WO2002005779A1

WO2002005779A1 - Composition, in particular cosmetic, containing dhea and/or its precursors or derivatives, and a vitamin

Info

Publication number: WO2002005779A1
Application number: PCT/FR2001/001792
Authority: WO
Inventors: Roland Roguet; Guy Courchay
Original assignee: L'oreal
Priority date: 2000-07-13
Filing date: 2001-06-08
Publication date: 2002-01-24
Also published as: AU2001267623A1; FR2811566B1; FR2811566A1

Abstract

The invention concerns a composition containing DHEA and/or a biological precursor and/or chemical or biological derivative thereof, characterised in that it further comprises at least a vitamin selected among vitamins B2, B3, B6, B8, B12, D and K. The invention also concerns cosmetic and dermatological uses of said composition, in particular for preventing skin ageing symptoms.

Description

Composition, in particular cosmetic, containing DHEA and / or its precursors or derivatives, and a vitamin

The present invention relates to a composition containing at least one compound chosen from DHEA and / or a biological precursor and / or a chemical or biological derivative thereof, and at least one vitamin chosen from vitamins B2, B3, B6 , B8, B12, D and K, as well as the use of said composition.

DHEA, or dehydroepiandrosterone, is a natural steroid produced primarily by the adrenal cortex. Exogenous DHEA, administered topically or orally, is known for its ability to promote keratinization of the epidermis (JP-07 196 467) and to treat dry skin by increasing endogenous production and sebum secretion and by strengthening thus the barrier effect of the skin (US Pat. No. 4,496,556). It has also been described in US Pat. No. 5,843,932 the use of DHEA for remedying atrophy of the dermis by inhibiting the loss of collagen and connective tissue. It has also been described in US Pat. No. 5,736,537 the oral use of DHEA esters, in particular DHEA salicylate, for regulating the atrophy of the skin due to thinning or general degradation of the dermis.

However, it appeared to the Applicant that the combination of DHEA with certain vitamins could make it possible to improve more effectively the visual and / or tactile aspect of the skin and / or appendages and in particular to prevent or treat more effectively signs of skin aging.

A subject of the present invention is therefore a composition containing at least one compound chosen from DHEA and / or a biological precursor and / or a chemical or biological derivative thereof, characterized in that it also comprises at least one vitamin chosen from vitamins B2, B3, B6, B8, B12, D and K.

DHEA has the following formula (I):

It is for example available from the company AKZO NOBEL.

By biological precursors of DHEA is meant its precursors which are capable of transforming into DHEA during metabolism. Examples of such precursors are Δ5-pregnenolone, 17α-hydroxy pregnenolone and 17α-hydroxy pregnenolone sulfate, without this list being limiting.

The term DHEA derivatives is understood to mean both its biological derivatives and its chemical derivatives. As biological derivatives, there may be mentioned in particular Δ5-androstene-3,17-diol and Δ4-androstene-3,17-dione, without this list being limiting. As chemical derivatives, mention may in particular be made of DHEA salts, in particular water-soluble salts, such as DHEA sulfate. Mention may also be made of esters, such as the esters of hydroxycarboxylic acids and of DHEA described in particular in US Pat. No. 5,736,537 or the other esters such as salicylate, acetate, valerate (or n-heptanoate) and enanthate of DHEA. Mention may also be made of the DHEA derivatives (DHEA carbamates, DHEA 2-hydroxy malonate esters and DHEA amino acid esters) described in application FR 00/03846 in the name of the Applicant. This list is obviously not exhaustive.

The precursors and derivatives of DHEA will hereinafter be called "DHEA analogues".

The concentration of DHEA and / or the like in the composition according to the invention is advantageously between 0.0001% and 10% by weight, preferably between 0.001% and 5% by weight, relative to the total weight of the composition.

The composition according to the present invention contains, in combination with DHEA and / or its analogs, at least one vitamin chosen from vitamins B2, B3, B6, B8, B12, D and K.

The above vitamins are known to have beneficial effects on the skin or its appendages. Vitamin B2 (riboflavin) has been recommended in the treatment of acne rosacea and seborrhea, because of its ability to act on the renewal and maintenance of tissues, skin and mucous membranes. She permits also to strengthen and tone the skin, nails and hair. Vitamin B3 (niacinamide) has been widely described as beneficial against skin roughness, and for improving the integrity of the barrier function of the stratum corneum, but also as an anti-inflammatory. Vitamin B6 (pyridoxine) and B8 (biotin) are known as anti-seborheic and can be used, as such, against acne and seborrheic alopecia. In the latter indication, vitamin B8 (or vitamin H) is particularly effective when combined with panthenol. Vitamin B8 is also indicated in the treatment of brittle nails and, more generally, in the prevention of the integrity of the skin and integuments. Vitamin B12 (cobalamin) contributes to the good condition of the skin. Vitamin D (ergocalciferol) has also been shown to improve the differentiation of keratinocytes and prevent their hyper-proliferation. Finally, vitamin K, and in particular vitamin K1 (menadione) is notably known in the treatment of disorders of the blood vessels and photoaging (WO 95/11015).

However, the Applicant has demonstrated that DHEA and / or its analogues, applied topically, themselves have an activity on the signs of skin aging and in particular the atrophy of the epidermis, the pigment spots, the appearance papery of the skin, wrinkles, sagging skin and dull complexion.

The Applicant therefore believes, without wishing to be bound by this theory, that the combination of at least one of the above vitamins with DHEA or the like could advantageously improve the visual and / or tactile appearance of the skin and / or of its appendages and in particular to prevent or combat skin aging.

More particularly, the combination of DHEA with at least one of vitamins B2, B6 and B8 could in particular make it possible to counter the hyper-seborrheic effect of DHEA applied to the skin, which may be undesirable in certain skin subjects oily, or prevent the formation of acneiform lesions in these same subjects, without harming the anti-aging properties of DHEA.

In addition, the effects of vitamin B8 on preventing hair loss make it possible to consider the association of this vitamin with DHEA in products capillaries where DHEA finds an application because of its beneficial effects on canities. ^•

A person skilled in the art will know how to vary the amount of vitamin (s) included in the composition according to the invention as a function of the desired effect and of the maximum admissible doses taking into account the bioavailability of these vitamins and their possible undesirable effects.

The composition according to the invention can be in all dosage forms normally used for topical application to the skin, in particular in the form of an aqueous or oily solution, of an oil-in-water or water-in-oil emulsion or multiple, of a silicone emulsion, a microemulsion or nanoemulsion, an aqueous or oily gel, a liquid, pasty or solid anhydrous product, an oil dispersion in an aqueous phase in the presence of spherules , these spherules possibly being polymeric nanoparticles such as nanospheres and nanocapsules or, better, lipid vesicles of ionic and / or nonionic type.

This composition can be more or less fluid and have the appearance of a white or colored cream, an ointment, a milk, a lotion, a serum, a paste, a foam. or a gel. It can optionally be applied to the skin in the form of an aerosol. It can also be in solid form, and for example in the form of a stick. It can be used as a care product and / or as a skin makeup product. Alternatively, it can be in the form of a shampoo or conditioner.

In a known manner, the composition of the invention may also contain the adjuvants usual in the cosmetic and dermatological fields, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, perfumes, fillers, filters, pigments, odor absorbers and coloring matter. The amounts of these various adjuvants are those conventionally used in the fields under consideration, and for example from 0.01 to 20% of the total weight of the composition. These adjuvants, depending on their nature, can be introduced into the fatty phase, into the aqueous phase, into the lipid vesicles and / or in nanoparticles. These adjuvants, as well as their concentrations, must be such that they do not harm the advantageous properties of the combination of active agents according to the invention.

When the composition according to the invention is an emulsion, the proportion of the fatty phase can range from 5 to 80% by weight, and preferably from 5 to 50% by weight relative to the total weight of the composition. The fats, emulsifiers and coemulsifiers used in the composition in the form of an emulsion are chosen from those conventionally used in the field under consideration. The emulsifier and the co-emulsifier are preferably present in the composition in a proportion ranging from 0.3 to 30% by weight, and preferably from 0.5 to 20% by weight relative to the total weight of the composition.

As fats which can be used in the invention, oils and in particular mineral oils (petroleum jelly oil), oils of vegetable origin (avocado oil, soybean oil), oils of animal origin (lanolin) can be used. ), synthetic oils (perhydrosqualene), silicone oils (cyclomethicone) and fluorinated oils (perfluoropolyethers). Fatty alcohols such as cetyl alcohol, fatty acids, waxes and gums and in particular silicone gums can also be used as fats.

As emulsifiers and coemulsifiers which can be used in the invention, mention may, for example, be made of fatty acid and polyethylene glycol esters such as PEG-100 stearate, PEG-50 stearate and PEG-40 stearate; fatty acid and polyol esters such as glyceryl stearate, sorbitan tristearate and oxyethylenated sorbitan stearates available under the trade names Tween® 20 or Tween® 60, for example; and their mixtures.

As hydrophilic gelling agents, mention may be made in particular of carboxyvinyl polymers (carbomers), acrylic copolymers such as acrylate / alkyl acrylate copolymers, polyacrylamides, polysaccharides, natural gums and clays, and, as lipophilic gelling agents, cite modified clays such as bentones, metal salts of fatty acids and hydrophobic silica. As active agents, depigmentants and keratolytic and / or scaling agents can be used in particular.

In the event of incompatibility, the active agents indicated above and / or the DHEA analogs according to the invention can be incorporated into spherules, in particular ionic or non-ionic vesicles and or nanoparticles (nanocapsules and / or nanospheres), so to isolate them from each other in the composition.

According to a variant of the invention, the - composition can be adapted for oral administration. In this case, it can be in the form of syrups, suspensions, solutions, emulsions, capsules, granules or tablets, for example.

The daily doses of DHEA or analogues administered orally can be between 1 and 100 mg / day, preferably between 25 and 75 mg / day. Preferably, DHEA or the like is present in the composition according to the invention in an amount allowing its administration at a dose of between 50 and 100 mg / day, said dosage being carried out in one or more doses, with a unit dose of 50 mg. .

The daily doses of vitamins administered orally will preferably be included in the ranges indicated in Table 1 below:

TABLE 1

In all cases, the composition according to the invention comprises an effective amount of DHEA or the like and of vitamin (s), sufficient to obtain the desired effect, and a physiologically acceptable medium.

The composition according to the invention finds in particular an application in improving the visual and / or tactile appearance of the skin and / or its integuments and in particular in the prevention and treatment of the signs of skin aging.

The present invention therefore also relates to the cosmetic use of the composition mentioned above for improving the visual and / or tactile appearance of the skin and / or its integuments and in particular for preventing or treating the signs of skin aging. The composition according to the invention is thus preferably used:

- to prevent or reduce the papery appearance of the skin, and / or - to improve the uniformity of the color of the skin and / or to whiten the skin and / or revive the radiance of the complexion, and / or

- to treat fine lines and wrinkles, and / or

- to combat sagging skin, and / or

- to fight against or prevent atrophy of the epidermis.

The present invention also relates to the cosmetic use of this composition for the treatment of the scalp and / or the hair and / or the nails.

The invention will now be illustrated by the following nonlimiting examples. In these examples, the quantities are indicated in percentage by weight.

Example 1 Composition for Oral Administration

Soft capsules are prepared, conventionally for those skilled in the art, having the following composition:

Hydrogenated soybean oil 40 mg

Wheat oil 95 mg

Soy lecithin: 20 mg Natural tocopherols 5 mg

Ascorbic acid 30 mg

Vitamin D 5 μg

DHEA 50 mg

These capsules can be administered by taking a daily capsule.

Example 2 -Composition for topical application

A treatment cream (oil-in-water emulsion) having the following composition is prepared, conventionally for a person skilled in the art:

Vitamin B3 1% DHEA 0.1%

2% glycerol stearate

Polysorbate 60 (Tween 60 ® sold by the company ICI) 1%

Stearic acid 1, 4%

Triethanolamine 0.7% Carbomer 0.4%

Liquid fraction of shea butter 12%

Perhydrosqualene 12%

Perfume 0.5%

Preservative QS Water QSP 100%

Claims

1. Composition containing at least one compound chosen from DHEA and / or a biological precursor and / or a chemical or biological derivative thereof, characterized in that it also comprises at least one vitamin chosen from vitamins B2, B3, B6, B8, B12, D and K.

2. Composition according to claim 1, characterized in that said biological precursor of DHEA is chosen from: Δ5-pregnenolone, 17α-hydroxy pregnenolone and 17oc-hydroxy pregnenolone sulfate.

3. Composition according to claim 1 or 2, characterized in that said biological derivative of DHEA is chosen from: Δ5-androstene-3,17-diol and Δ4-androstene-3,17-dione.

4. Composition according to any one of the preceding claims, characterized in that said chemical derivative of DHEA is chosen from: salts of DHEA and esters of DHEA.

5. Composition according to claim 4, characterized in that said DHEA salt is chosen from water-soluble salts, such as DHEA sulfate.

6. Composition according to claim 4, characterized in that said DHEA ester is chosen from: esters of hydroxycarboxylic acids and DHEA; DHEA salicylate; DHEA acetate; DHEA valerate; and DHEA enanthate.

7. Composition according to any one of the preceding claims, characterized in that it contains from 0.001 to 5% by weight of DHEA and / or precursor or derivative, relative to the total weight of the composition.

8. Cosmetic use of the composition according to any one of the preceding claims for improving the visual and / or tactile appearance of the skin and / or its integuments.

9. Cosmetic use of the composition according to any one of claims 1 to 7 for preventing or treating the signs of skin aging.

10. Cosmetic use of the composition according to any one of claims 1 to 7 for preventing or reducing the papery appearance of the skin and / or for improving the uniformity of the color of the skin and / or for whitening the skin and / or revive the radiance of the complexion, and / or to treat fine lines and wrinkles and / or to combat sagging skin, and / or to combat or prevent atrophy of the epidermis.

11. Cosmetic use of the composition according to any one of claims 1 to 7 for the treatment of the scalp and / or the hair and / or the nails.

AMENDED CLAIMS

[received by the International Bureau on December 3, 2001 (03.12.01); original claims 1-11 amended (2 pages)]

1. Composition adapted to be applied topically to the skin, scalp, hair or nails, containing (a) DHEA and (b) at least one vitamin chosen from vitamins B2, B3, B6, B8 and B12.

2. Composition containing (a) a biological precursor and / or a chemical or biological derivative of DHEA, and (b) at least one vitamin chosen from vitamins B2, B3, B6, B8, B12, D and K.

3. Composition according to claim 2, characterized in that said biological precursor of DHEA is chosen from Δ5-pregnenolone, 17α-hydroxy pregnenolone and 17α-hydroxy pregnenolone sulfate.

4. Composition according to claim 2, characterized in that said biological derivative of DHEA is chosen from Δ5-androstene-3,17-diol and Δ4-androstene-3,17-dione.

5. Composition according to claim 2, characterized in that said chemical derivative of DHEA is chosen from DHEA salts and DHEA esters.

6. Composition according to claim 5, characterized in that said DHEA salt is chosen from water-soluble salts, such as DHEA sulfate.

7. Composition according to claim 5, characterized in that said DHEA ester is chosen from: esters of hydroxycarboxylic acids and DHEA; DHEA salicylate; DHEA acetate; DHEA valerate; and DHEA enanthate.

8. Composition according to any one of the preceding claims, characterized in that it contains from 0.001 to 5% by weight of DHEA and / or precursor or derivative, relative to the total weight of the composition.

9. Cosmetic use of the composition according to any one of the preceding claims for improving the visual and / or tactile appearance of the skin and / or its integuments.

10. Cosmetic use of the composition according to any one of claims 1 to 8 for preventing or treating the signs of skin aging.

11. Cosmetic use of the composition according to any one of claims 1 to 7 for preventing or reducing the papery appearance of the skin and / or for improving the uniformity of the color of the skin and / or for whitening the skin and / or to revive the radiance of the complexion, and / or to treat fine lines and wrinkles and / or to combat sagging skin, and / or to combat or prevent atrophy of the epidermis.