WO2021072683A1 - Two-part composition for caring for keratin materials - Google Patents

Two-part composition for caring for keratin materials Download PDF

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Publication number
WO2021072683A1
WO2021072683A1 PCT/CN2019/111506 CN2019111506W WO2021072683A1 WO 2021072683 A1 WO2021072683 A1 WO 2021072683A1 CN 2019111506 W CN2019111506 W CN 2019111506W WO 2021072683 A1 WO2021072683 A1 WO 2021072683A1
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WO
WIPO (PCT)
Prior art keywords
weight
part composition
glycol
composition according
anhydrous
Prior art date
Application number
PCT/CN2019/111506
Other languages
French (fr)
Inventor
Shanshan ZANG
Original Assignee
L'oreal
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by L'oreal filed Critical L'oreal
Priority to PCT/CN2019/111506 priority Critical patent/WO2021072683A1/en
Priority to CN201980101320.7A priority patent/CN114555033A/en
Publication of WO2021072683A1 publication Critical patent/WO2021072683A1/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/676Ascorbic acid, i.e. vitamin C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/88Two- or multipart kits
    • A61K2800/882Mixing prior to application

Definitions

  • the present invention relates to a composition for caring for keratin materials such as the skin, in particular the face.
  • the present invention relates to a two-part composition for caring for keratin materials such as the skin, in particular the face.
  • the present invention also relates to a process for caring for keratin materials such as the skin, in particular the face.
  • Whitening active ingredients such as ascorbic acid (vitamin C) stimulates the synthesis of connective tissue, in particular of collagen, enhances the defences of skin tissue against damage by environmental agents such as ultraviolet radiation and pollution, compensates for any vitamin E deficiency of the skin, depigments the skin and has an anti-free radical function. These last two properties make it an excellent candidate as a cosmetic or dermatological active agent for combating and/or preventing skin ageing. Efforts have been made for a long time to formulate ascorbic acid in the cosmetic and dermatological fields, in various galenic forms, because of its numerous beneficial properties.
  • ascorbic acid is very sensitive to certain environmental parameters such as light, oxygen, water (through its pH and through the presence of traces of metals) .
  • the rapid degradation of ascorbic acid formulations occurs in the presence of these conditions, which is counter to the desired results.
  • several solutions have already been envisioned in the prior art.
  • Another solution consists in formulating the ascorbic acid in an acidic gel having a pH of not more than 3.5 and containing a high quantity of glycol, as described in WO-A-90/12572 incorporated herein by reference. Because of the acidic pH used and the presence of a large quantity of glycol, that is to say of solvent, this gel is poorly tolerated by the skin, whose pH is about 5.5. A repeated application of this gel to the skin causes irritation.
  • Another solution consists in using ascorbic acid in powdered form and in dissolving it in water just before use. Because of the high acidity of the solution obtained, it is aggressive and risks causing substantial irritation of the skin.
  • Another solution uses the freeze-drying of an aqueous solution containing an ester of ascorbic acid and hyaluronic acid; the freeze-dried product obtained is dissolved in water just before use.
  • This solution has the disadvantages of being complex and quite expensive as well as using an ascorbic acid derivative which is less effective than that of ascorbic acid itself.
  • the solution obtained is difficult to apply to the skin; it runs down the face and/or the body and is difficult to handle.
  • FR-A-2, 645, 740 describes a composition containing an oily phase, an aqueous phase and a solid phase to be mixed immediately before use, the solid phase containing one or more active agents (especially vitamin A) and an emulsifier, and being placed in the cap of a bottle containing the two liquid phases.
  • This packaging allows a long storage time of the composition before mixing the three phases by shaking. After mixing, however, the composition is stable for only a few hours. Furthermore, the mixture obtained is a coarse emulsion which is not homogeneous. This results in lower efficacy; indeed, the coarser the emulsion, the less satisfactory it is as a vehicle for an active agent. In addition, the solid dissolves poorly.
  • This three-phase composition cannot be used for an active agent with an acidic functional group, the acidic active agent carrying the risk of breaking the emulsion, or even of preventing its formation.
  • one object of the present is thus to provide a cosmetic product containing at least one active ingredient, which can achieve high dissolution rate of ascorbic acid, remain the effect of the active ingredient, cause no irritation to the skin and is cost economic.
  • Still another object of the present invention is to provide a process for caring for keratin materials such as the skin, in particular the face.
  • the present invention provides a two-part composition for caring for keratin materials comprising:
  • the present invention provides is a process for caring for keratin materials, comprising mixing the anhydrous part and the hydrous part of the two-part composition as described above together to form a solution and applying the solution to the keratin materials.
  • the water soluble active ingredient can quick dissolve in the hydrous part comprising a xanthan gum and at least one C 2 -C 6 glycol, i.e. a homogeneous solution can be formed after mixing the anhydrous part and hydrous part for less than 1 minute, even within 30 seconds.
  • the freshly mixed two-part composition presents visually pleasant transformation and appearance.
  • the two-part composition for caring for keratin materials according to the present invention comprises:
  • the anhydrous part means that no water is added on purpose and the water content is less than 0.1%by weight of the anhydrous part, in particular, there is no water in the anhydrous part.
  • the two-part composition can be used to care for keratin materials such as the skin, in particular the face after being shaked to form a homogeneous solution.
  • the two-part composition of the present invention comprises an anhydrous part containing at least one water soluble active ingredient.
  • the anhydrous part is consisted of the at least one water soluble active ingredient.
  • the anhydrous part comprises the at least one water soluble active ingredient and a disintegrating agent.
  • the anhydrous part is consisted of the at least one water soluble active ingredient and a disintegrating agent.
  • An active agent is one capable of bringing cosmetic effect to a user, especially to the skin, e.g., to face.
  • Such cosmetic effect can be, for example, whitening, anti-aging, hydrating, and/or moisturizing.
  • the active agents conventionally useful for a cosmetic product can be used in the anhydrous part according to the present invention, as long as it is water soluble.
  • composition of the present invention is particularly applicable to use water soluble active agents which are unstable in solvated state.
  • unstable we intend to mean an ingredient or composition undergoes significant change in its structure or properties within 2 months, or preferably 1 month, in solvent or solvated state. Such change may be any one undesirable for the cosmetic use, including, but not limited to, color change, degradation, decomposition, reaction with others, significant evaporation, deposition, crystallization, and the like.
  • water soluble active agents mentions can be made of water soluble vitamins.
  • Water soluble vitamins can be used in the anhydrous part as an active agent.
  • the useful examples of vitamin comprise vitamin C (ascorbic acid) , vitamin B group (e.g., vitamin B5 (panthenol) , vitamin B3 (niacinamide) , vitamin B1 and vitamin B2) , nicotinic acid, folic acid, pantothenic acid, the derivatives of these vitamins (in particular esters) and their mixtures.
  • vitamin C and vitamin B groups are preferably used.
  • Vitamin C is more preferably used.
  • vitamins that are suitable for use in the present invention may be represented, for example, by the products sold under the name ASCORBIC ACID 100 MESH, available from CSPC WEISHENG PHARMACEUTICAL, or from BASF.
  • Useful derivatives of water soluble vitamins comprise preferably 3-o-ethyl ascorbic acid, ascorbyl glucoside, or a mixture thereof.
  • the anhydrous part of the present invention may comprise the at least one water soluble active agent in a content ranging from 20%to 100%by weight, preferably from 40%to 95%by weight, especially from 50%to 90%by weight, relative to the total weight of the anhydrous part.
  • a disintegrating agent can be used in the anhydrous part, for the purpose of facilitating the disintegration of the water soluble active agent (s) when it is dissolved in a solvent, e.g., in water. Accordingly, the disintegrating agent is preferably mixed homogenously with the water soluble active agent.
  • the disintegrating agent is itself a binder for the active agent, or an additional binder is added, such that the disintegrating agent and the active agent is together formed into integrated solid state, e.g., particles, granules, spheres, beads, balls, bars, strips or the like, in either hollow or solid form.
  • integrated solid state e.g., particles, granules, spheres, beads, balls, bars, strips or the like.
  • the forms of granules, spheres, balls and the like are preferred.
  • the disintegrating agent is preferably selected from the group consisting of starches, e.g., corn starch, tomato starch, or wheat starch; a derivative of starch, e.g., pregelatinized starch, alpha starch, acrylic grafted starch or carboxymethyl starch sodium; saccharide or saccharide alcohol, or mixtures thereof.
  • Saccharide or saccharide alcohol is preferably used as disintegrating agent according to the present invention. More preferably, saccharide or saccharide alcohol serves itself as a binder. Useful saccharides comprise monosaccharide, disaccharide and polysaccharide. The corresponding alcohol of the saccharide may also be useful.
  • saccharides that are suitable for use in the present invention may be represented, for example, by the products sold under the name SUCRE SEMOULE SURFINE 250 from TEREOS.
  • the weight ratio of the disintegrating agent to the active agent in the anhydrous part ranges from 1: 100 to 1: 4, preferably from 1: 50 to 1: 5, or preferably from 1: 20 to 1: 10.
  • the anhydrous part is preferably a particle having a particle size of 20-40 mesh.
  • the anhydrous part is used as it is from the supplier without unpacked before mixed with the hydrous part.
  • the two-part composition of the present invention comprises from 0.1%to 20%by weight, preferably from 1%to 15%by weight, more preferably from 5%to 15%by weight of the anhydrous part, relative to the total weight of the two-part composition.
  • the two-part composition of the present invention comprises a hydrous part containing a xanthan gum and at least one C 2 -C 6 polyol.
  • Xanthan gum is a high molecular weight polysaccharide or hydrophilic colloid (also known as a gum) that is produced by fermentation of various species of the Xanthomonas, such as X. carotae, X. campestris, X. incanae, X. begoniae andX. malvacearum.
  • Xanthan gum may comprise in their structure three different monosaccharides, namely mannose, glucose and glucuronic acid, in salt form, such as in the form of the sodium salt.
  • Xanthan gum may have, for example, a viscosity ranging from 850 to 1600 cps for an aqueous composition containing 1%of xanthan gum (measured at 25°C. using a Brookfield viscometer, type LVT at 60 rpm) . It has a molecular weight ranging, for example, from 1 000 000 to 50 000 000.
  • Xanthane gums which are more particularly preferred are KELTROL marketed by KELCO, a 1%aqueous solution of which has a Brookfield LVT viscosity at 60 rpm of 1200 to 1600 cps, KELZAN S marketed by KELCO, a 1%aqueous solution of which has a Brookfield LVT viscosity at 60 rpm of 850 cP, Rhodopol 23, 23 U, and 23 C marketed by Rhone-Poulenc, a 0.3%aqueous solution of which has a Brookfield LVT viscosity at 30 rpm of 450.
  • the two-part composition of the present invention comprises from 0.01%to 2%by weight, preferably from 0.05%to 1%by weight, more preferably from 0.05%to 0.5%by weight, most preferably from 0.05%to 0.2%by weight of Xanthane gum, relative to the total weight of the two-part composition.
  • composition according to the present invention comprises at least one C2-C6 polyol.
  • a single type of polyol may be used, but two or more different types of polyol may be used in combination.
  • polyol here means an alcohol having two or more hydroxy groups.
  • the polyol may be a natural or synthetic polyol.
  • the polyol may have a linear, branched or cyclic molecular structure.
  • the C 2 -C 6 polyol may be selected from glycerin and derivatives thereof, and glycols and derivatives thereof.
  • the polyol may be selected from the group consisting of glycerin, diglycerin, ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, pentylene glycol, hexylene glycol, and a mixture thereof.
  • polyoll includes all possible isomer.
  • propylene glycol includes 1, 3-propylene glycol, 1, 2-propylene glycol and 1, 1-propylene glycol.
  • Butylene glycol includes 1, 4-butylene glycol, 1, 3-butylene glycol, 1, 2-butylene glycol, etc.
  • the two-part composition of the present invention comprises from 5%to 30%by weight, preferably from 10%to 30%by weight of C 2 -C 6 polyol, relative to the total weight of the two-part composition.
  • the two-part composition of the present invention comprises from 5%to 15%by weight of glycerin and from 5%to 15%by weight of dipropylene glycol, relative to the total weight of the two-part composition.
  • the inventors discovered that after mixing the anhydrous part with the hydrous part, fast dissolution of ascorbic acid is achieved at room temperature and a transparent cosmetic composition is obtained.
  • the aqueous part of the two-part composition according to the present invention also comprises water.
  • the water used may be sterile demineralized water and/or a floral water such as rose water, cornflower water, camomile water or lime blossom water, and/or a natural spring water or mineral water, for instance: Vittel water, Vichy basin water, Uriage water, Roche Posay water, Bourboule water, Enghien-les-Bains water, Saint Gervais-les-Bains water, Néris-les-Bains water, Allevar-les-Bains water, Digne water, Maizines water, Neyrac-les-Bains water, Lons-le-Saunier water, Eaux Bonnes water, Rochefort water, Saint Christau water, Fumades water, Tercis-les-bains water and Avene water.
  • the aqueous phase may also comprise reconstituted spring water, i.e. awater containing trace elements such as zinc, copper, magnesium, etc., reconstituting the characteristics of a spring water.
  • the aqueous part may also comprise water-miscible organic solvents (at room temperature: 25°C) , for instance monoalcohols containing from 2 to 6 carbon atoms, such as ethanol or isopropanol, and mixtures thereof.
  • water-miscible organic solvents at room temperature: 25°C
  • monoalcohols containing from 2 to 6 carbon atoms such as ethanol or isopropanol, and mixtures thereof.
  • the two-part composition according to the present invention may comprise an hydrous part in an amount ranging from 90%to 99.5%by weight, preferably from 95%to 98%by weight, even more preferably 95%to 97%by weight, relative to the total weight of the two-part composition.
  • the two-part composition can comprise an additional cosmetic active agent (s) other than the water soluble active ingredients as defined previously in the anhydrous part and/or the hydrous part depending on their nature.
  • additional cosmetic active agents that may be used in the two-part composition of the present invention, examples that may be mentioned include enzymes; flavonoids; moisturizers; anti-inflammatory agents; depigmenting agents; ⁇ -hydroxy acids; retinoids; antibacterial active agents; tensioning agents; ceramides; essential oils; UV-screening agents (or sunscreens) , anti-ageing agents (for example, sodium hyaluronate, salicylic acid, secale cereale (rye) seed extract) , whitening agents (for example, dipeptide diaminobutyroyl benzylamide diacetate) and mixtures thereof; and any other active agent that is suitable for the final purpose of the two-part composition.
  • enzymes for example, flavonoids; moisturizers; anti-inflammatory agents; depigmenting agents; ⁇ -hydroxy acids; retinoids; antibacterial active agents; tensioning agents; ceramides; essential oils; UV-screening agents (or sunscreens) , anti-ageing agents (for example, sodium hy
  • the two-part composition comprises an additional cosmetic active agent (s) selected from anti-ageing agents (for example, sodium hyaluronate, salicylic acid, secale cereale (rye) seed extract) and whitening agents (for example, dipeptide diaminobutyroyl benzylamide diacetate) in the hydrous part.
  • anti-ageing agents for example, sodium hyaluronate, salicylic acid, secale cereale (rye) seed extract
  • whitening agents for example, dipeptide diaminobutyroyl benzylamide diacetate
  • the two-part composition according to the present invention may also contain conventional cosmetic adjuvants or additives, which will be in the anhydrous part and/or the hydrous part depending on their nature, for instance fragrances, preserving agents, bactericides, opacifiers, dyes, softeners, buffers, electrolytes such as sodium chloride, or a pH regulator (for example citric acid or potassium hydroxide) , and mixtures thereof.
  • conventional cosmetic adjuvants or additives which will be in the anhydrous part and/or the hydrous part depending on their nature, for instance fragrances, preserving agents, bactericides, opacifiers, dyes, softeners, buffers, electrolytes such as sodium chloride, or a pH regulator (for example citric acid or potassium hydroxide) , and mixtures thereof.
  • the two-part composition for caring for keratin materials according to the present invention comprises, relative to the total weight of the two-part composition:
  • glycol selected from propylene glycol, dipropylene glycol and butylene glycol
  • the anhydrous part and the hydrous part are kept separate from one another in two separate containers or preferably one container.
  • the hydrous part may be packaged in the body of a container which is closed with a cap containing the anhydrous part, a perforable and/or detachable separator being provided between the anhydrous part and the hydrous part.
  • packages include those described in FR-A-2, 476, 607, FA-A-2, 453, 793 or FR-A-2, 645, 740, all incorporated herein by reference. Given the sensitivity of ascorbic acid to light, it is preferable to use an opaque and/or amber-colored bottle, which does not allow damaging radiation to pass through.
  • the user may then mix the anhydrous part and the hydrous part to obtain a homogeneous solution.
  • the water soluble active ingredient can quickly dissolve in the hydrous part upon mixing.
  • the mixing can be done by hand-shaking.
  • Another object of the present invention is to provide a process for caring for keratin materials.
  • the keratin materials include the skin, in particular the face.
  • the two-part composition according to the present invention may be used for caring for keratin materials.
  • the present invention providees is a process for caring for keratin materials, comprising mixing the anhydrous part and the hydrous part of the two-part composition as described above together to form a solution and applying the solution to the keratin materials.
  • compositions according to invention formula (inv. ) comprising the ingredients shown in table 1 were prepared, with all amounts expressed by percentages by weight of active matter with regard to the total weight of each composition.
  • the main components of the hydrous part of the two-part composition according to the present invention are all hydrophilic liquid ingredients at room temperature, thus no specific formulation process is needed for the preparation of the two-part compositions.
  • the two-part compositions were prepared as follows:
  • phase A as anhydrous part, the original package of which was not open until mixing
  • Phase A was added into the hydrous part 24 hours after formulation of the hydrous part and then a fresh-mixing process was conducted by hand-shaking at the frequency of three times per second to observe the time needed for complete dissolution of ascorbic acid in the hydrous part.
  • “fast dissolution” is achieved if the mixing and shaking is no longer than 1 minute, and the acceptable criterion of dissolution is achieved as no visible particles.
  • the skin feeling after application for each of the two-part compositions of invention and comparative formulas freshly mixed after formulation of the hydrous part were evaluated by a panel of 5 women, who are reactive to skin discomfort caused by cosmetic products and trained for the standard application method.
  • the freshly mixed compositions were transparent.
  • the panellists were asked to score for the skin feeling after application based on the following standards, wherein skin feeling includes watery and irritation.
  • Item Inv. 1 Inv. 2 Inv. 3 Comp. 1 Time to dissolve (Second) 40.4 41.4 42.2 59.2 Watery feeling 5 5 5 2 Irritation 5 5 5 2

Abstract

A two-part composition for caring for keratin materials comprises: a) an anhydrous part containing at least one water soluble active ingredient; and b) a hydrous part containing: i) a xanthan gum; and ii) at least one C2-C6polyol; wherein the anhydrous part and the hydrous part are separate. A process for caring for keratin materials, comprising mixing the anhydrous part and the hydrous part of the two-part composition as described above together to form a solution and applying the solution to the keratin materials.

Description

TWO-PART COMPOSITION FOR CARING FOR KERATIN MATERIALS TECHNICAL FIELD
The present invention relates to a composition for caring for keratin materials such as the skin, in particular the face. In particular, the present invention relates to a two-part composition for caring for keratin materials such as the skin, in particular the face. The present invention also relates to a process for caring for keratin materials such as the skin, in particular the face.
BACKGROUND
Whitening active ingredients such as ascorbic acid (vitamin C) stimulates the synthesis of connective tissue, in particular of collagen, enhances the defences of skin tissue against damage by environmental agents such as ultraviolet radiation and pollution, compensates for any vitamin E deficiency of the skin, depigments the skin and has an anti-free radical function. These last two properties make it an excellent candidate as a cosmetic or dermatological active agent for combating and/or preventing skin ageing. Efforts have been made for a long time to formulate ascorbic acid in the cosmetic and dermatological fields, in various galenic forms, because of its numerous beneficial properties.
Unfortunately, because of its chemical structure (alpha-ketolactone) , ascorbic acid is very sensitive to certain environmental parameters such as light, oxygen, water (through its pH and through the presence of traces of metals) . The rapid degradation of ascorbic acid formulations occurs in the presence of these conditions, which is counter to the desired results. In order to reduce and/or retard the degradation of ascorbic acid, several solutions have already been envisioned in the prior art.
One of such solutions consists in blocking the reactive site of ascorbic acid, namely the hydroxyl site, especially by esterification or etherification with phosphated, sulphated or alkylated compounds (see in U.S. Pat. No. 5,087,446, JP-A-69/115558 and JP-A-83/129892 all incorporated herein by reference) . Although more stable than ascorbic acid, these ascorbic acid derivatives are unfortunately much less effective than ascorbic acid itself.
Another solution consists in formulating the ascorbic acid in an acidic gel having a pH of not more than 3.5 and containing a high quantity of glycol, as described in WO-A-90/12572 incorporated herein by reference. Because of the acidic pH used and the presence of a large quantity of glycol, that is to say of solvent, this gel is poorly tolerated by the skin, whose pH is about 5.5. A repeated application of this gel to the skin causes irritation.
Another solution consists in using ascorbic acid in powdered form and in dissolving it in water just before use. Because of the high acidity of the solution obtained, it is aggressive and risks causing substantial irritation of the skin.
Another solution uses the freeze-drying of an aqueous solution containing an ester of ascorbic acid and hyaluronic acid; the freeze-dried product obtained is dissolved in water just before use. This solution has the disadvantages of being complex and quite expensive as well as using an ascorbic acid derivative which is less effective than that of ascorbic acid itself. In addition, the solution obtained is difficult to apply to the skin; it runs down the face and/or the body and is difficult to handle.
FR-A-2, 645, 740, incorporated herein by reference, describes a composition containing an oily phase, an aqueous phase and a solid phase to be mixed immediately before use, the solid phase containing one or more active agents (especially vitamin A) and an emulsifier, and being placed in the cap of a bottle containing the two liquid phases. This packaging allows a long storage time of the composition before mixing the three phases by shaking. After mixing, however, the composition is stable for only a few hours. Furthermore, the mixture obtained is a coarse emulsion which is not homogeneous. This results in lower efficacy; indeed, the coarser the emulsion, the less satisfactory it is as a vehicle for an active agent. In addition, the solid dissolves poorly. This three-phase composition cannot be used for an active agent with an acidic functional group, the acidic active agent carrying the risk of breaking the emulsion, or even of preventing its formation.
Other methods of stabilizing ascorbic acid include its coating (see, e.g., the technique described in FR-A-1, 600, 826 incorporated herein by reference) . This technique is, however, on the one hand expensive and can, on the other hand, impair the ascorbic acid, for example during heating.
Therefore, there is a need for a cosmetic product containing at least one active ingredient, which can achieve high dissolution rate of the active ingredient, remain the effect of the active ingredient, cause no irritation to the skin and is cost economic.
SUMMARY OF THE INVENTION
Thus, one object of the present is thus to provide a cosmetic product containing at least one active ingredient, which can achieve high dissolution rate of ascorbic acid, remain the effect of the active ingredient, cause no irritation to the skin and is cost economic.
Still another object of the present invention is to provide a process for caring for keratin materials such as the skin, in particular the face.
Thus, according to one aspect, the present invention provides a two-part composition for caring for keratin materials comprising:
a) an anhydrous part containing at least one water soluble active ingredient; and
b) a hydrous part containing:
i) a xanthan gum; and
ii) at least one C 2-C 6 polyol;
wherein the anhydrous part and the hydrous part are separate.
According to another aspect, the present invention provides is a process for caring for keratin materials, comprising mixing the anhydrous part and the hydrous part of the two-part composition as described above together to form a solution and applying the solution to the keratin materials.
Surprisingly, the inventors have found that the water soluble active ingredient can quick dissolve in the hydrous part comprising a xanthan gum and at least one C 2-C 6 glycol, i.e. a homogeneous solution can be formed after mixing the anhydrous part and hydrous part for less than 1 minute, even within 30 seconds.
In addition, the freshly mixed two-part composition presents visually pleasant transformation and appearance.
Other advantages of the present invention will emerge more clearly on reading the description and the examples that follow.
DETAILED DESCRIPTION OF THE INVENTION
The two-part composition for caring for keratin materials according to the present invention comprises:
a) an anhydrous part containing at least one water soluble active ingredient; and
b) a hydrous part containing:
i) a xanthan gum; and
ii) at least one C 2-C 6 polyol;
wherein the anhydrous part and the hydrous part are separate.
By "the anhydrous part" , it means that no water is added on purpose and the water content is less than 0.1%by weight of the anhydrous part, in particular, there is no water in the anhydrous part.
The two-part composition can be used to care for keratin materials such as the skin, in particular the face after being shaked to form a homogeneous solution.
Anhydrous part
The two-part composition of the present invention comprises an anhydrous part containing at least one water soluble active ingredient.
In some embodiments, the anhydrous part is consisted of the at least one water soluble active ingredient.
In some embodiments, the anhydrous part comprises the at least one water soluble active ingredient and a disintegrating agent.
In some embodiments, the anhydrous part is consisted of the at least one water soluble active ingredient and a disintegrating agent.
Water soluble active agent
An active agent is one capable of bringing cosmetic effect to a user, especially to the skin, e.g., to face. Such cosmetic effect can be, for example, whitening, anti-aging, hydrating, and/or moisturizing. The active agents conventionally useful for a cosmetic product can be used in the anhydrous part according to the present invention, as long as it is water soluble.
For the purpose of the present invention, the composition of the present invention is particularly applicable to use water soluble active agents which are unstable in solvated state.
For the purpose of the present invention, by “unstable” we intend to mean an ingredient or composition undergoes significant change in its structure or properties within 2 months, or preferably 1 month, in solvent or solvated state. Such change may be any one undesirable for the cosmetic use, including, but not limited to, color change, degradation, decomposition, reaction with others, significant evaporation, deposition, crystallization, and the like.
Among unlimited examples of water soluble active agents, mentions can be made of water soluble vitamins.
Water soluble vitamin
Water soluble vitamins can be used in the anhydrous part as an active agent. The useful examples of vitamin comprise vitamin C (ascorbic acid) , vitamin B group (e.g., vitamin B5 (panthenol) , vitamin B3 (niacinamide) , vitamin B1 and vitamin B2) , nicotinic acid, folic acid, pantothenic acid, the derivatives of these vitamins (in particular esters) and their mixtures.
Amongst others, vitamin C and vitamin B groups are preferably used. Vitamin C is more preferably used.
The vitamins that are suitable for use in the present invention may be represented, for example, by the products sold under the name ASCORBIC ACID 100 MESH, available from CSPC WEISHENG PHARMACEUTICAL, or from BASF.
Useful derivatives of water soluble vitamins comprise preferably 3-o-ethyl ascorbic acid, ascorbyl glucoside, or a mixture thereof.
According to an embodiment, the anhydrous part of the present invention may comprise the at least one water soluble active agent in a content ranging from 20%to 100%by weight, preferably from 40%to 95%by weight, especially from 50%to 90%by weight, relative to the total weight of the anhydrous part.
Disintegrating agent
A disintegrating agent can be used in the anhydrous part, for the purpose of facilitating the disintegration of the water soluble active agent (s) when it is dissolved in a solvent, e.g., in water. Accordingly, the disintegrating agent is preferably mixed homogenously with the water soluble active agent.
As the active agent and the disintegrating agent are both present in the anhydrous part, in order to keep homogeneous mixed state, it is preferable that the disintegrating agent is itself a binder for the active agent, or an additional binder is added, such that the disintegrating agent and the active agent is together formed into integrated solid state, e.g., particles, granules, spheres, beads, balls, bars, strips or the like, in either hollow or solid form. For rapid and unitary disintegration and dissolution of the active agent, the forms of granules, spheres, balls and the like are preferred.
Accordingly, the disintegrating agent is preferably selected from the group consisting of starches, e.g., corn starch, tomato starch, or wheat starch; a derivative of starch, e.g., pregelatinized starch, alpha starch, acrylic grafted starch or carboxymethyl starch sodium; saccharide or saccharide alcohol, or mixtures thereof.
Saccharide and saccharide alcohol
Saccharide or saccharide alcohol is preferably used as disintegrating agent according to the present invention. More preferably, saccharide or saccharide alcohol serves itself as a binder. Useful saccharides comprise monosaccharide, disaccharide and polysaccharide. The corresponding alcohol of the saccharide may also be useful.
Amongst the monosaccharide, preference may be made to glucose and fructose. Amongst the disaccharide, preference may be made to sucrose. Amongst the saccharide alcohol, preference may be made to sorbitol and mannitol.
The saccharides that are suitable for use in the present invention may be represented, for example, by the products sold under the name SUCRE SEMOULE SURFINE 250 from TEREOS.
If the disintegrating agent presents, the weight ratio of the disintegrating agent to the active agent in the anhydrous part ranges from 1: 100 to 1: 4, preferably from 1: 50 to 1: 5, or preferably from 1: 20 to 1: 10.
The anhydrous part is preferably a particle having a particle size of 20-40 mesh.
Generally, for the purpose of the present invention, the anhydrous part is used as it is from the supplier without unpacked before mixed with the hydrous part.
Preferably, the two-part composition of the present invention comprises from 0.1%to 20%by weight, preferably from 1%to 15%by weight, more preferably from 5%to 15%by weight of the anhydrous part, relative to the total weight of the two-part composition.
Hydrous part
The two-part composition of the present invention comprises a hydrous part containing a xanthan gum and at least one C 2-C 6 polyol.
Xanthan gum
Xanthan gum is a high molecular weight polysaccharide or hydrophilic colloid (also known as a gum) that is produced by fermentation of various species of the Xanthomonas, such as X. carotae, X. campestris, X. incanae, X. begoniae andX. malvacearum. Xanthan gum may comprise in their structure three different monosaccharides, namely mannose, glucose and glucuronic acid, in salt form, such as in the form of the sodium salt.
Xanthan gum may have, for example, a viscosity ranging from 850 to 1600 cps for an aqueous composition containing 1%of xanthan gum (measured at 25℃. using a Brookfield viscometer, type LVT at 60 rpm) . It has a molecular weight ranging, for example, from 1 000 000 to 50 000 000.
Xanthane gums which are more particularly preferred are KELTROL marketed by KELCO, a 1%aqueous solution of which has a Brookfield LVT viscosity at 60 rpm of 1200 to 1600 cps, KELZAN S marketed by KELCO, a 1%aqueous solution of which has a Brookfield LVT viscosity at 60 rpm of 850 cP, Rhodopol 23, 23 U, and 23 C marketed by Rhone-Poulenc, a 0.3%aqueous solution of which has a Brookfield LVT viscosity at 30 rpm of 450. ±50 cps, Deuteron XG marketed by Schoner GmbH., a 1%aqueous solution of which has a Brookfield LVT viscosity at 30 rpm of 1200 cps, and Actigum CX9 marketed by CECA, a 1%aqueous solution of which has a Brookfield LVT viscosity at 30 rpm of 1200 cps, KELZAN K9 C57 marketed by KELCO, a 11%aqueous solution of which has a Brookfield LVT viscosity at 60 rpm of 630 to 1,000 cP.
Preferably, the two-part composition of the present invention comprises from 0.01%to 2%by weight, preferably from 0.05%to 1%by weight, more preferably from 0.05%to 0.5%by weight, most preferably from 0.05%to 0.2%by weight of Xanthane gum, relative to the total weight of the two-part composition.
C 2-C 6 polyol
The composition according to the present invention comprises at least one C2-C6 polyol. A single type of polyol may be used, but two or more different types of polyol may be used in combination.
The term “polyol” here means an alcohol having two or more hydroxy groups.
The polyol may be a natural or synthetic polyol. The polyol may have a linear, branched or cyclic molecular structure.
The C 2-C 6polyol may be selected from glycerin and derivatives thereof, and glycols and derivatives thereof. The polyol may be selected from the group consisting of glycerin, diglycerin, ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, pentylene glycol, hexylene glycol, and a mixture thereof.
In the present invention, the definition of polyoll includes all possible isomer. For example, propylene glycol includes 1, 3-propylene glycol, 1, 2-propylene glycol and 1, 1-propylene glycol. Butylene glycol includes 1, 4-butylene glycol, 1, 3-butylene glycol, 1, 2-butylene glycol, etc.
In a preferred embodiment, the hydrous part containing at least one C 2-C 6 polyol selected from propylene glycol, dipropylene glycol, butylene glycol, glycerin and a mixture thereof.
Preferably, the two-part composition of the present invention comprises from 5%to 30%by weight, preferably from 10%to 30%by weight of C 2-C 6 polyol, relative to the total weight of the two-part composition.
In an embodiment, the two-part composition of the present invention comprises from 5%to 15%by weight of glycerin and from 5%to 15%by weight of dipropylene glycol, relative to the total weight of the two-part composition.
The inventors discovered that after mixing the anhydrous part with the hydrous part, fast dissolution of ascorbic acid is achieved at room temperature and a transparent cosmetic composition is obtained.
Water
The aqueous part of the two-part composition according to the present invention also comprises water.
The water used may be sterile demineralized water and/or a floral water such as rose water, cornflower water, camomile water or lime blossom water, and/or a natural spring water or mineral water, for instance: Vittel water, Vichy basin water, Uriage water, Roche Posay water, Bourboule water, Enghien-les-Bains water, Saint Gervais-les-Bains water, Néris-les-Bains water, Allevar-les-Bains water, Digne water, Maizières water, Neyrac-les-Bains water, Lons-le-Saunier water, Eaux Bonnes water, Rochefort water, Saint Christau water, Fumades water, Tercis-les-bains water and  Avene water. The aqueous phase may also comprise reconstituted spring water, i.e. awater containing trace elements such as zinc, copper, magnesium, etc., reconstituting the characteristics of a spring water.
The aqueous part may also comprise water-miscible organic solvents (at room temperature: 25℃) , for instance monoalcohols containing from 2 to 6 carbon atoms, such as ethanol or isopropanol, and mixtures thereof.
In particular, the two-part composition according to the present invention may comprise an hydrous part in an amount ranging from 90%to 99.5%by weight, preferably from 95%to 98%by weight, even more preferably 95%to 97%by weight, relative to the total weight of the two-part composition.
Additional cosmetic active agent (s)
Depending on the final purpose, the two-part composition can comprise an additional cosmetic active agent (s) other than the water soluble active ingredients as defined previously in the anhydrous part and/or the hydrous part depending on their nature.
As additional cosmetic active agents that may be used in the two-part composition of the present invention, examples that may be mentioned include enzymes; flavonoids; moisturizers; anti-inflammatory agents; depigmenting agents; α-hydroxy acids; retinoids; antibacterial active agents; tensioning agents; ceramides; essential oils; UV-screening agents (or sunscreens) , anti-ageing agents (for example, sodium hyaluronate, salicylic acid, secale cereale (rye) seed extract) , whitening agents (for example, dipeptide diaminobutyroyl benzylamide diacetate) and mixtures thereof; and any other active agent that is suitable for the final purpose of the two-part composition.
In some embodiments, the two-part composition comprises an additional cosmetic active agent (s) selected from anti-ageing agents (for example, sodium hyaluronate, salicylic acid, secale cereale (rye) seed extract) and whitening agents (for example, dipeptide diaminobutyroyl benzylamide diacetate) in the hydrous part.
It is easy for the skilled in the art to adjust the amount of the additional cosmetic active agent based on the final use of the two-part composition according to the present invention.
It is also easy for the skilled in the art to decide whether to add the additional cosmetic active agent (s) in the anhydrous part and/or the hydrous part.
Adjuvants or additives
The two-part composition according to the present invention may also contain conventional cosmetic adjuvants or additives, which will be in the anhydrous part and/or the hydrous part depending on their nature, for instance fragrances, preserving  agents, bactericides, opacifiers, dyes, softeners, buffers, electrolytes such as sodium chloride, or a pH regulator (for example citric acid or potassium hydroxide) , and mixtures thereof.
Needless to say, the skilled in the art will take care to select the optional adjuvant (s) added to the two-part composition according to the present invention such that the advantageous properties intrinsically associated with the two-part composition according to the present invention are not, or are not substantially, adversely affected by the envisaged addition.
It is easy for the skilled in the art to decide whether to add the adjuvant (s) in the anhydrous part and/or the hydrous part.
According to a preferred embodiment, the two-part composition for caring for keratin materials according to the present invention comprises, relative to the total weight of the two-part composition:
a) 5%to 15%by weight of ascorbic acid as anhydrous part; and
b) a hydrous part containing:
i) from 0.05%to 0.2%by weight of a xanthan gum; and
ii) from 5%to 15%by weight of glycerin and from 5%to 15%by
weight of a glycol selected from propylene glycol, dipropylene glycol and butylene glycol;
wherein the anhydrous part and the hydrous part are separate.
In order to store the two-phase composition according to the present invention, before the anhydrous part and the hydrous part, the anhydrous part and the hydrous part are kept separate from one another in two separate containers or preferably one container. In using a single container, the hydrous part may be packaged in the body of a container which is closed with a cap containing the anhydrous part, a perforable and/or detachable separator being provided between the anhydrous part and the hydrous part. These packages include those described in FR-A-2, 476, 607, FA-A-2, 453, 793 or FR-A-2, 645, 740, all incorporated herein by reference. Given the sensitivity of ascorbic acid to light, it is preferable to use an opaque and/or amber-colored bottle, which does not allow damaging radiation to pass through.
The user may then mix the anhydrous part and the hydrous part to obtain a homogeneous solution.
The water soluble active ingredient can quickly dissolve in the hydrous part upon mixing.
The mixing can be done by hand-shaking.
When the anhydrous part is mixed with the hydrous part by shaking, a great deal of bubbles appear, and dissolution can be seen. Then, the mixture turns into transparent.
Method and use
Another object of the present invention is to provide a process for caring for keratin materials.
The keratin materials include the skin, in particular the face.
The two-part composition according to the present invention may be used for caring for keratin materials.
Thus, according to another aspect, the present invention providees is a process for caring for keratin materials, comprising mixing the anhydrous part and the hydrous part of the two-part composition as described above together to form a solution and applying the solution to the keratin materials.
Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by those skilled in the art the present invention belongs to.
When the definition of a term in the present description conflicts with the meaning as commonly understood by those skilled in the art the present invention belongs to, the definition described herein shall apply.
Unless otherwise specified, all numerical values expressing amount of ingredients and the like which are used in the description and claims are to be understood as being modified by the term “about” . Accordingly, unless indicated to the contrary, the numerical values and parameters described herein are approximate values which are capable of being changed according to the desired purpose as required.
The term “and/or” used herein refers to one or all of the elements mentioned.
The terms "between" and "ranging from" used herein should be understood as including the limits.
The terms “containing” and “comprising” used herein respectively cover both the case that only the elements mentioned present and the case that other unmentioned elements in addition to the elements mentioned present.
All percentages in the present invention refer to weight percentage, unless otherwise specified.
The examples that follow are aimed at illustrating the two-part compositions according to the present invention, but are not in any way a limitation of the scope of the present invention.
EXAMPLES
Example 1: Preparation of compositions
The two-part compositions according to invention formula (inv. ) comprising the ingredients shown in table 1 were prepared, with all amounts expressed by percentages by weight of active matter with regard to the total weight of each composition.
Table 1
Figure PCTCN2019111506-appb-000001
Preparation process:
The main components of the hydrous part of the two-part composition according to the present invention are all hydrophilic liquid ingredients at room temperature, thus no specific formulation process is needed for the preparation of the two-part compositions. In particular, the two-part compositions were prepared as follows:
1. Provide phase A as anhydrous part, the original package of which was not open until mixing;
2. Mixing all ingredients from phase B at room temperature with agitation to obtain the hydrous part.
Example 2: evaluation of compositions
Evaluation of the dissolution behaviour
The dissolution behaviour of ascorbic acid in the hydrous part for each composition was evaluated as follows.
Phase A was added into the hydrous part 24 hours after formulation of the hydrous part and then a fresh-mixing process was conducted by hand-shaking at the frequency of three times per second to observe the time needed for complete dissolution of ascorbic acid in the hydrous part.
For the purpose of the present invention, “fast dissolution” is achieved ifthe mixing and shaking is no longer than 1 minute, and the acceptable criterion of dissolution is achieved as no visible particles.
It was observed that a great deal of bubbles appeared after the anhydrous part was mixed with the hydrous part by shaking, and dissolution could be seen. Then, the mixture turned into transparent.
The results of dissolution behavior were summarized in table 2.
Evaluation of the skin feeling
The skin feeling after application for each of the two-part compositions of invention and comparative formulas freshly mixed after formulation of the hydrous part were evaluated by a panel of 5 women, who are reactive to skin discomfort caused by cosmetic products and trained for the standard application method. The freshly mixed compositions were transparent.
The panellists were asked to score for the skin feeling after application based on the following standards, wherein skin feeling includes watery and irritation.
score  
5 Very good (very watery, no irritation)
4 Good
3 Acceptable
2 Poor
1 Very poor (very dry, obvious irritation)
The results of the average score of skin feeling were summarized in table 2.
Table 2
Item Inv. 1 Inv. 2 Inv. 3 Comp. 1
Time to dissolve (Second) 40.4 41.4 42.2 59.2
Watery feeling 5 5 5 2
Irritation 5 5 5 2
It is observed from the results above that ascorbic acid can quickly dissolve in the hydrous part for the invention formulas according to the present invention and the freshly mixed composition according to the present invention present good skin feeling upon application.

Claims (15)

  1. A two-part composition for caring for keratin materials comprising:
    a) an anhydrous part containing at least one water soluble active ingredient; and
    b) a hydrous part containing:
    i) a xanthan gum; and
    ii) at least one C 2-C 6 polyol;
    wherein the anhydrous part and the hydrous part are separate.
  2. The two-part composition according to Claim 1, wherein the water soluble active ingredient is a water soluble vitamin selected from the group consisting of vitamin C, vitamin B group e.g., vitamin B5, vitamin B3, vitamin B1 and vitamin B2, nicotinic acid, folic acid, pantothenic acid, esters of these vitamins and their mixtures.
  3. The two-part composition according to Claim 1 or 2, wherein the two-phase composition comprises 0.1%to 20%by weight, preferably from 1%to 15%by weight, more preferably from 5%to 15%by weight of ascorbic acid, relative to the total weight of the two-part composition.
  4. The two-part composition according to any one of Claims 1-3, wherein the Xanthan gum has a viscosity ranging from 850 to 1600 cps for an aqueous composition containing 1%of xanthan gum, as measured at 25℃ using a Brookfield viscometer at 60 rpm.
  5. The two-part composition according to any one of Claims 1-4, wherein the two-part composition comprises from 0.01%to 2%by weight, preferably from 0.05%to 1%by weight, more preferably from 0.05%to 0.5%by weight, most preferably from 0.05%to 0.2%by weight of Xanthane gum, relative to the total weight of the two-part composition.
  6. The two-part composition according to any one of Claims 1-5, wherein the C 2-C 6 polyol is selected from glycerin, diglycerin, ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, pentylene glycol and hexylene glycol, preferably selected from propylene glycol, dipropylene glycol, butylene glycol, glycerin and a mixture thereof.
  7. The two-part composition according to any one of Claims 1-5, wherein the two-part composition comprises from 5%to 30%by weight, preferably from 10%to 30%by weight of C 2-C 6 polyol, relative to the total weight of the two-part composition.
  8. The two-part composition according to any one of Claims 1-6, wherein the two-part composition comprises from 5%to 15%by weight of glycerin and from 5%to 15%by weight of a glycol selected from propylene glycol, dipropylene glycol and butylene glycol, relative to the total weight of the two-part composition.
  9. The two-part composition according to any one of Claims 1-8, wherein the two-part composition comprises the hydrous part in an amount ranging from 90%to 99.5%by weight, preferably from 95%to 98%by weight, even more preferably 95%to 97%by weight, relative to the total weight of the two-part composition.
  10. The two-part composition according to any one of Claims 1-9, wherein the two-part composition further comprises an additional cosmetic active agent selected from enzymes; flavonoids; moisturizers; anti-inflammatory agents; depigmenting agents; α-hydroxy acids; retinoids; antibacterial active agents; tensioning agents; ceramides; essential oils; UV-screening agents, anti-ageing agents, whitening agents and mixtures thereof.
  11. The two-part composition according to any one of claims 1-10, wherein the anhydrous part comprises the at least one water soluble active ingredient and a disintegrating agent.
  12. The two-part composition according to any one of claims 1-10, wherein the anhydrous part is consisted of the at least one water soluble active ingredient and a disintegrating agent.
  13. The two-part composition according to any of claims 11-12, wherein the disintegrating agent is selected from starches, e.g., corn starch, tomato starch, or wheat starch; a derivative of starch, e.g., pregelatinized starch, alpha starch, acrylic grafted starch or carboxymethyl starch sodium; saccharide or saccharide alcohol, or mixtures thereof.
  14. A two-part composition for caring for keratin materials comprising, relative to the total weight of the two-part composition:
    a) 5%to 15%by weight of ascorbic acid as anhydrous part; and
    b) a hydrous part containing:
    i) from 0.05%to 0.2%by weight of a xanthan gum; and
    ii) from 5%to 15%by weight of glycerin and from 5%to 15%by weight of a glycol selected from propylene glycol, dipropylene glycol and butylene glycol;
    wherein the anhydrous part and the hydrous part are separate.
  15. A process for caring for keratin materials, comprising mixing the anhydrous part and the hydrous part of the two-part composition according to any one of claims 1-14 together to form an a solution and applying the solution to the keratin materials.
PCT/CN2019/111506 2019-10-16 2019-10-16 Two-part composition for caring for keratin materials WO2021072683A1 (en)

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