FR3087337A1 - DERMATOLOGICAL COMPOSITION FOR THE PREVENTION AND / OR TREATMENT OF MASTODYNIA - Google Patents

Abstract

The subject of the present invention is a dermatological composition comprising a plant progesterone and at least one plant extract, said plant extract preferably having a soothing, anti-edematous, decongestant and / or anti-inflammatory effect. The dermatological composition is in particular suitable for topical use. The present invention also relates to a process for the preparation of such a dermatological composition. The present invention also relates to the use of plant progesterone as a breast pain reliever in dermatological compositions and the use of these dermatological compositions for the prevention and / or treatment of mastodynia.

Description

DERMATOLOGICAL COMPOSITION FOR THE PREVENTION AND / OR TREATMENT OF MASTODYNIA

Technical area

The present invention relates to the prevention and / or treatment of mastodynia.

State of the art

Mastodynia, also called breast pain, is one of the clinical manifestations of PMS. They are mainly due to a deficiency in progesterone.

This is a frequent problem, sometimes disabling in women in the genital area. Thus, 75% to 85% of young and pre-menopausal women suffer from it, as well as 60% to 70% of women of all ages.

These pains appear more or less early in the cycle. They range from sensitivity to contact to disabling pain, hampering movement and lying down. Any pressure can be very painful. Socio-professional and private repercussions can be significant. In addition, persistent mastodynia worries women.

The pathophysiology corresponds to a deficiency in progesterone, found in all dysovulation situations: beginning and end of genital activity, increase in BMI (Body Mass Index) (18% obesity, 30% overweight) , OMPK (Micro-Polycystic Ovary Syndrome), hypothyroidism, immediate consequences of stopping OP (Oestro-Progestative) contraception or implants, smoking and / or disturbed lifestyle.

Progesterone is a steroid hormone that is secreted in a normal cycle by granulosa cells, under the luteinizing action of LH (Luteinizing Hormone). The LH surge leads to the rupture of the follicle, then neo-angiogenesis invades the internal theca and the granulosa, which allows the diffusion of progesterone at the level of targets with self-regulation system by positive and negative feedback.

Progesterone deficiency is responsible for the extravasation of interstitial fluid from the blood to the tissues which then become congestive and edematous, responsible for mastodynia.

A medication currently used for the treatment of mastodynia is Progestogel gel, which combines synthetic progesterone and many excipients. However, on the one hand this drug has very low efficacy and, on the other hand, the excipients include in particular 96% ethanol, sometimes a source of irritation, as well as octyldodecanol, trolamine, macroglycerol, products likely to trigger skin reactions.

There is therefore a real need to provide an improved solution for the prevention and / or treatment of mastodynia, which is preferably more effective and has little or no side effects.

detailed description

Surprisingly, the inventor has demonstrated that a plant progesterone, in particular diosgenin, formulated within a dermatological composition suitable for topical application is effective in the prevention and / or treatment of mastodynia.

Advantageously, plant progesterone, preferably a diosgenin extracted from yam, can be used within an original combination of active agents comprising one or more other plant extracts, said combination of active agents making it possible to prevent and / or treat mastodynia. This combination of active agents is preferably formulated in a dermatological composition intended for topical application, in particular on the breasts.

Not only is this dermatological composition effective, but it does not include any excipient capable of causing side effects, such as alcohol or preservatives. In addition, all of the active ingredients in this composition are preferably entirely of plant origin.

The dermatological composition according to the invention therefore constitutes an effective alternative to the administration of oral progesterone or to ProgestogeL. It also has the advantage of not comprising synthetic progesterone. However, patients are looking for natural solutions and want to avoid synthetic hormones.

The application of the dermatological composition according to the invention by a gentle and rapid massage, for example less than a minute per breast, makes it possible to further improve the preventive and / or therapeutic effect of the composition.

Advantageously, the dermatological composition according to the invention allows transcutaneous penetration of the active agents and a prolonged release of natural progesterone, without peak. This extended release allows homeostasis at the dermo-epidermal junction, a guarantee of better efficiency.

In addition, the dermatological composition according to the invention has the advantage of penetrating quickly, of not sticking and not staining.

A first object of the invention is to provide a dermatological composition comprising a plant progesterone, preferably diosgenin, and at least one plant extract, said plant extract preferably having a soothing, anti-edematous, decongestant and / or anti- inflammatory.

The dermatological composition as defined above preferably comprises from 3% to 15% of plant progesterone.

The plant extract as defined above is preferably selected from the group consisting of an extract of Arnica montana, an extract of red vine, an extract of turmeric and an extract of Meadowsweet.

The dermatological composition as defined above preferably comprises:

(i) 1% to 15% of Arnica montana extract, (ii) 1% to 15% of red vine extract, (iii) 1% to 15% of turmeric extract and / or (iv) 1% to 15% of meadowsweet extract.

Diosgenin is preferably provided in a hydrophilic vectorized form.

The dermatological composition as defined above can be in the form of a gel, cream, milk, lotion or emulsion.

Another subject of the invention is a dermatological composition comprising a plant progesterone for use in the prevention and / or treatment of a mastodynia, such as a premenstrual mastodynia or a benign mastopathy.

The dermatological composition for use in the prevention and / or treatment of mastodynia is for example as defined above.

The dermatological composition is preferably applied by a massage of less than one minute on each breast.

Another object of the invention is the use of plant progesterone as a breast pain reliever in a dermatological composition.

Another subject of the invention is a process for preparing a dermatological composition suitable for the prevention and / or treatment of mastodynia, comprising a step of mixing a plant progesterone with at least one plant extract.

Plant progesterone

The progesterone used in the dermatological composition is a plant progesterone, preferably of natural origin.

Plant progesterone is preferably diosgenin.

Diosgenin is also called (25R) -5-Spirosten-3p-ol.

Although termed plant progesterone, diosgenin is a precursor of progesterone. In addition, diosgenin is not transformed into progesterone by the human body, whether it is used orally or topically.

Plant progesterone, in particular diosgenin, used topically, advantageously has a breast pain relieving effect.

Diosgenin is for example present in the tubers of plants, in particular in saponins.

Diosgenin is preferably extracted from a plant, for example from a plant of the genus Dioscorea, for example from yam.

The yam is for example selected from the group consisting of Dioscorea villosa (also called wild yam), Dioscorea zingiberensis, Dioscorea alata and Dioscorea burkilliana.

Diosgenin can be obtained by any technique well known to those skilled in the art, for example by enzymatic hydrolysis and / or acid hydrolysis of the tubers of yam, preferably pretreated to remove the starch and the fibers.

The diosgenin is preferably a purified diosgenin obtained from a plant, in particular from a plant extract, such as a yam tuber.

Other plant extract (s)

The dermatological composition also advantageously comprises at least one other plant extract.

The plant extract is preferably selected from a plant extract having a pain-relieving effect, an anti-edematous effect, a decongestant effect, an anti-inflammatory effect and combinations thereof.

Non-limiting examples of plant extract having a pain relieving effect include an extract of Meadowsweet (also called Filipendula ulmaria) or an extract of Arnica montana.

Non-limiting examples of plant extract having an anti-inflammatory effect include an extract of Meadowsweet, an extract of Arnica montana or an extract of turmeric.

Non-limiting examples of plant extract having an anti-edematous effect include red vine (also called Vitis vinifera) or a turmeric extract.

The plant extract is for example selected from the group consisting of an extract of Arnica montana, an extract of red vine, an extract of Queen of the meadows and an extract of turmeric.

The plant extract as defined above can be an extract of the whole plant or of at least part of the plant, such as for example the leaves, stem, root, tuber, flower, fruit, seed and / or skin.

The Arnica montana extract is preferably an extract from the flower, in particular from the whole flower head, stem, seed and / or root.

The red vine extract is preferably an extract of red vine leaf.

The Queen of Meadows extract is preferably an extract of the flowering tops of the Queen of Meadows.

Dermatological composition

The present invention particularly relates to a dermatological composition comprising a plant progesterone as defined above, preferably diosgenin.

Plant progesterone being soluble in alcohol, but not in water, it is preferably provided in a form allowing it to be hydrophilic.

The dermatological composition as defined above is preferably characterized in that the plant progesterone is provided in a hydrophilic vectorized form.

The vectorization of plant progesterone consists in associating plant progesterone with a vector, so as to improve its hydrophilic character.

The vector can be any suitable vector well known to those skilled in the art, such as a microcapsule, a liposome and / or a vesicle.

In an advantageous embodiment, the vector also allows a prolonged and peak-free release of plant progesterone, in particular by releasing plant progesterone from the vector at the time of application of the dermatological composition to the skin, in particular by massage.

The dermatological composition as defined above preferably does not include synthetic progesterone.

By "synthetic progesterone" is meant here a progesterone obtained from cholesterol or a cholesterol derivative or analog.

The dermatological composition as defined above preferably comprises from 3% to 15% of plant progesterone, preferably of diosgenin, more preferentially from 5% to 10% of plant progesterone, preferably of diosgenin.

Unless otherwise indicated, the percentages are here mass percentages. A composition comprising x% of a compound means, for example, that said composition comprises x grams of said compound per 100 g of composition.

Advantageously, the dermatological composition further comprises at least one plant extract having a soothing effect, an anti-edematous effect, a decongestant effect and / or an anti-inflammatory effect.

The plant extract is in particular as defined above.

The dermatological composition as defined above preferably comprises diosgenin and at least one plant extract having a soothing, anti-edematous, decongestant and / or anti-inflammatory effect.

Diosgenin and the plant extract (s) having a soothing, anti-edematous, decongestant and / or anti-inflammatory effect are preferably the only active ingredients in the dermatological composition.

By the term "active" is meant here a compound having an effect on the prevention and / or treatment of mastodynia.

The plant extract is preferably selected from the group consisting of an extract of Arnica montana, an extract of red vine, an extract of turmeric and an extract of Meadowsweet.

A preferred dermatological composition according to the invention is a composition as defined above comprising a plant progesterone, preferably diosgenin, and at least two or at least three plant extracts, said plant extracts being selected from the group consisting of an extract of Arnica montana, an extract of red vine, an extract of turmeric and an extract of Meadowsweet.

A preferred dermatological composition according to the invention is a composition as defined above comprising a plant progesterone, preferably diosgenin, an extract of Arnica montana, an extract of red vine, an extract of turmeric and an extract of Reine des near.

In an advantageous embodiment, the dermatological composition as defined above comprises a plant progesterone, preferably diosgenin, an extract of Arnica montana, an extract of red vine, an extract of turmeric and an extract of meadowsweet , to the exclusion of any other plant and / or any extract of another plant.

The dermatological composition is preferably a composition as defined above, characterized in that it comprises:

- 3% to 15% of plant progesterone, preferably 5% to 10%,

1% to 15% of Arnica montana extract, preferably 5% to 10%,% to 15% of red vine extract, preferably 5% to 10%,% to 15% of turmeric extract, preferably 5% to 10%, and / or 1% to 15% of meadowsweet extract, preferably 5% to 10%.

The dermatological composition as defined above can for example comprise:

- 5% to 10% of diosgenin,

- 5% to 10% of Arnica montana extract,

- 5% to 10% of red vine extract,

- 5% to 10% of turmeric extract and

- 5% to 10% of meadowsweet extract.

In an advantageous embodiment, the dermatological composition as defined above also comprises thermal water, preferably Vichy thermal water.

Vichy thermal water is used to improve skin hydration.

Vichy thermal water is therefore not an active ingredient in the sense of the invention.

By “Vichy thermal water”, also called “Vichy water”, is meant here water coming from one or at least one of the sources of the Vichy basin, such as for example water coming from the Celestins source, Chomel source, Grande Grille source, Hospital source, Lucas source, Lys source, Dome source, or mixtures thereof.

Vichy thermal water preferably comes from the Lucas spring.

Vichy thermal water is a water naturally rich in mineral salts and trace elements.

For example, the dermatological composition as defined above also comprises from 1% to 10% of thermal water, in particular Vichy thermal water, preferably from 2% to 5% of thermal water, in particular Vichy thermal water.

The dermatological composition as defined above is preferably suitable for topical use, in particular for application to the breasts.

The dermatological composition as defined above is for example in the form of a gel, cream, milk, lotion or emulsion.

In an advantageous embodiment, the dermatological composition, preferably in the form of an emulsion or a cream, comprises:

- 3% to 15% of plant progesterone, in particular of diosgenin, preferably 5% to 10% of plant progesterone, in particular of diosgenin, 1% to 15% of extract of Arnica montana, preferably of 5% to 10% extract of Arnica montana,

1% to 15% of red vine extract, preferably 5% to 10%, of red vine extract

1% to 15% of turmeric extract, preferably 5% to 10% of turmeric extract, and / or% to 15% of meadowsweet extract, preferably of 5% to 10% of extract of Meadowsweet, 10% thermal water, in particular Vichy thermal water, preferably 2% to 5% thermal water, in particular Vichy thermal water.

The dermatological composition as defined above preferably comprises only active ingredients of plant origin.

In a preferred embodiment, the dermatological composition as defined above does not include alcohol, in particular does not include ethanol.

In a preferred embodiment, the dermatological composition as defined above does not comprise ethanol, nor macroglycerol, nor trolamine, nor octyldodecanol.

In a preferred embodiment, the dermatological composition as defined above does not comprise any preservative, in particular does not comprise any chemical additive.

The dermatological composition as defined above can be prepared by a preparation process as defined below.

Use of plant progesterone as a breast pain reliever

The present invention also relates to the use of plant progesterone as a breast pain reliever in a dermatological composition, in particular suitable for topical use, in particular on the breasts.

The present invention also relates to the use as defined above of plant progesterone in association with at least one plant extract in a dermatological composition, for example simultaneously, separately, or spread over time.

Plant progesterone, preferably diosgenin, is especially as defined above.

The plant extract is in particular as defined above.

The invention particularly relates to the use as defined above of progesterone in combination with an extract of Arnica montana, an extract of red vine, an extract of turmeric and an extract of Meadowsweet in a dermatological composition, for example simultaneously, separately, or spread over time.

The combination of plant progesterone, preferably diosgenin, with at least one plant extract gives the dermatological composition as defined above a soothing effect and, preferably, at least one, more preferably at least two of the following effects or the following three effects: anti-edematous, decongestant and / or anti-inflammatory.

By "soothing effect" is meant here the reduction or disappearance of breast pain.

The soothing effect of a compound or a composition can be evaluated by any suitable method well known to those skilled in the art.

By "anti-edematous effect" is meant here the reduction or resorption of edema of the breast tissue.

Edema is a swelling of the tissues due to extravasation of the interstitial fluid from the blood into a tissue, for example in breast tissue.

The anti-edematous effect of a compound or a composition can be evaluated by any suitable method well known to those skilled in the art.

By "decongestant effect" is meant here the reduction in extravasation of tissue.

The decongestant effect of a compound or a composition can be evaluated by any suitable method well known to those skilled in the art.

By “anti-inflammatory” action, is meant here the reduction and / or disappearance of the inflammation of the breast tissue.

The anti-inflammatory effect of a compound or a composition can be evaluated by any suitable method well known to those skilled in the art.

Process for the preparation of a dermatological composition based on plant progesterone

The present invention also relates to a process for the preparation of a dermatological composition based on plant progesterone, said composition being in particular useful for the prevention and / or treatment of mastodynia.

The method as defined above notably comprises a step of mixing a plant progesterone, preferably diosgenin, with at least one plant extract.

Diosgenin, plant extract and dermatological composition are in particular as defined above.

The preparation process as defined above can comprise the following steps:

providing a diosgenin in vector hydrophilic form, mixing the diosgenin in a vector hydrophilic form with at least one plant extract.

The preparation process as defined above can comprise the following steps:

- vectorize a diosgenin, for example by means of a microcapsule, a liposome and / or a vesicle, to obtain a diosgenin in vectorized hydrophilic form, mix the diosgenin in vectorized hydrophilic form with at least one plant extract.

In the process as defined above, plant progesterone, in particular diosgenin in a hydrophilic vectorized form, can be mixed with an extract of arnica montana, an extract of red vine, an extract of meadowsweet, an extract turmeric and, optionally, thermal water, such as Vichy thermal water.

Prevention and / or treatment of mastodynia

Mastodynia, also called breast pain, is characterized by pain affecting at least one breast, usually both breasts. These breast pains are usually accompanied by inflammation, congestion and / or edema.

Mastodynia is preferably due to a deficiency in progesterone.

Mastodynia can for example be a premenstrual mastodynia or a benign mastopathy.

By the expression “treatment of a mastodynia”, one indicates here the suppression or the reduction of at least one symptom of mastodynia, preferably of the whole of the symptoms of mastodynia, in particular in a subject suffering from mastodynia .

The desirable effects of treating mastodynia include:

- the reduction or elimination of breast pain, this breast pain resulting in particular from breast edema, breast congestion and breast inflammation, the reduction or elimination of breast edema,

- the reduction or suppression of breast congestion and / or the reduction or suppression of breast inflammation.

By the expression "prevention of mastodynia", is meant here the prevention, at least partially, of the appearance of at least one of the symptoms of mastodynia, preferably all of the symptoms of mastodynia, especially in a subject likely to suffer from mastodynia.

The prevention of mastodynia makes it possible, preferably, to:

- prevent the appearance of breast pain or reduce their intensity and / or duration,

- prevent the appearance of breast edema or reduce its intensity and / or duration,

- prevent the appearance of breast congestion or reduce its intensity and / or its duration, and / or prevent the appearance of breast inflammation or reduce its intensity and / or its duration.

Dermatological composition for the prevention and / or treatment of mastodynia

The present invention also relates to a dermatological composition comprising a plant progesterone for use in the prevention and / or treatment of mastodynia.

The present invention also relates to a method for preventing and / or treating mastodynia in a subject, comprising the topical administration of a dermatological composition comprising a plant progesterone.

Plant progesterone and the dermatological composition are in particular as defined above.

The prevention and / or treatment of a mastodynia is notably as defined above in the section of the same name.

Mastodynia is for example a premenstrual mastodynia or a benign mastopathy.

The dermatological composition is preferably applied locally to each breast, for example by massage, preferably less than one minute, for example from 30 seconds to one minute.

The dermatological composition can for example be administered one to three times a day, preferably once a day.

For the treatment of mastodynia, the dermatological composition is preferably administered from the onset of breast pain until the onset of menstruation.

For the prevention of breast pain, the dermatological composition is preferably administered at least 15 ^th day of the menstrual cycle until the onset of menstruation. If a severe premenstrual syndrome, dermatological composition can be administered before, eg from the 10 ^th day of the menstrual cycle until menstruation.

The subject is a female mammal, preferably human.

When the subject is human, it is indifferently designated by the term "woman" or "patient".

The prevention and / or treatment of mastodynia concerns in particular any subject understood from puberty to pre-menopause.

The subject may also be a pregnant woman.

The subject is preferably between 10 and 60 years old, more preferably between 13 and 53 years old.

The subject preferably does not suffer from a malignant disease of the breast.

Other characteristics and advantages of the invention will emerge more clearly from the examples which follow, given by way of nonlimiting illustration.

EXAMPLES

Example 1: Dermatological composition for the prevention and / or treatment of mastodynia

The dermatological composition according to the invention is prepared by mixing in particular diosgenin extracted from vectorized yam by means of microcapsules, an extract of arnica montana, an extract of red vine, an extract of queen of the meadows, an extract of turmeric and Vichy thermal water.

The dermatological composition is in the form of a cream.

Example 2: Effect of the dermatological composition according to Example 1 Material and methods

The dermatological composition of Example 1 is tested on 20 volunteers, under dermatological control.

The volunteers are pre-menopausal and well-regulated women.

The composition is applied on the chest of volunteers over 10 days, starting from 15 ^th day of the menstrual cycle. The application is carried out by a gentle massage of less than a minute on each breast.

The monitoring of volunteers is carried out for 4 to 6 weeks.

Results

The dermatological composition thus allows effective and safe sedation. The product meets all the toxicological and dermatological tests imposed.

Claims (10)

1. Dermatological composition comprising a plant progesterone and at least one plant extract. 2. Dermatological composition according to claim 1, characterized in that the plant progesterone is diosgenin. 3. Dermatological composition according to claim 1 or 2, characterized in that the plant extract has a soothing, anti-edematous, decongestant and / or anti-inflammatory effect. 4. Dermatological composition according to one of claims 1 to 3, characterized in that said plant extract is selected from the group consisting of an extract of Arnica montana, an extract of red vine, an extract of turmeric and an extract of Meadowsweet. 5. Dermatological composition according to one of claims 1 to 4, characterized in that the plant progesterone is provided in a hydrophilic vectorized form. 6. Dermatological composition according to one of claims 1 to 5, characterized in that said composition is in the form of a gel, cream, milk, lotion or emulsion. 7. Dermatological composition for use in the prevention and / or treatment of mastodynia, characterized in that said dermatological composition comprises a plant progesterone. 8. Dermatological composition for use according to claim 7, characterized in that the dermatological composition is as defined in one of claims 1 to 6. 9. Use of plant progesterone as a breast pain reliever in a dermatological composition. 10. A method of preparing a dermatological composition according to one of claims 1 to 6, comprising a step of mixing a plant progesterone with at least one plant extract.