MEDICAMENT POUR APPLICATION EXTERNE ET UTILISATION D'UNE EMULSION HUILE DANS EAU POUR LEDIT MEDICAMENT

REMEDY FOR EXTERNAL APPLICATION, AND USE OF AN OIL-IN-WATER EMULSION FOR SAID REMEDY

Abrégé français

Ce médicament pour application externe, s'utilisant en particulier contre les maladies de la peau, contient une émulsion huile dans eau, dans laquelle se trouvent des minéraux à grains si fins qu'ils peuvent passer à travers les pores de la peau humaine.

Abrégé anglais

The invention relates to a remedy for external application, in particular to
prevent skin diseases. Said remedy has an oil-in-water
emulsion in which minerals are provided, the grain size thereof being so small
that the minerals can pass through the skin pores of human
skin.

Revendications

12
CLAIMS
1. Remedy for external application, characterized in that it comprises the
following constituents
- an oil-in-water emulsion,.and
- grained minerals which are present in ~rhe emulsion, the grain size thereof
being so small that the minerals can pass through the skin pores of human
skin.
2. Remedy according to claim 1, characterized in that the emulsion comprises
a stabilizer.
3. Remedy according to claim 2, characterized in that the stabilizer is
carboxymethylcellulose.
4. Remedy according to of claim 3, characterized in that
carboxymethylcellulose is present in a range of 0.025 to 0.75% by weight.
5. Remedy according to any one of clairns 1 to 4, characterized in that the
emulsion also comprises an antiseptic.
6. Remedy according to claim 5, characterized in that the antiseptic is tea
tree
oil.
7. Remedy according to any one of claims 5 and 6, characterized in that the
antiseptic is present in an amount between 0.001 to 1 % by weight.
8. Remedy according to any one of claims 1 to 7, characterized in that the
emulsion also comprises a surface-active agent.
9. Remedy according to claim 8, characterized in that the surface-active agent
is an anionic 15-30% surface-active agE:nt.

13
10. Remedy according to any one of claims 8 and 9, characterized in that the
surface-active agent is present in an amount between 0.0001 to 1 % by
weight.
11. Remedy according to any one of claims 1 to 10, characterized in that the
emulsion further comprises glycerine.
12. Remedy according to claim 11, characterized in that the glycerine is added
in an amount between 0.001 to 50% by weight.
13. Remedy according to any one of claims 1 to 12, characterized in that the
emulsion also comprises a fat-restoring skin milk.
14. Remedy according to claim 13, characterized in that the fat-restoring skin
milk is added in a weight range of 0.001 to 30% by weight.
15. Remedy according to any one of claims 1 to 14, characterized in that the
oil-
in-water emulsion is a mineral oil-in-water emulsion.
16. Remedy according to any one of claims 1 to 15, characterized in that the
oil-
in-water emulsion is a polydialkylsiloxane-in-water emulsion.
17. Remedy according to any one of claims 1 to 16, characterized in that the
grained minerals are amorphous pyrogenic silicic acid dissolved in oil and
emulsified in water with mineral ingredients.
18. Remedy according to claim 17, characfiarized in that the mineral
ingredients
are silicon, calcium and/or magnesium.
19. Remedy according to any one of claims 1 to 18, characterized in that it is
atomized.

14
20. Remedy according to claim 19, characterized in that, to be atomized, the
emulsion contains 0.2 - 1% by weight of mineral solution in oil, the rest is
water.
21. Use of the remedy as defined in any one of claims 1 to 20 for external
application.
22. Use of the remedy according to claim 21 wherein the external application
is
for the treatment of skin diseases.
23. Use of the remedy according to any one of claims 21 and 22, characterized
in that the remedy is applied by an atomizer.

Description

CA 02285012 1999-09-22
1
REMEDY FOR EXTERNAL APPLICATION, AND USE OF AN OIL-IN-WATER
EMULSION FOR SAID REMEDY
The present invention relates to a remedy for external
application, in particular for the treatment of skin
diseases, and to the use of an oil emulsion for producing
such a remedy.
A lot of remedies used to cure or relieve skin diseases
such as neurodermatitis (scabies), psoriasis (psora), acne,
dandruff, itchiness, herpes, shingles, burn wounds, scab,
sunburn and phlebalgia in the legs are well known in the
art. Not all bring satisfactory results. There is a need
for further remedies in this field.
Skin diseases like the above-mentioned are getting more
frequent. This is probably due to lots of environmental
influences and to modified environmental conditions. Skin
diseases are typically involving very troublesome accessory
symptoms. Itchiness occurs, which is often unbearable. The
disease is often aggravated or other problems occur due to
the fact that the smitten parts are too much rubbed or
scratched.
This is where the invention comes to bear. Its object is to
provide a remedy for external application, in particular
for the treatment of skin diseases, with the help of which
the clinical picture of the disease heals up soon and which
is easy to use.

i ~ ~ i
CA 02285012 2005-03-03
2
The solution of this object is to provide, on the basis of a remedy of the
type
mentioned above, an oil-in-water emulsion in which grained minerals are
provided, the grain size thereof being so small that the minerals can pass
through the skin pores of human skin, in particular amorphous, pyrogenic
silicic
acid dissolved in oil and emulsified in water with mineral ingredients like
silicon,
calcium and/or magnesium. The oil-in-water emulsion is preferably polydialkyl-
siloxane-in-water emulsion.
The decisive ingredients are the minerals contained in the
aqueous oil emulsion where they are extremely finely
dispersed. They are dispersed =so finely that their grain
size is smaller than the pore d__ameter of human skin. Thus
even the tiniest minerals may penetrate the skin. The
minerals are so tiny that they are not staying on the
surface where they would be filtered, but are absorbed by
the skin. Thus, the diseased skin gets the minerals it is
lacking.
The oil which proved most effecaive is a mineral oil. In
the mineral and oil emulsion, minerals like silicon,
calcium and traces of magnesium are extremely finely
dispersed. The emulsion is not ionogenic. The pH-value is
neutral with 5 to 7. Particular vreferred results have been
obtained when these minerals are present in an amount of
less than to by weight, prefer;~bly of less than O,lo by
weight of the emulsion. Other mi:zerals may also be present,
e.g. those belonging to the alaali and/or alkaline earth
group. The minerals are not dissolved. They are finely
dispersed.
It proved particularly preferable to add an emulsifier to the basic topical
composition. Commercial emulsifiers are used.

CA 02285012 2005-03-03
3
It proved particularly preferable to add a stabilizer to the basic topical
composition. Commercial stabilizers are used, such as for example
carboxymethylcellulose preferably used in an amount of from 0.025 to 0.75% by
weight of the total composition.
It also proved advantageous to add an anti;;eptic to the emulsion. Tea tree
oil is
particularly appropriate. On top of its antiseptic property, the composition
of tea
tree oil also soothes the skin and relieves itchiness. The antiseptic is
preferably
used in an amount of from 0.001 to 1 % by weight of the total composition.
It further proved advantageous to add a surface-active agent, in particular an
anionic surface-active agent 15 to 30%. ~~urface-active agents clean the skin
and act as emulsifiers. The surface-active agent is preferably used in an
amount
of from 0.0001 to 1 % by weight of the total composition.
It proved particularly advantageous to add glycerin to the emulsion. Glycerin
is
known as a moisture binding material for the skin. It also acts as an
emollient.
The glycerin is preferably used in an amount of from 0.001 to 50% by weight of
the total composition.
In order to confer a fat-restoring property on the remedy, a fat-restoring
additive
is added in cases in which restoring fat is desired, thus not for acne for
example.
Here, commercial compositions of skin milks for dry skin may be used. The fat-
restoring additive particularly contains oils, paraffins, stearates and so on.
The
fat-restoring skin milk is preferably used in an amount of from 0.001 to 30%
by
weight of the total composition.
Finally, the invention relates to the use of an oil-in-water emulsion
containing
finest grained minerals for producing a remedy for external application, in
particular to prevent skin diseases. In a preferred embodiment, the remedy is
so
fluid that it may be used in atomizers and sprayed on the skin. For being
atomized, the emulsion is preferably coni:aining 0.2-1 % by weight of mineral
solution in oil, the rest being water.

CA 02285012 1999-09-22
4
Tea tree oil exists in technical and pharmaceutical grades.
Both have the same effect in the remedy according to the
invention. The pharmaceutical embodiment has the advantage
to smell a little bit better.
The ingredients of 200 grams tea tree oil are typically the
following:
terpinene-4-oil 70 g
~-terpin oil 14 g
O-terpinene 46 g
~-terpinene 20 g
sigma cymene 20 g
1,8 cineole 20 g
~G-pinene 7 g
~-terpinolene 7 g
d-limonene 6 g
The remedy assists the body in self-healing. The tissue on
which the remedy was sprayed gets warm, since blood
circulation is much improved in this area. This also
contributes to heal and relieve. This is an advantage
constituting a particularity of the remedy according to the
invention. The increased blood circulation explains the
effect the remedy according to the invention has on for
example the treatment of phlebalgia.
E x a m p 1 a s
Example l:
An acne treating composition has the following ingredients:

CA 02285012 1999-09-22
5,000 g Demineralized Water
500 g Mineral Solution, emulsified in oil
200 g Tea Tree Oil
g Anionic surface-active agents 15 - 300
500 g Glycerin.
When applied on the skin, particularly when sprayed on it,
acne is healing in two stages. The already existing comedos
first dry up. Then, the skin effloresces and looks like
measles with lots of red spots. This occurs because the
10 hidden sebaceous follicles, which are not yet inflamed, are
brought to the surface of the skin. After that, the skin
becomes smooth.
Example 2:
For the production of a remedy for the treatment of
phlebalgia:
5,000 g Demineralized water
1,000 g Mineral Solution, emulsified in oil
100 g Tea Tree Oil
10 g Anionic Surface-Active Agents
1,000 g Glycerin.
After undergoing surgery on veins, the patient often
suffers from burning pain in the legs. By spraying the
fluid onto the legs, the pain vanishes. One treatment a day
is enough to remain free from pain.
Example 3:
Remedy for the treatment of neurodermatitis:

CA 02285012 1999-09-22
6
5,000 g Demineralized water
500 g Mineral Solution, emulsified in oil
200 g Tea Tree Oil
g Anionic Surface-Active Agents 15 - 300
500 g Glycerin
500 g Skin Milk for dry skin made of water, octyl
stearate, paraffin oil, castor oil, sorbitan oleate,
dimethicon tocopheryl acetate, heliotropins,
phenoxyethanol, magnesium sulphate, zinc sulphate.
The unbearable itchiness accompanying neurodermatitis eases
nearly immediately upon applying the remedy. Rubbing and
scratching as well as the constant aggravation of the
clinical picture they are causing are thus avoided. The
diseased skin parts heal very fast, actually within a few
days. The diseased, keratinized skin peels off like after
severe sunburn. It may also desquamate. The skin appearing
underneath is thin and red but normalizes very soon. It is
no longer smitten.
Example 4:
For the production of the remedy according to the
invention, formulas formulated within the following ranges
proved to be advantageous:
5,000 g Water
50-5,000 g Mineral Solution, emulsified in oil
10-2,000 g Tea Tree Oil
1-100 g Anionic Surface-Active Agents and
1-3,000 g Glycerin.

CA 02285012 1999-09-22
7
Preferred amounts of the fat-restoring additive in the
composition mentioned in Example 3are between 10 and
2, 000 g.
Example 5:
Novoskin/Dermac Amount
Water 7go
Glycerin 85% 80
Silicon sediments
Silica 2,450
Methyl Cellulose 0,050
Water 2,5%
Calcium sediments
Calcium Carbonate 0,74s
Methyl Cellulose 0,02a
Water 1,24%
Castor Oil 20
Malaleuca Oil 20
Dexpanthenol 10
Magnesium sediments
Magnesium Carbonate 0,2%
Methyl Cellulose 0,01%
Water 0,79%
Avocado Oil to
Ingredient Amount Function Standard
Water 78o Vehicle normal
Glycerin 850 8% Emollient Ph. Eur.
Purified Water 4,530 Vehicle Ph. Eur.
Colloidal Silica Anhydride 2,450 Cleanser Ph. Eur.

CA 02285012 1999-09-22
8
Castor Oil 2% Stiffener U.S.N.F.
Malaleuca Oil 2o Fragrance normal
Dexpanthenol 1o Provitamin Ph. Eur.
Avocado Oil to Fragrance normal
Potassium Carbonate 0,74% Cleanser Ph. Eur.
Magnesium Carbonate 0,2% Cleanser Ph. Eur.
Methyl Cellulose 0, 08 o Suspending
Agent Ph.
Eur.
Example 6:
Novoskin forte
Water 700
Silicon sediments
Silica 4,9%
Methyl Cellulose O,lo
Water 5%
Glycerin 850 80
Calcium sediments
Calcium Carbonate 1,480
Methyl Cellulose 0,040
Water 2,48%
Magnesium sediments
Magnesium Carbonate 0,40
Methyl Cellulose 0,02a
Water 1,58%
Castor Oil 2%
Malaleuca Oil 2%
Dexpanthenol 1s
Avocado Oil to

CA 02285012 1999-09-22
9
Ingredient Amount Function Standard
Water 70o Vehicle normal
Purified Water 9,06 Vehicle Ph. Eur.
o
Glycerin 85% 8% Emollient Ph. Eur.
Colloidal Silica Anhydride 4,9% Cleanser Ph. Eur.
Castor Oil 2s Stiffener U.S.N.F.
Malaleuca Oil 2% Fragrance normal
Potassium Carbonate 1,48% Cleanser Ph. Eur.
Dexpanthenol to Provitamin Ph. Eur.
Avocado Oil to Fragrance normal
Magnesium Carbonate 0,4s Cleanser Ph. Eur.
Methyl Cellulose 0,16% Suspending
Agent Ph.
Eur.
Example 7:
Novoskin mild
Water 80 0
Glycerin 850 80
Silicon sediments
Silica 2,45s
Methyl Cellulose 0,050
Water 2,50
Calcium sediments
Calcium Carbonate 0,740
Methyl Cellulose 0,02%
Water 1,24%
Castor Oil 20
Dexpanthenol to
Magnesium sediments
Magnesium Carbonate 0,20
Methyl Cellulose O,Olo
Water 1,79%

CA 02285012 1999-09-22
Avocado Oil 1~
Ingredient Amount Function Standard
Water 80o Vehicle normal
Glycerin 85% 8o Emollient Ph. Eur.
Purified Water 4,53% Vehicle Ph. Eur.
Colloidal Silica Anhydride 2,45% Cleanser Ph. Eur.
Castor Oil 2o Stiffener U.S.N.F.
10 Dexpanthenol 1o Provitamin Ph. Eur.
Avocado Oil 1% Fragrance normal
Potassium Carbonate 0,740 Cleanser Ph. Eur.
Magnesium Carbonate 0,2o Cleanser Ph. Eur.
Methyl Cellulose 0,080 Suspending
Agent Ph.
Eur.
The water used may be distilled water or water containing
the following ingredients:
Sodium 5,4 mg/1 or ppm
Potassium 1,1 mg/1 or ppm
Magnesium 24,6 mg/1 or ppm
Calcium 49,8 mg/1 or ppm
Chlorides 11,4 mg/1 or ppm
Sulphate 7,1 mg/1 or ppm
Hydrogen Carbonate 253,0 mg/1 or ppm
Example 8:
Composition of the oil emulsion with minerals

CA 02285012 1999-09-22
11
38 % solids, final size of grain of the minerals in the
range between 1 and 100 nanometres, preferably between 1
and 10 nanometres.
- = Quartz Powder, initial size 5 micrometres
30 20%
5 30 14% DolomiteBrick Powder, initial size 2 micrometres
- =
1 10 = Magnesium Powder approximately 3 micrometres
- 3%
O1 5 = Methyl Cellulose
- 1%
10 60 = Castor Oil, Pharmagrad
- 38%
2 40 = Water
- 22%
10 This blend is first kneaded intensively in a kneading
machine at a temperature of approximately 50°C. Then, it is
brought - inline - to a colloid mill. The colloid mill has
a cross gearing with a device for pumping aver and rotor
cooling. In a slow passage, the minerals are ground to the
size of 10-9 m. The castor oil emulsifies in the warm water
and is stabilized by methyl cellulose. In order to avoid
overheating during grinding, it is necessary to cool the
grinding body. The thus obtained mineral and oil emulsion
is stable and may be further diluted with water and
blended.