FR2645740A1 - Three-phase topical compositions which can be emulsified immediately before use and which are useful in cosmetology and/or dermatology - Google Patents

Abstract

The invention relates to a topical cosmetological and/or dermatological composition which takes the form of three distinct phases designed to be mixed immediately before use so as to obtain an emulsion and/or microemulsion, the aforementioned phases being a solid phase in pulverulent form, an aqueous phase and a lipophilic phase.

Description

The present invention, carried out at the Research Center
Dermatological and Cosmetological Pierre FABRE, concerns topical three-phase formulations which are extemporaneously emulsifiable and / or microemulsifiable containing active principles usable in cosmetology and / or dermatology.

Emulsification has been widely used in the preparation of dermatological and cosmetic creams and lotions because it facilitates the penetration of the active ingredient into the skin (ref. Remington
Pharmaceutical Sciences 15 th Ed - Mack Publishing Co. Easton p 327 (1937)). However, these emulsions are thermodynamically unstable, which is a disadvantage in obtaining the expiration time necessary for marketing.

 In many cosmetic and pharmaceutical applications, there is a need to obtain very stable emulsions and / or transparent or at least translucent emulsions.

 Microemulsions can be very useful for such uses because they are generally much more stable.

 These microemulsions have been used in the formulations of hygiene products, particularly in the solubilization of perfumes in aqueous systems.

 The object of the present invention is to prepare formulations which will make it possible to dissolve extemporaneously in the form of an emulsion and / or a microemulsion of cosmetic and / or pharmaceutical active ingredients which are unstable and / or not soluble in conventional formulations.

 More specifically, the present invention relates to a topical cosmetic and / or dermatological composition characterized in that it is in the form of three distinct phases, intended to be mixed extemporaneously so as to obtain an emulsion and / or microemulsion, said phases being a solid phase in powder form, an aqueous phase and a lipophilic phase.

In such a topical composition, the solid phase in the form of powder consists of - Surfactants selected from anionic derivatives and more
particularly magnesium lauryl sulfate, lauryl sulfosuccinate
and sodium cocoylisethionate, non-ionic derivatives and more
particularly ethoxylated lauryl alcohol and ethoxylated nonylphenols
general formula I
C9H19- C6H4- (O-CH2- CH2) n OH (I) in which n} 20; cationic derivatives and more particularly cetyldimethylbenzyl ammonium bromide and cetyltrimethyl ammonium chloride; and amphoteric derivatives and more particularly lauryl betaine and imidazoline derivatives.

- Emulsifiers and more particularly whey and powder
egg lecithin.

- Active ingredients not very stable in solution and / or hardly soluble
sands. These active ingredients are selected from vitamins and more
particularly derivatives of vitamin A, and TRETINOINE; the
enzymes and more particularly derivatives of keratinase and / or
hypoxygenase; antibiotics and / or antiseptics and more particularly
erythromycin and chlorexidine; derivatives sensitive to
oxidation and more particularly dioxyanthranol and dihydroxy
acetone; derivatives sensitive to hydrolysis and more particularly
acetylsalycilic acid and hydrocortisone acetate; drifts
sensitive to bacterial contamination and more particularly
animal and / or plant extracts; derivatives that are difficult to dissolve
and more particularly the antiallergic TlOXAMAST of formula II which has
is the subject of a patent application by the Applicant: "derived from
phenyl-4-thiazolyl- 2 oxamates useful in the treatment of asthma "
FR 2 429 210 No. 78 18500 of June 19, 1978 in the names of H. COUSSE, G.

MOUZIN, 3-P. TARAYRE and S. CASADIO

The lipophilic phase consists of - Vegetable oils and more particularly sweet almond oil,
avocado oil, coconut oil, wheat germ oil, mat oil,
olive oil, palm oil, sesame oil, soybean oil, oil
argan, evening primrose oil, borage oil, essential oils and
vegetable waxes.

- Animal oils and more particularly beaver oil,
turtle, mink oil, fish oils and animal waxes.

- Mineral oils and more particularly petrolatum oil and oil
silicone.

 According to the present invention, this lipid phase can also contain stable lipophilic derivatives and more particularly dyes, sunscreens, antioxidants, preservatives and also active principles.

 The aqueous phase may contain stable water-soluble derivatives and more particularly dyes, preservatives, and also active ingredients.

 According to the present invention, the three-phase formulation contains 0.1 to 10% by weight of the solid phase, 1 to 50% by weight of the lipophilic phase and 10 to 90% by weight of the aqueous phase.

 Finally, according to a preferred formulation, the composition preferably contains 1 to 5% by weight of the solid phase, 10 to 25% by weight of the lipophilic phase and 50 to 70% of the aqueous phase.

 The compositions obtained according to the present invention will be packaged in devices which are very particularly suitable for separately preserving the solid phase of the two aqueous and lipophilic phases combined together in a biphasic liquid phase.

 Figure 1 shows a possible embodiment of such a device.

 This device consists of a bottle (1) closed by a stopper (2) having a central recess open at the top so as to define a receiving cavity (3) for a solid phase, the stopper itself being closed by a sliding member. closing and drilling (4).

 This member (4) has the shape of a sliding hollow piston, is closed at the top to close off the cavity (3) and has a bevelled lower edge for piercing the seal formed by the bottom wall of the plug (2).

 When handling the device in the context of the present invention, a vertical manual push is exerted on the piston member (4) which then pierces the bottom wall of the plug (2) so as to allow the flow of the solid phase (A), contained in the receiving cavity (3), in the bottle (1) where the aqueous phase (C) and the lipophilic phase (B) are present.

 When the piston member (4) is pressed, the tightness of the entire device is preserved and therefore allows the three phases, now combined in the bottle, to be stirred before use.

 The following examples are intended to illustrate the invention without, however, being limiting in nature.

EXAMPLE 1
Phase A
Whey 1 to 5%
Phase B
Decamethylcyclopentasiloxane 10 to 20%
Provitamin A 0.05 to 1 Z
Tocopherol acetate 2 to 5% Orange essence 2 to 4X
Dye Yellow 0.002 to 0.004X
Phase C
Methionine Sebacate 0.5 to 2Z
Vitamin B6 0.5 to 2Z
Nettle extract 0.1 to 5%
Sabal extract 0.1 to 5Z
Triclosan 0.005 to 0.01%
FD and C green dyes 0.002 to 0.004%
Demineralized water qs 100 g
EXAMPLE 2
Phase A
1 to 2Z magnesium lauryl sulfate
Nonylphenolethoxylated 1%
Vitamin A acetate 0.5 to
Methionine 0.1 to 1%
Phase B
Halibut oil 20 to 25%
0.5 to 2X methionine sebacate
Nicotinamide 0.5 to 1X
Lavender essence l to 2X
Phase C
0.5-2% methionine sebacate
Vitamin PP 0.5 to 1%
Zinc sulfate 1 to 2%
Pyridoxine chloride 0.5 to 2%
D panthenol 0.05 to 1%
Imidazolidinylurea 0.05 to 0.15%
Demineralized water qs 100 g
EXAMPLE 3
Phase A
Egg lecithin l 3%
Lauryl betaine l at 2%
Collagen 0.5 to 1%
Phase B
Sweet almond oil 15 to 25Z
Tocopherol nicotinate 0.1 to 1%
Orange essence 0.1 to 1%
Parahydroxybenzoate
propyl 0.1 to 0.2%
Phase C
------- Vitamin PP 0.05 to 2Z
Zinc sulfate 1 to 2%
0.1 to 1% keratin protein hydrolyzate
Nipagin sodium 0.1 to 0.2X
Demineralized water qs 100 g
The formulations according to Examples 1 to 3 are more particularly intended for the treatment of alopecia and seborrhea disorders.

EXAMPLE 4
Phase A
Whey 1 to 3%
Lauryl betaine 0.5 to 1Z
Elastin 0.5 to 1%
Phase B
Mink oil 1 to 3Z
Soybean oil 20 to 25X
Vitamin A palmitate 0.1 to 1X
Phase C
Pyridoxine hydrochloride ia 2X
Nipagin sodium 0.1 to 2%
Demineralized water qs 100 g
EXAMPLE 5
Phase A
Cetyldiiethylbenzyiammonium bromide 1 to 2Z
Whey 2 to 3%
Vitamin A acid 0.01 to 0.03%
Vitamin E acetate 2 to 5%
Phase B Procollagen 0.2 to 5%
Sodium eyaluronate 0.01 to 0.05%.

1 to 2X wheat germ oil
Sesame oil 10 to 20Z
Vitamin A palmitate 0.1 to 0.5%
Vitamin F 1 to 2%
Phase C
Sodium pyroglutamate 0.5 to 2X
Nipagin sodium 0.1 to 0.2%
Demineralized water qs 100 g
The formulations according to Examples 4 to 5 are more particularly intended for the treatment of skin aging disorders.

EXAMPLE 6
Phase A
Dioxyanthranol 0.01 to 1%
Lauryl betaine 1 to 3%
Phase B
Borage oil 20 to 25%
Vitamin A palmitate 0.1 to 0.5%
Essence of Melaleuca 0.1 to 1%
Phase C
Urea 0.5 to 2X
Sodium salicylate 0.1 to 0.5%
Nipagin sodium 0.1 to 0.2%
Demineralized water qs 100 g
The formulations according to Example 6 are more particularly intended for the treatment of psoriasis disorders.

EXAMPLE 7
Phase A
TIOXAMAST 0.1 to 2X
Lauryl betaine 1 to 3%
Phase B
Sweet almond oil 20 to 30%
Vitamin E acetate 0.5 to 2%
Phase C
Sodium pyroglutamate 0.5 to 2%
Demineralized water qs 100 g
The formulations according to Example 7 are more particularly intended for the treatment of skin allergies.

EXAMPLE 8
Phase A
Ruscus extract 0.1 to 1%
Sweetclover extract 0.1 to 1X
Lyophilized bovine placenta I at 3%
Phase B
Sweet almond oil 20 to 25%
Vitamin F 1 to 3%
Vitamin A palmitate 0.5 to 1%
Phase C
Sorbitol 1 to 2%
Sodium dextran sulfate 0.2 to 0.5%
Demineralized water qs 100 g
The formulations according to Example 8 are more particularly intended for the treatment of rosacea.

EXAMPLE 9
Phase A
Dihydroxyacetone 0.1 to 2%
Whey 1 to 2%
Lauryl betaine 0.5 to 1%
Phase B
Sweet almond oil 20 to 25%
Vitamin A palmitate 1 to 2X
Vitamin F 1 to 2X
Phase C
Arginine tyrosinate 0.1 to 1%
0.2 to 2X sodium pyroglutamate
Demineralized water qs 100 g
The formulations according to Example 9 are more particularly
intended for the treatment of pigmentation disorders.

The topical formulations according to the present invention are
well tolerated and, depending on the choice of active ingredients, are useful in
cosmetology and / or in dermatological treatments.

Claims (15)

 1. topical cosmetic and / or dermatological composition, characterized in that it is in the form of three distinct phases, intended to be mixed extemporaneously so as to obtain an emulsion and / or microemulsion, said phases being a solid phase in a form pulverulent, an aqueous phase and a lipophilic phase.  2. Composition according to Claim 1, characterized in that the solid phase contains surfactants and / or emulsifiers as well as active principles which are not very stable in solution and / or which are difficult to dissolve.  3. Composition according to claim 2, characterized in that the surfactants are anionic, cationic, nonionic and / or amphoteric surfactants.  4. Composition according to one of claims 1 to 3, characterized in that the surfactants are more particularly selected from magnesium laurylsulfate, sodium laurylslulfosuccinate, sodium cocolisethionate, ethoxylated lauryl alcohol, ethoxylated nonylphenols, bromide of cetyldimethylbenzylammonium, cetyltrimethylammonium chloride, laurylbétalne and imidazoline derivatives.  5. Composition according to one of claims 1 to 4, characterized in that the emulsifiers are more particularly whey and egg lecithin powder.  6. Composition according to one of claims I to 5, characterized in that the active principles are vitamins and more particularly derivatives of vitamin A and tretinoin.  7. Composition according to one of claims 1 to 5, characterized in that the active principles are enzymatic derivatives and preferably derivatives of keratinase and / or lipoxygenase.  8. Composition according to one of claims 1 to 5, characterized in that the active principles are antibiotics and / or antiseptics and more particularly erythromycin and chlorexidine.  9. Composition according to one of claims I to 5, characterized in that the active principles are chosen from acetylsalycilic acid, hydrocortisone acetate and animal and / or plant extracts.  10. Composition according to one of claims 1 to 5, characterized in that the active principle is TIOXAMAST.  11. Composition according to one of claims 1 to 10, characterized in that the lipophilic phase consists of vegetable oil (s), animal oil (s) and / or mineral oil (s) (s).  12. Composition according to one of claims 1 to 11, characterized in that the lipophilic phase also contains stable lipophilic derivatives and more particularly dyes, sunscreens, antioxidants, preservatives, and also active ingredients.  13. Composition according to one of claims 1 to 12, characterized in that the aqueous phase contains stable water-soluble derivatives and more particularly dyes, preservatives and also active principles.  14. Composition according to one of claims I to 13, characterized in that it contains 0.1 to 10% by weight of the solid phase, I at 50% by weight of the lipophilic phase and 10 to 90% by weight of the aqueous phase.  15. Composition according to claim 14, characterized in that it preferably contains 1 to 5% by weight of the solid phase, 10 to 25% by weight of the lipophilic phase and 50 to 70% of the aqueous phase.