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
  • A61K9/10—Dispersions; Emulsions
  • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
• • 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
  • A61K36/13—Coniferophyta (gymnosperms)
  • A61K36/14—Cupressaceae (Cypress family), e.g. juniper or cypress
• • 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)
  • A61K36/61—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
  • 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)
  • A61K36/75—Rutaceae (Rue family)
• • 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
  • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• • 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
  • A61K8/06—Emulsions
  • A61K8/062—Oil-in-water 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
  • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
  • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
• • 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
  • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
  • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/10—General cosmetic use
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
  • A61K2800/30—Characterized by the absence of a particular group of ingredients
  • A61K2800/33—Free of surfactant
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/82—Preparation or application process involves sonication or ultrasonication

Definitions

• the present invention relates to the field of oil-in-water emulsions and more particularly proposes oil-in-water emulsions based on essential oils formulated without surfactant or any other substitute substance.
• patents FR27221 16 and FR2720644 propose, for their part, examples of use of solid particles which ensure the dispersion of one of the two phases in the other. These particles also have the advantage of offering product textures that are more advantageous for the consumer.
• Other solutions are proposed by patents CA2295533 and FR2771293, which respectively describe the use of a cationic gel and a lipophilic agent whose HLB (hydrophilic / lipophilic balance) is less than 3. The stability of the preparations made is then ensured by the structuring that allow these compounds at the hydrophilic / lipophilic interface.
• Dispersions or emulsions containing alcohol Dispersions or emulsions containing alcohol
• the invention relates to very simple compositions, consisting of an emulsion of an essential oil in an aqueous solution, this aqueous solution preferably being a hydrosol.
• these compositions are stable in the absence of any surfactant molecule and pleasant to use.
• These compositions containing only essential oils and an aqueous phase constitute a new and innovative galenic.
• the present invention relates to novel short and single galenical formulations of essential oils (HE) for use in aromatherapy.
• These formulations constitute stable emulsions of HE in an aqueous solution without addition of surfactant.
• Such emulsions can be obtained for example using the method using high frequency ultrasound, as described in the patent application WO2010 / 149668.
• This preparation process makes it possible in particular to prepare a stable oil-in-water emulsion.
• This method combines a lipid phase with an aqueous phase by subjecting the mixture to vibratory energy, in a closed container, by applying a transducer operating in a frequency range between 900 kHz and 3 MHz. In a preferred embodiment, the transducer operates at a higher frequency or equal to 1 MHz.
• a first subject of the invention therefore relates to an oil-in-water emulsion composition
• an oil-in-water emulsion composition comprising an aqueous solution and at least one HE, this composition not containing a surfactant and being obtained by an ultrasonic treatment whose vibration frequency is greater or equal to 1 MHz.
• compositions do not contain surfactant, emulsifier or any other substance or particle intended to stabilize the preparation with respect to phase separation.
• aqueous solution used to prepare the emulsion can be diverse. It is preferably an aqueous solution containing plant extracts, in particular a hydrosol, an infusion or a maceration of plants, or a fruit water.
• the aqueous solution is a hydrolate, pure or diluted, or a mixture of hydrolates.
• the quantity of HE contained in the compositions must be adapted so that the finished products can be used directly, for example in topical application, without presenting a risk for the users (irritations, itching, or even burns caused by HE in overdose).
• the proportion of HE contained in the compositions is generally less than 3%, for example 1%, 1, 5%, 2% or 2.5%.
• the amount of HE will be 2%.
• the oily phase is provided solely by the HE, to the exclusion of any other vegetable oil.
• the invention relates to compositions consisting of an emulsion of one or more HE in one or more aqueous solutions, in particular in one or more hydrosols.
• the composition contains a hydrolate and an HE from the same plant.
• This embodiment is particularly interesting because it makes it possible to propose an integral plant preparation comprising all the components extracted from the plant. Indeed, during the distillation of a plant on the one hand ⁇ and on the other hand the hydrolate (or distillation water) whose compositions are different, beyond the fact that ⁇ is a very concentrated extract relative to the hydrolate.
• composition comprising:
• an EO of pink and a hydrosol of rose preferably 2% of EO of pink.
• peppermint EO and peppermint hydrosol preferably 2% peppermint EO
• tea tree HE a tea tree HE and a tea tree hydrosol, preferably 2% of tea tree HE.
• the hydrolate and ⁇ may be the only ingredients.
• emulsions can be obtained from a mixture of aqueous solutions and / or a mixture of HE or from emulsions mixed with each other.
• Emulsions containing aqueous solution and HEs, excluding any texturizing agent, are liquid. So as to facilitate handling and use, gelling agents may be added without this denatures the emulsion, including its properties.
• compositions according to the invention may contain gelling agents, preferably of natural origin, such as xanthan gum or alginates.
• gelling agents preferably of natural origin, such as xanthan gum or alginates.
• the addition of gelling agents respects the naturalness and purity of the product and makes it possible to obtain a creamier and more pleasant texture when applied to the skin.
• the texture of the composition will depend on the amount of gelling agent added.
• the proportion of gelling agent will generally be less than 0.1%, preferably absent from the composition.
• the proportion of gelling agent will generally be between 0.1% and 0.8% of the composition.
• the proportion of gelling agent will generally be between 0.8% and 2% of the composition.
• the proportion of gelling agent will generally be between 2% and 5% of the composition.
• the gelling agents are added after emulsification according to the desired texture.
• moisturizing agents preferably of natural origin can be added to the composition, for example glycerin.
• moisturizing agents When moisturizing agents are added, their proportion is generally between 2% and 10% of the composition. In general, the moisturizing agents may be added before or after emulsification; however, if the agents are hydrophobic, they will be added before emulsification.
• compositions according to the invention do not contain a preservative. They are protected from microbial growth because of the presence of HE in the composition. The advantages of the compositions of the invention are numerous.
• compositions are natural and healthy and they have less allergenic risk.
• the compositions can be 100% organic. They also have other very interesting properties. The inventors have indeed shown that the activity of the active ingredients is preserved in the emulsified compositions without surfactant and that the effectiveness of the compositions (without surfactant) is higher than that of the products with surfactants, in proportion to equivalent active ingredients.
• compositions are stable. Their stability is ensured by the method, in particular and preferably by an ultrasound treatment whose vibration frequency is greater than or equal to 1 MHz, as described in the patent WO2010 / 149668. Their stability at room temperature is observed for at least 3 months and up to more than 12 months.
• compositions according to the invention are compositions for topical use that can be used in humans or animals.
• the aqueous solution of the composition is water and is a mixture of katafray HE, camphor rosemary HE, lemon eucalyptus HE and juniper EO. common.
• An example of such a composition is described in Example 1; it has the effect of causing heating after topical application.
• Such a composition is in the form of a lotion preparatory to the muscular effort.
• a second object of the invention relates to the use of a composition containing an oil-in-water emulsion based on a mixture of katafray HE, camphor rosemary, lemon eucalyptus and common juniper. as a preparation lotion for muscular effort.
• FIGURES
• FIGURE 1 presents a comparison of heating on skin with the application of the composition A (without surfactant, curve marked with the squares) with the composition A-TS (with surfactant, curve marked with circles).
• Composition A is prepared using the method described in Application WO2010 / 149668 and defined below:
• Table 1 Ingredients of the composition "preparation for the effort" An A-TS composition was prepared using the same method and using the same ingredients as for Composition A, with the difference that 1% Twin 80 is added as a surfactant. b. Measurement of the heating effect of the product "preparation for the effort"
• composition A In order to evaluate the heating effect of composition A, it was applied to the arm of healthy subjects. The test was performed as follows:
• a defined area of the subject's arm was spotted and cleaned (with soap, then rinsed and dried).
• the application surface is about 9 cm 2 , a square of 3 cm side).
• the graph shows a rise in temperature during the first 5 minutes after application, to reach a maximum corresponding to a temperature increase of 2.2 ° C. The temperature then decreases gradually, remaining still one degree higher than the temperature of the zone before application.
• composition A to induce a heating in the skin and thus also the muscle underlying the area tested.
• Such a composition can therefore be used as a preparation product for muscular effort, by topical application to the muscles that will be stressed. c. Comparison of the effectiveness of composition A with that of a composition
• A-TS containing surfactants In order to evaluate the effectiveness of the formulation without surfactant, a comparative study was carried out using in parallel a product having the same components as composition A and prepared with the same process but to which surfactants were added; this composition is called A-TS composition.
• FIG. 1 represents the temperature increase obtained after topical application of these two compositions. While the composition A allows a temperature increase of more than 2 ° C. (as described in the previous paragraph), the composition A-TS (curve A-TS) induces a very limited rise in temperature, generally less than 0.5 ° C.
• composition A formulated without surfactant is more effective to cause heating, the composition A-TS comprising a surfactant, while these two compositions have the same proportion of active ingredients. There is therefore a better activity of the active ingredients in a formulation without surfactant compared to the same dose of active ingredients in the presence of surfactant. This observation highlights the fact that a formulation without surfactant allows a better bioavailability of the active ingredients.
• An integral peppermint gel preparation according to the invention can be obtained from the following ingredients:
• Table 2 Composition of an integral gel of peppermint
• Both ingredients are emulsified under high frequency vibration, as described in patent application WO2010 / 149668.
• the pH of the preparation is then adjusted to 7, if necessary.
• a texturizer may optionally be added to the emulsion so as to obtain a texture that is less liquid and easier to apply. It is also possible to add to this composition, without modifying the properties of interest, a preservative and an antioxidant in respective proportions to ensure the non-degradation of the product over time.
• Example 2 Remarkably and similar to the observations of Example 1, a stable equivalent product (prepared without high frequency vibration treatment) can not be obtained without the addition of surfactant. In addition, a product prepared with the same protocol but containing in addition a surfactant will be less effective.
• the product according to the invention can be used directly for conventional applications of peppermint essential oil (headaches, digestion, etc.). In topical use, it does not require additional dilution. In particular, no dilution in an oil is necessary. The touch of the product is completely aqueous and its application therefore leaves no unpleasant feeling of stickiness and fat.
• An integral lavender gel preparation according to the invention can be obtained from the following ingredients:
• Both ingredients are emulsified under high frequency vibration, as described in patent application WO2010 / 149668.
• the pH of the preparation is then adjusted to 7, if necessary.
• a texturizer may optionally be added to the emulsion so as to obtain a texture that is less liquid and easier to apply. It is also possible to add to this formula, without changing its properties of interest, a preservative and an antioxidant in respective proportions to ensure the non-degradation of the product over time.
• the product according to the invention can be used directly for conventional applications of essential oil of lavender aspic (burns, insect bites, etc.). In topical use, it does not require additional dilution. In particular, no dilution in an oil is necessary. The touch of the product is completely aqueous and its application therefore leaves no unpleasant feeling of stickiness and fat.
• EXAMPLE 4 Formulation of an integral tea tree gel
• a tea tree integral gel preparation according to the invention can be obtained from the following ingredients:
• Table 4 Composition of an integral tea tree gel
• Both ingredients are emulsified under high frequency vibration, as described in patent application WO2010 / 149668.
• the pH of the preparation is then adjusted to 7, if necessary.
• a texturizer may optionally be added to the emulsion so as to obtain a texture that is less liquid and easier to apply. It is also possible to add to this formula, without modifying the properties of interest, a preservative and an antioxidant in respective proportions to ensure the non-degradation of the product over time. Remarkably and similar to the observations of the previous examples, a stable equivalent product (prepared without high frequency vibration processing) can not be obtained without the addition of surfactant. In addition, a product prepared with the same protocol but containing in addition a surfactant will be less effective.
• the product according to the invention can be used directly for conventional applications of tea tree essential oil (sore throat, acne, antiseptic, etc.). In topical use, it does not require additional dilution. In particular, no dilution in an oil is necessary. The touch of the product is completely aqueous and its application therefore leaves no unpleasant feeling of stickiness and fat.
• tea tree essential oil saliva throat, acne, antiseptic, etc.

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• 2017
  • 2017-10-16 FR FR1771085A patent/FR3072280A1/fr active Pending
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