CH714305A2 - Process for the preparation of topical formulations and prepared formulations. - Google Patents

Abstract

The present invention relates to a process for the preparation of a topical formulation, wherein the cosmetic formulation comprises a base composition and at least one dermatologically or cosmetically or pharmacologically active substance, characterized in that the basic composition is subjected to ultrasound treatment after combining all components , The present invention further relates to topical formulations obtainable by this method.

Description

Description: The present invention relates to a method for producing topical cosmetic or medical formulations, and to formulations produced using this method.

A topical formulation is understood to mean a product which is applied to the skin. For example, creams, lotions or gels may be mentioned.

[0003] Topical cosmetic and also topical medical formulations are usually provided as emulsions. Depending on the nature, it can be an oil-in-water emulsion (o / w) or a water-in-oil emulsion (w / o).

[0004] Emulsions are prepared using known emulsification processes. Here, an aqueous phase and an oil phase are processed together with the aid of an emulsifier and a mixing device to form an emulsion.

Cosmetic products and medical products to be applied topically must meet various requirements. For example, they should not be greasy after being applied to the skin, should be as odorless as possible, have sufficient water resistance and contain no harmful ingredients.

In the literature, formulations based on certain emulsifiers have been described which largely meet the above requirements.

[0007] DE 19 857 492 A1 describes a formulation which contains a phosphatidylcholine as an emulsifier. Phosphatidylcholine is a constituent of lecithin and is able to form a lamellar structure (DMS structure (dermatological matrix structure). Hydrogenated phosphatidylcholine described in DE 19 857 492 A1 is particularly suitable for topical formulations.

[0008] However, formulations based on phosphatidylcholine and in particular hydrogenated phosphatidylcholine have disadvantages. These formulations can only be prepared in a complex manner using high-pressure homogenization that has to be carried out repeatedly (Hans Lautenschläger, Österreichische Apothekerzeitung, 56 (14), 679 (2002)). In addition, it is necessary to add medium-chain triglycerides to the formulation in not insignificant amounts in order to achieve the property profile described above. This gives the formulation an undesirable odor after it has been applied to the skin.

In CH 711 598 A2 it has been proposed to produce such formulations with the aid of a fermentation process with bacterial or yeast cultures. However, this manufacturing process takes several days and is associated with the disadvantages that usually occur in fermentation processes.

[0010] Phosphatidylcholine is also expensive and can only absorb a comparatively small amount of oily substances or lipid substances. In DE 69 112 849 T2 it was therefore proposed to use a phospholipidic base substance instead of pure phosphatidylcholine which also contains other phosphatid components in addition to phosphatidylcholine. Nevertheless, according to this document, it is still necessary to use a not inconsiderable amount of phosphatidylcholine.

In DE 10 2011 110 749 A1 and the associated WO 2013/023 641 A2, it was therefore proposed to use a sugar fatty acid ester, preferably sucrose tristearate, as an emulsifier instead of phosphatidylcholine.

However, according to these documents, it is necessary to use a significant amount of sugar fatty acid ester (more than 6 wt .-%). This is disadvantageous because these connections are expensive. In addition, sugar fatty acid esters do not show some of the advantages of formulations based on phosphatidylcholine (such as water resistance) to the same extent.

There was therefore a need for a method with which formulations based on phosphatidylcholine or a sugar-fatty acid ester can be prepared in a simple and inexpensive manner.

[0014] This object is achieved by the present invention.

The present invention relates to a method for producing a topical formulation, wherein the cosmetic formulation comprises a base composition and at least one dermatologically or cosmetically or pharmacologically active substance, characterized in that an ultrasound treatment is carried out to produce the base composition becomes.

It has surprisingly been found that the preparation of topical formulations based on phosphatidylcholine or a sucrose fatty acid ester such as sucrose tristearate can be achieved in a simple manner if the formulation is homogenized by ultrasound treatment. According to the invention, the complex processes from the prior art, for example high-pressure homogenization, can be dispensed with.

In the method according to the invention, the process interruption problem that occurs in particular in connection with the high-pressure homogenization is significantly reduced. The method according to the invention is very easy to carry out due to ideally controllable process parameters, which results in considerably reduced personnel costs.

CH 714 305 A2 The method according to the invention can in principle be used to produce any topical formulation, but is particularly suitable for the preparation of the DMS formulations described above (formulations with a dermatological matrix structure) which are otherwise difficult to prepare.

[0019] In addition to the simplified preparation of such formulations, the present invention has further advantages.

It has surprisingly been found that the required amount of emulsifier can be considerably reduced in the process according to the invention without the required properties or the structure / consistency of the formulation being impaired thereby. According to the invention, it is sufficient not more than 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4% by weight. -% to use at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester in the base composition. This is a significant economic advantage since, as stated above, these emulsifiers are expensive.

Furthermore, according to the invention, it is not necessary to add medium-chain triglycerides to the formulation, in particular the base composition of the formulation. The formulations according to the invention meet the requirement profile for topical formulations, despite the small amounts of emulsifier and despite the absence of medium-chain triglycerides.

A medium-chain triglyceride is understood according to the invention as a compound in which fatty acids with chain lengths of C8 to C16 (the number indicates the number of carbon atoms in the fatty acid) are esterified with glycerol. Triglycerides with fatty acids of chain length C8 to C12 are particularly preferred. Products of this type are commercially available (e.g. Myritol 312 and 318, or Miglyol 810 and 812).

In addition, the formulations produced according to the invention have an increased absorption capacity for lipids or other additives, in particular water-soluble additives, in comparison to conventionally produced formulations, in particular DMS formulations, without the need to add thickening additives which damage the skin sensors moisturizing properties, as well as the structure and consistency of the formulation.

In addition, much finer structured lipid / water distributions can be generated by means of the method according to the invention, which can retain the desired structure (or consistency) much better despite a possibly higher amount of lipid to be incorporated, but in particular despite a higher amount of water to be incorporated.

Furthermore, the formulations according to the invention have a high temperature resistance and can therefore be used reliably even in persistently warm ambient conditions (temperatures up to 40 ° C.).

[0026] Furthermore, the formulations according to the invention are more compact than conventionally produced formulations, in particular DMS formulations. In other words, the formulations according to the invention have a lower proportion of air inclusions (even without a subsequent evacuation process) and therefore higher specific weights than lipid-water mixture formulations of identical composition, which were prepared in a conventional manner.

The essence of the present invention is to carry out the homogenization with the aid of an ultrasound treatment.

The formulations according to the invention are designed like conventional topical formulations, for example DMS formulations based on water and oil. The formulations according to the invention must be homogenized, i.e. the formulation must have a uniform consistency without local differences (e.g. phase boundaries). In order to achieve homogenization, the aqueous phase and the oil phase must be combined to form an emulsion. An emulsion is a homogeneous system on liquid phases, in which droplets of one phase are distributed homogeneously in the other liquid phase. If droplets of an oil phase are distributed in an aqueous phase, one speaks of an oil-in-water emulsion (o / w). If, on the other hand, droplets of an aqueous phase are distributed in an oil phase, one speaks of a water-in-oil emulsion (w / o). More complex emulsions consisting of more than two phases are also known.

Surprisingly, it has been found that, in the case of the formulations according to the invention, the preparation of an emulsion from an aqueous phase and an oil phase by means of ultrasound treatment succeeds in a simple and outstanding manner. This was not to be expected, since in the prior art a complex high-pressure homogenization, which had to be carried out repeatedly, had been described as necessary for comparable strain gauge formulations.

The formulation according to the invention comprises a so-called base composition and at least one dermatologically or cosmetically or pharmacologically active substance which is added to the base composition.

The process improvement of the present invention relates to the step of preparing the base composition, namely the homogenization of the base composition.

CH 714 305 A2 According to a preferred embodiment of the present invention, the ultrasound treatment is carried out at a temperature of the base composition in the range from 35 ° C. to 85 ° C., preferably in the range from 50 ° C. to 85 ° C., particularly preferably in the Range from 60 ° C to 80 ° C performed.

According to the invention, any conventional ultrasound device that provides sufficient power can be used for the ultrasound treatment to homogenize the base composition. According to a preferred embodiment of the present invention, the treatment with ultrasound should achieve an energy input into the base composition which is in the range from 200 Ws / g to 600 Ws / g, preferably in the range from 250 Ws / g to 500 Ws / g, particularly preferably in the range from 300 Ws / g to 450 Ws / g, based on the amount of composition to be homogenized. In the case of a sequential homogenization of the basic composition due to the sequential addition of different phases, the above energy input relates to the total energy input which is to be supplied to the system through all sequential homogenization stages.

The method of the present invention can be carried out, for example, with ultrasound devices from Hielscher. Such devices are commercially available.

The duration of the ultrasound treatment according to the invention depends on the base composition to be homogenized.

The production of base compositions for strain gage formulations up to their homogenization is known. Depending on the nature of the base composition, all components of the base composition can be combined in a container such as a reaction flask and then subjected to an ultrasound treatment in this container as described above. However, it is preferred according to the invention to prepare at least one aqueous phase and at least one oil phase of the base composition beforehand, and then to combine these phases and homogenize them according to the invention with the aid of an ultrasound treatment. In the case of the prior production of several aqueous and / or oily phases, the homogenization can be carried out sequentially after combining part of the previously prepared phases or in one step after combining all the previously prepared phases.

The at least one aqueous phase comprises water as a solvent and optionally water-soluble constituents of the base composition. Moisture substances are preferably suitable as water-soluble constituents of the base composition. However, it is also conceivable, for example, to add physiologically acceptable salts.

Moisturizing substances which can be used according to the invention can be polyols, urea or mixtures thereof. The polyols must be physiologically acceptable. Examples include glycol, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, glycerin, carbohydrates such as inositol (inositol), sorbitol (sorbitol), mannitol, palatinite, maltodextrin, dextrin, cyclodextrin, glucose, fructose, lactose, mannose, galactose and other saccharides. Glycerol, propylene glycol, pentylene glycol and urea are particularly preferred.

An exemplary aqueous phase of a base composition according to the invention consists of a mixture of water and at least one polyol as a moisturizing substance. A mixture of 60-90% by weight of water and 40-10% by weight of a mixture of glycerol and pentylene glycol is preferred.

The at least one aqueous phase is generally produced by combining the corresponding constituents, mixing and heating. The ingredients are placed in a container such as a reaction flask and mixed in a conventional manner (e.g. manually with a stick or preferably with a stirrer). The mixture is then preferably heated to 40 ° C. to 95 ° C., preferably 50 ° C. to 90 ° C.

The at least one oil phase comprises the emulsifier, which is preferably selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester, and other non-water-soluble components of the basic composition according to the invention.

An emulsifier preferred according to the invention is phosphatidylcholine. Phosphatidylcholine is part of lecithin and chemically composed of a glycerol unit, of which three hydroxyl groups two groups are esterified with (usually unsaturated) fatty acids, while the last hydroxyl group is connected with a phosphocholine residue. Lecithin is a mixture of various phospholipids that occurs naturally in various plants, for example soybeans, or egg yolk. Phosphatidylcholine can be extracted from lecithin and is commercially available.

[0043] According to a preferred embodiment of the present invention, the emulsifier is a hydrogenated phosphate diylcholine. Hydrogenated phosphatidylcholines are known and commercially available. The product Lipoid P-100-3 from Lipoid Cosmetics may be mentioned as an example. Hydrogenated phosphatidylcholines can be prepared from naturally occurring phosphatidylcholines by hydrogenating the double bonds in the unsaturated fatty acid chains.

Another preferred emulsifier according to the invention is a sucrose fatty acid ester. According to the invention, for example, mono-, di- or trifatty acid esters or polyester from sucrose can be used. The corresponding sucrose stearates (sucrose mono-, di- or tristearate) are preferred, with sucrose tristearate being the most preferred.

According to a preferred embodiment, the base composition according to the invention comprises at least one oil and / or at least one lipid as non-water-soluble constituents.

CH 714 305 A2 The oil used is preferably jojoba oil, almond oil or sunflower oil. However, other oils conventionally used in topical formulations and in particular DMS formulations, such as neutral oil, can also be used.

The lipid conventionally used in topical formulations and in particular DMS formulations can be lipids in the base composition according to the invention. Examples include: plant phytosterols (e.g. in shea butter), ceramide III and squalane.

According to a preferred embodiment, the base composition according to the invention can comprise further auxiliaries which are conventionally used in topical formulations and in particular DMS formulations. Depending on the solubility in water, these auxiliaries are formulated in the aqueous phase or the oil phase. Examples include fatty acids and fatty acid esters.

[0049] The at least one oil phase can be produced in a conventionally known manner. According to an embodiment according to the invention, the at least one oil phase is produced by combining the corresponding constituents, mixing and heating. The ingredients are placed in a container such as a reaction flask and mixed in a conventional manner (e.g. manually with a stick or preferably with a stirrer). The mixture is then preferably heated to 60 ° C. to 120 ° C., preferably 90 ° C. to 110 ° C.

The at least one oil phase should be mixed and heated until a clear or milky liquid is present.

According to one embodiment of the present invention, all components of the oil phase are mixed together to form a single oil phase. According to a further embodiment of the present invention, part of the components of the oil phase, for example emulsifier, oil and lipids, are mixed with one another to form an oil phase, and another part of the components of the oil phase, for example additives such as fatty acids and fatty acid esters, are mixed with one another to form a further oil phase , The two oil phases are then added sequentially to the aqueous phase, the oil phase with emulsifier preferably being added to the aqueous phase first.

Subsequently, according to an embodiment of the invention, separately produced phases (aqueous phase and oil phase) are mixed with one another sequentially or in one step and, after each mixing, are subjected to the ultrasound treatment according to the invention. In the case of several separate aqueous phases and / or oil phases, the respective phases are combined in the desired order and subjected to the ultrasound treatment according to the invention after each mixing.

Since, as mentioned above, the ultrasound treatment is carried out at a temperature in the range from 35 ° C. to 85 ° C., preferably in the range from 50 ° C. to 85 ° C., particularly preferably in the range from 35 ° C. to 75 ° C. , it may be necessary to cool the at least one oil phase to this temperature range before it is combined with the aqueous phase.

A preferred base composition of the present invention contains 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4 wt .-%, at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester; 10 to 30% by weight of an oil; 5 to 15% by weight of at least one humectant, 1 to 10% by weight of at least one lipid, 0 to 15% by weight of at least one additive, and 83.9 to 27.5% by weight of water, all of which are Percentages refer to the weight of the basic composition and the sum of all components is 100%.

A particularly preferred base composition of the present invention contains 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4% by weight, phosphate diylcholine; 10 to 30% by weight of an oil; 5 to 15% by weight of at least one humectant, 1 to 10% by weight of at least one lipid, 0 to 15% by weight of at least one additive, and 83.9 to 27.5% by weight of water, all of which are Percentages refer to the weight of the basic composition and the sum of all components is 100%.

Another particularly preferred base composition of the present invention contains 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 00.1 to 1.6% by weight, in particular preferably 0.2 to 1.4% by weight, sucrose fatty acid ester; 10 to 30% by weight of an oil; 5 to 15% by weight of at least one humectant, 1 to 10% by weight of at least one lipid, 0 to 15% by weight of at least one additive, and 83.9 to 27.5% by weight of water, all of which are Percentages refer to the weight of the basic composition and the sum of all components is 100%.

The topical formulation is then prepared from the base composition prepared as described above by combining the base composition produced with ultrasound treatment with at least one dermatologically or cosmetically or pharmacologically active substance and mixing the components.

According to the invention, any substance which is conventionally used in topical skin products or cosmetic products or has a corresponding effect can be used as a dermatologically or cosmetically active substance. According to a preferred embodiment, the dermatologically or cosmetically active substance is selected from the group consisting of water-soluble active substance extracts, oil-based active substance extracts, medicinal herbs, powdered active substances, and active substance solutions.

CH 714 305 A2 [0059] Merely by way of example may be mentioned 12-hydroxystearic, and 11-hydroxy palmitic acid, castor oil, hydrogenated castor oil, Rizinol-säureoctyldodecylester, 12-Hydroxystearinsäureoctylester, beeswax, Japan wax, carnauba wax, cetyl palmitate, cocoa butter, jojoba oil, shea butter, squalene, Squalane, cholesterol, choesteryl sulfate, hyaluron, phytosterols, lanolin, lanolin alcohols and their derivatives, ceramides, sphingolipids, sphinganine, sphinosin, sphingosine-1-phosphate, sphingomyelin, C12-C15-alkyl-benzoate and linoleic acid methyl ester , Plant extracts from, for example, Edelweiss, Laminaria ochroleuca, Alaria Esculenta or horsetail, as well as natural fatty oils, such as Avo-cado oil, wheat germ oil, macadamia nut oil, apricot kernel oil, almond oil, hemp oil, linseed oil, sesame oil, olive oil, sunflower oil, peanut oil in a natural and hydrated form.

Other active ingredients can include vitamins and provitamins (in particular A, B complex, C, E, D and their usual derivatives such as vitamin A acid, vitamin A acetate, vitamin A palmitate, vitamin C palmitate, vitamin E). acetate, palmitate and linoleate, alfacalcidol, calcitriol, colecalciferol, ergocalciferol, transcal-cifediol, calciprotriol, calcifediol, vitamin D3, ß-carotene, or panthenol, pantothenic acid, biotin).

Active substances which are intended for topical use can be used as pharmacological active substances. For example, the pharmacologically active substance can be a pain reliever or blood, preferably autologous blood.

Examples of other possible pharmacological active substances are: local anesthetics (for example lidocaine, benzocaine, polidocanol, isoprenaline, crotamiton, quinisocaine), HI antihistamines (for example meclozin, cetirizine, promethazine, terfenadine), antifungal agents (for example econazolol, isonazolol, isonazolol, , oxiconazole, tioconazole, fenticonazole, clotrimazole, miconazole, ketoconazole, itraconazole, Flucanazol) antinflammatorisch agents (anti-inflammatories, such as glucocorticoids and their derivatives such as triamcinolone acetonide; bufexamac, acetylsalicylic acid, Atlantoin), immunosuppressants (such as methotrexate, cyclosporine, retinoids (eg, isotretinoin , Acitretinoin, tazarotene), antiseptics (e.g. chlorhexidine, benzalkonium chloride), virustatic agents (e.g. aciclovir, penciclovir), extracts with specific effects (e.g. aloe vera extract, green tea extract, algae extract, echinacea extract, arnica extract, cucumber extract, hop extract , Bran extract, witch hazel extract, yeast extract, G ingko biloba extract), vegetable oils with specific effects (e.g. Rosemary oil, chamomile oil, sage oil, calendula oil, lavender oil, St. John's wort oil, lemon balm oil, sand dome oil, tea tree oil, cedarwood oil, cypress oil), as well as barrier-stabilizing acids (e.g. linoleic acid, 12-hydroxystearic acid, stearic acid, isostearic acid, palmitic acid, 11-hydroxypalmitate

The active ingredients also include covering substances and pigments, such as Magnesium oxide, magnesium carbonate, magnesium aluminum silicate, magnesium stearate, magnesium isostearate, talc, calcium carbonate, zinc oxide, zinc carbonate, zinc stearate, zinc laurate, titanium dioxide, iron oxide, iron hexacyanoferrate, bismuth oxychloride, aluminum oxide, aluminosilicate, silicon dioxide, aerosil, bomitride, mica and rock dust.

All active ingredients can be contained in the formulations according to the invention on their own or in a correspondingly meaningful combination. If it is necessary to adjust the pH of the formulation due to the presence of specific active ingredients, this can be done using suitable bases such as e.g. Sodium hydroxide, potassium hydroxide, trometamol, arginine or lysine.

As mentioned above, it is advantageously possible with the method according to the invention to provide topical formulations which, despite a comparatively small amount of emulsifier, meet the requirement profile for topical products and which, despite a comparatively small amount of emulsifier, can absorb a comparatively large amount of oil and / or lipid.

According to a further embodiment, the present invention therefore also relates to a topical formulation obtainable by the process according to the invention described above, comprising

0.01 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4 wt .-%, at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester;

5 to 30% by weight of an oil;

5 to 15% by weight of at least one humectant,

1 to 10% by weight of at least one lipid,

0 to 10% by weight of at least one additive,

2 to 10% by weight of at least one dermatologically or cosmetically or pharmacologically active substance,

86.99 to 22.5% by weight of water, where all percentages relate to the weight of the topical formulation and the sum of all components is 100%.

The amount of at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester, preferably hydrogenated phosphate diylcholine or sucrose tristearate, in the topical formulation is preferably 0.3 to 2.5% by weight, preferably 0.1 to 2 % By weight, more preferably 0.1 to 1.6% by weight, even more preferably 0.2 to 1.4% by weight, particularly preferably 0.4 to 0.7% by weight, based on the weight the topical formulation.

CH 714 305 A2 The amount of oil, preferably selected from the group consisting of jojoba oil, almond oil and sunflower oil, in the topical formulation is preferably 10 to 25% by weight, particularly preferably 15 to 25% by weight, based on the weight of the topical formulation.

The amount of lipid, preferably selected from the group consisting of shea butter, ceramide III B or squalane, in the topical formulation is preferably 1 to 5% by weight, particularly preferably 1.5 to 4% by weight, based on the weight of the topical formulation.

The amount of humectant, preferably selected from the group consisting of glycerol and glycols such as pentylene glycol, in the topical formulation is preferably 7 to 12 wt .-%, particularly preferably 8 to 10 wt .-%, based on the weight of the topical formulation.

The amount of the at least one optional additive, preferably selected from the group consisting of fatty acids and fatty acid esters, is preferably 1 to 9% by weight, particularly preferably 2 to 8% by weight, based on the weight of the topical formulation ,

The amount of at least one dermatologically or cosmetically or pharmacologically active substance in the topical formulation is preferably 3 to 8% by weight, particularly preferably 4 to 7% by weight, based on the weight of the topical formulation.

The formulation according to the invention can furthermore contain one or more additives, as are customarily used in topical formulations. For example, fillers, pigments or pH-modifying agents may be mentioned. If present, these additives are used in a total amount of 0.1 to 5% by weight, preferably 1 to 3% by weight, based on the weight of the topical formulation.

The remaining amount of the topical formulation up to 100 wt .-% consists of water.

The creams are suitable for dermatological, cosmetic or medical applications. They are particularly suitable for medical cosmetics since, according to a preferred embodiment, they do not have to contain any allergy potentials, no preservatives, no synthetic components or no dyes. Disorders of the skin barrier can be repaired immediately by applying the formulation according to the invention to the skin. Inflammation subsides, and as a result, allergens from the environment no longer penetrate the skin. In addition, the moisture content of the skin can no longer escape in an uncontrolled manner. This generates an improved proportion of skin moisture, which manifests itself in a smoother complexion and good skin feel.

The formulation according to the invention can be provided in the dosage forms customary for topical products. Examples include ointments, creams, lotions and gels. Such formulations are known to the person skilled in the art and need not be described further here.

The topical formulation according to the invention can be applied to the skin by simple application. The amounts to be applied and the application intervals depend on the type and amount of active ingredient.

The present invention is explained below on the basis of non-limiting examples.

Example 1: Preparation of a base composition based on phosphatidylcholine with ultrasound treatment. An aqueous phase according to Table 1 was prepared by mixing the components and heating to 75-80 ° C.

Table 1

Aqueous phase (% by weight based on total aqueous phase)

Water 70-90% by weight

Mixture of moisturizing substances 10-30% by weight. A first oil phase according to Table 2 was produced by mixing the components and heating to 100-110 ° C.

Table 2

Oil phase I (% by weight based on total oil phase I)

Lecithin 1-3% by weight

Jojoba oil 75-85% by weight

CH 714 305 A2

Table 2

Oil phase I (% by weight based on total oil phase I)

Mixture of lipids 12-24% by weight A second oil phase according to Table 3 was produced by mixing the components and heating to 70-75 ° C.

Table 3

Oil phase II (% by weight based on total oil phase II)

Fatty acids 50-70% by weight

Jojoba oil 0-10% by weight

Fatty acid ester 20-50% by weight A basic composition of a 1: 1: 1 mixture of the three phases above was prepared as follows. First, the aqueous phase heated as above and the oil phase I heated as above were combined and homogenized at a temperature of 60-85 ° C. using an ultrasound device from Hielscher (UP200ST) with an energy input of 10 to 50 Ws / g.

Subsequently, the oil phase II heated as above was added, and it was homogenized at a temperature of 60-85 ° C. with an ultrasound device from Hielscher (UP200ST) with an energy input of 350 to 390 Ws / g.

After cooling, a nice creamy-homogeneous, crystallizable cream (lamellar system) resulted from the emulsion formed in this way.

Comparative Example 1: Preparation of a Base Composition Based on Phosphatidylcholine with Rotor-Stator Homogenization A base composition was prepared analogously to that described in Example 1, with the difference that the homogenization was carried out as follows.

First, the aqueous phase heated as above and the oil phase I heated as above were combined and for 3 min. homogenized with a conventional rotor-stator homogenizer (device type: WiseT HG-15A; dispersing tool type: DH.WHG02015) at 10,000 rpm.

Subsequently, the oil phase II heated as above was added, and it was for 10 min. with a conventional rotor-stator homogenizer (device type: WiseT HG-15A; dispersing tool type: DH.WHG02015)

Homogenized at 000 rpm.

Even the mixture of aqueous phase and oil phase I could not be processed into a homogeneous mixture. Even increasing the speed of rotation of the rotor-stator homogenizer to 20,000 rpm and increasing the treatment time did not result in a homogeneous mixture.

After incorporation of the oil phase II and cooling, an inhomogeneous two-phase system was formed.

Comparative Example 2: Preparation of a base composition based on phosphatidylcholine with high-pressure homogenization A base composition was prepared analogously to that described in Example 1, with the difference that the homogenization was carried out as follows.

First, the aqueous phase heated as above and the oil phases I and heated as above were combined and for 3 min. homogenized with a conventional rotor-stator homogenizer (device type: WiseT HG-15A; dispersing tool type: DH.WHG02015) at 20,000 rpm.

The composition was then homogenized in a known manner at 960 bar and 90 ° C.

After cooling, no homogeneously crystallizable cream was formed. Even after two high pressure homogenizations under the above conditions, nothing changed in this result.

CH 714 305 A2

Example 2: Preparation of a night cream A base composition according to Example 1 was mixed with water and a mixture of various cosmetic active ingredients at 30 to 40 ° C. A night cream with the composition shown in Table 4 could be obtained without problems.

Table 4

night cream

Base composition according to Example 1 70-90% by weight

Water 5-20% by weight

Cosmetic ingredients 10-25% by weight

Example 3: Preparation of a lotion A base composition according to Example 1 was mixed with water and a mixture of different cosmetic active ingredients at 30 to 40 ° C. A very well flowable lotion with the composition given in Table 5 could be obtained without any problems.

Table 5

lotion

Base composition according to Example 1 40-60% by weight

Water 30-59% by weight

Cosmetic ingredients 1-10% by weight

Example 4: Preparation of a base composition based on sucrose stearate with ultrasound treatment. An aqueous phase according to Table 1 was prepared by mixing the components and heating to 75-80 ° C.

Table 1

Aqueous phase (% by weight based on total aqueous phase)

Water 70-90% by weight

Mixture of moisturizing substances 10-30% by weight. A first oil phase according to Table 2 was produced by mixing the components and heating to 100-110 ° C.

Table 2

Oil phase I (% by weight based on total oil phase I)

Sucrose stearate 1.5-4% by weight

Jojoba oil 75-85% by weight

Mixture of lipids 11-23.5% by weight A second oil phase according to Table 3 was produced by mixing the components and heating to 70-75 ° C.

CH 714 305 A2

Table 3 Oil phase II (% by weight based on total oil phase II) fatty acids 50-70% by weight jojoba oil 0-10% by weight fatty acid ester 20-50% by weight

A base composition of a 1: 1: 1 mixture of the three phases above was prepared as follows. First, the aqueous phase heated as above and the oil phase I heated as above were combined and homogenized at a temperature of 60-85 ° C. using an ultrasound device from Hielscher (UP200ST) with an energy input of 10 to 50 Ws / g.

Subsequently, the oil phase II heated as above was added, and it was homogenized at a temperature of 60-85 ° C with an ultrasound device from Hielscher (UP200ST) with an energy input of 350 to 390 Ws / g.

After cooling, a nice creamy-homogeneous, crystallizable cream (lamellar system) resulted from the emulsion formed in this way.

Comparative Example 3: Preparation of a base composition based on sucrose stearate with rotor-stator homogenization. A base composition was prepared analogously to that described in Example 4, with the difference that the homogenization was carried out as follows.

First, the aqueous phase heated as above and the oil phase I heated as above were combined and for 3 min. homogenized with a conventional rotor-stator homogenizer (device type: WiseT HG-15A; dispersing tool type: DH.WHG02015) at 10,000 rpm.

Subsequently, the oil phase II heated as above was added, and it was for 10 min. with a conventional rotor-stator homogenizer (device type: WiseT HG-15A; dispersing tool type: DH.WHG02015)

Homogenized at 000 rpm.

Even the mixture of aqueous phase and oil phase I could not be processed into a homogeneous mixture. Even increasing the speed of rotation of the rotor-stator homogenizer to 20,000 rpm and increasing the treatment time did not result in a homogeneous mixture.

After incorporation of the oil phase II and cooling, an inhomogeneous two-phase system was formed.

Comparative Example 4: Preparation of a base composition based on sucrose stearate with high-pressure homogenization. A base composition was prepared analogously to that described in Example 4, with the difference that the homogenization was carried out as follows.

First, the aqueous phase heated as above and the oil phases I and heated as above were combined and for 3 min. homogenized with a conventional rotor-stator homogenizer (device type: WiseT HG-15A; dispersing tool type: DH.WHG02015) at 20,000 rpm.

The composition was then homogenized in a known manner at 960 bar and 80 ° C.

After cooling, no homogeneously crystallizable cream was formed. Even after two high pressure homogenizations under the above conditions, nothing changed in this result.

Claims (15)

claims 1. A method for producing a topical formulation, the formulation comprising a base composition and at least one dermatologically or cosmetically or pharmacologically active substance, characterized in that an ultrasound treatment is carried out to produce the base composition. 2. The method according to claim 1, characterized in that the treatment with ultrasound at a temperature of the base composition in the range from 35 ° C to 85 ° C, preferably in the range from 50 ° C to 85 ° C, particularly preferably in the range from 35 ° C to 75 ° C is carried out. 3. The method according to claim 1 or 2, characterized in that the treatment with ultrasound results in an energy input into the base composition which is in the range from 200 J / g to 600 J / g, preferably in the range from 250 J / g to 500 J / g, particularly preferably in the range from 300 J / g to 450 J / g. CH 714 305 A2 4. The method according to any one of the preceding claims, characterized in that at least one aqueous phase and at least one oily phase of the base composition are prepared separately in a previous stage and the phases are then combined. 5. The method according to any one of the preceding claims, characterized in that the topical formulation is prepared by combining the base composition produced with ultrasound treatment with at least one dermatologically or cosmetically or pharmacologically active substance and mixing the components. 6. Basic composition for a topical formulation, in particular cosmetic or medical topical formulation, preferably obtainable by a process according to one of claims 1 to 5, containing 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4% by weight %, at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester; - 10 to 30% by weight of an oil; - 5 to 15% by weight of at least one humectant; - 1 to 10% by weight of at least one lipid; - 0 to 15 wt .-% of at least one additive; and - 83.9 to 27.5% by weight of water; where all percentages relate to the weight of the basic composition and the sum of all components is 100%. 7. Base composition according to claim 6, containing 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4% by weight , Phosphate diylcholine; - 10 to 30% by weight of an oil; - 5 to 15% by weight of at least one humectant; - 1 to 10% by weight of at least one lipid; - 0 to 15 wt .-% of at least one additive; and - 83.9 to 27.5% by weight of water; where all percentages relate to the weight of the basic composition and the sum of all components is 100%. 8. Base composition according to claim 6, containing 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4% by weight , Sucrose fatty acid ester; - 10 to 30% by weight of an oil; - 5 to 15% by weight of at least one humectant; - 1 to 10% by weight of at least one lipid; - 0 to 15 wt .-% of at least one additive; and - 83.9 to 27.5% by weight of water; where all percentages relate to the weight of the basic composition and the sum of all components is 100%. 9. Topical formulation, in particular cosmetic or medical topical formulation, preferably obtainable by a process according to one of claims 1 to 5, 0.01 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, particularly preferably 0.2 to 1.4% by weight , at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester; 5 to 30% by weight of an oil; - 5 to 15% by weight of at least one humectant; - 1 to 10% by weight of at least one lipid; - 0 to 10 wt .-% of at least one additive; -2 to 10% by weight of at least one dermatologically or cosmetically or pharmacologically active substance; - 86.99 to 22.5% by weight of water; where all percentages relate to the weight of the topical formulation and the sum of all components is 100%. 10. Topical formulation according to claim 9, characterized in that the phosphate diylcholine is a hydrogenated phosphate diylcholine. 11. Topical formulation according to claim 9, characterized in that the fatty acid component of the sucrose fatty acid ester is stearic acid. 12. Topical formulation according to one of claims 9 to 11, characterized in that the oil is selected from the group consisting of jojoba oil, almond oil, and sunflower oil. CH 714 305 A2 13. Topical formulation according to one of claims 9 to 12, characterized in that the dermatologically or cosmetically active substance is selected from the group consisting of water-soluble active substance extracts, oil-based active substance extracts, medicinal herbs, powdered active substances, and active substance solutions, respectively that the pharmacologically active substance is a pain reliever or blood, preferably autologous blood. 14. Topical formulation according to one of claims 9 to 13, characterized in that the formulation contains no medium-chain triglyceride. 15. Topical formulation according to one of claims 9 to 14, characterized in that the formulation is an ointment, a cream, a lotion or a gel.