DE102014113770A1 - Plaster with oily plant extracts - Google Patents

Abstract

The present invention describes a technical process for the preparation of a self-adhesive cosmetic or medical patch in which high concentrations of oily components are contained. Such oily components, typically CO2 extracts, essential oils or ethanolic extracts of vegetable origin, cause softening and greasing of the polymers used in the patch area and adhesive layers and thus lead to a practical uselessness of the patch. The object of this invention is therefore to provide a formulation containing liquid, softening, lipophilic plant extracts, this problem does not have. The object is achieved by a self-adhesive patch as a cosmetic or drug containing liquid, softening, lipophilic plant extract, preferably more than 1%, more preferably 2% to 20% of the proportion of adhesive matrix layers, characterized in that the softening function of this Ingredients by addition of brittle-brittle polymers at room temperature, in particular of polymethyl / butyl-methacrylate copolymers is compensated. Thus, a method is described for the first time and practically applicable for the routine, which allows to apply such oily plant extracts in higher concentrations in the field of self-adhesive plaster.

Description

Cosmetic patches have been known for a number of years. On the one hand, there are deep-rooted products in the traditional world of pharmaceuticals, on the other hand, here, following the application of the zeitgeist, products predominate that are more likely to be associated with cosmetics.

For example, warming or cooling products have played a significant role in sports, cosmetics and medicine for millennia. For example, there are many manufacturers of warming and, depending on the application, cooling oils and creams to prepare the body for sport, to relax before and after exercise, and to increase flexibility and general functioning during exercise. The term "warming" or "cooling" in addition to the physical heat formation is also extended to a feeling of warmth or cold feeling responsive material effect out.

For the treatment of muscular pain in physical conditions there are patches with capsaicinoids as active ingredients, which can dose-dependently set very strong heat stimuli. The mode of action of these products is based on the one hand on the promotion of blood circulation in the affected areas and on the other on an influence on the metabolism. For example, the release of substance P is stimulated by capsaicin. This molecule actively intervenes in the pain circulation and contributes to a reduction of the perceived pain. Capsaicinoids directly irritate the pain receptors of the skin and are already effective in low concentrations. This distinguishes them from many markedly mild warming (circulation-enhancing) or cooling-known plant extracts, e.g. in the form of essential oils.

WO002013030227A1 describes the use of warming, active ingredient-containing patches for cosmetic purposes. As active ingredients circulation-promoting active ingredients (vanilyl butyl ether, carnitine capsaicin caffeine) in a proportion of 0.01 to 20 wt.% In the adhesive are claimed using preferably decyl oleate as an excipient.

In addition to warming skin pads for sports or pain therapy applications as described above, drug-free treatments such as Kinesio have been established for the body nurturing physiotherapeutic applications in recent years. ln US 5861348 For the first time kinesiotherapy is described and claimed. Here, the application effect is based primarily on a mechanical effect. Another effect of the Kinesiotape is a cosmetic effect that decorates the body of the athlete and the athlete himself and the viewer in addition to the mechanical effect optically points to the affected body parts. Many athletes are motivated and stimulated by their own and others' attention and are therefore able to increase their performance and well-being.

Unlike Kinesio is the pure "Tapen" to understand. "Tapen" is another term for "functional bandage technique". This term describes associations that help to perform desired movements by partially immobilizing joints and avoiding other (painful) movements. The taping is completely different from the basic physiological orientation and effect-wise different to the Kinesio therapy. In contrast, no immobilization should be performed on Kinesio, the complete mobility of the "taped" area is completely preserved in kinesiotherapy. Both forms of therapy, however, own, to dispense with active ingredients.

It is desirable to combine cosmetic care as well as the therapeutic medical plaster in a broader scope with the benefits of a warming and / or cooling component. To achieve this, it is also often desirable to use natural plant extracts, but as described above, due to the mildness of their action, they must be used in considerable proportion to the paving mass in order to develop a nourishing, refreshing, other cosmetic or even medicinal effect , The constituents contained in these herbal extracts are obtained in various processes and are often present as oily extracts due to their lipid solubility (e.g., essential oils or CO2 extracts).

A problem with the production of patches with high oily weight fraction in the paving mass is that the paving mass is not solid and consistent by the oil. This results in a paste-like behavior, in which the plaster initially dissolves badly from the cover film ("release liner"), later as badly on the skin. The residues after use must be laboriously mixed with organic solvents, e.g. Benzine be removed. This made the useful use of essential oils, CO2 extracts and other oily plant extracts in higher weight concentration practically impossible.

The erfindungsgsgemäße use of brittle at room temperature polymers has been found in the literature so far hardly. So reported in other context the US 8,784,879 of "modifiers of cohesion" added. However, the choice of substances does not primarily indicate interchangeability of the terms with our brittle polymers: silicon dioxide, PVP, polyacrylic acid, bentonite and kaolin are mentioned

WO 2006/018 340 A2 describes drug-containing tapes for the treatment of joint diseases. The script mentions some herbal components, but is silent on the use of Zingiber officinal extracts.

DE 10056009 A1 discloses medicated matrix patches for the controlled delivery of hyperemic agents. The script also mentions some herbal components, but is silent on the use of Zingiber officinal extracts.

DE 19650471 A1 describes active ingredient-containing patches with a carrier material and a hot-melt adhesive applied thereto, which contains at least one hyperemicating active ingredient. The adhesive may be applied over the entire surface or partially, the latter to improve the air and water vapor permeability. Also this font mentions some herbal components, but is silent on the use of Zingiber officinal extracts.

DE 19749467 A1 describes active ingredient-containing patches with a carrier material and a hot-melt adhesive applied thereto, which contains at least one active ingredient, wherein the adhesive is foamed. The font is silent on the use of Zingiber officinal extracts.

WO 2013 030227 A1 describes the use of warming active ingredient patches for cosmetic purposes such as Celulite and Striae gravidarum. Particular mention is made of capsaicinoids (0.01-0.20%), nonivamide (0.01-0.15%), vanilyl butyl ether (0.5-2.5%), nicotinic acid benzyl ester (0.5-4.0%) , Rosemary oil (0.5-5.0%), capsiate (vanilin ester) (0.5-2.5%) and mustard oils (0.2-4.0%), among other pain-relieving pharmacological agents, warming and cooling essential oils and cosmetic skin care and circulation-promoting or toning agents. The font is silent on the use of Zingiber officinal extracts.

As mentioned above, all of the above mentioned documents mention some herbal extracts, but are silent in particular on the use of ginger extracts (Zingiber officinal extracts) in self-adhesive skin coverings. Furthermore, they in no way describe a solution to the problem of being able to use high percentages by weight of the oily extracts in a plaster matrix without losing their adhesive and coherent properties.

Warming or cooling essential oils or other oily plant extracts, such as zingiber officinals and its extracts, have been widely used as food in the culture of many peoples and extensively described in the literature for their health benefits and conditioning properties, and are ideal components for warming skin condition applications ,

The smell of the ginger is aromatic, the taste spicy. Essential ingredients are an essential oil, resin acids and neutral resin and gingerol, a sharp aromatic substance. Next ginger contains Zingiberen, Zingiberol, Shogaol and Diarylheptanoide. In addition, the ginger roots also contain the digestive, stomach-strengthening, appetite-stimulating and circulation-stimulating substances borneol, cineole, shoagol (a formation product of gingerol, whereby gingerol loses a hydroxy group) and zingerone, as well as vitamin C, magnesium, iron, calcium, potassium, sodium and phosphorus.

Young ginger sprouts serve as vegetables in the tropics. Pickled ginger comes from Japan, which is eaten between different sushi courses. Here he is also sought after as an aphrodisiac. Ginger is often used in beverage (ginger ale, ginger beer) and food industry. Ginger Ale is a ginger-flavored lemonade that was especially popular around the mid-20th century. Because of its stimulating effect on perspiration ginger is popular in hot countries as an additive in coffee or tea. Even pure ginger tea is in use. Ginger is one of the better known culinary herbs and spices both fresh and dried. It serves pure or in mixtures (curry, chutneys, jams, sauces) as a spice. Gingerbread, printen, rice pudding, fruit salad, tea and fruity cold dishes are also refined with ground ginger. Ginger plums or ginger nuts are pieces of fresh ginger in syrup. Other sweet ginger preparations include candied ginger (also coated with chocolate) and ginger jam, which is especially popular in Great Britain.

In medical applications, ginger has an antibacterial and antiviral effect, has an antiemetic effect (protects against vomiting), promotes blood circulation and increases bile juice production. The rhizomes have been used for a long time, especially in South and East Asia as a remedy z. B. used in coughing.

The viscous gals root stock (Oleoresin) is also described in the COSING database for cosmetic ingredients as plant extract CAS No. 84696-15-1 from Zingiber Officinale. It contains the essential oils and a percentage of pungent, the gingerols and Shogaols. Preparations from the ginger rhizome are said to have antioxidant, anti-emetic, anti-inflammatory and stimulating effects on the gastric juice, saliva and bile formation as well as the intestinal function and are therefore prescribed especially in traditional Asian medicine for the treatment of rheumatism, muscle aches or colds. Commission E and the European Scientific Cooperative on Phytotherapy (ESCOP) advocate the use of ginger roots for gastrointestinal complaints and nausea and vomiting. Externally applied ginger has a soothing effect, especially in the area of mucous membranes and skin wounds.

A feature of many warming or cooling herbal extracts, including the Zingiber Officinale oleoresin extracts is that they are compared to the medicinal use finding capsaicinoids significantly weaker circulation. Therefore, in order to develop a perceptibly pleasant nourishing and beneficial effect on the skin, they must be used in much higher concentrations than the capsaicinoids. When used in self-adhesive skin coverings, the resulting high oleoresin content is a technical problem in that it reduces, without further precautions, the bond strength of the overall matrix, as well as affecting the polymerization of the underlying fabric layer so as to compromise the consistency and stability of the overall structure. The result is usually a dissolution of the extract-containing matrix during wear, associated with a retention of unpleasant adhesive residue on the skin after removal of the patch.

The present invention describes for the first time technical solutions which allow the use of oily vegetable extracts, such as Zingiber Offcinale oleoresin extracts (eg CO2 extracts) in higher concentrations in cosmetic and medical self-adhesive skin conditions, without having the undesirable effects described the dissolution of the whole association ,

The term plaster used here encompasses, in addition to adhesive cosmetic / medical patches or matrices, all cosmetically / medically applicable skin conditions such as patch, pad, tapes, wipes, bandages, dressings, cataplasms, bandages and / or masks. Self-adhesive here means that the skin layer adheres to the skin due to the adhesive and does not need to be fixed by additional fasteners or masses. Numerous patches of the prior art are equipped with acrylate adhesives. Acrylate adhesives are characterized by a very low allergenic potential.

In US 8,017,162 a preparation of the red ginger is protected, which forms an ethanolic extract with the mandatory use of glucosamine. In a dependent claim, the use of this extract in addition to pills, tablets, drug powders, lotions, soft capsules, hard capsules and creams is also proposed for patches.

In US 5,869,533 a plaster for the fixation of an arthritis cream is claimed, consisting of a polymer, a capsaicine extract with the addition of further, in addition to ginger extract about 10 alternative active extracts and an adhesive layer.

US 6,653,352 still claims the use of five extracts besides ginger extract and some synthetic components in addition to the use of capsaicin and an analgesic; in subclaims dermal use intentions are listed as spray, sunscreen, etc.

The US patent application 20040247705 and 20040247706 use a patch to deliver parthenolides to the human body. Claim 4 of both applications is a claim for the additional addition of ginger extract.

Publications, in particular for the use of higher concentrations of oily plant extracts or, in particular, of oily ginger extracts in plaster-type systems, therefore do not occur. The object of the invention is therefore the solution to the problem that the lying in the mediation of the thermal experience effect of oily plant extracts in higher concentration, for example, and in particular the ginger extract succeeds with a sufficiently greasy formulation: Many of the cosmetic application and / or Transdermal therapy particularly suitable active ingredients are already at room temperature, but at least at usual processing temperatures of 60 to 80 ° C, noticeably volatile. This is disturbing because the difficult-to-predict extent of the respective Wirkstoff.-loss in the process can not achieve a safe dosage of the drug.

The choice of the brittle-polymer compound results from the compatibility with adhesives and an achievable bond strength and swelling of the material. We have the most experience in particular with copolymers of polymethacrylic acid with methanol and butanol, since it is a system swellable well with the selected extract substances. On the other hand, the use of other copolymers is still quite capable of this. In individual cases, an effect according to the invention could also be achieved with polyvinylpyrrolidone, a structurally differing copolymer. But also Eudragit E; a copolymeric methacrylate with respect to plastoid by cationic acting Dimethylaminoethyl monomer is altered; behaves almost as well. Polymeric substances which show brittle behavior between 0 ° -50 ° C. and are at least ethanol-soluble, preferably benzine-soluble or ethyl acetate-soluble, fulfill this object according to the invention.

The composition of the extracts also requires a certain definition. Thus, a large number of plant extracts are to be added here, if the potential for interference on the recipe structure by solvents contained is seen. It can therefore be assumed that even 2% of an emulsion of 50% by weight of a lipoid-soluble component in a matrix of hydrophilic constituents can exert their harmful effect on the cohesion.

It is therefore asked to understand that only material-technical aspects are used for the definition, in order to exclude a circumvention of this font. Lipophilic extract is therefore understood to mean exclusively the benzine- or ethyl acetate-soluble fraction of the plant extracts processed in the total. To 0.3 x 20 g / m ^2, ie 6 Suppose there be an adhesive composition of 80 g / m ² 20 g / m ² of a 30% iigen trituration gasoline-soluble extract blended so calculated G / m ^2, corresponding to 6% on the total basis weight of the Formulation, with non-diffusible components such as films and fabrics generally disregarded.

Another calculation example:

• Layer 1 contains 30 g / m ^{2 of} an adhesive without further additives Layer 2 contains 30 g / m ^{2 of} a butyl / methyl polymethacrylic ester copolymer (PLASTOID B)
• Layer 3 contains 40 g / m ^{2 of} an essential oil mixture (menthol / menthone) to which 5% butyl / methyl polymethacrylic ester copolymers, PLASTOID B) were added for faster cohesion formation
• Layer 4 again contains a pure adhesive of 60 g / m ²

It contains only a release liner and a polyester carrier fabric that will be left out of the calculation; the total basis weight is 160 g / m ² . The lipophilic portion of the plant extract makes up 40g / m ² · (100% - 5%) = 40 · 95% = 38g / m ² , ie 25.3%, the constructively used portion Plastoid B (butyl / methyl-polymethacrylic acid ester copolymers) is 30g / m ² (20%), totaling 32g / m ² .

The various calculation examples illustrate the way in which the calculations are developed in the claims and examples.

It is now also possible to add the brittle polymer to the adhesive in finely dispersed form or to profit in some other way from the solidifying effect. It has been found in the end that the path over a two- or three-layer central element, which may optionally be repeatedly included, is the most advantageous.

For this purpose, plastid B (butyl / methyl polymethacrylic acid ester copolymer) is first applied from solution and dried, and the lipophilic extract layer is applied immediately thereafter

Examples

Example 1:

A solution of butyl / methyl polymethacrylic acid ester copolymer is made 30% in ethyl acetate in solution. Coating and drying on a siliconized PET protective film take place at 30 g / m ² (layer 1).

A solution of 25% of butyl / methyl polymethacrylate ester copolymers in Migyol 812 (capric / caprylic triglyceride) is made in the heat (72 ° C) with constant stirring with homogeneous texture. 10 g of the homogeneous mixture are stirred homogeneously with 90 g ginger-CO2-extract (incl. Oleoresin) in the cool. 0.1% (based on the extract content) of jojoba oil and 0.02% of aloe vera powder are added. Layer 1 is then coated with 30 g / m ² with the polymer-containing composition described in the last sentence (layer 2)

Meanwhile, dissolving 10g of Oppanol B100, 5g of Oppanol B50 and 3g of Oppanol B15 on 1oog in aromatics-free gasoline, dissolve and coat as a self-contained layer of 50g / m2 and dry. After drying, layer 3 is laminated to the open part of the layer 2, which has just been coated as ginger extract, free from air bubbles. After a few hours of storage, the originally 3 layers have combined to form an externally uniform layer. However, the layer 1 shows only a slight release force to the siliconized PET film used. It can therefore be peeled off and replaced again with a 40 g / m ² coated acrylate layer (layer 4) on 75 μm PET (later release liner) as a laminate.

It now remains the task of connection with the woven fabric that is provided with an approximately 30 g / m ² -Schicht5 polyacrylate via lamination and then to the PIB (Oppanol) layer is laminated after removal of the PET protective layer. Conventional roller applicators are usually used for the solvent-containing components. The order of the ginger extract layer can with advantage over so-called. Mayer-bars (Drahtrakel) done.

The lipophilic extract content is calculated to be 14.2 percent by weight.

Example 2:

A solution of butyl / methyl polymethacrylic acid ester copolymer is made 30% in ethyl acetate in solution. Coating and drying on a siliconized PET protective film take place at 30 g / m ² (layer 1).

A solution of 25% of butyl / methyl polymethacrylate ester copolymers in Migyol 812 (capric / caprylic triglyceride) is made in the heat (72 ° C) with constant stirring with homogeneous texture. 10 g of the homogeneous mixture are stirred homogeneously with 90 g ginger-CO2-extract (incl. Oleoresin) in the cool. Layer 1 is then coated with 30 g / m ² with the polymer-containing composition described above (layer 2). Layer 3, prepared in the same way as layer 1, then laminated in a dried state.

Meanwhile, dissolve 10g of Oppanol B100, add 5g of Oppanol B50 and 3g of Oppanol B15 to 1oog in aromatics-free gasoline and coat and dry as a separate layer4 of approximately 50g / m2. After drying, layer 4 is air-free laminated on the open part of the opposite side just coated with ginger extract layer 1. After a few hours of storage, the originally 3 layers 1,2,3 have combined to form an externally uniform layer. However, the layer 1 shows only a small release force to the siliconized PET film used. It can therefore be peeled off and exchanged again with a 40 g / m ² coated acrylate layer (layer 5) on 75 μm PET (later release liner) as a laminate.

The task now remains to unite with the woven fabric which is lamination-coated with a polyacrylate about 30g / m ² layer 6 and then laminated to the PIB (Oppanol) layer 4 after removal of the PET protective layer. Conventional roller applicators are usually used for the solvent-containing components. The order of ginger extract layer can be done with advantage over so-called Mayer bars (wire bar). The lipophilic extract content is calculated to be 12.2% by weight.

Example 3:

A solution of butyl / methyl polymethacrylic acid ester copolymer is made 30% in ethyl acetate in solution. Coating and drying on a siliconized PET protective film take place at 50 g / m ² (layer 1).

A solution of 25% of butyl / methyl polymethacrylate ester copolymers in Migyol 812 (capric / caprylic triglyceride) is made in the heat (72 ° C) with constant stirring with homogeneous texture. 10 g of the homogeneous mixture are stirred homogeneously with 90 g peppermint oil in the cool. Layer 2 is then coated with 50 g / m ² with the polymer-containing composition described above. Layer 3, prepared in the same way as layer 2, then laminated in a dried state.

Meanwhile, dissolving 10g of Oppanol B100, 5g of Oppanol B50 and 3g of Oppanol B15 on 1oog in aromatics-free gasoline yields a solution and, as a separate layer 4, coated and dried at about 50g / m2. After drying, Layer 4 is air-free laminated to the open part of the just ginger extract coated layer 1. After a few hours of storage, the originally 3 layers have combined to form an externally uniform layer. However, the layer 1 shows only little separation power to the siliconized PET film used. It can therefore be peeled off and replaced again with a 40 g / m ² coated acrylate layer W (layer 5) on 75 μm PET (later release liner) as a laminate.

The task now remains to combine with a bi-elastic polyamide-elastane fabric which is provided with a layer of about 30 g / m ² polyacrylate (layer 6) by lamination and then to the PIB (Oppanol) layer 4 after removal of the PET protective layer is laminated. Conventional roller applicators are usually used for the solvent-containing components. The order of ginger extract layer can be done with advantage over so-called Mayer bars (wire bar). The lipophilic extract content here is calculated to be 16.6 percent by weight.

QUOTES INCLUDE IN THE DESCRIPTION

This list of the documents listed by the applicant has been generated automatically and is included solely for the better information of the reader. The list is not part of the German patent or utility model application. The DPMA assumes no liability for any errors or omissions.

Cited patent literature

• WO 00/2013030227 A1 [0004]
• US 5861348 [0005]
• US 8784879 [0009]
• WO 2006/018340 A2 [0010]
• DE 10056009 A1 [0011]
• DE 19650471 A1 [0012]
• DE 19749467 A1 [0013]
• WO 2013030227 A1 [0014]
• US8017162 [0024]
• US 5869533 [0025]
• US 6653352 [0026]
• US 20040247705 [0027]
• US20040247706 [0027]

Claims (13)

Self-adhesive patch as a cosmetic or pharmaceutical composition containing liquid, softening, lipophilic plant extract, preferably more than 1%, more preferably 2% to 20%, of the proportion of the adhesive matrix layers, characterized in that the softening function of these ingredients is brittle by addition at room temperature Brittle polymers, in particular of polymethyl / butyl-methacrylate copolymers is compensated. A patch prepared according to one or more of the preceding claims, characterized in that a triglyceride, preferably capric caprylic trigyceride, is added to the said liquid plant extract for solubilization, preferably in an amount of 2-15% by weight. Central element or repetitively present central elements of a plaster according to one or more of the preceding claims, characterized in that one from 1g / m ² to 1 kg / m ² , preferably 10 to 100 g / m ² precoated and predried, from brittle at room temperature brittle polymers, in particular polymethyl / butyl methacrylate existing material layer, by coating with 2-200g / m ² oily ingredients containing plant extract diffused an opposing balance of the layer composition is compared, so that there is a total cohesive, paving overall expression. Central element or repetitive existing central elements for paving according to one or more of the preceding claims, characterized in that from precoated and pre-dried, both sides existing layers of a brittle polymer for wrapping an oily plant extract, coated with 2-200g / m ² , which previously a proportion of preferably about 5-10% was added to hartspröden polymers, after diffusion compensation, a sufficiently shear-resistant layer for the construction of an effective patch with a total cohesive, paving-like overall expression results. Plaster structure comprising central elements of claim 2 or 3, characterized in that they are additionally supplemented on the skin side by an adhesive layer, preferably with a coating weight of 20-80 g / m ² . A plaster produced according to one or more of the preceding claims, characterized in that the said brittle-fractured polymer is added in ground form to one of the adhesive layers so as to be brittle-brittle by subsequent coating with 20-30 g / m ² with oil component, preferably with the addition of 2-5% Polymers, after diffusion compensation, a sufficiently shear-resistant layer for the construction of an effective patch with a total cohesive overall expression results. Plaster according to one or more of the preceding claims, characterized in that the coating solution Joyobaöl, aloe vera powder, dexpanthenol or other cosmetic or pharmaceutically active substances are added to modify the advantageous overall effect. Plaster structure containing central elements of claim 5 or 6, characterized in that the central elements are added to the plaster back side by an adhesive layer of esters of polyacrylic acid or other suitable adhesives, preferably with a coating weight of 20-80 g / m ² . Plaster structure of claim 8, characterized in that a support of stabilizing and diffusion-delaying polyethylene rests Plaster structure according to one or more of the preceding claims, characterized in that the backing is brought to the plaster backing by an externally resting layer of a textile fabric by hot stamping or surface bonding to the lateral conclusion. Plaster structure from one or more of the preceding claims, characterized in that ginger extract with gingerols and shogaols is used as the lipid extract Plaster structure according to one or more of the preceding claims, characterized in that the lipid extract used is an essential oil extracted from plants, for example peppermint oil, rosemary oil, wintergreen oil, etc. Plaster structure according to one or more of the preceding claims, characterized in that the lipid extract used is an essential oil extracted from plants, such as peppermint oil, rosemary oil, wintergreen oil, as a combination of these essential oils with oily ginger extract.

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