WO2019086195A1

WO2019086195A1 - Process for preparing topical formulations by means of ultrasound and formulations so obtained

Info

Publication number: WO2019086195A1
Application number: PCT/EP2018/077029
Authority: WO
Inventors: Joachim BIESOLD; Patrick KAMER
Original assignee: Cosmetolab Ag
Priority date: 2017-11-06
Filing date: 2018-10-04
Publication date: 2019-05-09
Also published as: CH714305B1; CH714305A2; DE112018005353A5

Abstract

The present invention relates to a process for preparing a topical formulation, the cosmetic formulation comprising a base composition and at least one dermatologically or cosmetically or pharmacologically active substance, characterized in that the base composition is treated by ultrasound once all components have been mixed. The present invention further relates to topical formulations obtainable by this process.

Description

METHOD FOR PRODUCING TOPICAL FORMULATIONS BY MEANS

ULTRASONIC AND MANUFACTURED FORMULATIONS

The present invention relates to a process for the preparation of topical cosmetic or medical formulations, as well as formulations produced by this process.

A topical formulation means a product which is applied to the skin. For example, mention may be made of ^cereals , lotions or gels.

Topical cosmetic and topical medical Formulierun ^¬ gen are usually provided as emulsions. Depending on its nature, it may be an oil-in-water emulsion (o / w) 15 or a water-in-oil emulsion (w / o).

Emulsions are prepared by known emulsification processes. In this case, an aqueous phase and an oil phase are processed together to form an emulsion with the aid of an emulsifier and a mixer.

Topically applied cosmetic products and Medizinalproduk ^¬ te must meet several requirements. For example, they may be neutral in odor as possible after the application of non-fat to the skin target 25 th, have sufficient Wasserre ^¬ consistency and do not contain ingredients harmful to health.

In the literature, formulations based on certain

30 emulsifiers described which meet the above requirements as far as possible. Thus, DE 198 57 492 A1 describes a formulation which contains a phosphatidylcholine as emulsifier. Phosphatidylcholine is an ingredient of lecithin and is able to form a lamellar structure (DMS structure (dermatological matrix structure).) Especially hydrogenated phosphatidylcholine described in DE 198 57 492 A1 is suitable for topical formulations.

However, formulations based on phosphatidylcholine and in particular hydrogenated phosphatidylcholine have disadvantages. These formulations can only be prepared in a complicated manner by using high-pressure homogenization (Hans Lautenschläger, Österreichische Apothekerzeitung, 56 (14), 679 (2002)). In addition, it is necessary to add medium-chain triglycerides in significant amounts to the formulation in order to achieve the above-described property profile. This gives the formulation after application to the skin but an undesirable odor. It has been proposed in CH 711598 A2 to prepare such formulations by means of a fermentation process with bacterial or yeast cultures. However, this manufacturing process takes several days and is associated with the usually occurring in Fermentati ^¬ onsprozessen disadvantages.

Phosphatidylcholine is also expensive and can only absorb a comparatively small amount of oily substances or lipid substances. In DE 691 12 849 T2 it has therefore been proposed, instead of using pure phosphatidylcholine, to use a phospholipid basic substance which, in addition to phosphatidylcholine, also contains other phosphatide components. Nevertheless, according to this document, it is still necessary to use a not inconsiderable amount of phosphatidylcholine. In DE 10 2011 110 749 AI and the associated WO 2013/023641 A2, it has therefore been proposed, instead of using phosphatidylcholine, to use a sugar fatty acid ester, preferably sucrose tristearate, as emulsifier.

However, according to these documents, it is necessary to use a considerable amount of sugar fatty acid ester (more than 6% by weight). This is disadvantageous because these compounds are expensive. In addition, sugar fatty acid esters do not have some of the benefits of phosphatidylcholine-based formulations (such as water resistance) to the same extent.

There was therefore a need for a method by which phosphatidylcholine or a fatty acid ester based formulations can be prepared in a simple and cost effective manner.

This object is achieved by the present invention. The present invention relates to a process for the preparation of a topical formulation, wherein the cosmetic formulation comprises a basic composition and at least one dermatologically or cosmetically or pharmacologically active substance, characterized in that a treatment with ultrasound is carried out for the preparation of the basic composition.

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 homogenization of the formulation takes place by means of ultrasound treatment. On the elaborate Prior art methods, for example high pressure homogenization, can be dispensed with according to the invention.

In the method according to the invention, the process interruption problem occurring in particular in connection with high-pressure homogenization is markedly reduced. The method according to the invention is very easy to carry out due to ideally adjustable process parameters, resulting in considerably reduced personnel costs.

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

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

It has surprisingly been found that in the process according to the invention the required amount of emulsifier can be considerably reduced without thereby impairing the required properties or the structure / consistency of the formulation. According to the invention, it is sufficient not more than 2.5 wt .-%, preferably 0.1 to 2 wt .-%, more preferably 0.1 to 1.6 wt .-%, particularly preferably 0.2 to 1.4 wt .-% of 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, it is according to the invention not required, the Formu ^{¬-regulation,} in particular the base composition of the formulation medium chain triglycerides to add. The formulations according to the invention fulfill the requirement profile for topical formulations despite the small amounts of emulsifier and despite the absence of medium-chain triglycerides.

According to the invention, a medium-chain triglyceride is understood as ^{meaning 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. Especially before ^¬ are Trains t triglycerides with fatty acids of chain length C8 to C12. Products of this type are commercially available (eg Myritol 312 and 318, or Miglyol 810 and 812).

In addition, the formulations according to the invention produced as compared to conventionally prepared formulations, in particular DMS formulations, an increased capacity for lip- ide or other additives have, especially water-soluble set materials to ^¬ without the need for thickening additive additives ^¬ must be zugege ben which the skin Sensitivity that affects moisture-wicking properties, as well as the structure and consistency of the formulation. In addition, substantially finer structured lipid / water distributions can be generated by means of the method according to the invention which, despite a lipid fraction which may be incorporated at a higher level, but in particular despite a higher water content, can considerably better preserve the desired structure (or consistency).

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

Furthermore, the formulations according to the invention are more compact than conventionally prepared formulations, in particular DMS formulations. In other words, the formulations according to the invention have a smaller proportion of air inclusions

(Even without subsequently applicable evacuation process) and thereby higher specific gravity than identically together ^¬ set lipid-water mixture formulations, which were prepared in a conventional manner.

The core of the present invention is the implementation of the homogenization by means of an ultrasonic treatment.

The novel formulations are designed as conventional topical formulations, for example DMS formulations based on water-oil. The inventive formulations have to be homogenized, that is, the formulation must have a uniform consistency without local differences (eg phases ^¬ limits). 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 homogeneously distributed in the other liquid phase. Are droplets of a Ölpha ^¬ se dispersed in an aqueous phase, it is called an oil-in-water emulsion (o / w). If, on the other hand, droplets of an aqueous phase are dispersed in an oil phase, this is called a water-in-oil emulsion (w / o). There are also more complicated structured emulsions of more than two phases known.

Surprisingly, it has been found that, in the case of the formulations ^{according to} the invention, the preparation of an emulsion from a aqueous phase and an oil phase by means of ultrasonic treatment succeed in a simple and excellent manner. This was not to be expected, since in the prior art for comparable DMS formulations an expensive high-pressure homogenization which had to be carried out several times was described as necessary.

The inventive formulation comprises a so-called Ba ^¬ sis composition and which of the Ba sis composition is added at least one dermatologically or cosmetically or pharmacologically active substance.

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

Ultrasonic treatment according to a preferred embodiment of the present invention at a temperature of the base composition in the range of 35 ° C to 85 ° C, preferably in the range of 50 ° C to 85 ° C, more preferably in the range of 60 ° C to 80 ° C performed.

According to the invention, any conventional ultrasound apparatus can be used for ultrasound treatment for homogenizing the base composition, which provides adequate performance. According to a preferred embodiment of the present invention should be achieved in the basic composition by treatment with ultrasound an energy input which is in the range of 200 Ws / g to 600 Ws / g, preferably ^¬, in the range of 250 Ws / g to 500 Ws / g, more preferably in the range of 300 Ws / g to 450 Ws / g, based on the Men ^¬ ge to be homogenized composition. In the case of sequential homogenization of the base composition due to sequential addition of different phases, the above standing energy entry on the entire energy entry, wel ^¬ cher is to be fed to the system over all sequential Homogenisierungsstufen. The method of the present invention can be carried out, for example, with ultrasonic 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 preparation of basic compositions for DMS formulations until their homogenization is known. Depending on the nature of the base composition, all components of the base composition may be combined in a container such as a reaction flask and then sonicated in this container as described above. However, it is preferred in the invention, previously min ^¬ least produce an aqueous phase and at least one oil phase of Ba sis composition, and to combine these phases to homogenize subsequently and according to the invention by means of a ultrasonic treatment ^¬. In the case of the preceding preparation of several aqueous and / or oily phases, the homogenization can be carried out sequentially after combining a part of the previously prepared phases or in one step after combining all previously prepared phases.

The at least one aqueous phase in this case comprises water as solvent and optionally water-soluble constituents of the basic composition. As water-soluble constituents of the Ba ^¬ sis composition preferably moisturizing substances come into question. It is also conceivable, for example, the addition Physiologist ^¬ cally 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, glycerol, carbohydrates such as inositol (inositol), sorbitol (sorbitol),

Mannitol, palatinit, maltodextrin, dextrin, cyclodextrin, glucose, fructose, lactose, mannose, galactose and other saccharides. Particularly preferred are glycerol, propylene glycol, pen ^¬ tylene glycol and urea.

An exemplary aqueous phase of an inventive Ba ^¬ sis composition consists of a mixture of water and at least one polyol as a moisturizer substance. Preference is given to a mixture of 60-90% by weight of water and 40-10% by weight of a mixture of glycerol and pentylene glycol.

The at least one aqueous phase is usually by ^¬ For the respective ingredients, mixing and heating sammengeben prepared. The ingredients are placed in a container such as a reaction flask and in a conventional manner

(e.g., manually with a stick, or preferably with a stirrer). Subsequently, the mixture is preferably heated to 40 ° C to 95 ° C, preferably 50 ° C to 90 ° C. The at least one oil phase here comprises the emulsifier, which is preferably selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester, and further non-water-soluble constituents of the novel base composition.

A preferred emulsifier according to the invention is phosphatidylcholine. Phosphatidylcholine is a constituent of lecithin and is chemically composed of a glycerol unit, of which three roxyl groups two groups are esterified with (usually unsaturated) fatty acids, while the last hydroxyl group is connected to ei ^¬ nem Phosphocholinrest. Lecithin is a naturally occurring mixture of various phospholipids in various plants, for example soybeans, or egg yellow.

Phosphatidylcholine can be extracted from lecithin and is commercially available.

According to a preferred embodiment of the present invention, the emulsifier is a hydrogenated phosphate diylcholine. Hydrogenated phosphatidylcholines are known and commercially available ^¬ Lich. By way of example, the product Lipoid P-100-3 of the company called Lip ^¬ oid cosmetics. Hydrogenated phosphatidylcholines can be prepared from naturally occurring phosphatidylcholines by hydrogenating the double bonds in the unsaturated fatty acid chains.

Another emulsifier preferred according to the invention is a sucrose fatty acid ester. According to the invention, for example, mono-, di- or triflic acid esters or polyesters of sucrose can be used. Preference is given to the corresponding sucrose stearates (sucrose mono-, di- or tristearate), with sucrose tristearate being the most preferred. The inventive base composition comprises in a preferred embodiment as non-water soluble Bestandtei ^¬ le at least one oil and / or at least one lipid.

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, for example, ^neutral oil, can likewise be used. As lipid, lipids conventionally used in topical formulations and in particular DMS formulations can be used in the base composition according to the invention. Examples include: phytosterols phytosterols (eg in Shea Butter), ceramide III and squalane.

According to a preferred embodiment, the basic composition according to the invention may comprise further auxiliaries which are conventionally used in topical formulations and in particular DMS formulations. ^¬ to these excipients in the aqueous phase or the oil phase depending on the water solubility formulated. ^{By way of} example, fatty acids and fatty acid esters may be mentioned. The at least one oil phase can be prepared in a conventionally known manner. According to an embodiment of the invention, the at least one oil phase is prepared by combining the corresponding ingredients, mixing and heating. The ingredients are added to a container such as a reaction flask and mixed in a conventional manner (eg manually with a rod or preferably with a stirrer). Subsequently, the mixture is 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, a part of the components of the oil phase, for example emulsifier, oil and lipids, are mixed together to ei ^¬ ner oil phase and another part of the components of Oil phase, for example, additives such as fatty acids and Fettsäu ^¬ ester, mixed together to form another oil phase. The two oil phases are then added sequentially to the aqueous phase, wherein preferably the oil phase with emulsifier of the aqueous phase is added first.

Subsequently, according to an embodiment of the invention, separately prepared phases (aqueous phase and oil phase) are mixed together sequentially or in one step and subjected to the inventive ultrasound treatment after each mixing. 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 inventive ultrasound treatment after each mixing.

Since, as mentioned above, the ultrasonic treatment is to be carried out at a temperature in the range of 35 ° C to 85 ° C, preferably in the range of 50 ° C to 85 ° C, more preferably in the range of 35 ° C to 75 ° C is it optionally erforder ^¬ Lich, the cool down phase at least one oil to this temperature range, before it is combined with the aqueous phase.

A preferred base composition of the present invention contains from 0.1 to 2.5% by weight, preferably from 0.1 to 2% by weight, more preferably from 0.1 to 1.6% by weight, most preferably from 0.2 to 1 4% by weight of 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 wt .-% of at least one humectant, 1 to 10 wt .-% of at least one lipid, 0 to 15 wt .-% of at least one additive, and 83.9 to 27.5 wt .-% water, wherein all percentages are based on the weight of the base composition and the sum of all components is 100%. A particularly preferred base composition of the present invention contains from 0.1 to 2.5% by weight, preferably 0.1 to 2% by weight, more preferably 0.1 to 1.6% by weight, most preferably 0.2 to 1.4 % By weight, phosphate diylcholine; 10 to 30% by weight of an oil; From 5 to 15% by weight of at least one humectant, from 1 to 10% by weight of at least one lipid, from 0 to 15% by weight of at least one additive, and from 83.9 to 27.5% by weight of water, all of them Percentages based on the weight of the base composition and the sum of all components is 100%.

Another particularly preferred base composition of the ahead ^¬ invention contains 0.1 to 2.5 wt .-%, preferably 0.1 to 2 wt .-%, more preferably 0 0.1 to 1.6 wt .-%, particularly preferably 0.2 to 1.4% by weight, sucrose fatty acid ester; 10 to 30% by weight of an oil; 5 to 15 wt .-% of at least one Feuchthal ^¬ testoffs, 1 to 10 wt .-% of at least one lipid, 0 to 15 wt .-% of at least one additive, and 83.9 to 27.5 wt .-% water, wherein all percentages are based on the weight of the base composition and the sum of all components is 100%.

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

As dermatologically or cosmetically active agent inventions can be used dung according to any substance which is conventionally employed for this purpose in topical skin agents, or cosmetic products, or has a corresponding effect on ^¬. According to a preferred embodiment, the dermato- logically or cosmetically active substance selected from the group consisting of water-soluble active substance extracts, oil-based active substance extracts, medicinal herbs, powdered active ingredients, and active ingredient solutions.

Examples which may be mentioned are: 12-hydroxystearin and 11-hydroxypalmitic acid, castor oil, hydrogenated castor oil, octyl dodecyl ricinoleic acid, octyl 12-hydroxy-stearate,

Beeswax, Japan wax, carnauba wax, cetyl palmitate, cocoa butter, jojoba oil, shea butter, squalene, squalane, cholesterol, cholesteryl sulfate, hyaluron, phytosterols, lanolin, lanolin alcohols and their derivatives, ceramides, sphingolipids, sphinganine, sphinosine, sphingosine-1 phosphate, sphingomyelin, C12-C15 alkyl benzoate, linoleic acid methyl and ethyl ester, plant extracts of, for example, Edelweiss, Laminaria ochroleuca, Alaria esculenta or horsetail, and natural fatty oils such. As avocado oil, wheat germ oil, macadamia nut oil, apricot oil, almond oil, hemp oil, linseed oil, sesame oil, olive oil, sunflower oil, peanut oil in natural and hydrogenated form.

Other active ingredients may 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, transcalcifediol, calciprotriol, calcifediol, vitamin D3, beta-carotene, or panthenol, pantothenic acid, biotin).

As pharmacological agents it is possible to use active substances which are intended for topical application. In ^¬ play, the pharmacologically active substance, a pain medication or blood, preferably autologous blood, his. Examples which may be as a further possible pharmacological action ^¬ materials include: local anesthetics (eg, lidocaine, benzocaine, buttocks lidocanol, isoprenaline, crotamiton, quinisocaine) HI antihistamines (eg meclizine, cetirizine, promethazine, Terfena- din), antifungals (eg. Econazole, bifonazole, isoconazole, oxiconazole, tioconazole, fenticonazole, clotrimazole, miconazole, ketoconazole, itraconazole, flucanazole), anti-inflammatory agents (anti-inflammatory agents such as glucocorticoids and their derivatives such as triamcinolone acetonide, bufexamac, acetylsalicylic acid, atlanto), immunosuppressants (eg, methotrexate, ciclosporin, retinoids (eg, isotretinoin, acitretinoin, tazarotene), antiseptics (eg, chlorhexidine, benzalkonium chloride), antivirals (eg, acyclovir, penciclovir), extracts having specific effects (e.g. ., aloe vera extract, green tea extract, Algenex- extract, Echinacea extract, arnica extract, cucumber extract, Hopfenex ^gas tract, carrot extract, Kleieextrakt, Hamamelisex tract, He ^¬ fairy extract, gingko biloba extract), vegetable oils with specific effects (eg. As rosemary oil, camomile oil, sage oil, calendula oil, lavender oil, St. John's wort oil, melissa oil, Sanddomöl, tea tree oil, cedar oil, cypress oil) as well as accessible stabilizing acids (eg. B. linoleic acid, 12-hydroxystearic acid, stearic acid, Isoste ^¬ arinsäure, palmitic acid, 11-hydroxypalmitic

The active ingredients include mutatis mutandis, covering substances and pigments such. Example, magnesium oxide, magnesium carbonate, aluminum silicate Magnesi ^¬, magnesium stearate, magnesium isostearate, Valley ^¬ Kum, calcium carbonate, zinc oxide, zinc carbonate, zinc stearate, zinc laurate ^¬, titanium dioxide, iron oxide, iron hexacyanoferrate, knowledge mutoxychlorid, alumina, aluminosilicates, silica, Ae Rosil, Bomitride, mica and minerals.

All active ingredients can be used alone or in a correspondingly meaningful combination in the formulations according to the invention. be hold. If it should be necessary to adjust the pH of the formulation due to the presence of specific active ingredients, this can be done by means of suitable bases such as sodium hydroxide, potassium hydroxide, trometamol, arginine or lysine.

As mentioned above, it is with the inventive procedural ^¬ ren advantageously possible topical formulations bereitzustel ^¬ len, which despite a comparatively low amount of emulsifier meet the requirement profile for topical products and, despite a comparatively low amount of emulsifier a comparatively large amount of oil and / or lipid be able to record.

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 wt .-%, preferably 0.1 to 2 wt .-%, more preferably 0.1 to 2 wt .-%, more preferably 0.1 to 1.6 wt .-%, particularly preferably 0.2 to 1.4 Gew. ~ 6 min least one emulsifier selected from the group ^¬ be detached from Phosphatdiylcholin and säureester a Sucrosefett-;

5 to 30% by weight of an oil;

From 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,

From 86.99 to 22.5% by weight of water,

where all percentages are by weight of the topical formulation and the sum of all components is 100%. The amount of the at least one emulsifier selected from the group consisting of phosphate diylcholine and a sucrose fatty acid ester, preferably hydrogenated phosphate diylcholine or sucretrystearate, in the topical formulation is preferably 0.3 to 2.5% by weight, preferably 0.1 to 2 wt .-% before ^¬ ferred 0.1 to 1.6 wt .-%, more preferably 0.2 to 1.4 wt .-%, particularly preferably 0.4 to 0.7 wt .-%, based on the Weight of the topical formulation.

The amount of oil, preferably selected from the group best ^¬ starting from jojoba oil, almond oil, and sunflower oil, in the topi ^¬ rule formulation is preferably 10 to 25 wt .-%, particularly preferably 15 to 25 wt .-%, based on the weight to ^¬ european formulation.

The amount of lipid, preferably selected from the group ^¬ be detached from shea butter, Ceramide III B or squalane, in the topical formulation is preferably 1 to 5 wt .-%, particularly preferably 1.5 to 4 wt .-%, based on the weight of to ^¬ european formulation.

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

The amount of the at least one optional additive, before ^¬ preferably selected from the group consisting of fatty acids and Fettsäureestern is preferably 1 to 9 wt .-%, particularly preferably 2 to 8 wt .-%, 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, more preferably 4 to 7% by weight, based on the weight of the topical formulation.

The inventive formulation may further contain one or more additives such as are commonly used in topical Formulie ^¬ approximations used. 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% by weight consists of water.

The creams are suitable for dermatological, cosmetic or me ^¬ dizinische applications. They are particularly suitable for the medi ^¬ ical cosmetics, as they form must contain no allergy potential, no preservatives, no synthetic ingredients or no Farbstof ^¬ fe according to a preferred execution. Disorders of the skin barrier can be repaired immediately by applying the formulation according to the invention to the skin. Inflammation decreases, and as a result, environmental allergens are no longer able to penetrate the skin. In addition, the moisture content of the skin can no longer escape ^¬ uncontrollably. This improved skin moisture content is generated, which is manifested in a geschmeidi ^¬ Geren complexion and good skin feel.

The inventive formulation can be provided in the usual topical Pro ^¬-products dosage forms. Examples include ointments, creams, lotions and gels. Derar- term formulations are known in the art and need not be further described here.

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

The present invention will be explained below by way 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 the total aqueous phase)

Water 70-90 wt. O

0

Mixture of moisturizing substances 10-30 wt

0

A first oil phase according to Table 2 was prepared by mixing the components and heating to 100-110 ° C.

Table 2

Oil phase I (wt .-% based on total oil phase I)

Lecithin 1-3% by weight

Joj obaöl 75-85 wt. O

0

Mixture of lipids 12-24 wt

0

A second oil phase according to Table 3 was prepared by mixing the components and heating to 70-75 ° C Table 3

Oil phase II (wt .-% based on total oil phase II)

Fatty acids 50-70% by weight

Joj oba oil 0-10% by weight

Fatty acid ester 20-50% by weight

A base composition of a 1: 1: 1 mixture of the three above phases was prepared as follows. First, the heated above aqueous phase and the like vorste ^¬ starting heated oil phase I were added together and at a temperature of 60-85 ° C with an ultrasonic instrument from Hielscher

(UP200ST) with an energy input of 10 to 50 Ws / g homogenization ^¬ Siert.

Subsequently, the above heated oil phase II ^¬ be supplied, and it was (UP200ST) homogenised at a temperature of 60-85 ° C with an ultrasonic instrument from Hielscher with an energy input from 350 to 390 Ws / g.

After cooling, a nice creamy homogeneous, crystallizable cream (lamellar Sys tem ^¬) originated from the thus formed emulsion.

Comparative Example 1 Preparation of a Basis Composition Based on Phosphatidylcholine with Rotor-Stator Homogenization

A base composition was prepared analogously as described above in ^Example 1 with the difference that the homogenization was carried out as follows.

First, the above-heated aqueous phase and the above-heated oil phase I were combined and allowed to stand for 3 minute homogenized at 10,000 rpm with a conventional rotor-stator homogenizer (instrument type: WiseT HG-15A; dispersing tool type: DH.WHG02015). Subsequently, the above heated oil phase II supplied ^¬ give, and it was for 10 min. homogenized at 10,000 rpm with a conventional rotor-stator homogenizer (instrument type: WiseT HG-15A; dispersing tool type: DH.WHG02015). Already the mixture of aqueous phase and oil phase I could not be processed to a homogeneous mixture. Even an increase in the rotational speed of the rotor-stator homogenizer at 20000 U / min and an extension of the treatmen ^¬ averaging time yielded 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 phosphatidylcholine-based base composition with high-pressure homogenization

First, the above-heated aqueous phase and the above-heated oil phases I and II were combined and stirred for 3 minutes. homogenized at 20000 rpm with a conventional rotor-stator homogenizer (instrument type: WiseT HG-15A; dispersing tool type: DH.WHG02015).

Subsequently, the composition was homogenized in a known manner at 960 bar and 90 ° C. After cooling, no homogeneously crystallizable Cre ^¬ me. Even after two times high-pressure homogenization under the above conditions, nothing changed in this result.

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. It could be obtained without problems a night cream with the composition given in Table 4.

Example 3: Preparation of a lotion

A base composition according to Example 1 was mixed with water and a mixture of various cosmetic active ingredients at 30 to 40 ° C. It could be easily obtained a very flowable lotion with the composition shown in Table 5.

Table 5

lotion

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

Water 30-59% by weight

Cosmetic agents 1-10% by weight Example 4: Preparation of a base composition based on sucrose stearate with ultrasound treatment

A base composition of a 1: 1: 1 mixture of the three above phases was prepared as follows. First, the heated above aqueous phase and the like vorste ^¬ starting heated oil phase I were added together and at a temperature from 60-85 ° C with an ultrasonic device from Hielscher

(UP200ST) with an energy input of 10 to 50 Ws / g homogenization ^¬ Siert. Subsequently, the above heated oil phase II ^¬ be supplied, and it was (UP200ST) homogenised at a temperature of 60-85 ° C with an ultrasonic instrument from Hielscher with an energy input from 350 to 390 Ws / g. After cooling, a nice creamy homogeneous, crystallizable cream (lamellar Sys tem ^¬) originated from the thus formed emulsion.

Comparative Example 3: Preparation of a Sucrose Stearate Based Composition with Rotor-Stator Homogenization

A base composition was prepared analogously as described above in ^Example 4 with the difference that the homogenization was carried out as follows.

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

Subsequently, the above heated oil phase II supplied ^¬ give, and it was for 10 min. homogenized at 10,000 rpm with a conventional rotor-stator homogenizer (instrument type: WiseT HG-15A, dispersing tool type: DH.WHG02015).

Already the mixture of aqueous phase and oil phase I could not be processed to a homogeneous mixture. Even one Increasing the rotational speed of the rotor-stator homogenizer at 20000 U / min and an extension of the treatmen ^¬ averaging time yielded 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 Sucrose Stearate Based Composition with High Pressure Homogenization

A base composition was prepared analogously as described above in ^Example 4 with the difference that the homogenization was carried out as follows. First, the above-heated aqueous phase and the above-heated oil phases I and II were combined and stirred for 3 minutes. homogenized at 20000 rpm with a conventional rotor-stator homogenizer (instrument type: WiseT HG-15A; dispersing tool type: DH.WHG02015).

Subsequently, the composition was homogenized in a known manner at 960 bar and 80 ° C.

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

Claims

Process for producing a topical formulation, wherein the formulation comprises a base composition and at least one dermatologically or cosmetically or pharmacologically active substance, characterized in that a treatment with ultrasound is carried out to produce the base composition.

Method according to claim 1, characterized in that the treatment with ultrasound at a temperature of the base composition in the range of 35°C to 85°C, preferably in the range of 50°C to 85°C, particularly preferably in the ^range of 35°C to 75°C is carried out.

Method according to claim 1 or 2, characterized in that the treatment with ultrasound achieves an energy input into the base composition which is in the range from 200 J/g to 600 J/g, preferably in the range of 250 J/g to 500 J/g, particularly preferably in the range from 300 J/g to 450 J/g.

Method according to one of the preceding claims, characterized in that in a previous stage at least one aqueous phase and at least one oily phase of the ^base composition are prepared separately and the phases are then combined.

Method according to one of the preceding claims, characterized in that the topical formulation is prepared by ^adding the base composition produced with ultrasound treatment to at least one dermatological or cosmetically or pharmacologically active substance and mixing the components.

Base composition for a topical formulation, in particular special cosmetic or medical topical ^formulation , preferably obtainable by a process according to one of claims 1 to 5

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, of 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,

where all percentages refer to the weight of the base composition and the sum of all components is 100%.

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% by weight of at least one additive, and

83.9 to 27.5% by weight of water,

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, of sucrose fatty acid ester;

10 to 30% by weight of an oil;

0 to 15% by weight of at least one additive, and 83,

9 to 27.5% by weight of water,

Topical formulation, in particular cosmetic or medical ^topical formulation, preferably obtainable by a method 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% by weight of at least one additive,

86.99 to 22.5% by weight of water,

where all percentages refer 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.

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 ingredient extracts, oil-based active ingredient extracts, medicinal herbs, powdered active ingredients, and active ingredient solutions , or that the pharmacologically active substance is a painkiller or blood, ^preferably your own blood.

14. Topical formulation according to one of claims 9 to 13, characterized in that the formulation does not contain any 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.