DE10317982A1 - Use of a molded body comprising a nonprotein gelling agent for external application, especially cosmetic or therapeutic - Google Patents

Abstract

Molded body comprising a nonprotein gelling agent, optionally one or more active ingredients and optionally one or more auxiliary agents is used for external application, is new. Independent claims are also included for: (1) molded body comprising at least 10 %, by weight of a nonprotein gelling agent having, as a 1 % solution or suspension in water at 20 [deg]C and pH 6-8, a viscosity of less than 2000 mPas, 0.000001-50 %, by weight of one or more active ingredients, 0.1-70 %, by weight of one or more auxiliary agents and up to 20 %, by weight water; (2) combination of at least one molded body as above and at least one aqueous solution containing one or more active ingredients and/or auxiliary agents in a matching spatial arrangement.

Description

The The invention relates to the use of a shaped body containing at least a scaffold, where Proteins are excluded, possibly one or more active substances and optionally one or more auxiliaries for external use, a process for the production of the moldings mentioned and new moldings.

From the German patent specifications DE 42 01 1 72 . DE 42 01 1 73 such as DE 42 01 179 pellets for pharmaceutical or cosmetic use are described which have scaffolders based on proteins. The pellets are used in particular for the manufacture of oral pharmaceutical formulations. The pellets are produced by dropping dispersions of the protein scaffolders and optionally cosmetic or pharmaceutical active ingredients into cryogenic inert liquids, preferably liquid nitrogen, and then separating the frozen pellets and freeze-drying them. In order to form pellets under these conditions, however, the presence of protein scaffolders, in particular collagen or collagen derivatives, is necessary, since only the protein scaffolders mentioned can form stable pellets under these conditions. This is probably related to the special intermolecular interactions of the protein molecules.

The Size of after pellets produced in the aforementioned German patent specifications specified in the general part of the descriptions with 0.2 to 12 mm. In the examples, however, the maximum size achieved is only 4 mm. This is an average size, i.e. the pellets are subject more or less large fluctuations in size.

In particular for the outer cosmetic However, relatively large moldings of uniform shape and application are used Size preferred. The end user can easily handle such molded articles. Powder, or small pellets or irregularly shaped articles for this Usually unsuitable purposes. One strives to form one to provide such a size which allow one dosage form to be used per application. Also convey larger moldings that e.g. can be designed in color, also a stronger aesthetic Impression.

The Use of protein scaffolders is also in some cases not preferred. Some end users are increasingly using the application purely herbal products, especially in cosmetics. The reasons therefor result, among other things, from fundamental, ethical considerations.

The Protein processing usually still requires complicated processes Preparation steps. Furthermore, the properties of the protein scaffolders for external use on the skin in its range of properties in many cases limited, because they are always composed of the same amino acids.

It there is therefore an increasing desire for cosmetic or pharmaceutical Formulations, in particular moldings for external use, which are not based on protein. However, if you want scaffolders on a vegetable basis Basis, such as Alginates, according to the in the above-mentioned patents process used, it is surprising determined that in this way no shaped bodies with regular shapes, especially in sufficient size and with sufficient solubility, like you for the external application are required.

Numerous publications are concerned with the production of oral formulations, the production of which involves a freeze-drying step. So are from the EP-A-0352190 compositions consisting of solid and porous unit forms are known which comprise micro- or nanoparticles. These are manufactured, among other things, in such a way that pastes are placed in cavities of a mold and then lyophilization is carried out. The task of EP-A-0352190 was to find oral formulations with a taste mask that would quickly dissolve in water. A topical application of the formulations is not mentioned. Similarly, the EP-A-0399902 Formulations produced by freeze-drying, which also serve to provide taste-masked, rapidly soluble pharmaceutical formulations. From the US-A-4758598 formulations produced by freeze-drying are known which are also used exclusively for oral use. From the US-A-4079018 soluble carrier materials for the administration of medicaments for oral use are known. From the US 4,695,463 Controlled release delivery systems for oral administration are described. Furthermore are from the EP-A-0412449 Freeze-dried compositions are known, but do not have a regular geometry. However, none of the above documents discloses the possibility of producing relatively large-sized, regular shaped articles which are easy to dissolve on the skin when used externally and are able to act as active substance carriers.

The The object of the present invention was therefore a new one Use of molded articles containing active ingredients, the scaffolders to provide, which are not based on proteins, for external use. The moldings should be relatively large adequate cohesion, i.e. mechanical strength, have to be regularly shaped, at loosen the application on the skin easily and become a pleasant one feeling of use to lead. Furthermore, these moldings should be suitable, various active ingredients such as cosmetic Active substances and therapeutic or pharmaceutical active substances and as a carrier therefor act.

The The invention thus provides the use of a shaped body, containing at least one scaffolding agent, with the exception of proteins, possibly one or more Active substances and optionally one or more auxiliary substances for external use.

Under a molded body In the sense of the invention one understands a regularly shaped geometric Body, e.g. especially spheres, cuboids, pyramids, stars but also natural ones Shaped moldings such as. those in the form of animals, e.g. Marine animals like e.g. Starfish, seafood, such as mussels, etc. plants and parts of plants, such as leaves etc. According to the process for producing the used according to the invention moldings all of these forms are accessible, According to the invention comprises a plurality of the shaped bodies mentioned in a container. Also it can be a mixture of moldings of different geometries act. The moldings can be individually packaged. However, it is particularly preferred in cosmetic application, a plurality of the shaped bodies in contact with one another in a container in front.

The volumes of the moldings used are not limited per se due to the method of their production. The volumes are preferably at least about 0.1 cm ³ , preferably 0.3 cm ³ , more preferably at least about 0.5 cm ³ , even more preferably at least about 0.8 cm ³ . The volumes used are expediently restricted up to about 6 cm ³ , preferably up to about 5 cm ³ , more preferably up to about 4 cm ³ . The size of the moldings is determined, inter alia, by the location of the external application of the moldings. For example, use on larger areas of the body or on the hair (e.g. direct application of the moistened molded articles on the back, etc., or use as a bath additive) enables the use of larger molded articles, whereas smaller articles (e.g. cheek, etc.) use smaller molded articles are preferred.

The Diameter of a shaped body (maximum distance between two points in a molded body of any Geometry) is conveniently included at least about 3 mm, preferably at least about 5 mm, more preferred at least about 7 mm, more preferably at least about 8 mm to towards expedient about 60 mm, preferably about 50 mm, more preferably about 40 mm, more preferably about 30 mm.

On particularly preferred molded body has a substantially spherical geometry, the Ball diameter between 3 to 30 mm, preferably between 5 and 20 mm, more preferably between 7 and 15 mm, more preferably between 8 and 13 mm.

The molded body used according to the invention contains at least one scaffold former, with the exception of proteins. The scaffolders are generally so-called hydrocolloids, ie (partially) water-soluble, natural or synthetic polymers which form gels or viscous solutions in aqueous systems. The scaffolders are appropriately selected from polysaccharides or synthetic polymers. The scaffolding agent is preferably selected from the group of the polysaccharides. Polysaccharides include, for example, homoglycans or heteroglycans, such as alginates, especially sodium alginate, carrageenan, pectins, tragacanth, guar gum, locust bean gum, agar agar, gum arabic, xanthan, natural and modified starches, dextrans, dextrin, maltodextrins, chitosan , Glucans such as β-1,3-glucan, β-1,4-glucan such as cellulose, mucopolysaccharides such as hyaluronic acid etc. Synthetic polymers include for example: cellulose ethers, polyvinyl alcohol, polyvinyl pyrrolidone, synthetic cellulose derivatives such as methyl cellulose, carboxy cellulose, carboxymethyl cellulose Cellulose esters, cellulose ethers such as hydroxypropyl cellulose, polyacrylic acid, polymethacrylic acid, poly (methyl methacrylate) (PMMA), Polymethacrylate (PMA), polyethylene glycols etc. Mixtures of several framework builders can also be used. Alginates are particularly preferred according to the invention, and sodium alginate is particularly preferred. Low-viscosity scaffolders are preferred, in particular calcium-free sodium alginates (sodium alginate with a calcium content <3% by weight, more preferably <2% by weight, still more preferably <1.5% by weight), ie such scaffolders which preferably have a viscosity of less than 2000 mPas, more preferably less than 1000 mPas, most preferably less than 100 mPas (ie a solution of 1 g of the framework builder in 99 ml of distilled water (1% solution w / w) at 20 ° C and a pH of 6-8 has a viscosity of less than 2000, 1000 or 100 mPas). The use of such low-viscosity scaffolders, such as sodium alginate, is preferred on the one hand due to the production process, on the other hand, the use of such low-viscosity scaffolders leads to easier solubility of the formulation or, when water is added, to a higher rate of disintegration or dissolution and thus for easier spreadability on the skin. In particular, the use of low-viscosity alginate types can lead to a higher dissolution rate of the moldings used according to the invention.

The polysaccharides preferably used according to the invention as scaffolders advantageously have average molar masses of suitably about 10 ³ to about 10 ⁸ , preferably about 10 ⁴ to 10 ⁷ .

The framework former are kind to the skin and lead preferably when used on the skin to form a film, the one protective Has function.

To clarify, should still be mentioned that the wording "scaffolding, with the exception of proteins, "im Not the presence of protein-based active substances, like enzymes, hormones etc.

The used according to the invention moldings optionally contain one or more active ingredients, preferably at least one active ingredient. Active ingredients include cosmetic ones in particular or therapeutic or pharmaceutical active substances suitable for external use on. Preferably contains the one used according to the invention moldings at least one cosmetic and / or pharmaceutical active ingredient. Accordingly the moldings used according to the invention are preferred cosmetic or therapeutic agents. Cosmetic moldings or Shaped body produced using cosmetic active ingredients The meaning of the invention are essentially means in the sense of the food and Consumer Goods Act (LMBG), i.e. substances or preparations made of substances intended for this are, externally on people for cleaning, care, or to influence the appearance or body odor, or to be used to impart smell impressions, unless, for the most part are intended to be diseases, ailments, physical damage or pathological ailments to alleviate or eliminate. In this sense it is about the used according to the invention cosmetic moldings for example about bath preparations, Skin washing and cleaning agents, skin care products, in particular facial skin care products, Eye cosmetics, lip care products, nail care products, foot care products, Hair care products, in particular shampoos, hair conditioners, hair softener etc., light stabilizers, skin tanning agents, Depigmenting agents, deodorants, antihydrotics, hair removal agents, Insect repellents etc. or such agents in combination.

Examples of cosmetically optionally also, for example, dermatological, therapeutically active compounds include: antiacne agents, antimicrobial agents, antiperspirant agents, astringent agents, deodorant agents, depilatory agents, skin conditioning agents, skin-smoothing agents, agents for increasing skin hydration such as, for. As glycerin or urea, sunscreen, keratolytics, free radical scavengers, antiseborrhoea, antidandruff agents, antiseptic agents, agents for treating the signs of aging and / or agents that modulate the differentiation and / or proliferation and / or pigmentation of the skin, vitamins such as vitamin C, active substances with an irritating side effect, such as alpha-hydroxy acids, β-hydroxy acids, alpha-keto acids, β-keto acids, retinoids (retinol, retinal, retinoic acid), anthralines (dioxyanthranol), anthranoids, peroxides (especially benzoyl peroxide), minoxidil , Lithium salts, antimetabolites, vitamin D and its derivatives; Catechins, flavonoids, ceramides, fatty substances such as mineral oils, such as paraffin oils or petroleum jelly oils, silicone oils, vegetable oils such as coconut oil, sweet almond oil, apricot oil, corn oil, jojoba oil, olive oil, avocado oil, sesame oil, palm oil, eucalyptus oil, rosemary oil, lavender oil, lavender oil, lavender oil, lavender oil, lavender oil, lavender oil, lavender oil Cardamom oil, orange blossom oil, soybean oil, bran oil, rice oil, rapeseed oil and castor oil, wheat germ oil and vitamin E isolated therefrom, evening primrose oil, vegetable lecithins (e.g. soy lecithin), sphingolipids / ceramides isolated from plants, animal oils or fats such as tallow, lanolin, butter oil, fatty acid esters Esters of fatty alcohols and waxes with a melting point corresponding to the skin temperature (animal waxes, such as beeswax, carnauba wax and candelilla wax, mineral waxes, such as microcrystalline waxes, and synthetic waxes, such as polyethylene or silicone waxes), and all for cosmetic purposes suitable oils, as mentioned, for example, in the CTFA treatise, Cosmetic Ingredient Hand-Book, 1st Edition, 1988, The Cosmetic, Toiletry and Fragrance Association, Inc., Washington, polyunsaturated fatty acids, essential fatty acids (e.g. gamma-linolenic acid ), Enzymes, coenzymes, enzyme inhibitors, hydrating agents, skin-calming agents, detergents or foam-forming agents, and inorganic or synthetic matting fillers, abrasive agents.

Farther can Plant active ingredient extracts or extracts obtained therefrom or Individual substances mentioned become. Generally, the plant active ingredient extract is usually selected from the group consisting of solid plant extracts, liquid plant extracts, hydrophilic plant extracts, lipophilic plant extracts, individual Plant ingredients; and their mixtures, such as flavonoids and their aglyka: rutin, quercetin, diosmin, hyperoside, (neo) hesperidin, Hesperitin, ginkgo biloba (e.g. ginkoflavone glycosides), crataegus extract (e.g. oligomeric procyanidins), buckwheat (e.g. rutin), Sophora japonica (e.g. rutin), birch leaves (e.g. quercetinglycosides, hyperoside and rutin), elderflowers (e.g. Rutin), linden flowers (e.g. essential oil with quercetin and farnesol), St. John's wort oil, (e.g. olive oil extract), Calendula, arnica (e.g. oily extracts of the flowers with essential oil, polar excerpts with flavonoids), lemon balm (e.g. flavones, essential oil); Immune stimulants: Echinacea purpurea (e.g. alcoholic extracts, Fresh plant juice, pressed juice), electherococcus senticosus; Alkaloids: Rauwolfia (e.g. Prajmalin), evergreen (e.g. Vincamine); other phytopharmaceuticals; Aloe, horse chestnut (e.g. aescin), garlic (e.g. garlic oil), Pineapple (e.g. bromelaine), ginseng (e.g. ginsenosides), milk thistle fruits (e.g. extract standardized on silymarin), butcher's broom root (e.g. ruscogenin), Valerian (e.g. Valepotriate, Tct.Valerianae), Kava-Kava (e.g. Kavalactone), Hop flowers (e.g. Hop bitter substances), extr.passi-florae, gentian (e.g. ethanol.extract), anthraquinone-containing drug extracts, e.g. Aloe-containing aloe vera juice, pollen extract, algae extracts, Licorice root extracts, Palm extract, galphimia (e.g. mother tincture), mistletoe (e.g. aqueous ethanol). Extract), phrosterols (e.g. beta-sitosterol), woolen flowers (e.g. aqueous alcohol). Extract), Drosera (e.g. liqueur wine extract), Sea buckthorn fruit (e.g. juice or sea buckthorn oil obtained from it), marshmallow root, primrose root extract, Fresh plant extracts from mallow, comfrey, ivy, horsetail, Yarrow, plantain (e.g. pressed juice), nettle, celandine, Parsley; Plant extracts from Norolaena lobata, Tagetes lucida, Teeoma siems, Momordica charantia, and aloe vera extracts.

preferred cosmetic active ingredients are natural and synthetic moisturizing factors such as B. glycerin, urea and ceramides, skin protection agents, skin whiteners, vitamins, antioxidants, so-called antiaging agents, anti-irritants, sunscreens, Etc.

in the Difference from those described above essentially in the Shaped bodies used in cosmetics are the therapeutically used shaped bodies (medicinal products) to those that have at least one pharmaceutical or therapeutic in particular also contain dermatological active ingredient and which in Are intended, among other things, to: Diseases, suffering, body damage or to heal, alleviate or prevent pathological symptoms. Such Agents or active ingredients are for the external application determined, which are skin-active ingredients but also transdermal Active substances can act. For example, they include; medium for the treatment of skin diseases, external analgesics, z. B. dextropropoxyphene, pentazocin, pethidine, buprenorphine; Antirheumatic / anti-inflammatory drugs (NSAID), e.g. B. indomethacin, diclofenac, naproxen, ketoprofen, ibuprofen, Flurbiprofen, salicylic acid and derivatives such as acetylsalicylic acid, oxicams; Steroid hormones, e.g. B. betamethasone, dexamethasone, methylprednisolone, Ethinyl estradiol, medroergotamine, dihydroergotoxin; Gout remedies, z. B. Benzbromaron, Allopurinol; Dermatics externa, including antibacterial Agents, antifungals, antiviral agents, anti-inflammatory Active ingredients, antipruritic active ingredients, anesthetic active ingredients, e.g. B. benzocaine, corticoids, acne agents, anti-parasitic agents; externally applicable hormones; Veins therapeutics; Immunosuppresives etc. all for the external Application.

preferred therapeutic agents are analgesics, e.g. Immunosuppressants, hormones, Agents for the treatment of skin diseases, such as neurodermatitis, of utopian dermatitis etc., and anti-herpes remedies.

Also the scaffolding, in particular the polysaccharides can have certain therapeutic effects Have effects (this is how the preferred scaffolding agent works (Sodium) alginate to some extent antiviral), but they are no active substances in the sense of the invention.

The moldings used according to the invention may also contain one or more auxiliaries. Auxiliaries include: surface-active agents in addition to the above-mentioned detersive surfactants, such as dispersants, emulsifiers, etc., fillers, pH adjusting agents, such as buffering agents, stabilizers, cosolvents, pharmaceutically and cosmetically customary or other dyes and pigments, preservatives, plasticizers, lubricants or lubricants , etc. This is a particularly preferred auxiliary Squalane.

The Shaped body according to the invention serve external application in humans or animals. The external application takes place so that the molded body according to the invention with water or aqueous solution, the contains one or more active substances and / or auxiliary substances, moistened or is dissolved in water. Depending on the amount of liquid and solubility of the molded material that are used, the molded body can be completely dissolved to form a solution or disintegrate to form a gel. If the molded body according to the invention in a larger amount of water solved, it is usually a bathing application and this application is according to the invention in external use contain. However, the application is preferably carried out in such a way that the moldings are also used a small amount of water or an active and / or auxiliary solution Formation of a gel can be moistened directly on the skin or in the hair and be rubbed or massaged in there.

The The present invention also relates to a combination containing at least one of the moldings used according to the invention and at least one aqueous Solution, which contains one or more active substances and / or auxiliary substances, in one belonging together, spatial Arrangement (application package, set, kit-of-parts etc.). With the drug solution can e.g. for solutions of volatile Active ingredients and / or auxiliary substances act on the basis of the manufacturing process should not be introduced into the shaped body by freeze-drying or can, such as. certain proportions of essential oils, perfumes Etc.

ever according to the quantity and type of active substances present and / or contains auxiliaries the one used according to the invention moldings preferably at least about 10% by weight of the scaffold based on the Total weight of the molded body, preferably at least about 15, more preferably 30, more preferably at least about 50% by weight up to 100% by weight of the scaffolding agent, especially polysaccharides, like sodium alginate.

The moldings generally also contain residues of water. Depending on the type of Active ingredient (hydrophilic, hydrophobic), the water content can be up to 20% by weight. The water content can change after manufacture of the shaped body change by freeze-drying during storage, usually increase. Prefers is the water content of the molded body after production at about 2 to 15, more preferably 2 to 12 Wt .-%.

The used according to the invention moldings contain from 0 to 85% by weight, preferably from 0.000001% by weight up to 50% by weight of one or more active ingredients. The proportions hang very much depends on whether the active ingredient is a cosmetic or therapeutic agent, in particular the therapeutic Active substances may come in very small quantities.

The moldings contain from 0 to 85% by weight of one or more auxiliary substances. The moldings can Contain 0.1 to 70% by weight of the auxiliaries, more preferably 5 up to 60% by weight of auxiliaries.

In particular in use with an additional drug solution are also shaped bodies applicable only from the hydrophilic scaffold and if necessary additional Auxiliary materials exist.

On preferred excipient is squalane. This is a cosmetic oil. The squalane has a surprising effect improved solubility despite its hydrophobic nature of the shaped body what the external application relieved on the skin. Squalane also has skin care Effects, although not an active ingredient in the sense of the invention. In a preferred embodiment contains the molded body of about 10 to 60% by weight squalane (can be determined by extraction with diethyl ether using the method of Weibull Stoldt in Official Collection of Examination Procedures ASU according to §35 LMBG) The classification of the substances mentioned above into the category the auxiliary substances in the context of the present invention do not exclude that these auxiliaries also have certain cosmetic and / or therapeutic Can have effects.

• – mindestens 10 Gew.-% eines oder mehrerer Gerüstbildner, insbesondere Polysaccharide, wie Natriumalginat, insbesondere calciumfreies Natriumalginat, dessen 1-gewichtsprozentige Lösung oder Suspension in Wasser (1 g in 99 ml Wasser bei 20°C, pH 6–8) bevorzugt eine Viskosität von weniger als 2000, bevorzugt weniger als 1000, besonders bevorzugt weniger als 100 mPas aufweist,
• – 0,000001 Gew.-% bis zu 50 Gew.-% eines oder mehrerer Wirkstoffe,
• – 0,1 bis 70 Gew.-% Gew.-% eines oder mehrerer Hilfsstoffe, wie insbesondere Squalan, sowie
• – bis zu 20 Gew.-%, bevorzugt bis zu 15 Gew.-% Wasser,

mit der Maßgabe, dass der Formkörper keine Proteine als Gerüstbildner aufweist.A particularly preferred shaped body contains:

• - At least 10% by weight of one or more scaffolders, in particular polysaccharides, such as sodium alginate, in particular calcium-free sodium alginate, whose 1% by weight solution or suspension in water (1 g in 99 ml of water at 20 ° C., pH 6-8) preferably one Has a viscosity of less than 2000, preferably less than 1000, particularly preferably less than 100 mPas,
• - 0.000001% by weight up to 50% by weight of one or more active substances,
• 0.1 to 70% by weight of one or more auxiliaries, such as in particular squalane, and
• Up to 20% by weight, preferably up to 15% by weight of water,

with the proviso that the shaped body has no proteins as scaffolders.

• – eine Dichte von 0,005 g/cm³ bis zu 0,8 g/cm³ bevorzugt 0,01 g/cm³ bis zu 0,8 g/cm³,
• – ein Volumen von 0,1 cm³ bis 6 cm³, bevorzugt 0,8 cm³ bis 6 cm³, und
• – einen Durchmesser (maximaler Abstand zwischen zwei Punkten des Formkörpers) von mindestens 6 mm auf.

The shaped body used according to the invention, such as, for example, the composition mentioned above, containing at least one scaffold former, with the exception of proteins, optionally has one or more active ingredients and optionally one or more auxiliaries for external use,

• A density of 0.005 g / cm ³ up to 0.8 g / cm ^3, preferably 0.01 g / cm ³ up to 0.8 g / cm ³ ,
• A volume of 0.1 cm ³ to 6 cm ³ , preferably 0.8 cm ³ to 6 cm ³ , and
• - A diameter (maximum distance between two points of the molded body) of at least 6 mm.

The used according to the invention moldings make porous moldings with homogeneous distribution of the ingredients (apart from possibly existing coatings).

The dissolution rate the used according to the invention Moldings, measured according to a method for measuring the “disintegration time of tablets and capsules "with a test apparatus according to PharmEU is preferably less than 4 Minutes, more preferably less than 1 minute (for molded articles with 9 mm diameter lies after <20 Seconds of complete hydration without a recognizable core).

• (a) Herstellen einer Lösung oder Suspension, die mindestens ein Biopolymeres, ggf. einen oder mehrere physiologisch aktive Wirkstoffe sowie ggf, einen oder mehrere Hilfsstoffe enthält,
• (b) Giessen der Lösung in eine Form,
• (c) Gefrieren der Lösung in der Form und
• (d) Gefriertrocknung der gefrorenen Lösung unter Bildung des Formkörpers.

The moldings used according to the invention can be obtained by a process which comprises the following steps:

• (a) preparing a solution or suspension which contains at least one biopolymer, possibly one or more physiologically active substances and, if appropriate, one or more auxiliary substances,
• (b) pouring the solution into a mold,
• (c) freezing the solution in the mold and
• (d) Freeze-drying the frozen solution to form the shaped body.

Possibly can between these steps further steps are carried out in particular it is possible after step (c), machining the surface of the shaped bodies mechanical processing or by spraying with e.g. Drug solutions, dye solutions and / or the dissolution rate to carry out modifying means. The molded body preferably has however no surface coating on and is homogeneous, in the sense of an equal distribution of the components over the entire molded body built up.

Appropriately in the preparation so that you first have an aqueous solution of the scaffold manufactures and then optionally one or more active ingredients or one or more Adds auxiliaries and mixes.

In order to the molded body sufficient mechanical stability can be imparted it required the solution or suspension a certain concentration of the scaffold having. This concentration depends Naturally depends on the type of scaffold used. It is expedient to be at least about 0.1% by weight, based on the total amount of the solution, preferably at least about 0.25% by weight up to about 20% by weight, preferably less than 15 % By weight, more preferably less than 10% by weight (weight of the framework builder based on the total weight of the solution). Higher concentrations are not preferred, because then the viscosity of the solution becomes too high, and thereby the processability of the solution is difficult. The amount of that contained in the solution or suspension Scaffold-forming agent significantly influences the density (weight of the molded body based on the volume of the geometric shape of the shaped body) of the obtained Molding. The density is in turn an important variable for the rate of dissolution of the molded body Moisten with water or an active and / or auxiliary solution. ever higher the Concentration of the scaffolding agent in the solution is the higher the density (the lower the degree of porosity) of the shaped body and vice versa. From the point of view of density / degree of porosity or the dissolution rate becomes the concentration of the scaffold preferred in the solution or suspension prepared in step (a) selected from an area from about 0.25% to about 15% by weight. The concentration of the preferred used scaffolding Sodium alginate is preferably from 0.5 to 5% by weight, preferably 1 to 4% by weight.

The densities of the moldings used according to the invention are advantageously approximately 0.01 g / cm ³ up to 0.8 g / cm ³ , preferably about 0.015 g / cm ³ up to 0.5 g / cm ³ , preferably about 0.02 g / cm ³ up to 0.1 g / cm ³ . The term density, as used in the present case, denotes the weight of the shaped body in relation to the volume of the outer geometric shape of the shaped body.

The Weight of the individual moldings depends of course its size. in the the weight of the individual molded articles is generally included about 10 to 200 mg, preferably 20 to 100 mg. For example, balls of 1 2 mm in diameter a weight in the range of preferably 20 to 80 mg, more preferably 30 to 60 mg.

For bullets other preferred diameters are calculated.

The Preparation of the solution, which is subjected to freeze drying is preferably carried out in such a way that first a solution of the scaffold builder is produced and then in the solution of the scaffolders any active substances or auxiliaries present are incorporated become. If oil-soluble active ingredients are used, these are preferred in oils optionally used as auxiliary substances (in particular Squalane) solved and subsequently the solution of the scaffold builder added. This method of production has the advantage that it is stable solutions or form suspensions. No emulsifiers are needed, and it takes place during no phase separation of the solution or suspension during processing when using oil-soluble or oily auxiliary or active ingredients instead.

The solution so prepared is then poured into a mold which has the cavities corresponding to the shaped bodies desired have geometric shapes. The shape preferably consists of rubber, silicone rubber, vulcanized rubber (rubber) etc. Preferred are rubber molds. The molding materials can optionally coated. The cavities of the molded body, in the the solution is infused, generally have the shape of the desired molding on. That is, the volume of the cavity is essentially the volume the later obtained molded body equivalent.

There the volume of in the cavities filled solutions or suspensions during freezing increases (density difference between Water and ice), the cavities are usually not completely filled. It become complete in this way symmetrical shaped body receive. This is for example after the drop-in method in cryogenic solutions (as in liquid Nitrogen) not possible because there are asymmetrical temperature distributions, so that there are always more or less strong deviations from a regular form result. Such irregularly shaped moldings are however not in the field of cosmetic end products he wishes. This usually means that this is done using the dropping method manufactured molded body require mechanical post-processing, which after the process as used in the invention is not required. In the case of the dropping process moldings Such post-processing becomes more and more necessary with increasing volume of the molded body, since there are clear external irregularities in this process occur that appear more particularly in the case of larger moldings.

To filling the solution into the cavities the form becomes the solution or suspension frozen. The solution can be cooled or frozen done in any way. Cooling is preferably carried out at the used according to the invention Cold air blowing process. Other methods include e.g. immersing the molds in liquid Gases, e.g. immersion in liquid nitrogen. The cooling rate influences the size of the educated Ice crystals. These in turn influence the pore size distribution of the formed body. Become a few big ones Crystals formed, the molded body has few large pores on. If many small crystals are formed, the shaped body has many small pores. The crystals become smaller the higher the cooling the solution or suspension.

The Freezing temperature that is required depends among other things on how much the freezing point is lowered by those contained in the solution Active substances or auxiliary substances. The temperature is expediently below the freezing point of water to the temperature of liquid nitrogen (-196 ° C). Prefers the freezing temperature is about –20 down to –80 ° C. After this Freeze the solution or suspension become the shaped body removed from the mold and possibly subjected to post-processing. Post-processing can be done mechanically, e.g. through a surface treatment (Grinding, roughening etc.). Furthermore there is a coating treatment possible such as. spraying with a saline solution, e.g. to form less soluble Forms of scaffolders, especially when using sodium alginate and salt solutions more valuable Metal ions. A color solution can also be applied superficially to the frozen moldings that are too colored moldings leads.

The moldings are then subjected to freeze drying. Freeze drying can be carried out in a manner known per se, as described, for example, in DE 4328329 C2 or DE 4028622 C2 ,

The Invention is illustrated by the following examples.

EXAMPLES

Example 1 (sodium alginate ball, Diameter 12 mm)

Basic version only alginate 2 g Protanal LF 10/60 (Na alginate) 98 g water

2 g of Na alginate (Protanal LF 10/60) are added to 98 g of water with stirring (2% solution w / w). The homogeneous (degassed) mixture is poured into molds, frozen out with air blowing, removed from the mold and then in freeze-dried in a known manner. About 110 balls are obtained.

Example 2 (sphere, diameter 12 mm)

Alginate with squalane 2 g Protanal LF 10/60 (Na alginate) 1 g Squalane 97 g water

2 g of Na alginate are stirred added to 97 g of water and mixed homogeneously. Then will with stirring 1 g of squalane was added. The homogeneous (degassed) mixture is poured into molds, frozen out with blowing air, from the Formed and then freeze-dried in a manner known per se.

Example 3 (sphere, diameter 9 mm)

Alginate with squalane and glycerin 2.0 g Protanal LF 10/60 (Na alginate) 0.9 g squalane 0.6 g glycerin 96.5 g water

2 g of Na alginate are stirred dissolved in 96.5 g of water. Subsequently is stirring a mixture of 0.9 g squalane and 0.6 g glycerol was added. The homogeneous (degassed) mixture is poured into molds, under Air blown out frozen, taken out of the mold and then in freeze-dried in a known manner.

Example 4: (sphere, diameter 12 mm)

Alginate with squalane and urea 2.0 g Protanal LF 10/60 (Na alginate) 1.0 g squalane 1.0 g urea 96.0 g water

2 g of Na alginate and 1.0 g of urea are dissolved in 96.0 g of water with stirring. Then 1.0 g of squalane is added with stirring. The homogeneous (degassed) mixture is poured into molds, frozen out with blowing air, removed from the mold and then in a manner known per se freeze-dried.

Example 5: (sphere, diameter 12 mm)

Alginate with squalane and ceramides 2.0 g Protanal LF 10/60 (Na alginate) 1.5 g squalane 0.01 g ceramide 96.4 g water

2 g of Na alginate are stirred dissolved in 96.4 g of water. Subsequently is stirring a mixture of 1.5 g of squalane and 0.01 g of ceramides was added. The homogeneous (degassed) mixture is poured into molds, under Air blown out frozen, taken out of the mold and then in freeze-dried in a known manner.

Claims (14)

1 use of a shaped body, containing at least one scaffolding agent, with the exception of proteins, possibly one or more Active substances and optionally one or more auxiliary substances, for external use. Use according to claim 1 for external cosmetic use. Use according to claim 1 for external therapeutic use. Use according to one of claims 1 to 3, wherein the scaffolding agent is at least one polysaccharide or a derivative thereof. Use claim according to one of claims 1 to 4, wherein the scaffold Is sodium alginate. Use according to one of claims 1 to 5, wherein the shaped body has a volume of 0.1 cm ³ to 6 cm ³ , and the geometric shape of a sphere. Use according to one of claims 1 to 6, wherein the shaped body is obtainable by freeze-drying a frozen solution or dispersion containing at least one scaffold builder, with the exception of proteins, possibly one or more Active substances and optionally one or more auxiliary substances. Use according to claim 7, wherein the shaped body is obtainable by a process that includes the steps: (a) Manufacture a solution or suspension containing at least one biopolymer, if appropriate one or more physiologically active substances and, if appropriate contains one or more auxiliary substances, (b) pour the solution into a form, (c) freezing the solution in the mold and (D) Freeze-drying the frozen solution to form the shaped body. Use of the shaped bodies according to one of claims 1 to 8, where the external application the molded body done directly by the end user. Use of the shaped bodies according to one of claims 1 to 8, wherein the molded body with water or an aqueous solution or several active substances and / or auxiliary substances to form one Gels moistened and applied to the skin or hair. Shaped article containing: - at least 10% by weight of one or more framework formers, the 1% by weight solution or suspension of which in water at 20 ° C and pH 6-8 has a viscosity of less than 2000 mPas, - 0.000001% by weight % up to 50% by weight of one or more active substances, - 0.1 to 70% by weight% of one or more auxiliary substances, and - up to 20% by weight water, with the proviso that the shaped body has no proteins as scaffolders. moldings according to claim 11, wherein the scaffolding agent Is sodium alginate. Shaped body, preferably according to claim 11 or 12, containing at least one framework, with the exception of proteins, optionally one or more active substances and optionally one or more auxiliary substances for external use, which - a density of 0.01 g / cm ³ to 0 , 8 g / cm ³ , - a volume of 0.1 cm ³ to 6 cm ³ , and - a diameter (maximum distance between two points of the molded body) of at least 6 mm. Combination containing at least one shaped body such as in one of the claims 1 to 13 defines as well as at least one aqueous solution, the one or more Contains active substances and / or auxiliary substances in related, spatial Arrangement.