Classifications

• • 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
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
  • A01K13/00—Devices for grooming or caring of animals, e.g. curry-combs; Fetlock rings; Tail-holders; Devices for preventing crib-biting; Washing devices; Protection against weather conditions or insects
  • A01K13/003—Devices for applying insecticides or medication
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01K—ANIMAL HUSBANDRY; AVICULTURE; APICULTURE; PISCICULTURE; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
  • A01K27/00—Leads or collars, e.g. for dogs
  • A01K27/007—Leads or collars, e.g. for dogs with insecticide-dispensing means
• • A—HUMAN NECESSITIES
  • A44—HABERDASHERY; JEWELLERY
  • A44C—PERSONAL ADORNMENTS, e.g. JEWELLERY; COINS
  • A44C5/00—Bracelets; Wrist-watch straps; Fastenings for bracelets or wrist-watch straps
  • A44C5/0007—Bracelets specially adapted for other functions or with means for attaching other articles
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61D—VETERINARY INSTRUMENTS, IMPLEMENTS, TOOLS, OR METHODS
  • A61D7/00—Devices or methods for introducing solid, liquid, or gaseous remedies or other materials into or onto the bodies of animals
• • 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
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/658—Medicinal preparations containing organic active ingredients o-phenolic cannabinoids, e.g. cannabidiol, cannabigerolic acid, cannabichromene or tetrahydrocannabinol
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/348—Cannabaceae
  • A61K36/3482—Cannabis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
  • A61K36/534—Mentha (mint)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/55—Linaceae (Flax family), e.g. Linum
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
• • 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
  • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• • 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
  • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• • 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
  • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
• • 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
  • 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
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• • C—CHEMISTRY; METALLURGY
  • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
  • C08K—Use of inorganic or non-macromolecular organic substances as compounding ingredients
  • C08K5/00—Use of organic ingredients
  • C08K5/04—Oxygen-containing compounds
  • C08K5/13—Phenols; Phenolates
• • C—CHEMISTRY; METALLURGY
  • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
  • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
  • C08L23/00—Compositions of homopolymers or copolymers of unsaturated aliphatic hydrocarbons having only one carbon-to-carbon double bond; Compositions of derivatives of such polymers
  • C08L23/02—Compositions of homopolymers or copolymers of unsaturated aliphatic hydrocarbons having only one carbon-to-carbon double bond; Compositions of derivatives of such polymers not modified by chemical after-treatment
  • C08L23/04—Homopolymers or copolymers of ethene
  • C08L23/08—Copolymers of ethene
  • C08L23/0846—Copolymers of ethene with unsaturated hydrocarbons containing atoms other than carbon or hydrogen
  • C08L23/0853—Ethylene vinyl acetate copolymers
• • C—CHEMISTRY; METALLURGY
  • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
  • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
  • C08L75/00—Compositions of polyureas or polyurethanes; Compositions of derivatives of such polymers
  • C08L75/04—Polyurethanes

Definitions

• the present invention is in the field of treatments for the relief of various symptoms related to pain or stress. More specifically, the present invention relates to a device for topical application in the form of a polymer matrix containing at least one active agent from the cannabinoid family, alone or as a mixture with other active agents. The present invention preferably relates to the device in the form of a collar, its use for improving the well-being and mobility of an animal to which the device is applied, and its method of preparation.
• the plant must have a delta-9-tetrahydrocannabinol (THC) content of less than 0.2%, CBD products are prohibited if they contain THC in any amount.
• THC delta-9-tetrahydrocannabinol
• THC-free cannabinoids are used to improve the quality of life they provide to humans and animals affected by situations such as pain, stress, anxiety, epilepsy and spasms, arthritis, nausea or even dermatological problems since ancient times. These cannabinoids were primarily administered orally, or sublingually.
• cannabidiol oils are formulated either as a semi-solid (ointments, creams, gels) or as a liquid (milks, emulsions, lotions).
• the aforementioned topical application dosage forms require repeated applications to produce the desired systemic effects.
• the application of such topical products is not easy and not optimum for obtaining effective penetration through the hair of the animal, or for long-term treatment.
• One of the objectives of the invention is to provide a more
• a solid polymer matrix as a vehicle for topical application. and / or transdermal cannabinoids, alone or in combination with other active agents, said matrix making it possible to obtain a composition having stable incorporated active agents.
• stable according to the invention is meant a physical stability of the device and a chemical stability of the assets within the device.
• physical stability is meant the absence of exudation confirming the good incorporation of the active phase, the mechanical strength of the device, in particular the resistance to deformation, the flexibility or the hardness required for the end use.
• chemical stability is meant the absence of degradation of the main asset or assets, said degradation of the asset to be less than 10% of the amount initially introduced into the device.
• the device according to the invention must be stable to evaporation, risk of loss in particular by leaching, and offering, in use, a continuous, controlled, effective and progressive diffusion of the active ingredients on the subject to be treated.
• One of the objectives of the present invention is also to provide a device whose manufacturing process remains simple to implement and transposable on an industrial scale.
• the prior art in the field of polymers describes difficulties in incorporating active agents into said polymers. It is in fact necessary to be able to incorporate the active ingredient in a total and stable manner within the polymer, while avoiding uncontrolled release or release.
• the prior art describes various solutions such as the addition of numerous specific ingredients to make the active ingredient incorporated, or proposes to integrate the active ingredient within structures of particulate type more or less complex to produce. .
• the process for obtaining the device according to the invention makes it possible to obtain the incorporation of liquid assets, within the structural polymer of the matrix without resorting to the use of specific ingredients or to integrate the active ingredient in any particulate form.
• the device according to the present invention can be defined as topical application, because it is for local use, applied to the skin or coat of the subject to be treated.
• the device of the present invention can also meet the definition of a person skilled in the art of a transdermal device since it consists of a polymer matrix serving as a support for the active agents and produced in order to allow the release of said active agents for their diffusion in the subject to be treated so that the active agents can reach the cannabinoid receptors.
• the terms “topical” and “trans dermal” applied to the device of the present invention will be considered without distinction.
• Trans dermal systems containing cannabinoid derivatives are described in the prior art. However, these all describe reservoir or matrix-type systems, made up of at least two or even several layers of different materials with different functions. These transdermal systems consist of at least one adhesive layer in order to fix the device on the subject, a reservoir layer containing the active ingredient (s) to be conveyed and an impermeable outer layer.
• the prior art does not describe a non-adhesive, single-layer system making it possible to simply incorporate and diffuse a cannabinoid-type active agent as proposed by the present invention.
• the systems described are complex to produce and not suitable for use on an animal subject covered with a coat.
• monolayer polymer matrix is meant a matrix consisting of a single layer of polymer and not the juxtaposition of several layers as commonly described in the prior art.
• monopolymer according to the invention is meant a matrix consisting of the same polymer. Said same polymer may for its part be a homopolymer or a copolymer.
• a homopolymer is a polymer derived from a single species (real, implied or hypothetical) of monomer. All of the repeat units of a homopolymer are of the same chemical nature.
• a copolymer is a polymer obtained from at least two different monomers, called comonomers; it contains at least two types of repeat patterns. .
• Figure 1 illustrates the release kinetics of BCD from the device according to an embodiment of the invention according to Example 10.
• Figure 2 illustrates the release kinetics of CBD from the devices according to
• CBD cannabidiol
• a first object of the present invention is a device
• the cannabinoid active agent comprising a solid polymer matrix, incorporating an active composition containing at least a first active ingredient consisting of a cannabinoid in the form of an oil or an isolate extracted from hemp, or cannabis, alone or in combination with other active ingredients .
• the active agents used in combination with the cannabinoid active agent can be chosen from painkillers, anti-inflammatories, soothing or anesthetic active agents.
• the cannabinoid-type active agents can also be combined with insecticidal or pest-repellent active agents.
• the cannabinoids used are preferably cannabidiol (CBD) which can be used in the form of powder, liquid, solution, oil or isolate, extracted from the hemp plant.
• CBD oil is preferably understood to mean an oil rich in cannabinoids, it is meant more particularly rich in phytocannabinoids and terpenes identified in the genes of hemp. Said oils are in particular the oils obtained from the plants Cannabis sativa, Cannabis indica and Cannabis ruderalis.
• the CBD oil used contains between 50 and 95% cannabidiol (CBD) and preferably between 80 and 90% CBD in addition to different terpenes.
• the CBD oil used according to the present invention may contain THC (otherwise known as full spectrum CBD oil - "Full spectrum").
• the oil used is an oil, called a broad spectrum oil, the THC content of which is less than 0.2%,
• CBD oil or “hemp oil rich in CBD” will be used interchangeably to denote CBD in the form of an oil extracted from hemp rich in Cannabidiol (CBD), and whose THC content is less than 0.2% w / w.
• CBD Cannabidiol
• CBD is present in an amount between 0.01 and 10% w / w, preferably between 0.1 and 5% by total device weight.
• the cannabidiol and terpenes purification and extraction system can in particular but not exclusively be based on a patented technology which preserves the terpenes and lipids of the plant, by freeing itself from unwanted compounds such as Delta-9-THC, waxes and chlorophyll, as described in particular in patent application US2018 / 0333446 incorporated here in full by reference.
• the CBD used is in the form of an isolate.
• isolate according to the present invention is meant in particular a crystalline powder obtained by extraction of the hemp plant, with a CBD concentration greater than or equal to 99%.
• the CBD isolate used in the composition is present in an amount between 0.01 and 10% w / w, preferably between 0.1% and 5% w / w, more preferably between 0.5% and 2.5% w / w of the composition.
• the active agents which can be used in combination with the cannabinoids are essential oils, or monoterpene derivatives of essential oils of the alcohol, aldehydes or esters type.
• these active ingredients are chosen from linalool, menthol or the essential oils of peppermint, lavender, lavandin, Italian helicrysum, cedar, lemon, lemongrass, carrot, ginger, niaouli, sweet orange, clove, Eucalyptus citriodora, Eucalyptus radiata, geranium, valerian, Nepeta Cataria, chamomile, Ylan Ylang, clary sage, mandarin, sandalwood, bergamot, marjoram, frankincense, geranium, thyme, juniper or their mixtures.
• the CBD oil or the CBD isolate will be combined with menthol, Linalool, essential oil of peppermint, Eucayptus citriodora, lavender, lavandin, valerian, or Nepeta Cataria.
• the active ingredients are the CBD isolate or CBD oil and the essential oil of peppermint or the oil of Eucayptus citriodora for their soothing and / or anti-inflammatory action. -pain coupled with that of CBD.
• the active ingredients in the form of essential oils or compounds of essential oils are present in an amount between 0.5 and 20% w / w, preferably between 0.5 and 15% w / w, and more preferably between 0.5 and 6% by total weight of the device.
• the polymer matrix consists of thermosetting or thermoset polymers, chosen from cast polyurethane, reactive silicones and epoxy resins, preferably cast polyurethane.
• thermosetting or thermoset polymers chosen from cast polyurethane, reactive silicones and epoxy resins, preferably cast polyurethane.
• the cast polyurethane matrix in accordance with the present invention, is described in patent FR2992325, incorporated here in full by reference.
• polymers constituting the solid matrix are chosen from thermoplastic polymers, biodegradable or not, chosen from the group formed by polyolefins and their derivatives, ethylenebutyl acrylates, polyamides, copolyamides and their derivatives, polychlorides of vinyls (PVC), polyurethanes (TP U) and their derivatives, styrenics and their derivatives, vulcanized thermoplastics, agropolymers and their derivatives, polyesters and their derivatives, taken alone or as a mixture.
• the polyolefins and derivatives can in particular be chosen from polyethylenes (PE), polypropylenes (PP), copolymers of ethylene and of vinyl acetate (EVA).
• the styrenics and their derivatives can be chosen in particular from polystyrene-poly (ethylene-butylene) -polystyrene (SEBS) copolymers, polystyrene-polyisoprene-polystyrene (SIS) copolymers, polystyrene-polybutadiene-polystyrene (SBS) copolymers.
• SEBS polystyrene-poly (ethylene-butylene) -polystyrene
• SIS polystyrene-polyisoprene-polystyrene
• SBS polystyrene-polybutadiene-polystyrene copolymers.
• the copolyamides and their derivatives can in particular be chosen from block-friend ethers (EBA).
• the agropolymers and their derivatives can in particular be chosen from polysaccharides, starch,
• the thermoplastic polymer which can be used according to the invention is chosen from a polyolefin and their derivatives or a polyurethane and their derivatives. More preferably, the polymer matrix constituting the device according to the present invention is a thermoplastic consisting of copolymers of ethylene and vinyl acetate (EVA) or of polyurethane with a polyether or polyester unit (TP U).
• EVA ethylene and vinyl acetate
• TP U polyether or polyester unit
• the TPU will be preferred for a device with a transparent, translucent appearance.
• the polymer represents between 40 and 99% by weight of the device.
• the polymer matrix is in an amount sufficient to complete the 100% (qs 100%) of the composition of the device.
• thermoplastic polymer which can be used according to the invention is non-adhesive. Indeed, an adhesive device would not be suitable for application to the animal's coat.
• thermoplastic polymer which can be used according to the invention is not water soluble.
• the matrix constituting the device according to the invention is a single-layer and monopolymeric matrix only, and not constituted by an association of several sequences of polymers different .
• the formulation additives can be dispersants, solvents, vectorizers, propenetrants, plasticizers, stabilizers, dyes, or perfumes, in order to be added to the composition according to the invention depending on the effect. research.
• oils of organic, synthetic, mineral or vegetable origin such as mixtures of succinate, glutarate and adipate, oils omega 3 polyunsaturated fatty acid type, fatty acid esters, glycol ethers, or squalene and its derivatives.
• the device according to the invention comprises vectorizers, or propenetrants which can facilitate the vectorization of the active ingredient on the subject's skin or coat and / or the transcutaneous passage of the active ingredients.
• these vectorizers, propenetrants are lipophilic compounds.
• coconut oil jojoba oil, hemp oil, macadamia oil, linseed oil or sweet almond oil
• krill oil diethylene glycol monoethyl ether, marketed under the name of Transcutol V, isopropyl myristate, or squalene derivatives, preferably 2,6,10,15,19,23-hexamethyltetracosane, also called perhydrosqualene or dodecahydrosqualene marketed under the name of Squalane.
• These ingredients will be present in an amount of between 0.1 and 30% w / w, preferably between 0.5 and 15% w / w, more preferably between 1 and 6% by total weight of the device.
• the device also comprises a plasticizer compound.
• the plasticizer has a role in the release of the active agents from the polymer matrix, and that the nature and the concentration of plasticizer make it possible to modulate the release of the active agents.
• plasticizer which can be used in the device according to the invention, mention may be made of ethylhexyldiphenyl phosphate, dioctyl adipate, diisooctyl adipate, dibutyl adipate, dimethyl adipate, dioctyl glutarate. dimethyl, dimethyl succinate, taken alone or as a mixture.
• the mixture of plasticizer composed of dimethyl adipate, of dimethyl glutarate and of dimethyl succinate is used in the form of the commercial mixture called Coasol.
• the plasticizers will be different from phthalates, the use of which is controversial due to their toxicity.
• the plasticizer or the mixture of plasticizer is present in an amount of between 0 and 50% by weight,
• the plasticizer makes it possible to confer on the matrix the plastic properties desired for its use.
• the plasticizer also has a role of softening the polymer materials used in order to give the device the chosen flexibility or hardness.
• one of the objects of the present invention is a device in the form of a collar for animals. Said collar therefore requires sufficient flexibility to be adapted to the shape of the animal's neck but while retaining the desired shape, structure and the desired diffusion properties of the active ingredient.
• the polymer matrix according to the invention comprises at least one plasticizer.
• stabilizers and / or antioxidants may be added to the composition of the device according to the invention at a concentration of between 0 and 5% w / w, preferably between 0 and 1.5% by total weight of the composition.
• concentration of between 0 and 5% w / w, preferably between 0 and 1.5% by total weight of the composition.
• Colorants as well as perfumes may also be added to the composition.
• the dyes can be present in liquid or solid form.
• the perfume is chosen from the perfume of vanilla, lime, lavender, violet, apple, apricot, patchouli, bamboo green leaves and can be adapted to the indication. and the user.
• the device according to the invention comprises, in% by weight of the device:
• CBD isolate or CBD oil are between 0.01 and 10% of CBD isolate or CBD oil.
• the device according to the invention comprises, in% by weight of the device:
• CBD isolate or CBD oil are between 0.01 and 10% of CBD isolate or CBD oil.
• the device according to the invention comprises, in% by weight of the device:
• CBD isolate Between 0.1 and 5% of CBD isolate, Between 0.5 and 15% by weight of active ingredients in the form of essential oil and / or essential oil compounds,
• the device according to the invention comprises, in% by weight of the device:
• CBD isolate Between 0.1 and 5% of CBD isolate,
• CBD isolate Between 0.1 and 5% of CBD isolate,
• additives of vectoring type more preferably squalane
• plasticizers preferably a mixture of phosphate
• Ethylhexyldiphenyl Dimethyl Adipate, Dimethyl Glutarate, and Dimethyl Succinate or Dimethyl Glutarate.
• the device is in the form of a collar, a
• the device is made in the form of a necklace or a bracelet.
• the process for obtaining the device is an injection molding process.
• the device is a collar for pets and in particular a collar for dogs or cats.
• a second object of the present invention is the device consisting of a solid polymer matrix incorporating a solution of active ingredients containing at least one CBD isolate or one CBD oil for its use in the treatment or relief of pain or stress. in a human or animal subject. More particularly, having regard to the properties of CBD in combination with the other active agent (s) according to the invention, the device allows by its application to regulate the pain induced, in particular by inflammatory disorders, immuno-induced or not.
• the device makes it possible to regulate skin pain or pruritus, muscle pain, joint pain, tendonitis as well as rheumatic pain such as for example osteoarthritis or arthritis in a human and animal subject.
• the device according to the invention can also be used to regulate the stress of a human or animal subject.
• the present invention therefore relates to the device for topical / transdermal application, in a thermoplastic polymer matrix loaded with active ingredients, in particular cannabidiol, for its use in the relief of pain or stress in a human or animal subject to be treated.
• Said device is characterized in that it is brought into contact with the skin and / or the coat.
• said device makes it possible to provide relief from the pain or stress of an animal, characterized in that it is applied in contact with the skin and / or the coat in the form of a collar.
• the active agents are thus released from the collar and, by topical application, penetrate the skin, in particular transported via the sebum.
• the present invention therefore also relates to the device for its use for improving the mobility and the well-being of a subject and more particularly of an animal.
• the present invention also relates to the device according to the invention for its
• the transdermal patch according to the invention has the advantage of delivering the active ingredient in a gradual, continuous and measured manner, and over a longer period of time.
• the desired application time of the devices according to the invention is between 30 min for a rapid effect to several months for a long-term effect.
• the device according to the invention is applied for a period of 1 to 60 days, preferably for 28 days (4 weeks). In fact, according to a preferred embodiment, this time of 4 weeks is a time necessary and sufficient to treat a human or animal subject against pain or stress before a possible new application if necessary.
• the present invention also relates to a method of making the device according to
• the choice of the process and in particular of the mixing temperatures allows a process to be carried out in a few steps and without having to resort to the addition of specific ingredients or particulate structure to aid in the incorporation. active ingredients within the polymer matrix.
• the first step of the process therefore consists in introducing the polymer into a reactor
• the polymer will be heated to a temperature of between 10 to 15 degrees Celsius below its melting point, at a temperature sufficient to give a structure to the polymer making it possible to open the networks to facilitate the incorporation of the active agents. without reaching the fusion of said polymer.
• the reactor will be heated between 80 and 90 degrees Celsius, preferably between 90 and 95 ° C.
• the reactor will be heated between 45 and 90 degrees Celsius, preferably between 70 and 75 ° C. The reactors are then stirred.
• the second step of the process consists in preparing the liquid active phase according to the following protocol: weigh and mix the ingredients such as plasticizers and vectors, and stir to homogenize in order to obtain a clear mixture. The active agents are then added with stirring at room temperature until a clear, translucent homogeneous mixture is obtained.
• the third step of the process consists of the gradual addition of the active phase to the
• the present invention also relates to the product obtained by the defined process
• the invention relates to a topical application device consisting of a monolayer polymer matrix characterized in that the polymer is selected from the group consisting of a copolymer of ethylene and vinyl acetate and a polyurethane, said matrix also being characterized in that it comprises at least one cannabinoid derivative and between 0.5% and 20% by total weight of the matrix of at least one essential oil or a monoterpene derivative of essential oils.
• the invention relates more particularly to a device, characterized in that the polymer is non-adhesive. [49].
• the invention relates more particularly to a device, characterized in that the polymer is a copolymer of ethylene and vinyl acetate or a polyurethane.
• the invention relates to said device, characterized in that the cannabinoid derivative is cannabidiol, preferably free of delta-9-tetrahydrocannabinol. More preferably, said device is characterized in that the cannabidiol is present in the form of a CBD isolate or a CBD oil, said CBD isolate contains at least 90% CBD and said CBD oil comprises between 80 and 90% CBD.
• the invention also relates to the preceding device characterized in that it also comprises at least one essential oil or monoterpene derivatives of essential oils, chosen from linalool, menthol or the essential oils of lavender, lavandin, Italian helicryse. , cedar, lemon, lemongrass, carrot, ginger, niaouli, sweet orange, clove, Eucalyptus citriodora, Eucalyptus radiata, peppermint, geranium, valerian, Nepeta Cataria, chamomile, Ylan Ylang, clary sage, tangerine, sandalwood, bergamot, marjoram, frankincense, geranium, thyme, juniper or their mixtures.
• essential oils chosen from linalool, menthol or the essential oils of lavender, lavandin, Italian helicryse. , cedar, lemon, lemongrass, carrot, ginger, niaouli, sweet orange, clove, Eucalypt
• the device according to the present invention is also characterized in that it comprises a vectorizing compound chosen from oils of organic, synthetic, mineral or vegetable origin, esters such as mixtures of succinate, glutarate and adipate, omega 3 polyunsaturated fatty acid type oils, fatty acid esters, glycol ethers, or squalene and its derivatives.
• oils of organic, synthetic, mineral or vegetable origin esters such as mixtures of succinate, glutarate and adipate, omega 3 polyunsaturated fatty acid type oils, fatty acid esters, glycol ethers, or squalene and its derivatives.
• the device is characterized in that it also comprises a plasticizer compound chosen from ethylhexyldiphenyl phosphate, dioctyl adipate , diisooctyl adipate, dibutyl adipate, dimethyl adipate, dimethyl glutarate, dimethyl succinate, taken alone or as a mixture.
• a plasticizer compound chosen from ethylhexyldiphenyl phosphate, dioctyl adipate , diisooctyl adipate, dibutyl adipate, dimethyl adipate, dimethyl glutarate, dimethyl succinate, taken alone or as a mixture.
• the device is also characterized in that it is in the form of a necklace, a bracelet, a patch, a medallion, or a textile coating, and preferably in the form of a collar.
• the invention relates to a device, for topical application, in thermoplastic polymer matrix, loaded with active ingredients for its use in the relief of pain or stress in an animal, characterized in that said device is placed in contact with the skin and / or the coat, and in that the device comprises at least one cannabidiol isolate, free from delta-9-tetrahydrocannabinol, at least one essential oil or one compound of an essential oil and at least one non-adhesive thermoplastic polymer selected from a polyurethane or a copolymer of ethylene and vinyl acetate.
• the present invention also relates to the device defined above for its use in relieving stress or muscle, joint, or rheumatic pain, such as tendonitis, arthritis and osteoarthritis.
• the invention also relates to the use of a device according to the present invention
• the invention also relates to a method of manufacturing a device consisting of a thermoplastic polymer matrix comprising at least one non-adhesive thermoplastic polymer selected from a polyurethane or a copolymer of ethylene and vinyl acetate, and of that the active ingredients comprise at least one cannabidiol isolate, free of delta-9-tetrahydrocannabinol or a cannabidiol oil free of delta-9-tetrahydrocannabinol and between 0.5 and 20% w / w of at least one essential oil or a compound of an essential oil, said process comprising the steps of bringing the polymer to a chosen temperature, of preparing the active phase, of mixing the active phase with the polymer, then shaping the device, characterized in that said process does not include a step of adding specific excipients or a particulate structure to help the incorporation of the active agents into the polymer matrix.
• the invention also relates to the product obtained by the process described above.
• EVA ethylene vinyl acetate
• the active ingredients namely hemp oil rich in cannabinoids and peppermint oil
• the active ingredients are introduced at room temperature.
• Add linseed oil homogenize the mixture is then added transcutol V as a propenetrant.
• the mixture is stirred weakly using a magnetic bar in order to obtain a homogeneous mixture which constitutes the solution of painkiller active agent.
• a cylindrical mixer is preheated to 70 ° C in an oil bath.
• the EVA pellets ACUDIA ® PA-5348
• the solution obtained previously is introduced into the mixer, still with gentle stirring.
• the mixture is left to stir until all the liquid is completely absorbed by the polymer, then the temperature is lowered to 25 ° C.
• the mixer is emptied, the compound thus obtained is stored in a package sealed against air and humidity.
• the term “compound” is understood to mean the term well known to those skilled in the art to denote the polymer loaded with active agent.
• the polymer loaded with active ingredients obtained above is injected in a collar weighing approximately 41 g at the nozzle outlet for a length of 75 cm.
• This collar is intended to be worn by a dog around the neck to relieve various pain such as osteoarthritis.
• a cylindrical mixer is preheated to 70 ° C in an oil bath.
• the EVA pellets ACUDIA ® PA-5348
• the solution obtained previously is introduced into the mixer, still with gentle stirring.
• the mixture is left to stir until all the liquid is completely absorbed by the polymer, then the temperature is lowered to 25 ° C.
• the mixer is emptied, the compound thus obtained is stored in a package sealed against air and humidity.
• the polymer loaded with active ingredients obtained above is injected in a collar weighing approximately 41 g at the nozzle outlet for a length of 75 cm.
• This collar is intended to be worn by a dog around the neck to relieve various pain such as osteoarthritis.
• a cylindrical mixer is preheated to 70 ° C in an oil bath.
• the EVA pellets ACUDIA ® PA-5348
• the solution of active agents obtained previously is introduced into the mixer, still with gentle stirring.
• the mixture is left to stir until all the liquid is completely absorbed by the polymer, then the temperature is lowered to 25 ° C.
• the mixer is emptied, the compound thus obtained is stored in a package sealed against air and humidity.
• the polymer loaded with active agents obtained above is injected in a medallion weighing approximately 15 g at the nozzle outlet.
• This medallion is intended to be worn as a collar by a dog to soothe it in circumstances likely to generate stress.
• Example 4 is the development of a monopolymeric active matrix that can be injected in the form of a bracelet.
• the manufacturing process is similar to that of Examples 1 to 3 above
• the manufacturing process is similar to that of Example 5 above.
• the manufacturing process is similar to that of Example 6 above.
• the manufacturing process is similar to that of Example 5 above.
• Example 12 In vitro study of the release kinetics of CBD from the devices according to the invention
• An amount is obtained in mg or a percentage relative to the amount initially incorporated.
• the analysis is performed by reverse phase HPLC, with external calibration using a certified CBD standard.
• the device according to the invention according to Example 10 in the form of a collar made it possible to efficiently and stably incorporate the desired active ingredients, including CBD.
• the above results and the corresponding curve in FIG. 1 prove a gradual release over time of CBD for long-term treatment of the subject to be treated, such as the dog. At 28 days, it can be noted that the plateau is not reached and that the release continues.
• the device according to the invention according to Example 5 in the form of a collar made it possible to effectively incorporate the desired active ingredients, including CBD.
• Example 11 in the form of a collar made it possible to effectively incorporate the desired active ingredients, including CBD.

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• 2020
  • 2020-06-25 EP EP20749927.8A patent/EP3990024B1/fr active Active
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