FR2680686A1 - THREE-PHASE LOTION FOR BODY, PHARMACEUTICAL OR COSMETIC USE. - Google Patents

Abstract

The lotion consists of an upper oily phase, an intermediate silicone phase and a lower aqueous phase and contains at least one volatile silicone soluble both in the oily phase and in the silicone phase.

Description

The present invention relates to a three-phase lotion intended

  for bodily, pharmaceutical or cosmetic use.

  Multi-phase lotions are known in particular as a vehicle for cosmetic or pharmaceutical active principles and comprise at least two mutually insoluble fluid phases, which has the effect that they are present at rest in the form of separate layers. The user of such a lotion proceeds, before its application to the body, to its agitation for a few seconds in order to produce an emulsion After use, the distinct phases then reform into a

more or less variable time.

  The advantage of multi-phase lotions is to be able to contain, for example in the fatty phase, a lipophilic active principle and at the same time to contain in the aqueous phase a hydrophilic active principle without the two active principles being able to come into contact at rest. This is important in the case of active ingredients which are incompatible with each other or with

some vehicles.

  It is described, for example, in British patent application No. 2 206 048, mainly two-phase lotions consisting of an aqueous phase containing polyols and / or alcohols, an oily phase containing volatile silicones and a surfactant. can be of the type

dimethicone copolyol.

  However, for two-phase lotions, there are drawbacks linked to a large interface surface area between the two phases, which does not completely prevent the unwanted interaction of the various active ingredients. Tri-phase lotions have therefore been proposed, characterized by an intermediate phase consisting of silicone oils, in particular polydimethylsiloxanes (hereinafter PDMS), which are neither soluble nor in the fatty phase.

  neither in the lower aqueous phase.

  These lotions have been described in German patent application DE 30 09 763 which illustrates in its example 4 a lotion consisting of an aqueous phase, a hydrophobic phase comprising PDMS and a third fatty phase consisting of paraffin fluid, octyl-2-dodecanol

and decyl oleate.

  A three-phase cosmetic lotion has also been described in

  Japanese Patent Application (Publication No.) 57-144,210.

  Tri-phase lotions of this type, however, have a certain number of drawbacks, in particular with regard to the long phase separation time after use and also with regard to their cosmetic effect: the presence of an oil layer. silicone intermediate -2- can give the user an unpleasant oily feeling on the skin

  depending on the type and concentration of oil.

  In fact, it is desirable for this type of lotion to present, from the emulsified state, a separation of the phases within a period of not less than 5 minutes so as to allow the user to use the emulsion without being constantly forced to move the container In addition, it is desirable that this period is less than 24 hours for the visual aesthetic effect of the reformation of the three phases to occur within a reasonable time It has now been discovered, unexpectedly and surprising that the addition to such a three-phase lotion of an amount of at least one volatile silicone, preferably to the silicone phase of the lotion, has the effect of reducing the separation time of the two upper phases of the lotion tri-phase and at the same time bring to the product

  a freshness effect when it is applied to the skin.

  The present invention therefore relates to a three-phase lotion intended for bodily, cosmetic or pharmaceutical use, comprising an upper oily phase, an intermediate silicone phase and a lower aqueous phase characterized in that it contains at least one volatile silicone.

  It is understood in the context of this description

  that the expression "oily phase" excludes silicone oils.

  The lotion according to the invention, which does not necessarily contain a surfactant, is of additional interest since this ingredient, often present in cosmetic compositions, is liable to irritate

the skin.

  The absence of this ingredient also makes it possible to carry out

  savings on the final cost of the lotion according to the invention.

  The volatile silicones which are used according to the invention are

  both soluble in the oily phase and in the silicone phase.

  As volatile silicones, cyclomethicones of formula -CH Si 'O -CH 3 n can be used

  o N is an integer from 3 to 8.

  Among the particularly preferred cyclomethicones, mention will be made of

  cyclopentadimethylsiloxane (n = 5) and cyclotetradimethylsiloxane (n = 4).

  -3- It is possible in particular to use the products sold by the company DOW CORNING under the names "DC FLUID 244", "DC FLUID 245", "DC FLUID

344 "and" DC FLUID 345 ".

  Other cyclomethicones which can be used according to the invention are those sold by the company GOLDSCHMIDT under the name "ABIL K 4"; by the company RHONE POULENC under the names "SILBIONE 70045 V 2" and "SILBIONE HUILE 70045 V 5; as well as by the company UNION CARBIDE under the

  names "VOLATIL SILICONE 7158" and "VOLATIL SILICONE 7207".

  As other type of volatile silicone, the PDMSs of formula may also be mentioned

CH CH CH

CH 3-i If CH

CH 3 CH 3

  o N is an integer less than or equal to 3.

  For the sake of precision, it is necessary to express the proportions of the oily and silicone phases as well as of the volatile silicone relative to the total weight of these three constituents (hereinafter called the non-aqueous constituents) because the proportion of aqueous phase according to the invention can vary widely (between 5 and 90% and preferably between 40 and 80% relative to the total weight of the lotion) depending on the desired use. Thus, in general, the lotion according to the invention can comprise, relative to the total weight of the nonaqueous constituents, from 1 to 70% of volatile silicone; from 10 to 60% of an oily phase; and

  from 10 to 55% of a silicone phase.

  According to a preferred embodiment, the lotion according to the invention

  contains 25 to 60% volatile silicone.

  According to a particularly preferred embodiment, the lotion according to the invention comprises: from 25 to 60% of volatile silicone from 15 to 45% of an oily phase; and from 15 to 45% of a silicone phase, relative to the total weight

non-aqueous constituents.

  In order to ensure better settling of the phases, it is preferable that the viscosities of the different phases are between

certain limits.

4 2680686

  Thus, the silicone phase must generally have a

  viscosity between 5 and 800 mm 2 / s and preferably between 10 and 400 i Mm 2 Is.

  This does not however prevent certain constituents of the mixture of the silicone phase from being able individually to exhibit a viscosity beyond these limits. The oily phase must generally have a viscosity

  between 3 and 400 mm 2 / s and preferably between 10 and 200 mm 2 / s.

  In order to ensure the formation of a three-phase lotion (and not a two-phase lotion), the oily phase should be formulated so that it is less dense than the silicone phase In any event, the oily and silicone phases are less dense than water and therefore form the

  upper and intermediate layers of the lotion according to the invention.

  It is however preferable in order to ensure a good visual effect that

  the density of the three phases is between precise limits.

  As regards the silicone phase, its density can thus be between 0.92 and 0.99 g / cm 3 and preferably between 0.93 and 0.97 g / cm 3 and the density of the oily phase can be between 0.80 and 0.96 and

  preferably between 0.88 and 0.91 g / cm 3.

  Although the density and viscosity of the oily phase are specified above this does not prevent that certain constituents of any mixture of oils can have values individually outside the

given limits.

  For the lower aqueous phase of the lotion according to the invention, mainly water is used which optionally contains water-soluble active principles in a proportion of 1 to 50%, preferably between 3

  and 30%, by weight relative to the total weight of the aqueous phase.

  According to a preferred embodiment of the invention, it is possible to add to the aqueous phase an alcohol present, preferably, at a concentration of between 0.0001 and 1% relative to the total weight of the

lotion.

  According to another preferred embodiment of the invention, it is possible to add to the aqueous phase at least one gelling agent which has the effect of improving the formation of an emulsion during the stirring of the three-phase lotion. As gelling agent, it is possible to use, for example, those having a low flow threshold (that is to say gels which can flow under their

  own weight) and low gelling power.

  They are gelling agents of the natural type, such as galactomannans such as guar and carob, carrageenans such as Dgalactopyrannose, alginates such as sodium alginates

2680686

  (polymannuronate and guluronate), celluloses and its derivatives such as methylcellulose, ethylcellulose, propylcellulose, hydroxypropylmethyl cellulose, xanthan gums such as those consisting of the following monomers: D-glucose, D-mannose and acid Dglucuronic, or they are synthetic gelling agents of the carboxyvinyl polymer type such as those sold under the name "CARBOPOL" by the company GOODRICH or glyceryl polymethacrylates such as those sold under the name "LUBRAJEL" by the Company GUARDIAN; The gelling agent may be present in an amount of 0.01 to 10% by weight

  relative to the total weight of the aqueous phase.

  When using such a gelling agent, it is preferable to use an amount sufficient to obtain a viscosity of the aqueous phase generally between 0.01 and 20 poises (1 to 200 mm 2 / s) and

  preferably between 0.01 and 2 poises (1 and 20 mm 2 / s).

  Thus, the representative proportions for each category of gelling agent are as follows: for galactomannans, carrageenans and alginates, from 0.01 to 2% and preferably from 0.05 to 0.5% by weight relative to the phase aqueous; for celluloses and derivatives, from 0.01 to 10%, and preferably from 0.3 to 7%; for xanthan gums from 0.01 to 0.3% and preferably from 0.01 to 0.1%; and for synthetic gelling agents from 0.01 to 2% and preferably

from 0.05 to 0.5%.

  When a gelling agent is used, the amount of this agent must be such that the aqueous phase has a density of between 0.98 and

  1.5 g / cm 3 and preferably between 0.99 and 1.3 g / cm 3.

  The silicone phase of the lotion according to the invention can comprise any silicone-based, fluid, non-volatile, pharmaceutically and / or cosmetically acceptable product (or mixture of products) such as silicone oils, in particular polydimethylsiloxanes (PDMS), trimethylsiloxysilicates (designation from the Cosmetic Toiletry and Fragrance Association of Washington) in association with PDMS, polydimethylsiloxane-ols, polyphenylmethylsiloxanes, trimethylsilyl monopentaerythritol. The PDMS which can be used according to the present invention have the following general formula:

-6 2680686

CH lCHC CH Si O Si O Si CH

CH 3 CH 3 N CH 3

  o N is an integer from 3 to 2000 corresponding to a viscosity included

between 1.5 mm 2 / s and 2.5 106 mm 2 / s.

  Among the commercially available PDMSs which are suitable for the present invention, mention may be made of: "DC FLUID 200" (of viscosity between 1 mm 2 / s and 2500 mm 2 / s) sold by the company DOW CORNING; "VISCASIL 60 M" (60,000 mm 2 / s), "SF-1214" and "SF-1236" sold by GENERAL ELECTRIC; "ABIL 10" and "ABIL K 3" sold by the company GOLDSCHMIDT;

  "RHODORSIL 47 V 10", "SILBIONE 70047 V 10", "SILBIONE 70047 V

  "and" SILBIONE 70047 V 300 "sold by the company RHONE POULENC;" SILICONE OIL L 45 "(10 to 100 mm 2 / s) sold by the company UNION

CARBID;

  Among the trimethylsiloxysilicates which can be used according to the invention, mention may be made of the following commercial products: "DC FLUID 593" sold by the company DOW CORNING; and "SILICONE SSX 4267", "SILICONE SS 4230" and "SILICONE SS 4267"

  sold by GENERAL ELECTRIC.

  The polydimethylsiloxane-ols which can be used according to the invention have the following formula:

OH H 3 OH

HO Si Si -0 Si OH

OH LCH 3 N OH

  o N is an integer between 3 and 2000.

  Among these, mention may be made of the following commercial products: "DC Q 21403" (100 mm 2 / s) and "DC Q 2-I 401" sold by the Company

DOW CORNING.

  The polyphenylmethylsiloxanes which can be used according to the invention have the following formula:

R R

I I

R Si O -Si R KR i R _n R

RIR N R

-7-

  o R represents CH 3 and / or C 6 H 5 and N is an integer from 3 to 2000.

  Among these, mention may be made of the following commercial products "DC FLUID 556" sold by the company DOW CORNING; "ABIL AV 200", "ABIL AV 350 and" ABIL AV 1000 "sold by the company GOLDSCHMIDT; and

  "SILICONE VP 1120" sold by the company WACKER.

  The trimethylsilyl monopentaerythritol usable according to the invention has the following formula C t CH O -Si (CH 3) 3 l When using trimethylsiloxysilicates these are

  present in a weight ratio to PDMS from 10 to 35.

  The oily phase of the lotion according to the invention may consist of any fluid oil (or mixture of oils) stable at the usual temperature of use for cosmetic and pharmaceutically or cosmetically acceptable products such as vegetable or animal oils, oils mineral or synthetic and

fatty acid triglycerides.

  Among the vegetable or animal oils, modified or not, there may be mentioned for example sweet almond oil, avocado oil, castor oil, olive oil, jojoba oil, sunflower oil, wheat germ oil, sesame oil, peanut oil, grape seed oil, soybean oil, rapeseed oil, oil safflower, coconut oil, corn oil, hazelnut oil, shea butter, oil

  palm, kernel oil, calophyllum oil.

  Among the mineral oils that may be mentioned, for example, petrolatum oil. Among the fatty acid triglycerides include caprylic / capric triglycerides, triglycerides C 10 to C 18 and

triglycerides C 12 to C 18.

  The lotion according to the invention can be applied as it is to the skin or to the hair to bring therein the properties inherent in its

constituent ingredients.

  However, it is preferable to incorporate therein at least one active principle in order to ensure, for example, a slimming, hydrating activity,

  sunscreen, anti-aging or emollient.

  As mentioned above, there is no limitation as to the choice of active ingredients to be incorporated since the fat-soluble principles - 8- can be dissolved in the oily phase and the water-soluble principles

  can be dissolved in the aqueous phase.

  Among the liposoluble active principles, retinol may be mentioned as an anti-aging agent, and as slimming agents and emollients DL nicotinate alpha-tocopherol, the oily extract of ginseng root (Panax ginseng), the oily extract of climbing ivy ( Hedera Helix), the oily extract of arnica dry flowers (Arnica Montana L), the oily extract of rosemary (Rosmarinus Officinalis N), the oily extract of marigold (Calendula Officinalis), the oily extract of sage ( Salvia Officinalis L), oily extract of St. John's wort (Hypericum Perforatum), oily extract of ulmaire (Filpendula Ulmarin L), oily extract of orthosiphon (Ortosifon

  Stamincus Benth), oily extract of seaweed (Fucus Vesiculosus).

  It is possible to add essential oils as perfuming and slimming agents such as the essence of Ceylon cinnamon, the essence of Siberian pine, the essence of Ceylon nutmeg, the essence of virgin wood, perfumes , preservatives, antioxidants,

pigments or UV filters.

  Among the liposoluble UV filters, mention may be made of ethyl-2-hexyl-4-paramethoxy-cinnamate sold under the name "PARSOL MCX" by the company GIVAUDAN and hydroxy-2-methoxy-4-benzophenone sold under the name " UVINUL M 40 "by BASF Among UV filters

  water-soluble, there may be mentioned hydroxy-2-methoxy-4-benzophenone-5-

  sulfonic sold under the name "UVINUL M 540" by the company BASF.

  Among the water-soluble active principles that may be mentioned are slimming agents such as xanthine derivatives such as caffeine, theobromine, theophylline, L-carnitine, dimethyl aminoethyltheophylline hydrochloride, silicon derivatives of the methylsilanol theophyllinacetate alginate type, vegetable derivatives of the free acid escine type, total climbing ivy saponins, climbing ivy hydroglycolic extracts, brown algae hydroglycolic extracts, birch bark hydroglycolic extract, fresh wild pansy extract, l dry aqueous extract of sage leaf, moisturizers such as glycerin, propylene glycol, sorbitol, proline, pyrrolidone carboxylic acid and its sodium derivative, urea, collagen, Aloe Vera gel , hyaluronic acid and its sodium derivative, di-methylsilanol hyaluronate, allantoin,

  preservatives, dyes, UV filters.

  One can also consider, according to the invention, the active ingredients which partially dissolve in at least two of the phases

  constitutive of the lotion according to the invention.

  Among the principles which are water-soluble but also partially liposoluble, mention may be made of xanthic bases such as caffeine. On the other hand, alpha-tocopherol nicotinate is very soluble in oils but partially soluble in water. As mentioned above, lipophilic active ingredients can be included in the oily phase and at the same time include hydrophilic active ingredients in the aqueous phase, although the

  active ingredients may be incompatible with each other.

  By way of illustration, there may be mentioned: 1 Sodium stearate soluble in the oily phase and hexamidine diisethionate soluble in the aqueous phase at p H acid

(less than 6).

  2 Calcium stearate soluble in the oily phase and potassium sulphate soluble in the aqueous phase The intermediate silicone phase slows the formation of the calcium sulphate precipitate

insoluble in water.

  In addition, certain active principles which are unstable in the presence of water, such as retinol, can nevertheless be formulated according to the invention insofar as the intermediate phase prevents contact between the phase

  upper and lower aqueous phase.

  It is also possible to incorporate into the lotion according to the invention other substances usual in cosmetics and in pharmacology such as preservatives, dyes and perfumes, etc. The lotion according to the invention is prepared by simple mixing of the ingredients in a sequence It is however preferable to add the volatile silicone to the non-volatile silicone constituents before adding them to the oily constituent (s). Then add a

  sufficient water for the intended use for the lotion.

  The three-phase lotion according to the invention is suitable for all cosmetic and / or dermatological applications possibly depending on the

  type of active ingredient (s) incorporated.

  It is particularly suitable for example in the case of a lotion

  slimming, for friction massages.

  It can also consist of an anti-sun, make-up removing, hair toning body lotion after shampooing, etc. The invention will now be illustrated in a nonlimiting manner by the following examples of formulation in which A represents the phase

  oily, B represents the silicone phase and C represents the aqueous phase.

EXAMPLES OF COMPOSITIONS

  EXAMPLE 1 Sunscreen Lotion (A) Soybean Oil Hydroxy-2-methoxy-4benzophenone sold under the name "UVINIL M 40" by the company BASF Parfum Conservatives, antioxidant (B) Polydimethylsiloxane sold under the name "DC FLUID 200" (350 mm 2 / s) by the company DOW CORNING

"VOLATIL SILICONE 7158"

  18% 2% qs qs 33%% (C) Methylsilanol mannuronate sold under the name "ALGISIUM" by the company EXSYMOL Preservatives, colorant Water qs

0.1% MA

  qs% After mixing, the decanting lotion in three phases in 1 hour and the silicone

  volatile is distributed between the oily phase and the silicone phase.

  EXAMPLE 2 Hydrating body lotion (A) Apricot oil D acetate, L-alpha-tocopherol (B) "DC FLUID 200" (10 mm 2 / s)

"VOLATIL SILICONE 7158"

  (C) Methylsilanol theophyllinacetate alginate sold under the name "THEOPHYLLISILANE" by the company EXSYMOL Galactopyrannose sulfate sold under the name "AUBY GUM x 2" by the company SANOFI Water qs% 1%% 22%

0.1% MA

0.07%

  % After mixing, the emulsified lotion decanted in three phases in volatile silicone is distributed between the oily phase and the silicone. 1/2 hour and phase -10-

-1 to 2680686

  EXAMPLE 3 Slimming lotion (A) Rapeseed oil 13% Mineral oil, apricot kernel oil and ivy extract sold under the name "VEGETOL HUILEUX DE LIERRE 4149" by the company GATTEFOSSE 2% Colorant, fragrance qs Preservatives, anti -oxidizer qs (B) "DC FLUID 200" (350 mm 2 / s) 3% "DC FLUID 200" (10 mm 2 / s) 7%

"VOLATIL SILICONE 7158" 25%

  (C) Caffeine 0.5% "AUBY GUM x 2" 0.1% Preservatives qs Colorings qs Water qs 100 After mixing, the emulsified lotion settles in three phases in 1 hour and

  volatile silicone is distributed between the oily phase and the silicone phase.

  EXAMPLE 4: Body perfume lotion (A) Wheat germ oil 16% Concentrate "88-1383" sold by the Company Créations aromatiques 1% (B) "DC FLUID 200" (350 mm 2 / s) 2 Z "DC FLUID 200 "(10 mm 2 / s) 8%

"VOLATIL SILICONE 7158" 22%

  (C) Glycerin 2% "AUBY GUM x 2" 0.1% Preservatives qs Colorants qs Distilled water qs 100 After mixing, the emulsified lotion settles in three phases over 1 hour and

  volatile silicone is distributed between the oily phase and the silicone phase.

  -12- EXAMPLE 5: Slimming lotion (A) Rapeseed oil 20% Perfume qs Preservatives, antioxidants qs Colorant 0.0004% (B) Polydimethylsiloxane-ol sold under the name "DC Q 2-1403" by the company DOW CORNING 7%

"VOLATIL SILICONE 7158 '26%

  (C) Caffeine 0.5% Preservatives qs Distilled water qs 100 After mixing, the lotion completely settles in three phases over 12 hours and the volatile silicone is distributed between the oily phase and the silicone phase. -13-

Claims (15)

  1 tri-phase lotion intended for body use comprising an upper oily phase, an intermediate silicone phase, and a lower aqueous phase, characterized in that it contains at least one volatile silicone.   2 tri-phase lotion according to claim 1, characterized in that the proportion in aqueous phase varies between 5 and 90% and of   preferably between 40 and 80% by weight relative to the total weight of the lotion.   3 tri-phase lotion according to claim 1 or 2, characterized in that it comprises by weight relative to the total weight of the volatile silicone and the oily and silicone phases: from 1 to 70% of at least one volatile silicone, from 10 to 60% of an oily phase, and   from 10 to 55% of a silicone phase.   4 tri-phase lotion according to claim 1, 2 or 3, characterized in that the volatile silicone corresponds to the following formula: CH 3 CH 3 n   o N is an integer from 3 to 8.   Tri-phase lotion according to any one of the claims   above, characterized in that the volatile silicone is chosen from   cyclopentadimethylsiloxane and cyclotetradimethysiloxane.   6 tri-phase lotion according to any one of claims   above characterized in that the silicone phase consists of at least one of the PDMS optionally in combination with a trimethyl siloxysilicate, polydimethylsiloxanes-ols, polyphenyl methyl   siloxanes and trimethylsilyl monopentaerythritol.   7 tri-phase lotion according to any one of claims   above, characterized in that it comprises from 25 to 60% of volatile silicone.   8 tri-phase lotion according to any one of claims   above, characterized in that it comprises: from 25 to 60% of volatile silicone; from 15 to 45% of an oily phase; and   from 15 to 45% of a silicone phase.   9 tri-phase lotion according to any one of claims   above, characterized in that the aqueous phase comprises a gelling agent.   Tri-phase lotion according to claim 9, characterized in that the gelling agent is of the natural type chosen from galactomannans, carrageenans, alginates, celluloses or cellulose derivatives, xanthan gums or from the synthetic type chosen from   carboxyvinyl polymers, or glyceryl polymethacrylates.   11 tri-phase lotion according to any one of claims 9   and 10, characterized in that the gelling agent is a carrageenan.   12 tri-phase lotion according to any one of claims   previous characterized in that the different phases have the following viscosities: for the oily phase, from 3 to 400 and preferably from 10 to mm 2 / s - for the silicone phase, from 5 to 800 and preferably from 10 to 400 mm 2 / s; and   for the aqueous phase from 1 to 200 and preferably from 1 to 20 mm 2 / s.   13 tri-phase lotion according to any one of claims   above characterized in that the different phases have the following densities: for the oily phase, from 0.80 to 0.96 and preferably from 0.88 to 0.91 g / cm 3 for the silicone phase, from 0.92 to 0.99 and preferably from 0.93 to 0.97 g / cm 2 and for the aqueous phase from 0.98 to 1.5 and preferably from 0.99 at 1.3 g / cm 3.   14 Tri-phase lotion according to any one of claims   above, characterized in that the oily phase consists of at least one vegetable oil, one animal oil, one mineral oil or   synthetic or at least one fatty acid triglyceride.   Tri-phase lotion according to any one of the claims   above, characterized in that it also contains liposoluble and / or water-soluble cosmetic and / or dermatological active principles,   dyes, perfumes or preservatives.   16 Tri-phase lotion according to claim 15, characterized in that the active principles are chosen from slimming agents, moisturizing agents, anti-aging agents, emollient agents and UV filters. -14- -15-   17 tri-phase lotion according to any one of claims   previous characterized in that it contains alcohol in a content between 0.0001 and 1%.   18 tri-phase lotion according to any one of claims   above, characterized in that it is free of surfactant.