WO2007069015A2

WO2007069015A2 - Cosmetic compositions based on essential oils and use thereof in pain relief

Info

Publication number: WO2007069015A2
Application number: PCT/IB2006/003502
Authority: WO
Inventors: Eddy Phelizon
Original assignee: Deylon Sarl
Priority date: 2005-12-13
Filing date: 2006-12-07
Publication date: 2007-06-21
Also published as: WO2007069015A3; FR2894483A1; FR2894483B1; EP1971353A2

Abstract

The present invention relates to the field of the essentials of life, and in particular to the fields of cosmetology and dermatology. The invention relates more specifically to cosmetic compositions for pain relief, characterized in that they are composed of essential oils of lavender, of cypress, of Melaleuca and of geranium and also mother tinctures of plantain and of tormental, the whole incorporated into an aqueous-alcoholic carrier. Use of the cosmetic compositions for pain relief and the healing of skin lesions.

Description

Cosmetic compositions based on essential oils and their use in the relief of pain

The present invention relates to the necessities of life, more particularly to the field of cosmetology and dermatology.

It relates more particularly to the field of phytotherapy and aromatherapy.

The subject of the invention is specifically cosmetic compositions, and more specifically phytotherapeutic compositions based on a mixture of essential oils intended to relieve pain, and to facilitate the repair and treatment of dermal tissues damaged by the manifestations. cold sores such as cold sores.

Herpes labialis is caused mainly by the herpes simplex virus type 1. It is classically called cold sore. It is the most common form of herpes.

In their lifetime, 90% of all subjects come into contact with the herpes simplex virus type 1, most often before the second year of life. Viruses get into the body through the skin or mucous membranes. Contamination can occur from the first contact with an affected person. However, this primary infection often goes unnoticed or is manifested by herpetic gingivostomatitis (a foul smell of breath in children). Once the virus is installed in the human body, it persists for life. After primary infection, the viruses are stored in the nerve ganglia and can remain inactive for years without being detected by the immune system.

Different stimuli such as solar radiation, psychic stress, hormonal factors, local stimuli such as burns or other diseases can cause viruses to become active and develop as a cold sore on the surface. skin. At first there is a feeling of tension and tingling. After a few hours, painful vesicles appear, arranged in groups and filled with a clear, highly infectious liquid. The vesicles break and dry out. The duration of the symptoms does not generally exceed 10 days.

Cold sores, by their recurrence and recurrence, are a frequent reason for consultation in general medicine. This benign affection is highly uncomfortable, as much by the sensation of discomfort that it induces, as by the unattractive aesthetic aspect that it generates. The active drug ingredient of choice currently recognized and available on the market for cold sores is aciclovir, an antiviral molecule, and its derivatives, such as ganciclovir. Usable by see cutaneous, aciclovir is widely marketed. In the event of a major surge, this medication may be prescribed orally or even intravenously.

It should be noted that the action of aciclovir results from the blocking of viral replication by inhibiting its DNA polymerase. Aciclovir monophosphate is also incorporated into the viral chain, putting an end to its elongation. However, the virus stored in the ganglia, are removed from the action of aciclovir and therefore are not destroyed.This is why after stopping treatment, a herpes outbreak can occur at any time.

In addition, the level of effectiveness is even more important that the drug is applied early, before the manifestation of clinical signs, which of course is hardly feasible or even feasible.

It appears that aciclovir prevents replication of the virus but does not support local skin lesions caused by herpes, and that it does not eradicate herpes disease in a subject: intracellular "reservoir" viruses can to manifest at any time.

This is why the current treatment of cold sores appears as incompletely satisfactory.

In addition, dermatoses are often over-infected by certain germs that develop in quantity, while breaking the local skin balance. There is a possibility of superinfection of the herpes lesion area. Various bacteria or Candida fungi can be found.

In view of the above, it should be noted that there is a real need to improve the management of traditional treatment of herpes labial flare, beyond the simple local antiviral treatment, since the usual treatment regimen is not concerned. relief of pain and repair of injured tissue. Now, it is precisely the inflammatory phenomenon, the induration of the damaged tissues, which causes the discomfort and the pain noted.

The compositions which are the subject of the invention are intended to promote the repair of damaged tissues, an aspect not supported by the antiviral treatment, while acting on the painful consequences of cold sores.

These compositions consist of a mixture of vegetable essential oils of plants. They consist more precisely of a mixture consisting of four essential oils and two mother tinctures.

They consist specifically of the combination of essential oils of Lavender, Cypress, Melaleuca alternifolia and Geranium, and plant tincture of Plantain and Tormentille, all incorporated in an excipient or an inert vehicle, non-toxic, acceptable for the skin and mucous membranes.

The essential oils of plants have an immediate effect on the superficial blood circulation. They are therefore able to accelerate the efficiency of the drainage of damaged tissues. The draining and anti-inflammatory properties of some essential oils help to reduce the local compression of nerve endings, which causes pain.

Thus, it is conceivable to use the compositions which are the subject of the invention not only for the adjunctive treatment of cold sores, but also for any type of labial and peri-labial lesions, as well as for the small affections of the herpes labialis. mouth of the mouth ulcer type.

The essential oils are devoid, compared to conventional antiviral and antimicrobial drugs, microbial or viral resistance effect and any addiction of germs to these essential oils, which allows frequent use, particularly suitable for recurrent herpes outbreaks.

In addition to the essential oils, the compositions which are the subject of the invention comprise plants in another stabilized form: the mother tinctures. Here again, the methods for obtaining and controlling mother tinctures are described in the European Pharmacopoeia, allowing the use of constant products. These are alcoholic extracts.

The cutaneous lesions are sensitive to light and in particular lesions of herpetic origin. It is thus recommended to protect the injured areas from sun exposure and in particular from UV rays. As a result, it will be useful to include the compositions a sun filter UV.

The invention therefore consists of a mixture of several essential oils and mother tinctures, characterized in that the mixture contains the following active ingredients:

1) Lavender essential oil

It has analgesic, antiseptic and healing properties. Its main components are: d-pinene

- d-camphene

- d-sylvestrene cymene - sabinol

- valerianic acid

2) Essential oil of Melaleuca alternifolia

It has broad-spectrum anti-infective and anti-viral properties. Its main components are:

terpinene-4-ol

- gamma-terpinene and alpha-terpinene - alpha-terpinol

- alpha-pinene sabinene

- limonene cineole - p-cymene terpinolene

- aromadendrene

3 ^" ) Geranium essential oil

It has healing, antiseptic and analgesic properties. Its main components are:

- citronellol

- geraniol - terpinol

- linalool

- borneol

- eugenol phellandrene

4) Cypress essential oil

It has antibacterial properties, and venous and lymphatic decongestion. Its main components are: - Monoterpenes: alpha-pinene, delta-3-carene, terpilonene, limonene, myrcene, gamma-terpinene, camphene, thuyene, sabinene, alpha-terpinene, beta-pinene, para-cymene - Monoterpenols: terpinene-4-ol, cedrol, alpha-terpineol, linalool, borneol

- Sesquiterpenes: beta-caryophyllene, alpha-humolene, gamma-muurolene, delta-cadinene, germacrene-D-

Terpene Esters: Bornyl Acetate

5) Plantain mother tincture,

It has antibacterial properties, conferred by the aucubine it contains, hence a common use in skin inflammation. Its main components are: aucubine

- chorogenic acid tannins, neochlorogenic acid coumarin - flavonoids

5) Tormentille mother tincture,

Its high tannin content gives it astringent properties. Its main components are:

- tannins

- Agrimonine gallic acid, ellagic acid

- gallates of catechol

According to one form of the invention, it is possible to add to this combination lavender alcoholate whose properties are substantially the same as those of the essential oil of lavender.

These active ingredients are incorporated in a water-alcoholic excipient suitable for the topical route, that is to say the local application on the skin (cutaneous application) and the mucous membranes.

It has been investigated the possibility of using an excipient capable of reinforcing the properties of the mixture of active ingredients of phytotherapic origin. Thus it has been determined that an easily volatile hydroalcoholic vehicle proves to be a wise choice. Indeed, the use of an aqueous and alcoholic mixture allows, by a phenomenon of evaporation during application to the skin, an instantaneous lowering of the local temperature on the application zone. This leads to a local vasoconstriction which contributes, with the feeling of freshness, to the pain, which is precisely the goal sought together with the action of the active ingredients.

In order to obtain a homogeneous composition that is easy to apply, a suitable solution consists in obtaining a composition of semi-liquid consistency.

Preferably, the excipient used is a mixture of acrylic acid polymer, water and alcohol.

Preferably, the acrylic acid polymer is a product of the range sold under the brand name "CARBOPOL®" (Goodrich).

A sunscreen may be added to the excipient gel, such as Parsol® MCX, in proportions varying preferably from 0.1 to 7% by weight relative to the composition of the gel.

It is also possible to incorporate in the compositions flavoring or odoriferous natural or artificial substances, in order to make the application of the product more pleasant.

However, we must take into account the existence of people wishing to use only products with reduced alcohol content.

Also, there should be alternative formulations low in alcohol, which contain the active ingredients defined above for each essential oil used.

A solution of choice for this problem is to use, in replacement of the mother tinctures, alcohol-free plant extracts such as hydro-glycolic extracts of plants; it is also possible to reduce the content of the compositions to Lavender alcoholate and / or to replace the alcohol at 96 ° or 60 ° used as an excipient with alcohol at 20 °.

The compositions according to the invention are intended for use by topical application at a rate of one to several applications per day on the injured areas.

The following examples illustrate the invention without limiting it. The percentages are by weight or by volume of the total preparation.

EXAMPLE 1 Example of Production of the Compositions Subject of the Invention

The active products consisting of the essential oils and the mother tinctures are first mixed. This mixture is then incorporated into the hydroalcoholic excipient to obtain the desired fluidity.

In particular, a gel whose initial formula is defined as follows can be used as a hydroalcoholic excipient:

Example 2: Variant of the Previous Formulation, with Lower Alcohol Content

In this variant of the composition, the mother tinctures are replaced by hydro-glycolic extracts, and the desired consistency of the hydroalcoholic excipient gel is obtained using alcohol at 20 ° instead of the alcohol at 96 ° or 60 ° C. °.

Lavender essential oil 0.5% to 25%

Cypress essential oil 0.5% to 25%

Essential oil of Melaleuca alternifolia 0.5% to 25%

Geranium essential oil 0.5% to 25%

Hydro-glycolic extract of Plantain 0.5% to 50%

Hydro-glycolic Tormentilla Extract 0.5% to 50%

Example 3: formulation including aromas

Example 4: Process for producing the compositions according to the invention

1) Mixture of active ingredients

All of the essential oils and mother tinctures or hydro-glycolic extracts are miscible with each other, there is no fear of lack of homogeneity of their mixture.

The starting tincture is the mother tinctures or the hydro-glycolic extracts of Plantain and Tormentille. After homogenization by stirring, the four essential oils are incorporated one after the other, stirring the mixture between each addition.

Optionally, complete with Lavender Alcoholate to adjust to the desired volume. A final homogenization of the liquid by stirring is then performed.

2) Incorporation into the excipient

The above-defined mixture is incorporated in a hydrophilic vehicle, in particular a hydroalcoholic gel, avoiding the inclusion of air bubbles in the composition. The gelling product is a carbomer gel, or polyacrylamide, or cellulose derivative.

Preferably, the hydroalcoholic gel has the formula defined as follows:

In order to obtain the desired consistency and viscosity for skin application and depending on the chosen application device, a sufficient and appropriate amount of alcohol is added at 96 °, 60 ° or 20 °.

4) Conditioning

The packaging must be adapted to the mode of application to the skin, as well as to the consistency defined for the compositions (fluid, semi-solid, solid), such as ointments, creams, gels, water-in-silicone emulsions, oil-in-water emulsions, water-in-oil emulsions, or liposomes.

The compositions comprising a significant amount of volatile products, it is necessary to ensure a good seal capping system.

Compositions comprising essential oils and extracts of plants sensitive to light, should be used containers or opaque packaging.

In the case of a semi-solid consistency such as a gel, it may be used for example a packaging consisting of a stick provided with a metal rollerball. This ball makes it possible to regulate the flow and to ensure a measured delivery of the product.

Preferably, a metal ball coated with a gold film is used. This avoids any potential allergies due to contact with nickel may enter the composition of the metal ball. In addition, the very high thermal conductivity of gold allows, when applied to the herpes zone, to increase the freshness effect induced by the gel, by promoting the caloric pumping at the level of the lesion.

In the case of a solid consistency, we can use a container provided with a free end for direct application of the product, such as a stick lip. Another suitable packaging and allowing the single use is the wipe, which is soaked compositions according to the invention before packaging in aluminum foil to have a sealed package.

It is also possible to condition the product in the form of patches intended to be affixed directly to the lesion area.

5) Analytical control of the compositions:

The active ingredients constituted by essential oils are those defined in the monographs provided for by the European Pharmacopoeia.

Thin layer chromatography and gas chromatogram examination appear as analytical techniques of choice for checking the sample composition of the mixture.

For products not containing a monograph, the quality having the analytical composition delivered by the supplier of the products concerned must be taken as a reference. The same is true of excipients.

As regards the final compositions including the excipients, the physical properties, in particular the fluidity and the viscosity, are evaluated according to the conventional control methods.

Claims

1. Cosmetic or dermatological phytotherapeutic compositions, characterized in that they contain an association of essential oils of Lavender, Cypress, Melaleuca alternifolia and Geranium, as well as the mother tincture of Plantain and the mother tincture of Tormentil, in an inert vehicle or vehicle, non-toxic, acceptable for the skin and mucous membranes.

2. Compositions according to claim 1, characterized in that the mother tinctures of Plantain and Tormentille are replaced by hydro-glycolic extracts of

Plantain and Tormentille.

3. Compositions according to claim 1 or claim 2, characterized in that the mixture is included in an excipient or hydroalcoholic vehicle easily volatile.

4. Compositions according to the preceding claims, characterized in that they are in the form of ointments, creams, gels, water-in-silicone emulsions, oil-in-water emulsions, water-in-oil emulsions, or liposomes.

5. Compositions according to the preceding claims, characterized in that the active products in the mixture according to claim 1 are present in proportions by weight or by volume of the order of:

- Lavender essential oil: 0.5% to 25%

Cypress essential oil: 0.5% to 25%

Essential oil of Melaleuca alternifolia: 0.5 to 25%

Geranium essential oil: 0.5% to 25%

Mother tincture or hydro-glycolic extract of Plantain: 0.5% to 50% - Mother tincture or hydro-glycolic Tormentil extract: 0.5% to 50%

Lavender Alcoholate: 0% to 40%

Hydroalcoholic gel excipient: 1% to 95%

96% alcohol: 1% to 30%

6. Compositions according to claim 3, characterized in that the alcoholic excipient is a gel formed of a mixture of acrylic acid polymer, water and alcohol.

7. Compositions according to the preceding claim, characterized in that the acrylic acid polymer is the product marketed under the brand name.

CARBOPOL® (Goodrich).

8. Compositions according to the preceding claims, characterized in that it incorporates flavoring substances.

9. Compositions according to any one of claims 1 to 8, characterized in that they are applied to the skin or the mucous membranes by means of a container provided, at the end intended for the application, a ball to regulate the flow and ensure a measured delivery of the product.

10. Compositions according to any one of claims 1 to 8, characterized in that the solid consistency compositions are applied to the skin or mucous membranes by means of a container provided with a free end allowing the direct application of the product .

11. Compositions according to any one of claims 1 to 8, characterized in that they are applied to the skin or mucous membranes by means of wipes previously soaked in product.

12. Compositions according to any one of claims 1 to 8, characterized in that they are applied in the form of patches directly on the lesion area.

13. A method of manufacturing a composition according to the preceding claims, characterized in that one mixes the mother tinctures or the hydro-glycol extracts of Plantain and Tormentille, which one adds the essential oils of Lavender, Cypress, Melaleuca alternifolia, and Geranium, then possibly the Lavender alcoholate, and that one mixes this mixture of active products in a hydrophilic vehicle, then that one adds there alcohol with 96 °, with 60 ° or 20 ° to obtain the desired fluid consistency.

14. Method according to the preceding claim, wherein the hydrophilic vehicle is a hydroalcoholic gel.

15. Use of the compositions according to claims 1 to 13, topically applied to one to several applications per day on the injured areas.