DE202018000087U1 - Cosmetic agent for skin rejuvenation - Google Patents
Cosmetic agent for skin rejuvenation Download PDFInfo
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- DE202018000087U1 DE202018000087U1 DE202018000087.6U DE202018000087U DE202018000087U1 DE 202018000087 U1 DE202018000087 U1 DE 202018000087U1 DE 202018000087 U DE202018000087 U DE 202018000087U DE 202018000087 U1 DE202018000087 U1 DE 202018000087U1
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- 239000002537 cosmetic Substances 0.000 title claims abstract description 8
- 230000003716 rejuvenation Effects 0.000 title claims abstract description 6
- OHCQJHSOBUTRHG-KGGHGJDLSA-N FORSKOLIN Chemical compound O=C([C@@]12O)C[C@](C)(C=C)O[C@]1(C)[C@@H](OC(=O)C)[C@@H](O)[C@@H]1[C@]2(C)[C@@H](O)CCC1(C)C OHCQJHSOBUTRHG-KGGHGJDLSA-N 0.000 claims abstract description 27
- SUZLHDUTVMZSEV-UHFFFAOYSA-N Deoxycoleonol Natural products C12C(=O)CC(C)(C=C)OC2(C)C(OC(=O)C)C(O)C2C1(C)C(O)CCC2(C)C SUZLHDUTVMZSEV-UHFFFAOYSA-N 0.000 claims abstract description 13
- OHCQJHSOBUTRHG-UHFFFAOYSA-N colforsin Natural products OC12C(=O)CC(C)(C=C)OC1(C)C(OC(=O)C)C(O)C1C2(C)C(O)CCC1(C)C OHCQJHSOBUTRHG-UHFFFAOYSA-N 0.000 claims abstract description 13
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- BUHVIAUBTBOHAG-FOYDDCNASA-N (2r,3r,4s,5r)-2-[6-[[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]amino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol Chemical compound COC1=CC(OC)=CC(C(CNC=2C=3N=CN(C=3N=CN=2)[C@H]2[C@@H]([C@H](O)[C@@H](CO)O2)O)C=2C(=CC=CC=2)C)=C1 BUHVIAUBTBOHAG-FOYDDCNASA-N 0.000 description 1
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- RQFCJASXJCIDSX-GIMIYPNGSA-N [(2s,3r,4s,5s)-5-(2-amino-6-oxo-3h-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@H]1O[C@@H](COP(O)(O)=O)[C@H](O)[C@@H]1O RQFCJASXJCIDSX-GIMIYPNGSA-N 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/08—Anti-ageing preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Dermatology (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Kosmetisches Mittel zur Hautverjüngung, dadurch gekennzeichnet, dass es den Wirkstoff Forskolin, entweder in Reinform oder als Bestandteil eines Pflanzenextraktes beinhaltet, oder dass es als Wirkstoff bereits existierende oder noch zu entwickelnde chemische Derivate des Forskolins, die dem Forskolin in seiner Eigenschaft als Rezeptor unabhängigem Stimulator der zellularen cAMP-Synthese ähneln, beinhaltetCosmetic agent for skin rejuvenation, characterized in that it contains the active ingredient forskolin, either in pure form or as part of a plant extract, or that it as an active ingredient already existing or yet to be developed chemical derivatives of forskolin, the forskolin in its capacity as a receptor independent stimulator similar to cellular cAMP synthesis
Description
Bereich der Erfindung: Die vorliegende Erfindung fällt in den Bereich der Kosmetik und bezieht sich auf den kosmetischen Gebrauch von Wirkstoffen zur Hautverjüngung.Field of the Invention: The present invention is in the field of cosmetics and relates to the cosmetic use of skin rejuvenation agents.
Altersabhängig, Hauttyp bedingt und durch Umwelteinflüssen beeinträchtigt, verändert sich die einstmals glatte, faltenfreie, jugendliche Haut. Mit zunehmendem Alter wird die Haut dünner, die dermale Matrix verliert an Substanz und UV-Licht führt zu epidermal/dermaler DNA-Schädigung und irregulärem Kollagenabbau. Dadurch wird die Haut schlaff und faltig und verliert ihren jugendlichen Glanz. Da die Haut und insbesondere die Gesichtshaut stets der Betrachtung durch andere Menschen ausgesetzt ist, und eine jugendliche Haut für Lebensfreude, Schaffenskraft und Attraktivität steht, wird bei Alterszeichen der Haut nach Abhilfe gesucht.Age-dependent, skin-type conditioned and affected by environmental influences, the once smooth, wrinkle-free, youthful skin changes. With age, the skin becomes thinner, the dermal matrix loses substance and UV light leads to epidermal / dermal DNA damage and irregular collagen degradation. As a result, the skin becomes flabby and wrinkled and loses its youthful shine. Since the skin and especially the facial skin is always exposed to the consideration of other people, and a youthful skin for zest for life, creativeness and attractiveness, is looking for a remedy for age signs of the skin.
Problem: Den Alterszeichen der Haut kann man aktuell nur durch Injektion von marktgängigen Fillern, die z. B. Hyaluronsäure enthalten, Botox oder auch mit chirurgischen Maßnahmen Abhilfe schaffen. Alle marktüblichen Antiaging-Cremes versagten bislang im Test, und ihre Versprechungen bezüglich Faltenreduktion konnten nicht bestätigt werden. Antiaging Maßnahmen wie Filler- oder Botoxinjektion und chirurgisches Facelifting sind kostspielig, invasiv und oft von unerwünschten Nebenwirkungen begleitet. Zu den unerwünschten Nebenwirkungen zählen z. B. Hämatome, Fibrosierungen, Überkorrekturen, übermäßige Mimik-Lähmungen und Narbenbildungen. Es gibt somit aktuell keine kostengünstigen, nebenwirkungsfreien Behandlungen, die eine befriedigende Faltenminderung und Hautverjüngung ermöglichen würden.Problem: The age sign of the skin can currently only by injection of marketable fillers, the z. As hyaluronic acid, Botox or even with surgical measures remedy. All commercially available anti-aging creams have so far failed in testing and their promises of wrinkle reduction could not be confirmed. Antiaging measures such as filler or botox injection and surgical facelift are costly, invasive and often accompanied by unwanted side effects. Among the undesirable side effects include z. As hematomas, fibrosis, overcorrections, excessive facial expressions paralysis and scarring. Thus, there are currently no cost effective, side effect-free treatments that would allow satisfactory wrinkle reduction and skin rejuvenation.
Lösung: Dieses Problem wird durch die in den Schutzansprüchen 1 bis 3 aufgeführten Merkmale gelöst.Solution: This problem is solved by the features listed in claims 1 to 3.
Erreichte Vorteile: Mit der Erfindung wird erreicht, dass an den Hauttyp angepasste Formulierungen, die großflächig und ohne Hautreizungen anwendbar sind, zur deutlichen Hautglättung und Verminderung der Faltentiefe führen, ohne dass es zu irgendeinem Zeitpunkt zu einer Beeinträchtigung des Aussehens kommt. Ein weiterer Vorteil ist die kostengünstige Herstellung und eine zeitlich unbeschränkte Anwendbarkeit eines erfindungsgemäßen Mittels.Advantages achieved: With the invention it is achieved that formulations adapted to the skin type, which are applicable over a large area and without skin irritation, lead to significant smoothing of the skin and reduction of the wrinkle depth, without any impairment of the appearance at any time. Another advantage is the cost-effective production and a time-unlimited applicability of an agent according to the invention.
Detaillierte Beschreibung der Erfindung: Die aktive Komponente, des erfindungsgemäßen kosmetischen Mittels ist der die cAMP-Synthese stimulierende Wirkstoff Forskolin, sei es in Reinsubstanz oder als Bestandteil eines Pflanzenextraktes, oder seine gleichartig wirksamen, chemischen Derivate.Detailed Description of the Invention: The active component of the cosmetic composition of the invention is the cAMP synthesis-stimulating agent, forskolin, whether in pure or as part of a plant extract, or its chemically similar chemical derivative.
Zytosolisches cAMP reguliert die zelluläre Calciumhomöostase und ist damit essentiell für alle Lebensvorgänge. cAMP erfüllt diese zentrale Funktion durch Aktivierung der „Sarko/endoplasmatischen Reticulum Ca2+-ATPase” (SERCA), die cytosolisches Ca2+ unter ATP-Verbrauch in die zellulären Calciumspeicher des sarkoplasmatischen oder endoplasmatischen Retikulums überführt. Diese Rückführung der zellulären Ca2+-Ionen in die intrazellulären Speicher ist essentiell für sämtliche zellulären Calciumsignale, die z. B. zur Kontraktion von Skelettmuskulatur und Herzmuskel führen, oder z. B. die Freisetzung von dermalen Matrixmolekülen aus Fibroblasten ermöglichen. Für das Hautorgan reguliert cAMP im Zusammenspiel mit Ca2+-Ionen u. a. die zellulären Differenzierungsleistungen der Keratinozyten, die geordnete Zellteilung im Stratum basale der Epidermis und die dermale Matrixsynthese. Ein sinkender epidermaler cAMP-Spiegel führt zu vermehrter basaler Zellteilung, Schuppenbildung und Differenzierungsmängeln, die die Hautbarriere schwächen und zu Juckreiz und Trockenheit führen. Im Bereich der Dermis führen sinkende cAMP-Spiegel der Fibroblasten zu verminderter Matrixsynthese insbesondere zu verminderter Hyaluronsäuresynthese.Cytosolic cAMP regulates cellular calcium homeostasis and is therefore essential for all life processes. cAMP accomplishes this central function by activating the "sarco / endoplasmic reticulum Ca2 + ATPase" (SERCA), which transfers cytosolic Ca2 + with ATP consumption into the cellular calcium stores of the sarcoplasmic or endoplasmic reticulum. This recycling of cellular Ca 2+ ions into the intracellular stores is essential for all cellular calcium signals, e.g. B. lead to contraction of skeletal muscle and heart muscle, or z. B. allow the release of dermal matrix molecules from fibroblasts. For the skin organ regulates cAMP in interaction with Ca2 + ions u. a. the cellular differentiation of keratinocytes, the ordered cell division in the stratum basale of the epidermis and the dermal matrix synthesis. Decreasing epidermal cAMP levels lead to increased basal cell division, dandruff and differentiation deficiencies that weaken the skin barrier and cause itching and dryness. In the dermis, decreasing cAMP levels of the fibroblasts lead to reduced matrix synthesis, in particular to reduced hyaluronic acid synthesis.
Für die vorliegende Erfindung sind zwei altersabhängige zellphysiologische Veränderungen von Bedeutung:
- 1. Die Enzymaktivität der Adenylatzyklasen sinkt mit zunehmenem Alter, und es ist altersabhängig eine abnehmende zelluläre cAMP-Synthese in verschiedenen Geweben zu beobachten.
- 2. Die Guanylatzyklasen, also die Enzyme, die das zyklisches Guanosinmonophosphat (cGMP) synthetisieren, werden in verschiedenen Geweben mit zunehmendem Alter vermindert exprimiert. Dadurch sinkt dort der zelluläre cGMP-Spiegel altersabhängig und die gemischtspezifischen PDEs (PDE1, 2, 3, 10 und 11), die sowohl cAMP wie auch cGMP abbauen, hydrolysieren vermehrt cAMP. Mit zunehmendem Alter steigt daher tendentiell der zelluläre cAMP-Abbau.
- 1. The enzyme activity of adenylate cyclases decreases with increasing age and, depending on age, decreasing cellular cAMP synthesis is observed in various tissues.
- 2. The guanylate cyclases, that is, the enzymes that synthesize the cyclic guanosine monophosphate (cGMP), are expressed less in different tissues with increasing age. As a result, the cellular cGMP level decreases age-dependently and the mixed-specific PDEs (PDE1, 2, 3, 10 and 11), which degrade both cAMP and cGMP, increasingly hydrolyze cAMP. As a result, cellular cAMP degradation tends to increase with age.
Altersabhängig sinkt also nicht nur die Synthesekapazität für cAMP, sondern es steigt gleichzeitig der cAMP-Abbau. Altersabhängig ist daher mit abnehmenden zellulären cAMP-Spiegeln und einer chronischen cAMP-Unterversorgung zu rechnen, die zu mehr oder weniger umfangreichen Funktionseinbußen führt. Das erfindungsgemäße Mittel zur Hautverjüngung setzt hier an, indem es die kutane cAMP-Synthese zuverlässig soweit steigert, dass Differenzierungs- und Funktionszustände sich wieder denjenigen eines jugendlichen Alters annähern können.Not only does the synthesis capacity for cAMP decrease, depending on age, it also increases cAMP degradation. Age-dependent, therefore, is to be expected with decreasing cellular cAMP levels and a chronic cAMP deficiency, which leads to more or less extensive loss of function. The skin rejuvenation agent according to the invention starts here by reliably increasing the cutaneous cAMP synthesis to such an extent that differentiation and functional states can once again approach those of an adolescent age.
Konkret unterstützt das erfindungsgemäße Mittel durch Anhebung des dermal/epidermalen cAMP-Spiegels die gesunde Hautstruktur, deren Kennzeichen eine glatte, gut durchblutete Oberfläche ist. Es kommt zu einer dermalen Gefäßerweiterung und Zunahme der dermalen Matrix, insbesondere durch Zunahme dermaler Hyaluronsäure. Dadurch kommt es zu einer Straffung und Glättung der Hautoberfläche.Specifically, the agent of the invention by raising the dermal / epidermal cAMP level supports the healthy skin structure, the hallmark of a smooth, well-perfused Surface is. It comes to a dermal vasodilation and increase in the dermal matrix, in particular by increasing dermaler hyaluronic acid. This leads to a tightening and smoothing of the skin surface.
Diese Eigenschaften werden durch ein erfindungsgemäßes Mittel gewährleistet, das den Wirkstoff in ausreichender Konzentration enthalten muss. Die Anwendung des Wirkstoffes erfordert seine Lösung in einem geeigneten Lösungsmittel, das bei Forskolin vorzugsweise 96%iges Ethanol ist, welches eine Forskolin-Lösungskonzentration von ca. 13% ermöglicht. Nach Schutzanspruch 2 lässt sich eine passende Galenik formen, die der optimalen Wirkstoff-Penetration und -Permeation dient, und die den Wirkstoff bevorzugt in einem Konzentrationsbereich von 0,3% bis 8% enthält. Nach Schutzanspruch 3 können Wirkstoff-Konzentrationen auch außerhalb dieses Bereiches zur Anwendung kommen. Von denen im Schutzanspruch 2 beschriebenen Applikationsformen wird zur Anwendung im Bereich der Lippen eine 1%ige Forskolincreme, z. B. eine 1%ige Ungt. emulsificans aquosum DAB (UEA), bevorzugt. Eine entsprechende Rezeptur ist wie folgt formuliert: 1 g Forskolin gelöst in 10 ml Ethanol 96%, UEA ad 100.0These properties are ensured by an agent according to the invention which must contain the active ingredient in sufficient concentration. The application of the active ingredient requires its solution in a suitable solvent, which is preferably 96% ethanol in the case of forskolin, which makes possible a forskolin solution concentration of about 13%. According to claim 2 protection can form a suitable galenics, which serves the optimal drug penetration and permeation, and preferably contains the drug in a concentration range of 0.3% to 8%. According to protection claim 3, drug concentrations can also be used outside of this range. Of those described in the protection claim 2 application forms for application in the area of the lips a 1% Forskolincreme, z. B. a 1% ung. emulsificans aquosum DAB (UEA), preferred. A corresponding formulation is formulated as follows: 1 g forskolin dissolved in 10 ml ethanol 96%, UEA ad 100.0
Unbedenklichkeit der vorliegenden Erfindung: Forskolin ist ein Inhaltsstoff der Pflanze Plectranthus barbatus, die bereits seit vielen Jahrhunderten in der ayurvedischen Medizin, aber auch in der brasilianischen und afrikanischen Volksmedizin als traditionelles Heilmittel bei verschiedenen inneren Erkrankungen eingesetzt wird, so dass bezgl. der systemischen Verträglichkeit primär keine Bedenken bestehen.Safety of the present invention: Forskolin is an ingredient of the plant Plectranthus barbatus, which has been used for many centuries in Ayurvedic medicine, but also in Brazilian and African folk medicine as a traditional remedy for various internal diseases, so that respect. Systemic compatibility primarily there are no concerns.
Ein Standardisierungsverfahren für Coleus forskohlii-Extrakte ist 2001 in den USA patentiert worden (ForsLean®,
Um das allergene Potential einer Zubereitung im Sinne der vorliegenden Erfindung zu testen, wurden Applikationsversuche (offen und okklusiv) an gesunder Haut der volaren Unterarme und im Gesicht über längere Zeit (ca. 6 Monate) durchgeführt und dokumentiert. Außer einem Forskolin-Erythem, das die Wirksamkeit der erfindungsgemäßen Salbe klinisch sichtbar macht, konnten keine Hautveränderungen im Applikationsbereich beobachtet werden. Insbesondere kam es zu keiner Sensibilisierung oder entzündlichen Hautreizung.In order to test the allergenic potential of a preparation in the sense of the present invention, application tests (open and occlusive) on healthy skin of the volar forearms and on the face over a longer period of time (about 6 months) were carried out and documented. Apart from a forskolin erythema, which makes the effectiveness of the ointment of the invention clinically visible, no skin changes in the application area could be observed. In particular, there was no sensitization or inflammatory skin irritation.
ZITATE ENTHALTEN IN DER BESCHREIBUNG QUOTES INCLUDE IN THE DESCRIPTION
Diese Liste der vom Anmelder aufgeführten Dokumente wurde automatisiert erzeugt und ist ausschließlich zur besseren Information des Lesers aufgenommen. Die Liste ist nicht Bestandteil der deutschen Patent- bzw. Gebrauchsmusteranmeldung. Das DPMA übernimmt keinerlei Haftung für etwaige Fehler oder Auslassungen.This list of the documents listed by the applicant has been generated automatically and is included solely for the better information of the reader. The list is not part of the German patent or utility model application. The DPMA assumes no liability for any errors or omissions.
Zitierte PatentliteraturCited patent literature
- US 5804596 [0013] US 5804596 [0013]
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| DE202018000087.6U DE202018000087U1 (en) | 2018-01-08 | 2018-01-08 | Cosmetic agent for skin rejuvenation |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5804596A (en) | 1997-02-27 | 1998-09-08 | Sabinsa Corporation | Method of preparing a forskohlin composition from forskohlin extract and use of forskohlin for promoting lean body mass and treating mood disorders |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5804596A (en) | 1997-02-27 | 1998-09-08 | Sabinsa Corporation | Method of preparing a forskohlin composition from forskohlin extract and use of forskohlin for promoting lean body mass and treating mood disorders |
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