MXPA98002825A - Pharmaceutical, cosmetic or dermo-pharmaceutical patch for the release of various active compounds of nature difere - Google Patents
Pharmaceutical, cosmetic or dermo-pharmaceutical patch for the release of various active compounds of nature difereInfo
- Publication number
- MXPA98002825A MXPA98002825A MXPA/A/1998/002825A MX9802825A MXPA98002825A MX PA98002825 A MXPA98002825 A MX PA98002825A MX 9802825 A MX9802825 A MX 9802825A MX PA98002825 A MXPA98002825 A MX PA98002825A
- Authority
- MX
- Mexico
- Prior art keywords
- patch according
- polymer layer
- acid
- active compound
- patch
- Prior art date
Links
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Abstract
Patch, comprising a hydrophobic polymer layer, fixed on a support layer and containing: a) first particles of at least one water-soluble active compound, b) second oil particles, c) at least one fat-soluble active compound. The polymer layer also contains third particles of a hydro-absorbent agent, dispersed homogeneously in the polymer layer. This patch allows the conditioning and controlled administration of a set of nutrients and / or skin repairs of a different nature and also has an excellent adhesive power on the skin.
Description
PHARMACEUTICAL, COSMETIC OR DERMO-PHARMACEUTICAL PATCH FOR THE RELEASE OF VARIOUS ACTIVE COMPOUNDS OF
DIFFERENT NATURE
The present invention relates to a patch that allows the controlled release in the epidermis of at least two pharmaceutical, cosmetic or dermo-pharmaceutically active compounds, mainly compounds that have different solubilities. According to the invention, it is, in particular, a first group of fat-soluble active ingredients, and a second group of water-soluble active compounds. In the description of the present invention given below is designated by the term "patch" an active release system having a composite structure in the form of layers which, for application on the skin, ensures the release of the active product by transdermia. As far as the fat-soluble active compound is concerned, it is mainly a compound, capable of being solubilized in an apolar medium such as an oily medium. As for the water-soluble active compound, it is present in solid form, mainly in the form of particulate powder or in the form of granules. REF: 27153 It is known to use patches that allow, through transdermia, to penetrate active compounds. Such patches generally have a structure comprising several successive layers in the following order: a first layer, called a support layer generally occlusive, that is, constituted by a material impervious to the active compound so as to prevent the evaporation of the latter and facilitate transdermia; a second layer, called the polymer layer, fixed on the support layer and containing the active compound, this layer being able to come into direct contact with the skin; optionally, to facilitate fixing the patch on the skin, a layer of an adhesive material applied to the surface of the polymer layer and permeable to the active compound; finally, a separable layer of protection, which hermetically covers the polymer layer, so that it protects it from any external contamination during the storage time prior to the use of the patch. In particular, according to US Pat. No. 5,232,702, a patch structure consisting of an occlusive support layer and comprising, fixed thereon, a layer of polymer in a matrix of a silicone polymer is known, which includes, is dispersed state, fatty substances and hydrophilic active compounds. While this patch form is more particularly suitable for the release of water-soluble active compounds, this document does not disclose the release of supplementary active compounds of lipophilic nature. On the other hand, an occlusive patch adapted for the treatment of wrinkles of the aforesaid genus has been described in Patent W096 / 14 822, which comprises, in an anhydrous matrix, a water-soluble active compound in the form of a powder, and can also contain , this matrix an oil, used as a penetration agent. Additionally, Patent FR-A-2 738 744 describes a patch for the controlled release of at least one cosmetic or dermo-pharmaceutically active compound, which carries a reserve layer, fixed on a support layer, the reserve layer being constituted by a hydrophobic polymer matrix in which particles of the possibly unstable active compound are dispersed in oxidizing medium and particles of at least one water-absorbing agent, the reserve layer being anhydrous. It is also known from DE-A-42 10 165, a patch consisting of a silicone matrix containing a fat-soluble active, a water-soluble active and an oil that increases the penetration of the lipid-soluble active, this active being water-soluble in the form of particles, dispersed in the matrix. The present invention proposes a controlled release system comprising an anhydrous polymer matrix in which an oil is dispersed in the form of droplets, this matrix being intended to simultaneously release lipophilic active compounds and hydrophilic active compounds. The use of an anhydrous polymer matrix in which an oil is dispersed, has the advantage of being able to obtain a particularly flexible patch, intended to adhere to the non-planar skin surfaces, of large radius of curvature, and which is not annoying for areas of skin fold. Tests carried out by the applicant have shown that, in certain cases of the previous patches, the adhesion on the skin was difficult to secure, which is the case mainly when a relatively important portion of oil is incorporated. It has been found, in a completely surprising manner, that the addition to the matrix of a hydroabsorbent agent concurs to a significant improvement of the patch adhesion power of the invention. On the other hand, the Applicant has found that, by dispersing in a specific hydrophobic polymer matrix, a suitable amount of oil, in which a first lipophilic active compound had been dissolved, it was possible to obtain a patch comprising an anhydrous polymer layer, but still allowing excellent controlled release of a second powdery active compound of hydrophilic nature. The patch allows, in a completely surprising way, that the addition to the matrix of a hydroabsorbent agent leads to a significant improvement in the adhesion power of the patch of the invention. On the other hand, the Applicant has observed that, by dispersing in a specific hydrophobic polymer matrix, an adequate amount of oil, in which a first lipophilic active compound had been dissolved, it was possible to obtain a patch comprising an anhydrous polymer layer, but still allowing an excellent controlled release of a second powdery active compound of hydrophilic nature. The patch allows, mainly, the conditioning and the controlled administration of a group of skin-friendly and / or skin-repairing substances of lipophilic and hydrophilic nature, and mainly lipophilic or hydrophilic active substances that tend to inactivate each other, when they are in association. It has also been found in a completely surprising and unexpected way that it was impossible to condition in the same polymeric matrix one (or more) active hydrophilic compound (s), one or more active compound (s) ( s) lipophilic (s), and one or (several) oil (s). Thus, it was possible to carry out, for example, a stable association of particles of a water-soluble compound, unstable, in aqueous medium or in open air and / or of a fat-soluble active compound also unstable in aqueous medium or in open air, in an oil unsaturated, drying in the open air, without risk of degradation of the active compounds and without risk of oil hardening. Thus, the present invention relates to a pharmaceutical, cosmetic or dermopharmaceutical patch comprising a hydrophobic polymer layer, fixed on a support layer and containing: a) first particles of at least one water-soluble active compound, b) second oil particles, c) at least one fat-soluble active compound, characterized in that the polymer layer also contains third particles of a water-absorbing agent, dispersed homogeneously in the polymer layer. According to a first embodiment, the fat-soluble active compound is solubilized in the oil. According to another embodiment, the fat-soluble active compound is in the form of particles, in the form of powder or granules, dispersed in the polymer layer. The oil which can be used according to the invention can be chosen from the following oils, alone or in mezcal, among which may be mentioned: oils of animal, vegetable or mineral origin and especially animal or vegetable oils formed by fatty acid esters and of polyols, particulate liquid triglycerides, for example, sunflower, soybean, pumpkin, grape seed, sesame, hazelnut, pistachio, apricot, almond or avocado oils;
fish oils, sunflower tpcaprocaprylate, or vegetable or animal oils of formula R ^ COOR, represents the remainder of a higher fatty acid comprising from 7 to 19 carbon atoms t R_ represents a branched hydrocarbon chain containing 3 to 3 carbon atoms. at 20 carbon atoms, for example, Purcellm oil; wheat seed oil, calofile oil, sesame oil, coriander oil, safflower oil, passion fruit oil, rosehip oil, macadamia oil, fruit nuggets (grapes, currants, orange, kiwi), rapeseed oil, of copra, peanut, evening primrose, palm, castor, flax, jojoba, chia, olive or cereal seeds such as wheat seed oil, rice bran oil, charity oil; acetylglycerides, octanoates, decanoates or ricmoleates of alcohols or polyalcohols; triglycerides of fatty acids; of glycerides; paraffin oil, petroleum jelly, perhydrosqualene; fatty alcohols (stearyl alcohol, cetyl alcohol) and fatty acids (stearic acid) and their esters; the plialkyl (Ci-C.) siloxanes and mainly those of terminal groups tnmetilsililo, preferably those whose viscosity is lower than 0.06 pr / s, among which can be cited linear polydi ethosoloxanes and alkylmethylpolysiloxanes such as cetildi ethyl ketone (called CTFA) . Mention may also be made of partially fluorinated hydrocarbon oils or perfluorinated oils and especially perfluoropolyethers and perfluoroalkanes. The oily phase, ie, the oil droplets dispersed in the polymer layer, is present in a portion ranging from 0.1% to 30% by weight with respect to the total weight of the composition. Preferably, this percentage is between 5 and 25. When the compositions according to the invention are used for the cosmetic treatment of the skin or with a dermatological object, the active compound contained in the oily phase is chosen, more particularly, among the antioxidants, anti-free radicals, moisturizers, depigmenting, lipo-regulators, slimming, anti-acne, anti-psoriatic, anti-seborrheic, antihistaminic, anti-aging, anti-wrinkle, keratolytic, anti-inflammatory, refreshing, healing, vascular, antibacterial, antifungal, antiperspirant , skin conditioners, immunomodulators and nitrites.
Among the lipophilic active substances dissolved in the oily phase, which can be used for transdermal treatment in the context of the present invention, the following compounds can be mentioned as examples: Da-tocopherol, DL-α-tocopherol, Da-tocopherol acetate , DL-α-tocopherol acetate, ascorbyl palmitate, vitamin F and vitamin F glycerides, vitamin D, vit ian D ^, rethex, retic esters, reticulate palmetto, reticulate propionate, β-carotene, D- panthenol, farnesol, farnesyl acetate; jojoba and gooseberry oils rich in essential fatty acids; salicylic acid n-ochlanno-l-5 and its esters, salicylic acid and its esters; alkyl esters of α-hydroxy acids such as citric acid, lactic acid, glycolic acid; Asian acid, madecassic acid, asiaticoside, total extract of gotu kola; ß-glucirretinic acid, a-bisabolo, ceramides such as 2-oleo? lam? no-l, 3-octadecane; fitanotpol, phospholipids of marine origin rich in essentially polyunsaturated fatty acids, ethoxyquin; rosemary extract, melissa extract, quercetma, dried microalgae extract; the anti-flalamatopos, mainly steroidians, as well as the biostimulating agents such as certain hormones or lipid and / or protein synthesis compounds. The concentration of the lipophilic active compound in the oily phase that can be used depends on the nature of the vegetable oil used. Typically, this concentration may be from 0.01% to 201 weight based on the total weight of the oily phase. Arriving 1-to-case, the oily phase can comprise, in addition, lipophilic surfactants, for example sucrose distearate, diglyclopellate distearate, tetraglyceryl tristearate, decaglyceryl decastearate, diglyceryl monostearate, hexaglyceryl tristearate, decaglyceryl pentast stearate, sorbitan monostearate, tristearate sorbitan, diethylene glycol monostearate, glycerol ester and plamitic and stearic acids, polyoxyethylenated monostearate 2 OE (comprising oxyethylene units), glyceryl mono and dibehenate, pentaerythritol tetrastearate. The particles of one (or several) active compound (s), water-soluble (s), when the compositions according to the invention are used for the cosmetic treatment of the skin or with a dermatological purpose, are chosen from the active ingredients. hydrophilic used conventionally as antioxidants, anti-free radicals, moisturizing, depigmenting, lipo-regulating, slimming, anti-acne, anti-seborrheic, anti-aging, anti-wrinkle, keratolytic, anti-inflammatory, refreshing, healing, vascular protectors, antibacterials, antifungals, antiperspirants, deodorants, skin conditioners, immunomodulators and nutrients. The patches according to the present invention, the hydrophilic active compound, can be chosen, for example, between ascorbic acid and its biologically compatible salts, enzymes, antibiotics such as clmdamicin phosphate, tensor effect compounds such as powders, soybean or wheat proteins, a-hydroxy acids, and their salts, hydroxylated polyacids, sucrose and their derivatives, urea, amino acids, oligopeptides, water-soluble plant extracts, and yeasts, protein hydrolyses such as collagen and elastin, hyaluronic acid, mucopolysaccharides, vitamins B_, B, H, PP, panthenol, folic acid, acetilaslicilic acid, allantoin, glyceric acid, kojic acid, hydroquinone, etc. . Advantageously, the water-soluble active compound is present in the polymer layer in a proportion ranging from 0.2% to 20% by weight, based on the total weight of said layer. Preferably, the particles of the water-soluble active compound have an average size between 0.2 μm and 0.5 μm. According to an interesting aspect of the invention, it is possible to condition in the same matrix one (or several) active compound (s) hydrophilic (s), sensitive (s) to hydrolysis, one (or several) active compound (s) (s) lipophilic (s) sensitive to oxidation, and one (several) oil (s) sensitive to oxidation as well. Under these conditions, it is also possible to use a water-soluble active, incompatible with the fat-soluble active compound or with oil, in conventional topical preparations of the cream or lotion type. Furthermore, it is possible, for example, to make an association of vitamin C particles in an unsaturated oil containing vitamin A without the risk of degradation of the vitamins and without risk of oil polymerization.
Advantageously, the matrix forming the polymer layer may contain particles of at least one hydro-absorbing agent dispersed homogeneously in said matrix. In fact, upon contact of the moisture of the skin, the particles of the hydro-absorbent agent capture the water, thus favoring the solubilization of the solid, water-soluble active compound. In some way, by this "in situ" solubilization of the water-soluble active, its bioavailability is almost instantaneous, and any eventual interaction with the other compounds present in the polymeric layer is minimized. The moisture of the skin can play the role of a solubilizer of the water-soluble active substance, the more so as the support layer of the patch creates occlusive conditions. Among the hydro-absorbent agents that may be present in the hydrophobic polymer matrix in the dispersed state, there may be mentioned, preferably, the polyacrylates, cross-linked superabsorbents with a high water content, such as those marketed by the NORSOLOR Company under the name Aquakeep®, polyvinyl alcohol; carboxyvinyl polymers such as those commercialized by the GOODRICH Company under the names "Carbopol®"; semi-synthetic cellulose derivatives such as carboxymethylcellulose; natural substances such as starches, natural gums (guar gum, gum arabic, gum traitor), casein, phytocolloids (carrageenans, alginates, agar-agar), cotton fibers and gelatin. It is also possible to use a hydro-absorbent agent in the form of freeze-dried or atomized emulsion powder particles. Advantageously, the particles of the hydro-absorbing agent have an average size of between about 0.2 μm and about 1.5 mm. It is particularly important to use according to the invention the crosslinked polyacrylates "superabsorbents" whose presence in the dispersed state in the hydrophobic polymer matrix favors, after hydration, a better diffusion of the hydrophilic active compound. Thanks to the presence of these "superabsorbent" agents, a better adhesion of the patch on the skin is obtained, especially when a prolonged application is desired. The hydro-absorbent agent as defined above is preferably present in a proportion ranging from about 0.1% to about 30- by weight and, more particularly, ranging from 0.5% to 10% by weight relative to the total weight of the polymer layer. In the patches according to the present invention, the hydrophobic polymer matrix is, for example, based on a silicone polymer or a polyurethane of the polyurethane polyester or polyurethane polyether type. When the polymer matrix is based on a silicone polymer, the silicone prepolymer is preferably chosen from the linear organopolysiloxanes substituted on the silicon atom by groups chosen from an alkyl group of 1 to 6 carbon atoms, aryl or ar (alkyl) in C -C;), the terminal silicon atoms being trisubstituted. Such organopolysiloxanes are described mainly in US Pat. Nos. 2 541 137, 2 723 966, 2 863 846, 2 890 188, 2 927 907, 3 002 951, 3 035 016. Particularly preferred is a silicone prepolymer comprising The following units:
wherein: R represents an alkyl or alkoxy group containing from 1 to 7 carbon atoms, a vinyl or phenyl group, and in which n is chosen in the range from about 100 to about 5,000. Among the particularly preferred organopolysiloxanes according to the invention, mention may be made of those known under the names SILASTIC 382®, Q7-4635®, Q7-4650®, Q7-4735®, Q7-4750®, Q7-4765®, MDX 4- 4210® and DC 3.6486® marketed by the Dow Corning Company. The silicone prepolymer used is preferably crosslinked at moderate temperatures such as room temperature, using an acceptable biological crosslinking catalyst in the resulting polymer matrix and which is compatible with the active compound dispersed in the latter.
By crosslinking catalyst, it is understood, according to the present invention, the assignment of a crosslinking agent and a catalyst. When the silicone prepolymer carries hydroxy groups, such as terminal hydroxy groups, there may be mentioned, as a crosslinking agent, tetrapropoxysilane [Si- (O-CH2-CH2-CH3) 4] in association with a tin-based catalyst. When the silicone prepolymer carries vinyl groups, the latter can be crosslinked in the presence of a dimethyl silicone polymer in association with a catalyst such as a platinum-based catalyst. When the polymer matrix is based on a polyurethane, it is obtained from a prepolymer of the polyester-polyol or polyether-polyol type known in the state of the art. Among polyester-polyols, mention may be made of those obtained by reaction of bi- or tpfunctional alcohols on acids such as adipic acid, terephthalic acid and, more generally, any of the polyfunctional acids. Among the polyether polyols, mention may be made of those obtained by alkoxylation by reacting diols such as ethylene glycol or propylene glycol or polyols such as trimethylolpropane, glycerol, pentaepritol, sorbitol, etc., with oxides such as ethylene oxide, the propylene oxide or its mixture. The polyacidial agent for the formation of polyurethanes in an isocyanate or polusocyanate, in particular toluenediusocyanate, diphenylmethane-4,4'-dusocyanate, 1,5-naphthalenediocyanate, or isophorone-mono-succinate. The crosslinking catalyst or the polyaddition agent is preferably used in an amount such that crosslinking or polyaddition is not complete in order that the polymer layer itself has a satisfactory self-adhesive character so as to advantageously avoid that the support layer is finally coated with a layer of adhesive. Finally, in order to strengthen the strength of the elongation of the polymer matrix, the polymer layer may comprise a weft, constituted for example by a sheet of a perforated plastic material, of a sheet of non-perforated material, or of a non-stretchable mesh, the non-woven material being formed and the mesh of natural or synthetic fibers, such as polyamide, as described in French Patent No. 92 05623 (FR-A-2 620 914). The support layer or occlusive layer of the patches according to the present invention can be constituted by any suitable material impermeable to the active compounds contained in the adjacent polymer layer. The support layer not only has the function of supporting the polymer layer but also serves as a protective coating thereof. It can be of the same dimension as the polymer layer or larger dimension such that they extend beyond the periphery of the polymer layer and outward, so that the surface surrounding the polymer layer can receive eventually adhesive means. Suitable materials for the backing layer include high and low density polyethylene films, polypropylene, polyvinyl chloride, polyester films such as ethylene polyphthalate, ethylene vinyl acetate and polyurethane copolymers. . These materials can also be present in a layered form with at least one sheet of metal such as a sheet of aluminum. The support layer can be of any suitable thickness that provides the desired support and protection functions. Preferably, the thickness of the support layer is between about 0.2 mm and about 1.5 mm. The patches according to the present invention can also be protected by the presence of a separable or peelable protective layer adjacent to the polymer layer and / or for packaging in a suitable packaging, mainly impermeable to water and water vapor. When the polymer layer is protected by a separable protective layer, it is lifted at the time of use. It can be constituted by any material impermeable to the active compound, as well as any other component present in the polymer matrix. Among the materials that can be used, a sheet of siliconized paper or a sheet of thermoplastic material treated to make it anti-adherent, for example with the aid of a varnish, can be cited. Preferably, this separable protective layer is constituted by polyethylene. In a known way, the patches of the present invention can be cut according to a suitable contour corresponding to the area of the surface of the skin to be treated, for example in the form of a mask for application on the face, mainly for application on the contours of oos, on the bags under the oos, on the forehead. Of course, the patches according to the present invention can be cut out in any other form necessary for an application on a certain area of the body. In general, the size of a patch according to the invention is between 0.25 cm: and 500 cm. "Thus, for a patch intended for depigmentation of pigmented spots on the skin, it may present a small size, less than 1 cirr , while a slimming action patch can have a large surface, sufficient to cover a part of a thigh, for example, the patches constituted and cut in this way can be used, after the removal of the separable protection layer, on a The surface of the skin to be treated is applied directly to a skin, the perspiration water of which will provide the desired release of the active hydrophilic compounds, they can also be pre-numerated in the water for a time preferably comprised between approximately 5 and 30 seconds, or the skin after having moistened them previously, for example with the help of a sponge. of perspiration of the skin is sufficient to obtain the release of the hydrophilic active compound on the surface of the skin to be treated, from the hydrophobic polymer matrix containing it. In the patches an embodiment of the present invention, the polymer matrix constituting the polymer layer is prepared by intimate mixing under agitation of the silicone or polyurethane prepolymer, of the hydrophilic active compounds, and of the hydro-absorbing agent, the two in the form of particles, as well as the oil comprising in the dissolved state the lipophilic compounds mentioned above. The mixture obtained in this way is then added at a low temperature, generally at room temperature, either with crosslinking catalyst if the prepolymer is a silicone polymer, either an isocyanide or polusocyanate if the prepolymer is a polyester-polyol or a polyether polyol. The mixture is then introduced into a hopper and poured onto a polyethylene sheet, for example, which constitutes the separable or peelable protection film of the patch. Underneath the hopper is arranged a doctor blade that makes it possible to equalize the thickness of the polymer layer of the polymeric matrix, this thickness generally being between 0.1 mm and 12 mm. A weft sheet is then applied as defined above, then before calendering, a sheet of the backing layer or occlusive can also be a polyethylene sheet. The polymerization or polyaddition is preferably carried out at room temperature, in order not to deteriorate the active compound (s). Generally, the polymerization or polyaddition is completed after about 24 hours at room temperature. After calendering, and before the polymerization or polyaddition is complete, the composite structure obtained can be trimmed immediately into the desired shapes, which allows to obtain tight edges that avoid any spill phenomenon. The following examples make it possible to illustrate the present invention.
EXAMPLE 1
To 8 g of polyacrylate powder (Aquakeep® marketed by the NORSOLOR Company), 10 g of sweet almond oil containing 0.2 g of alltrans-retinol and 2 g of vitamin C microcpstalma were added. 43 g of organopolysiloxane DC3.6486® (marketed by DOW CORNING) was added. Under agitation at 1500 rpm, 1.7 g of Medical Grade Curmg Agent crosslinking catalyst was added and stirring was maintained for a few minutes. The product homogenized in this way was introduced into a hopper and spread with the help of a doctor blade in a layer of 0.8 mm thickness on a polyethylene sheet with a thickness of 200 μm. This sheet can be pre-treated on the surface to reduce its adhesion. On the polyethylene sheet thus coated, a weft constituted by a polyamide or polyethylene mesh comprising meshes with an opening of 1 mm and a thickness of 0.3 mm was applied. A film of polyethylene (without anti-adherent treatment) of 30 μm thickness constituting the support or occlusive layer of the patch was then applied, and the assembly was calendered. Thus, an assembly comprising a support or occlusive layer and a self-adhesive polymer layer formed by a partially cross-linked silicone polymer matrix was obtained, this assembly also comprising a separable protection layer. From this set, different patch shapes could be cut out according to the desired uses. The patches after trimming were then packaged in polyethylene sachets. During use, the patch, after removal of the separable protective layer, was applied directly on the contour of an eye, for example, for a period of about 30 minutes. After having removed the patch, it was visually verified that the outline of the o or treated with the help of this patch, had a remarkable appearance more smooth and more relaxed than the other untreated eye. This patch had a good adhesive power on the skin.
EXAMPLE 2
To 8 g of polyacrylate powder (Aquakeep® marketed by NORSOLOR Company), 12 g of castor oil containing 0.3 g of D-α-tocopherol and 2 g of microcpstammo sodium lactate were added.
43 g of organopolysiloxane DC3.6486® was added
(marketed by the DOW CORNING Company). Under agitation at 1,500 rpm, 1.7 g of Medical Grade Curing Agent crosslinking catalyst was added and stirring was maintained for a few minutes. A patch was made analogously to that of Example 1. After the application of this patch on the skin for 12 hours, a good adhesive power was still found. A conservation test at 45 ° C for 48 hours showed that neither castor oil nor tocopherol degraded.
EXAMPLE 3
To 8 g of polyacrylate powder (Aquakeep® marketed by the NORSOLOR Company), were added
g of jojoba oil, 0.6 g of ß-carotene and 15 g of hydroxyprolma microcpstalma. 43 g of organopolysiloxane DC3.6486 (marketed by DOW CORNING) was added. Under agitation at 1,500 rpm, 1.7 g of its Medical Grade Curing Agent crosslinking catalyst was added and the stirring was maintained for a few minutes. In a manner analogous to Example 1, a patch was made, whose action was repairing the photodeteporated, emollient and catalyzing skin. The adhesive power of this patch on the skin, evaluated after 12 hours, was satisfactory.
EXAMPLE 4
To 10 g of sesame oil containing 0.2 g of hexyl nicotmate, 1.5 g of urea and 0.5 g of caffeine powder were added. 43 g of organopolysiloxane DC3.6486® (marketed by DOW CORNING) was added. Ba or stirring at 1,500 rpm, 1.7 g of its Medical Grade Curing Agent crosslinking catalyst was added and stirring was maintained for a few minutes. A patch was made analogous to that of Example 1. After application for 15 minutes, this patch increased the vascular microcirculation of the skin and favored the metabolism of subcutaneous fats.
It is noted that in relation to this date, the best method known by the applicant to carry out the present invention, is the conventional one for the manufacture of the objects to which it refers. Having described the invention as above, the content of the following is claimed as property:
Claims (24)
1. patch characterized in that it comprises a hydrophobic polymer layer, fixed on a support layer and containing: a) first particles of at least one water-soluble active compound, b) second oil particles, c) at least one fat-soluble active compound, characterized in that the polymer layer also contains third particles of a hydro-absorbing agent dispersed homogeneously in the polymer layer.
2. Patch according to claim 1, characterized in that the liposoluble active compound is solubilized in oil.
3. Patch according to claim 1, characterized in that the fat-soluble active compound is in the form of particles, dispersed in the polymer layer.
4. Patch according to any of claims 1 to 3, characterized in that the hydro-absorbent agent is selected from cross-linked superabsorbent polyacrylates, polyvinyl alcohol, carboxyvinyl polymers, semi-synthetic derivatives of cellulose, starches, gums of guar, arabic or adragante, casein, phytocolloids, cotton fibers and gelatin.
5. Patch according to any of claims 1 to 4, characterized in that the hydro-absorbent agent is in the form of particles of a lyophilized or atomized emulsion powder.
6. Patch according to any of the preceding claims, characterized in that the hydro-absorbent agent is present in the polymer layer in a proportion ranging from approximately 0.1% to approximately 30% by weight relative to the total weight of said layer.
7. Patch according to any of the preceding claims, characterized in that the particles of the hydro-absorbent agent have an average size comprised between approximately 0.2 μm and approximately 1.5 mm.
8. Patch according to any of the preceding claims, characterized in that the oil is chosen from mineral, animal, vegetable or synthetic oils or their mixtures.
9. Patch according to any of the preceding claims, characterized in that the oil is present in the polymer layer in a proportion ranging from 0.1% to 30%, relative to the total weight of the polymer layer.
10. Patch according to any of the preceding claims, characterized in that the fat-soluble active compound is present in the polymer layer in a proportion ranging from 0.1% to 20 * by weight, with respect to the total weight of the oil.
11. Patch according to any of the preceding claims, characterized in that the fat-soluble active compound is selected from the following compounds: Da-tocopherol, DL-a-tocopherol, Da-tocopherol acetate, DL-a-tocopherol acetate, palmitate ascorbyl, vitamin F and glycerides of vitamin F, vitamin D, vitamin D, vitamin D, retinol, retinol esters, retinol palmitate, retinol propionate, β-carotene, D-panthenol, farnesol, farnesyl acetate; jojoba and gooseberry oils rich in essential fatty acids; salicylic acid and its esters, n-ochlane-1-salicylic acid and its esters, alkylesters of α-hydroxy acids such as citric acid, lactic acid, glycolic acid; Asian acid, adecásico acid, asiaticosido, total extract of centella asiatica; ß-glucirretinic acid, a-bisabolo, ceramides such as 2-oleo? lammo-l, 3-octadecane; fitanotpol, phospholipids of marine origin rich in essentially polyunsaturated fatty acids, ethoxyquin; rosemary extract, melissa extract, quercetma, dried microalgae extract; the steroid anti-inflammatopes.
12. Patch according to any of the preceding claims, characterized in that the active compound is present in the polymer layer in a proportion ranging from 0.2% to 20a by weight relative to the total weight of said layer.
13. Patch according to any of the preceding claims, characterized in that the water-soluble active compound is in the form of particles, whose average particle size is between 0.2 μm and 0.5 mm.
14. A patch according to any of the preceding claims, characterized in that the water-soluble active compound is chosen from the following compounds: ascorbic acid and its biologically compatible salts, enzymes, antibiotics, tensor effect compounds, a-hydroxy acids and their salts , hydroxylated polyacids, sucrose and its derivatives, urea, amino acids, oligopeptides, water-soluble plant extracts, and yeasts, protein hydolysics, hyaluronic acid, mucopolysaccharides, vitamins B, Be, H, PP , panthenol, folic acid, acetyloslylic acid, allantoin, glyceric acid, kojic acid, hydroquinone.
15.Parche according to any of the preceding claims, characterized in that the hydrophobic polymer layer is based on a silicone polymer or a polyurethane.
16. Patch according to any of the preceding claims, characterized in that it is self-adhesive.
17. Patch according to claim 1, characterized in that the polymer layer based on silicone polymer is obtained by crosslinking a linear organopolysiloxane substituted on the silicon atoms by groups chosen from an alkyl group of 1 to 6 carbon atoms, aryl or ar (C 1 -C 2 alkyl), the terminal silicon atoms being trisubstituted by an alkyl group of 1 to 6 carbon atoms.
18. Patch according to claim 15, characterized in that the silicone polymer comprises units: wherein R represents an alkyl or alkoxy group containing from 1 to 7 carbon atoms, a vinyl or phenyl group, and in which n is selected in the range from about 100 to about 5,000.
19. A patch according to claim 18, characterized in that the polymer layer based on a polyurethane is obtained by polyaddition of a polyester polyol or a polyether polyol in the presence of an isocyanate or polyisocyanate chosen from toluene diisocyanate, 4,4 '. -difenildiisocianato, the 1, 5-naf alendiisocianato, and the isoforonadiisocianato.
20. Patch according to any of the preceding claims, characterized in that it also contains a weft interleaved between the polymer layer and the support layer.
21. Patch according to claim 20, characterized in that the weft is chosen between a sheet of a perforated plastic material, a non-woven sheet of natural or synthetic fibers and a non-stretchable mesh of natural or synthetic fibers.
22. Patch according to any of the preceding claims, characterized in that the thickness of the polymer layer is between approximately 0.1 mm and 12 mm.
23. Patch according to any of the preceding claims, characterized in that the support layer is constituted by a polymer selected from high and low density polyethylenes, polypropylenes, polyvinyl chloride, ethylene and vinyl acetate copolymers, polyesters and the polyurethanes.
24. Patch according to any of the preceding claims, characterized in that the thickness of the support layer is between approximately 0.2 mm and 1.5 mm.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9704498 | 1997-04-11 |
Publications (1)
Publication Number | Publication Date |
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MXPA98002825A true MXPA98002825A (en) | 2000-07-01 |
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