DE102007018225A1 - Cosmetic or dermatological formulation for promoting regeneration of skin flora, and for use in cosmetic skin care, comprise root parts or ethanolic extracts of Geranium - Google Patents

Abstract

The cosmetic or dermatological formulation includes root parts or ethanolic extracts of the Geranium. The phenoxyethanol, parabens, organic acids and their salts, benzethonium chloride, piroctone olamine, silver compounds, formaldehyde and formaldehyde cleavers or 3-iodo-2-propynyl-butylcarbamate (IPBC), and additionally lactic acid bacteria, particularly Lactobacillus stimulans and a humectant, particularly glycerin are also provided. ACTIVITY : Dermatological. MECHANISM OF ACTION : None given.

Description

The Invention includes cosmetic or dermatological preparations with Pelargonium reniforme / sidoides.

Our Skin is colonized by a variety of bacterial species. Ideally dominate those with a positive health effect, the so-called commensal bacteria, over as well occurring harmful germs. Device this system Out of balance, looks, health and well-being the skin is impaired.

The Skin of patients with atopic dermatitis is almost always with Staphylococci colonized. Investigations show that up to 30 percent of the healthy and over 80 percent of the atopic the skin is colonized with staphylococci. These and similar Germs thrive well on atopic dermatitis, so due to the decreased skin barrier function in atopic dermatitis, too an increased responsiveness of the immune system is busy.

The Staphylococcal superinfection can be caused by topical antibiotic therapy and also by topical steroids containing the reduce bacterial adhesion, be treated. There are anti-inflammatory and immunomodulating drugs suitable, which improve the skin condition and reduce the bacterial density. Also known are antiseptic tinctures and local anti-staphylococcal antibiotic Treatments with fusidic acid and / or mupirocin.

Desirable so there is another way to in particular a cosmetic or dermatological preparation, which, applied topically, leads to a germ reduction, in particular of Staphylococcus aureus.

Desirable It is in particular that this preparation in Atopikern, where the skin flora an increased concentration of staphylococci shows topically applied to an improvement of the atopic Skin condition leads.

Desirable In addition, the preparation is a nourishing Has an effect on the damaged or treated skin.

From the treatment of acute and chronic infectious diseases of the respiratory, - neck, nose and ear Umckaloabo ^® (registered trademark of ISO-Arzneimittel GmbH & Co. KG) is known.

Umckaloabo ^® is known as a natural defense against infection. It is an ethanolic extract from the roots of the South African Cape Pelargonium (Pelagonium reniforme / sidoides, Medical Information Umckaloabo ^® , as of May 2006).

Scopoletin und Umckalin, bei den kondensierten Gerbstoffen um Proanthocyanidine, die hauptsächlich aus Gallocatechin- und Epigallocatechin-Monomeren aufgebaut sind.The root extract of the available drug (extract: ^EPs® 7630) can be obtained by percolation and / or maceration. The extract contains, among other things, multiply substituted benzopyranone derivatives and condensed tannins. The benzopyranone derivatives are 2 to 4-membered hydroxy-, methoxy- and / or sulfoxy-substituted 2 to 4-membered 2H-1-benzopyran-2-ones such as. Scopoletin

Scopoletin and umckalin, in the condensed tannins to proanthocyanidins, which are mainly composed of gallocatechin and epigallocatechin monomers.

100 g Umckaloabo ^® solution contains an ethanolic extract (1 + 10) from roots of Pelargonium reniforme / sidoides 80.0 g, 12% alcohol and 85% glycerol.

• • Bakterien werden an der Vermehrung gehindert,
• • die körpereigene Virenabwehr wird gestärkt und
• • zäher Schleim wird gelöst.

The well-known Umckaloabo ^® mode of action is:

• • Bacteria are prevented from reproducing,
• • the body's own virus defense is strengthened and
• • tough mucus is loosened.

Geranium (Pelargonium, Greek: pelargós = stork) is a genus the beak-billed family. These were used as ornamental plants cultivated and falsely named for a long time Geraniums. The roots of this plant are the foundation from Umckaloabo.

The Cape Pelargonium (Pelargonium reniforme / sidoides) belongs to the family Geraniaceae, the groupage of root tubers. The Cape Pelargonium consists of 20-80 cm tall shrubs with deep red-black Blossoms. The ingredients are essentially coumarins, Gallic acid derivatives, quercetin, flavan-3-ols, phytosterols.

Umckaloabo ^® is used in the treatment of acute and chronic infectious diseases, especially in the respiratory and ear, nose and throat. A topical application is not described.

Umckaloabo ^® was approved on 10 December 2005 by the German Medicines Agency (Federal Institute for Drugs and Medical Devices, BfArM) according to the German Medicines Act as a medicine for the treatment of acute bronchitis (Medical Information Umckaloabo ^® , as of May 2006, approval number: 6189629.00.00) ,

In addition, there are other studies on the use of almond and paranasal sinusitis in children with acute non-group A beta-hemolytic Streptococcus tonsillopharyngitis: A randomized, double-blind, placebo-controlled trial ( Bereznoy W, Riley DS, Wassmer G, Heger M.). Aging. Ther. Health Med. 9/2003, 68-79 ).

The Mechanisms of action of the extract have been in the past in West German university research institutions. These studies showed that Umckaloabo has a threefold effect against viruses, against bacteria and against mucus should possess.

The extract EPs 7630 was able to increase the production of the body's own β-interferon in the event of an infection. It is thus able to protect cells from destruction by viruses. ( Kolodziej H, Schulz V: Umckaloabo - from the traditional application to the modern phytopharmaceutical, DAZ 2003; 12: 1303-1312 ).

Also known is a moderate direct antibacterial activity against various Gram-positive bacteria and Gram-negative bacteria ( Kolodziej H, Schulz V: Umckaloabo - from the traditional application to the modern phytopharmaceutical, DAZ 2003; 12: 1303-1312 ). However, these effects are relatively weak and can not explain the clinical efficacy. In contrast, potent indirect antibacterial effects have been demonstrated to inhibit the attachment of bacteria to the airway mucosa, which is the first step in infection, but also to infiltrate and pass the bacteria into the deeper tissue layers that allow the infection to spread Umckaloabo prevents ( Conrad A: 4th and 5th Congress Phytopharmaceuticals and Phytotherapy - Research and Practice, Berlin 2005 and 2006 ).

However, it is not known to use Umckaloabo ^® as or in cosmetics.

It is therefore desirable to make the known effects of Umckaloabo ^® extract for cosmetic / dermatological applications available

The The invention relates to cosmetic or dermatological preparations comprising parts or extracts of geranium, especially of roots Pelargonium, and in particular their ethanolic extracts.

Farther The invention includes the use of parts or extracts of the Pelargonium, especially the roots of geranium and their ethanolic extracts, for the manufacture of a medicament or a Cosmetics for topical skin treatment or care.

• – Extrakte, wässrige und ethanolische Auszüge, Teil- oder Vollextrakte
• – Lösungen, Mischungen, Gemenge
• – Trockensubstanz
• – insbesondere Teile oder Extrakte der Wurzel der Kapland-Pelargonie (Pelargonium reniforme/sidoides)
• – Benzopyranonderivate, insbesondere in 5- bis 8-Position zwei- bis vierfach mit Hydroxy, Methoxy und/oder Sulfooxy substituierte 2H-1-Benzopyran-2-one, z. B. Scopoletin; Umckalin, kondensierte Gerbstoffe, Proanthocyanidine, die hauptsächlich aus Gallocatechin- und Epigallocatechin-Monomeren aufgebaut sind,
• – und weitere mögliche Einsatzformen der Pelargonie

verstandenAmong parts or extracts of geranium is according to the invention

• - extracts, aqueous and ethanolic extracts, partial or full extracts
• - Solutions, mixtures, mixtures
• - dry matter
• - especially parts or extracts of the root of the Cape Pelargonium (Pelargonium reniforme / sidoides)
• - Benzopyranonderivate, especially in the 5- to 8-position two to four times with hydroxy, methoxy and / or sulfooxy substituted 2H-1-benzopyran-2-ones, z. Scopoletin; Umckalin, condensed tannins, proanthocyanidins, which are mainly composed of gallocatechin and epigallocatechin monomers,
• - and other possible uses of geranium

Understood

• – der ethanolischen Extrakt mit 12% Ethanol (Apothekenware, Umckaluabo^®)
• – Trockenextrakt der Wurzel, erhältlich z. B. von Symrise, Neo Extrapone Pelargonium reniforme, Symrise Prod.-Nr.: 600405) aus ethanolisch/wässrige Destillation oder rein ethanolischer Extraktion
• – ein Pflanzenextrakt basierend auf Wasser und Propylenglycol, wobei der Wirkstoff mit 70:30 Ethanol/Wasser extrahiert wurde, wobei 1 kg Extrakt den ethanolisch wässrigen Auszug von 150 g Trockensubstanz beinhaltet (umgerechnet 1350 g frisches Pflanzenmaterial).

Preference is given to using in the preparations according to the invention:

• - the ethanolic extract with 12% ethanol (pharmacy goods, Umckaluabo ^® )
• Dry extract of the root, available e.g. From Symrise, Neo Extrapone Pelargonium reniforme, Symrise Prod. No .: 600405) from ethanolic / aqueous distillation or pure ethanolic extraction
• - A plant extract based on water and propylene glycol, wherein the active ingredient was extracted with 70:30 ethanol / water, wherein 1 kg of extract contains the ethanolic aqueous extract of 150 g of dry matter (converted 1350 g of fresh plant material).

As well are the term Pelargoniumextrakte the aforementioned compositions to understand the at least one of the compounds chosen from the group multiply substituted benzopyranone derivatives and condensed Include tannins.

Prefers be ethanolic extracts from the roots of pelagonium reniforme / sidoides with preferably 12 vol% ethanol used.

To the Proof of activity were the ethanolic extracts to 1 wt.% in emulsions (O / W and W / O) used to produce an antimicrobial Check effect on topical application.

• 1. ohne Konservierungssystem
• 2. zusätzlich zum bestehenden Konservierungssystem
• 3. sowie als Vergleich die Formulierung mit Konservierungssystem ohne Extrakt untersucht

In the series of experiments described below, the antimicrobial influence of the extract used on the cosmetic formulation (O / W, W / O) was investigated. Here, 1% of the extract in the formulation

• 1. without preservation system
• 2. in addition to the existing preservation system
• 3. and as a comparison, the formulation with preservative system without extract examined

in the Conservation stress test was the Absterbekinetik to the usual Germ spectrum consisting of gram-positive staphylococci (aureus and epidermidis), Gram-negative pseudomonads (aeruginosa, putida, cepacia) and Escherchia coli, as well as on yeasts (Candida albicans) and fungi (Aspergillus niger).

Instead of a germ reduction was carried out in E. coli, Ps. putida and candida albicans germinate a growth, in Aspergillus a marginal reduction (1 power of ten germ reduction within 28 days) and at the Species Ps. Aeruginosa there is a significant germ reduction.

In another study was 1% by weight of the ethanol extract the root pelagonium reniforme / sidoides and 0.8% by weight of phenoxyethanol, 0.3% by weight of methylparaben and 0.1% by weight of propylparaben in one O / W and a W / O emulsions used.

Tested the selective effect on gram-positive staphylococci (epidermides and aureus) in the preservation challenge test.

It could hereby surprisingly a synergism in the Germ number reduction can be observed.

• Konservierungssystem: 0,8% Phenoxyethanol, 0,35 Methylparaben, 0,1% Propylparaben Emulgatorsystem: Sorbitanstearate, Cetylalkohol

After 24 h, a germ reduction of 4 orders of magnitude was carried out. This phenomenon could be reconstructed in two different O / W formulations with different emulsifier systems. O / W I preservative system + 1% umckaluabo extract OW II preservation system analogue O / WI OW III Without preservation with 1% Umckaluabo extract Test germ mixture: Staphylococcus aureus / epidermides initial bacterial count CFU / g 270000 270000 270000 Germ number after 24 h <10 15000 24000 Germ number after 7 days <10 100 100 Germ number after 14 <10 <10 <10 Tg Germ number after 28 days <10 <10 <10

• Preservative system: 0.8% phenoxyethanol, 0.35 methylparaben, 0.1% propylparaben emulsifier system: sorbitan stearate, cetyl alcohol

1% Umckaloabo extract works in combination with the existing preservative system synergistic to the reduction of gram-positive staphylococci aureus and epidermides out of the wording.

These specific synergistic effect of Pelargonium extract with known cosmetic preservatives or stabilizers, such as phenoxyethanol, parabens and / or, organic acids as well their salts, benzethonium chloride, piroctone olamine. Silver compounds, Formaldehyde and formaldehyde releaser, IPBC (iodopropynyl butyl carbamate), Kathon CG and other customary preservative systems was surprising and unpredictable.

Especially in a preparation based on an O / W emulsion showed advantageous Bacteria reduction numbers. As known to those skilled in the art, hold themselves Microorganisms in the water phase of cosmetic preparations on. Antimicrobial ingredients need to work to be able to, also in the water phase or in the interface Be water / oil. To target antimicrobial effectiveness to be able to unfold, may be effective substances not be immobilized by formula ingredients, what does theirs mean Bioavailability in the system must be guaranteed be. An O / W formulation is here a more suitable system than a W / O emulsion to a good bioavailability of the substance to ensure.

According to the invention by the cosmetic or dermatological preparation Pelargonium parts or extracts prefer extracts from the roots of Pelagonium reniforme / sidoides, especially in atopic persons, at which the skin flora an increased concentration of staphylococci shows, an advantageous skin treatment and / or care for the first time possible.

A Presentation in an emulsion basis appears above also beneficial because the atopic skin is extremely dry and should be maintained very intensively. Again, the invention provides Preparation remedy.

Of the Content of pelargonium extracts or parts is advantageous between 0.01-50 wt.%, In particular between 0.01 and 10 wt.%, Particularly advantageously between 0.1 and 2 wt.% Each based on the total weight of the preparation.

The Preparation according to the invention preferably comprises at least 0.1% by weight, a proportion of 0.5 is particularly advantageous up to 5% by weight, in particular about 1% by weight, of the proportion of parts or extracts the geranium. When using the extract, the unit value refers on the proportion of the extract.

Prefers are ethanolic extracts from the roots of Pelagonium reniforme / sidoides with preferably 12% by volume of ethanol.

in principle is the topical application of the invention Compounds in different, in particular W / O as well as O / W formulations and other cosmetic dosage forms possible and prefers. In particular, a preparation based on is advantageous an O / W emulsion.

When According to the invention, cosmetic and / or dermatological Formulation can be put together as usual and in particular for the treatment and care of the skin and / or hair, as a make-up product in decorative cosmetics or as Sunscreens or so-called pre or Aftersunpräparat serve. Accordingly, the inventive Formulations - depending on their structure - for example used as skin protection cream, face cream, Cleansing Milk, Sunscreen Lotion, Nourishing Cream, Day or night cream, etc.

It Of course, the person skilled in the art knows that demanding cosmetic or dermatological compositions mostly not Without the usual auxiliaries and additives are conceivable. These include, for example, bodying agents, fillers, Perfume, dyes, emulsifiers, additional active ingredients such as vitamins or proteins, light stabilizers, stabilizers, insect repellents, Alcohol, water, salts, antimicrobial, proteolytic or keratolytic active substances, preservatives, bactericides, substances for preventing foaming, pigments which are coloring Have effect, thickener, moisturizing and / or moisturizing Substances, fats, oils, waxes or other common Components of a cosmetic or dermatological formulation such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents, silicone derivatives or moisturizers etc.

parts or extracts of geranium, especially ethanolic extracts from the roots of the pelagonium reniforme / sidoides with preferred 12% by volume ethanol can be used to make a medicine or cosmetics are used. Depending on the therapy or treatment measure can dermatologically effective according to the invention or make cosmetic preparations, the latter a a use for the therapeutic treatment of the human and animal body is excluded.

Prefers is the use of the preparation according to the invention for cosmetic skin care.

The Problems with skin dryness can be added with humectants treated so that the use of humectants, here primarily glycerol, in the inventive Preparations is preferred.

Lactic acid bacteria (Lactobacilli) In particular Lactobacillus stimulans can be the fast Promote regeneration of the protective skin flora. Stimulated by the release of growth-promoting substances he the settlement of his healthy relatives. Because the quick balancing of skin irritations has a high cosmetic relevance are Such microorganisms for use in lotions or Creams and also described in healing ointments or patches.

A Combination of parts or extracts of geranium, in particular ethanolic extracts from the roots of the pelagonium reniforme / sidoides, with lactic acid bacteria (lactobacilli), in particular Lactobacillus Stimulant is thus also a preferred combination.

The following examples describe preparations according to the invention. The proportions relate to weight percentages based on the respective total mass of the preparation. O / W cream example 1 2 3 4 5 6 7 8th Sorbitan stearate 2 Cetearyl Alcohol, PEG 40 Castor Oil, Soldium Cetearyl Sulfate 3 Polysorbate 60 1 2.25 Polyglyceryl-3-methyl glucose distearate 2 PEG-40 stearates 1.8 0.8 0.8 Glyceryl stearate 0.7 2.7 3 Potassium Cetyl Phosphate + Hydrogenated Palm Glycerides 2.5 Polyglyceryl-3 distearate 3 Lanolin alcohol 0.5 Stearyl alcohol 2 2 Cetearyl alcohol 2 2 2.5 1 3 1 2 2 Cetyl alcohol 1 1 0.5 Paraffin perliquidum 6 3 0.5 Cetyl palmitate 8th petrolatum 2 C12-15 alkyl benzoates 1.5 4 2.5 3 2 octyldodecanol 3 4 2.5 3 3 Dicaprylyl ether 2 4 2.5 2 Isohexadecan 1 3 Dimethicone 1 2 1 1 2 Cyclomethicone 2 3 1 2 2 isopropyl palmitate 1 Isohexadecan 5 1 Caprylic / Capric triglycerides 2 2 2 shea butter 1 2 avocado oil 1 squalane 1 Xanthan gum 12:15 hydroxyethyl 0.1 0.1 carrageenan 0.1 Alkyl acrylate crosspolymer 0.5 0.4 0.4 0.4 0.3 Ammonium acryloyl demethyl taurate 0.1 Polyacrylic Carbomer 0.25 0.1 Acrylate Crosspolymer 0.4 Water demon. Ad 100 Ad 100 Ad 100 Ad 100 Ad 100 Ad 100 Ad 100 Ad 100 butylene 2 glycerin 5 10 10 7.5 5 10 7.5 8th tocopheryl acetate 0.5 0.5 panthenol 2 1,2 hexanediol 0.5 1,2-octanediol 0.5 Ubiquinone (Q10) 12:05 TiO2 1 1 ethylhexylmethoxycinnamate 2 3 5 2 ethylhexyl 2-cyano-3-diphenylacrylate (octocrylene) 5 butylmethoxydibenzoylmethane 1 Citric acid / sodium citrate qs Sodium ascorbyl phosphate 12:01 Pelargonium reniforme / sidoides Umckaluabo extract (ethanolic 12%) 1 0.5 0.6 2 3 5 Pelargonium reniforme / sidoides dry extract 0.2 0.4 Trisodium EDTA 0.15 0.15 0.1 0.15 0.1 Fillers (distarch phosphate, SiO2, talc, aluminum stearate, aluminum Starch octenyl succinate, corn starch, rice starch, nylon-12, tabioca starch) 3 1.5 1 3 Propylparaben 12:05 0.1 0.05 0.05 0.05 0.1 methylparaben 0.1 0.3 0.15 0.2 0.1 0.1 0.1 phenoxyethanol 0.45 0.8 0.4 0.8 0.5 0.5 0.3 benzethonium 0.1 Piroctone Olamine 0.05 dehydroacetic 0.3 sodium hydroxide qs qs qs qs qs qs qs qs

QUOTES INCLUDE IN THE DESCRIPTION

This list The documents listed by the applicant have been automated generated and is solely for better information recorded by the reader. The list is not part of the German Patent or utility model application. The DPMA takes over no liability for any errors or omissions.

Cited non-patent literature

• - Bereznoy W, Riley DS, Wassmer G, Heger M.). Aging. Ther. Health Med. 9/2003, 68-79 [0017]
• - Kolodziej H, Schulz V: Umckaloabo - from traditional application to modern phytopharmaceutical, DAZ 2003; 12: 1303-1312 [0019]
• - Kolodziej H, Schulz V: Umckaloabo - from traditional application to modern phytopharmaceutical, DAZ 2003; 12: 1303-1312 [0020]
• - Conrad A: 4th and 5th Congress Phytopharmaceuticals and Phytotherapy - Research and Practice, Berlin 2005 and 2006 [0020]

Claims (9)

Cosmetic or dermatological preparation comprising parts or extracts of geranium. Cosmetic or dermatological preparation comprising Parts of the roots of geranium and / or ethanolic extracts the geranium. A preparation according to claim 1 or 2 comprising between 0.01-50% by weight, in particular between 0.01 and 10% by weight, particularly advantageous between 0.1 and 2 wt.% Each based on the total weight of the preparation, parts or extracts of geranium. A preparation according to claim 1, 2 or 3 comprising phenoxyethanol, Parabens, organic acids and their salts, benzethonium chloride, Piroctone Olamine, silver compounds, formaldehyde and Formaldehydabspalter and / or IPBC. Preparation according to one of the preceding claims additionally comprising lactic acid bacteria (lactobacilli), in particular Lactobacillus stimulans. Preparation according to one of the preceding claims additionally comprising humectants, in particular glycerol. Preparation according to one of the preceding claims as O / W emulsion. Use of a preparation according to one of the preceding Claims to promote the regeneration of the skin flora. Use of a preparation according to one of the preceding Claims for cosmetic skin care.