Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
  • A61K47/34—Macromolecular 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/44—Oils, 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/04—Dispersions; Emulsions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
  • A61K9/0017—Non-human animal skin, e.g. pour-on, spot-on
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/08—Solutions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P33/00—Antiparasitic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier 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
  • A61Q17/02—Barrier 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q5/00—Preparations for care of the hair
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q5/00—Preparations for care of the hair
  • A61Q5/02—Preparations 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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• Health & Medical Sciences (AREA)
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• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
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• Tropical Medicine & Parasitology (AREA)
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• Agricultural Chemicals And Associated Chemicals (AREA)

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• 2017
  • 2017-09-14 FR FR1770962A patent/FR3070865A1/fr active Pending
• 2018
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  • 2018-09-13 WO PCT/EP2018/074763 patent/WO2019053134A1/fr unknown
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