WO1997026917A1

WO1997026917A1 - Composition for treating skin affections and process for its preparation

Info

Publication number: WO1997026917A1
Application number: PCT/EP1997/000269
Authority: WO
Inventors: Johannes Schreuder
Original assignee: Chemisch Adviesbureau Drs. J.C.P. Schreuder B.V.
Priority date: 1996-01-23
Filing date: 1997-01-21
Publication date: 1997-07-31
Also published as: AU1593697A; NO983215D0; NO983215L; EP0876159A1

Abstract

There is described a multifunctional composition for the treatment of chapped, sore and/or inflamed skin parts, comprising at least the following ingredients: (a) an oil fraction comprising straight or branched paraffinic oils, having from 10 to 60 carbon atoms in the chain; (b) an emulsifying system mainly comprising (b,i) mono- and/or diglycerides of high unsaturated and saturated fatty acids, and (b,ii) ethoxylated triglycerides, esterified with fatty acids; (c) vitamin E, or a derivative thereof; (d) methionine; (e) a pH regulating system; (f) a stabilizer consisting of montmorillonite; (g) water ad 100 % by weight, and the preparation and use of said composition.

Description

COMPOSITION FOR TREATING SKIN AFFECTIONS AND PROCESS FOR ITS PREPARATION. The invention relates to a composition for treating skin affections, to a process for its preparation, and to the application of said composition. In particular the invention relates to a multifunctional composition for the treatment of chapped, sore and/or inflamed skin parts such as lips, nose opening edges, eyelids and the like, while such composition does not contain ingredients which may disturb the biological equilibrium of said skin part.

Specifically, the composition of the invention heals, relieves and softens chapped, sore or inflamed lips, nose opening edges, eyelids and the like, affected by a Herpes Simplex virus type, such as fever blister and/or affections by winter weather and/or intensive sunshine.

The before mentioned affections can also be caused by flu or menstruation.

Many compositions have already been proposed for this purpose n the course of the last decade. However, the .up to now available prior art compositions have the disadvantage that they cause a burning, irritated and/or inflamed feeling, usually caused by constituents which significantly disturb the biological equilibrium of the affected skin parts . As a consequence, said prior art compositions usually d d not relieve the irritation or even pam, and certainly did not heal the affected skin in an efficient way.

Therefore one object of the present invention is to provide a multifunctional composition for the treatment of chapped, sore and/or inflamed skin parts such as lips, nose opening edges, eyelids and the like, which during application does not cause a burning, irritated and/or inflamed feeling and which facilitate an almost immediate relief and healing, and the constituents of which do not disturb the biological equilibrium of the affected sk n parts. Another object of the present invention is to provide a process for the preparation of said composition.

As a result of extensive and lengthy research and experimentation, such compositions have surprisingly been found.

Accordingly, the present invention provides a multifunctional composition for the treatment of chapped, sore and/or inflamed skin parts such as lips, nose opening edges, eyelids and the like, characterised by at least the following ingredients :

{a) An oil fraction comprising straight or branched paraffinic oils, having from 10 to 60 carbon atoms in the chain, and preferably from 15 to 25 carbon atoms, in an amount of from 10 to 60 % by weight, and preferably from 15 to 25 % by weight, relative to the weight of the complete composition, having a boiling range between 100 and 500°C at atmospheric pressure and a viscosity of preferably at most 35 mm²/s, preferably of at most 30 mm^/s, at 25°C, while the paraffinic oils may optionally be mixed with esters of higher natural fatty acids, which are preferably unsaturated, and of higher natural aliphatic alcohols, which are preferably unsaturated, of at most 20 carbon atoms in the chain, in an amount of from 0 to 2 % by weight, and preferably from 0.5 to 2 % by weight, relative to the weight of the complete composition;

(b) An emulsifying system mainly comprising

(b,i) mono- and/or diglycerides of higher unsaturated and saturated fatty acids, in an amount of from

0.5 to 3 % by weight, relative to the weight of the complete composition, e. g. Tegomuls (trademark), and

(b,ii) ethoxylated triglycerides esterified with fatty acids, according to the general formula

wherein n, m and p represent the same or different integers of from 0 to 20, under the condition that at least one of the symbols n, m and p has a value of from 5 to 20, preferably from 7 to 15, and wherein R represents the same or different saturated or unsaturated, and preferably the same unsaturated hydrocarbon residue, derived from vegetable or animal oil (e.g. Tagat TO) . The weight ratio between the amount of mono- and/or diglycerides on the one hand and of the ethoxylated triglycerides on the other hand may vary from 10 to 100 parts by weight of mono- and/or diglycerides per part by weight of ethoxylated triglycerides and preferably from 15 to 50 parts by weight of mono- and/or diglycerides per part by weight of ethoxylated triglycerides, whereas the amount of the complete emulsifying system, relative to the weight of the complete composition, may vary from 0.5 to 3.5 % by weight and preferably from 2 to 3 % by weight, relative to the weight of the total composition. (c) Vitamin E, or a derivative thereof which may easily provide vitamin E itself by conversion on the affected skin, such as Covitol (trademark), in an amount of from 0.1 to 5 % by weight, and preferably from 0.5 to 4 % by weight, and most preferably from 1 to 3 % by weight, relative to the weight of the total composition;

(d) Methionine, in the form of its L or D isomer or mixtures thereof, preferably L-methionine, or a derivative thereof which may easily provide methionine by conversion on the affected skin, in an amount of from 0.1 to 5 % by weight and preferably from 0.5 to 3 % by weight and most preferably from 1 to 2 % by weight, relative to the weight of the complete composition;

(e) A pH regulating system to adjust the pH of a present aqueous phase, including at least demineralized water and methionine, to be in the range of from 4.4 to 5.0 and more preferably from 4.5 to 4.9, comprising preferably citric acid, zinc carbonate and sodium hydroxide, or citric acid, zinc carbonate and potassium hydroxide, each of the components occurring n an amount of from 0.05 to 2.5 % by weight, relative to the weight of the complete composition.

More preferably citric acid, zinc carbonate and sodium hydroxide occur in amounts of from 0.5 to 2 % by weight, from 0.05 to 0.2 % by weight and from 0.5 to 1 % by weight, respectively, relative to the weight of the complete composition.

The pH of the final complete composition is adjusted by said pH regulating system to the range of from 4.8 to 5.1 with citric acid or sodium hydroxide. (f) A stabilizer, consisting of at least one montmorillonite, the free oxygen sites of which are occupied by quaternary groups (quaternary modified montmorillonites) . Examples of such stabilizers which are preferably included are Bentone (trademark) or Propoloid (trademark) . Said stabilizers are included in the composition in amounts of from 0.1 to 1.5 % by weight and preferably from 0.5 to 0.7 % by weight, relative to the weight of the complete composition.

(g) Water ad 100 % by weight.

Preferably demineralized water is used in amounts of from 65 to 75 % by weight, relative to the weight of the complete composition.

In addition to the before mentioned primary indispensable ingredients, one or more secondary ingredients also can be present in the complete compositions, such as;..

(h) At least one preservative.

Preferably different types are present in the continuous ultimately formed oily phase.

For example esters of parahydroxy benzoic acid may occur in the oily phase as well as in the aqueous phase.

Preferably the methyl and/or the (iso)propyl ester is present in an amount of from 0.1 to 1 % by weight and most preferably in amounts from 0.5 to 0.7 % by weight, relative to the weight of the complete composition.

Most preferably mixtures of methyl, propyl and butyl p-hydroxybenzoate are used, e.g. Phenonip (trademark) . It will be appreciated by a person skilled in the art, that these before mentioned preservatives may be completely or partially replaced by other preservatives, e.g. Germall II (trademark) or Hydroconserv (trademark), and if so, said other preservatives are present preferably in an amount of from 0.1 to 0.5 % by weight.

More preferably the preservatives occur in the aqueous phase in a total amount of from 0.3 to 0.4 % by weight;

(l) Glycerol, in an amount of from 1 to 4 % by weight and more preferably from 1 to 3 % by weight.

( ] ) A gel forming agent, such as carraghenate, preferably consisting of a polysaccharide with sulphonic ac d residues, and preferably a gel forming agent of natural origin such as one derived from seaweeds . The sulphonic acid residues have optionally been converted into salts or esters of glycol, propylen glycol and glycerol (resulting in the so-called modified carraghenates) .

The gel forming agent, e. g. the carraghenates, n amounts of from 0.1 to 5 % by weight, relative to the weight of the complete composition and preferably from 0.5 to 2 % by weight, cause a gel structure m the final composition. Such a complete composition shows a viscosity of 200 to 5000 mPa-s (centipoises) at 25°C, enabling an adequate application of the composition.

It will be appreciated by a person skilled in the art that the carraghenate may be completely or partially replaced by alternative gel forming means, such as carboxy methyl cellulose, esterified by polyacrylic acid e. g Carbopol (trademark), or hydroxy ethyl cellulose, n amounts which provide the viscosity values in the above range. (k) Perfume, in an amount of from 0.1 to 2 % by weight, preferably 0.1 to 0.3 % by weight, relative to the weight of the complete composition. Examples of such perfumes are sage oil or jacaranda.

(1) at least one protein, obtainable from aqueous extraction of plants, such as aloe vera, in amounts of from 0.1 to 0.5 % by weight, relative to the weight of the complete composition, and preferably from 0.1 to 0.3 % by weight.

The compositions according to the present invention as specified hereinbefore, are characterized by a relatively low viscosity and high stability, which guarantees an easy application, without a 'greasy" feeling or stickiness, due to the fast penetration into the skin tissue, and moreover by a healing, relieving and softening activity.

Another aspect of the present invention is formed by a process for the preparation of the hereinbefore specified compositions .

The complete continuous oily phase is prepared in one or more steps of said process, composed of oil fractions, the optional esters of fatty acids and alcohols, the emulsifying system, the stabilizer, vitamin E or a derivative thereof and the optional preservative, wherein in one or more separate steps at least one dispersed aqueous phase is prepared, composed of demmeralized water, citric acid or a citrate, zinc carbonate and sodium or potassium hydroxide, methionine, glycerol, gel forming agent, protein, and preservative and perfume

The composition according to the present invention is prepared by composing both phases and mixing them together at a temperature of 10 to 40°C, followed by additional stirring and homogenizing until an average particle size of the dispersed aqueous phase of at most 5 μ and preferably smaller than 3 μ is reached, while the pH of the final complete composition is adjusted within the range of from 4.8 to 5.1.

According to a preferred embodiment of the process to prepare the composition of the present invention, n a first step the oil fraction, the optional esters of unsaturated fatty acids and alcohols, the emulsifying system and the stabilizer are mixed and homogenized at a temperature from 60 to 90°C, whereafter the homogeneous mixture is cooled back to a temperature of at most 30°C.

The cooled mixture is mixed in a second step with vitamin E or a derivative thereof which can easily be transformed nto said vitamin, and with the perfume, until a homogeneous mixture is obtained.

The aqueous phase is normally prepared at a temperature of from 10 to 40°C and preferably from 20 to 30°C by subsequent addition of demineralized water n an amount of about one third of the total amount n the final composition, of the citric acid, of zinc carbonate and of sodium or potassium hydroxide under gently stirring until complete dissolution. If necessary the pH of the homogeneous solution is adjusted to the range of from 4.6 to 4.8 by addition of sodium or potassium hydroxide or citric acid. To this aqueous solution the remainder of the desired total amount of water, methionine, glycerol, carraghenate, preservative and protein are added whereafter the pH is again adjusted to the range of from 4.5 to 4.8.

The finally obtained aqueous phase is added to the oily phase under stirring vigorously and subsequent homogenizing at a temperature in the range of from 10 to 40°C and preferably from 20 to 30°C, whereafter the pH of the complete dispersion, having dispersed aqueous phase particles cf an average size of at most 5 μ, is in the range of from 4.9 to 5.1.

Another aspect of the present invention is formed by the application of the before specified composition, i. e. the treatment of the chapped, sore and/or inflamed skin of lips and nose opening edges, eyelids and the like, with the hereinbefore specified composition.

Such an application comprises a method being usual for said compositions, characterized by application and evenly spreading the composition on the skin area involved, in an amount of from 20 to 100 ml/m² skin area.

This treatment should preferably be performed 2 to 3 times a day.

The invention is illustrated by the following examples, however without restricting its scope to these specific embodiments .

Example 1

Under stirring and heating to a temperature of 80°C the following ingredients are combined:

paraffinic oil I, boiling range 295-390°C

Shell Ondina 15 (trademark) 10.000 kg

paraffinic oil II, boiling range 290-500°C

Shell Ondina 68 (trademark) 6.000 kg

mono- and diglycerides, Tegomuls SB (trademark) 2.280 kg

quaternary modified montmorillonite, Bentone 38 (trademark) 0.660 kg

Batch

I oleyl decalate, Cetiol V (trademark) 1.000 kg

ethoxylated triglycerides, .Tagat TO (trademark) 0.050 kg

The homogeneous mixture is cooled to 30°C and mixed with

vitamin E, Covitol (trademark; 2.000 kg

Batch perfume (sage oil) 0.125 kg II perfume (jacaranda) 0.075 kg

to a homogeneous mixture. An aqueous phase is prepared by mixing together:

f water 21.417 kg

I Batch i citric acid 1.133 kg

III ₍ zinc carbonate BCP49 0.700 kg

[ sodiumhydroxide (97 %) 0.150 kg

whereafter the pH of the aqueous solution is adjusted with either citric acid or sodium hydroxide to a pH of from 4.60 to 4.80, and

( water 49.610 kg L-methionme 1.000 kg

Batch glycerol 1.26 2.000 kg IV carraghenate, Aubygum X2 (trademark; 1.000 kg preservatives 0.600 kg protein, aloe vera 0.200 kg

The batches III and IV are combined and mixed with the mixture of batches I and II under vigorously stirring and homogenzmg until an average particle size of the dispersed phase of 3 μ is obtained, whereafter the pH of the complete composition was 5.0.

Example 2

According to the same procedure as described m Example 1, a composition was prepared from the following ingredients:

paraffinic oil I 14.700 kg paraffinic oil II 3.200 kg mono- and diglycerides 2.100 kg

Batch quaternary modified montmorillonite 0.650 kg

I ethoxylated triglycerides 0.050 kg and vitamin E 2.200 kg

Batch perfume (sage oil) 0.140 kg

II perfume (jacaranda) 0.075 kg and

/^'water 21.340 kg

Batch citric acid 1.130 kg

III zinc carbonate 0.700 kg potassium hydroxide (97 %) 0.155 kg and water 48.105 kg

L-methionine 1.300 kg glycerol 1.800 kg

Batch carraghenate 1.200 kg

IV preservatives 0.700 kg protein 0.400 kg

ExamDle 3

According to the same procedure as described in Example 1, a composition was prepared from the following ingredients:

paraffinic oil I 12.200 kg paraffinic oil II 3.200 kg

Batch mono- and diglycerides 2.200 kg

I ethoxylated triglycerides 0.055 kg quaternary modified montmorillonite 0.645 kg and fvitamin E 2.100 kg

Batch perfume (sage oil) 0.140 kg II perfume (jacaranda) 0.080 kg and water 21.500 kg

Batch citric acid 1.130 kg III zinc carbonate 0.700 kg sodium hydroxide 0.160 kg and water 49.690 kg

L-methionine 1.500 kg glycerol 2.500 kg atch carraghenate 1.300 kg

IV preservative 0.600 kg

I protein 0.300 kg

Example 4

According to the same procedure as described in Example 1, composition was prepared from the following ingredients:

_j paraffinic oil I 12 .000 kg paraffinic oil II 3 .400 kg

Batch mono- and diglycerides 2 .200 kg I ethoxylated triglycerides 0 .060 kg

Iquaternary modified montmorillonite 0 .640 kg and vitamin E acetate, D-isomer 2 .300 kg

Batch perfume (sage oil) 0 400 kg II perfume (jacaranda) 0 080 kg and water 21 900 kg

Batch citric acid 1 130 kg III zmc carbonate 0 700 kg sodium hydroxide (97 % 0 160 kg and r.water 50 250 kg

D,L-methιonιne 2 000 kg glycerol 2 000 kg

Batch preservative 0. 600 kg IV protein 0. 380 kg H

The hereinbefore specified compositions show a high stability and a fast healing, relieving and softening activity when applied on sore, chapped and/or inflamed skin of lips and nose opening edges .

Claims

1. Multifunctional composition for the treatment of chapped, sore and/or inflamed skin parts such as lips, nose opening edges, eyelids and the like, characterized by at least the following ingredients:

(a) An oil fraction comprising straight or branched paraffinic oils, having from 10 to 60 carbon atoms in the chain, in an amount of from 10 to 60 % by weight, relative to the weight of the complete composition, having a boiling range between 100 and 500°C at atmospheric pressure and a viscosity of at most 35 mm^/s _at 25°C, while the paraffinic oils may optionally be mixed with esters of higher natural fatty acids, which are preferably unsaturated, and of higher natural aliphatic alcohols, which are preferably unsaturated, of at most 20 carbon atoms in the chain, in an amount of from 0 to 2 % by weight, relative to the weight of the complete composition;

(b) an emulsifying system mainly comprising

(b,ι) mono- and/or diglycerides of higher unsaturated natural fatty acids, in an amount of from 0.5 to 3 % by weight, relative to the weight of the complete composition, and

(b.ii) ethoxylated triglycerides esterified with fatty acid, according to the general formula

wherein n, m and p represent the same or different integers of from 0 to 20, under the condition that at least one of the symbols n, m and p has a value of from 5 to 20, preferably from 7 to 15, and wherein R represents the same or different saturated or unsaturated, and preferably the same unsaturated hydrocarbon residue, derived from vegetable or animal oil,

whereby the weight ratio between the amount of mono- and/or diglycerides on the one hand and of the ethoxylated triglycerides on the other hand may vary from 10 to 100 parts by weight of mono- and/or diglycerides per part by weight of ethoxylated triglycerides, whereas the amount of the complete emulsifying system, relative to the weight of the complete composition, may vary from 0.5 to 3,5 % by weight.

(c) vitamin E, or a derivative thereof which may easily provide vitamin E itself by conversion on the affected skin in an amount of from 0.1 to 5 % by weight, relative to the weight of the total composition; (d) methionine, in the form of its L or D isomer or mixtures thereof, preferably L-methionine, cr a derivative thereof which may easily provide methionine by conversion on the affected skin, n an amount of from 0.1 to 5 % by weight, relative to the weight of the complete composition;

(e) a pH regulating system to adjust the pH of a present aqueous phase including at least demmeralized water and methionine, to be in the range of from 4 4 to 5.0, comprising preferably citric acid, zinc carbonate and sodium hydroxide or citric acid, z nc carbonate and potassium hydroxide, each of the components occurring n an amount of from 0.05 to

2.5 % by weight, relative to the weight of the complete composition;

(f) a stabilizer consisting of at least one montmorillonite the free oxygen sites of which are occupied by quaternary groups in an amount of from 0.1 to 1.5 % by weight, relative to the weight cf the complete composition;

(g) water ad 100 % by weight.

2. Composition according to claim 1, comprising

(a) an o l fraction, comprising straight or branched paraffinic oils in an amount of from 15 to 25 % by weight, mixed with esters of unsaturated higher natural aliphatic alcohols in an amount of from 0.5 to 2 % oy weight;

(b) an emulsifying system mainly comprising (b,i) mono- and/or diglycerides of higher unsaturated and saturated fatty acids, in an amount of from 0.5 to 3 % by weight,

5 (b,ii) ethoxylated triglycerides according to the general formula of claim 1 wherein n, m and p are the same or different and each has a value from 7 to 15, and R is defined as in claim 1,

0 whereby the weight ratio between the amount of mono-, and/or diglycerides and of the ethoxylated triglycerides is in the range of from 15 to 50 parts by weight of mono- and/or diglycerides per part by weight of ethoxylated triglycerides, whereas the i amount of the complete emulsifying system, relative to the weight of the complete composition, is in the range of from 2 to 3.5 % by weight;

(c) vitamin E in an amount of from 1 to 3 % by weight, 0 relative to the weight of the complete composition;

d) L-methionine in an amount of from 1 to 2 % by weight;

(e) a pH regulating system to adjust the pH of the 5 aqueous system to be in the range of from 4.5 to 4.9, comprising citric acid, zinc carbonate and sodium hydroxide in amounts of 0.5 to 2 % by weight, from 0.5 to 1 % by weight and 0.05 to 0.2 % by weight, respectively; 0

(f) the stabilizer in an amount of from 0.5 to 0.7 % by weight;

(g) water ad 100 % by weight. c 3. Composition according to claims 1 or 2, comprising additionally:

(h) at least one preservative in an amount of from 0.1 to 1 % by weight, preferably from 0.5 to 0.7 % by weight, relative to the weight of the complete composition;

(i) glycerol in an amount of from 1 to 4 % by weight, preferably from 1 to 3 % by weight, relative to the weight of the complete composition;

(j) a gel forming agent in an amount of from 0.1 to 5 % by weight, preferably from 0.5 to 2 % by weight, relative to the weight of the complete composition;

(k) perfume in an amount of from 0.1 to 2 % by weight, relative to the weight of the complete composition;

(1) at least one protein, obtainable from aqueous extraction of plants, such as aloe vera, in an amount of from 0.1 to 0.5 % by weight, preferably from 0.1 to 0.

3 % by weight, relative to the weight of the complete composition.

4. Process for the preparation of a composition according to any of claims 1 to 3, characterized by the preparation in one or more steps of the complete continuous oily phase, composed of the oil fraction, the optional esters of fatty acids and alcohols, the emulsifying system, the stabilizer, vitamin E or a derivative thereof, the perfume and the optional preservative, and by the preparation in one or more steps of at least one dispersed aqueous phase composed of demineralized water, citric acid or a citrate, zinc carbonate and sodium or potassium hydroxide, methionine, glycerol, gel forming agent, protein, and preservative, and by mixing together both phases at a temperature in the range of from 10 to 40°C, followed by additional stirring and homogenizing until an average particle size of the dispersed aqueous phase of at most 5 μ, and preferably smaller than 3 μ, is reached, while the pH of the final complete composition is adjusted within the range of from 4.8 to 5.1.

Process according to claim 4, characterized in that

in a first step the oil fraction, the optional esters of fatty acids and alcohols, the emulsifying system and the stabilizer are mixed and homogenized at a temperature from 60 to 90°C, whereafter the homogeneous mixture is cooled back to a temperature of at most 30°C,

whereafter the cooled mixture is mixed in a second step with vitamin E or a derivative thereof which can easily be transformed into said vitamin, and with the perfume until a homogeneous mixture is obtained;

and that the aqueous phase is prepared by subsequent addition of demineralized water in an amount of about one third of the total amount in the final composition, of citric acid, of zinc carbonate and of sodium or potassium hydroxide under gently stirring until complete dissolution, whereafter, if necessary, the pH of the homogeneous solution is adjusted to the range of from 4.6 to 4.8 by addition of sodium or potassium hydroxide or citric acid, and the remainder of the desired total amount of water, methionine, glycerol, carreghenate, preservative and protein are added to the aqueous solution, whereafter the pH is again adjusted to the range of from 4.6 to 4.8, and that the finally obtained aqueous solution is added to the oily phase under stirring vigorously and subsequent homogenizing at a temperature in the range of from 10 to 40°C, preferably from 20 to 30°C, whereafter the pH of the complete dispersion, having dispersed aqueous phase particles of an average size of at most 5 μ is in the range of from 4.9 to 5.1.

6. Use of a composition according to any of claims 1 to 3, comprising the application and evenly spreading on chapped, sore and/or inflamed lips, nose opening edges, eyelids and the like, of said composition in an amount of from 20 to 100 ml/m² skin area.