Oral formulation containing dimethylglycine to improve the condition of hair and scalp.

Description

[0001] The present invention relates to an oral composition containing dimethylglycine and / or a salt of dimethylglycine and amylopectin. Furthermore, the present invention relates to the (cosmetic and / or medicinal) use of this composition for improving the condition of the hair and / or scalp, for promoting the metabolism of the hair and / or scalp, for promoting hair growth, and / or for treating and / or preventing hair loss. The present invention also relates to a dietary supplement for promoting the metabolism of the hair and / or scalp, for promoting hair growth, and / or for treating and / or preventing hair loss.

[0002] Human hair has largely lost its function as a protective barrier for the body. However, healthy hair holds great cultural significance for both women and men worldwide and is often seen as a sign of prosperity and health. Consequently, thinning hair, for example due to hair loss, often negatively impacts quality of life.

[0003] The causes of hair loss are diverse and range from age-related hair loss to genetically or hormonally caused disorders, autoimmune disorders, metabolic disorders including malnutrition, to infections, trauma, tumors and medications such as cytostatics and anticoagulants.

[0004] Hair loss caused by hormones such as androgens is called androgenetic alopecia (also known as AGA) and is considered the most common cause of hair loss, particularly in men but also in women. A distinction can be made between male and female patterns of hair loss. Other common forms of non-scarring alopecia include telogen effluvium (TE), a diffuse hair loss, and acute, inflammatory, circular hair loss, also known as alopecia areata (AA).

[0005] Hair growth and regrowth depend on an adequate supply of nutrients to the hair follicles, which is provided via the blood.

[0006] Reduced blood flow (microcirculation) to the scalp can thus promote or even cause hair loss. For example, in bald men, blood flow to the vertex region of the scalp is significantly lower than in men with normal scalp hair. This significantly reduced microcirculation can therefore explain hair loss as well as the lack of hair regrowth (transition from telogen to anagen), for example, in androgenetic alopecia. Overall, hair loss can therefore be considered one of the first clinical signs of reduced blood flow in the peripheral vessels.

[0007] On the other hand, the influence of nutrient deficiencies on hair structure and hair growth is also discussed. Effects on hair growth include acute telogen effluvium (TE), a known consequence of sudden weight loss or reduced protein intake, and diffuse alopecia, which occurs with niacin deficiency. Studies have also reported possible links between nutrient deficiencies and chronic TE, androgenetic alopecia (AGA), female pattern hair loss (FPHL), and alopecia areata (AA) (Guo EL, Katta R. Diet and hair loss: effects of nutrient deficiency and supplement use. Dermatol Pract Concept. 2017;7(1): 1).

[0008] Micronutrients such as vitamins and minerals play an important, but not entirely clear, role in the normal development of hair follicles and the function of immune cells. Accordingly, numerous studies suggest a link between hair loss and micronutrient deficiencies.

[0009] An overview of the role of vitamins and minerals such as vitamin A, vitamin B, vitamin C, vitamin D, vitamin E, iron, selenium and zinc in non-scarring alopecia is given by Almohanna et al. (Almohanna, Hind M et al. "The Role of Vitamins and Minerals in Hair Loss: A Review." Dermatology and therapy vol. 9,1 (2019): 51-70).

[0010] Guo and Katta describe the research situation regarding a deficiency of or supplementation with iron, zinc, niacin, fatty acids, selenium, vitamin D, vitamin A, vitamin E, folic acid, biotin, amino acids and proteins, as well as antioxidants.

[0011] Similarly, a review article by Goldberg and Lenzy addresses changes in hair due to general malnutrition and micronutrient deficiencies in certain patient groups (Goldberg LJ, Lenzy Y. Nutrition and hair. Clin Dermatol. 2010 Jul -Aug;28(4):412-9).

[0012] Finally, a possible role of dietary supplements such as amino acids, vitamins and trace elements, essential fatty acids, coenzymes Q and A, bioflavonoids, inositol, methylsulfonylmethane (MSM), dimethylglycine (DMG), silica, kelp, green tea extract, saw palmetto extract and grape seed extract in the prevention of hair loss is described in a review article by Jain et al. (Jain, Pushpendra & Joshi, Himanshu & Das, Debajyoti. (2012). Drug that Causes Hair Loss and Promotes Hair Growth- A Review. International Journal of Research in Pharmaceutical and Biomedical Sciences. 3. 1476-82).

[0013] A deficiency in such micronutrients could be a modifiable risk factor for the development, prevention and treatment of alopecia.

[0014] While vitamin and mineral supplements are relatively inexpensive and readily available, their use requires knowledge of which vitamins and minerals are helpful in treating hair loss. To date, however, few studies have investigated the effect of micronutrient supplementation on hair growth in patients with micronutrient deficiencies and alopecia to establish a link between hair loss and micronutrient deficiencies, and there is even less literature on the effects of supplementation in individuals without nutrient deficiencies.

[0015] Furthermore, there is evidence that an overdose of certain micronutrients, such as vitamin A, vitamin E or selenium, can even promote hair loss (Almohanna et al.; Guo and Katta).

[0016] In summary, dietary supplements can have both positive and negative effects on hair loss, and unless a nutrient deficiency is found, there is little evidence as to what type of supplementation is suitable to restore hair growth or prevent further hair loss.

[0017] In addition, there are currently only a few approved pharmaceutical treatment options for hair loss, such as androgenetic alopecia, and the existing treatments are either not sufficiently effective or come with unpleasant side effects. The situation is similarly unfavorable for treatment options for acute, inflammatory, circular hair loss (alopecia areata) and for hair loss caused by other factors.

[0018] This highlights the continued need for improved treatment methods, particularly for oral formulations that combat hair loss and have no or negligible side effects. Specifically, there is a need for readily available and easy-to-use dietary supplements. Similarly, there is a need for pharmaceutical-grade formulations without side effects, as well as cosmetic products.

[0019] WO 03 / 026438 describes a creatine delivery system. This creatine delivery system may also contain other bioactive ingredients such as nutraceuticals, carbohydrates, plant compounds, and vitamins.

[0020] Based on this, the object of the present invention was to provide a well-tolerated composition for the treatment of hair and scalp, in particular for the prevention and / or treatment of hair loss. Furthermore, this composition should be suitable for oral administration and overcome the disadvantages of compositions known from the prior art.

[0021] This problem was surprisingly solved by the composition according to claim 1 and its use according to claim 8. Preferred embodiments are described in the dependent claims.

[0022] According to the invention, the problem is solved by providing an oral composition which a) dimethylglycine and / or a salt of dimethylglycine, and b) contains amylopectin, wherein the weight ratio of the amount of amylopectin in the composition to the total amount of amylopectin and amylose in the composition is 0.9 to 1.0, wherein the composition contains 0.1 to 25.0 wt% dimethylglycine and / or a salt of dimethylglycine.

[0023] According to the invention, component b) is the polysaccharide amylopectin, which can be present in the form of a starch-like composition consisting of amylopectin and amylose, wherein the proportion of amylopectin in the starch-like composition is at least 90%. The remaining proportion of the starch-like composition, up to 10%, can be amylose.

[0024] According to the invention, the proportion of amylopectin in the total amount of amylopectin and amylose, also with respect to the oral composition according to the invention, is at least 90%. Correspondingly, the proportion of amylose, if present, is up to 10% of the total amount of amylopectin and amylose, also with respect to the entire oral composition according to the invention. In other words, according to the definition of component b), it is essential to the invention that the composition has the highest possible proportion of amylopectin compared to the proportion of amylose.

[0025] Accordingly, according to the present invention, the weight ratio of the amount of amylopectin in the composition to the total amount of amylopectin and amylose in the composition is 0.9 to 1.0, wherein the weight ratio of 1.0 by definition means that no amylose is present in the composition.

[0026] It has surprisingly been shown that the composition according to the invention, comprising dimethylglycine and / or a salt of dimethylglycine as well as one or more amylopectins, exhibits excellent efficacy in the treatment of hair loss, particularly hereditary and age-related hair loss. The composition activates the scalp and significantly improves the supply of nutrients and oxygen to the scalp and hair roots. Furthermore, it is extremely well-tolerated both medically and cosmetically; in particular, the composition is especially well-tolerated medically.

[0027] Dimethylglycine ( N,N Dimethylglycine (D-dimethylglycine) occurs in plants, animals, and humans, although it is produced in humans only in very small amounts. It is formed as an intermediate in the multi-step biosynthesis of glycine from choline through the transamination of betaine by betaine homocysteine ​​methylase.

[0028] N,N-Dimethylglycine, also (dimethylamino)acetic acid, is represented by the following chemical formula 1:

[0029] According to the present invention, it was surprisingly found that dimethylglycine and / or a salt of dimethylglycine is not only suitable for topical application, but in combination with amylopectin is also excellently suited as an oral preparation for improving the condition of the hair and scalp, in particular for the treatment or prevention of hair loss.

[0030] This was particularly surprising because starch, whose main component is amylopectin, was commonly used in the prior art as an inert carrier or filler and even as a placebo in application studies, and thus starch or its components amylopectin and amylose were not attributed any effect (Morganti, P., et al. (1998). "EFFECT OF GELATIN-CYSTINE AND SERENOA REPENS EXTRACT ON FREE RADICALS LEVEL AND HAIR GROWTH." J Appl Cosmetol 16: 57-64).

[0031] According to the invention, not only dimethylglycine but also its salts, solvates, and hydrates are used. These are preferably pharmaceutically or cosmetically acceptable salts of dimethylglycine. The salt is particularly preferably a water-soluble salt with a solubility in water of at least 10 g / L at 20°C.

[0032] In a preferred presentation, the salt of dimethylglycine is an alkali, alkaline earth, or ammonium salt of dimethylglycine.

[0033] Examples include sodium, potassium, calcium, magnesium, and ammonium salts. In the ammonium salts, the ammonium cation bears one to four alkyl groups, each with one to four carbon atoms independent of one another. The sodium and potassium salts of dimethylglycine are preferred, particularly the sodium salt of dimethylglycine, namely sodium dimethylglycinate (sodium N,N-dimethylglycinate).

[0034] In an alternative preferred embodiment, the salt of dimethylglycine can be the salt of an inorganic and / or organic acid containing dimethylglycine.

[0035] Examples of salts of dimethylglycine with an inorganic acid are the hydrochloride, hydrobromide, hydroiodide, hydrogen sulfate, sulfate, hydrogen sulfite, sulfite, hydrogen carbonate, carbonate, monophosphate, diphosphate, and triphosphate of dimethylglycine, as well as mixtures thereof. The hydrochloride of dimethylglycine, namely dimethylglycine hydrochloride ( N,N -Dimethylglycine hydrochloride).

[0036] Examples of salts of dimethylglycine with an organic acid are the acetate, lactate, citrate, succinate, fumarate, maleate, and benzoate of dimethylglycine, as well as mixtures thereof. According to the invention, the dimethylglycine and / or salt of dimethylglycine is preferably selected from the group consisting of dimethylglycine, sodium dimethylglycinate, and dimethylglycine hydrochloride.

[0037] It is assumed that, according to the invention, dimethylglycine and / or a salt of dimethylglycine improves cell activity and oxygen turnover in keratinocytes, thereby also promoting cell activity in the (scalp) skin and hair follicles. Furthermore, the (scalp) skin is smoothed and the skin barrier is strengthened. According to the invention, it thus achieves a significant hair root and (scalp) skin strengthening effect, particularly in the treatment of skin stressed or weakened by everyday life or age, as well as hair loss, such as hereditary and age-related hair loss.

[0038] The composition according to the invention further contains amylopectin, wherein the weight ratio of the amount of amylopectin in the composition to the total amount of amylopectin and amylose in the composition is 0.9 to 1.0. Suitable weight ratios according to the invention are in particular: 0.90; 0.91; 0.92; 0.93; 0.94; 0.95; 0.96; 0.97; 0.98; 0.99; 1.00.

[0039] In a preferred embodiment, the weight ratio of the amount of amylopectin in the composition to the total amount of amylopectin and amylose in the composition is 0.95 to 1.00, more preferably 0.96 to 1.00, more preferably 0.97 to 1.00, more preferably 0.98 to 1.00, more preferably 0.99 to 1.00.

[0040] Accordingly, the weight ratio of the amount of amylose in the composition to the total amount of amylopectin and amylose in the composition is 0 to 0.1. In a preferred embodiment, the weight ratio of the amount of amylose in the composition to the total amount of amylopectin and amylose in the composition is 0 to 0.05, more preferably 0 to 0.04, more preferably 0 to 0.03, more preferably 0 to 0.02, more preferably 0 to 0.01.

[0041] The levels of amylopectin and amylose can be determined using methods known in the field. Suitable methods are described, for example, in the publication Brust H, Orzechowski S, Fettke J. Starch and Glycogen Analyses: Methods and Techniques. Biomolecules. 2020; 10(7): 1020.

[0042] Amylopectin, along with amylose, is a component of starch.

[0043] The term "starch" refers to a polysaccharide with the formula (C₆H₁₀O₂)n, which consists of α-D-glucose units. These D-glucose units are linked together via glycosidic bonds, with linear chains formed by α-1,4-glycosidic bonds, which can be branched by α-1,6-glycosidic bonds. Starch usually consists of 20–30% amylose and 70–80% amylopectin.

[0044] Starch is a natural component of potatoes, cassava, cereals (e.g. wheat, corn, rice) and legumes (e.g. peas, lentils, white or red beans, chickpeas).

[0045] Amylose is a polysaccharide composed of α-D-glucose monomers forming linear chains with a helical structure. Amylose has a molar mass between 100,000 and 1,000,000 g / mol, corresponding to approximately 1,000 α-D-glucose monomers (in cereal starches) to 4,500 α-D-glucose monomers (in potato starches) linked by α-1,4-glycosidic bonds. At high molar masses, occasional α-1,6-glycosidic branches also occur.

[0046] Amylopectin is a polysaccharide composed of α-D-glucose monomers forming highly branched structures. These α-D-glucose monomers are linked by α-1,4-glycosidic bonds. Approximately every 10–50 monomers, preferably every 10–30 monomers, more preferably every 10–25 monomers, more preferably every 10–20 monomers, and most preferably every 12–15 monomers, a side chain is linked by an α-1,6-glycosidic bond, resulting in a tree-like branching pattern. These side chains can be short (12 to 20 glucose units), long (30 to 45 glucose units), or very long (averaging 60 glucose units) (FA Schüll: Influence of specific starch properties on the brewing process, Dissertation, Technical University of Munich 2012, pp. 12–13). Due to this difference in structure, amylopectin forms coils or tufts at the molecular level.Amylopectin exhibits branched structures, with branching points primarily located at the C6 atom (Habermehl, Hammann, Krebs: Natural Product Chemistry. An Introduction. 2nd edition. Springer, Berlin 2002, ISBN 978-3-540-43952-3). It has a high molar mass of 10,000,000 to 200,000,000 g / mol (C. Bächtle, P. Winkler and B. Stellbrink: A Question of the Right Starch. In: Chemistry in Our Time 45, 250-255 (2011); F.A. Schüll: Influence of Specific Starch Properties on the Brewing Process, Dissertation, Technical University of Munich 2012, p. 12: 3.0-4.1 million g / mol for amylopectin from barley).

[0047] The term "highly branched amylopectin" refers to a polysaccharide composed of α-D-glucose monomers with particularly highly branched structures. The α-D-glucose monomers are linked to each other by α,4-glycosidic bonds. An α-1,6-glycosidic side chain is linked approximately every 10-30 monomers, preferentially every 10-25 monomers, more preferentially every 10-20 monomers, and most preferentially every 12-15 monomers, resulting in a tree-like branching pattern.

[0048] As used herein, the terms "amylose" and "amylopectin" refer to polysaccharides consisting of α-D-glucose monomers according to the definitions above, the meanings of which do not overlap.

[0049] Amylopectin can be obtained by separating amylose and amylopectin from natural plant starch using chemical, physical, or enzymatic methods, for example, by enzymatic treatment with amylases. The properties of amylopectin can also be modified using similar methods.

[0050] According to the invention, amylopectin is obtained from natural plant starch selected from potato starch (Amylum solani), wheat starch (Amylum tritici), rice starch (Amylum oryzae), corn starch (Amylum maydis), millet starch (Amylum sorghum), or combinations thereof. In a preferred embodiment, the amylopectin used in the oral composition of the present invention is amylopectin from corn, potato, or millet starch.

[0051] According to the invention, it is further possible that the amylopectin is not a waxy grain or that the amylopectin is not obtained from a waxy grain. In one embodiment, the amylopectin is not waxy maize or is not obtained from waxy maize.

[0052] According to the present invention, the amylopectin contains one or more types of amylopectin which may differ in terms of the degree of branching (frequency of branches and length of side chains) and molecular weight.

[0053] In a preferred embodiment, the amylopectin is composed of at least 1000 D-glucose monomers, preferably at least 4500, more preferably at least 5000, more preferably at least 10000 D-glucose monomers, which are linked together by α-1,4-glycosidic bonds.

[0054] In a further preferred embodiment, the amylopectin contains a side chain of D-glucose monomers linked α-1,6-glycosidically approximately every 10-50 monomers, preferably approximately every 10-30 monomers, more preferably approximately every 10-25 monomers, more preferably approximately every 10-20 monomers, and most preferably approximately every 12-15 monomers.

[0055] In a further preferred embodiment, the side chains of the amylopectin each comprise about 5-60 monomers, preferably about 10-30 monomers each, more preferably about 10-20 monomers each, and more preferably about 10-15 monomers each. The monomers mentioned are all α-D-glucose monomers.

[0056] The term "D-glucose monomers", as used herein, refers to α-D-glucose monomers.

[0057] In a further preferred embodiment, the amylopectin has a molar mass of at least 100,000 g / mol, preferably at least 100,000 g / mol up to 200,000,000 g / mol, more preferably at least 1,000,000 g / mol up to 200,000,000 g / mol, and more preferably at least 10,000,000 g / mol up to 200,000,000 g / mol.

[0058] The composition according to the invention may contain, in addition to amylopectin b), further polysaccharides, provided that the weight ratio of the amount of amylopectin in the composition to the total amount of amylopectin and amylose in the composition is 0.9 to 1.0.

[0059] In a preferred embodiment, the composition according to the invention does not contain conventional starch, wherein the term "conventional starch" as used herein refers to starch with a composition of 20-30% amylose and 70-80% amylopectin.

[0060] In a further preferred embodiment, the composition according to the invention does not contain amylose.

[0061] The composition according to the invention contains dimethylglycine and / or a salt of dimethylglycine in a proportion of 0.1 wt.% to 25.0 wt.%, based on the total weight of the composition. In a preferred embodiment, the composition according to the invention contains dimethylglycine and / or a salt of dimethylglycine in a proportion of 1 wt.% to 20.0 wt.%, more preferably 2 wt.% to 18.0 wt.%, in each case based on the total weight of the composition. In a preferred embodiment of the invention, the composition according to the invention may contain 1 wt.%, 2 wt.%, 3 wt.%, 4 wt.%, 5 wt.%, 6 wt.%, 7 wt.%, 8 wt.%, 9 wt.%, 10 wt.%, 11 wt.%, 12 wt.%, 13 wt.%, 14 wt.%, 15 wt.%, 20 wt.%, or 25 wt.% dimethylglycine and / or a salt of dimethylglycine, in each case based on the total weight of the composition.

[0062] Preferably, the composition according to the invention contains dimethylglycine and / or a salt of dimethylglycine as a pure chemical substance, including the respective solvates and hydrates (e.g., the dihydrate of sodium dimethyl glycinate), since this increases the purity of the composition and reduces the occurrence of undesirable side effects. For this reason, the composition according to the invention preferably contains the chemical derivatives of dimethylglycine selected from methylglycine, trimethylglycine, (2-hydroxyethyl)trimethylammonium, and trimethylhydroxybutyrobetaine, in concentrations of less than 0.01% by weight, based on the total weight of the composition. Particularly preferred are the compositions according to the invention that are completely free of these derivatives.

[0063] In a preferred embodiment, the composition according to the invention c) contains at least one further active ingredient, wherein the at least one further active ingredient is selected from amla extract, amylodextrin, β-carotene, biotin, carnitine, curcumin, echinacea, ectoin, iron, folic acid, pomegranate extract, green tea extract, millet extract, millet oil, pumpkin seed oil, creatine, L-cysteine, L-lysine, niacin, niacinamide, pantolactone, pantothenic acid, piperine, procyanidin, rosemary extract, saw palmetto extract, horsetail extract, selenium, silicon, taurine, tocopheryl acetate, tomato extract, ubiquinone-10, vitamin B1, vitamin B2, vitamin B6, vitamin B12, vitamin C, vitamin E, zinc and combinations thereof, in particular selected from zinc, biotin, millet extract, selenium and combinations thereof.

[0064] Amla extract is an extract from the Indian gooseberry (Phyllanthus emblica). In the composition according to the invention, amla extract can be present in an amount of 0.1–50.0 wt.%, preferably 1–30 wt.%, more preferably 5–25 wt.%, in each case based on the total weight of the composition.

[0065] In the composition according to the invention, amylose is preferably present in an amount of 0-5 wt%, based on the total weight of the composition. Amylodextrin is a conversion product of starch using dilute acids. Amylodextrin (6 C 6 H 10 O 6 + 2 H 2 O) is a compound isomeric to starch. Amylodextrin can also be obtained as the end product of the hydrolysis of amylopectin by β-amylase. In the composition according to the invention, one or more amylodextrins may be present in an amount of 0.1-10.0 wt%, preferably 1-5 wt%, based on the total weight of the composition.

[0066] Beta-carotene is a precursor of vitamin A and is therefore also called provitamin A. In the composition according to the invention, beta-carotene can be present in an amount of 0.01–1.0 wt.%, preferably 0.05–0.5 wt.%, in each case based on the total weight of the composition.

[0067] Biotin, also known as vitamin B7 or vitamin H, is a water-soluble vitamin from the B complex. According to the invention, biotin can further reduce hair loss and strengthen the skin. In the composition according to the invention, biotin can be present in an amount of 0.001–10.0 wt.%, preferably 0.005–1.0 wt.%, based on the total weight of the composition.

[0068] In the composition according to the invention, carnitine can be present in an amount of 0.001 wt.% to 10.0 wt.%, preferably 0.005 wt.% to 7.50 wt.%, in each case based on the total weight of the composition.

[0069] In the composition according to the invention, curcumin can be contained in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0070] Echinacea can stimulate blood circulation in the scalp, thus supplying the hair follicles with oxygen- and nutrient-rich blood, which has a further stabilizing effect on the hair and especially the hair root. In the composition according to the invention, echinacea can be present in an amount of 0.001% to 10.0% by weight, preferably 0.005% to 7.50% by weight, based on the total weight of the composition.

[0071] Ectoin is a cyclic amino acid and, according to the invention, further stabilizes the natural structure of hair. In the composition according to the invention, ectoin can be present in an amount of 0.001 wt.% to 10.0 wt.%, preferably 0.005 wt.% to 7.50 wt.%, in each case based on the total weight of the composition.

[0072] In the composition according to the invention, iron can be present in an amount of 0.01-1.0 wt.%, preferably 0.05-0.5 wt.%, in each case based on the total weight of the composition.

[0073] In the composition according to the invention, folic acid can be present in an amount of 0.001-1.0 wt.%, preferably 0.05-0.5 wt.%, in each case based on the total weight of the composition.

[0074] In the composition according to the invention, pomegranate extract can be included in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0075] In the composition according to the invention, green tea extract can be included in an amount of 0.1-10.0 wt.%, preferably 1.0-5.0 wt.%, based on the total weight of the composition.

[0076] In the composition according to the invention, millet extract can be contained in an amount of 0.01-40.0 wt.%, preferably 1-35 wt.%, more preferably 5-30 wt.%, in each case based on the total weight of the composition.

[0077] In the composition according to the invention, millet oil can be contained in an amount of 0.01-30.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0078] In the composition according to the invention, pumpkin seed oil can be contained in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0079] The composition according to the invention can contain creatine from 0.001 wt.% to 10.0 wt.%, preferably from 0.005 wt.% to 7.50 wt.%, in each case based on the total weight of the composition.

[0080] In the composition according to the invention, L-cysteine ​​can be contained in an amount of 0.01-20.0 wt.%, preferably 0.1-1.0 wt.%, in each case based on the total weight of the composition.

[0081] In the composition according to the invention, L-lysine can be contained in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0082] In the composition according to the invention, niacin can be contained in an amount of 0.1-10.0 wt.%, preferably 0.5-5.0 wt.%, in each case based on the total weight of the composition.

[0083] Niacinamide (also known as nicotinamide) is the amide of nicotinic acid and is also called vitamin B3. In addition to other properties, such as reducing oxidative stress, niacinamide has a hair growth-stimulating effect according to the invention. The composition according to the invention can contain 0.001 wt.% to 10.0 wt.%, preferably 0.005 wt.% to 7.50 wt.%, based on the total weight of the composition.

[0084] Pantolactone belongs to the group of substituted lactones and, according to the invention, further stimulates the growth factors of the hair roots. The composition according to the invention can contain 0.001 wt.% to 10.0 wt.%, preferably 0.005 wt.% to 7.50 wt.%, based on the total weight of the composition.

[0085] In the composition according to the invention, pantothenic acid can be present in an amount of 0.01-10.0 wt.%, preferably 0.1-2.0 wt.%, in each case based on the total weight of the composition.

[0086] In the composition according to the invention, piperine can be contained in an amount of 0.01- 5.0 wt.%, preferably 0.05-2.0 wt.%, in each case based on the total weight of the composition.

[0087] In the composition according to the invention, procyanidin can be contained in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0088] In the composition according to the invention, rosemary extract can be contained in an amount of 0.001–20.0 wt.%, preferably 0.01–5.0 wt.%, in each case based on the total weight of the composition.

[0089] In the composition according to the invention, saw palmetto extract can be contained in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0090] In the composition according to the invention, horsetail extract can be contained in an amount of 0.01-1.0 wt.%, preferably 0.1-1.0 wt.%, in each case based on the total weight of the composition.

[0091] In the composition according to the invention, selenium can be contained in an amount of 0.0001-0.5 wt.%, preferably 0.001-0.01 wt.%, in each case based on the total weight of the composition.

[0092] In the composition according to the invention, silicon (silicic acid) can be contained in an amount of 0.01-10.0 wt.%, preferably 0.1-5.0 wt.%, in each case based on the total weight of the composition.

[0093] According to the invention, taurine or 2-aminoethanesulfonic acid also acts as an antioxidant, further stabilizing the skin and hair, and in particular the hair root. The composition according to the invention can contain taurine from 0.001 wt.% to 10.0 wt.%, preferably from 0.005 wt.% to 7.50 wt.%, based on the total weight of the composition.

[0094] Tocopheryl acetate exhibits antioxidant properties and, according to the invention, further stabilizes the skin and hair, and in particular the hair root. The composition according to the invention can contain tocopheryl acetate in amounts from 0.001 wt.% to 10.0 wt.%, preferably from 0.005 wt.% to 7.50 wt.%, based on the total weight of the composition.

[0095] In the composition according to the invention, tomato extract can be contained in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0096] Ubiquinone-10 (Q10 or coenzyme Q10) is a quinone derivative. Q10, which belongs to the ubiquinone pool, is considered an antioxidant and, according to the invention, has a stabilizing effect on the skin and hair, and in particular on the hair root. In the composition according to the invention, ubiquinone-10 can be present in amounts from 0.001 wt.% to 10.0 wt.%, preferably from 0.005 wt.% to 7.50 wt.%, based on the total weight of the composition.

[0097] In the composition according to the invention, vitamin B1 (thiamine) can be contained in an amount of 0.01-5.0 wt.%, preferably 0.05-1.0 wt.%, in each case based on the total weight of the composition.

[0098] In the composition according to the invention, vitamin B2 (riboflavin) can be contained in an amount of 0.01-5.0 wt.%, preferably 0.05-1.0 wt.%, in each case based on the total weight of the composition.

[0099] In the composition according to the invention, vitamin B6 can be present in an amount of 0.01-5.0 wt.%, preferably 0.05-0.5 wt.%, in each case based on the total weight of the composition.

[0100] In the composition according to the invention, vitamin B12 can be contained in an amount of 0.00001-0.01 wt.%, preferably 0.00005-0.0005 wt.%, in each case based on the total weight of the composition.

[0101] In the composition according to the invention, vitamin C can be contained in an amount of 0.1-20.0 wt.%, preferably 1-15 wt.%, in each case based on the total weight of the composition.

[0102] In the composition according to the invention, vitamin E can be contained in an amount of 0.01-10.0 wt.%, preferably 0.1-5.0 wt.%, in each case based on the total weight of the composition.

[0103] Zinc, as a substance with antimicrobial effect, can be added to the composition according to the invention in an amount of 0.01-30.0 wt.%, preferably 0.1-5.0 wt.%, in each case based on the total weight of the composition.

[0104] According to the invention, the composition is administered orally. Oral administration means internal use.

[0105] In a preferred embodiment, the composition according to the present invention is a dietary supplement, in particular a dietary supplement to promote the metabolism of the hair and / or scalp and / or to promote hair growth and / or to treat and / or prevent hair loss.

[0106] Compositions according to the invention, in particular for food supplements, are preferably in the form of capsules, lozenges, tablets, pills and other similar dosage forms, powder sachets, liquid ampoules, bottles with dropper inserts and similar dosage forms of liquids and powders for the intake of the product.

[0107] In a preferred embodiment, the components, in particular a) dimethylglycine and / or a salt of dimethylglycine, b) amylopectin, wherein the weight ratio of the amount of amylopectin in the composition to the total amount of amylopectin and amylose in the composition is 0.9 to 1.0, wherein the composition contains 0.1 to 25.0 wt% dimethylglycine and / or a salt of dimethylglycine, and c) the other active ingredient(s) for the treatment of the hair and / or scalp, if present, as well as one or more suitable carrier material(s), are contained in the composition according to the invention as a compressed tablet or in a capsule, e.g. a hard gelatin capsule or soft gelatin capsule.

[0108] Suitable carrier substances include, but are not limited to, vegetable oils such as coconut oil, soybean oil, soy lecithin, sunflower oil, olive oil, palm oil, rapeseed oil and linseed oil; beeswax; sugar alcohols such as sorbitol, mannitol, isomalt, maltitol, lactitol, xylitol and erythritol; monosaccharides such as dextrose (glucose), mannose, fructose; disaccharides such as maltose; and indigestible carbohydrates such as cellulose and pectins.

[0109] According to the invention, one or more vegetable oils are preferably used as a carrier substance in capsules. For tablets, one or more sugars or sugar alcohols, preferably xylitol, are preferably used.

[0110] The composition according to the invention can be produced by methods known to those skilled in the art.

[0111] The present invention further relates to the use of the composition according to the invention for improving the condition of the hair and / or the scalp and / or for promoting the metabolism of the hair and / or the scalp and / or for promoting hair growth and / or for treating and / or preventing hair loss.

[0112] The term hair loss includes alopecia areata (circular hair loss), alopecia androgenetica (hereditary hair loss) in women and men, diffuse alopecia (diffuse hair loss), age-related hair loss (senescent alopecia) and hair loss caused by chemotherapy.

[0113] The most preferred type of hair loss to be treated is hereditary hair loss (androgenetic alopecia).

[0114] Age-related hair loss (senescent alopecia) is also particularly preferred for treatment.

[0115] The use is primarily cosmetic or medical.

[0116] Surprisingly, the use according to the invention not only led to a reduction in daily hair loss, but also to an increase in hair density and positive effects on hair root activity compared to a control group, whereby hair density and hair root activity were determined by established standard methods from the field of dermatology before and after administration (see, among others, Serrano-Falcón C, Fernandez-Pugnaire MA, Serrano-Ortega S. Hair and scalp evaluation: the trichogram.).

[0117] The following compositions are intended to illustrate the invention without limiting it to the specific examples. Experimental section

[0118] The following compositions were prepared using methods known to those skilled in the art. The quantity of each component was chosen such that its weight fraction in the premix corresponds to the specified weight fractions. Example 1

[0119] Composition in tablet form, containing the following components: nutrient single dose % by weight Vitamin C 100 mg 7,28 Vitamin E (α-tocopherol) 6.8 mg 0,50 Vitamin B2 1.4 mg 0,10 Vitamin B12 2 µg 0,0001 zinc 20 mg 1,46 Piperine 10 mg 0,73 Pantothenic acid 9 mg 0,66 Biotin / Vitamin H 150 µg 0,01 Folic acid 312 µg 0,02 Silicon 20 mg 1,46 L-Cysteine 6 mg 0,44 Millet extract 400 mg 29,12 L-Lysine 100 mg 7,28 Na- N,N -Dimethylglycinat 200 mg 14,56 highly branched amylopectin 500 mg 36,40 Sugar alcohol as a carrier substance qs qs Example 2

[0120] Composition in the form of a capsule containing the following components: nutrient single dose % by weight Vitamin C 110 mg 11,20 Vitamin E (α-tocopherol) 20 mg 2,04 niacin 18 mg 1,83 zinc 5 mg 0,51 Pantothenic acid 6 mg 0,61 Natural tomato extract 66 mg 6,72 β-Carotene / Provitamin A 2 mg 0,20 Vitamin B6 1.8 mg 0,18 Vitamin B2 (Riboflavin) 1.4 mg 0,14 Vitamin B1 (Thiamine) 1.3 mg 0,13 Folic acid 312 µg 0,03 Biotin 150 µg 0,02 selenium 32 µg 0,0033 Vitamin B12 2 µg 0,0002 N,N -Dimethylglycin - hydrochlorid 150 mg 15,28 highly branched amylopectin 600 mg 61,10 Vegetable oil as a carrier substance qs qs Example 3

[0121] Composition in the form of a capsule containing the following components: nutrient single dose % by weight Biotin 1 0,02 Vitamin C 100 1,98 Vitamin E (α-tocopherol) 7 0,14 zinc 20 0,40 selenium 0,2 0,004 iron 8 0,16 Silicon 20 0,40 Saw palmetto extract 500 9,89 Horsetail extract 25 0,49 Amla extract 1000 19,79 pumpkin seed oil 400 7,91 Procyanidin 400 7,91 Green tea extract 200 3,96 Rosemary extract 3 0,06 Curcumin 500 9,89 Piperine 10 0,20 Pomegranate extract 500 9,89 millet oil 400 7,91 L-Cysteine 10 0,20 L-Lysine 200 3,96 N,N -Dimethylglycin - hydrochlorid 150 2,97 highly branched amylopectin 600 11,87 Vegetable oil as a carrier substance qs qs Reference example 1

[0122] Composition in tablet form (without sodium dimethylglycinate and highly branched amylopectin) containing the following components: nutrient single dose % by weight Vitamin C 100 mg 7,28 Vitamin E (α-tocopherol) 6.8 mg 0,5 0 Vitamin B2 1.4 mg 0,10 Vitamin B12 2 µg 0,0001 zinc 20 mg 1,46 Piperine 10 mg 0,73 Pantothenic acid 9 mg 0,66 Biotin / Vitamin H 150 µg 0,01 Folic acid 312 µg 0,02 Silicon 20 mg 1,46 L-Cysteine 6 mg 0,44 Millet extract 400 mg 29,12 Lysine 100 mg 7,28 Sugar alcohol as a carrier substance qs qs Study design and results

[0123] 1. In an in vitro study, the effect of sodium dimethylglycinate in combination with highly branched amylopectin was investigated in a cell culture model using human keratinocyte cells. For this purpose, HaCaT cells were cultured for 1, 3, 5, and 7 days in DMEM medium (including fetal calf serum and an antibiotic-antifungal mix), and the viability and proliferation of the cells were determined using appropriate measurement methods, as well as the expression of growth factors relevant to cell growth. Proof of viability:

[0124] For this measurement, a so-called MTT assay was used to determine cellular metabolic activity as an indicator of cell viability and cytotoxicity. This colorimetric assay is based on the reduction of a yellow tetrazolium salt (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide or MTT) to purple formazan crystals by metabolically active cells.

[0125] Human epidermal keratinocyte cells (HaCaT) were seeded in a 96-well plate at a cell density of 5,000 cells / well and cultured in medium (DMEM with 10% FBS, 1% penicillin-streptomycin, 0.5% Fungizone). The cell culture medium was changed the following day (start of treatment) and after further 24, 48, and 72 hours of cultivation at 37°C and 5 vol% CO2, either without (control) or with the existing concentrations of sodium dimethylglycinate (DMG), highly branched amylopectin, and the combination of DMG and highly branched amylopectin. Viability was measured analogously to previously published studies in BI Tóth, N. Dobrosi, A. Dajnoki, G. Czifra, A. Oläh, AG Szöllösi, I. Juhäsz, K. Sugawara, R. Paus, T. Biro, J Invest Dermatol 2011, 131, 1095-1104. Evidence of proliferation:

[0126] A CyQUANT assay was performed to measure proliferation. In this fluorescence-based assay, the fluorescent dye used binds to DNA (deoxyribonucleic acid), with the amount of cellular DNA being a direct measure of the number of cells within a sample.

[0127] Human epidermal keratinocyte cells (HaCaT) were seeded in a 96-well plate at a cell density of 5,000 cells / well and cultured in medium (DMEM with 10% FBS, 1% penicillin-streptomycin, 0.5% Fungizone). The cell culture medium was changed the following day (start of treatment) and after further 24, 48, and 72 hours of cultivation at 37°C and 5 vol% CO2, either without (control) or with the existing concentrations of sodium dimethylglycinate (DMG), highly branched amylopectin, and the combination of DMG and highly branched amylopectin. The measurement of proliferation was carried out analogously to previously published studies in A. Oläh, BI Tóth, I. Borbirö, K. Sugawara, AG Szöllösi, G. Czifra, B. Pal, L. Ambrus, J. Kloepper, E. Camera, The Journal of clinical investigation 2014, 124, 3713-3724. Evidence of gene expression:

[0128] Human epidermal keratinocyte cells (HaCaT) were seeded in a 6-well plate at a cell density of 140,000 cells / well and cultured in medium (DMEM with 10% FBS, 1% penicillin-streptomycin, 0.5% Fungizone) at 37°C and 5 vol% CO2. The following day (start of treatment), the cell culture medium was changed with or without the previously added concentrations of sodium dimethylglycinate (DMG), highly branched amylopectin, and the combination of DMG and highly branched amylopectin, and the cells were harvested after 24 hours. Gene expression was measured by qRT-PCR based on previously published studies in BV Diaz, M.-C. Lenoir, A. Ladoux, C. Frelin, M. Démarchez, S. Michel, Journal of Biological Chemistry 2000, 275, 642-650.

[0129] It has been shown that with Na-dimethylglycinate in combination with highly branched amylopectin, the parameters relevant for the growth of HaCaT cells were positively influenced and the expression of growth factors (e.g. HGF, KGF, VEGF, GM-CSF) was significantly increased compared to the treatment of HaCaT cells with only Na-dimethylglycinate or with only highly branched amylopectin.

[0130] 2. The composition according to the invention from Example 1 (verum composition with sodium dimethylglycinate and highly branched amylopectin) and the composition from Reference Example 1 (placebo composition without sodium dimethylglycinate and highly branched amylopectin) were also administered in a randomized, controlled, and joint-labeled study to a group of 60 male and female subjects for 6 months. The subjects were asked to subjectively assess the reduction in their hair loss after completion of the administration, and these results were recorded using questionnaires. Simultaneously, hair density and hair root activity were determined before and after administration using established standard dermatological methods (see, among others, Serrano-Falcón C, Fernández-Pugnaire MA, Serrano-Ortega S. Hair and scalp evaluation: the trichogram). During or after the administration, the hair density and hair root activity were determined using established standard dermatological methods (see, among others, Serrano-Falcón C, Fernández-Pugnaire MA, Serrano-Ortega S. Hair and scalp evaluation: the trichogram).After oral administration of the composition according to the invention from Example 1, more subjects reported less hair loss compared to the control group receiving the placebo composition. Objective measurements showed that oral administration of the composition according to the invention from Example 1 resulted in an increase in hair density and positive effects on hair root activity compared to the control group.

Claims

1. Oral composition containing a) dimethylglycine and / or a salt of dimethylglycine, and b) amylopectin, wherein the weight ratio of the amount of amylopectin in the composition to the total amount of amylopectin and amylose in the composition is 0.9 to 1.0, and wherein the composition contains 0.1 to 25.0 wt.% dimethylglycine and / or a salt of dimethylglycine.

2. Composition according to claim 1, wherein the amylopectin is composed of D-glucose monomers which are joined together by α-1,4-glycosidic bonds, and wherein approximately every 10 to 30 monomers a side chain of D10 glucose monomers is linked by α-1,6-glycosidic bonds.

3. Composition according to claim 2, wherein the side chains of the amylopectin each comprise about 5-60 monomers, preferably about 10-30 monomers, more preferably in each case about 10-20 monomers, more preferably about 10-15 monomers.

4. Composition according to any one of the preceding claims, wherein the amylopectin has a molar mass of at least 100,000 g / mol.

5. Composition according to any one of the preceding claims, wherein the composition further comprises: c) at least one additional active ingredient selected from amla extract, amylodextrin, β-carotene, biotin, carnitine, curcumin, echinacea, ectoin, iron, folic acid, pomegranate extract, green tea extract, millet extract, millet oil, pumpkin seed oil, creatine, I-cysteine, I-lysine, niacin, niacinamide, pantolactone, pantothenic acid, piperine, procyanidin, rosemary extract, sage palm extract, horsetail extract, selenium, silicon, taurine, tocopheryl acetate, tomato extract, ubiquinone-10, vitamin B1, vitamin B2, vitamin B6, vitamin B12, vitamin C, vitamin E, zinc, and combinations thereof.

6. Composition according to any of the preceding claims, wherein the composition is a dietary supplement to promote hair and / or scalp metabolism and / or promote hair growth and / or treat and / or prevent alopecia.

7. Composition according to any of claims 1 to 6 for use in the treatment and / or prevention of alopecia.

8. Composition for use in the treatment and / or prevention of alopecia according to claim 7, wherein the alopecia is selected from alopecia areata (patchy hair loss), androgenetic alopecia (hereditary hair loss) in women and men, diffuse alopecia (diffuse hair loss), age-related alopecia (senescent alopecia), and alopecia caused by chemotherapy.

9. Cosmetic use of the composition according to any one of claims 1 to 6.

10. Cosmetic use according to claim 9 for improving the condition of the hair and / or scalp and / or for promoting the metabolism of the hair and / or scalp and / or for promoting hair growth.