U.S. patent application number 13/328186 was filed with the patent office on 2012-04-12 for self-adhesive skin patch and combination set for cosmetic skin care.
This patent application is currently assigned to BEIERSDORF AG. Invention is credited to Stefan BODENSCHATZ, Christian GAEDE, Carsten HARTKOPF, Soeren JASPERS, Katharina POST, Jens SCHULZ, Karl-Heinz WOELLER.
Application Number | 20120089105 13/328186 |
Document ID | / |
Family ID | 36636337 |
Filed Date | 2012-04-12 |
United States Patent
Application |
20120089105 |
Kind Code |
A1 |
JASPERS; Soeren ; et
al. |
April 12, 2012 |
SELF-ADHESIVE SKIN PATCH AND COMBINATION SET FOR COSMETIC SKIN
CARE
Abstract
The present invention relates to a skin patch comprising a
matrix adhering to the skin and containing at least one active
cosmetic substance and a combination with a skin wrapping to
generate an effective compression for the treatment of cellulite
and/or striae.
Inventors: |
JASPERS; Soeren;
(Schenefeld, DE) ; HARTKOPF; Carsten; (Hamburg,
DE) ; GAEDE; Christian; (Neu Wulmstorf, DE) ;
BODENSCHATZ; Stefan; (Buxtehude, DE) ; POST;
Katharina; (The Hague, NL) ; SCHULZ; Jens;
(Schenefeld, DE) ; WOELLER; Karl-Heinz; (Hamburg,
DE) |
Assignee: |
BEIERSDORF AG
Hamburg
DE
|
Family ID: |
36636337 |
Appl. No.: |
13/328186 |
Filed: |
December 16, 2011 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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11547098 |
Jan 10, 2007 |
8101216 |
|
|
PCT/EP2006/061137 |
Mar 29, 2006 |
|
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13328186 |
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Current U.S.
Class: |
604/307 ;
424/729; 514/263.34; 514/556 |
Current CPC
Class: |
A61K 8/0208 20130101;
A61P 17/00 20180101; A61F 2013/00902 20130101; A61F 13/08 20130101;
A61F 13/0213 20130101; A61Q 19/06 20130101; A61K 8/8147 20130101;
A61K 8/90 20130101; A61F 13/0209 20130101; A61K 8/4953 20130101;
A61F 13/0223 20130101; A61K 8/44 20130101; A61K 8/42 20130101; A61Q
19/00 20130101 |
Class at
Publication: |
604/307 ;
514/556; 424/729; 514/263.34 |
International
Class: |
A61F 13/02 20060101
A61F013/02; A61Q 19/00 20060101 A61Q019/00; A61K 8/81 20060101
A61K008/81; A61K 8/92 20060101 A61K008/92; A61K 8/97 20060101
A61K008/97; A61K 8/72 20060101 A61K008/72 |
Foreign Application Data
Date |
Code |
Application Number |
May 13, 2005 |
DE |
102005023149.7 |
Nov 11, 2005 |
DE |
102005053909.2 |
Claims
1. A skin patch, wherein the skin patch comprises a matrix which is
capable of adhering to human skin and comprises at least one
polymer and one or more active cosmetic substances which comprise
carnitine, and wherein the skin patch is capable of exerting a
pressure on skin, which pressure is up to 10 mm Hg.
2. The skin patch of claim 1, wherein the pressure is at least 4 mm
Hg.
3. The skin patch of claim 1, wherein the at least one polymer gels
in water.
4. The skin patch of claim 3, wherein the at least one polymer
comprises a polymer of at least one of acrylic acid and a salt
thereof.
5. The skin patch of claim 4, wherein the at least one polymer
comprises a polymer of sodium acrylate and acrylic acid.
6. The skin patch of claim 1, wherein the skin patch comprises from
0.01% to 10% by weight of carnitine, based on a total weight of the
matrix.
7. The skin patch of claim 6, wherein the skin patch comprises from
0.1% to 1% by weight of carnitine.
8. The skin patch of claim 1, wherein the skin patch comprises at
least one further active cosmetic substance.
9. The skin patch of claim 8, wherein the at least one further
active cosmetic substance comprises white tea extract.
10. The skin patch of claim 1, wherein the skin patch further
comprises caffeine.
11. The skin patch of claim 1, wherein the skin patch further
comprises capsaicin.
12. The skin patch of claim 4, wherein the matrix comprises from 2%
to 55% by weight of the polymer of at least one of acrylic acid and
a salt thereof.
13. The skin patch of claim 5, wherein the matrix comprises from 5%
to 30% by weight of the polymer of sodium acrylate and acrylic
acid.
14. The skin patch of claim 1, wherein the skin patch comprises a
polymer of sodium acrylate and acrylic acid, carnitine, water,
sodium carboxymethylcellulose, dihydroxyaluminum aminoacetate,
hydroxypropylcellulose, glycerol, disodium edetate, kaolin, methyl
para-hydroxybenzoate, propylene glycol and castor oil.
15. The skin patch of claim 1, wherein the matrix exhibits an
adhesion time value of higher than 5.
16. A skin patch, wherein the skin patch comprises a matrix which
is capable of adhering to human skin and comprises at least one
polymer and one or more active cosmetic substances, the one or more
active substances comprising from 0.1% to 1% by weight of
carnitine, based on a total weight of the matrix, and the at least
one polymer comprising a polymer of at least one of acrylic acid
and a salt thereof, and wherein the skin patch is capable of
exerting a pressure on skin, which pressure is from 4 mm Hg to 7 mm
Hg.
17. The skin patch of claim 16, wherein the at least one polymer
comprises a polymer of sodium acrylate and acrylic acid.
18. The skin patch of claim 17, wherein the matrix comprises from
5% to 30% by weight of the polymer of sodium acrylate and acrylic
acid.
19. The skin patch of claim 17, wherein the patch exhibits an
adhesion time value of higher than 5.
20. A kit comprising the skin patch of claim 1 and a gas and vapor
permeable skin wrapping.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] The present application is a continuation of U.S. patent
application Ser. No. 11/547,098, which is a National Stage of PCT
Application No. PCT/EP2006/061137, filed Mar. 29, 2006. The entire
disclosure of the parent application is expressly incorporated by
reference herein.
[0002] The present invention relates to a skin patch comprising a
matrix which adheres to the skin and contains at least one active
cosmetic substance and a combination with a skin wrap to produce an
effective compression for treating cellulite and/or stretch marks
of the skin, such as, e.g., striae.
[0003] Cellulite (medical term: dermopanniculosis) is not a
disease, but a cosmetic problem.
[0004] The reasons for cellulite lie above all in the special
structure of female skin and in the reaction to female hormones.
Fat cells are stored in the hypodermis. Their quantity is already
determined in infancy and cannot be influenced by diet or sport.
The fatty acids from diet are converted into fats in the fat cells
and are stored in the connective tissue in a nodular manner. If
these fats are not broken down for a long period (e.g., sport) and
if the body in addition is overfed, the cells can expand by a
multiple of their size. The enlarged cells then push through the
connective tissue and the feared orange peel skin occurs, also
known as cellulite.
[0005] The further consequences in old age are small varicose
dilatations of the cutaneous veins, varicose veins, thrombosis and
leg complaints. The thighs often also store superfluous fat that is
absorbed through the diet. The unsightly thickening at the sides of
the thighs, also known as saddle bags, combined with cellulite, is
often a great strain on those affected.
[0006] The so-called body wrap principle is known for treating
cellulite. A special body wrap gel is applied to the problem areas
thereby and they are subsequently wrapped in a wrapping foil. A
heat effect is thereby produced and a purification of the tissue
takes place through the active substances of the body wrap gel and
the heat development.
[0007] Through the application of the gel and the wrap shorts, the
lymphatic circulation is to be stimulated and through the heat
generation toxins, fats and wastes are to be removed from the body.
In this manner Striae are also reduced, cellulite is reduced and
the so-called saddle bags are also reduced after only a few
treatments.
[0008] Anti-cellulite plasters (e.g., "Perfect Slim Cellulite
Patch" from L'Oreal) are also known, the components of which, such
as seaweed or caffeine, promote the smoothing of the unsightly
dimples. The beauty plasters in particular make the application
easier for women who are tired of having to apply cream all the
time. Thus areas particularly affected can be treated in a targeted
manner. The advantage of a patch of this type lies in the
continuous dispensing of active substances over eight hours by the
plaster. Moreover, these can also be used at night.
[0009] The preparation CREALITE by Creaderm uses nanotechnology
against cellulite for the first time. Caffeine is transported
through the skin into the subcutaneous fatty tissue with
liposomes.
[0010] CREALITE contains large-dose caffeine (2%) in a specially
suitable carrier. Caffeine withdraws water from the cells and in
addition inhibits the enzyme cyclic M3',5'-nucleotide
phosphodiesterase, through which a weight loss is to be achieved.
The fat cells which are very much enlarged with cellulite are to be
made smaller thereby and the skin is to appear tauter and smoother
again.
[0011] WO 05/007127, WO 04/093865, WO 04/074216 and WO 04/060268
likewise highlight numerous cosmetic active substances and
treatment methods for cellulite.
[0012] EP 1181926, EP 728472 and EP 493151 likewise disclose in
particular cosmetics containing caffeine for cellulite
treatment.
[0013] The object of the present invention is to disclose
alternatives for the treatment of cellulite.
[0014] Stretch marks in the skin after pregnancy which impair the
on the aesthetic appearance are an annoying cosmetic phenomenon.
So-called stretch marks are also called striae. This is not a
disease, but a purely cosmetic problem.
[0015] Skin stretch marks (striae) are tears in the subcutaneous
tissue. They occur on the abdomen, hips or breast. Striae are
bluish red at first, then yellowish white. They have a similar
appearance to scars. They occur whenever the skin is overstretched
and at the same time the elasticity of the skin has decreased. A
high cortisone level promotes the formation of stretch marks. This
hormone allows the skin to retain more water and it reduces the
elasticity of the skin.
[0016] If the skin is stretched by a pregnancy or weight gain,
small tears occur in the elastic tissue. The skin becomes thinner
at the affected areas and the blood vessels shine through in a
bluish color. Later the areas form a scar and the marks become
white. Unfortunately, they will not disappear again.
[0017] Pregnant women, people in puberty, competitive athletes,
people undergoing hormone treatment and people with increased
weight are the groups most affected by Striae.
[0018] During pregnancy there is a higher cortisone level in the
blood. Stretch marks occur here in the skin of the abdomen in the
case of many women. They are called "striae gravidarum" or
pregnancy stretch marks.
[0019] Once stretch marks are present, according to the current
standard of knowledge they cannot be completely reduced. A
reduction and abatement up to 50% is possible. It also applies to
laser treatments that they do not usually achieve the desired
success.
[0020] The object of the present invention is therefore also to
provide a skin patch that renders possible a treatment of the skin
areas affected by striae and brings about a cosmetic improvement of
these skin areas.
[0021] The skin is exposed to constantly changing environmental
influences and over time is subject to a number of changes. Thus
changes in the barrier properties, the degree of skin wrinkles and
elasticity, pigmentation and in particular, due to exogenic
influences, also inflammatory reactions and, e.g., also
after-reactions of the skin to the impact of UV radiation
result.
[0022] The barrier effect of the skin can be quantified via the
determination of the transepidermal water loss (TEWL). This is the
evaporation of water from the interior of the body without
including the loss of water during sweating. The determination of
the TEWL value has proven to be extraordinarily informative and can
be used for the diagnosis of cracked or chapped skin, to determine
the tolerance of surfactants with different chemical structures and
the like.
[0023] The proportion of water in the top dermal layer is very
important for the beauty and well-groomed appearance of the skin.
It can be favorably influenced to a limited extent by introducing
moisture regulators.
[0024] Cosmetic skin care means primarily strengthening or
rebuilding the natural function of the skin as a barrier against
environmental influences, e.g., dirt, chemicals, microorganisms,
and against the loss of endogenous substances, e.g., water, natural
fats, electrolytes.
[0025] If this function is impaired, an intensified absorption of
toxic or allergenic substances or an attack by microorganisms
leading to toxic or allergic skin reactions can occur.
[0026] The aim of skin care is furthermore to compensate for the
loss by the skin of lipids and water caused by daily washing. This
is particularly important if the natural regenerative ability is
insufficient. Moreover, skin care products should protect against
environmental influences, in particular sun and wind, and delay
skin aging.
[0027] Chronological skin aging is caused, e.g., by endogenous,
genetically determined factors. The following structural damage and
functional disorders, which can also come under the term "senile
xerosis", can occur, e.g., in the epidermis and the dermis due to
aging:
(a) dryness, roughness and the formation of small lines due to
dryness, (b) itching and (c) reduced regreasing by sebaceous glands
(e.g., after washing).
[0028] Exogenous factors, such as UV light and chemical noxae, can
have a cumulative effect. In the epidermis and dermis, in
particular due to exogenic factors, e.g., the following structural
damage and functional disorders occur in the skin:
(d) increased susceptibility to mechanical stress (e.g.,
cracking).
[0029] Products for the care of sensitive, itchy or dry skin or
products for the treatment or prophylaxis of DNS damage are known
per se. However, their effectiveness is limited.
[0030] It is therefore the object of the present invention to
provide in particular cosmetic skin patches that offer an
additional effective protection from harmful oxidation processes in
the skin as well as offering additional protection from or helping
to reduce dryness, roughness and the formation of wrinkles due to
dryness, itching, reduced regreasing by sebaceous glands, e.g.,
after washing, and increased susceptibility to mechanical stress,
e.g., cracking.
[0031] Preparations are known in the prior art which, applied to
the skin or the mucous membranes, are to have a moisturizing and
cooling effect. In the literature for example ionic compounds, in
particular ammonium salts, are described as cooling agents.
Isopropanol gels with added camphor and menthol are also widely
used as cooling preparations, and essential oils, primarily camphor
and menthol, but also derivatives thereof, e.g., menthyl lactate or
menthyl-3-hydroxybutyrate, are generally frequently incorporated
into cooling compositions.
[0032] Menthol, camphor and derivatives thereof, as well as other
essential oils, lower the stimulus threshold of neuronal cold
receptors and thus produce a cold sensation. However, they often
cause an increase in blood supply at the same time, which in
contrast generates a sensation of heat. The application of these
substances, especially on irritated skin, is at any rate
problematic. Moreover, many of these compounds have poor water
solubility. Their use is consequently limited to a few cosmetics
and dermatics.
[0033] The object of the present invention is therefore also to
provide a skin patch that does not have the listed disadvantages or
has a reduced level thereof while moisturizing, cooling and/or
increasing blood supply.
[0034] In the case of plaster systems that contain active
substances and remain on the skin for a long time, a main focus is
naturally on the skin tolerance of the adhesive matrix. It is
expected to be not irritating to the skin, to have good adhesion,
in particular over a longer application period, and to guarantee a
painless removal of the plaster or pad without leaving a residue.
This expectation is not met by many known adhesive substances, such
as rubber, silicone, resins or styrene hydrocarbons, which are used
in particular to improve the adhesive properties. These known
adhesive substances often lead to the occurrence of skin
irritations, allergies, macerations and/or a painful removal of the
plaster from the skin.
[0035] The therapeutic mechanism of plasters or cosmetic matrices
for administering cosmetic substances into and onto the skin are
subject to an analogous functional principle such as Transdermal
Therapeutic Systems (TTS). The terms plaster,
cosmetic/dermatological matrices and cosmetic/dermatological pads
are used synonymously below.
[0036] Transdermal Therapeutic Systems for dispensing active
substances into or through the skin have been known for a long time
and represent plaster-type systems, in particular delivering
medicinal agents
[0037] The topical application of cosmetic and dermatological
active substances via plaster systems or cosmetic matrices offers
two main advantages: [0038] firstly, this form of administration
produces first-order release kinetics of the active substance,
thereby allowing a constant level of the active substance to be
maintained in the skin over a long period of time. [0039] secondly,
an additional intensive care of the skin can be effected via
suitable systems.
[0040] The time-dependent release of the cosmetic active substance
from a TTS occurs depending on its TTS/skin distribution
coefficient and its diffusion in the region of the TTS and the
skin.
[0041] Both factors are determined by the composition of the
matrix, thereby allowing the amount released per time unit and the
duration of effectiveness to be directly influenced. Usually
hydrocolloids, solubilizers and enhancers are used, allowing an
improved solubility and diffusion as well as a faster transfer of
the substance from TTS into the skin.
[0042] Ideally, first-order release kinetics are achieved, allowing
the release of equal quantities per time unit.
[0043] One embodiment of transdermal systems of this type which has
been well described in the technical literature is that of matrix
systems or monolithic systems in which the active cosmetic agent is
incorporated directly into the pressure-sensitive adhesive. In the
ready-to-apply product a pressure-sensitive adhesive matrix of this
kind, comprising the active substance, is equipped on one side with
a backing, which is impermeable for the active substance, while on
the opposite side there is a backing film equipped with a release
layer, which is removed prior to application to the skin
(kleben&dichten, No. 42, 1992, pp. 26 to 30).
[0044] The aforementioned properties of a TTS avoid the need for
frequently repeated application and avoid burdening the skin with
high concentrations of active substances, and so reduce irritation
to the skin, which is unavoidable in the event of repeated
administration of liquid and semisolid administration forms.
[0045] In summary, the advantages of the TTS lie in a distinctly
improved compliance on the part of users, which is attributable to
the simple and rapid administration and to the long-lasting
efficacy of transdermal therapeutic systems.
[0046] One basic requirement of a TTS is effective adhesion to
skin, which must be maintained over the entire period of the
intended dosing of the active substance, and another is the ability
for the TTS to be removed without leaving any residue. Painful
redetachment of the active substance patch after a prolonged period
of wear is a frequent observation. Apart from adhesives which are
coated in solution onto the backing, the adhesives used also
include solvent-free systems, such as hot-melt adhesives. A feature
of these adhesives is that in the course of their coating it is
possible to forego the use of organic solvent and dispersion media.
Hot-melt adhesives are converted to a liquid form by heating and
are applied thus as a melt to the respective patch backing. Apart
from technical aspects, such as solvent processing, plant design
with anti-explosion measures, and environmental protection
strictures, medical reasons also play a part in the choice of
solvent-free adhesives. Transdermal therapeutic systems are
generally applied to healthy, intact skin.
[0047] Self-adhesive matrix systems for administering active
cosmetic substances are among traditional applications in Asia,
particularly in Japan, and are defined in the Japanese
pharmacopoeia under the term "cataplasm." Cataplasms, accordingly,
are commonly prepared by mixing glycerin, water or other suitable
liquids with finely pulverized active substances, with the addition
of essential oils.
[0048] Glycerin functions here as a humectant, in order to prevent
the cataplasms from drying out prematurely in use.
[0049] Whereas in the traditional Asian preparations natural
thickeners such as alumina, etc., are employed, recent decades have
seen the use, more and more, of modern synthetic raw materials,
such as polyacrylic acid as a gel former, for example, for their
production. This allows the cataplasms, which are commonly pasty,
to be produced as hydrogel matrices having improved attractiveness
and user-friendliness. EP 1 136 057 describes an aqueous gel system
for cosmetic use without backing or liner, with a light
transmittance of min. 70%.
[0050] EP 0 507 160 describes cataplasms containing lidocaine.
[0051] A disadvantage of the cataplasms described is that the
production of the base matrices requires many different individual
components such as gel formers, thickeners, plasticizers,
humectants, stabilizers, emulsifiers, pH regulators, antioxidants,
etc., and possibly also solubilizers and penetration enhancers in
the case of active substance cataplasms. Since the adhesive
performance and consistency of such a matrix is a function of the
interaction of all of the individual components, targeted product
development/optimization with regard to these fundamental product
requirements is, correspondingly, time-consuming and difficult.
[0052] The production of polymer matrices, especially gel matrices,
from polyacrylates has likewise been known for many years and is
described for example in EP 0 507 160, JP 11-228340 and JP
04178323. Gel matrices are used, among other things, as an adhesive
base and as an active substance reservoir in transdermal systems.
Such systems have an adequate bond strength, especially to moist
skin (buccal patches), but because of inadequate cohesiveness
cannot be removed again completely when required.
[0053] In order to form a gel with a defined structure it is
necessary for polyacrylic acid to be cross-linked. The nature of
the cross-linker makes a critical contribution to the structure of
the resultant gel. The customary cross-linking agents may be metal
ions (e.g.: Al.sup.3+ ions), or organic compounds. Cross-linking
with aluminum salts proceeds via the coordination of the oxygen
functions of the polyacrylic acid to the Al.sup.3+ ions. A very
close-meshed gel with high viscosity is formed, the viscosity of
the gel being controllable only via the amount of cross-linker
(Handbook of Pressure Sensitive Adhesive Technology, page 458 ff,
1999).
[0054] JP 11-228340 discloses polyacrylic acid-based gels which
utilize Al.sup.3+ compounds as cross-linkers. The use of the
mandatory aluminum compound as a cross-linking agent is limited,
since otherwise the physical properties of the gel are impaired. If
the proportion of aluminum cross-linker is too high the gel becomes
too hard.
[0055] Further examples of cross-linking with polyvalent metal ions
are known from the literature, e.g., U.S. Pat. No. 3,900,610 (zinc
salts), U.S. Pat. No. 3,770,780 or U.S. Pat. No. 3,790,533
(titanium compounds). Ionic cross-linking with metal ions leads to
hard, viscous polymer gels with low tack (Handbook of Pressure
Sensitive Adhesive Technology, page 458 ff, 1999).
[0056] EP 303445 discloses a patch with a monolithic gel matrix
based on water-soluble polymers. Mandatory constituents are
clebopride or a pharmaceutically acceptable salt thereof as active
substance, water, water absorbers, and water-soluble polymers. As
water-soluble polymers one skilled in the art is able to select
from a range of known polymers such as polyvinyl alcohol, gelatin,
polyacrylic acid, sodium polyacrylates, methylcellulose,
carboxymethylcellulose, polyvinylpyrrolidone, rubber and other
cross-linkable polymers and also mixtures thereof.
[0057] EP 976382 describes a patch comprising a matrix composed of
a system which is hydrophilically gelling in aqueous phase and
which is formed from gelan gum and at least one further
hydrocolloid. Gelan gum is claimed mandatorily. Gelan gum is
understood by one skilled in the art, as defined by technical
dictionaries, to comprise hydrocolloids obtained from the following
marine plants: Agardhiella tenera, Furcellaria fastigiata, Hypnea
cervicornis, musciformis, spicifera, Suhria vitata. Nor is there
any mention of the essential aspects of self-adhesive properties,
the adjustability of bond strength and elasticity of the resultant
matrices.
[0058] A further problem associated with the cross-linking of
polyacrylic acid to form a self-adhesive matrix or gel is that a
matrix once produced, having defined physical properties,
viscosity, tack, etc., must have the same defined properties in a
later production process. This reproducibility is difficult if not
impossible to realize with the cross-linking technologies that are
currently known.
[0059] It is also known that the adhesive composition of the
plaster can be employed as the matrix comprising the active
substance. In addition to self-adhesive compositions applied from
solution, hot-melt self-adhesive compositions have also been
proposed for this purpose, as for example in EP 0 663 431 A, EP 0
452, 034 A, EP 0 305 757 A, DE-A 43 10 012, DE-A 42 22 334 and DE-C
42 24 325. The active substances listed in these documents, if
named at all, are systemic ones.
[0060] As examples of active substance plasters, mention may be
made of the active substance plasters which aid the circulation,
belonging to the group of locally active therapeutic systems. The
use of such plasters is indicated for the treatment of rheumatic
complaints, sciatica, lumbago, stiff neck, shoulder/arm pain and
muscular strains and sprains, muscular aching, or muscle, joint and
nerve pain in the region of the locomotor system.
[0061] Capsaicin and nonivamide are known active substances in such
locally acting plasters that aid the circulation. Because of their
use on the locomotor system they are in general required to adhere
strongly. Usually, the plasters are coated over their whole area
with a resin-rubber adhesive composition which comprises the active
substance.
[0062] However, plasters of this kind, which usually have to be
applied over a relatively large area, in some cases exhibit
mechanical skin irritations after removal in the case of sensitive
patients. After a prolonged period of application, their removal is
to some extent painful.
[0063] A further disadvantage of the known thermally active
plasters with an adhesive composition based on natural rubber which
is applied in the form of a solution with organic solvents to the
plaster backing is the comparatively low rate of release of the
active substance.
[0064] The abovementioned disadvantages, and further disadvantages,
apply also to active substance plasters comprising substances other
than those mentioned.
[0065] For example, WO 94/02123 describes an active substance
plaster based on pressure-sensitive hot-melt adhesive compositions
and comprising low-melting and/or readily volatile active
substances in a concentration of from 2.5 to 25% by weight.
[0066] Tapes or wound dressings can be fixed to joints or to the
thigh only unsatisfactorily due to the mechanical stress. A
frequent change of dressing is also customary in order to provide
suitable active substances to the area to be treated on or around
the joint.
[0067] In order to master the problem, plasters with substantial
adhesion, shorts or stocking-like bandages are provided.
[0068] The object of the present invention is therefore also to
provide an improvement in application for the care of the skin with
skin patches. In particular it is an object of the present
invention to provide a cellulite treatment set that is simple to
use, also applicable for individual circumstances, sizes, areas of
skin, and has no disadvantages regarding conventional cellulite
treatments.
[0069] These objects are attained through a skin patch according to
claim 1. Preferred embodiments of the patch are disclosed in the
subordinate claims. Moreover, the invention also covers the use
thereof. Furthermore, the objects are attained through a care set,
comprising a skin patch and a wrapping.
[0070] It was surprising, and extremely astonishing to one skilled
in the art, that a skin patch comprising [0071] a matrix adhering
to human skin, [0072] at least one cosmetic active substance,
whereby the active substance is contained in the matrix, attains
the stated object.
[0073] The skin patch according to the invention encompasses all
cosmetically applicable patches, such as patch, pad, wipes,
plaster, dressings, cataplasm, bandages, masks.
[0074] According to the invention, a cosmetic, not a medicinally
effective active substance, is contained in the adhesive
matrix.
[0075] Polymers, polyisobutylenes or cataplasms which gel in water
are preferred as the self-adhesive matrix. An adhesive mass based
on polyacrylic acid or polyacrylates is particularly preferred.
[0076] The proportion of polymer which gels in water, such as,
e.g., polyacrylic acid gel in the matrix regulates the adhesion. In
particular the matrices disclosed in DE 10260873 and DE 10056010
are herewith an integral part of the present invention.
[0077] Polyacrylates that are advantageous according to the
invention are acrylate-alkyl acrylate copolymers, in particular
those from the group of carbomers or carbopols (Carbopol.RTM. is
actually a registered trademark of B. F. Goodrich Company). In
particular, the acrylate-alkyl acrylate copolymers which are
advantageous according to the invention are characterized by the
following structure:
##STR00001##
where R' is an alkyl radical, in particular a long-chain alkyl
radical, and x and y represent numbers which symbolize the
respective stoichiometric proportion of each of the comonomers.
[0078] According to the invention, particular preference is given
to acrylate copolymers and/or acrylate-alkyl acrylate copolymers
which are available under the trade names Carbopol.RTM. 1382,
Carbopol.RTM. 981 and Carbopol.RTM. 5984 from B. F. Goodrich
Company, preferably polyacrylates from the group of Carbopol grades
980, 981, 1382, 2984, 5984 and particularly preferably Carbomer
2001.
[0079] Also advantageous are copolymers of C.sub.10-30-alkyl
acrylates and one or more monomers of acrylic acid, of methacrylic
acid or esters thereof which are crosslinked with an allyl ether of
sucrose or an allyl ether of pentaerythritol.
[0080] The polymer which forms a gel in water, especially
polyacrylic acid and/or copolymers thereof, is used preferably in
an amount of 2-55% by weight, or preferably between 5-30% by
weight.
[0081] The polymer matrices are produced without the use of organic
solvents, preferably at 40-95.degree. C., in standard commercial
mixers/compounders or, continuously, in suitable extruders.
[0082] A further suitable polymer which forms a gel in water is,
inter alia, baobab flour.
[0083] For example, the combination of polymer which gels in water
(polyacrylic acid), sea algae extract, such as alginates and/or
agar agar, and monohydric or polyhydric alcohol has proven to be
advantageous. In this manner, using water, polymer which gels in
water, sea algae extract and monohydric or polyhydric alcohol as
starting materials, soft, smooth, self-adhesive hydrogel matrices
can be produced in a targeted fashion as a basis for production and
use as plasters, US, cataplasms or cosmetic pad/matrices.
[0084] In order to produce particular performance properties it is
possible for the polymer matrices to be admixed with appropriate
plasticizers, solubilizers, penetration enhancers, neutralizing
agents such as, e.g., tromethamol
(2-amino-2-(hydroxymethyl)-1,3-propanediol), triethanolamine
(2,2',2''-nitrilotriethanol) or NaOH, fillers and/or other known
additives, although it is not mandatory to add them.
[0085] In one embodiment which is particularly preferred in
accordance with the invention, the polymer matrix or gel matrix
contains active dermatological or active cosmetic substances for
controlled local and/or systemic delivery onto/into the skin, in
amounts of in total up to 35% by weight, preferably up to 15% by
weight, in particular up to 2% by weight.
[0086] Since the matrix according to the invention is optionally
also an application form which contains water, a cooling effect is
obtained in addition, this effect already per se being cosmetically
pleasant and contributing to well-being.
[0087] This positive effect can be intensified by the addition of
further care constituents. Besides glycerin it is possible in
particular to add serinol (3-amino-1,2-propanediol) and/or
isoserinol (2-amino-1,3-propanediol) and also urea and PCA
(pyrrolidone-carboxylic acid) as moisturizers. It is of course also
possible to add further substances for this purpose.
[0088] Polyisobutylene PIB is also preferably used as a matrix
system according to the invention.
[0089] In addition to PIB polyisobutylene, hydrophobic base
polymers such as SIS (styrene/isoprene/styrene)-triblock
copolymers, SBS (styrene/butadiene/styrene)-triblock copolymers,
SBR (copolymers of styrene and butadiene), synthetic and/or natural
polyisoprenes, polyamide, polyester, co-polyester, polyurethane
and/or mixtures thereof are also possible as further matrices. From
the multiplicity of known polymer matrices, polyacrylates and
polyisobutylenes are particularly preferred.
[0090] Polyisobutylenes as the matrix base fulfill the requirements
of a self-adhesive, gentle and painlessly detachable polymer matrix
with particular effectiveness, and so it is logical to select the
polyisobutylenes with preference as a matrix base.
[0091] SBR is a generic term for copolymers of styrene and
butadiene, which contain both monomers usually in a weight ratio of
approx. 23.5:76.5, in exceptional cases also 40:60, and the
macromolecules of which predominantly have the structural units I
and II:
##STR00002##
[0092] Water containing matrices according to the invention can be
used in order to provide very dry areas of skin with moisture.
[0093] The polymer matrix according to the invention is thus
extremely well suited as plaster, pad or skin patch for skin care
and in particular for simple cooling purposes and, in addition
equipped to be self-adhesive, easy to use.
[0094] It is also advantageous for the polymer matrix to be free of
solvents to accordingly avoid the disadvantages of the prior
art.
[0095] A preferred active cosmetic substance is carnitine,
3-hydroxy-4-(trimethylammonium)-butyric acid betaine, with the
structure
##STR00003##
[0096] The L form of carnitine is widespread in animal tissue, and
a characteristic component of striated muscle primarily in dark
types of meat. In vegetable foodstuffs, such as fruit, vegetables
and grains, L-carnitine is present in only small amounts (<4
mg/100 g).
[0097] The total amount of L-carnitine in the human body is approx.
20-25 g. 98% of the reserves are stored in the cardiac musculature
and skeletal muscles.
[0098] L-Carnitine serves as a carrier molecule in the transport of
long-chain fatty acids through the mitochondrial membrane into the
mitochondrial matrix chamber, while medium-chain and short-chain
fatty acids can pass through it even without esterification with
L-carnitine.
[0099] L-Carnitine is offered in numerous products as a food
supplement. The target groups are (endurance) athletes and
overweight people, to whom L carnitine is offered to improve
performance or as a slimming aid ("fat burner"). The effectiveness
is very controversial in both cases. Since a lack of L carnitine is
very rare among healthy people, no advantage can be anticipated
from a carnitine supplement. Carnitine is not exhausted in its
biochemical function as a carrier, so that an increase in
conversion in the area of lipometabolism does not lead to an
increased need for carnitine. Conversely, an increased absorption
of carnitine does not lead to an increase of fatty acid oxidation.
An excess of carnitine is eliminated via the kidneys.
[0100] In the case of cardiovascular disease, through an increase
in the .beta.-oxidation of the fatty acids, increased ATP levels, a
reduction in the blood count and tissue fat count (free fatty
acids) and through an increase in the supply of blood to the heart,
L-carnitine can improve the cardiac output and overall increase the
heart's resistance to stress. In addition, a certain
immunostimulation function is ascribed to L-carnitine, which is
attributed to an increase in the activity of the granulocytes, T
lymphocytes and killer cells.
[0101] However, it has surprisingly been proven that a
self-adhesive matrix containing carnitine has a positive effect on
the reduction of cellulite. The lymphocirculation is
stimulated.
[0102] A skin patch according to the invention preferably
containing carnitine is therefore suitable for the care of areas of
the skin affected by cellulite.
[0103] Likewise a skin patch comprising a combination of an
adhesive matrix of polyacrylic acid polymer and the active cosmetic
substance carnitine has proven to be an advantageous treatment
method of the areas of the skin affected by striae.
[0104] It is therefore preferred according to the invention to use
the skin patch comprising polyacrylic acid polymers and carnitine
contained therein for the cosmetic treatment of the areas of the
skin affected by striae.
[0105] Carnitine or derivatives thereof are used in a proportion of
from 0.01 to 10% by weight, preferably from 0.1 to 1% by weight, in
particular 0.5% by weight, based on the total mass of the
matrix.
[0106] Caffeine is preferably to be selected as a further active
cosmetic substance according to the present invention.
[0107] Caffeine or also theine, guaranine, 1,3,7-trimethylxanthine,
methyltheobromine, having the structure
##STR00004##
is found bound to chlorogenic acid in coffee beans (0.8-2.5%), in
dried black tea (up to 5%; this tea caffeine also used to be called
theine).
[0108] Caffeine has a lipolytic effect on the fatty tissue
(increase in the free fatty acids). Furthermore the diuretic effect
of coffee is also known.
[0109] Another preferred active substance within the scope of the
present invention is capsaicin,
(E)-N-(4-hydroxy-3-methoxybenzyl)-8-methyl-6-nonenamide; FEMA 3404,
having the structure
##STR00005##
[0110] Capsaicin as a natural raw material is not usually
understood to be the pure substance, but a mixture of capsaicin
homologs with similar physiological effect, the so-called
capsaicinoids. Thus the monograph of USP 28 describes capsaicin
with a content of at least 55% capsaicin, the total contents of
capsaicin and dihydrocapsaicin of at least 75% and the total
contents of all other capsaicinoids, such as, e.g.,
nordihydrocapsaicin, as no more than 15%.
[0111] The term capsaicin thus can cover all the following homologs
in different composition:
##STR00006##
[0112] According to the invention the capsaicinoids can be
incorporated as a powdery substance mixture as well as in the form
of extracts containing capsaicin of different concentrations. For
example, such extracts can be termed capsicum oleoresin or
extractum capsici (fluidum) but are not limited thereto.
[0113] Likewise according to the invention, the capsaicinoids can
be used in the form of triturations or pulverizations of the fruit
components of the original hot pepper plants, e.g., as so-called
chili powder.
Another homolog of the capsaicin according to the invention is
nonanoic acid vanillylamide, also known as nonivamide for
short.
##STR00007##
[0114] Nonivamide is produced synthetically and accordingly is
called "synthetic capsaicin."
[0115] Even in small amounts, capsaicinoids on the mucous membranes
cause tingling or a sensation of heat. For example, capsaicinoids
are found in the known ABC plasters.
[0116] The term capsaicin used in the following encompasses all the
natural and synethic capsaicinoids in all combinations and
technical forms of application. In this regard, the mass ratios for
capsaicin refer to the absolute amounts of the respective
capsaicinoid/s in the matrix according to the invention, and not to
the content or the amount of the form of the raw material
containing capsaicin.
[0117] In contrast to the active substance cocktail known from the
prior art, which in part are physiologically questionable,
according to the invention only one (carnitine), two
(carnitine--capsaicin, carnitin--caffeine) or three
(carnitine--capsaicin--caffeine) are used.
[0118] Advantageously these active substances are integrated
together into the self-adhesive matrix and are released therefrom
onto the skin within the application time.
[0119] According to the invention the ratio of carnitine or
derivatives thereof to capsaicin and/or caffeine is preferably 1 to
100 to 1, advantageously 1 to 1. That is, with a preferred
proportion of carnitine of 0.5% by weight, a proportion of 0.5% by
weight of caffeine has proven to be extremely effective.
[0120] The known heating effect of capsaicin, in combination with
carnitine and its reduction effect of the tissue fats, leads to a
reduction, already effective in low concentration, of the so-called
orange-peel skin, cellulite.
[0121] Surprisingly, it has been shown that the combination of
carnitine and capsaicin and/or caffeine leads to a synergy with
respect to the care and treatment of deficient skin conditions,
such as orange-peel skin or cellulite, Small varicose dilatations
of the cutaneous veins, varicose veins or areas of the skin
affected by striae.
[0122] The patchaccording to the invention which contains carnitine
alone and/or in combination with capsaicin and/or caffeine in the
matrix of the skin patch, shows an advantageous effect on the skin
thus treated, the lymphatic circulation and the development of heat
are stimulated.
[0123] This synergy is shown surprisingly positively in a skin
patch that is in contact with the skin for several hours, up to
eight hours.
[0124] In addition to carnitine, capsaicin and/or caffeine, other
suitable active substances for the purposes of the invention can be
added to the listed cosmetic matrices/pads either individually or
in combination, in particular active substances that have a
positive influence on the condition of the skin. Thus it has been
shown that active substances for positively influencing aging skin
which reduce the development of lines or else existing lines.
Therefore, particularly preferred active substances are
bioquinones, in particular ubiquinone Q10, creatine, creatinine,
carnitine, acetyl carnitine, biotin, isoflavone and isoflavonoids,
genistein, arctiin, cardiolipin, lipoic acid, antifreezing
proteins, hop and hop-malt extracts, and or substances promoting
the restructuring of the connective tissue, isoflavones and plant
extracts containing isoflavones, such as, e.g., soya and clover
extracts, which can also be used very readily in the matrices
according to the invention. It is also found that the matrix is
particularly suitable for using active substances for aiding the
skin functions in dry skin (such as, for example, vitamin C,
biotin, creatine, creatinine, propionic acid, glycerin, green tea
extracts, white tea extracts or solutions, eucalyptus oil, urea and
mineral salts, such as, for example, NaCl, sea minerals and
osmolytes, such as, for example, taurine, inositol, betaine,
quaternary ammonium compounds. In a similar way, the incorporation
of active substances for alleviating or positively influencing
irritative skin conditions, whether for sensitive skin in general
or for skin irritated by noxae (UV light, chemicals) has proven to
be advantageous. Mention is made here of active substances such as
sericosides, various extracts of licorice, licochalcone A,
silymarin and silyphos, dexpanthenol, ethanol, inhibitors of
prostaglandin metabolism, in particular cyclooxygenase, and of
leukotriene metabolism, in particular 5-lipoxygenase, but also the
5-lipoxygenase inhibitor protein, FLAP. The incorporation of
pigmentation modulators has also proven to be advantageous. Mention
is made here of active substances which reduce the pigmentation of
the skin and thus lead to a cosmetically desired lightening of the
skin and/or reduce the appearance of age spots and/or lighten
existing age spots, such as tyrosine sulfate, dioic acid
(8-hexadecene-1,16-dicarboxylic acid), lipoic acid and liponamide,
various extracts of licorice, kojic acid, hydroquinone, arbutin,
fruit acids, in particular alpha-hydroxy acids (AHAs), bearberry
(Uvae ursi), ursolic acid, ascorbic acid, green tea extracts,
aminoguanidine and/or pyridoxamine. In the same way, the matrices
according to the invention proved to be an excellent basis for
active substances that bring about an enhanced/more rapid tanning
of the skin (Advanced Glycation Endproducts (AGE), lipofuscins,
nucleic acid oligonucleotides, purines and pyrimidines,
NO-releasing substances, be it with or without the influence of UV
light.
[0125] The use of green tea extract is preferred, since in
combination with carnitine the effect of caring for the skin and
above all of reducing cellulite could be observed.
[0126] The secret of white tea is based on its careful preparation,
so that it remains virtually unchanged. White tea extracts contain
a high proportion of polyphenols, they are among the most highly
effective antioxidants, which render free radicals harmless. The
research concerned with these aspects of white tea is still
relatively young. White teas are commercially available under the
names Yin Zhen (silver needle) and Yin Long (silver dragon).
[0127] The use of white tea extract is therefore preferred since in
combination with carnitine the effect of caring for the skin and
above all of reducing cellulite could be observed.
[0128] Including carnitine, capsaicin and/or caffeine, the matrix
contains a total of active substances of up to 35% by weight,
preferably up to 15% by weight, very particularly preferably
0.02-2% by weight, based on the total mass of the matrix.
[0129] For the prophylaxis of oxidative and degenerative damage and
in particular for the treatment of such damage it has surprisingly
been found advantageous to add antioxidants to the cosmetic
matrices/pads. The antioxidants are advantageously selected from
the group consisting of amino acids, e.g., glycine, lysine,
arginine, cysteine, histidine, tyrosine, tryptophan, and
derivatives thereof (as salt, ester, ether, sugar, nucleotide,
nucleoside, peptide and/or lipid compound), imidazoles, e.g.,
urocanic acid, and derivatives thereof as salt, ester, ether,
sugar, nucleotide, nucleoside, peptide and/or lipid compound,
peptides such as D,L-carnosine, D-carnosine, L-carnosine, anserine
and derivatives thereof, e.g., as salt, ester, ether, sugar, thiol,
nucleotide, nucleoside, peptide and/or lipid compound, carotenoids,
carotenes, e.g., .alpha.-carotene, .beta.-carotene, .psi.-lycopene,
phytoene, and derivatives thereof, e.g., as salt, ester, ether,
sugar, nucleotide, nucleoside, peptide and/or lipid compound,
chlorogenic acid and derivatives thereof, as salt, ester, ether,
sugar, thiol, nucleotide, nucleoside, peptide and/or lipid
compound, aurothioglucose, propylthiouracil and other thiols, e.g.,
thioredoxin, lipoic acid, glutathione, cysteine, cystine, cystamine
and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl
and lauryl, palmitoyl, oleyl, .gamma.-linoleyl, cholesteryl and
glyceryl esters, and also salts thereof, dilauryl thiodipropionate,
distearyl thiodipropionate, thiodipropionic acid and derivatives
thereof, as salt, ester, ether, sugar, thiol, nucleotide,
nucleoside, peptide and/or lipid compound, and also sulfoximine
compounds, e.g. homocysteine sulfoximine, buthionine sulfones,
penta-, hexa-, heptathionine sulfoximine, in very low tolerated
doses, e.g., pmol to .mu.mol/kg. Additionally (metal) chelating
agents, e.g., apoferritin, desferral, lactoferrin, .alpha.-hydroxy
fatty acids, palmitic acid, phytic acid, and derivatives thereof,
as salt, ester, ether, sugar, thiol, nucleotide, nucleoside,
peptide and/or lipid compound, .alpha.-hydroxy acids, e.g., citric
acid, lactic acid, malic acid, humic acid, bile acid, bile
extracts, bilirubin, biliverdin, melanin, EDTA, EGTA and
derivatives thereof, unsaturated fatty acids and their derivatives,
e.g., .gamma.-linolenic acid, linoleic acid, oleic acid, folic acid
and derivatives thereof, furfurylidenesorbitol and its derivatives,
ubiquinone, ubiquinol, plastoquinone and derivatives thereof, as
salt, ester, ether, sugar, thiol, nucleotide, nucleoside, peptide
and lipid compound, vitamin C and derivatives, e.g., ascorbyl
palmitate, Mg-ascorbyl phosphate, ascorbyl acetate, tocopherols and
derivatives, e.g. vitamin E acetate, Trolox.RTM., and also phenolic
compounds and plant extracts comprising them, such as flavonoids,
for example, e.g., glycosylrutin, ferulic acid, caffeic acid,
furfurylideneglucitol, butylated hydroxytoluene, butylated
hydroxyanisole, nordihydroguaiacic acid, nordihydroguaiaretic acid,
trihydroxybutyrophenone and derivatives thereof, as salt, ester,
ether, sugar, nucleotide, nucleoside, peptide and lipid compound,
uric acid and derivatives thereof, mannose and derivatives thereof,
as salt, ester, ether, sugar, thiol, nucleotide, nucleoside,
peptide and lipid compound, zinc and its derivatives, e.g., ZnO,
ZnSO.sub.4, selenium and its derivatives, e.g., selenium
methionine, ebselen, stilbenes and derivatives thereof, e.g.,
stilbene oxide, trans-stilbene oxide, and the derivatives that are
suitable in accordance with the invention, as salt, ester, ether,
sugar, thiol, nucleotide, nucleoside, peptide and/or lipid
compound, of these stated active substances.
[0130] The matrix will contain the antioxidant or antioxidants in
amounts of 0-35% by weight, preferably 0-15% by weight, very
preferably 0.02%-2%.
[0131] Further examples of active substances which can be used
include essential oils. By essential oils are meant plant-derived
concentrates which as natural raw materials are used primarily in
the fragrance and foodstuffs industries and are composed more or
less of volatile compounds. Examples that may be mentioned of these
compounds include 1,8-cineol, limonene, menthol, borneol and
camphor. The term "essential oils" is often used for the volatile
constituents still present in the plants. In their true sense,
however, essential oils are understood to be mixtures of volatile
compounds prepared by steam distillation from plant raw
materials.
[0132] Essential oils are composed exclusively of volatile
components, whose boiling points are in general between 150 and
300.degree. C. They include predominantly hydrocarbons or
monofunctional compounds such as aldehydes, alcohols, esters,
ethers and ketones. Parent compounds are mono- and sesquiterpenes,
phenylpropane derivatives and longer-chain aliphatic compounds.
[0133] In some essential oils, one constituent is dominant, for
example, eugenol in clove oil, at more than 85%, while other
essential oils constitute complex mixtures of the individual
constituents. Often the organoleptic properties are determined not
by the main components but by subsidiary or trace constituents,
such as, for example, by the 1,3,5-undecatrienes and pyrazines in
galbanum oil. The number of identified components in many of the
commercially significant essential oils is up into the hundreds.
Very many constituents are chiral, with very often one enantiomer
being predominant or being present exclusively, such as (-)-menthol
in peppermint oil or (-)-linalyl acetate in lavender oil, for
example.
[0134] Preferred essential oils that may be mentioned include oleum
eucalypti, oleum menthae piperitae, oleum camphoratum, oleum
rosmarini, oleum thymi, oleum pini sibricum and oleum pini
silvestris, and the terpenes 1,8-cineol and levomethanol.
[0135] Further essential oils that may be mentioned include oleum
abietis albae, oleum anisi, oleum aurantii floris, oleum
bergamottae, oleum calendulae infusum, oleum camphoratum, oleum
caryophylli, oleum chamomillae, oleum cinnamomi ceylanici, oleum
citri, oleum citronellae, oleum cupressi, oleum cymbopogonis, oleum
jecoris, oleum lavendulae, oleum macidis, oleum majoranae, oleum
melaleucae viridiflorae, oleum melissae, oleum menthae arvensis,
oleum menthae piperatae, oleum millefolium, oleum myrrhae, oleum
myrte, oleum oregani, oleum pini sibricum, oleum pinisilvestris,
oleum salviae, oleum santali, oleum terebinthinae rectificat, oleum
thymi, oleum valerianae, oleum zingiberis and/or tea tree oil.
[0136] Peppermint oils are essential oils obtained by steam
distillation from leaves and blossoms of various varieties of
peppermint, and occasionally also those from Mentha arvensis.
[0137] Citrus oils are essential oils obtained from the peel of
citrus fruits (bergamot, grapefruit, lime, mandarin, orange,
lemon), often also called agrumen oils.
[0138] Citrus oils are composed largely of monoterpene
hydrocarbons, principally limonene (exception: bergamot oil, which
contains only about 40%).
[0139] Menthol can be used for example for surface anesthesia in
cases of skin irritation as a result of light burns. The products
used in this way generate a pleasant feeling of cold and can be
used for cooling skin irritations, e.g., mild sunburn and shaving
burn that do not require specialist medical treatment.
[0140] Menthol has three asymmetric C atoms and accordingly exists
in four diastereomeric pairs of enantiomers (cf. the formulae; the
other four enantiomers are the corresponding mirror images).
##STR00008##
[0141] The diastereoisomers, which can be separated by
distillation, are referred to as neoisomenthol, isomenthol,
neomenthol [(+) form: a constituent of Japanese peppermint oil] and
menthol. The most important isomer is (-)-menthol (levomenthol),
shining prisms with a strong peppermint-like odor.
[0142] \As further active substances it is possible to add camphor,
for example, to the matrix in order to treat skin irritations/mild
pain, neuralgias and inflammation. By camphor is meant 2-bornanone,
1,7,7-trimethylbicyclo[2.2.1]heptan-2-one; see diagram below.
##STR00009##
[0143] For advantageous embodiments of hydrogels/cataplasms of the
invention it is also possible to mention in addition active
hyperemic substances such as synthetic active substances such as
nicotinic acid derivatives, preferably benzyl nicotinate or propyl
nicotinate, and anti-inflammatories and/or analgesics.
[0144] By way of example mention may be made of nicotinic acid
benzylester
##STR00010##
Benzyl nictotinate.
[0145] Flavone and its derivatives, often also collectively called
"flavones," are also advantageous additives in the sense of the
present invention. They are characterized by the following basic
structure (substitution positions indicated):
##STR00011##
[0146] Some of the more important flavones, which can also be used
with preference in preparations of the invention, are listed in the
table below:
TABLE-US-00001 OH substitution positions 3 5 7 8 2' 3' 4' 5'
Flavone - - - - - - - - Flavonol + - - - - - - - Chrysin - + + - -
- - - Galangin + + + - - - - - Apigenin - + + - - - + - Fisetin + -
+ - - + + - Luteolin - + + - - + + - Campherol + + + - - - + -
Quercetin + + + - - + + - Morin + + + - + - + - Robinetin + - + - -
+ + + Gossypetin + + + + - + + - Myricetin + + + - - + + +
[0147] In nature, flavones occur ordinarily in glycosylated
form.
[0148] In accordance with the invention the flavonoids are
preferably chosen from substances of the generic structural
formula
##STR00012##
where Z.sub.1 to Z.sub.7 are chosen independently of one another
from H, OH, alkoxy and also hydroxyalkoxy, where the alkoxy and
hydroxyalkoxy groups respectively may be branched and unbranched
and may have 1 to 18 C atoms, and where Gly is chosen from mono-
and oligoglycoside residues.
[0149] In accordance with the invention the flavonoids can,
however, also be chosen advantageously from substances of the
generic structural formula
##STR00013##
where Z.sub.1 to Z.sub.6 are chosen independently of one another
from H, OH, alkoxy and also hydroxyalkoxy, where the alkoxy and
hydroxyalkoxy groups respectively may be branched and unbranched
and may have 1 to 18 C atoms, and where Gly is chosen from mono-
and oligoglycoside residues.
[0150] Such structures can be chosen with preference from
substances of the generic structural formula
##STR00014##
where Gly.sub.1, Gly.sub.2 and Gly.sub.3 independently of one
another represent monoglycoside residues or Gly.sub.2 and Gly.sub.3
may also, individually or together, represent saturations by
hydrogen atoms.
[0151] Preferably Gly.sub.1, Gly.sub.2 and Gly.sub.3 are chosen
independently of one another from hexosyl radicals, particularly
rhamnosyl radicals and glucosyl radicals. However, other hexosyl
radicals can as well be used with advantage where appropriate,
examples being allosyl, altrosyl, galactosyl, gulosyl, idosyl,
mannosyl and talosyl. It may also be of advantage in accordance
with the invention to use pentosyl radicals.
[0152] Z.sub.1 to Z.sub.5 advantageously are chosen independently
of one another from H, OH, methoxy, ethoxy and also
2-hydroxyethoxy, and the flavone glycosides have the structure:
##STR00015##
[0153] The flavone glycosides of the invention which become of
particular advantage are those from the group represented by the
following structure:
##STR00016##
where Gly.sub.1, Gly.sub.2 and Gly.sub.3 independently of one
another represent monoglycoside residues or oligoglycoside
residues. Gly.sub.2 and Gly.sub.3 may also, individually or
together, represent saturations by hydrogen atoms.
[0154] Preferably Gly.sub.1, Gly.sub.2 and Gly.sub.3 independently
of one another are chosen from hexosyl radicals, in particular
rhamnosyl radicals and glucosyl radicals. However, other hexosyl
radicals can as well be used with advantage where appropriate,
examples being allosyl, altrosyl, galactosyl, gulosyl, idosyl,
mannosyl and talosyl. It may also be an advantage in accordance
with the invention to use pentosyl radicals.
[0155] In the sense of the present invention it is particularly
advantageous to choose the flavone glycoside or glycosides from
.alpha.-glucosylrutin, .alpha.-glucosylmyricetin,
.alpha.-glucosylisoquercitrin, .alpha.-glucosylisoquercetin and
.alpha.-glucosylquercitrin.
[0156] Of particular preference in accordance with the invention is
.alpha.-glucosylrutin.
[0157] Also advantageous in accordance with the invention are
naringin (aurantiin, naringenin-7-rhamnoglucoside), hesperidin
(3',5,7-trihydroxy-4'-methoxyflavanone-7-rutinoside, hesperidoside,
hesperetin-7-O-rutinoside), rutin
(3,3',4',5,7-pentahydroxyflyvone-3-rutinoside,
quercetin-3-rutinoside, sophorin, birutan, rutabion, taurutin,
phytomelin, melin), troxerutin
(3,5-dihydroxy-3',4',7-tris(2-hydroxyethoxy)flavone-3-(6-(O-(6-deoxy-.alp-
ha.-L-mannopyranosyl)-.beta.-D-glucopyranoside)), monoxerutin
(3,3',4',5-tetrahydroxy-7-(2-hydroxyethoxy)-flavone-3-(6-(O-(6-deoxy-.alp-
ha.-L-mannopyranosyl)-.beta.-D-gluco-pyranoside)), dihydrorobinetin
(3,3',4',5',7-pentahydroxyflavanone), taxifolin
(3,3',4',5,7-penta-hydroxyflavanone), eriodictyol-7-glucoside
(3',4',5,7-tetrahydroxyflavanone-7-glucoside), flavanomarein
(3',4',7,8-tetrahydroxyflavanone-7-glucoside) and isoquercetin
(3,3',4',5,7-pentahydroxyflavanone-3-.beta.-D-glucopyranoside)) or
derivatives thereof.
[0158] According to the invention, the requirement for a
self-adhesive skin patch is met surprisingly simply and
effectively. The skin patch according to the invention comprising
preferably carnitine as active substance and polyacrylic acid as
the basis of the adhesive matrix, on the one hand has a good
adhesion to the skin, which must be maintained over the entire
period of the intended dosage of the active substance, and on the
other hand a removability that is pain-free and does not leave any
residue.
[0159] Since adhesion and consistency of an adhesive matrix
containing the active substance result from the interaction of the
individual components, actually the production of a skin patch is
associated with many problems, as shown in the prior art.
[0160] However, these problems surprisingly have been solved by the
particularly preferred variant. A skin patch according to the
invention has proven to be preferred in which a combination of
preferred polyacrylate adhesive mass (sodium
polyacrylate/polyacrylic acid sol. 20%), carnitine as active
cosmetic substance and the following constituents of the patch are
selected:
[0161] Water, sodium carboxymethylcellulose, dihydroxyaluminum
aminoacetate, hydroxypropylcellulose, glycerol, disodium edetate,
kaolin, methyl parahydroxybenzoate, propylene glycol and/or ricinus
communis (castor oil).
[0162] The skin patches preferred according to the invention and
thus produced can be easily placed onto the skin and due to the
special adhesive force, exert a pressure on the skin which reduces
the appearance of cellulite or striae.
[0163] The essential influencing variable on exerting pressure is
the material of the plaster and its consistency. If it is, e.g., a
relatively flexible, elastic material, the material can avoid the
pressure generated on being applied to the skin. Thus no pressure
is exerted on the skin. However, if the material is rigid and
inflexible, this is not compatible with the patient's comfort when
worn for a long time.
[0164] Further influencing variables on the pressure exerted, which
also indirectly concern the plaster material properties, are:
[0165] stretchability of the material upon application, i.e., when
the plaster is greatly stretched over the skin and corresponding
adhesion to the skin, the skin could be contracted and the pressure
is directed in a counter-productive manner [0166] moisture of the
skin and thus also moisture-permeability of the material [0167]
adhesion to the skin [0168] dynamic pressures and/or shear forces
by motion of the area of the skin.
[0169] According to the invention, these influencing variables are
optimally coordinated with one another through the preferably
selected constituents of the adhesive matrix, the carrier material
and the active cosmetic substances.
[0170] It has proven to be advantageous according to the invention
for the reduction of the skin phenomena affected by cellulite if
the skin patch has an adhesion time value of greater than 5 s. The
adhesion time value is determined according to a standard
measurement method, as outlined briefly below.
[0171] A measurement of the adhesion time value is carried out on a
test instrument according to FIG. 1.
[0172] FIG. 1 shows an inclined plane with a pitch of 30.degree. on
which the skin patch to be tested is placed with the adhesive side
(3) uppermost. The upper and lower part is covered by cardboard (2)
so that a stretch of 5 cm remains. The steel ball (1) is placed at
the head of the inclined plane.
[0173] Before each measurement, steel balls (diameter 19.0 mm, mass
28.2 g) are cleaned of all greasy residue and other contaminants
first in toluene and then in anhydrous acetone. The flash time of
the solvent up to the use of the steel balls must be at least 2
minutes and may be no longer than 10 minutes.
[0174] The self-adhesive skin patch to be tested is placed with the
carrier side down in the middle of an inclined plane (30.degree.)
so that the patch ends overlap the markings made at the side on the
inclined plane. Then the upper part of the inclined plane, starting
from the upper edge, is covered by means of a sheet of paper
(standard copier paper or comparable quality), for a length of 10
cm, the paper is, if necessary, folded over the edge and secured
from slipping by a steel pin.
[0175] Below the covered portion of the inclined plane, the
measuring length follows the skin patch with the adhesive mass
layer revealed. The length of the respective measuring length is 5
cm. Subsequently, the lower part of the plane, starting from the
lower edge of the respective measuring length, is likewise covered
with paper. Then a steel ball is placed by hand (wear powder-free
gloves) on the upper end of the inclined plane and allowed to roll
with the slightest possible application of force. As soon as the
steel ball comes to a stop on the skin patch, a stop watch is
started (see FIG. 1).
[0176] The steel ball must be held by the adhesive layer of the
patch within the revealed section of the skin patch for at least 5
seconds in order to meet the requirement of the adhesion time
value, i.e., it must reach an adhesion time value of greater than
5.
[0177] These tests have shown that the skin patches according to
the invention comprising the following constituents show a
corresponding adhesion time value. The matrix according to the
invention and adhering to the human skin and containing carnitine
as the active cosmetic substance, has an adhesion time value of
greater than 5 and thus has the necessary characteristic in order
to meet the requirements for the adhesive force over the duration
of application (of up to 8 h), a pain-free removal leaving no
residue and an adhesion with no irritation of the skin.
[0178] A polyacrylate adhesive mass containing carnitine and the
special constituents* with an adhesion time value >5 is
preferred.
TABLE-US-00002 TABLE adhesion time value Adhesive mass Active
substance Adhesion time value [s] Polyacrylates* Carnitine >5
Polyacrylates* Carnitine, capsaicin >5 Polyacrylates* Carnitine,
caffeine (1:1) >5 *Polyacrylates containing: sodium
polyacrylate/polyacrylic acid sol. 20%, water, sodium
carboxymethylcellulose, dihydroxyaluminum, aminoacetate,
hydroxypropylcellulose, glycerol, disodium edetate, kaolin, methyl
parahydroxybenzoate, propylene glycol and ricinus communis (castor
oil).
[0179] For use as a patch, plaster or cosmetic matrix/cosmetic pad,
the gel matrices of the invention are pressed, rolled or the like
as a layer onto a release medium made of paper, film or the like
and are laminated on the reverse with any desired backing material
such as, for example, a polymer film, textiles or the like. With
particular preference in accordance with the invention the gel
matrices are applied in the hot state by a metering pump to a
backing material, and with very particular preference are
configured in a three-dimensional form by means of corresponding
cavities in the presses or roller mechanisms. The shape of the
plaster or cosmetic matrix produced is determined by the shape of
the cavities and is not subject to any restriction; it may, for
example, be ellipsoidal with edges which flatten off, or may, for
example, be angular in configuration.
[0180] With particular advantage the gel matrix of the invention is
applied on a flexible cover layer, particularly when used as a skin
patch, plaster or cosmetic matrix. A corresponding plaster or a
corresponding cosmetic matrix is constructed from a backing such as
films, nonwovens, wovens, foams, etc., the adhesive matrix, and
liner film, liner paper or release paper in order to protect the
adhesive matrix prior to the use of the plaster.
[0181] In a further preferred embodiment of the invention, backings
used are polymer films, nonwovens, wovens and combinations thereof.
Backing materials available for selection include polymers such as
polyethylene, polypropylene, polyesters, polyethers,
polyether-ester copolymers and polyurethane or else natural
fibers.
[0182] In summary it can be stated that suitable backing materials
encompass all rigid and elastic sheet-like structures of synthetic
and natural raw materials. Preference is given to backing materials
which can be employed such that they fulfill properties of a
functional dressing. Listed by way of example are textiles such as
wovens, knits, lays, nonwovens, laminates, nets, films, foams and
papers. In addition it is also possible for these materials to be
pretreated and/or after-treated. Customary pretreatments are corona
and hydrophobization; common after-treatments are calendering,
heat-treating, laminating, punching and enveloping.
[0183] It is particularly advantageous if the backing material is
sterilizable, preferably .gamma.(gamma)-sterilizable.
[0184] These backing materials in accordance with the invention can
be, e.g., provided point-wise with strongly adhesive polymers such
as polyisobutylene,
[0185] SEBS block polymers, natural rubbers and/or synthetic
rubbers, polyurethane or the like by screen printing or analogous
methods, which outwardly overlap the applied hydrogel matrix at the
side edges. Matrices of the invention manufactured in this form can
be affixed self-adhesively to parts of the body that are under
severe mechanical stress, such as elbows or knee joints, where the
inherent adhesion of the hydrogels/cataplasms is no longer
sufficient for durable application.
[0186] Finally the matrix can be enveloped or provided with an
anti-adhesive backing material, such as siliconized paper. On its
self-adhesive side which later faces the skin, the cosmetic matrix
of the invention is lined over its whole width, until used, usually
with an anti-adhesive backing material. This protects the
self-adhesive layer from the gel matrix's adhesive, which possesses
good skin compatibility and which has preferably been applied by a
transfer method, and additionally stabilizes the product as a
whole. The lining can be designed, in a known way, in once piece
or, preferably, in two parts.
[0187] Further embodiments may be such that between the reverse of
the matrix and the lining backing there is a second matrix
possessing higher active-substance solubility, as a reservoir.
Instead of a second matrix and backing, this might also be a
thermoformed film with pure active substance.
[0188] Located on part (e.g., at the edge) of the adhesive side of
the matrix is a second matrix possessing high bond strength for the
purpose of additional fixing, but possessing insufficient
active-substance solubility.
[0189] The active substance-free matrix is located between two
non-anchoring films and is utilized for fixing.
[0190] The subject matter of the present invention is further the
use of the cosmetic skin patch for skin care, in particular of
those parts of the skin affected by cellulite or striae. In
particular the use of the active-substance-doped gel matrices for
use as PADs for the cosmetic and beneficial treatment of unwanted
skin phenomena, such as cellulite or striae, is to be emphasized
with preference.
[0191] The use of the polymer matrix as cosmetic or dermatological
pads or plasters is suitable particularly in a flat embodiment with
a total area of 0.2 to 1000 cm.sup.2. With this, for example, large
(up to 1000 cm.sup.2) regions on the thighs are covered for the
purpose of treating the orange-peel skin.
[0192] Preference is given to the use of the self-adhesive polymer
matrix in two- or three-dimensional embodiment with a polymer
matrix weight fraction of 0.1 to 1000 g, in particular of 14 g per
patch. The shape in this case may be round, oval, angular or
designed in accordance with the sections of the skin.
[0193] The invention further covers the combination of the skin
patch with a wrapping compressing the skin up to a certain
pressure.
[0194] It is known from tests that the lymphatic circulation of the
skin can be stimulated by compression. However, if the compression
is too strong, it can lead to blockages and as a result to edema or
thrombosis.
[0195] The pressure values of the patches or set applied to human
skin have been determined as another characteristic value of the
skin patches or the set according to the invention.
[0196] The measurement was carried out in a single-axis tensile
test in accordance with DIN 53835--tensile stress with repeated
stress between constant yield strengths and immediate reverse at
the reverse points. The upper yield strength was established at
30%. The determination of the tensile force relating to elongation
of the patch under stress was made in the 5.sup.th cycle for the
elongation that corresponded to the elongation of the patch after
application to the leg. The calculation of the pressure was made
using Laplace's equation from tensile force, leg circumference and
patch or wrapping width.
[0197] The pressures determined according to the invention were
between approx. 4-7 mmHg.
[0198] Patches according to the invention which comprise such
pressure values are therefore preferred.
[0199] A patch or a set is therefore preferred according to the
invention which consists of skin patch and wrapping that generates
a pressure of up to a maximum of 10 mm Hg on the skin.
[0200] The set is thereby designed as described at the outset, so
that a maximum pressure of 10 mm Hg is generated on the skin.
[0201] A wrap is known from the prior art which is called
"wrapping". A type of cellophane casing is thereby drawn over the
areas of the skin affected by cellulite. A disadvantage is the
completely occlusive covering of the skin, which can lead to skin
macerations, itching and other unpleasant skin phenomena.
[0202] The invention was designed to avoid these disadvantages.
[0203] Bandages, tape, stockings, shorts and/or cuffs can be
contemplated as wrapping as well as a combination thereof.
[0204] According to the invention a cuff is selected as a wrapping,
which is elastic up to a certain degree and air-permeable and
steam-permeable.
[0205] The cuff preferably has a conical section. Thus when applied
to the thigh a disadvantageous greater compression on the upper
section of the thigh towards the hip is avoided.
[0206] The cuff is equipped with one end being self-adhesive to
itself so that it can be attached to itself.
[0207] The result of this is that there is no need to supply
different cuffs for users with differing sizes and shapes.
According to the invention, due to the elasticity and the
properties of closing itself, the cuff thus covers all the standard
sizes and a "one size fits all" situation is advantageously created
for the manufacturer.
[0208] Advantageously markings are made on the cuff that make it
easy for the user to generate sufficient pressure with the cuff,
depending on the circumference of the thigh.
[0209] Numerous materials based on film, nonwoven, woven, gel or
foam are already known as a backing material for the cuff and are
also used in practice. The materials must be tolerated by the skin,
permeable to air and steam as well as possible to mold well and
soft. Due to these requirements, often a carrier that is as thin or
soft as possible is preferred. For handling and in use, however,
sufficient strength and if necessary a limited stretchability are
also required of the backing material. Furthermore the backing
material should also have sufficient strength and a limited
stretchability even after being soaked.
[0210] Thin backings, in particular those of nonwovens, are readily
permeable to air and steam.
[0211] Suitable backing materials encompass elastic sheet-like
structures of synthetic and natural raw materials. Preference is
given to backing materials which can be employed such that they
fulfill properties of a functional dressing. Listed by way of
example are textiles such as wovens, knits, lays, nonwovens,
laminates, nets, films, foams and papers which have a
stretchability of at least 10% at a stress of 10 N/cm. Moreover,
combinations of the listed materials are also suitable.
[0212] In addition it is also possible for these materials to be
pretreated and/or after-treated. Customary pretreatments are corona
and hydrophobization; common after-treatments are calendering,
heat-treating, laminating, punching and enveloping, UV/IR
irradiation or electron irradiation.
[0213] The invention thus advantageously covers a combination of
self-adhesive skin patch and cuff according to the invention. This
combination is predestined as a set for skin care and in particular
for the treatment of cellulite.
[0214] In application the set according to the invention can
comprise a cuff and 4 to 10 patches so that a long-term and thus
effective treatment is ensured.
[0215] In skin care, and in particular in the treatment of
cellulite, the skin patch according to the invention,
advantageously containing carnitine or carnitine and capsaicin, is
applied to, e.g., the side portion of the thigh. Due to the
self-adhesive property of the skin patch with an adhesion time
value of >5, this is immediately fixed and does not slip.
Subsequently the user can if necessary turn over the cuff and close
it easily because of the end closing to itself, depending on the
desired degree of pressure and the size of the thigh.
[0216] Due to the advantageous design of the skin patch with skin
care ingredients, non-irritating adhesive matrix, pain-free
detachability and cuff that is not irritating to the skin and is
permeable to air and steam, the user will not experience any
unpleasantness, even with longer application.
[0217] A preferred application time is up to 8 hours, so that
according to the invention the skin patch can be preferably worn
overnight.
* * * * *