CH711598B1 - Process for the preparation of dermatological and cosmetic preparations with pronounced lamellar structures using phosphatidylcholine and fermentation by microorganisms. - Google Patents

Abstract

Process for the preparation of cosmetic or pharmaceutical products for topical use consisting of a mixture of phosphatidylcholine (preferably hydrogenated), vegetable oils and / or fats and / or waxes, water and / or hydrous plant extracts, mono- or polysaccharides, which is mixed with microorganisms whereby the initial droplet-shaped pre-emulsion converts over a period of several days into a pronounced lamellar membrane structure having skin physiological properties.

Description

Description of the Related Art As early as 1995, the inventor and applicant developed and marketed products called DMS (Derma Membrane Structure), which were prepared on the basis of hydrogenated phosphatidylcholine, medium chain triglycerides, cosmetic actives, and high pressure homogenization. These cosmetic products were able to do without conventional emulsifiers altogether. The lipophilic and hydrophilic components of the cream also exhibited lamellar structures for the first time, similar to those of the lipid matrix of the stratum corneum. The lamellar structures conformed to the skin physiology and protect the skin against the ingress of external substances and regulate the transepidermal water loss through the skin.

The formation of the lamellar structures is dependent on the geometric packing factors, such as the volume of the fatty acid chains, the critical chain length, and area occupied by the headgroup (Israelachvili, JN In Intermolecular and Surface Forces, 2nd Ed., Jovanovich, Η.B. Academic Press Ltd., London 1994). This means that not every amphiphilic substance can form lamellar structures or membranes. The best known lipid capable of forming such lamellar structures is phosphatidylcholine (PC), also part of the human cell membrane. Phosphatidylcholine is found in a high concentration in soya lecithin.

DE 1985 7 492, EP 1 259 218 and DE 10 2006 015 544 from Kuhs GmbH describe formulations based on hydrogenated phosphatidylcholine, medium-chain triglycerides, mixed with different active ingredients. However, the preparation of these formulations can not be done with conventional emulsification. To produce it requires a special high pressure homogenization, the process must also be repeated several times (Hans Lautenschläger, Österreichische Apothekerzeitung, 56 (14), 679 (2002).

DE 10 2011 110 749 by Gabriele Blume describes a production process according to which preparations with a lamellar structure can be prepared with a simple emulsion technique. Here, however, the so valuable for the skin phosphatidylcholine is replaced by sucrose tristearates.

Phosphatidylcholine, especially the hydrogenated, however, shows a pronounced barrier-stabilizing effect. The skin barrier is stabilized by PCH-containing preparations with lamellar structure in such a way that after the application of the transepidermal water loss (TEWL) changes only slightly when external substances act on the skin. The protection thus obtained is also characterized by a high water resistance and resistance to sweat. For this reason, the use of hydrogenated phosphatidylcholine is highly desirable for cosmetic or dermatological preparations.

Object of this invention The object of this invention was to develop a method by which it is possible, using the known since 1995 ingredients for membrane structure creams, in particular using hydrogenated phosphatidylcholine, stable cream bases for topical application to produce, which have a qualitatively and quantitatively better lamellar structure than by the method previously used with high-pressure homogenization.

Description of the Invention It has now been found that o.b. Membrane structure preparations prepared with hydrogenated phosphatidylcholine, medium chain triglycerides and cosmetic or pharmaceutical agents after fermentation by microorganisms, having pronounced lamellar structures. Advantages of this type of preparation over the conventional method are that can be dispensed with a complex high-pressure homogenization and that the slow fermentation quantitatively and qualitatively much more pronounced multilamellar layers arise, which is very similar to the human skin barrier and their protective functions significantly increased.

By a so-called. Cryofixation and subsequent microscopic observation in the SEM could be found that the multilamellar layers arise much more pronounced than is the case with conventional high-pressure homogenization.

It could be clearly shown that by fermentation with at least one of the lactic acid bacteria of the species Lactobacillus acidophilus, Lactobacillus bulgaricus, Lactobacillus brevis and Streptococcus lactis and / or yeast cultures, especially at least one of the species Saccharomyces cerevisae, Candida utillis, Kluyveromyces lactis , or by the action of the reaction products formed during the fermentation, a quantitatively and qualitatively much better crosslinking takes place to multilamellar stratifications (see Fig. 2), as is done by conventional applied high-pressure homogenization. In the high-pressure homogenization, a mixture of droplet form and lamellar stratification arises predominantly.

Depending on the choice of microorganisms very valuable reaction products can be additionally formed for the skin, such as vitamins A, vitamin B1, B2, B6, B12, vitamin D, folic acid, niacin, enzymes.

In the erfindungsmässig, biotechnological production, a pre-emulsion is initially produced with a predominantly droplet shape, which then by adding the o.b. Over a period of several days, it completely transforms into a multilamellar membrane structure (see Appendix I, Fig. 1 [before fermentation] and Fig. 2 [after fermentation]).

This is clearly due to an increase in viscosity of the pre-emulsion, after progressing fermentation recognizable. Viscosity curve: The initially liquid, milky consistency changes to a creamy consistency as the fermentation progresses, which can only be explained by the transition from a droplet form to a multilamellar structure.

Initial viscosity of the emulsified mixture: 100 mPas

Viscosity after 3 days maturation at 18-23 ° C: 1,200 mPas

Viscosity after 4 days maturation at 18-23 ° C: 2,000 mPas

Viscosity after 5 days of ripening at 18-23 ° C: 4,000 mPas By this biotechnical method of producing membrane-structure preparations, these can also be declared as 100% biological or as probiotic or prebiotic preparations.

Example 1: Production of a membrane structure cream by fermentation by yeast cultures, a mixture of Saccharomyces cerevisae, Candida utillis, Kluyveromyces lactis 2% phosphatidylcholine hydrogenated 25% almond oil 3% shea butter 5% glucose 65% water

Example 2 Preparation of a Membrane Structure Concentrate by Fermentation with a Mixture of Lactobacteria and Yeasts of o.b. Type: 24% phosphatidylcholine hydrogenated 24% neutral oil (medium chain triglycerides) 5% glucose 2% lactose 45% water

Production method: The components are heated to 70-80 ° C and homogenized with conventional homegenizing. After cooling the mixture to 20 ° C the emulsion with liquid consistency about 0.5-1% of a mixture of bacterial and yeast cultures are added and the mixture stored 3-7 days at a constant temperature of 18 ° -23 ° C. The bioreactor is designed so that anaerobic fermentation, ie under exclusion of air, can take place and the resulting carbon dioxide can escape. The bacterial cultures consist mainly of lactobacilli of the species Lactobacillus acidophilus, Lactobacillus bulgaricus, Lactobacillus brevis and Streptococcus lactis. The yeasts are especially Saccharomyces cerevisae, Candida utillis and Kluyveromyces lactis.

Example 3 Production of a day cream by means of a prefefed membrane structure concentrate: 10% MS concentrate (MS 24 KbA) 35% almond oil raf. 5% pentylene glycol nat. 0.2% Na-hyaluronate 2% Aigen extract 0.3% Perfume oil 47.5% water.

Preparation: All components can be combined cold, at room temperature, regardless of the order, and by means of a stir bar or the like. be mixed or homogenized.

Claims (13)

By cold manufacturing, the manufacturing costs and the space required for a production can be significantly reduced. Heat-sensitive substances can be incorporated immediately. This example recipe shows a very nice consistency and a very good storage stability of more than 30 months. It also has a complete lamellar structure, which optimally absorbs the skin and enhances its protective barrier. claims 1. A process for the preparation of cosmetic or pharmaceutical products for topical use, characterized in that a mixture of 1.) phosphatidylcholine, preferably hydrogenated, 0.1-30% 2.) Vegetable oils and / or fats and / or waxes 0 , 5-50% 3.) water and / or hydrous plant extracts 10-90% 4.) mono- or polysaccharides 0.1-20% mixed, homogenized, preferably at a temperature of 40-90 ° C, then at 10 Is then cooled to -40 ° C and then treated with at least one of the bacterial cultures of the type Lactobacillus acidophilus, Lactobacillus bulgaricus, Lactobacillus brevis, Streptococcus lactis and / or at least one of the yeast cultures of the type Saccharomyces cerevisae, Candida utillis and Kluyveromyces lactis. 2. The method according to claim 1, characterized in that the mixture before or after the fermentation cosmetic and / or pharmaceutical agents are added. 3. The method according to any one of claims 1 to 2, characterized in that the mixture extracts of the plant Edelweiss, Leontopodium Alpinum, are added. 4. The method according to any one of claims 1 to 2, characterized in that the mixture extracts of the plant Pistacius Lentiscus, also called mastic or Mastiha be added. 5. The method according to any one of claims 1 to 2, characterized in that the mixture extracts of algae, in particular of the genus Laminaria ochroleuca and / or Alaria Esculenta and / or microalgae, are added. 6. The method according to any one of claims 1 to 2, characterized in that the mixture of vegetable kernel oils, especially grapeseed oil and / or cranberry oil and / or rosehip seed oil, and / or almond oil and / or argan oil are added. 7. The method according to any one of claims 1 to 6, characterized in that the mixture hyaluronic acid or Na-hyaluronate is added. 8. The method according to any one of claims 1 to 7, characterized in that the mixture plant extracts of aloe and / or horsetail be added. 9. The method according to any one of claims 1 to 8, characterized in that the mixture vitamins and / or provitamins and / or enzymes and / or coenzymes and / or proteins are added. 10. The method according to any one of claims 1 to 9, characterized in that form by the fermentation or by the reaction products of the fermentation multilammelar layers. 11. The method according to any one of claims 1 to 10, characterized in that the microorganisms are inactivated or killed after completion of the fermentation and the finished product no longer contains living germs. 12. The method according to any one of claims 1 to 10, characterized in that the end product contains such a high concentration of active bacteria and / or yeast, which prevent colonization with pathogenic germs. 13. The method according to any one of claims 1 to 12, characterized in that a concentrate is prepared, which is added only in a second step at a later time with hydrophilic and / or lipophilic components and active ingredients and processed into a cosmetic or dermatological preparation ,