Composition and uses for influencing hair growth

Abstract

The invention describes a combination of at least one aromatase inhibitor selected from the group of chemical-synthetic aromatase inhibitors and aromatase inhibition exhibiting extracts of soya beans and rapeseed, respectively, and at least one plant extract that contains one or more active ingredient substance(s) extracted from the plant, which is(are) selected from the group of 5α reductase type I and/or type II inhibitors and androgen receptor blockers, said combination being contained for example in a composition and having special properties for influencing hair growth. Uses of this combination are also described.

Claims

1. A method for treatment of alopecia in a person in need thereof, the method consisting essentially of topically applying to said person an effective amount of a composition consisting essentially of: (i) at least one aromatase inhibitor, selected from the group consisting of a.) a chemical-synthetic aromatase inhibitor which inhibits aromatase by covalent binding of the aromatase, wherein the chemical-synthetic aromatase inhibitor is selected from the group consisting of 4-acetoxy-androstenedione and 4-hydroxy-androstenedione or a 4-carboxylic acid ester derivative thereof, and b.) an aromatase inhibiting extract of rapeseed; (ii) at least one plant extract wherein the plant extract consists essentially of a mixture of 5α reductase type I inhibitors, 5α reductase type II inhibitors, androgen receptor blockers, phytosterols and flavonoids, wherein the plant extract is at least 90% by weight phytosterols and/or flavonoids based on the total plant extract, and wherein the at least one plant extract is an extract selected from the group consisting of saw palmetto (Serenoa serrulata fruit extract) and stinging nettle, and (iii) suitable carriers and/or excipients and/or additives, wherein said composition is formulated as a cream, a gel, an ointment or an emulsion.

2. The method according to claim 1, wherein the at least one aromatase inhibitor inhibits 5α reductase.

3. The method according to claim 1, wherein (i) is a combination of a.) a chemical synthetic aromatase inhibitor; and b.) an aromatase inhibiting extract of rapeseed.

4. The method according to claim 1, wherein the saw palmetto extract is an ethanol extract of saw palmetto fruits.

5. The method according to claim 1, wherein the chemical-synthetic aromatase inhibitor is 4-acetoxy-androstenedione.

Description

EXAMPLES 1-8

(1) In the following Examples 1-8, the given ingredients (active ingredients and mixtures of active ingredients, respectively) for preparation of tinctures for influencing the hair growth were respectively applied to men and women.

(2) Hair Growth Head Men:

EXAMPLE 1

(3) AQUA 14.24%, DIMETHYL ISOSORBIDE 10%, SERENOA SERRULATA FRUIT EXTRACT 0.99%, 4-HYDROXY-ANDROSTENEDIONE 0.6%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE) OIL UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%,

(4) and rest ALCOHOL DENAT. (70%).

EXAMPLE 2

(5) AQUA 14.24%, DIMETHYL ISOSORBIDE 10%, SERENOA SERRULATA FRUIT EXTRACT 0.99%, ACETOXYANDROSTENEDIONE 0.6%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE) OIL UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and rest ALCOHOL DENAT. (70%).

EXAMPLE 3

(6) AQUA 14.33%, DIMETHYL ISOSORBIDE 10%, SERENOA SERRULATA FRUIT EXTRACT 1%, GLYCINE SOYA (SOYBEAN) STEROLS 0.5%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE) OIL UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and rest ALCOHOL DENAT. (70%).

EXAMPLE 4

(7) AQUA 14.33%, DIMETHYL ISOSORBIDE 10%, SERENOA SERRULATA FRUIT EXTRACT 1%, BRASSICA CAMPESTRIS (RAPESEED) STEROLS 0.5%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA

(8) (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE) OIL UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and rest ALCOHOL DENAT. (70%).

(9) Hair Growth Head Women:

EXAMPLE 5

(10) AQUA 14.33%, DIMETHYL ISOSORBIDE 10%, 4-HYDROXY-ANDROSTENEDIONE 0.7%, SERENOA SERRULATA FRUIT EXTRACT 0.8%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE) OIL

(11) UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05, and rest ALCOHOL DENAT. (70%).

EXAMPLE 6

(12) AQUA 14.33%, DIMETHYL ISOSORBIDE 19%, ACETOXYANDROSTENEDIONE 0.7%, SERENOA SERRULATA FRUIT EXTRACT 0.8%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE) OIL UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and rest ALCOHOL DENAT. (70%).

EXAMPLE 7

(13) AQUA 14.23%, DIMETHYL ISOSORBIDE 10%, GLYCINE SOYA (SOYBEAN) STEROLS 1%, SERENOA SERRULATA FRUIT EXTRACT 0.6%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE) OIL UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%,

(14) and rest ALCOHOL DENAT. (70%).

EXAMPLE 8

(15) AQUA 14.23%, DIMETHYL ISOSORBIDE 10%, BRASSICA CAMPESTRIS (RAPESEED) STEROLS 1%, SERENOA SERRULATA FRUIT EXTRACT 0.6%, URTICA DIOICA (NETTLE) EXTRACT 1%, TUSSILAGO FARFARA (COLTSFOOT) LEAF EXTRACT 0.2%, RETINYL PALMITATE 0.05%, TOCOPHEROL 0.02%, ZINC PCA 0.2%, EQUISETUM ARVENSE EXTRACT 0.2%, MALVA SYLVESTRIS (MALLOW) EXTRACT 0.4%, DISODIUM CYSTINYL DISUCCINATE 0.2%, PIROCTONE OLAMINE 0.2%, TRIDECYL SALICYLATE 0.2%, NIACINAMIDE 0.1%, HAMAMELIS VIRGINIANA (WITCH HAZEL) EXTRACT 0.4%, OLEA EUROPAEA (OLIVE)

(16) OIL UNSAPONIFIABLES 0.4%, BIOTIN 0.2%, UREA 0.25%, PEG-40 HYDROGENATED CASTOR OIL 0.05%, PROPYLENE GLYCOL 0.05%, LACTIC ACID 0.05%, and rest ALCOHOL DENAT. (70%).

EXAMPLES 9-14

(17) In the following Examples 9-14, said ingredients for preparation of creams for influencing the re-growth of hair and the removal of hair (face and body) were used.

(18) Hair Removal Body:

EXAMPLE 9

(19) DIMETHYL ISOSORBIDE 6%, PERSEA GRATISSIMA (AVOCADO) OIL 4%, OCTYLDODECANOL 3.9%, TRIDECYL SALICYLATE 2%, C12-13 ALKYL LACTATE 2%, CETEARYL ISONONANOATE 2%, CAPRYLIC/CAPRIC TRIGLYCERIDE 1.9476%, POLYGLYCERYL-3 METHYLGLUCOSE DISTEARATE 1.9%, AMMONIUM ACRYLOYLDIMETHYLTAURATE/VP CO POLYMER 0.85%, SERENOA SERRULATA FRUIT EXTRACT 0.9%, BRASSICA CAMPESTRIS (RAPESEED) STEROLS 0.5%, GLYCINE SOYA (SOYBEAN) STEROLS 0.5%, TOCOPHERYL ACETATE 0.9%, TOCOPHEROL 0.0175%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERIN 0.9552%, XYLITOL 0.9%, SORBITOL 0.9%, PALMATINE 0.0024%, COCO-GLUCOSIDE 0.052%, ETHYLHEXYLGLYCERIN 0.3%, LACTIC ACID 0.12%, SORBITAN LAURATE 0.09%, 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 rest AQUA

(20) (66.7423%).

EXAMPLE 10

(21) DIMETHYL ISOSORBIDE 6%, PERSEA GRATISSIMA (AVOCADO) OIL 4%, OCTYLDODECANOL 3.9%, TRIDECYL SALICYLATE 2%, C12-13 ALKYL LACTATE 2%, CETEARYL ISONONANOATE 2%, CAPRYLIC/CAPRIC TRIGLYCERIDE 1.9476%, POLYGLYCERYL-3 METHYLGLUCOSE DISTEARATE 1.9%, AMMONIUM ACRYLOYLDIMETHYLTAURATE/VP COPOLYMER 0.85%, SERENOA SERRULATA FRUIT EXTRACT 0.9%, ACETOXYANDROSTENEDIONE 0.5%, TOCOPHERYL ACETATE 0.9%, TOCOPHEROL 0.0175%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERIN 0.9552%, XYLITOL 0.9%, SORBITOL 0.9%, PALMATINE 0.024%, COCO-GLUCOSIDE 0.052%, ETHYLHEXYLGLYCERIN 0.3%, LACTIC ACID 0.12%, SORBITAN LAURATE 0.09%, POLOXAMER 407 0.5%, NYLON-12 0.06%, LECITHIN 0.028%, ASCORBYL PALMITATE 0.0175%, AMMONIA 0.0175%, PHENOXYETHANOL 0.8%, XANTHANGUM 0.1%, and rest AQUA (67.2423%).

EXAMPLE 11

(22) DIMETHYL ISOSORBIDE 6%, PERSEA GRATISSIMA (AVOCADO) OIL 4%, OCTYLDODECANOL 3.9%, TRIDECYL SALICYLATE 2%, C12-13 ALKYL LACTATE 2%, CETEARYL ISONONANOATE 2%, CAPRYLIC/CAPRIC TRIGLYCERIDE 1.9476%, POLYGLYCERYL-3 METHYLGLUCOSE DISTEARATE 1.9%, AMMONIUM ACRYLOYLDIMETHYLTAURATE/VP COPOLYMER 0.85%, SERENOA SERRULATA FRUIT EXTRACT 0.9%, 4-HYDROXY-ANDROSTENEDIONE 0.5%, TOCOPHERYL ACETATE 0.9%, TOCOPHEROL 0.0175%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERIN 0.9552, XYLITOL 0.9%, SORBITOL 0.9%, PALMATINE 0.024%, COCO-GLUCOSIDE 0.052%, ETHYLHEXYLGLYCERIN 0.3%, LACTIC ACID 0.12%, SORBITAN LAURATE 0.09%, 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 rest AQUA (67.2423%).

(23) Hair Removal Face:

EXAMPLE 12

(24) DIMETHYL ISOSORBIDE 6%, PERSEA GRATISSIMA (AVOCADO) OIL 4.5%, OCTYLDODECANOL 4.4%, TRIDECYL SALICYLATE 2%, C12-13 ALKYL LACTATE 2%, CETEARYL ISONONANOATE 2%, CAPRYLIC/CAPRIC TRIGLYCERIDE 1.9476%, POLYGLYCERYL-3 METHYLGLUCOSE DISTEARATE 1.9%, BRASSICA CAMPESTRIS (RAPESEED) STEROLS 0.5%, GLYCINE SOYA (SOYBEAN) STEROLS 0.48%, SERENOA SERRULATA FRUIT EXTRACT 0.9%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERIN 0.9552%, XYLITOL 0.9%, SORBITOL 0.9%, AMMONIUM ACRYLOYLDIMETHYLTAURATE/VP COPOLYMER 1.25%, PALMATINE 0.024%, COCO-GLUCOSIDE 0.052%, TOCOPHERYL ACETATE 0.9%, TOCOPHEROL 0.0175%, ETHYLHEXYLGLYCERIN 0.3%, LACTIC ACID 0.12%, SORBITAN LAURATE 0.09%, 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 rest AQUA

(25) (65.3407%).

EXAMPLE 13

(26) DIMETHYL ISOSORBIDE 6%, PERSEA GRATISSIMA (AVOCADO) OIL 4.5%, OCTYLDODECANOL 4.4%, TRIDECYL SALICYLATE 2%, C12-13 ALKYL LACTATE 2%, CETEARYL ISONONANOATE 2%, CAPRYLIC/CAPRIC TRIGLYCERIDE 1.9476%, POLYGLYCERYL-3 METHYLGLUCOSE DISTEARATE 1.9%, ACETOXYANDROSTENEDIONE 0.68, SERENOA SERRULATA FRUIT EXTRACT 0.9%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERIN 0.9552%, XYLITOL 0.9%, SORBITOL 0.9%, AMMONIUM ACRYLOYLDIMETHYLTAURATE/VP CO POLYMER 1.25%, PALMATINE 0.024%, COCO-GLUCOSIDE 0.52%, TOCOPHERYL ACETATE 0.9%, TOCOPHEROL 0.0175%, ETHYLHEXYLGLYCERIN 0.3%, LACTIC ACID 0.12%, SORBITAN LAURATE 0.09%, 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 rest AQUA (65.6407%).

EXAMPLE 14

(27) DIMETHYL ISOSORBIDE 6%, PERSEA GRATISSIMA (AVOCADO) OIL 4.5%, OCTYLDODECANOL 4.4%, TRIDECYL SALICYLATE 2%, C12-13 ALKYL LACTATE 2%, CETEARYL ISONONANOATE 2%, CAPRYLIC/CAPRIC TRIGLYCERIDE 1.9476%, POLYGLYCERYL-3 METHYLGLUCOSE DISTEARATE 1.9%, 4-HYDROXY-ANDROSTENEDIONE 0.68%, SERENOA SERRULATA FRUIT EXTRACT 0.9%, CAPRYLOYL GLYCINE 0.1%, TRIBEHENIN 0.9%, GLYCERIN 0.9552%, XYLITOL 0.9%, SORBITOL 0.9%, AMMONIUM ACRYLOYLDIMETHYLTAURATE/VP CO POLYMER 1.25%, PALMATINE 0.024%, COCO-GLUCOSIDE 0.052%, TOCOPHERYL ACETATE 0.9%, TOCOPHEROL 0.0175%, ETHYLHEXYLGLYCERIN 0.3%, LACTIC ACID 0.12%, SORBITAN LAURATE 0.09%, 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 rest AQUA (65.6407%).

(28) The following application Examples 1 and 2 illustrate the results obtained with representatively selected compositions of preparation Examples (1-14) in cases with problems of hair growth and with excess hairiness on body and face, respectively.

Application Examples 1 and 2

Application Example 1

Influence on the Head Hair in Women and Men With Genetic Alopecia

(29) In 10 women aged between 40 and 60 years and in 12 men aged between 34 and 64 with severe genetic alopecia lotion preparations with the following combinations of active ingredients were applied:

(30) In women: A lotion having the composition according to Example 6 (n=4) and according to Example 5 (n=6), respectively.

(31) In men: A lotion having the composition according to Example 2 (n=12).

(32) Results:

(33) Already after 3 months, all men and women exhibited both a positive influence on the hair growth (amount of hair) and an increase in the thickness of the hair. In addition to an extremely remarkable increase in hair growth (amount of hair), after 6 months a considerable increase in the thickness of the hair appeared. Surprisingly, nearly all women (n=9) and nearly all men (n=10) exhibited a re-pigmentation of the hair and, therefore, a return to the original hair color.

Application Example 2

Excessive Hair Growth on the Legs (n=35) and So-Called “Facial Hair on the Chin and Upper Lip of Women” (in German: “Damenbart”) (n=6) in Women

(34) Application to the Hair Growth on the Legs in Women:

(35) For 6 months, women exhibiting a strong hair growth on the legs (n=35) have been given a cream having the composition according to Example 10 (N=15) or Example 11 (n=20).

(36) Results:

(37) The examination covered 180 days with examination time points in 30-day intervals. The results were surprising. A reduction of the amount and thickness of hair could be detected already after 30 days. After 180 days, the amount of hair per examination area was reduced by 89%, whereas in nearly 70% of the remaining hair a complete depigmentation occurred, and in more than 95% of the women the remaining hair substantially decreased in thickness, thus becoming very fine. The results were identical for both cream preparations, thereby both showing the same biological effectiveness.

(38) Same effects could be detected in 6 women having so-called “facial hair on the chin and upper lip of women” by the application of a cream having the composition according to Example 13:

(39) It is postulated that the selected combination of active substances results in a suppression of both the local estradiol and the local dihydrotestosterone generation, and, moreover, the possible effect of the circulating dihydrotestosterone in the hair papilla is blocked via blocking of the androgen receptors, for example based on the effects of the saw palmetto extract.