• 专利附录
  • 专利说明
  • 权利要求
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    • 专利摘要:
    A composition comprisingviii) at least one vitamin B compound;ix) cysteine or a derivative thereof;x) lysine or a derivative thereof;xi) procyanidin or a derivative thereof;xii) a xanthonoid;xiii) methionine or a derivative thereof; andxiv) collagen;or any pharmaceutically acceptable salts or esters thereof.
    公开号:EP3695832A1
    申请号:EP20157498.5
    申请日:2020-02-14
    公开日:2020-08-19
    发明作者:Nils K. MORTENSEN；Audrey Wong MORTENSEN
    申请人:Dui Clinique As；
    IPC主号:A61K36-00
    专利说明:
    [0001] The invention relates to a composition for retarding hair loss or facilitating hair growth or regrowth. The invention also relates to the use of the composition as a hair growth or regrowth product, to a method for enhancing hair growth or hair regrowth, and to the use of the composition in the preparation of a medicament for the treatment or prevention of hair loss. Background to the invention
    [0002] Hair loss can be caused by a number of factors. Hair loss can be genetic (e.g. male pattern baldness), or can be caused by various other factors such as an illness, stress, cancer treatment, weight loss or iron deficiency. There are various types of hair loss such as male-pattern hair loss, female-pattern hair loss, alopecia areata, or telogen effluvium.
    [0003] The two main treatments for male pattern baldness are minoxidil and finasteride. Minoxidil can also be used to treat female pattern baldness. These treatments, however, do not work for everyone and can be expensive. Furthermore, common side effects for minoxidil include burning or irritation of the eye, itching, redness or irritation at the treated area, and unwanted hair growth elsewhere on the body. The use of finasteride has been associated with sexual function side effects.
    [0004] Other hair loss treatments include steroid injections, steroid creams, immunotherapy, light treatment, tattooing, hair transplants, scalp reduction surgery, artificial hair transplants. Many of those treatments have disadvantages in terms of cost, effectiveness, side-effects and/or invasiveness.
    [0005] It would clearly be desirable to provide a composition for retarding hair loss or facilitating hair growth/regrowth, in particular on the human scalp, by using a non-invasive, cost-efficient treatment with few or no side effects.
    [0006] The present invention addresses at least some of the above issues. The particular combination of ingredients in the composition is beneficial in that hair (re-)growth is enhanced, yet the ingredients are unharmful, cheap, and the composition can simply be ingested daily, without the need for any invasive procedures. Summary of the invention
    [0007] In a first aspect, the present invention provides a composition comprising:i) at least one vitamin B compound; ii) cysteine or a derivative thereof; iii) lysine or a derivative thereof; iv) procyanidin or a derivative thereof; v) a xanthonoid; vi) methionine or a derivative thereof; and vii) collagen; or any pharmaceutically acceptable salts or esters thereof.
    [0008] In a further aspect, the invention provides the use of the composition as herein defined as a hair growth or regrowth product.
    [0009] In a further aspect, the invention provides the composition as defined herein for use in the treatment or prevention of hair loss.
    [0010] In a further aspect, the invention provides a method for enhancing hair growth or hair regrowth in a human in need thereof, comprising administering an effective amount of the composition as defined herein to a patient.
    [0011] In a further aspect, the invention provides the use of the composition as defined herein in the preparation of a medicament for the treatment or prevention of hair loss.
    [0012] The features of the aspects and/or embodiments indicated herein are usable individually and in combination in all aspects and embodiments of the invention where technically viable, unless otherwise indicated. Detailed description of the invention
    [0013] The present invention provides a composition for the treatment or prevention of hair loss. The compositions thus act to promote hair growth/regrowth and/or reduce the rate of hair loss.
    [0014] The composition of the invention comprises i) at least one vitamin B compound ii) cysteine; iii) lysine; iv) procyanidin; v) xanthonoid; vi) methionine; and vii) collagen; or any pharmaceutically acceptable salts or esters thereof.
    [0015] As a general point, when particular vitamins are referred to herein, the term is intended to cover conventional derivatives of such vitamins (e.g. acetates), salts, solvates or hydrates thereof, where technically appropriate. For example, the term vitamin B1 would cover thiamine hydrochloride, the term vitamin B5 covers D-calcium pantothenate, the term vitamin B6 covers pyridoxine hydrochloride, and the term vitamin E covers alpha tocopheryl acetate.
    [0016] Where wt% amounts are given for vitamins or aminoacids, the wt% relates to the amount of actual vitamin or actual amino acid required in the composition rather than the weight of the compound used. For example, where the composition comprises thiamine HCl, D-calcium pantothenate, pyridoxine hydrochloride, L-cysteine HCI monohydrate, or L-lysine monohydrochloride, the indicated wt% values relate to the amount of thiamine, pantothenate, pyridoxine, L-cysteine and L-lysine respectively. We do not count the weight of the inactive counter ion. The wt% values indicate the desired range of the active agent therefore. Vitamins
    [0017] Typically, the composition of the invention comprises one or more vitamin B compounds, e.g. at least two, at least three, at least four, at least five, at least six, or at least seven different vitamin B compounds. The vitamin B compounds of the invention are preferably selected from vitamin B1, B2, B3, B5, B6, B7, B9 and B12. In a particular embodiment, all of vitamins B1, B2, B3, B5, B6, B7, B9 and B12 are present in the composition.
    [0018] Vitamin B1 covers thiamine or a derivative thereof such as a salt thereof, such as thiamine hydrochloride. Vitamin B2 covers riboflavin or a derivative thereof such as a salt thereof.
    [0019] Vitamin B3 covers nicotinamide or a derivative thereof.
    [0020] Vitamin B5 covers pantothenic acid or a derivative thereof such as a salt thereof, such as calcium pantothenate (e.g. D-calcium pantothenate), as well as pantothenol.
    [0021] Vitamin B6 covers pyridoxine or a derivative thereof such as a salt thereof, such as pyridoxine hydrochloride.
    [0022] Vitamin B7 covers biotin or a derivative thereof, e.g. D-biotin.
    [0023] Vitamin B9 covers folic acid or a derivative thereof such as a salt thereof.
    [0024] Vitamin B12 covers cyanocobalamin or a derivative thereof.
    [0025] It is preferred if the composition comprises at least Riboflavin or a derivative thereof (vitamin B2) and D-Biotin or a derivative thereof (vitamin B7). Typically, the amount of riboflavin in the composition is 0.001-0.2 wt%, e.g. 0.005-0.2 wt%, 0.01-0.1 wt%, or 0.01-0.05 wt%, based on the total weight of the composition.
    [0026] Typically, the amount of D-Biotin in the composition is 0.0001-0.01 wt%, e.g. 0.001-0.005 wt% based on the total weight of the composition.
    [0027] Typically, component i) of the composition (i.e. the totality of vitamin B compounds) is present in an amount of 0.05-5.0 wt%, based on the total weight of the composition, such as 0.1-2.0 wt%, e.g. 0.2-1.0 wt%, based on the total weight of the composition.
    [0028] In a particular embodiment, the composition further comprises ascorbic acid (vitamin C). Preferably, the ascorbic acid is present in an amount of 0.1-5.0 wt%, e.g. 0.5-3.0 wt% or 1.0-2.0 wt%, based on the total weight of the composition.
    [0029] In a particular embodiment, the composition further comprises at least one vitamin E or a derivative thereof, such as alpha-tocopheryl acetate. Preferably the at least one vitamin E is present in an amount of 0.05-5.0 wt%, e.g. 0.1-1.0 wt%, based on the total weight of the composition.
    [0030] In a most preferred embodiment, the composition comprises a plurality of vitamin B compounds, vitamin C, and vitamin E. Metal Salt(s)
    [0031] In a particular embodiment, the composition comprises at least one organic metal salt, preferably wherein the metal is selected from Zn, Fe, Cu, and Mg.
    [0032] In a particular embodiment, the composition of the invention comprises an organic iron salt, e.g. ferrous fumarate, preferably in an amount of 0.05-5.0 wt% of Fe, e.g. 0.1-1.0 wt% of Fe, based on the total weight of the composition. The addition of iron can be beneficial as iron deficiency has been identified as a cause of hair loss.
    [0033] In a further particular embodiment, the invention comprises at least two, preferably at least three organic metal salts selected from Zn, Fe, Cu and Mg salts. Suitable salts include zinc gluconate, ferrous fumarate, and copper gluconate.
    [0034] As a source of magnesium, it is preferred if the composition contains magnesium hydroxide carbonate.
    [0035] Preferably, the composition comprises metal salts of Zn, Fe, Cu and/or Mg, in a total amount of 0.5-10 wt%, e.g. 1-5 wt% based on the weight of metal ion(s) with respect to the total weight of the composition.
    [0036] In a further embodiment, the composition comprises a Se compound (i.e. a source of selenium). Preferably, the composition comprises 0.0001-0.01 wt% Se based on the total weight of the composition. Preferably, the Se compound is L-Selenomethionine. Amino acids and other compounds
    [0037] The composition of the invention comprises cysteine or a derivative thereof. This is preferably L-cysteine or an L-cysteine derivative such as L-cysteine HCI monohydrate. The cysteine is preferably present in an amount of 0.1-10 wt%, e.g. 0.2-5.0 wt% or 0.5-3.0 wt%, based on the total weight of the composition.
    [0038] The composition of the invention comprises lysine or a derivative thereof. This is preferably L-Lysine or an L-lysine salt such as L-lysine monohydrochloride. The lysine is preferably present in an amount of 1-20 wt%, e.g. 2-15 wt% or 5-12 wt%, based on the total weight of the composition.
    [0039] The composition of the invention comprises procyanidin or a derivative thereof. This is preferably procyanidin B-2, such as procyanidin B-2 extracted from apples. The procyanidin is preferably present in an amount of 0.5-15 wt%, e.g. 1-10 wt% or 2-8 wt%, based on the total weight of the composition.
    [0040] The composition of the invention comprises a xanthonoid. This is preferably a natural xanthonoid such as mangostin (i.e. mangosteen extract). The xanthonoid is preferably present in an amount of 0.1-10 wt%, e.g. 0.2-5.0 wt% or 0.5-3.0 wt%, based on the total weight of the composition.
    [0041] The composition of the invention comprises methionine or a derivative thereof. This is preferably L-methionine. The methionine is preferably present in an amount of 0.1-5 wt%, e.g. 0.2-3.0 wt% or 0.5-2.0 wt%, based on the total weight of the composition. Collagen
    [0042] The composition of the invention requires a carrier which is preferably collagen, typically hydrolysed collagen. Preferably, the collagen is the most abundant component of the composition. Typically, the collagen is present in at least 20 wt%, e.g. at least 30 wt%, 40 wt% or 50 wt%, based on the total weight of the composition. Preferably, the collagen is present in an amount of 30-90 wt%, e.g. 40-80 wt%, 50-70 wt%, or 55-65 wt%, based on the total weight of the composition. The reference herein to 'collagen' also encompasses a mixture of two or more collagens. Thus, for example, if two different collagens are present, the amounts described above are for the mixture of collagen.
    [0043] In a particular embodiment, the collagen is from fish. In a further embodiment, the collagen is Derapro-100 collagen. Further Additives
    [0044] The composition of the invention typically comprises further additives selected from chlorophyll (e.g. E144ii), silicon dioxide (e.g. E551), flavourings (e.g. natural extract flavourings), citric acid anhydrous, sucralose, or inulin. These further additives are preferably present in a total amount of 1.0-15 wt%, based on the total weight of the composition, e.g. 5.0-10 wt% based on the total weight of the composition. Composition
    [0045] Typically, in the composition of the invention, the sum of components i)-vi) makes up 5-50 wt% of the composition, such as 10-30 wt% of the composition.
    [0046] In a further embodiment, the sum of components i)-vii) makes up 60-90 wt% of the composition, such as 65-85 wt%, e.g. 70-80 wt%.
    [0047] In a particular embodiment, the composition comprises: i) at least one vitamin B compound; ii) cysteine or a derivative thereof; iii) lysine or a derivative thereof; iv) procyanidin B-2; v) mangosteen extract; vi) methionine or a derivative thereof; vii) collagen; viii) ascorbic acid.
    [0048] In a particular embodiment, the composition comprises: i) at least two vitamin B compounds; ii) cysteine or a derivative thereof; iii) lysine or a derivative thereof; iv) procyanidin B-2; v) mangosteen extract; vi) methionine or a derivative thereof; vii) collagen; viii) ascorbic acid ix) vitamin E.
    [0049] In a particular embodiment, the composition comprises: i) at least 4 vitamin B compounds; ii) cysteine or a derivative thereof; iii) lysine or a derivative thereof; iv) procyanidin B-2; v) mangosteen extract; vi) methionine or a derivative thereof; vii) collagen; viii) ascorbic acid; and ix) vitamin E.
    [0050] In a particular embodiment, the composition comprises: Ascorbic acid Vitamin E (e.g. DL-alpha tocopheryl acetate) Riboflavin D-Biotin An organic Zn salt (e.g. zinc glutonate) A selenium source (e.g. L-selenmethionine) Cysteine or a derivative thereof (e.g. L-cysteine HCI monohydrate) Lysine or a derivative thereof (e.g. L-lysine monohydrochloride) Procyanidin or a derivative thereof (e.g. Procyanidin B-2 fraction extracted from apples) A Xanthonoid (e.g. Mangosteen extract) Methionine or a derivative thereof (e.g. L-methionine) Collagen (preferably hydrolysed collagen, e.g. Derapro 100 collagen).
    [0051] In a further particular embodiment, the invention comprises: Ascorbic acid Vitamin E (e.g. DL-alpha tocopheryl acetate) Riboflavin D-Biotin An organic Zn salt (e.g. zinc glutonate) An organic Fe salt (e.g. zinc glutonate) A selenium source (e.g. L-selenmethionine) Cysteine or a derivative thereof (e.g. L-cysteine HCI monohydrate) Lysine or a derivative thereof (e.g. L-lysine monohydrochloride) Procyanidin or a derivative thereof (e.g. Procyanidin B-2 fraction extracted from apples) A Xanthonoid (e.g. Mangosteen extract) Methionine or a derivative thereof (e.g. L-methionine) Collagen (preferably hydrolysed collagen, e.g. Derapro 100 collagen).
    [0052] In a particular embodiment, the composition comprises: Beta carotene Ascorbic acid Vitamin E (e.g. DL-alpha tocopheryl acetate) Thiamine hydrochloride Riboflavin Nicotinamide D-calcium pantothenate Pyridoxine hydrochloride Cyanocobalamin D-Biotin Folic acid Zinc glutonate Ferrous fumarate Copper gluconate L-selenmethionine Magnesium hydroxide carbonate Cysteine (e.g. L-cysteine HCL monohydrate) Lysine (e.g. L-lysine monohydrochloride) Procyanidin (e.g. Procyanidin B-2 fraction extracted from apples) Xanthonoid (e.g. Mangosteen extract) Methionine (e.g. L-methionine) Collagen (preferably hydrolysed collagen, e.g. Derapro 100 collagen).
    [0053] In a further embodiment, the invention further comprises chlorophyll, silicon dioxide, natural flavourings, citric acid anhydrous, sucralose and/or inulin. Uses
    [0054] The composition of the present invention is for use in the prevention or treatment of hair loss. The hair loss can be caused by alopecia areata, cancer treatment (e.g. chemotherapy), iron deficiency, a medication side-effect, or weight loss. The compounds of the invention can be used for clinical causes of hair loss as described above, or non-clinical causes, e.g. male-pattern hair loss (MPHL) and female-pattern hair loss (FPHL).
    [0055] Essentially the composition of the invention is for retarding hair loss or facilitating hair growth/regrowth, in particular on the human scalp, by using a non-invasive, cost-efficient treatment with few or no side effects.
    [0056] The composition is typically ingested daily. It may therefore be suitable for oral administration, e.g. tablet, capsule and so on. In a particular embodiment, the composition is in the form of a powder. Such a powder can be mixed with water for drinking. In a particular embodiment, the composition is to be taken at a dose of 2-10 g/day, e.g. 4-8 g/day. Example 1
    [0057] The following composition was prepared: Input (of raw ingredient) / mg wt% Active part / mg Beta carotene, 20% 27 0.45 Beta carotene 4.5 Ascorbic acid powder 95.61 1.58 Vit C 75 DL-alpha tocopheryl acetate 50% 46.95 0.78 Vit E 15 Thiamine hydrochloride 1.794 0.03 Vit B1 1.2 Riboflavin 1.572 0.03 Vit B2 1.4 Nicotinamide 17.69 0.30 Vit B3 16 D-calcium pantothenate 9.054 0.15 Vit B5 7.5 Pyridoxine hydrochloride 2.856 0.05 Vit B6 2.1 Cyanocobalamin (vit B12, 1.0%) 0.63 0.01 Vit B12 0.0045 D-Biotin 0.144 >0.01 Biotin 0.11 Folic acid 0.138 >0.01 Vit B9 0.1 Zinc glutonate 103 1.72 Zn 12 Ferrous fumarate 83.08 1.3 Fe 27 Copper gluconate 8.31 0.13 Cu 1 L-selenmethionine 10.3 0.05 Se 0.05 Magnesium hydroxide DC E.P. 397.73 6.63 Mg 150 L-cysteine HCL monohydrate 144.93 2.4 L-cysteine 100 L-lysine monohydrochloride 625 10.41 L-lysine 500 Procyanidin B-2 fraction extracted from apples 300 5.0 300 Mangosteen extract 100 1.67 100 L-methionine 50.77 0.85 L-methionine 50 Chlorphyll E144ii 4.212 0.07 Chlorophyll 4 silicon dioxide E551 51.55 0.85 Silics 50 Derapro 100 collagen 3500 58 Collagen 3500 Natural strawberry flavour 120 2.0 Natural vanilla extract flavour 60 1.0 Citric acid anhydrous 6 0.1 sucralose 6 0.1 inulin 225.68 3.75TOTAL 6000 mg 100 Example 2
    [0058] A 15 yr old patient suffering from alopecia areata was treated with the composition of example 1. Her hair growth returned to normal.
    权利要求:
    Claims (15)
    [0001] A composition comprising
    i) at least one vitamin B compound;
    ii) cysteine or a derivative thereof;
    iii) lysine or a derivative thereof;
    iv) procyanidin or a derivative thereof;
    v) a xanthonoid;
    vi) methionine or a derivative thereof; and
    vii) collagen;or any pharmaceutically acceptable salts or esters thereof.
    [0002] A composition as claimed in claim 1, wherein the composition comprises at least Riboflavin (vitamin B2) and Biotin (vitamin B7), or any pharmaceutically acceptable salts or esters thereof, as vitamin B compounds.
    [0003] A composition as claimed in claim 1 or 2, wherein the composition comprises two or more different vitamin B compounds, preferably selected from riboflavin, biotin, thiamine, nicotinamide, pantothenate, pyridoxine, cyanocobalamin and/or folic acid, and any combination thereof.
    [0004] A composition as claimed in any preceding claim wherein the composition further comprises at least one, preferably all, of the following: vitamin C, vitamin E (e.g. DL-alpha tocopheryl acetate), zinc gluconate, and a selenium source (e.g. L-selenmethionine).
    [0005] A composition as claimed in any preceding claim, wherein one or more of the following requirements applies:ii) is L-cysteine, iii) is L-lysine, and/or vi) is L-methionine, or any pharmaceutically acceptable salts or esters thereof, and in any combination thereof.
    [0006] A composition as claimed in any preceding claim, wherein
    i) comprises at least riboflavin and D-biotin, preferably i) comprises thiamine hydrochloride, riboflavin, nicotinamide, D-calcium pantothenate, pyridoxine hydrochloride, cyanocobalamin, D-Biotin and folic acid;
    ii) is L-cysteine HCI monohydrate;
    iii) is L-lysine monohydrochloride;
    iv) is Procyanidin B-2 fraction extracted from apple;
    v) is mangostin;
    vi) is L-methionine; and/or
    vii) is hydrolysed collagen from fish,or any combinations thereof.
    [0007] A composition as claimed in any preceding claim, wherein collagen component vii) is present in an amount of 40-80 wt%, preferably 50-70 wt%, based on the total weight of the composition.
    [0008] A composition as claimed in any preceding claim, wherein the sum of components i)-vi) makes up 5-50 wt% of the composition, such as 10-30 wt% of the composition.
    [0009] A composition as claimed in any preceding claim wherein the sum of components i)-xii) makes up 60-90 wt% of the composition, such as 65-85 wt%, e.g. 70-80 wt%.
    [0010] A composition as claimed in any preceding claim, wherein said composition is in powder form.
    [0011] The use of a composition as claimed in claims 1-10 as a hair regrowth product.
    [0012] A composition as claimed in claims 1-10 for use in the treatment or prevention of hair loss.
    [0013] A composition for use as claimed in claim 12 wherein the hair loss is caused by alopecia areata, cancer treatment (such as chemotherapy), iron deficiency, a medication side-effect, or weight loss.
    [0014] A composition for use as claimed in claim 12, comprising administering the composition to a human at a dosage of 2-10 g/day, such as 4-8 g/day.
    [0015] A method for enhancing hair growth or hair regrowth in a human in need thereof comprising administering a composition as claimed in claims 1-10.
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    GB2581369A|2020-08-19|
    GB201902054D0|2019-04-03|
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