FR2639224A1 - - Google Patents

Abstract

The stable emulsion comprises a first component which is a wax, a gel or a hydrocarbon oil; a second component which is a polyvalent alcohol; and a third component which is an emulsifying agent. According to the invention, the emulsion is substantially anhydrous. Use in particular for producing a pharmaceutical composition in which the excipient consists of the above stable emulsion.

Description

The present invention relates to an emulsion for a base, which can be

  used as is, or as a base to which additional ingredients can be added. According to a first aspect of the invention, there is provided a stable emulsion, which is substantially anhydrous and contains a first component, which is a wax, a gel or a hydrocarbon oil; a second component, which is a polyhydric alcohol; and a third constituent who is an agent

emulsifier.

  According to a second aspect of the invention, there is provided a stable emulsion which comprises a first component, which is a wax, a gel or a hydrocarbon oil; a second component, which is a polyhydric alcohol; a third component which is an emulsifying agent; and water, in an amount constituting not more than% by weight, and preferably not more than 40% by weight

compared to the emulsion.

  Any wax, gel or suitable hydrocarbon oil may be used. A particularly suitable product is petrolatum. A preferred vaseline is white petrolatum B.P. It is a mixture

  saturated, bleached, purified hydrocarbons.

  In its normal semi-solid state, it is a two-phase colloidal system or gel comprising high molecular weight hydrocarbons dispersed in microcrystalline or amorphous waxes. Alternatively, petrolatum can be used (eg yellow petrolatum). Details about these products are presented in the

examples below.

  The polyhydric alcohol may advantageously be an aliphatic polyalcohol, for example glycerol or

sorbitol or propylene glycol.

  The emulsifier may be any suitable emulsifier.

  It may, for example, comprise a sulphated higher alcohol having a long carbon chain, from C 10 to C 20. It is advantageously an anionic self-emulsifying wax, which may be a partially sulfated mixture of cetyl alcohol and stearyl alcohol. A particularly suitable emulsifier is the emulsifying wax B.P., which can be obtained for example under the designations LANETTE SX, CRODEX A, CYCLOCHEM or CYCLONETTE WAX. It is believed that "LANETTE", "CRODEX", "CYCLOCHEM" and "CYCLONETTE" are registered trademarks, respectively by Ronsheim & Moore (Great Britain), Croda (Great Britain), Witco (Great Britain) and Witco (Great Britain) . An appropriate anhydrous emulsion can be prepared using about 10 to 40% by weight of the gel, wax or oil, about 60 to 90% by weight of the polyalcohol and

  an amount of emulsifier not exceeding 12%.

  A representative anhydrous emulsion according to the invention may contain from 20 to 30% (preferably about 25%) by mass of petrolatum, from 70 to 80% (preferably about 72%) by weight of glycerol and from 3.5 to 0% (preferably about 4%) by weight of wax

emulsifier B.P.

  The emulsion provided by the invention may be an alcohol-in-oil emulsion in which the polyalcohol is the dispersed phase and the wax, the gel or the hydrocarbon oil is the continuous phase, or an oil-in-l emulsion. alcohol, wherein the wax, gel or hydrocarbon oil is the dispersed phase and the polyhydric alcohol is the continuous phase. The nature of the formed emulsion (alcohol-in-oil or oil-in-alcohol) turns out to depend solely on the relative proportions of the two constituents. Without wishing to be bound by the theory, it seems that the droplets of the dispersed phase are coated with the emulsifying agent, and that these coated droplets are dispersed in the phase.

  continues to give a stable product.

  The viscosity of the emulsion can be adjusted by varying the proportion of the wax, gel or oil. An increase in the proportion increases the viscosity. Decreasing the proportion decreases the viscosity. The emulsion can advantageously be prepared by using a mixing tank, into which the constituents are sent from their own feed tanks. The multi-OH component (such as glycerol) can be advantageously heated to a temperature of about 55 to 90 ° C, and the other major component, such as petrolatum, can be advantageously heated to about 55-90 ° C. The emulsifier can then be advantageously mixed with petroleum jelly and then incorporated in a final base mixture with glycerol. Mixing can be done

  using a helical mixer.

  The invention extends to a process for preparing a stable emulsion, which comprises heating a wax, a gel or a hydrocarbon oil at a temperature of 55 to 90 ° C; adding a suitable emulsifying agent to the wax, gel or hot hydrocarbon oil; heating a polyhydric alcohol at a temperature of 55 to C; and mixing the hot polyalcohol with the hot mixture of the wax, the gel or the hydrocarbon oil and the agent

  emulsifier, to form a homogeneous mixture.

  The preferred mixing temperature for each of the wax, gel or hydrocarbon oil and polyhydric alcohol components is 75 to 80 ° C. Preferably, these constituents are at substantially the same temperature as when they are mixed with each other. Simultaneous heating of the constituents and their mixing makes it possible to obtain, without the presence of water, a homogeneous mixture of the hydrocarbon wax and the polyalcohol. After mixing the constituents over the indicated temperature range, the mixture is cooled to give the homogeneous product. The product, at room temperature, is

usually a soft gel.

  If desired, other products may be added, for example perfumes, drugs or other active pharmaceutical ingredients, cosmetic active ingredients or the like. Specific examples are the following: antimycotics, such as: - amphotericin (for example in an amount of about 3% by weight with respect to the emulsion), - clotrimazole (for example in an amount of about 1% by weight relative to the emulsion), - econazole (for example about 1%), and - miconazole (for example about 2%); anti-inflammatory agents, such as: - betamethasone-17 valerate (e.g., about 0.1%), - hydrocortisone (e.g., about 1%), -d prednisolone (e.g., about 0.5%), clobetasone butyrate (e.g. about 0.05%), and - indomethacin (e.g., about 0.1%); antiseptic agents such as: cetrimide (e.g., about 0.5%), and cetylpyridium chloride (e.g., about 0.5%); and sunscreen / ultraviolet absorbing agents such as: - sulisobenzone (e.g., about 8%), - ethylmethyl p-methoxyannamate (e.g., about 6%), and -benzyl salicylate (e.g.

at 7%).

  Additives soluble in water or soluble in an oil can be added to the emulsion according to the invention and mixed at room temperature for

  give a stable and homogeneous product.

  The emulsion provided by the invention can be used as a cosmetic base for application to the skin. It can also be used for the administration of other cosmetic materials, or for the local administration, to a patient, of active pharmaceutical ingredients. In addition, it can be used as a base for hair straightening. When the emulsion is for use with drugs, the preferred polyalcohol component may be propylene glycol propane-1,2-diol (i.e.

C3H802).

  Thus, the invention also extends to the use of an emulsion according to the invention, intended to prepare a substance or composition for application to human skin or hair, and also to a substance or composition for application. cosmetic or therapeutic on the skin or human hair when it is prepared

  from an emulsion according to the invention.

  In addition, and as stated above, if it is to be used as a sunburn cream, it may contain other substances,

to stop the action of the sun.

  Tables A and B below give details respectively of the characteristics of petrolatum.

white and yellow petrolatum.

(a) WHITE VASELINES 7

  WHITE VASELINE WAXREX 521 (STANDARD WHITE)

WHITE VASELINE

BP / USP 76613

Ii i VALUES RE-

  PROPERTIES METHOD SPECIFICATION PRESENTATIVES

  Color, Lovibond IP 17 1.5 Y / 0.3 R max 0.5.Y / 0.1 R (2 "cell) Melting point & IP 31 38 - 56 50 drop, (C) Penetration at 25 ' C, ASTM 150 180 160 id (mm) D937 j Viscosity (mm2 / sec) ASTM none specific 11.9 to 100 C fixed D445 BP absorption 0.50 max -0.06 light (0.05% solution) at 290nm) Organic materials BP No release - Conforms to odor odor acrid Sulphated ash BP 0.1% max Complies Acidity / alkalinity BP / USP 'neutral vis-à-Compliant

turn screw

  nesol in the conditions; Test Density 60/60 F USP 0.815 - 0.880 0, 877 (15.6 / 15.6.C) t Organic acids USP No more than Compliant 400 μl of

0.100 N NAOH

  Penetration, d (mm) ASTM 100 - 300 160 Fixed oils, USP None Material Conforms to grease and oily or solid resins after test Calcination residue; USP 0.1% max Compliant (b) PETROLATUMS (YELLOW PETROLATUMS)

WAXREX 562 WAXREX 541

PETROLATUM USP YELLOW YELLOW

  (YELLOW PETROLATUM) (YELLOW SC) (STANDARD YELLOW)

PROPERTIES METHOD 76796 76814

  Color, Lovibond IP 17 35 Y / 3R 1.5 Y / 1.5 R (2 "cell) Max. (1.5" cell) Melting Point C ASTM IP 53 - 58 58 - 65 D127 Penetration at 25 ° C , ASTM 210 - 245 160 - 180 D937 Viscosity (mm2 / sec) ASTM 10.5-16.5 6.5 - 8, 25

at 98.9'C D445

  Absorption of BP absorbance at absorbance at

light 29 nm less than 29 nm

  less than 0.75 less than 0.75 Organic matter BP / USP no odor no foreign odor acrid detectable detectable Ashes sulphate BP max 0.1% max 0.1% Density at USP 0.815-0.880 0.815-0.880

6 / 15,6'C

  Organic acids IUSP No more than Not more than 400% of 400 μl of NaOH 0.01 N NaOH 0.01 N Penetration ASTM 150-180 dmm 150-180 dmm

  Fixed oils, USP None

  fats and resins

  loose or solid solid does not separate after test after test "WAXREX" is a trademark of TEXACO which

is a German company.

  "76796", "76814" and "76613" are the TEXACO identification numbers for the petrolatums specified in Tables (a) and (b). "LOVIBOND" is an instrument trade name provided by British Drug Houses and used for the purpose of comparing

and to match colors.

  "ASTM D937" is an abbreviation of "American Society of

Testing Materials, D937 Test ".

  "IP17" is the abbreviation of International

Pharmacopoeia, test No. 17 ".

  "IP31" is the abbreviation of International

Pharmacopoeia, Test No. 31 ".

  "BP" is an abbreviation of "British Pharmacopoeia" "USP" is an abbreviation of "United States Pharmacopoeia". "Y" is the abbreviation for "Yellow", and "R" is the abbreviation for "Red". So,

  1 ", 5Y / 0.3R max" means "1.5 yellow / 0.3 red maximum".

  The invention is now described with the aid of the following nonlimiting example, in which the wax, the gel or the hydrocarbon oil (that is to say the first constituent) is white petrolatum, polyalcohol ( that is, the second constituent) is glycerol, and the emulsifying agent (i.e. the third

constituent) is the LANETTE SX.

  Glycerol is a syrupy liquid that absorbs moisture from the air and is known by the name

  Propane-1,2,3-triol chemical with the formula C3H803.

  LANETTE SX comprises a colloidal dispersed mixture consisting of 90 parts of "LANETTE" O and 10 parts of sodium alkylsulfate. Its CTFA designation is cetearyl alcohol and sodium lauryl sulphate. It is a yellow to white granulated mass containing approximately 99% fats, 0.235 to 0.279 mval-g, a maximum of 1.4% inorganic salts, a maximum of 1.0% water, a pH (in suspension at 1%) of 6.5 to 8 and a solidification temperature of 50 to 54 C. "CTFA" is the abbreviation of

  "Cosmetic Toiletry and Fragrances Association".

  The mixture of the constituents may be implemented using the apparatus illustrated in the accompanying drawings, in which: FIG. 1 is a schematic representation of an apparatus for the preparation of an emulsion according to the invention ; and Figure 2 is a three-dimensional representation

of a piece of equipment.

  In FIG. 1, the reference numeral 10 generally indicates an apparatus for the preparation

an emulsion according to the invention.

  To stay brief and facilitate the description,

  the apparatus is described in its orientation in use, as shown in FIG. 1, and the words such as "horizontal", "up", "above", etc., which indicate in a manner generally a relative position or direction, should not be considered as limiting. The apparatus 10 comprises two feed tanks 12 and 14, each having a capacity of 285 kg of glycerol, and a feed tank 16 which can contain 196 kg of petrolatum. These tanks may consist of any heating tank. Preferably, these are electrically heated tanks (for example Vulcan tanks), which facilitate regulation.

fine temperatures.

  The tanks 12, 14 and 16 communicate with a mixing tank 18 open at its upper part, through connecting pipes 20 and a manifold 22. The tank 18 has a maximum capacity of 1000 kg. The connecting pipes 20 are connected to valves 24, which allow a manual adjustment of the

  discharge rate of the contents of the tanks 12, 14, 16.

  The collector 22 comprises a helical mixer (not shown), having five turns 360 ', and intended to mix the contents of the feed tanks 12, 14 and 16 before introduction into the mixing tank 18. The helical mixer has been specially developed to give a suitable primary mixture of the hot liquid before it enters the mixing tank 18. The diameter of the helical mixer must be large enough to accept the flow of liquid from the tanks 12, 14 and 16 when the valves 24 are fully open. The lower end portion of the helical mixer is disposed at an angle of 30 'to the horizontal above the mixing tank

open 18.

  A pump with an electric motor 26 is provided for recycling the contents of the mixing tank 18, the contents of which are sent, by pumping, and after passing through an opening 28 arranged in the bottom of the tank 18, in the tank 18 located at immediate vicinity of its upper opening, through a pipe 30 whose diameter is between 12 and 40 mm, and return from

of the tank 18.

  The preferred size of the motor (not shown) corresponds to a 1.1 kw, 50 Hz, 1390 rpm motor, which is connected to a transmission designed to reduce the number of revolutions to 226 rpm. The motor drives a cylinder 32, of circular section, hard nitrile rubber, which can rotate about its longitudinal axis and in a direction indicated by the arrow 34. The cylinder 32 is fitted with a soft friction inside an envelope tubular, or stator (not shown). The outer surface 26 of the cylinder defines a helical groove 38, which extends between opposite ends of the cylinder 32. In use, the cylinder 32 is driven at about 226 rpm. The content of the mixing tank 18 enters the pump 26 and, along the groove 36 is sent in the direction indicated by the arrow 40, before entering the pipe 30 and being

returned to the mixing tank 18.

  The following nonlimiting example illustrates the invention. In each of the tanks 12 and 16, 200 kg of glycerol were introduced and 14 196 kg of petrolatum were introduced into the tank. Glycerol and petrolatum in these tanks were slowly heated to 73-75C. Then 38 kg of LANETTE SX was added to the vaseline of the tank 14, and the mixture obtained was stirred until the LANETTE SX

dissolve in petroleum jelly.

  When the contents of the reservoirs 12, 14 and 16 have reached the desired temperature and the SX LANETTE has dissolved in petrolatum, the glycerol and vaseline / LANETTE SX have been removed at a rate (adjustable by the intermediate of the valves 24) so as to maintain as much as possible in the tanks 12, 14 and 16 the same glycerol / vaseline mass ratio as that

which originally existed.

  Glycerol and petrolatum were introduced by gravity into the mixing tank 18 via the

  helical mixer installed in the manifold 22.

  As soon as the evacuation of the reservoirs 12, 14 and 16 was triggered, the pump 30 was started, which initiated the circulation of the glycerol / vaseline / LANNETTE SX mixture. As soon as the contents of the reservoirs 12, 14 and 16 had been completely discharged into the mixing tank 18,

  circulates the resulting mixture for about 1 hour.

  The mixture took on a lighter color and reflected as if it had been forced through the cylinder 32. It is believed that the relative narrowness of the pipe 30 through which the mixture was pumped upon its return to the tank 18 contributed to the clarification of the

color.

  After about 1 hour of circulation, the resulting product was allowed to stand for several hours, or at least until the temperature of the mixture in the

  mixing tank 18 has fallen to about 30-35 C.

Then we added perfume.

  The mixture was allowed to cool to room temperature. It was allowed to stand during this cooling period, except for a brief moment every 2 hours, when mixing was induced by

  pump 30 to allow circulation of the mixture.

  The emulsion obtained was in the form of a slightly tacky, soft, gray to white gel, which was found to be extremely stable. It has been found, for example, that the product can be boiled and even heated at temperatures above 120 ° C without any noticeable separation of constituents. After cooling to room temperature, the product was identified in its original form. In addition, freezing the product for several days caused no separation, either in the frozen state or after returning to ambient temperature. Thus, temperature fluctuations did not affect

  undesirably the stability of the product.

  In another example, in which the mixing operation of petrolatum and glycerol was not to subject their mixture to friction and pressure similar to those applied to the mixture from the tank 18 when it was forced to through the cylinder 32 and the pipes 30, the color of the emulsion obtained was darker, its texture was not as

  fine and its eventual brilliance was much weaker.

  The anhydrous product does not promote bacterial growth and, moreover, does not require or contain any preservatives. Water can be added in amounts of up to 65%, without the use of any preservative. It seems that this is due to

the preservative action of glycerol.

  In its anhydrous or hydrated state, the product of the invention has extremely good moisturizing properties of the skin and can be advantageously applied to the skin or the hair. It softens the skin and leaves it a slight glow, particularly marked and pleasant on darker skin. The constituents of

  Glycerol type have a lightening effect on the skin.

  It is believed that the product will prove particularly suitable for black afro hairstyles because

  gels the hair and gives it a shiny black appearance.

  The product is a benefit for those who suffer from dry skin and turns dry skin, callous or cracked, for example on the heels, into healthy skin and

flexible.

  The emulsion of the invention may further be used as a bath or shower gel. Its user spreads a small amount on his body or face, adds water and rubs into the skin, the milky lotion obtained. The skin

becomes flexible, but not greasy.

  Creams comprising the emulsion may contain water in amounts of up to 60%, preferably up to and especially 20% relative to the total mass of the first, second and third

  constituents of the emulsion. These creams can be used

  as nutritional creams or sunscreens, or as vehicles for therapeutically active ingredients, for use as antiseptics, corticosteroids, etc. Lotions are formed by adding water to the emulsion in amounts of 30 to 92%, preferably 50 to 50% and most preferably 40% to the total mass of the first, second and third components. emulsion. This gives a very soft lotion, which can be used for applications

  similar to those mentioned above for creams.

  In brief, the emulsion according to the invention, at least as shown in the examples, is a stable product which can be easily diluted with oil and / or water to produce several different cosmetic or pharmaceutical preparations, including the face creams, hand and body lotions, preparations for hair care, medicinal preparations in the form of gels, creams and lotions and, when diluted with light oils, other products for which it is desirable

  use a cream base free of preservatives.

  Even in an anhydrous state, it has excellent moisturizing properties. In addition, it is not allergenic and its preparation is relatively simple and

cheap.

Claims (15)

  A stable emulsion comprising a first component which is a wax, a gel or a hydrocarbon oil; a second component which is a polyhydric alcohol; and a third component which is an emulsifier, and characterized in that the emulsion is substantially anhydrous. A stable emulsion comprising a first component which is a wax, a gel or a hydrocarbon oil; a second component which is a polyhydric alcohol; a third component which is an emulsifying agent; and characterized in that it contains water in a quantity not   greater than 60% by weight relative to the emulsion.   3. Emulsion according to claim 2, in the form of a cream and characterized in that it contains water in an amount of 0 to 40% by weight relative to the emulsion. 4. Emulsion according to any one of   preceding claims, characterized in that the agent   emulsifier comprises at least one sulfated higher alcohol   having a carbon chain length of C 0 -C 20.   5. Emulsion according to any one of   preceding claims, characterized in that the agent   emulsifier comprises an anionic emulsifying wax constituting about 1 to 14% of the total mass of the first and second constituent.   6. Emulsion according to any one of   preceding claims, characterized in that the   wax, the gel or the hydrocarbon oil comprises a petrolatum, and the polyhydric alcohol comprises glycerol or sorbitol or propylene glycol.   7. Emulsion according to any one of   preceding claims, characterized in that the   wax, the gel or the hydrocarbon oil and the polyalcohol are present in the following proportions relative to the total mass of the first and second constituents: 10 to 40 %: 60 to 90%.   8. Emulsion according to any one of   preceding claims, characterized in that   comprises petrolatum, glycerol and emulsifying wax BP in the following proportions relative to the total mass of the first and second constituents: %: 70. 80%: 3.5 to 10%.   A pharmaceutical composition which comprises a medicament and an excipient or carrier therefor and characterized in that the excipient or vehicle comprises an emulsion according to any one of preceding claims.   10. A process for emulsifying a wax, a gel or a hydrocarbon oil, and a polyalcohol, which process is characterized in that it comprises the steps of: heating a wax, a gel or a hydrocarbon oil at a temperature of 55 to 90 C; adding a suitable emulsifying agent to the wax, gel or hot hydrocarbon oil; heating a polyhydric alcohol at a temperature of 55 to C; and mixing the hot polyalcohol with the hot mixture of wax, gel or hydrocarbon oil and the agent   emulsifier, to form a homogeneous mixture.   11. The method of claim 10, wherein the wax, the gel or the hydrocarbon oil is a petrolatum at a temperature of 75 to 80 C, the polyhydric alcohol is glycerol or sorbitol or propylene glycol at a temperature of 75 to 80 C, and the emulsifying agent comprises   an anionic self-emulsifying wax.   12. The method of claim 10 or 11, characterized in that it comprises the step of mixing together the wax, the gel or the hydrocarbon oil, the emulsifier and the polyalcohol in the following proportions by weight: 20 to 30%: 3.5 to 10%: 70 to 80%, relative to the mass of the wax, gel or oil hydrocarbon and polyalcohol.   13. Use of an emulsion according to one   any of claims 1 & 8 to prepare a   susbtance or a composition for application on the skin or human hair.   14. A substance or composition for cosmetic or therapeutic application to human skin or hair as prepared with an emulsion according to   any of claims 1 to 8.   15. Stable emulsion as prepared by   the method according to any of claims 10 to 12.