Composition and uses for influencing hair growth
Abstract
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12 claims: 7 independent, 5 dependent
- 1Zastrzeżenia patentowe 1. Kompozycja, w szczególności o właściwości wpływania na wzrost włosów, znamienna tym, że kompozycja ta zawiera połączenie (i) co najmniej jednego inhibitora aromatazy, wybranego z grupy ekstraktów rzepaku wykazuj ących hamowanie aromatazy, i (ii) co najmniej jednego ekstraktu roślinnego, który zawiera jedną lub większą liczbę substancji czynnych wyekstrahowanych z rośliny, wybraną/wybranych z grupy obejmującej inhibitory 5a-reduktazy typu I i/lub typu II i blokery receptora androgenowego, przy czym co najmniej jeden ekstrakt roślinny jest z palmy sabałowej (Serenoa Serrulata Fruit Extract).
- 2Kompozycja według zastrzeżenia 1, znamienna tym, że inhibitor aromatazy ma właściwość hamowania również 5a-reduktazy.
- 3Kompozycja według zastrzeżenia 1, znamienna tym, że składnik (i) stanowi wyłącznie ekstrakt z rzepaku.
- 4Kompozycja według zastrzeżenia 1, znamienna tym, że składnik (i) jest taki, że ekstrakt z rzepaku jest połączony z syntetyzowanym chemicznie inhibitorem aromatazy.
- 5Kompozycja według któregokolwiek z poprzednich zastrzeżeń, znamienna tym, że ekstraktem z palmy sabałowej jest etanolowy ekstrakt z owoców palmy sabałowej.
- 6Kompozycja według któregokolwiek z poprzednich zastrzeżeń, znamienna tym, że ekstrakt roślinny składnika (ii) stanowi ekstrakt bogaty w fitosterole i/lub flawonoidy.
- 7Kompozycja według zastrzeżenia 4-6, znamienna tym, że syntetyzowany chemicznie inhibitor aromatazy stanowi 4-hydroksyandrostendion lub jego pochodna w postaci estru kwasu 4-karboksylowego.
- 8Kompozycja według zastrzeżenia 7, znamienna tym, że pochodną w postaci estru kwasu 4-karboksylowego jest 4-acetoksyandrostendion.
- 9Kompozycja według jednego z poprzednich zastrzeżeń, znamienna tym, że poza składnikiem (i) i (ii) nie dodaje się dalszych substancji czynnych, w szczególności nie dodaje się metali toksycznych, takich jak miedź, lecz co najwyżej odpowiednie nośniki, substancje pomocnicze i dodatki.
- 10Kompozycja według któregokolwiek z poprzednich zastrzeżeń, znamienna tym, że formułuje się j ą odpowiednio do podawania miejscowego.
- 11Zastosowanie kompozycji według któregokolwiek z zastrzeżeń 1-10 do zastosowania kosmetycznego.
- 12Nie-terapeutyczne zastosowanie kompozycji według jednego z zastrzeżeń 1 do 10, • do zmniejszania wzrostu włosów na ciele lub na twarzy, • do usuwania włosów, • do depigmentacji owłosienia na ciele u kobiet, i/lub • do sprzyjania wzrostowi włosów w odniesieniu do włosów na skórze głowy, przy czym utrzymuje się pigmentacj ę włosów lub sprzyja się repigmentacji włosów. Uprawniony:LUCOLAS-M.D Ltd. Pełnomocnik: mgr inż. Agnieszka Marszałek Rzecznik patentowy
Independent claims12
156 paragraphs in 1 section, as filed
[0001] The present invention relates to a composition that is particularly suitable for affecting hair growth as well as its related uses.
[0002] For many decades, research into hormone-dependent hair growth has been dominated by androgens. To this day, androgen metabolism and androgen receptors are the targets of both systemic pharmacological effects on hair growth in medicine and local cosmetic attempts to regulate hair growth.
However, it has long been known that estrogens also have a significant effect on hair follicles in terms of growth and cycle. Namely, by binding to local estrogen receptors.
[0003] Accordingly, it has been observed that an increase in local estradiol levels as a result of topical administration of estradiol caused body hair growth. The opposite observation could be made with topical administration of estradiol to the scalp: in this case, elevated estradiol levels or elevated local estradiol effects lead to hair loss. The basis for a positive effect on scalp hair is that each hair follicle is a unique "microcosm" that has the ability to completely self-regenerate. It is based on the interactions of its epithelial components and mesenchyme. These interactions also apply to the local formation and interaction of sex hormones.
These mechanisms obviously play the same important role in body hair, although in part acting against each other. In addition to their regulatory function in the hair follicle cycle, these factors also play an important role in hair pigmentation.
The key concept is therefore that, as a rule, estrogens and androgens have the effect of directly modulating hair growth and, in addition, indirectly act by changing the expression of important factors modulating hair growth. The basis of this concept is that two basic enzymes for the genesis of active sex hormones, aromatase for the conversion of testosterone to estradiol and 5-α-reductase (type I and type II) for the conversion of testosterone to dihydrotestosterone, are strongly expressed and active in the area of hair follicles. The same applies to the expression of α and β estrogen receptors and androgen receptors. This means that the skin not only has a protective and regulatory function, but also that the skin is an important endocrine organ.
[0004] In the past, it has been suggested to use aromatase inhibitors as cosmetic agents and for affecting hair growth, as e.g. as discussed in WO 96/08231 A.
[0005] In a series of documents, extracts of lobster palm (Serenoa repens) are mentioned, mainly in connection with pharmaceutical and therapeutic concepts, see e.g. JP 2007230888 A for androgen independent cancer; US 2006246153 A with regard to benign prostatic hyperplasia (BPH); JP 2007051129 A as a component of the composition for an angiotensin type II1 receptor antagonist or as an inhibitor of angiotensin I converting enzyme; WO 03/030887 A in the treatment of sexual dysfunction or erectile dysfunction; US 6599540 for the prevention and / or treatment of prostate cancer; US 2002001633 A for the treatment of, inter alia, BPH and prostate cancer; DE 10127897 for the treatment of osteoporosis or related diseases; WO 01/39656 A for the treatment of symptoms associated with lower urinary tract dysfunction (LUTS) and BPH; FR 2791255 regarding the antiandrogenic effect of cosmetic and dermo-pharmaceutical compositions; JP 2000256204 A for compositions with increased inhibitory activity against prostatic hyperplasia; WO 99/21009 A for the production of suitable extracts from saw palmetto; WO 97/03639, for topical cosmetic applications on the skin; EP-A-0204877 as a topical dermatological composition for the treatment of acne; suitably in combination with other active ingredients as well as carriers. In addition, the following documents cover hair applications, see e.g. JP 2002322050 relates to the composition of Sabal Palm Extract, cystine (raw hair material), citric acid and theanine for activating hair root and promoting hair growth by oral administration, US 2001 033849 A relates to cosmetic compositions containing fatty acids and anti-androgenic sterols from Sabal palm extract and / or Cucurbita seeds (Cucurbita pepo), US 6019976 relates to medicinal preparations containing saw palmetto extract, vitamin B6, vitamin B3, zinc salt and L-arginine for the treatment of male pattern baldness by topical application to hair, JP 11 092340 A applies to the preparation of saw palmetto extract and a certain amount of oil-soluble ingredient from Allium sativum L to promote blood flow and subsequent expected improvement of regeneration hair, and therefore, for the treatment or prevention of male baldness, JP 60215608A relates to saw palmetto extract for a hair strengthening preparation, WO 03/013561 A relates to pharmaceutical and / or cosmetic compositions containing saw palmetto extracts and Vitis vinifera as effective ingredients for the treatment and prevention of hair loss, dandruff and seborrhea, as well as WO 98/33472 relates to extracts from saber palm or their ingredients for for the prevention and / or treatment of androgenetic alopecia and / or hirsutism.
[0006] WO 91102516 A relates to the use of coleus extract for skin pigmentation, whereby additional substances such as xanthine, theophylline, tyrosine, quinine, skin irritants, 5a-reductase inhibitors and Sabal palm extract may be used, however, this document discloses with reference to EP-AO 293 837, which concerns the effect of melanocytes on hair roots, that is, in the treatment of hair - that, especially with regard to metabolism, there are significant differences between melanocytes in the hair follicles and melanocytes in the skin.
[0007] Other documents relate to attempts to influence, and in particular, inhibition of 5α reductase.
[0008] US 7238 375 B1 describes four complexes 1-4, where complexes 1-3 should prevent hair loss and complex 4 should promote hair growth. Complex 2 includes a mixture of copper ions, palm extract (Serenoa repens), extract from Pygeum (Pygeum africanum), nettle extract (Urtica dioica), zinc, vitamin B6 and linolenic acid.
US7105573B2 and US2007 / 0066661A1 relate to further proposals for the treatment of alopecia and other diseases associated with hair follicles.
In an article by W.CHEN et al., "Cutaneous Androgen Metabolism: Basic Research and Clinical Perspectives," J Invest Dermatol. vol. 119, No. 5, November 2002, pp. 992-1007, generally describes androgen metabolism in the skin; and in the article by R. HOFFMANN and R.HAPPLE, "Current understanding of androgenetic alopecia. Part I: Etiopathogenesis ”, Eur J Dermatol. Volume 10, No. 4, June 2000, p. 319-327 gives a general overview of the knowledge of androgenetic alopecia (AGA), with both articles cited giving the impression of the complexity of biochemical foundations in anatomical regions that are relevant to skin and hair related phenomena.
In ME SAWAYA ME, "Different Levels of 5a-Reductase Type I and II, Aromatase, and Androgen Receptor in Hair Follicles of Women and Men with Androgenetic Alopecia", J Invest Dermatol. volume 109, no. 3, September 1997, pp. 296-300 differences in the occurrence of androgen receptor and steroid converting enzymes (5α reductase, aromatase) in men and women were described and it was speculated whether they could be responsible for the different clinical picture of AGA in men and women.
A list of possible active ingredients that can be assigned to the appropriate plants can be found in Dr. Duke's Phytochemical and Ethnobotanical Databases,
URL:<a href="http://www.ars-grin.gov/duke">http://www.ars-grin.gov/duke</a>.
[0009] As explained above, influencing hair growth relates to an extremely complex system. This is reflected in the appropriately high level of complexity of biochemical analyzes and suggestions regarding their impact. However, despite the large number of trials carried out with respect to existing solutions, it has not been possible to develop an appropriate balance regarding the differentiated local effects of relevant metabolites such as estrogens (especially estradiol) and androgens (in particular dihydrotestosterone), depending on whether hair growth or for hair removal or prevention of hair regrowth after epilation or depilation, depending on the area of skin to be treated, i.e. on one side of the scalp and body including the face (especially in the chin area) on the other, and depending on whether it affects women or men. A satisfactorily differentiated solution for targeted influence in both men and women has not yet been discovered. In particular, hair depigmentation is an unpredictable problem when affecting hair growth.
[0010] Therefore, it is an object of the present invention to provide an improved composition for affecting hair growth and hair pigmentation.
[0011] The present invention thus provides the subject matter defined in the claims.
[0012] According to the invention, it has been surprisingly found that in the case where at least one aromatase inhibitor selected from the group of rapeseed extracts exhibiting aromatase inhibition, (component (i)) is combined with at least one plant extract (component (II)), which contains one or more active substances extracted from the plant, selected / selected from the group consisting of type I and / or type II 5a-reductase inhibitors and androgen receptor blockers, wherein at least one plant extract is of the sabal palm (Serenoa Serrulata Fruit Extract), not only targeted, controllable influencing of hair growth is achieved, but at the same time hair pigmentation is controlled. In this way, either hair depigmentation in women can be achieved or, on the other hand, protection against hair depigmentation in men.
[0013] The new combination according to the present invention is characterized in that it can advantageously influence the growth of hair in a targeted manner, namely depending on whether it concerns hair growth or hair removal or inhibition of new hair growth depending on the body area respectively (scalp / scalp or body / face / chin area), depending on whether it affects women or men. It has surprisingly been found that the combination according to the invention allows targeted and differentiated influence of metabolites that are important for hair growth, such as estradiol and dihydrotestosterone, with respect to local conditions - i.e. aimed at promoting scalp / scalp hair growth in a man or woman and hair removal or inhibiting new hair growth after epilation or depilation on the body (including the chin area), in a man or woman - combined with the possibility of beneficial effects on hair pigmentation, in particular hair repigmentation, and therefore a return to the natural hair color.
[0014] For the differentiated combined effects of the invention, it is important to quickly and appropriately lead to effective aromatase inhibition, therefore, component (i) is selected from aromatase inhibiting rapeseed extracts. [0015] As a chemically synthesized aromatase inhibitor that can be used in the composition, a substance known to perform this function may be used, cf. e.g. AMH Brodie in: "J. Steorid Biochem. Molec. Biol. ", Volume 49, No. 4-6, p. 281-287 (1994), as well as PE Goss and KMEH Gwyn in: "Journal of Clinical Oncology", vol. 12, No. 11, pp. 2460-2470 (1994), and for the detection of aromatase inhibition see for example AMH Brodie et al. in: "J. Biochem Steroid. Molec. Biol. ", Vol. 7, p. 787793 (1976) and DA Marsh et al. in: "J. Med. Chem. ", Vol. 28, pp. 788-795 (1985). Suitable aromatase inhibitors can, for example, be selected from the following group of compounds:
Steroid aromatase inhibitors:
4-hydroxyandrost-4-en-3,17-dione (formestane and lentarone), 6-methyleneandrostra-1,4-diene-3,17-dione (exemestane),
10- (2-propynyl) ester-4-en-3,17-dione (MDL 18962)
7-alpha substituted androstenedione 1,4,6-androstatriene-3,17-dione (ATD) derivatives
10-oxirane- or 10-thiane-substituted androgens 10-propargylester-4-en-3,17-dione derivative 10-propargylester-4-en-3,17-propionate-10- (2-propynyl) 13-retro- antiprogestin
14-alpha-hydroxy-4-androstene-3,6,17-trion (14-alpha-OHAT)
16- or 19-substituted androst-4-enes 19- (cyclopropylamino) androst-4-en-3,17-dione 19- (ethylenedithio) androst-4-en-3,17-dione 19-oxiranyl- and 19- tiiranylo-steroids
19-thiomethyl- and 19-azido-androstenedione
1-methyl-androsta-1,4-diene-3,17-dione (atamestane)
2,2-dimethyl-4-hydroxy-4-androstene-3,17-dione
3-alpha-methoxyandrost-4-ene-6,17-dione derivative of 3-beta-hydroxyandrost-4-en-6-one
3-deoxyandrogen-19-ulenized derivatives of 3-oxo-17-beta-carboxamidosteroids
4- (phenylthio) -4-androsten-3,17-dione
4- (tiopodstawiony) -4-androsten-3,17-dione
4-acetoxy-4-androstene-3,17-dione
4-aminoandrostendion
4-androstene-3,6,17-trion 4-hydroxyandrostendione (4-OHA)
4-methoxy-4-androstene-3,17-dione
4-oxidized androst-5-en-17-one and its 7-oxo derivatives 4-thi-substituted derivatives of 4-androstene-3,17-dione 4-thi-substituted derivatives of 4-androstene-3,17-dione
5-alpha-dihydronorethindrone (norethindrone metabolite)
5-alpha-reduced C19 steroids
5-alpha-androstan-17-one with a carbonyl function at C3 and / or C-6 or without 6-alpha-7-alpha-cyclopropane derivatives androst-4-ene
6-alpha-fluorotestosteron
6-beta-propynyl-substituted steroids 6,7-aziridinyl steroid and related compounds 6-alkyl analogues delta-1,4,6-androgens
6-alkyl- and 6-arylandrost-4-ene-3,17-dione
6-alkylandrost-4-en-3,17-dions 7 alpha and 7-beta-arylaliphatic substituted androst-4-en-3,17-dions
6-alkylandrosta-4,6-diene-3,17-dione and its 1,4,6-triene analogs 6-alkyl-substituted androgens
6-phenylaliphatic substituted C19-steroids with a 1,4-diene, 4,6-diene or 1,4,6-triene structure
6-bromoandrostendion
6-hydroxyiminoandrostenedione 6-methyleneandrosta-1,4-diene-3,17-dione (FCE 24304) 6-methyleneandrosta-1,4-diene-3,17-dione (FCE 24304)
6-phenylaliphatic substituted androst-4-ene-3,17-dions 6-substituted analogs androst-4-ene
7-alpha- (4'-amino) phenylthio-4-androstene-3,17-dione
7-alpha-substituted androsta-1,4-diene-3,17-dions
7-alpha-substituted androstenedione
7-alpha- (4'-amino) phenylthio-4-androstene-3,17-dione 7-alpha-arylaliphatic androsta-1,4-dien-3,17-diones 7-alpha-substituted androstenedions
7-substituted 4,6-androstadiene-3,17-dions
7-substituted steroids androst-4-en-3,6-dione derivatives androst-5-en-7,17-dione derivatives 19-nor- and 5-beta-6-beta-epoxy substituted on the A or B ring androst derivatives -4-en-3,6,17-trione steroids with an A-ring bridged bromoacetoxy-4-androstene-3-one delta-1,4,6-androgens delta-4,6-androgen epimeric 6-hydroperoxyandrostenedione ester-4 -en-3,17-dione (MDL 18 962), ester-4-en-3,6,17-trion flavonoids
RU48 [0016] Nonsteroidal aromatase inhibitors: 6 - [(4-chlorophenyl) (1H-1,2,4-triazol-1-yl) methyl] -1-methyl-1H-benzotriazole (vorazol), 2,2'- [5- (1H-1,2,4-triazol-1-ylmethyl) -1,3-phenylene] bis (2-methylproprionitrile) (arimidex),
4- [1- (cyanophenyl) -1- (1,2,4-triazolyl) methyl] benzonitrile (letrozole), {4- (5,6,7,8-tetrahydroimidazo [1,5a] pyridin-5- yl) benzonitrile (fadrozole) pyridoglutethimide (rogletimide) aminoglutethimide 1,2-imidazolylmethylcyclopentanol derivatives
1 - [(benzofuran-2-yl) phenylmethyl] triazoles and -tetrazoles
1- [benzofuran-2-yl) phenylmethyl] imidazoles (substituted)
1- (benzofuran-2-ylmethyl) imidazoles N, N-disubstituted 5aminopyrimidine derivatives
1-imidazolyl (alkyl) substituted di- and tetrahydroquinoline
1-pentyl-3- (4-aminophenyl) pyrrolidine-2,5-dione
1-phenyl-3-azabicyclo [3.1.0] hexane-2,4-dione
1-phenyl-3-azabicyclo [3.1.0] hexane-2,4-dione and 3- (4-aminophenyl) piperidine-2,6-dione 3-cycloalkyl-substituted 3- (4-aminophenyl) 3-alkylated analogs piperidine-2,6-dione derivatives of 3-ethyl-3- (4-pyridyl) piperidine-2,6- and 5-alkyl analogues of 3-ethyl-3- (4-pyridyl) piperidine-2,6-dione derivatives 4 amino-4H-1,2,4-triazole
4-cyclohexylaniline, aminoglutethimide, benzimidazole and imidazole compounds, delta-1,4-bisnorcholadiene, delta-1-testolactone, imidazole derivatives of pyrrolidone and piperidone imidazolyl-1,3,5-triazine MR 20492 and MR 20494 (two indinidinone derivatives) indans and tetralins derivative triazine SEF19 substituted pyridines testololactone [0017] Other aromatase inhibitors:
FR901537 8-bromo-cyclic adenosine monophosphate hexamethylmelamine derivative (SAE9) letrozole (CGS 20267) mefloquine
MPV-2213ad
Nn-octanoylornicotine and other nornicotine derivatives
Org 33201
R 76713 and R 76713 sesquiterpene lactone
SH 489
TAN-931 thyrotropin derivatives tobacalkaloid
YM511 [0018] For the names of these substances and their availability, see for example "Rote Liste", Cantor Publishing House, Aulendorf (DE), 2003.
[0019] Regarding the effectiveness of aromatase inhibition on the one hand and gentle treatment of skin areas for the beneficial local and topical application of the composition on the other hand, rapeseed extract (Brassica campestris, Rapeseed) is used. Suitable rapeseed extracts for use in accordance with the invention as an aromatase inhibitor component can be obtained in such a way that each fraction is obtained by extraction and, if necessary, the selective separation and isolation of these components from rapeseed and rapeseed oil that have aromatase inhibiting properties. Rapeseed extracts may additionally advantageously exhibit 5a-reductase inhibiting properties, which, as described below, is an even more favorable mode of action. Selective isolation of the extract fraction with aromatase and / or 5α-reductase inhibiting properties can be confirmed using appropriate fraction tests for appropriate inhibitory activity and can be collected in each case, any of the known specific inhibition tests can be used in any case. [0020] The combined action according to the invention is achieved by further using at least one plant extract that contains the active substance extracted from the plant, selected from the group consisting of type I and / or type II 5a-reductase inhibitors and androgen receptor blockers and wherein the at least one plant extract is a Saw Palm Extract (Serenoa Serrulata Fruit Extract). The use of a plant extract has significant advantages for the purposes of the invention compared to the use of single chemically synthesized 5α-reductase inhibitors and is preferred, e.g. because in this case steroid phytosterols and / or flavonoids are obtained as particularly preferred active substances according to the invention and / or because If appropriate, a complete mixture of structurally and functionally different active ingredients can usually be obtained. Thus, according to the invention, a plant extract is particularly preferred which contains many ingredients in the form of active substances extracted from the plant, i.e. it contains a mixture of active ingredients which are selected from the group consisting of type I and / or type II 5a-reductase inhibitors and receptor blockers androgen.
[0021] Plant extracts that exhibit type I and / or type II 5a-reductase inhibition, preferably both types I and type II, are in particular extracts from the following plants, alone or in combination, respectively: Sabal palm extract (Serenoa repens); Taxus chinensis (Pilg.) Rehd., Canarium pimela Koenig, Heteropanax fragrans (Roxb.) Seem., Andrographis paniculata (Burm.f.) Nees, Acer palmatum, Zosteraceae, Zostera sp., Yacon (a natural plant from Peru, belonging to the genus Asteraceae, botanical name: Polymnioa sonchifolia), sesame, gooseberry (genus Phyllanthus from the family Euphorbiaceace, botanical name: Phyllanthus Emblica), Striga asiatica (L.) O. Kuntze, Butea monosperma (Lam.) Taub., Alangium chinense (Lour.) Harms, Alternanthera sessilis (L.) R. Br., Procryis wightiana wall ex Wedd., Desmodium triflorum (L.) DC., Stephania japonica Miers. , Polypodium vulgare, Quercus plant (genus), Psidium guajava L, Plumbago zeylanicum L., Cyperus rotundus L., Ricinus communis L., Embelia ribes Burm. f., Jangkang, Daun trawas, Cuachalalat (comes from the Acapulco region in southern Mexico), Piper Methysticum (genus Piper, family Piperaceae), Impatiens balsamina L., Thuja orientalis (family of cypresses), plants of the genus Coriandrum such as Corlandrum sativum L., Cassia auriculata (in particular the bark), Quercus pedunculata (in particular the fruit), Rumex cyprius, Sumilax zeylanica, Phyllanthus nuriri, Woodfordia fruticosa, Lagerstroemia speciosa, Cymbopogon nardus, Glycyrrhiza glaamanda or Rheumens, (family Iridaceae), Rosa rugosa Thunb, Saxifraga stolonifera Meerburg, Garcinia mangostana L., Nephelium lappaceum L., Pyrola japonica Klenza, Trichosanthes cucumeroides Maxim, Kadsura japonica Dunal, Cuscuta australis R. Dr., Cuscuta japonica Choisy, Euchre. , Lilium makinoi Koidzumi, balbatimone, Rosaceae as peach, Rosa rugasa, Rosa odorata, Rosa odorata, R. coptophyllus, Rosa centifolia, sanguisorba officinalis L. or Pseudocydonia siensis, Lequminosae, Polygoni Multiflori Radix, Chaenomelis Fructus, Zanthoxylic Fructus, Thujae Orientalis, Landium domesticum Jack var. Duku (Duku) or Landium domesticum Jack var. Langsat (Langsat) from the family Meliaceae, Uncaria gambir, fennel, Polygala, licorice, Pharbitis, plantain, cloves, areca nuts, rosin, Stachys betonica, Geranium herb, Pounellae spical, Bupleurum elatum, Artenisiae capaeis frillaris Flos, semen, Nepetae herba, Dichroa, Valeriana officinalis. In the context of the present invention, the composition comprises at least one plant extract as indicated in claim 1, under (ii). [0022] Plant extracts that have the effect of blocking the androgen receptor (anti-androgen) are in particular the following extracts, respectively alone or in combination:
Chromolaena odoratum (L.) KR, coconut oil, Cuban royal palm (Roystonea regia), Pygeum africanum, Serenoa repens, Cucurbita pepo, Albizia lebbeck (L.) Benth (from bark), Roystonea regia (from fruit), Ruta graveolens L , Azadirachta indica A. Juss (from leaves), Momordica charantia (from seeds), Ganoderma lucidum, Echinacea purpurera, Belamcanda chinensis, Citrus aurantium, Echinacea purpurea, Silybum marianum (milk thistle), Crotalaria juncea Linn, Pygeum africanum, pumpkin seed oil especially flavonoid-rich ingredients; Trifoleum pratense] pine (Pinus), spruce (Picea), rye (flower pollen extract), soybean, Pygeum africanum, Hypoxis rooperi (root), nettle (Urtica dioica), Cordia multispicata (triterpenoid extract) from Brazil, Myricae Cortex ( Myrica rubra Sieb. et Zucc., Myricaceae, from bark), Pygeum africanum (Tadenan; African plum bark extract), Azadirachta indica, Sophora flavescens, Hibiscus rosa sinesis, Dalbergia cochinchinensis, Fructus Psoraleae, Striga orobanchioides and Vitex negundo.
[0023] Extracts of saber palm fruit (Serenoa Serrulata
Fruit Extract) (in particular ethanol extract), from pumpkin seeds, nettle, Taxus chinensis (Pilg.) Rehd., Canarium pimela Koenig, Heteropanax fragrans (Roxb.) Seem. and An8 drographis paniculata (Burm.f.) Nees because they inhibit 5α-reductase (type I and type
II), while also blocking androgen receptors.
The composition according to the invention comprises the combination according to claim 1.
[0024] In general, the extract can be obtained from the whole plant or a part thereof, e.g. from leaves, stems or branches, from bark, flowers, fruits, roots and the like. Preferably, prior to extraction, the plant source has been ground, crushed or pulverized. Further optional treatment steps are heating, refluxing, filtration, concentration, spray drying, freeze drying. Preferably, a selective isolation step is added in which the extracted sample is separated, e.g. by using appropriate chromatographic methods, and isolating the appropriate fractions with the desired effect and, if appropriate, subjecting it to further purification. Thus, for example, selective isolation can take place by determining and verifying the appropriate desired effect and / or by testing for a significant content of flavonoids and / or preferably phytosterols, in particular beta-sitosterol, stigmasterol and campesterol. The plant extract of component (ii) is particularly preferably an extract rich in phytosterols and / or flavonoids, i.e. the proportion of phytosterols and / or flavonoids relative to the total plant extract of component (ii) is e.g. at least 50% by weight, even more preferably at least 75% by weight, in particular at least 90% by weight
In order to isolate the basic beneficial components in the form of steroids from said plants, they are preferably extracted with organic solvents, for example methanol, ethanol, hexanol, glycol such as ethylene glycol or 1,3-butylene glycol, acetone, hexane, benzene, toluene, chloroform. Ethanol is a particularly preferred extraction agent.
[0026] According to the invention, it is particularly advantageous if component (i) or component (ii), and even better, when both components simultaneously inhibit (s) type I or type II 5a-reductase, and further preferably both isoforms , in order to ensure a multifunctional mechanism of action without the need for admixing further active substances and thus potentially producing adverse side effects. Thus, an optimized combination of active substances is obtained, in particular having a beneficial effect on positive hair growth in relation to scalp hair with the possibility of hair repigmentation with a further significant slowdown in hair growth in relation to body hair (as well as to the so-called " beard on the chin and above the upper lip in women ”) assuming that only the aromatase inhibitor, in the form of rapeseed extract, it is combined with the plant extract of component (ii) as defined in claim 1 as the active substance without adding further pharmacologically active substances but only suitable carriers, excipients or additives, depending on the formulation desired. This is particularly the case when an aromatase inhibitor is used which inhibits aromatase through a covalent bond with an aromatase, in particular using 4-hydroxyandrostenedione, 4-acetoxyandostendione or a 4-ester derivative thereof, the ester group may contain common alkyl groups such as an ester methyl, acetyl, n- or iso-propyl, n-, sec- or t-butyl.
[0027] It is assumed that when component (i) according to claim 1 is used in combination with the plant extract of ingredient (ii) according to claim 1, a multimodal mechanism of action is obtained, without the need for other potentially interfering active substances, namely, in addition to aromatase inhibition, simultaneous inhibition of 5α-reductase (type I and type II), and also blocking the androgen receptor.
[0028] The amounts of the above-mentioned active constituents, i.e. in each case an aromatase inhibitor, a palm tree extract and possibly an additional 5α-reductase inhibitor, are, for example, independently in each case in the range from 0.0001 to 50% by weight , preferably from 0.001 to 20% by weight, more preferably from 0.01 to 10% by weight, in particular 0.1 to 5% by weight, in each case based on the total weight of the composition.
[0029] In addition to the above-mentioned active ingredients, the composition of the invention may usually contain conventional carriers, excipients or additives. In particular, additives that are suitable for topical administration are contemplated. Suitable carriers or additives include, for example, vegetable oils such as almond oil, olive oil, peach kernel oil, peanut oil, castor oil and the like, plant extracts, essential oils, vitamin oils, fats and fat substances, lipids , phospholipids, hydrocarbons such as paraffin, petrolatum, lanolin, waxes etc., detergents, further skin active ingredients such as lecithin, wool fatty alcohols, carotene, etc., skin conditioners, fragrances, cosmetics, alcohols, water and water mixtures, glycerin, glycols, urea, talc, preservatives, sunscreen, dyes such as titanium white and zinc white, and antioxidants or the like, as well as mixtures listed substances, but not limited to them. Water generally serves as a base substance, so that, usually, the addition of emulsifying agents such as fatty alcohol sulfates, alkaline soaps, lecithins, triethanolamine and the like gives an O / W or W / O emulsion. Commercially available skin care products can also be used as a base mixture in addition to the active substances.
Suitable use forms for the compositions of the invention are, for example, an ointment, cream, gel, emulsion, lotion, aerosol, powder, oil or the like. Preferably, the composition according to the invention is, however, free of questionable, undesirable or even toxic additives, in particular free of metal components such as copper.
[0030] The invention will be explained in more detail by means of the following examples, which are not intended to be limiting. Data in% means weight% of the given composition.
Examples 1-8:
[0031] In Examples 1-8 below, the given ingredients (active ingredients or mixtures of active ingredients) for the preparation of alcohol solutions affecting hair growth were used in men and women, respectively.
Head hair growth in men:
Reference example 1 (outside the scope of the claims):
[0032] WATER 14.24%, DIMETHYL ISOSORBID 10%, FRUIT EXTRACT SERENOA SERRULATA (SERENOA SERRULATA FRUIT EXTRACT) 0.99%, 4HYDROKSY-ANDROSTENDION 0.6%, EXTRACT WITH URTICA DIOICA (EXTRACT) 1% TUSSILAGO FARFARA LEAVES (coltsfoot) 0.2%, RETINOL PALMITEATE 0.05%, TOKOFEROL 0.02%, PCA ZINC 0.2%, EXTRACT WITH EQUISETUM ARVENSE 0.2%, EXTRACT WITH MALVA SYLVESTRIS (SLIGHT) 0.4 %, DIODINE CYSTINLYDIBRUSTINATE 0.2%, OLAMINE PYROCONON 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, EXTRACT WITH HAMAMELIS VIRGINIANA (VIRGINIAN EYELID) 0.4%, EXTRACT FROM NON-FROZEN OLE EUROPEA OIL (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED RYCIN OIL , PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and others ALCOHOL DENATE. (70%).
Reference example 2 (outside the scope of the claims):
[0033] WATER 14.24%, DIMETHYL ISOSORBID 10%, FRUIT EXTRACT
SERENOA SERRULATA 0.99%, ACETOXYANDROSTENDION 0.6%, EXTRACT
WITH URTICA DIOICA 1%, TUSSILAGO FARFARA LEAF EXTRACT (COLOR) 0.2%, RETINOL PALMITATE 0.05%, TOKOFEROL 0.02%, PCA ZINC 0.2%, EQUISETUM ARVENSE EXTRACT 0.2% , EXTRACT FROM MALVA SYLVESTRIS (SLAVE) 0.4%, CYSTINYL DI DISTRIBUTITE 0.2%, OLAMINE PIROKTON 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMID 0.1%, EXTRACT WITH HAMAMELIS VIRGINIAN (OJSK WISH) 4%, EXTRACT FROM SMOOTHING OIL OLEA EUROPEA (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED CASTLE OIL PEG-40 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and other ALCOHOL DENATE. (70%).
Reference example 3 (outside the scope of the claims):
[0034] WATER 14.33%, DIMETHYL ISOSORBID 10%, FRUIT EXTRACT SERENOA SERRULATA 1%, STEROLE GLYCINE SOYA (SOYA) 0.5%, EXTRACT FROM URTICA DIOICA (NETTLE) 1%, EXTRACT FROM TARARA LARGE ) 0.2%, RETINOL PALMATE 0.05%, TOKOFEROL 0.02%, PCA ZINC 0.2%, EXTRACT FROM EQUISETUM ARVENSE 0.2%, EXTRACT FROM MALVA SYLVESTRIS 0.4%, CYSTINYL DI DISTISSURATE , 2%, OLAMINE PIROKTON 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMID 0.1%, EXTRACT WITH HAMAMELIS VIRGINIANA (VIRGINIAN EYELID) 0.4%, EXTRACT FROM NON-FROZEN OLE EUROPEA OIL (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED RYCIN OIL , PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and others ALCOHOL DENATE. (70%).
Example 4:
[0035] WATER 14.33%, DIMETHYL ISOSORBID 10%, FRUIT EXTRACT SERENOA SERRULATA 1%, STEROLE BRASSICA CAMPESTRIS (RAPE SEEDS) 0.5%, EXTRACT WITH URTICA DIOICA (CARBON) 1%, EXTRACT FARSLAR COLUMN) 0.2%, RETINOL PALMATE 0.05%, TOKOFEROL 0.02%, PCA ZINC 0.2%, EXTRACT FROM EQUISETUM ARVENSE 0.2%, EXTRACT FROM MALVA SYLVESTRIS 0.4%, CYSTINYL DI DISTRIBUTION 0.2%, OLAMINE PIROKTON 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMID 0.1%, EXTRACT WITH HAMAMELIS VIRGINIANA (VIRGINIAN EYELID) 0.4%, EXTRACT FROM NON-FROZEN OLE EUROPEA OIL (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED RYCIN OIL , PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and others ALCOHOL DENATE. (70%).
Head hair growth in women:
Reference example 5 (outside the scope of the claims):
[0036] WATER 14.33%, DIMETHYL ISOSORBID 10%, 4-HYDROXYANDROSTENDION 0.7%, FRUIT EXTRACT SERENOA SERRULATA 0.8%, EXTRACT FROM URTICA DIOICA (CARE) 1%, EXTRACT FROM TARBARA LEAF 0.2%, RETINOL PALMATE 0.05%, TOKOFEROL 0.02%, ZINC PCA 0.2%, EXTRACT FROM EQUISETUM ARVENSE 0.2%, EXTRACT FROM MALVA SYLVESTRIS 0.4%, CYSTINYL DI DISTISSURATE 2%, OLAMINE PIROKTON 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMID 0.1%, EXTRACT WITH HAMAMELIS VIRGINIANA (VIRGINIAN EYELID) 0.4%, EXTRACT FROM NON-FROZEN OLE EUROPEA OIL (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED RYCIN OIL , PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05, and others ALCOHOL DENATE. (70%).
Reference example 6 (outside the scope of the claims):
[0037] WATER 14.33%, DIMETHYL ISOSORBID 19%, ACETOXYANDROSTENDION 07%, FRUIT EXTRACT SERENOA SERRULATA 0.8%, EXTRACT FROM URTICA DIOICA (CEREAL) 1%, EXTRACT FROM LEAF TUSSARAGA FARSARA , RETINOL PALMATE 0.05%, TOKOFEROL 0.02%, ZINC PCA 0.2%, EXTRACT FROM EQUISETUM ARVENSE 0.2%, EXTRACT FROM MALVA SYLVESTRIS (SLAVE) 0.4%, DIODE CYSTINYL DI DISTRIBUTATE 0.2%, PYROCONE 0.2% OLAMINS, 0.2% TRIDECYL SALICYLATE, 0.1% NIACINAMIDE, EXTRACT WITH HAMAMELIS VIRGINIANA (VIRGINIAN EYELID) 0.4%, EXTRACT FROM NON-FROZEN OLE EUROPEA OIL (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED RYCIN OIL , PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and others ALCOHOL DENATE. (70%).
Reference example 7 (outside the scope of the claims):
[0038] WATER 14.23%, DIMETHYL ISOSORBID 10%, STYER GLYCINE SOYA 1%, EXTRACT FROM SERENOA FRUIT 0.6%, EXTRACT FROM URTICA DIOICA (NETTLE) 1%, EXTRACT FROM TARARIL LEAF ) 0.2%, RETINOL PALMATE 0.05%, TOKOFEROL 0.02%, PCA ZINC 0.2%, EXTRACT FROM EQUISETUM ARVENSE 0.2%, EXTRACT FROM MALVA SYLVESTRIS 0.4%, CYSTINYL DI DISTISSURATE , 2%, OLAMINE PIROKTON 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMID 0.1%, EXTRACT WITH HAMAMELIS VIRGINIANA (VIRGINIAN EYELID) 0.4%, EXTRACT FROM NON-FROZEN OLE EUROPEA OIL (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED RYCIN OIL , PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and others ALCOHOL DENATE. (70%).
Example 8:
[0039] WATER 14.23%, DIMETHYL ISOSORBID 10%, STEROLE BRASSICA CAMPESTRIS (RAPE SEEDS) 1%, FRUIT EXTRACT SERENOA SERRULATA 0.6%, EXTRACT WITH URTICA DIOICA (NETTLE FLAX), 1%, EXTRA FACE COLUMN) 0.2%, RETINOL PALMATE 0.05%, TOKOFEROL 0.02%, PCA ZINC 0.2%, EXTRACT FROM EQUISETUM ARVENSE 0.2%, EXTRACT FROM MALVA SYLVESTRIS 0.4%, CYSTINYL DI DISTRIBUTION 0.2%, OLAMINE PIROKTON 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMID 0.1%, EXTRACT WITH HAMAMELIS VIRGINIANA (VIRGINIAN EYELID) 0.4%, EXTRACT FROM NON-FROZEN OLE EUROPEA OIL (OLIVE) 0.4%, BIOTIN 0.2%, UREA 0.25%, HYDRATED RYCIN OIL , PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and others ALCOHOL DENATE. (70%).
Examples 9-14:
[0040] In examples 9-14 below, these ingredients were used to make creams that affect new hair growth and hair removal (face and body).
Body hair removal:
Example 9:
[0041] 6% DIMETHYL ISOSORBID, FREE PERSEA OIL (AVOCADO)
4%, octyldodecanol 3.9%, TRIDECYL SALICYLATE 2%, C12C13-ALKYL MELATE 2%, CETHYLSTEARYL ISONONATE 2%, TRIGLYCERIDE
CAPRYLIC-CAPRYIN 1.9476%, POLYGLYCERINE DISTERATE-3 I
METHYLGLUCOSE 1.9%, COPOLYMER AMMON ACRYLYLDIMETHYLURURINATE 0.85%, SERENOA FRUIT EXTRACT
SERRULATA 0.9%, STEROLE BRASSICA CAMPESTRIS (RAPE SEEDS) 0.5%, STEROLE GLYCINE SOYA (Soya) 0.5%, TOKOFEROL ACETATE 0.9%, TOKOFEROL 0.0175%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERINE 0.9552%, KSYLITOL 0.9%, SORBITOL, 0.9%, PALMATIN 0.0024%,
COCONUT OIL POLYGLUCOSID (COCO-GLUCOSIDE) 0.052%, ETHYLOXYLOGLYCERINE 0.3%, LACTIC ACID 0.12%, SORBITANIUM LAURINATE 0.09%, POLOXAMER 407 0.5%, NYLON-12 0.06%, LECY 0.06% , ASCORBYL PALMATE 0.0175%, AMMONIA 0.0175, PHENOXYETHANOL 0.8%, Xanthan gum 0.1%, and the remainder WATER (66.7423%).
Reference example 10 (outside the scope of the claims):
[0042] DIMETHYL ISOSORBID 6%, PERSEA GRATISSIMA OIL (AVOCADO) 4%, OTHYLODODECANOL 3.9%, TRIDECYL SALICYLATE 2%, C12C13-ALKYL 2% MELATE, CETHYLEXAPLYCRYLYLETRYLYRYLATE POLYGLYCERINE DISTYRATE-3 AND METHYLGYLUCOSE 1.9%, COPYLIMER AMMON ACRYLYLDIMETHYLURURINATE 0.85%, FRUIT EXTRACT SERENOA SERRULATE 0.9%, ACETOXYANDROSTENDOL0.0%, OCTOCOL 0.09% CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERINE 0.9552%, KSYLITOL 0.9%, SORBITOL 0.9%, PALMATIN 0.024%, POLYLUCLUCOSIDE OF COCONUT OIL ACIDS 0.052%, ETHYLEXEXYLOGLYCERINE 0.3%, LACTIC ACID 0.12%, LAURINATE SORBITE 407 0.5%, NYLON-12 0.06%, LECITHIN 0.028%, ASCORBYL PALMITATE 0.0175%, AMMONIA 0.0175%, PHENOXYETHANOL 0.8%, XANTHANGUM 0.1%, and WATER (67.2423) %).
Reference example 11 (outside the scope of the claims):
[0043] DIMETHYL ISOSORBID 6%, PERSEA GRATISSIMA OIL (AVOCADO) 4%, OTHYLODODECANOL 3.9%, TRIDECYL SALICYLATE 2%, C12C13-ALKYL MELATE 2%, CETHYLEXAPLYCRYLYLETRYLYRYLATE POLYGLYCERINE-3 DISTARATE AND METHYLGYLUCOSE 1.9%, COPYLIMER AMMON ACRYLYLDIMETHYLURURINATE 0.85%, FRUIT EXTRACT SERENOA SERRULATE 0.9%, 4-HYDROXYANDROSTENDOL 0.75%, %, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERINE 0.9552, XYLITOL 0.9%, SORBITOL 0.9%, PALMATIN 0.024%, POLYLUCLUCOSIDE OF COCONUT OIL ACIDS 0.052%, ETHYLOHEXYLGLYCERINE 0.3%, LACTIC ACID 0.12%, LAURINATE SORBANATE 40% 0.5%, NYLON-12 0.06%, LECITHIN 0.028%, ASCORBYL PALMITATE 0.0175%, AMMONIA 0.0175, PHENOXYETHANOL 0.8%, XANTAN RUBBER 0.1%, and WATER residue (67.2423% ).
Facial hair removal:
Example 12:
[0044] 6% DIMETHYL ISOSORBID, FREE PERSEA OIL (AVOCADO)
4.5%, octyldodecanol 4.4%, TRIDECYL SALICYLATE 2%, C12C13-ALKYL MELATE 2%, CETHYLSTEARYL ISONATE 2%, TRIGLYCERIDE
CAPRYLIC-CAPRYIN 1.9476%, POLYGLYCERINE DISTERATE-3 I
METHYLGLUCOSE 1.9%, STEROLE BRASSICA CAMPESTRIS (SEEDS
RAPE) 0.5%, GLYCINE SOY STEROLES (SOYA) 0.48%, EXTRACT WITH
FRUIT SERENOA SERRULATA 0.9%, CAPRYLOYL GLYCINE 0.1%,
TRIBEHENIN 0.9%, GLYCERINE 0.9552%, KSYLITOL 0.9%, SORBITOL 0.9%,
Copolymer of ammonium acryloyl dimethylurinate and vinylpyrrolidone 1.25%, palmatine 0.024%, polyglucoside of coconut oil acids 0.052%, TOKOFEROL ACETATE 0.9%, TOKOFEROL 0.0175%,
ETHYLHYXYLGLYCERINE 0.3%, LACTIC ACID 0.12%, SORBITANATE LAURINATE 0.09%, POLOXAMER 407 0.5%, NYLON-12 0.06%, LECITHINE 0.028%, ASCORBYL PALMATE 0.0175%, AMMONIA 0.0175 %, PHENOXYETHANOL 0.8%, XANTAN RUBBER 0.1%, and residual WATER (65.3407%).
Reference example 13 (outside the scope of the claims):
[0045] DIMETHYL ISOSORBID 6%, PERSEA GRATISSIMA OIL (AVOCADO) 4.5%, OCTYLDODECANOL 4.4%, TRIDECYL SALICYLATE 2%, C12C13-ALKYL 2% MELATE, CETHYLEXAPLYCRYLYRYLATE %, POLYGLYCERINE-3 DISTEINATE AND METHYLGYLUCOSE 1.9%, ACETOXYANDROSTENDION 0.68, FRUIT EXTRACT SERENOA SERRULATA 0.9%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERINE 0.9552%, XYLITOL 9%, SORBITOL 0.9%, COPPER POLYMER, AMYL ACRYLYLDIMETHYLURURINATE 1.25%, PALMATIN 0.024%, POLYGLUCOSIDE ACID OF COCONUT OIL 0.52%, TOKOFEROL ACETATE 0.9%, TOKOFEROL 0.0175%, ETHYLOHEXYLOGLYCERINE 0.3%, LACTIC ACID 0.12%, SORBITANIUM LAURINATE, 0.09%, 0% 0% 5%, NYLON-12 0.06%, LECITHIN 0.028%, ASCORBYL PALMITATE 0.0175%, AMMONIA 0.0175%, PHENOXYETHANOL 0.8%, Xanthan gum 0.1%, and WATER residue (65.6407%) .
Reference example 14 (outside the scope of the claims):
[0046] DIMETHYL ISOSORBID 6%, PERSEA GRATISSIMA OIL (AVOCADO) 4.5%, OCTYLDODECANOL 4.4%, TRIDECYL SALICYLATE 2%, C12C13-ALKYL 2% MELATE, CETHYLEXAPLYCRYLYRYLATE %, POLYGLYCERINE-3 DISTYLATE AND METHYLGYLUCOSE 1.9%, 4-HYDROXY-ANDROSTENDION 0.68%, FRUIT EXTRACT SERENOA SERRULATA 0.9%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERINE 0.9552 %, KSYLITOL 0.9%, SORBITOL 0.9%, Copolymer of ammonium acryloyl dimethylurinate and vinylpyrrolidone 1.25%, palmatine 0.024%, polyglucoside of coconut oil acids 0.052%, toocferol acetate 0.9%, toocferol 0.0175%, ethylcellyloxy , 09%, POLOXAMER 407 0.5%, NYLON-12 0.06%, LECITHIN 0.028%, ASCORBYL PALMITATE 0.0175%, AMMONIA 0.0175%, PHENOXYETHANOL 0.8%, Xanthan gum 0.1%, and WATER residue (65.6407%).
[0047] The following examples of use 1 and 2 show the results obtained using selected representative compositions of production examples (1-14), in cases of problems related to hair growth or excessive body and facial hair.
Application examples 1 and 2:
Application example 1: Effect on scalp in men and women with genetic alopecia:
[0048] In 10 women aged 40 to 60 years and 12 men aged 34 to 64 years, with severe genetic alopecia, lotion preparations with the following combinations of active ingredients were used:
In women: a lotion having composition according to reference example 6 (n = 4) or according to reference example 5 (n = 6)
For men: a lotion having a composition according to reference example 2 (n = 12).
Results:
[0049] Already after 3 months, all men and women had a positive effect on both hair growth (hair quantity) and hair thickness increase. In addition to a particularly significant increase in hair growth (hair quantity), a significant increase in hair thickness was found after 6 months. Surprisingly, almost all women (n = 9) and almost all men (n = 10) exhibited hair repigmentation and therefore a return to their original hair color.
Application example 2: excessive leg hair (n = 35) and so-called facial hair on the chin and above the upper lip in women (n = 6):
Application for leg hair in women:
[0050] For 6 months, women with severe leg hair (n = 35) were administered a cream having the composition according to reference example 10 (N = 15) or reference example 11 (n = 20).
Results:
[0051] The study covered 180 days, with a 30-day interval between study time points. The results were surprising. Already after 30 days a reduction in the amount and thickness of hair was found. After 180 days, the amount of hair in the area under study decreased by 89%, while about 70% of the remaining hair had a complete depigmentation, and more than 95% of the women had a substantial reduction in the thickness of the remaining hair, so they became very thin. The results were the same for both cream formulations, so both showed the same biological efficacy.
[0052] The same results were found in 6 women with so-called facial hair on the chin and above the upper lip when using a cream having the composition according to reference example 13: It is believed that selected combinations of active substances lead to a reduction in the production of both local estradiol and local dihydrotestosterone, and in addition to blocking the possible action of dihydrotestosterone in the circulation of hair bulbs, by blocking androgen receptors, for example based on the action of sabal palm extract.
25 members in 12 offices
Priority claims2
| Document | Office | Kind | Date |
|---|---|---|---|
| 102008012988 | Germany | A | |
| 2009001644 | European Patent Office (EPO) | W |
Members25
| Document | Office | Kind | |
|---|---|---|---|
| DE102008012988A1 | Germany | A1 | |
| CA2717806A1 | Canada | A1 | |
| WO2009109402A2 | World Intellectual Property Organization (WIPO) | A2 | |
| WO2009109402A3 | World Intellectual Property Organization (WIPO) | A3 | |
| EP2262471A2 | European Patent Office (EPO) | A2 | |
| WO2009109402A8 | World Intellectual Property Organization (WIPO) | A8 | |
| CN101969921A | China | A | |
| JP2011514345A | Japan | A | |
| US2011117218A1 | United States of America | A1 | |
| RU2010140915A | Russian Federation | A | |
| US2013142890A1 | United States of America | A1 | |
| RU2491914C2 | Russian Federation | C2 | |
| JP5658570B2 | Japan | B2 | |
| JP2015028044A | Japan | A | |
| BRPI0908792A2 | Brazil | A2 | |
| EP2262471B1 | European Patent Office (EPO) | B1 | |
| ES2558806T3 | Spain | T3 | |
| PL2262471T3This record | Poland | T3 | |
| HUE026198T2 | Hungary | T2 | |
| CA2717806C | Canada | C | |
| BRPI0908792B1 | Brazil | B1 | |
| US11052059B2 | United States of America | B2 | |
| US2021290579A1 | United States of America | A1 | |
| US11324711B2 | United States of America | B2 | |
| US11974977B2 | United States of America | B2 |
Numbers
- Application
- 9716740
Titles2
- English
- COMPOSITION AND USES FOR INFLUENCING HAIR GROWTH
- Polish
- KOMPOZYCJA I ZASTOSOWANIA DO WPŁYWANIA NA WZROST WŁOSÓW
Classification
- CPC, 23
- A61K8/63
- A61K31/215
- A61K8/97
- A61Q5/08
- A61Q7/00
- A61Q7/02
- A61K2800/782
- A61K36/185
- A61K31/5685
- A61K36/13
- A61K36/19
- A61K36/25
- A61K36/31
- A61K36/32
- A61K36/42
- A61K36/48
- A61K36/889
- A61K45/06
- A61K31/56
- A61K8/9755
- A61K8/9789
- A61K8/9794
- A61P17/14
- IPC, 19
- A61K36 889
- A61K8 63
- A61K8 97
- A61K31 215
- A61K31 56
- A61K31 5685
- A61K36 13
- A61K36 185
- A61K36 19
- A61K36 25
- A61K36 31
- A61K36 32
- A61K36 42
- A61K36 48
- A61K45 06
- A61P17 14
- A61Q5 08
- A61Q7 00
- A61Q7 02