stability over time is restricted and whose manufacturing process is complex. Advantageously, the present invention proposes the use of benzyl alcohol dispersed in an oil, which avoids all these problems and makes it possible to obtain a very important efficacy pediculicide, lenticide and reinforced repellent, in a single application with great ease of use. especially for children. The composition according to the invention is also effective against fleas, demodex, chiggers and scabies.
L'invention a donc aussi pour objet l'utilisation d'une solution huileuse constituée au moins par une phase dispersante huileuse dans laquelle est dispersée de l'alcool benzylique, en application topique sur la peau, les phanères, les muqueuses ou le cuir chevelu, dans la prévention et le traitement des parasitoses chez l'être humain ou l'animal. The subject of the invention is therefore also the use of an oily solution consisting at least of an oily dispersing phase in which benzyl alcohol is dispersed, for topical application to the skin, superficial body growths, mucous membranes or scalp. , in the prevention and treatment of parasitosis in humans or animals.
L'invention est à présent décrite en détails. The invention is now described in detail.
DÉFINITIONS DEFINITIONS
Dans la présente demande, la forme singulière d'un mot peut comprendre le pluriel, et inversement, à moins que le contexte indique le contraire. Ainsi, les références " un", "une", et "le", "la" comprennent les pluriels de ces termes. Par exemple, la référence à "une solution" ou "une composition" comprend une pluralité de ces "solutions" ou "compositions".  In the present application, the singular form of a word may include the plural, and vice versa, unless the context indicates otherwise. Thus, the references "a", "an", and "the", "the" include the plural of these terms. For example, the reference to "a solution" or "a composition" includes a plurality of such "solutions" or "compositions".
Par « particules colloïdales » au sens de l'invention on entend des particules en suspension dont la taille est comprise entre un nanomètre (10-9 m) et une dizaine de micromètres. Par « phase dispersante huileuse » ou « huile » ou « composant huileux » ou « phase huileuse » au sens de l'invention on entend une huile dans laquelle est dispersée au moins une molécule. By "colloidal particles" in the sense of the invention means suspended particles whose size is between one nanometer (10-9 m) and ten micrometers. For the purposes of the invention, the term "oily dispersing phase" or "oil" or "oily component" or "oily phase" means an oil in which at least one molecule is dispersed.
Par « rinçable » au sens de l'invention on entend l'action de rincer la composition selon l'invention présente sur les cheveux ou la peau sans avoir à ajouter un savon ou un shampoing supplémentaire en plus de la composition.  For the purposes of the invention, the term "rinse" means the action of rinsing the composition according to the invention present on the hair or the skin without having to add an additional soap or shampoo in addition to the composition.
DESCRIPTION DÉTAILLÉE DE L'INVENTION DETAILED DESCRIPTION OF THE INVENTION
L'invention a donc pour objet une composition sous forme d'une solution huileuse constituée au moins par une phase dispersante huileuse dans laquelle est dispersée de l'alcool benzylique.  The subject of the invention is therefore a composition in the form of an oily solution constituted at least by an oily dispersing phase in which benzyl alcohol is dispersed.
La phase dispersante huileuse représente préférentiellement entre 5 et 95,5% en poids par rapport au poids total de la composition. L'alcool benzylique dans la composition est préférentiellement présent à au moins 0,5% en poids par rapport au poids total de la composition, notamment à au moins 1%. Encore plus préférentiellement, il est compris entre 0,5 et 20% en poids par rapport au poids total de la composition, notamment entre 1 et 20%. The oily dispersing phase preferably represents between 5 and 95.5% by weight relative to the total weight of the composition. The benzyl alcohol in the composition is preferably present at least 0.5% by weight relative to the total weight of the composition, in particular at least 1%. Even more preferentially, it is between 0.5 and 20% by weight relative to the total weight of the composition, in particular between 1 and 20%.
La phase dispersante huileuse peut être constituée par toute huile adaptée à une utilisation sur la peau et le cuir chevelu. En particulier, la phase dispersante huileuse peut être composée par du myristate d'isopropyle et/ou un mélange de glycérides d'esters de polyéthylène glycol et/ou un ou plusieurs triglycéride(s) caprylocaprique(s) et/ou un ou plusieurs silicone(s) et/ou une ou plusieurs huile(s) végétale(s) comme l'huile d'olive et/ou une ou plusieurs huiles minérales comme la paraffine. The oily dispersing phase may be any oil suitable for use on the skin and scalp. In particular, the oily dispersant phase may be composed of isopropyl myristate and / or a mixture of glycerides of polyethylene glycol esters and / or one or more caprylocapous triglyceride (s) and / or one or more silicone (s) and / or one or more vegetable oil (s) such as olive oil and / or one or more mineral oils such as paraffin.
La forme particulière de la solution huileuse, combinée à l'action de l'alcool benzylique, permet de noyer et d'asphyxier les parasites, en particulier les poux et les lentes. De plus, certaines huiles, comme le myristate d'isopropyl et l'alcool benzylique sont capables de dissoudre la chitine de l'exosquelette des parasites (poux, puces, demodex) et des lentes ce qui renforce encore l'efficacité de la composition.  The particular form of the oily solution, combined with the action of benzyl alcohol, makes it possible to drown and asphyxiate the parasites, in particular the lice and the nits. In addition, certain oils, such as isopropyl myristate and benzyl alcohol are able to dissolve the chitin of the exoskeleton parasites (lice, fleas, demodex) and nits, which further enhances the effectiveness of the composition.
La composition selon l'invention, en plus de la phase dispersante huileuse et de l'alcool benzylique, peut contenir également moins un agent tensioactif encore appelé surfactant. La présence de l'agent tensioactif permet de diminuer la tension superficielle du milieu ce qui facilite la pénétration de la formulation au sein des parasites, en particulier des poux et des lentes, contribuant ainsi à renforcer l'efficacité de la composition. De plus il permet de faciliter la rinçabilité de la composition selon l'invention.  The composition according to the invention, in addition to the oily dispersing phase and benzyl alcohol, may also contain less surfactant also called surfactant. The presence of the surfactant makes it possible to reduce the surface tension of the medium, which facilitates the penetration of the formulation into the parasites, in particular lice and nits, thus contributing to reinforcing the effectiveness of the composition. In addition, it facilitates the rinsability of the composition according to the invention.
En effet, la composition selon l'invention est préférentiellement rinçable et la présence d'un ou plusieurs agent(s) tensioactif(s) permet d'améliorer l'étape de rinçage de la composition après application. Ainsi, le caractère rinçable de la composition selon l'invention facilite son utilisation en particulier sur le cuir chevelu ou le pelage des animaux, le traitement pouvant être réalisé en une seule étape sans besoin d'appliquer un shampoing additionnel.  Indeed, the composition according to the invention is preferably rinsable and the presence of one or more agent (s) surfactant (s) improves the rinsing step of the composition after application. Thus, the rinsable nature of the composition according to the invention facilitates its use, in particular on the scalp or the fur of animals, the treatment can be carried out in a single step without the need to apply additional shampoo.
Le ou les agent(s) tensioactif(s) présent(s) dans la composition selon l'invention peuvent être choisi(s) parmi les agents tensioactifs anioniques, les agents tensioactifs cationiques, les agents tensioactifs amphotères et les agents tensioactifs non ioniques. Il peut s'agir en particulier d'un ou plusieurs des agent(s) tensioactif(s) suivant(s) : les carboxylates, les esters sulfuriques d'alcools primaires, les sulfonates, le bromure de cétrimide, la lécithine, les esters d'acides gras de polyols, les esters de saccharose, les esters d'acides gras polyoxyéthylénés, les esters du sorbitane, les esters du sorbitane polyoxyéthyénés, les esters d'acide gras polyoxyéthylénés, les poloxamères, des mélanges d'esters de polyéthylène glycol et de glycérides. The agent (s) surfactant (s) present in the composition according to the invention may be chosen from anionic surfactants, cationic surfactants, amphoteric surfactants and nonionic surfactants. It may be in particular one or more of the following surfactant (s): carboxylates, sulfuric esters of primary alcohols, sulfonates, cetrimide bromide, lecithin, esters of polyol fatty acids, sucrose esters, polyoxyethylenated fatty acid esters, sorbitan esters, polyoxyethylenesorbitan esters, polyoxyethylenated fatty acid esters, poloxamers, polyethylene glycol ester mixtures and glycerides.
Préférentiellement la composition comprend comme agent tensioactif un mélange d'esters de polyéthylène glycol et de glycérides comme le PEG-8 CAPRYLIC/CAPRIC GLYCERIDE (Labrasol®) ou le PROPYLENE GLYCOL LAURATE (Lauroglycol®), seuls ou en association. Preferably the composition comprises as surfactant a mixture of polyethylene glycol esters and glycerides such as PEG-8 caprylic / capric GLYCERIDES (Labrasol ®) or propylene glycol LAURATE (Lauroglycol ®) alone or in combination.
Avantageusement ces tensioactifs sont liquides, très fluides, et faiblement voire non irritants. Les agents tensioactifs présents dans la compositions selon l'invention sont compris entre 10 et 50% en poids par rapport au poids total de la composition. Advantageously, these surfactants are liquid, very fluid, and weakly or non-irritating. The surfactants present in the compositions according to the invention are between 10 and 50% by weight relative to the total weight of the composition.
Selon un mode de réalisation particulier de l'invention la composition comprend : According to a particular embodiment of the invention, the composition comprises:
Entre 0,5 et 20%, notamment entre 1 et 20% d'alcool benzylique,  Between 0.5 and 20%, especially between 1 and 20% of benzyl alcohol,
- Entre 10 et 50% d'agent(s) tensioactif(s), et  Between 10 and 50% surfactant (s), and
Entre 5 et 60% de phase dispersante huileuse.  Between 5 and 60% oily dispersant phase.
La composition selon l'invention peut également comprendre des particules colloïdales. Préférentiellement les particules colloïdales présentes dans la composition selon l'invention ont un diamètre compris entre 5 et 100 nm. The composition according to the invention may also comprise colloidal particles. Preferably, the colloidal particles present in the composition according to the invention have a diameter of between 5 and 100 nm.
Elles peuvent être constituées par des particules de dioxyde de silicium d'alumine, d'argiles, des billes de silice, des billes de verre, de l'oxyde de fer, du silicate de fer, du silicate de magnésium ou du dioxyde de titane, seules ou en mélanges.  They may consist of particles of alumina silicon dioxide, clays, silica beads, glass beads, iron oxide, iron silicate, magnesium silicate or titanium dioxide. , alone or in mixtures.
Les particules colloïdales lorsqu'elles sont présentes dans la composition selon l'invention, le sont préférentiellement à raison de 0,1 à 20% en poids par rapport au poids total de la composition, en particulier entre 0,1 et 5%. The colloidal particles when they are present in the composition according to the invention are preferably in a proportion of 0.1 to 20% by weight relative to the total weight of the composition, in particular between 0.1 and 5%.
Avantageusement les particules colloïdales améliorent encore l'efficacité de la composition selon l'invention, en particulier contre les lentes et les poux. Elles s'agglomèrent au niveau des spiracles, orifices respiratoires des lentes provoquant ainsi leur asphyxie.  Advantageously, the colloidal particles further improve the effectiveness of the composition according to the invention, in particular against nits and lice. They agglomerate at the level of spiracles, breathing holes of the nits thus causing their asphyxiation.
S'il s'agit de particules de silice, de par leur charge négative, elles présentent une affinité particulière pour les composant de la chitine des insectes qui est chargée positivement ce qui explique le tropisme particulier des particules de silice pour la carapace des parasites. La chitine de la carapace des arthropodes et donc des poux et des lentes est un polymère de N- acetylglucosamine qui présente des charges positives de par la présence de la fonction aminé. Les particules de silice chargées négativement se fixent par des liaisons électrostatiques sur la chitine des arthropodes et donc des poux et des lentes obstruent les spiracles des parasites empêchant leur respiration provoquant ainsi leur mort. L'obstruction des spiracles des poux et des lentes inhibe également l'excrétion de l'eau des parasites créant un choc osmotique propice à leur mort. If they are silica particles, because of their negative charge, they have a particular affinity for the components of the chitin of the insects which is positively charged, which explains the particular tropism of the silica particles for the shell of the parasites. The chitin of the carapace of arthropods and thus lice and nits is a polymer of N-acetylglucosamine which has positive charges due to the presence of the amine function. Negatively charged silica particles bind electrostatically to the chitin of arthropods and thus lice and nits obstruct parasite spiracles preventing their breathing thus causing their death. The obstruction of the spiracles of the lice and the nits also inhibits the excretion of the water of the parasites creating an osmotic shock favorable to their death.
La composition selon l'invention peut aussi comprendre au moins un agent antioxydant comme le butylhydroxytoluène, le butylhydroxyanisol ou le palmitate d'ascorbyle, et/ou un ou plusieurs composés pédiculicides tels que le malathion, les perméthrines et les essences végétales pédiculicides ou répulsives. Ces essences peuvent être par exemple l'essence d'anis, l'huile de l'arbre à thé, l'essence de myrte, l'essence de lavande, l'huile de neem ainsi que des substances décrites comme inhibiteur de la croissance des lentes comme le Farnesol et le Nérolidol. Il est possible également d'incorporer des substances répulsives à l'égard des poux comme par exemple l'essence de myrte, de la citronnelle, de l'éthyl butylacetylaminopropionate (IR 3535) , le DET (Diéthyltoluamide) , les huiles essentielles de citron, de lavande, de géranium rosat, de romarin cinéole, le tea-tree, l'huile essentielle de céleri.  The composition according to the invention may also comprise at least one antioxidant agent such as butylhydroxytoluene, butylhydroxyanisol or ascorbyl palmitate, and / or one or more pediculicidal compounds such as malathion, permethrines and pediculicidal or repulsive plant essences. These species can be, for example, aniseed oil, tea tree oil, myrtle oil, lavender oil, neem oil and substances described as growth inhibitors. nits such as Farnesol and Nerolidol. It is also possible to incorporate substances that are repellent for lice, such as myrtle oil, citronella, ethyl butylacetylaminopropionate (IR 3535), DET (diethyltoluamide), lemon essential oils. , lavender, rose geranium, rosemary cineole, tea-tree, celery essential oil.
La viscosité de la solution peut être adaptée afin de correspondre à différentes formes d'application et de présentations galéniques. The viscosity of the solution can be adapted to correspond to different forms of application and galenic presentations.
Sans agent gélifiant la solution peut en particulier être appliquée sous forme de lotion ou de spray. Sa viscosité est préférentiellement comprise entre 1,00 χ 10~3 et 1,0 mPa.s. (viscosimètre Brookfield LVT, Cylindre 3, Vitesse 12 à 20°C). Without gelling agent the solution may in particular be applied in the form of a lotion or spray. Its viscosity is preferably between 1.00 χ 10 ~ 3 and 1.0 mPa.s. (Brookfield LVT viscometer, Cylinder 3, Speed 12 at 20 ° C).
En présence d'agent gélifiant la viscosité peut atteindre une texture de gel qui s'étend comme un gel coiffant et ne coule pas dans les yeux. Dans ce cas la viscosité est préférentiellement comprise entre 1,0 à 100 mPa.s. (viscosimètre Brookfield LVT, Cylindre 3, Vitesse 12 à 20°C). Par ailleurs, la solution huileuse selon l'invention peut être gélifiée, par exemple en ajoutant des composants de type copolymères de siloxane et/ou de polyamides, comme ceux commercialisés par la société CRODA sous la marque Oléocraft LP20®. In the presence of gelling agent the viscosity can reach a gel texture that extends like a styling gel and does not flow into the eyes. In this case, the viscosity is preferably between 1.0 and 100 mPa.s. (Brookfield LVT viscometer, Cylinder 3, Speed 12 at 20 ° C). Furthermore, the oil solution of the invention can be gelled, for example by adding siloxane copolymer type components and / or polyamides, such as those sold by the company Croda under the trade name LP20 Oléocraft ®.
Selon un mode de réalisation particulier de l'invention, la solution huileuse est constituée par :  According to a particular embodiment of the invention, the oily solution consists of:
-entre 0,1 et 15% en poids d'alcool benzylique  between 0.1 and 15% by weight of benzyl alcohol
-Entre 0,1 et 15% en poids de particules colloïdales, notamment de silice colloïdale,  Between 0.1 and 15% by weight of colloidal particles, in particular of colloidal silica,
- entre 10 et 50% en poids d'agents tensioactifs,  between 10 and 50% by weight of surfactants,
- entre 5 et 60 % en poids d'une phase dispersante huileuse, - entre 1 et 15 % en poids de copolymère de siloxane et de polyamide pour épaissir la formulation. between 5 and 60% by weight of an oily dispersing phase, between 1 and 15% by weight of siloxane and polyamide copolymer for thickening the formulation.
Avantageusement, la composition selon l'invention est stable, transparente, lavable à l'eau et très peu voire non irritante. Elle est très efficace à la fois contre les poux, en particulier les poux de tête, et contre les lentes. Elle agit également plus rapidement que les produits de l'art antérieur.  Advantageously, the composition according to the invention is stable, transparent, washable with water and very little or no irritant. It is very effective against both head lice, especially head lice, and against nits. It also acts faster than the products of the prior art.
De plus, la composition selon l'invention ne nécessite pas l'ajout d'un conservateur complémentaire, l'alcool benzylique joue également ce rôle.  In addition, the composition according to the invention does not require the addition of a complementary preservative, benzyl alcohol also plays this role.
La solution huileuse selon l'invention peut être obtenue par la mise en œuvre d'un procédé comprenant les étapes suivantes, préférentiellement à température ambiante :  The oily solution according to the invention can be obtained by carrying out a process comprising the following steps, preferably at ambient temperature:
- préparation de la phase huileuse dispersante contenant l'alcool benzylique en mélangeant au moins un composant huileux avec de l'alcool benzylique,  preparation of the oily dispersing phase containing the benzyl alcohol by mixing at least one oily component with benzyl alcohol,
- éventuellement solubilisation du ou des tensioactif(s) dans la phase huileuse, - optionally solubilization of the surfactant (s) in the oily phase,
- éventuellement ajout d'au moins un antioxydant dans la phase huileuse, optionally adding at least one antioxidant to the oily phase,
- éventuellement dispersion des particules colloïdales dans phase huileuse.  - optionally dispersion of the colloidal particles in the oily phase.
Dans le cas où l'on souhaite gélifier la préparation, le procédé peut comprendre également une étape supplémentaire préférentiellement après les autres étapes, qui consiste à chauffer à environ 50°C la solution huileuse et à disperser un agent gélifiant comme un copolymère de polysiloxane et de polyamide, puis à faire refroidir la préparation.  In the case where it is desired to gel the preparation, the process may also comprise a further step, preferably after the other steps, which consists in heating the oily solution to about 50 ° C. and dispersing a gelling agent such as a polysiloxane copolymer and of polyamide, then to cool the preparation.
La composition selon l'invention peut se présenter sous différentes formes galéniques comme une lotion, un gel ou un shampoing. Elle peut également être intégrée dans une autre composition se présentant notamment sous forme de lotion, de gel, de shampooing ou de mousse capillaire destinée à être appliquée sur le cuir chevelu et les cheveux humains ou sur le pelage d'animaux. Ainsi, l'invention a également pour objet une composition sous forme de lotion, de gel, de shampooing ou de mousse capillaire destinée à être appliquée sur le cuir chevelu et les cheveux humains ou sur le pelage d'animaux, comprenant une solution huileuse selon l'invention.  The composition according to the invention may be in different galenical forms such as a lotion, a gel or a shampoo. It may also be incorporated into another composition, in particular in the form of a lotion, gel, shampoo or hair mousse intended to be applied to the scalp and human hair or to the coat of animals. Thus, the subject of the invention is also a composition in the form of a lotion, a gel, a shampoo or a hair mousse intended to be applied to the scalp and human hair or to the animal's coat, comprising an oily solution according to the invention.
Les compositions selon l'invention seules ou intégrées dans des lotions, gels, shampoings, mousses, etc. peuvent être appliquées sur la peau humaine, le cuir chevelu et les cheveux humains mais également sur les pelages d'animaux, en particulier des animaux domestiques. On peut citer notamment les chevaux les ânes les volailles , les chats, les chiens, etc. Avantageusement, les solutions huileuses selon l'invention ou les compositions les contenant peuvent être appliquées sur cheveux (ou poils) secs ou humides. Elles sont rinçables à l'eau. Ainsi l'invention permet de réunir au sein de la même formulation un produit pédiculicide lorsque qu'une infestation est diagnostiquée en appliquant sur cheveux secs le produit, et un produit préventif répulsif lorsque qu'une infestation est déclarée dans l'environnement des sujets en appliquant dans ce cas le produit sur cheveux mouillés et en s'en servant de shampooing. The compositions according to the invention alone or incorporated in lotions, gels, shampoos, foams, etc. can be applied to human skin, scalp and human hair, but also to animal fur, especially domestic animals. These include horses, donkeys, poultry, cats, dogs, etc. Advantageously, the oily solutions according to the invention or the compositions containing them may be applied to hair (or hair), dry or moist. They are rinsable with water. Thus, the invention makes it possible to combine within the same formulation a pediculicidal product when an infestation is diagnosed by applying the product to dry hair, and a preventive repellent product when an infestation is declared in the environment of the subjects in question. applying in this case the product on wet hair and using shampoo.
Un mode d'application consiste à imprégner la chevelure sèche avec une solution huileuse et à rincer la chevelure simplement avec de l'eau entre cinq minutes et une heure après l'application.  One method of application is to impregnate the dry hair with an oily solution and rinse the hair simply with water between five minutes and one hour after application.
Il n'est pas nécessaire de répéter l'application après 7 jours étant donné la remarquable efficacité de la préparation sur les lentes.  It is not necessary to repeat the application after 7 days given the remarkable effectiveness of the preparation on the slow ones.
L'une des propriétés de la présente invention est de laisser un cheveux soyeux peignable et esthétiquement parfait contrairement aux produits concurrents qui laissent les cheveux rêches, gras et difficilement coiffable.  One of the properties of the present invention is to leave a silky hair combable and aesthetically perfect unlike competing products that leave hair rough, greasy and difficult to style.
Les compositions selon l'invention ont un pouvoir de dissolution important notamment vis-à- vis de la spumaline, colle naturelle et forte sécrétée par les lentes qui rend difficile leur décrochage. Ainsi l'application des formulations permet une élimination facilitée des lentes à l'aide d'un peigne adapté ce qui est un avantage supplémentaire par rapport à d'autres produits anti poux qui rendent les cheveux rêches et peu peignables.  The compositions according to the invention have a high dissolution capacity especially vis-à-vis the spumaline, natural glue and strong secreted by the nits that makes it difficult to unhook. Thus the application of the formulations allows easy removal of the nits with the aid of a suitable comb which is an additional advantage over other anti-lice products that make the hair rough and poorly combable.
L'invention a donc également pour objet une composition selon l'invention (ou toute composition l'incluant) pour une utilisation en application topique sur la peau, les phanères, les muqueuses, le pelage ou le cuir chevelu, dans la prévention et le traitement des parasitoses chez l'être humain ou l'animal. En particulier l'invention vise l'utilisation de la composition dans le traitement des pédiculoses de la tête (lutte et prévention contre les poux de tête et les lentes), mais également pour la prévention et le traitement du demodex, de la galle et des parasitoses provoquées par des puces et des aoûtats.  The invention therefore also relates to a composition according to the invention (or any composition including it) for use in topical application to the skin, superficial body growths, mucous membranes, fur or scalp, in the prevention and control of treatment of parasitosis in humans or animals. In particular the invention relates to the use of the composition in the treatment of pediculosis of the head (control and prevention against head lice and nits), but also for the prevention and treatment of demodex, gall and parasitic diseases caused by fleas and chiggers.
L'invention est à présent illustrée par des exemples de compositions selon l'invention et par des essais en particulier comparatifs avec un produit sous forme de solution aqueuse émulsionnée à base d'alcool benzylique connue sous le nom d'Ulesfia®. EXEMPLES The invention is now illustrated by examples of compositions according to the invention and by particularly comparative tests with a product in the form of emulsified aqueous solution based on benzyl alcohol known under the name of Ulesfia ® . EXAMPLES
Plusieurs exemples de compositions selon l'invention sont présentés dans les Tableaux ci- dessous.  Several examples of compositions according to the invention are presented in the tables below.
Tableau 1 : exemples de compositions selon l'invention.  Table 1: Examples of compositions according to the invention.
Les formulations Al A2 A3 sont gélifiées et contiennent de l'Oléocraft LP20. Al A2 A3 formulations are gelled and contain Oléocraft LP20.
Les formulations A4 A5 A6 sont liquides. A4 A5 A6 formulations are liquid.
Les formulations Al A2 A3 A5 A6 renferment de la silice colloïdale.  Al A2 A3 A5 A6 formulations contain colloidal silica.
Tableau 2: exemples de compositions selon l'invention.  Table 2: Examples of compositions according to the invention.
Les formulationsBAl B2 B3 sont gélifiées et contiennent de l'Oléocraft LP20. Les formulations B4 B5 B6 sont liquides. The formulations BIL B2 B3 are gelled and contain Oleocraft LP20. The formulations B4 B5 B6 are liquid.
Les formulations Bl B2 B4 B5 B6 renferment de la silice colloïdale.  Formulations B1 B2 B4 B5 B6 contain colloidal silica.
Tableau 3: exemples de compositions selon l'invention.  Table 3: Examples of compositions according to the invention.
Les formulations G 1 G2 G3 sont gélifiées et contiennent de l'Oléocraft LP20. G 1 G 2 G 3 formulations are gelled and contain Oleocraft LP20.
Les formulations Ll L2 L3 sont liquides. LI L2 L3 formulations are liquid.
Les formulations Gl G2 Ll L2 renferment de la silice colloïdale.  Gl G2 L1 L2 formulations contain colloidal silica.
Les formulations Gl G3 Ll L3 contiennent 1% d'alcool benzylique. Gl G3 L1 L3 formulations contain 1% benzyl alcohol.
Les formulations G2 L2 contiennent 5% d'alcool benzylique. G2 L2 formulations contain 5% benzyl alcohol.
Ces formulations sont stables, facilement rinçables et leur procédé de fabrication sont simples et compatibles avec les équipements industriels usuels. These formulations are stable, easily rinsable and their manufacturing process are simple and compatible with the usual industrial equipment.
Les compositions sont obtenues par la mise en œuvre du procédé suivant :  The compositions are obtained by the implementation of the following process:
Remplir la cuve principale avec la quantité souhaitée d'alcool benzylique, Ajouter progressivement la phase huileuse sous agitation lente et non turbulente, Ajouter les agents tensioactifs liquides avec les mêmes paramètres d'agitation, - Dans le cas où les tensioactifs sont cireux, élever légèrement la température de la cuve (40°C) et attendre leur dissolution complète,  Fill the main tank with the desired quantity of benzyl alcohol, Gradually add the oily phase with slow and non-turbulent stirring, Add the liquid surfactants with the same stirring parameters, - In the case where the surfactants are waxy, raise slightly the temperature of the tank (40 ° C) and wait for their complete dissolution,
Dans le cas des formulations gélifiées, dissoudre les pastilles d'Oléocraft dans la cuve, Disperser la silice colloïdale sous agitation plus énergique, et : In the case of gelled formulations, dissolve Oléocraft pellets in the tank, Disperse the colloidal silica with more vigorous stirring, and:
• dans le cas des formulations liquides : • in the case of liquid formulations:
Procéder au conditionnement dans des flacon classiques ou munis de systèmes de pulvérisation · dans le cas des formulations gélifiée :  Pack in conventional vials or with spray systems · in the case of gelled formulations:
Procéder au étapes de conditionnement de préférence à une température supérieure à 25°C  Proceed with the conditioning steps preferably at a temperature above 25 ° C
Les performances pédiculicides de ces formulations ont été testées ci-après. The pediculicidal performances of these formulations have been tested below.
ESSAIS : EVALUATION DE L'EFFICACITÉ PEDICULICIDE ET LENTICIDE DE L'INVENTION TESTS: EVALUATION OF THE EFFICACY PEDICULICIDE AND LENTICIDE OF THE INVENTION
Les essais ont été réalisés dans le but d'évaluer l'efficacité des compositions des exemples du Tableau 3 : Gl G2 G3 Ll L2 L3 contre un témoin d'eau distillée en comparaison avec le Produit Ulsefia®. The tests were carried out in order to evaluate the effectiveness of the compositions of the examples of Table 3: Gl G2 G3 L1 L2 L3 against a distilled water control in comparison with the Ulsefia ® Product.
Efficacité sur les poux Effectiveness on lice
L'objectif est d'évaluer l'efficacité pédiculicide des exemples Gl G2 G3 Ll L2 L3 contre un témoin d'eau distillée et en comparaison avec le Produit Ulsefia®. The objective is to evaluate the pediculicidal efficacy of Gl G2 G3 L1 L3 L3 samples against a distilled water control and in comparison with the Ulsefia ® product.
Pour réaliser les tests d'efficacité, le protocole opératoire est décrit en suivant.  To perform the efficacy tests, the operating protocol is described in the following.
Des lots d'une centaine de poux sont : Lots of hundreds of lice are:
- déposés dans le couvercle d'une boîte de Pétri de 5,5cm de diamètre,  - placed in the lid of a petri dish 5.5 cm in diameter,
- transvasés dans le fond de la boîte de Pétri tapissée d'une rondelle de papier filtre, - immergés par 300μΙ d'eau distillée, ou par 300 μΙ des exemples Gl G2 G3 Ll L2 L3 , et 300 μΙ du Produit Ulsefia® à l'aide d'une micropipette, - transferred into the bottom of the petri dish lined with a filter paper disk, - submerged by 300μΙ of distilled water, or 300 μΙ examples Gl G2 G3 Ll L2 L3, and 300 μΙ Product Ulsefia ® in using a micropipette,
- et enfin placés, boîte ouverte, dans une plus grande boîte parallélépipédique de 5,5 x 7 cm à moitié ouverte.  - and finally placed, open box, in a larger box parallelepiped of 5.5 x 7 cm half open.
L'ensemble est laissé à température ambiante. On observe alors l'état des poux à T0 effet immédiat (jusqu'à 2mn environ), à 5 minutes, à 15 minutes, à 30 minutes, 1, 3, 6 et 12 heures. A chaque observation, les poux morts sont notés puis comptabilisés ; La moyenne des résultats obtenus avec chaque échantillon (eau distillée, les produits Gl G2 G3 Ll L2 L3 , le Produit Ulsefia®, sont présentées dans le tableau suivant. The whole is left at room temperature. The condition of the lice is then observed with immediate effect (up to about 2 minutes), 5 minutes, 15 minutes, 30 minutes, 1, 3, 6 and 12 hours. At each observation, dead lice are noted and then counted; The average of the results obtained with each sample (distilled water, Gl G2 products G3 Ll L2 L3, the Ulsefia ® Product, are presented in the following table.
Les résultats exprimés en pourcentage de poux morts observés aux différentes périodes de temps sont présentés dans le Tableau 2. The results expressed as percentage of dead lice observed at different time periods are presented in Table 2.
Tableau 4 - Mortalité des poux exprimée en pourcentage en fonction du temps d'exposition aux différents produits  Table 4 - Mortality of lice expressed as a percentage according to the time of exposure to different products
Ces résultats montrent que le produit Ulesfia®, émulsion aqueuse d'alcool benzylique atteint 100% de mortalité après une heure d'application . These results show that the product Ulesfia ® , aqueous emulsion of benzyl alcohol reaches 100% mortality after one hour of application.
On constate que l'ensemble des formulations de la présente invention agissent plus rapidement dès les cinq premières minutes.  It is found that all the formulations of the present invention act more rapidly as early as the first five minutes.
Ce qui est particulièrement remarquable sont les performances des formulations Gl et Ll qui renferment des concentrations d'alcool benzylique de 1% et qui présentent des efficacités comparables aux formulations G2 et L2 qui elles sont dosées à 5% d'alcool benzylique ce qui démontre clairement le caractère surprenant de la présente invention  What is particularly remarkable are the performances of formulations G1 and L1 which contain concentrations of benzyl alcohol of 1% and which have efficiencies comparable to G2 and L2 formulations which are dosed at 5% of benzyl alcohol, which clearly demonstrates the surprising nature of the present invention
On constate également que les formulations Gl G2 Ll L2 qui contiennent des particules colloïdales présentent des performances améliorées par rapport aux formulations G3 et L3 qui n'en contiennent pas. Gl G2 L1 L2 formulations which contain colloidal particles have also been found to have improved performances compared with formulations G3 and L3 which do not contain them.
Efficacité sur les lentes Efficiency on nits
Un carré de tissu de 1,5 cm de côté porteur d'une centaine de lentes est déposé dans le couvercle d'une boîte de Pétri (5,5 cm de diamètre). 300 μΙ d'eau distillée ou les produits Gl G2 G3 Ll L2 L3 , le produit Ulsefia®, sont versés sur les lentes de façon que celles-ci soient totalement recouvertes et que les compositions versées diffusent rapidement sur le tissu porteur de lentes. A 1.5 cm square of fabric carrying a hundred nits is placed in the lid of a petri dish (5.5 cm in diameter). 300 μl of distilled water or Gl G2 G3 L1 L3 L3 products, the Ulsefia ® product, are poured onto the nits so that they are completely covered and the poured compositions diffuse rapidly on the nerve-bearing tissue.
Les carrés de tissus et leurs lentes sont ensuite posés sur une rondelle de papier filtre, humidifié par ΙΟΟμΙ de d'eau distillée, tapissant le fond de la boîte de Pétri.  The tissue squares and their nits are then placed on a washer of filter paper, moistened with ΙΟΟμΙ of distilled water, lining the bottom of the petri dish.
Les boîtes de Pétri sont placées à l'étuve à 28 C° et 60% d'humidité relative durant 5 et 15 minutes, puis lavées et rincées à l'eau distillée avant d'être déposées sur une nouvelle rondelle de papier filtre. The petri dishes are placed in an oven at 28 ° C and 60% relative humidity for 5 and 15 minutes, then washed and rinsed with distilled water before being deposited on a new filter paper washer.
Les boîtes de Pétri sont placées à l'étuve à 28C° et 60% d'humidité relative durant une quinzaine de jours (jusqu'à éclosion des lentes).  Petri dishes are placed in an oven at 28 ° C and 60% relative humidity for a fortnight (until hatching nits).
Les lentes sont observées à partir du 6ème jour jusqu'au I5ème jour, afin de noter les éclosions et de les comptabiliser. Chaque fois que cela est possible les poux éclos sont récupérés et nourris. Nits are observed from the 6th day until I5 th day to note outbreaks and accounted for. Whenever possible, the hatched lice are recovered and fed.
Les résultats obtenus exprimés en pourcentage de lentes mortes sont présentés dans le Tableau 5 suivant.  The results obtained expressed as a percentage of slow dead are presented in the following Table 5.
Tableau 5 - Mortalité des lentes exprimée en pourcentage après un temps d'exposition de 5 et 15 minutes  Table 5 - Nitrogen mortality expressed as a percentage after a 5 and 15 minute exposure time
Ces résultats montrent que le produit Ulesfia® sous la forme d'une émulsion dosée à 5% d'alcool benzylique possède une faible activité lenticide même après un temps de contact de 15 minutes . These results show that the Ulesfia ® product in the form of an emulsion dosed with 5% of benzyl alcohol has a low lenticidal activity even after a contact time of 15 minutes.
On constate par contre pour les produits de la présente invention une activité remarquable pour l'ensemble des formulations Gl G2 G3 Ll L2 L3.  On the other hand, the products of the present invention show a remarkable activity for all the formulations G1 G2 G3 L1 L2 L3.
De façon surprenante les formule contenant 1% d'alcool benzylique (Gl G3 Ll L3) présentent une activité équivalente aux formulations qui en renferment 5% (G2 & L2)  Surprisingly, the formula containing 1% of benzyl alcohol (G1 G3 L1 L3) has an activity equivalent to the formulations which contain 5% (G2 & L2)
Une telle efficacité n'a jamais été décrite dans l'art antérieur pour des préparations à base d'alcool benzylique pour les lentes particulièrement rebelles aux traitement pédiculicides en général. A l'instar de ce qui est constaté pour les poux les formulations qui renferment des particules colloïdales présentent une efficacité encore améliorée ( Gl G2 Ll L2) par rapport aux formulations qui en sont dépourvues (G3 et L3). Such efficacy has never been described in the prior art for benzyl alcohol preparations for slow ones particularly resistant to pediculicidal treatment in general. As is the case for lice, formulations containing colloidal particles have an even better efficiency (Gl G2 L1 L2) compared to formulations that are free of them (G3 and L3).

Claims

REVENDICATIONS
1. Composition sous forme d'une solution huileuse constituée au moins par une phase dispersante huileuse dans laquelle est dispersée de l'alcool benzylique. 1. Composition in the form of an oily solution consisting at least of an oily dispersing phase in which is dispersed benzyl alcohol.
2. Composition selon la revendication 1, caractérisée en ce qu'elle comprend au moins 0,5 % d'alcool benzylique en poids par rapport au poids total de la composition.  2. Composition according to claim 1, characterized in that it comprises at least 0.5% benzyl alcohol by weight relative to the total weight of the composition.
3. Composition selon l'une des précédentes revendications, caractérisée en ce qu'elle comprend entre 0,5 et 20% d'alcool benzylique en poids par rapport au poids total de la composition.  3. Composition according to one of the preceding claims, characterized in that it comprises between 0.5 and 20% of benzyl alcohol by weight relative to the total weight of the composition.
4. Composition selon l'une des précédentes revendications, caractérisée en ce que la phase dispersante huileuse est composée par du myristate d'isopropyle et/ou un mélange de glycérides d'esters de polyéthylène glycol et/ou un ou plusieurs triglycéride(s) caprylocaprique(s) et/ou un ou plusieurs silicone(s) et/ou une ou plusieurs huile(s) végétale(s).  4. Composition according to one of the preceding claims, characterized in that the oily dispersant phase is composed of isopropyl myristate and / or a mixture of glycerides of polyethylene glycol esters and / or one or more triglyceride (s) caprylocaprique (s) and / or one or more silicone (s) and / or one or more vegetable oil (s).
5. Composition selon l'une des précédentes revendications, caractérisée en ce qu'elle comprend également au moins un agent tensioactif.  5. Composition according to one of the preceding claims, characterized in that it also comprises at least one surfactant.
6. Composition selon la précédente revendication, caractérisée en ce que le ou les agent(s) tensioactif(s) sont choisi(s) parmi les agents tensioactifs anioniques, les agents tensioactifs cationiques, les agents tensioactifs amphotères et les agents tensioactifs non ioniques.  6. Composition according to the preceding claim, characterized in that the agent (s) surfactant (s) are selected (s) from anionic surfactants, cationic surfactants, amphoteric surfactants and nonionic surfactants.
7. Composition selon l'une des revendications 5 ou 6, caractérisée en ce que le ou les agent(s) tensioactif(s) sont choisi(s) parmi les carboxylates, les esters sulfuriques d'alcools primaires, les sulfonates, le bromure de cétrimide, la lécithine, les esters d'acides gras de polyols, les esters de saccharose, les esters d'acides gras polyoxyéthylénés, les esters du sorbitane, les esters du sorbitane polyoxyéthyénés, les esters d'acide gras polyoxyéthylénés, les poloxamères, des mélanges d'esters de polyéthylène glycol et de glycérides.  7. Composition according to one of claims 5 or 6, characterized in that the agent (s) surfactant (s) are selected (s) from carboxylates, sulfuric esters of primary alcohols, sulfonates, bromide cetrimide, lecithin, polyol fatty acid esters, sucrose esters, polyoxyethylenated fatty acid esters, sorbitan esters, polyoxyethylenated sorbitan esters, polyoxyethylenated fatty acid esters, poloxamers, mixtures of polyethylene glycol esters and glycerides.
8. Composition selon l'une des revendications 5 à 7, caractérisée en ce qu'elle comprend entre 10 et 50% d'agent(s) tensioactif(s) en poids par rapport au poids total de la composition.  8. Composition according to one of claims 5 to 7, characterized in that it comprises between 10 and 50% agent (s) surfactant (s) by weight relative to the total weight of the composition.
9. Composition selon l'une des précédentes revendications, caractérisée en ce qu'elle comprend également des particules colloïdales d'un diamètre compris entre 5 et 100 nm.  9. Composition according to one of the preceding claims, characterized in that it also comprises colloidal particles with a diameter of between 5 and 100 nm.
10. Composition selon la précédente revendication, caractérisée en ce que les particules colloïdales sont constituées par des particules de dioxyde de silicium d'alumine, d'argiles, des billes de silice, des billes de verre, de l'oxyde de fer, du silicate de fer, du silicate de magnésium, du dioxyde de titane, seules ou en mélanges. 10. Composition according to the preceding claim, characterized in that the colloidal particles consist of particles of silicon dioxide of alumina, clays, silica beads, glass beads, iron oxide, iron silicate, magnesium silicate, titanium dioxide, alone or in mixtures.
11. Composition selon l'une des revendications 9 ou 10, caractérisée en ce qu'elle comprend entre 0,1 et 20% de particules colloïdales en poids par rapport au poids total de la composition.  11. Composition according to one of claims 9 or 10, characterized in that it comprises between 0.1 and 20% of colloidal particles by weight relative to the total weight of the composition.
12. Composition selon l'une des précédentes revendications, caractérisée en ce qu'elle comprend également au moins un agent antioxydant.  12. Composition according to one of the preceding claims, characterized in that it also comprises at least one antioxidant agent.
13. Composition selon l'une des précédentes revendications, caractérisée en ce qu'elle comprend également un ou plusieurs composés pédiculicide(s).  13. Composition according to one of the preceding claims, characterized in that it also comprises one or more pediculicidal compounds (s).
14. Composition selon la revendication 13, caractérisée en ce que le ou les agent(s) pédiculicide(s) sont choisi(s) parmi le malathion, les perméthrines et les essences végétales pédiculicides ou répulsives.  14. A composition according to claim 13, characterized in that the agent (s) pediculicide (s) are selected (s) from malathion, permethrines and pediculicidal or repellent vegetable essences.
15. Composition selon l'une des précédentes revendications, caractérisée en ce que la phase dispersante huileuse représente entre 5 et 95,5% en poids par rapport au poids total de la composition.  15. Composition according to one of the preceding claims, characterized in that the oily dispersant phase is between 5 and 95.5% by weight relative to the total weight of the composition.
16. Composition se présentant sous forme de lotion, de gel, de shampooing ou de mousse capillaire destinée à être appliquée sur le cuir chevelu et les cheveux humains ou sur le pelage d'animaux, comprenant une composition selon l'une des précédentes revendications.  16. Composition in the form of lotion, gel, shampoo or hair mousse intended to be applied to the scalp and human hair or on animal hair, comprising a composition according to one of the preceding claims.
17. Composition selon l'une des précédentes revendications pour une utilisation en application topique sur la peau, les phanères, le pelage, les muqueuses ou le cuir chevelu, dans la prévention et le traitement des parasitoses chez l'être humain ou l'animal.  17. Composition according to one of the preceding claims for use in topical application to the skin, superficial body growth, peeling, mucous membranes or scalp, in the prevention and treatment of parasitosis in humans or animals. .
18. Composition pour son utilisation selon la revendication 17, pour la prévention et le traitement des pédiculoses de la tête.  18. Composition for its use according to claim 17 for the prevention and treatment of pediculosis of the head.
19. Composition pour son utilisation selon la revendication 17, pour la prévention et le traitement du demodex, de la gale ou des parasitoses provoquées par des puces ou des aoûtats.  19. A composition for its use according to claim 17 for the prevention and treatment of demodex, scab or parasitosis caused by fleas or chiggers.
EP18782315.8A 2017-09-14 2018-09-13 Oil solution of benzyl alcohol, and use in the prevention and treatment of parasitoses Pending EP3681462A1 (en)

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FR1770962A FR3070865A1 (en) 2017-09-14 2017-09-14 OIL SOLUTION OF BENZYL ALCOHOL AND USE IN THE PREVENTION AND TREATMENT OF PARASITOSES
PCT/EP2018/074763 WO2019053134A1 (en) 2017-09-14 2018-09-13 Oil solution of benzyl alcohol, and use in the prevention and treatment of parasitoses

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FR3070865A1 (en) 2017-09-14 2019-03-15 Concept OIL SOLUTION OF BENZYL ALCOHOL AND USE IN THE PREVENTION AND TREATMENT OF PARASITOSES
FR3085821B1 (en) * 2018-09-19 2021-09-10 Invictus OILY SUSPENSION OF SUBMICRONIC MINERAL PARTICLES TO FIGHT AGAINST LICE
FR3103105B1 (en) 2019-11-15 2021-11-26 Dermowave composition in the form of a rinsable oily solution to fight against lice
FR3134968A1 (en) 2022-04-28 2023-11-03 Nadine PAGNOTTA GRISLAIN Oily anti-lice composition based on liquid alkanes and its uses

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FR955753A (en) 1950-01-19
US6849614B1 (en) 1998-07-28 2005-02-01 Ecosmart Technologies, Inc. Synergistic and residual pesticidal compositions containing plant essential oils
DK1215965T3 (en) 1999-09-16 2004-02-16 Durminster Ltd Method and Preparation for Combating Arthropods
US6663876B2 (en) 2002-04-29 2003-12-16 Piedmont Pharmaceuticals, Llc Methods and compositions for treating ectoparasite infestation
US6793931B2 (en) 2002-07-11 2004-09-21 Summers Laboratories, Inc. Ectoparasite asphyxiator compositions and methods for their applications
EP2975943A4 (en) * 2013-03-15 2016-09-14 Tyratech Inc Lice control composition and method
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