WO2018064985A1 - 一种富勒烯及其衍生物在制备促进毛发生长产品中的应用 - Google Patents
一种富勒烯及其衍生物在制备促进毛发生长产品中的应用 Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/44—Elemental carbon, e.g. charcoal, carbon black
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/58—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
Definitions
- the invention also requires a Chinese patent submitted by the Chinese Patent Office on December 14, 2016, the application number CN201611155549.3, and the invention name is "a composition against the head infection, itching prevention and its preparation method and application" Priority of the application, the entire contents of which are incorporated herein by reference.
- the present invention also claims priority to Chinese Patent Application No. 201611155550.6, entitled “A Composition for the Treatment of Seborrheic Alopecia", filed on December 14, 2016, to the Chinese Patent Office, the entire contents of which is incorporated by reference. In the present invention.
- the invention belongs to the field of biomedicine, and particularly relates to the application of fullerene and its derivatives in preparing products for promoting hair growth.
- fullerenes Since its discovery in 1985, fullerenes have received much attention due to their special physical and chemical properties. In recent years, fullerene molecules and their derivatives, complexes, and inclusion complexes have been found to have excellent physiological activities such as antioxidant activity, antibacterial activity, and anticancer activity. Among many water-soluble fullerenes, attention has been paid to the excellent physiological activity and stability of fullerol (C60(OH)n). A number of methods for the preparation of fullerol have also been developed including: 1. Tetrabutylammonium hydroxide (TBAH) catalyzed alkaline synthesis (J. Chem. Soc. Chem.
- Alopecia is a common clinical onset of hair. With the improvement of living standards, people's requirements for beauty and hairdressing are becoming more and more urgent. The research of modern medicine and traditional medicine has received more and more attention. Hair loss, although not a serious disease, has a greater impact on people's mental and psychological. At present, the common clinical hair loss is as follows: 1. Androgenetic alopecia (AGA) has a family history and is an androgen-dependent hereditary offense. The pathological feature is that the proportion of hair follicles in the growing period and the resting period is from normal. :1 is reduced to 5:1, the hair follicles are gradually reduced and the hair follicle density is reduced from 326 cm 2 of normal adults to 278 cm 2 .
- AGA Androgenetic alopecia
- alopecia areata is a functional disease that can occur in any part of the body of localized plaque alopecia, nervous system disorders are important factors.
- 3 seborrheic alopecia is also known as early baldness, the main pathogenesis and genetic, male hormone, seborrhea and other related. Due to excessive secretion of oil in the head, the hair is greasy, which causes the scalp to be damp and greasy. The dust in the air is mixed with dandruff. It is dirty and does not smell when it is not washed for a few days.
- the patent CN200910071736 discloses a traditional Chinese medicine composition for treating hair loss, including Shuai, Angelica, Chuanxiong, Atractylodes, Night vine, Ligustrum lucidum, Cuscuta, Spatholobus, Shouwu, Jijinjin, Hawthorn meat, and Xianling.
- CN201310347018 discloses a traditional Chinese medicine composition for treating hair loss, which comprises 15 kinds of raw materials, Rehmannia glutinosa, Polygonum, Radix Rehmanniae, Hawthorn, Eclipta, Yam, Arborvitae, Ginseng, Codonopsis, Poria, Mudanpi, Alisma, and Zhi. Mother, earth bones, silver Bupleurum.
- Patent 201610482648 discloses a re-starting nourishing dew and a preparation method thereof, which can improve hair loss and improve hair by extracting active ingredients from a mixture of hops, mulberry, Polygonum multiflorum, Corydalis, saffron, and peony bark according to a reasonable ratio. The role of quality.
- CN201510025222 An anti-hair loss shampooing hair care composition comprising Saw Palmetto extract and Lemongrass as a main component, the composition effectively preventing or reducing hair loss.
- the above patents have a slow onset of action and are prone to recurrence after stopping the administration. Can not completely solve the problem of hair loss patients.
- the topical topical drug minoxidil which is approved by the FDA for external treatment of androgenetic alopecia, can effectively inhibit hair loss and promote hair regeneration.
- the current method for treating hair loss in minoxidil has slow onset and side effects.
- the hair growth promoting product is at least one of a hair follicle vascular endothelial cell growth factor promoter, a hair growth agent, a hair conditioner, a gettering agent, and a hair growth agent.
- the hair growth promoting product is any one of a combination of an oil form of an fullerene and a derivative thereof, an aqueous solution, and a composition of a traditional Chinese medicine.
- One embodiment of the present invention the use of the fullerene of the present invention and its derivatives for promoting hair growth.
- the fullerene and its derivatives of the present invention are capable of promoting the expression of vascular endothelial growth factor in the hair follicle of the head.
- the fullerene and its derivatives of the present invention are capable of treating hair loss caused by a decrease in hair follicle vascular endothelial growth factor.
- the fullerene and its derivatives of the invention can up-regulate the vascular endothelial growth factor VEGF content of hair follicles, especially the hair follicle vascular endothelial growth factor VEGFR-2 content.
- the hair loss according to the present invention includes androgenetic alopecia, alopecia areata, seborrheic alopecia, and androgenetic alopecia and alopecia areata.
- the fullerene derivative of the present invention is a water-soluble fullerene derivative including a hydroxyl fullerene, an amino fullerene, a hollow fullerol, and/or a metal fullerol.
- the water-soluble fullerene derivative is an amino fullerene
- amino fullerene is prepared by the following method:
- One of the solid fullerenes includes hollow fullerene C 2n , metal fullerene M@C 2n , M 2 @C 2n , MA@C 2n , M 3 N@C 2n , M 2 C 2 @C 2n , At least one of M 2 S@C 2n , M 2 O@C 2n and M x A 3-x N@C 2n , wherein M and A are independently selected from the group consisting of Sc, Y and lanthanide metal elements, 30 ⁇ n ⁇ 60, 0 ⁇ x ⁇ 3;
- step (b) spin drying the solution obtained in the step (a), and dissolving the remaining solid after spin drying with a dilute acid solution
- the dilute acid solution is a mineral acid solution, and the concentration of the dilute acid solution is 0.5 to 1.5 mmol/L;
- step (c) adjusting the pH of the solution obtained in step (b) is 4 to 6, and dialysis to a solution having a conductivity of less than 1 ⁇ s/cm;
- step (d) treating the solution obtained in the step (c) with an anion exchange resin, and dialysis to a solution having a conductivity of less than 1 ⁇ s/cm.
- the water-soluble fullerene derivative is a hydroxyl fullerene obtained by mixing a solid fullerene with a hydrogen peroxide solution and an alkali solution.
- a hydroxyl fullerene obtained by mixing a solid fullerene with a hydrogen peroxide solution and an alkali solution.
- hydroxyfullerene is prepared by the following method:
- the solid fullerene is mixed with a hydrogen peroxide solution and an alkali solution, wherein the alkali solution comprises at least one of an aqueous sodium hydroxide solution, an aqueous potassium hydroxide solution, and an aqueous tetrabutylammonium hydroxide solution, and the solid fullerene includes a hollow fullerene.
- M and A are independently selected from the group consisting of Sc, Y and a lanthanide metal element, 30 ⁇ n ⁇ 60, 0 ⁇ x ⁇ 3; in the alkali solution
- the content of the base is 8 to 15% by weight; based on the total mass of the hydrogen peroxide solution, the content of hydrogen peroxide in the hydrogen peroxide solution is 20 to 40% by weight; the hydrogen peroxide and the hydrogen in the mixed solution
- the volume ratio of the alkali solution is 7: (1 to 4); the reaction is carried out under heating and stirring treatment, the heating temperature of the heating and stirring treatment is 50 to 80 degrees Celsius, and the stirring rate is 600 to 1500 rpm/min.
- the preparation of the hydroxyfullerene is obtained by the following method:
- the solution obtained in the step (b) is subjected to dialysis treatment, and the dialysis to the solution has a conductivity of less than 1 ⁇ s/cm;
- the water-soluble fullerene derivative is a hollow fullerol and/or a metal fullerol; the bulk material of the hollow fullerol is C 2n ; the bulk material of the metal fullerol Is any one of M@C 2n , M2@C 2n and MA@C 2n , wherein M and A are both metal elements, and both M and A are selected from any of Sc, Y and lanthanide metal elements.
- M and A are both metal elements, and both M and A are selected from any of Sc, Y and lanthanide metal elements.
- the hollow body material Fuller alcohol may be C 60; fullerenols bulk material of the metal may be Gd @ C 82.
- the hydroxyl group in the hollow fullerol and/or metal fullerol may be from 15 to 35, specifically 22.
- Fuller said hollow alcohol and / or a metal hydroxy fullerenols merely modified, e.g., C 60 (OH) 22.
- the main direction of hair follicle research is the mutual regulation of hair follicles, involving multiple genes, growth factors, morphogenetic family and signaling pathways such as transforming growth factor (TGF), fibroblast growth factor (FGF)/Wnt pathway. , BMP family, and epidermal growth factor, vascular endothelial growth factor, stem cell growth factor and the like. These families and factors are composed of corresponding receptors, ligands, cytoplasmic endoplasms, and nuclear transcription factors.
- TGF transforming growth factor
- FGF fibroblast growth factor
- BMP family and epidermal growth factor
- vascular endothelial growth factor vascular endothelial growth factor
- stem cell growth factor and the like.
- VEGF vascular endothelial growth factor
- VEGF family members are classified into VEGFR-1, VEGFR-2 and VGEGFR-3 by binding to vascular endothelial cell-specific VEGF receptor-mediated microvascular proliferation, enhanced vascular permeability and endothelial cell proliferation. Proliferation of VEGF in endothelial cells is mainly mediated by VEGFR-2. Since VEGF is only expressed in the hair follicles during the growth phase, VEGF expression in the hair follicles of androgenetic alopecia and alopecia areata is weakened or even disappeared.
- Another embodiment of the present invention the use of the fullerene of the present invention and its derivatives in the preparation of a hair growth promoting product.
- the hair growth promoting product is an aqueous solution of the water-soluble fullerene derivative hollow fullerol and/or metal fullerol.
- the aqueous solution of the water-soluble fullerene derivative may have a mass concentration of 100 to 10,000 ppm, specifically 800 to 1500 ppm, 800 ppm, 1000 ppm or 1500 ppm.
- the hair growth promoting product of the present invention is a hair follicle vascular endothelial cell growth factor promoter comprising a combination of fullerene and oil, ie, fullerene oil, aqueous solution of amino fullerene, One or more of aqueous solutions of hydroxyfullerene.
- the promoter of the invention can promote the expression of vascular endothelial growth factor in the hair follicle of the hair follicle; up-regulate the vascular endothelial growth factor VEGF content of the hair follicle, especially the hair follicle vascular endothelial growth factor VEGFR-2, thereby treating the hair follicle vascular endothelial growth factor Hair loss caused by the decline.
- a method for using a hair follicle vascular endothelial growth factor promoting agent of the present invention fullerene oil can be used for application, and aqueous solution of amino fullerene and aqueous solution of hydroxyfullerene can be used for application or oral administration.
- fullerene oil wherein the fullerene is present in the fullerene oil at a concentration of 0.01 to 20 mg/ml; further preferably The fullerene concentration in the fullerene oil is 0.1 mg/mL to 15 mg/mL; further preferably, the fullerene concentration in the fullerene oil is 1-10 mg/ml.
- the fullerene in the fullerene oil of the present invention is a hollow fullerene and/or a metal fullerene.
- the oil includes, but is not limited to, extracts of plant seeds, flowers, rhizomes, etc., such as olive oil, soybean oil, linseed oil, green thorn oil, rapeseed oil, sweet almond oil, sunflower oil, safflower oil , grape seed oil, evening primrose oil, borage seed oil, angelica oil, ginger oil, jojoba oil, walnut oil, avocado oil, mango oil, castor oil, almond oil, shea butter, rose hip oil , coconut oil, palm oil, gluten oil, wheat germ oil, calendula oil, aloe oil, palm oil, sweet almond oil, corn oil, grape seed oil, etc.; or a mixture of one or more; further preferably fullerene oil For fullereene olive oil.
- extracts of plant seeds, flowers, rhizomes, etc. such as olive oil, soybean oil, linseed oil, green thorn oil, rapeseed oil, sweet almond oil, sunflower oil, safflower oil , grape seed oil,
- the fullerene powder is ball-milled and refined by 0.05-1 ⁇ m, and the refined fullerene powder is mixed with oil, placed in a ball mill at 500-1000 rpm, and ball milled for 8-20 hours to obtain Fuller.
- the olefin oil suspension is heated to 40-60 ° C, and protected by nitrogen. After stirring for 12-72 hours, it is centrifuged and filtered to obtain a fullerene oil solution.
- the fullerene powder is ball milled and refined to 0.05-1 ⁇ m, thoroughly mixed with the oil, and then placed in a ball mill at 500-700 rpm, ball milled for 6-10 h to obtain a fullerene oil suspension, and then mixed.
- the suspension is heated to 40-50 ° C for ultrasonic and nitrogen protection, and stirred and heated for 10-15 h to fully dissolve the fullerenes in the oil, and centrifuged and filtered to obtain fullerene oil.
- the head hair follicle vascular endothelial growth factor promoting agent of the invention can be used for one of the active ingredients of health care products or medicines or foods or skin care products or hair products, and is composed of a pharmaceutically acceptable carrier or a traditional Chinese medicine extract.
- the dosage is 0.01-99.99%.
- the hair growth promoting product of the present invention is a composition for preventing head infection, antipruritic and destabilizing; the composition can not only eliminate itching and dandruff, but also treat bacterial infection. Sexual alopecia promotes hair loss in patients.
- a composition for combating head infection, anti-itch and anti-de-stabilization which is composed of the following weight
- the raw materials are: 10-500 parts of linseed oil, 10-500 parts of sea buckthorn oil, 10-500 parts of camellia oil, 10-500 parts of juniper oil, 10-500 parts of geranium oil, 30-500 parts of menthol, 1-400 parts of licorice extract, 1-400 parts of jujube extract, 1-400 parts of peony bark extract, 1-400 parts of pan pomegranate extract, 1-400 parts of Centella asiatica extract, and extract of Ligusticum chuanxiong Hort.
- the composition is resistant to head infection, itching and de-stabilization, which is prepared from the following raw materials by weight: 50-400 parts of linseed oil, 50-400 parts of sea buckthorn oil, camellia oil 50-400 parts, 50-400 parts of juniper oil, 50-400 parts of geranium oil, 50-400 parts of menthol, 5-200 parts of licorice extract, 5-200 parts of jujube extract, and 5-200 pieces of peony bark extract 5 parts, Pan Pomegranate extract 5-200 parts, Centella asiatica extract 5-200 parts, Chuanxiong extract 5-200 parts, black tea extract 5-200 parts, plant sterol 5-100 parts, pepper extract 0.5- 100 parts, 5-100 parts of glutinous rice extract, 5-100 parts of ginger extract, 5-100 parts of aloe extract, 5-100 parts of hop extract, 5-100 parts of Eclipta extract, Angelica extract 5 -100 parts, 5-100 parts of Ginkgo biloba extract, 5-100 parts of Noni extract, 5-100
- the composition is resistant to head infection, itching and de-stabilization, which is prepared from the following raw materials by weight: linseed oil 100-300 parts, sea buckthorn oil 100-300 parts, camellia oil 100-300 parts, 100-300 parts of juniper oil, 100-300 parts of geranium oil, 70-200 parts of menthol, 10-100 parts of licorice extract, 10-100 parts of jujube extract, 10-100 pieces of peony bark extract 10 parts of Pan Pomegranate extract, 10-100 parts of Centella asiatica extract, 10-100 parts of Chuanxiong extract, 10-100 parts of black tea extract, 10-50 parts of plant sterol, and 0.5- of pepper extract 10 parts, 10-50 parts of glutinous rice extract, 10-50 parts of ginger extract, 10-50 parts of aloe extract, 10-50 parts of hop extract, 10-50 parts of Eclipta extract, Angelica extract 10 -50 parts, 10-50 parts of Ginkgo biloba extract, 10-50 parts of Noni extract, 5-20 parts
- a composition for combating head infection, anti-itch and anti-de-stabilization which is prepared from the following raw materials by weight: 150-250 parts of linseed oil, 150-250 parts of sea buckthorn oil, mountain tea 150-250 parts of oil, 130-180 parts of juniper oil, 150-250 parts of geranium oil, 100-150 parts of menthol, 20-70 parts of licorice extract, 20-70 parts of jujube extract, 20-70 parts of peony bark extract 70 parts, Pan pomegranate extract 20-70 parts, Centella asiatica extract 20-70 parts, 20-70 parts of Ligusticum chuanxiong Hort., 20-70 parts of black tea extract, 20-40 parts of phytosterol, 0.5-2 parts of pepper extract, 10-50 parts of glutinous rice extract, ginger extract 10-50 parts, aloe extract 10-50 parts, hop extract 10-50 parts, Eclipta prostrata extract 10-50 parts, angelica extract 10-50 parts, ginkgo extract 10
- the best composition is a composition for combating head infection, anti-itch and anti-de-stabilization, which is prepared from the following raw materials by weight: 200 parts of linseed oil, 200 parts of sea buckthorn oil, 200 parts of camellia oil, and 150 parts of pine oil, 150 parts of geranium oil, 100 parts of menthol, 50 parts of licorice extract, 70 parts of jujube extract, 50 parts of peony bark extract, 50 parts of pan pomegranate extract, 40 parts of Centella asiatica extract, Sichuan 50 parts of alfalfa extract, 50 parts of black tea extract, 30 parts of phytosterol, 0.7 parts of capsicum extract, 30 parts of glutinous rice extract, 20 parts of ginger extract, 30 parts of aloe extract, 30 parts of hop extract, and ink dry 30 parts of lotus extract, 40 parts of angelica extract, 30 parts of ginkgo extract, 30 parts of noni extract, 10 parts of oat dextran, 40 parts of inositol, 30
- the antipruritic anti-debonding hair-generating composition of the present invention and a pharmaceutically acceptable carrier are in an acceptable dosage form.
- the pharmaceutically acceptable carrier may be from 0.1 to 99.9% by weight based on the total weight of the formulation.
- the pharmaceutical compositions are in the form of a pharmaceutically acceptable preparation. Medicinal preparations are tablets, capsules, granules, pills, powders, ointments, suspensions, injections, powders, suppositories, creams, drops, or patches.
- the tablet is a sugar-coated tablet, a film-coated tablet, an enteric-coated tablet or a sustained-release tablet;
- the capsule is a hard capsule, a soft capsule, a sustained release capsule;
- the powder injection is Freeze-dried powder injection.
- the pharmaceutically acceptable carrier is selected from the group consisting of: mannitol, sorbitol, sorbic acid or potassium salt, sodium metabisulfite, sodium hydrogen sulfite, sodium thiosulfate, cysteine hydrochloride, thioglycolic acid, methionine, vitamin A, Vitamin C, vitamin E, vitamin D, azone, EDTA disodium, EDTA calcium sodium, monovalent alkali metal carbonate, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulfuric acid, phosphoric acid, amino acid, chlorine Sodium, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivatives, cellulose and its derivatives, alginate, Gelatin, polyvinylpyrrolidone, glycerin, propylene glycol,
- composition of the present invention as a preparation form, an effective amount of the inventive compound contained in each dose is 0.1 to 1000 mg, and each dose means each preparation unit, such as each tablet of a tablet, each capsule, May also mean each time Take a dose, such as taking 100mg each time. While the amount of active ingredient contained in the dosage unit form can vary, it will generally be in the range of from 1 to 1000 mg, depending on the potency of the active ingredient selected.
- compositions of the Invention In the preparation of solid or semisolid pharmaceutical preparations in the form of powders, tablets, dispersible powders, capsules, capsules, suppositories and ointments, solid carriers can be employed.
- the solid carrier which can be used is preferably one or more selected from the group consisting of a diluent, a flavoring agent, a solubilizing agent, a lubricant, a suspending agent, a binder, a swelling agent and the like, or may be an encapsulating substance.
- 5 to 70% of the micronized active ingredient is contained in the carrier.
- Suitable solid carriers include magnesium carbonate, magnesium stearate, talc, sucrose, lactose, pectin, dextrin, starch, gelatin, methylcellulose, sodium carboxymethylcellulose, low boiling waxes, cocoa butter, and the like. Because of their ease of administration, tablets, powders, cachets, and capsules represent the most advantageous oral solid preparations.
- Liquid preparations of the invention include solutions, suspensions and emulsions.
- an injection preparation for parenteral administration may be in the form of water or a water-propylene glycol solution, adjusting its isotonicity, pH, etc. to suit physiological conditions of a living body.
- Liquid preparations can also be prepared in the form of solutions in polyethylene glycol, aqueous solutions.
- An oral aqueous solution can be prepared by dissolving the active ingredient in water, followed by the addition of a suitable amount of coloring, flavoring, stabilizing and thickening agents.
- the micronized active ingredient can be dispersed in viscous materials such as natural and synthetic gums, methylcellulose, sodium carboxymethylcellulose, and other known suspending agents to prepare aqueous suspensions suitable for oral administration.
- Dosage unit form of the formulation refers to physically discrete units suitable as a single dose, each unit containing a calculated predetermined amount of active ingredient that produces the desired therapeutic effect.
- Such dosage unit forms can be in the form of a package such as a tablet, a capsule or a powder in a vial or vial, or an ointment, gel or cream in a tube or vial.
- a component of the composition may be separated and mixed with the adjuvant according to the formulation process requirements.
- water-soluble components such as licorice extract, jujube extract, peony bark extract, pan pomegranate extract, centella asiatica extract, Chuanxiong extract, black tea extract, plant sterol, Capsicum extract, glutinous rice extract, ginger extract, aloe extract, hop extract, Eclipta extract, Angelica extract, Ginkgo biloba extract, Noni extract, oat glucan, inositol, biotin It is added to the aqueous phase, and linseed oil, sea buckthorn oil, camellia oil, thyme oil, juniper oil, geranium oil, menthol, tocopheryl acetate, fullerene, and the like are added to the oil phase.
- Preferred dosage forms of the invention are emulsions, sprays, compositions and excipients by weight ratio (1-5): (5-10).
- One embodiment of the present invention preferably comprises an emulsion prepared from an anti-itching anti-debonding hair-generating composition, water, and an emulsifier.
- the emulsifiers described above include, but are not limited to, the formation of an emulsion requiring mechanical force and the other to be adapted.
- An emulsifier comprising a natural emulsifier, a synthetic emulsifier, and a solid powder emulsifier.
- the natural emulsifiers include, but are not limited to, gum arabic, tragacanth, glycerin, soybean phospholipid, gelatin, egg yolk, agar, sodium alginate, chalk, pectin, foot, cholesterol, and the like.
- the synthetic emulsifier includes, but is not limited to, sodium lauryl sulfate, sodium cetyl sulfate, cetyl alcohol, cetyltrimethylammonium bromide or tetradecyltrimethylammonium bromide, Tween, Division Disc, cellulose and its derivatives, methyl cellulose carboxymethyl cellulose, and the like.
- the solid powder emulsifier includes, but is not limited to, diatomaceous earth, magnesium hydroxide, aluminum hydroxide, silica, alumina, kaolin, calcium hydroxide, zinc hydroxide, magnesium stearate, and the like.
- the invention provides a method for preparing an anti-head infection, anti-itch anti-de-solidification hair-curing agent, comprising the following steps:
- One embodiment of the present invention is preferably a spray prepared from an anti-itching anti-debonding hair-generating composition, water, and a solubilizing agent. The specific steps are:
- the present invention preferably comprises licorice extract, jujube extract, peony bark extract, pan pomegranate extract, centella asiatica extract, Chuanxiong extract, black tea extract, plant sterol, chili
- the extract, the glutinous rice extract, the ginger extract, the aloe extract, the hop extract, the Eclipta prostrata extract, the angelica extract, the ginkgo extract, and the noni extract are respectively water extracts, for example, water decoction.
- the linseed oil high in unsaturated fatty acid, has excellent affinity and penetration to the skin, and the various fatty acids contained therein are easily absorbed by the skin, and are used to replenish the lipid components required for the skin, anti-inflammatory and anti-proliferative. It has a good effect on alleviating erythema and inflammatory reactions caused by ultraviolet rays, and has obvious effects on the treatment of skin allergies and eczema.
- the seabuckthorn oil the anti-inflammatory effect of the volatile oil compound, promotes capillary blood circulation, and the phospholipid compound such as lecithin in seabuckthorn is a biologically active component, which promotes cell metabolism, is a multivitamin and biological activity.
- a complex of matter it nourishes the skin, promotes metabolism, anti-allergy, bactericidal and anti-inflammatory, promotes epithelial cell regeneration, repairs the skin, maintains the acidic environment of the skin, and has strong permeability.
- the camellia oil activating blood circulation to remove phlegm, treating eczema, and treating skin lice.
- the juniper oil the helper of oily congested skin, can also improve the sebum of the scalp, purifying characteristics can improve acne, pore blockage, dermatitis, epidemic eczema, dryness.
- the geranium oil balances sebum secretion and can treat eczema and skin lice.
- the menthol has the effects of reducing inflammation, relieving pain, cooling and relieving itching.
- the licorice extract tonifying spleen and replenishing qi, clearing away heat and detoxifying, and absorbing ultraviolet rays.
- the jujube extract is rich in protein, fat, sugar, carotene, B vitamins, vitamin C, vitamin P, and nutrients such as calcium, phosphorus, iron and cyclic adenosine monophosphate.
- the peony bark extract analgesic, hemostasis, antibacterial, dandruff, itching, conditioning hair, moisturizing, soft, bright, and promote hair growth.
- the guava extract treats skin eczema, itching, enthusiasm, and is rich in various vitamins and trace elements.
- the Centella asiatica extract antibacterial and anti-inflammatory, treating herpes zoster caused by viruses or bacteria, promoting blood circulation and removing blood stasis.
- the Angelica extract Angelica essential oil, hematopoiesis, anti-oxidation, scavenging free radicals, anti-inflammatory analgesia.
- the noni extract noni fruit powder, can activate cells and nourish the brain.
- the Eclipta prostrata extract water extract, improve cellular immunity and humoral immunity, nourish liver and kidney, cool blood to stop bleeding.
- the sage extract sage essential oil calms tension, improves headaches and migraine, and relieves anxiety.
- the saw palmetto extract water extract, effectively inhibits 5a-reductase activity, reduces dihydrotestosterone production and antagonizes the binding of androgen to androgen receptor in prostate tissue, and promotes liver and kidney.
- the hop extract Jianweixiaoshi, soothe the diuretic, and effectively inhibit 5a-reductase activity.
- the fullerene is a hollow fullerene and/or a fullerene derivative.
- the hollow fullerene comprises one or more of C 60 , C 70 , C 76 , C 84 , preferably C 60 or C 70 or a mixture of C 60 and C 70 ; the fullerene derivative includes but not It is limited to C 60 -(OH)n, C 70 -(OH)n, C 60 -(COOH)n, C 70 -(COOH)n (n is 4-30).
- the Chuanxiong extract has the functions of activating blood circulation, relieving phlegm and relieving pain.
- the black tea extract has the functions of antibacterial and anti-inflammatory, can be used for scavenging free radicals, and can inhibit viruses.
- the phytosterol has a strong anti-inflammatory effect, can inhibit the absorption of cholesterol, and promote the degradation of cholesterol.
- the pepper extract has anti-inflammatory analgesic, cold and dampness.
- the glutinous rice extract has an anti-inflammatory effect and inhibits the occurrence of edema and inflammation.
- the ginger extract contains 6-gingerol active ingredient, has anti-inflammatory and anti-oxidation effects, and treatment of hair follicles with 6-gingerol can cause apoptosis of hair follicle dermal papilla cells, thereby inhibiting hair growth.
- the aloe extract moisturizing effect, smooth hair, can reduce the production of dander.
- Seborrheic alopecia is mostly associated with excessive accumulation of androgen in the scalp.
- Eclipta prostrata, sage, saw palmetto and hop are sebum regulating agents, and can inhibit 5a-reductase activity and alleviate seborrheic alopecia. Seborrheic alopecia is often accompanied by severe dermatitis.
- Flaxseed oil, sea buckthorn oil, camellia oil, juniper oil, geranium oil and peppermint oil have antibacterial, anti-inflammatory and soothing effects on the skin.
- the nutrition comes from blood, the liver is the main blood, rooted in the kidney, the kidney is the main bone, and its glory is in the hair, so the production and shedding, and the rise and fall of the kidney and liver
- the stagnation is closely related, so the extract of peony bark in the group is the yin and yin, and the guava, centella, chuanxiong and angelica extracts are the medicines, and the effect of qi and blood is supplemented.
- Ginger and Noni are the adjuvants.
- Fullerene is a long-acting antioxidant, a free radical scavenger, which is compounded with a variety of essential oil extracts to stabilize the active ingredients of essential oils. It also removes free radicals from the scalp and activates hair follicles.
- the dosage form of the invention can be used quantitatively according to the needs of the patient.
- Patients with hair loss should use clean before using this product.
- Towels are cleaned on the scalp, and the scalp is heat-treated with a clean hot towel for 20-30 minutes (temperature control is about 40 °C).
- the hot hole can open the pores to facilitate the penetration of the drug, and use the fingers to pick up a small amount of hair products for hair loss.
- the part is evenly massaged, and the hair loss part is cleaned with water after a certain period of time. Every morning and evening, after 7-15 days, the original hair loss part will have different degrees of new hair growth.
- the hair growth promoting product of the present invention is a composition for treating seborrheic alopecia, which is capable of treating not only baldness but also seborrheic dermatitis alopecia, especially Androgen-dependent hereditary offense is effective.
- the present invention provides a composition for treating seborrheic alopecia, which is prepared from the following raw materials by weight: 0.1-5 parts of peony bark extract, 0.1-5 parts of arborvitae leaf extract, rosemary extract 0.1 -5 parts, 0.1-5 parts of tea tree extract, 0.1-5 parts of angelica extract, 0.1-5 parts of Astragalus membranaceus extract, 0.1-5 parts of Eclipta prostrata extract, 0.01-2 parts of sage extract, saw palmetto Extract 0.01-2 parts, hop extract 0.01-2 parts, Noni extract 0.01-2 parts, biotin 0.01-0.05 parts, inositol 0.1-2 parts, hydrolyzed wheat protein 0.1-1 parts, oat glucan 0.1-1 part, 0.1-5 parts of zinc gluconate, 0.1-5 parts of peppermint, 0.01-1 part of biophenol phenol acetate, 0.001-10 parts of fullerene and its corresponding derivatives.
- a composition for treating seborrheic alopecia is prepared from the following raw materials by weight: peony bark extract 0.3-3 parts, arborvitae leaf extract 0.3-3 parts, rosemary extract 0.2 -3 parts, 0.1-3 parts of tea tree extract, 0.2-2 parts of angelica extract, 0.2-2 parts of Astragalus membranaceus extract, 0.2-2 parts of Eclipta prostrata extract, 0.1-2 parts of sage extract, saw palmetto Extract 0.05-1.5 parts, hop extract 0.05-1.5 parts, Noni extract 0.1-1 part, biotin 0.01-0.03 parts, inositol 0.1-1 part, hydrolyzed wheat protein 0.1-0.5 part, oat dextran 0.1-0.5 parts, 0.5-3 parts of zinc gluconate, 1-3 parts of peppermint, 0.03-0.06 parts of tocopheryl acetate, 0.01-5 parts of fullerenes and their corresponding derivatives.
- a composition for treating seborrheic alopecia is prepared from the following raw materials by weight: peony bark extract 0.3-2.5 parts, arborvitae leaf extract 0.3-2.5 parts, rosemary extract 0.2-2.5 parts, 0.1-2 parts of tea tree extract, 0.2-1.5 parts of angelica extract, 0.2-1.5 parts of Astragalus membranaceus extract, 0.2-1.5 parts of Eclipta prostrata extract, 0.1-1.5 parts of sage extract, saw Palm extract 0.08-1.5 parts, hop extract 0.08-1.5 parts, Noni extract 0.08-1 parts, biotin 0.01-0.03 parts, inositol 0.1-0.5 parts, hydrolysis Wheat protein 0.2-0.4 parts, oat dextran 0.2-0.4 parts, zinc gluconate 2-3 parts, peppermint 1-3 parts, tocopheryl acetate 0.03-0.06 parts, fullerenes and their corresponding derivatives 0.01- 2 servings.
- a composition for treating seborrheic alopecia is prepared from the following raw materials by weight: 0.5-2 parts of peony bark extract, 0.5-2 parts of arborvitae leaf extract, rosemary extract 0.5-2 parts, 0.3-1 part of tea tree extract, 0.3-1 part of angelica extract, 0.3-1 part of Astragalus membranaceus extract, 0.3-1 part of Eclipta extract, 0.3-1 part of sage extract, saw 0.1-1 part of palm extract, 0.1-1 part of hop extract, 0.5-1 part of Noni extract, 0.01 part of biotin, 0.1 part of inositol, 0.3 part of hydrolyzed wheat protein, 0.3 part of oat dextran, gluconic acid 1 part zinc, 2 parts mint, 0.05 part biophenol phenol acetate, 0.03-0.6 parts of fullerene and its corresponding derivatives.
- a composition for treating seborrheic alopecia is prepared from the following raw materials by weight: 1 part of peony bark extract, 1 part of arborvitae leaf extract, 1 part of rosemary extract, tea tree 1 part extract, 1 part of angelica extract, 1 part of Astragalus membranaceus extract, 1 part of Eclipta prostrata extract, 1 part of sage extract, 0.3 part of Saw palmetto extract, 0.7 part of hop extract, Nori extract 0.8 parts, 0.01 parts of biotin, 0.1 part of inositol, 0.3 parts of hydrolyzed wheat protein, 0.3 parts of oat dextran, 1 part of zinc gluconate, 2 parts of menthol, 0.05 part of biophenol phenol acetate, fullerene and corresponding 0.01 parts of the derivative.
- compositions for treating seborrheic alopecia and a pharmaceutically acceptable carrier in an acceptable dosage form.
- a unit dose of the medicament may contain 0.1 to 1000 mg of the pharmaceutically active substance of the present invention, and the balance is a pharmaceutically acceptable carrier.
- the pharmaceutically acceptable carrier may be from 0.1 to 99.9% by weight based on the total weight of the formulation.
- composition for treating hair loss of the present invention preferably in the form of a unit dose of a pharmaceutical preparation, can be formulated into any pharmaceutically acceptable dosage form when formulated into a pharmaceutical preparation.
- the composition of the present invention is an external dosage form such as a gel, an ointment, an emulsion, a dressing, a plaster or the like.
- composition of the present invention may be added with some pharmaceutically acceptable carriers as needed, and the pharmaceutical preparation may be prepared by conventional techniques such as mixing the pharmaceutically active substance with a pharmaceutically acceptable carrier.
- the pharmaceutically acceptable carrier is selected from the group consisting of: mannitol, sorbitol, sorbic acid or potassium salt, sodium metabisulfite, sodium hydrogen sulfite, sodium thiosulfate, cysteine hydrochloride, thioglycolic acid, methionine, vitamin A, Vitamin C, vitamin E, vitamin D, azone, EDTA disodium, EDTA calcium sodium, monovalent alkali metal carbonate, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulfuric acid, phosphoric acid, amino acid, chlorine Sodium, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mann
- the dosage form of the invention is a hydrogel having a composition to substrate weight ratio (1-5): (5-10), preferably 3-5:5-7.
- the substrate includes 1,3-butanediol, methyl cellulose, hydroxyethyl cellulose, citric acid, hyaluronic acid, LRI (PPG-26 butanol-26, PEG-40 hydrogenated castor oil) , EDTA-2Na, carbomer, gum arabic, benzoin, agar, dextrin, gelatin, pectin, sodium alginate, polyacrylic acid, polyvinyl alcohol, sodium hyaluronate one or more.
- LRI PPG-26 butanol-26, PEG-40 hydrogenated castor oil
- the present invention relates to a seborrheic alopecia hydrogel preparation
- a seborrheic alopecia hydrogel preparation comprising the following raw materials in parts by weight: 0.1-5 parts of peony bark extract, 0.1-5 parts of arborvitae leaf extract, rosemary extract 0.1-5 a portion, 0.1-5 parts of tea tree extract, 0.1-5 parts of angelica extract, 0.1-5 parts of astragalus extract, 0.1-5 parts of Eclipta prostrata extract, 0.01-2 parts of sage extract, saw palmetto extract 0.01-2 parts, hop extract 0.01-2 parts, Noni extract 0.01-2 parts, biotin 0.01-0.05 parts, inositol 0.1-2 parts, hydrolyzed wheat protein 0.1-1 parts, oat dextran 0.1- 1 part, 0.1-5 parts of zinc gluconate, 0.1-5 parts of peppermint, 0.01-1 part of biophenol phenol acetate, 0.001-10 parts of fullerene and its corresponding derivatives, 0.1% of 1,3-
- the present invention treats a seborrheic alopecia hydrogel preparation comprising the following raw materials by weight: 0.3-3 parts of peony bark extract, 0.3-3 parts of arborvitae leaf extract, rosemary extract 0.2- 3 parts, 0.1-3 parts of tea tree extract, 0.2-2 parts of angelica extract, 0.2-2 parts of Astragalus membranaceus extract, 0.2-2 parts of Eclipta prostrata extract, 0.1-2 parts of sage extract, saw palmetto extract 0.05-1.5 parts, hop extract 0.05-1.5 parts, Noni extract 0.1-1 part, biotin 0.01-0.03 parts, inositol 0.1-1 part, hydrolyzed wheat protein 0.1-0.5 part, oat dextran 0.1 -0.5 parts, 0.5-3 parts of zinc gluconate, 1-3 parts of peppermint, 0.03-0.06 parts of tocopheryl acetate, 0.01-2 parts of fullerenes and their corresponding derivatives, 0.1% of 1,3-butanediol -10 parts,
- the present invention treats a hair loss gelling agent comprising the following raw materials in parts by weight: 0.5-2 parts of peony bark extract, 0.5-2 parts of arborvitae leaf extract, rosemary extract 0.5- 2 parts, 0.3-1 part of tea tree extract, 0.3-1 part of angelica extract, 0.3-1 part of Astragalus membranaceus extract, 0.3-1 part of Eclipta extract, and sage 0.3-1 parts of extract, 0.1-1 part of saw palmetto extract, 0.1-1 part of hop extract, 0.5-1 part of Noni extract, 0.01 part of biotin, 0.1 part of inositol, 0.3 part of hydrolyzed wheat protein, oatmeal 0.3 parts of dextran, 1 part of zinc gluconate, 2 parts of menthol, 0.05 part of biophenol phenol acetate, and 0.03-0.6 parts of fullerene and its corresponding derivatives.
- a hair loss gelling agent comprising the following raw materials in parts by weight: 0.5-2 parts of peony bark extract, 0.5-2 parts
- a method for preparing a seborrheic alopecia composition according to the present invention comprises the following steps:
- step (2) adding fullerenes and their corresponding derivatives to the mixed extract of step (1), adding tocopherol acetate and menthol to obtain a fullerene mixture, and then solubilizing with a solubilizing agent, fully solubilizing After that, leave it overnight, filter, and take the supernatant I for use;
- the fullerene and its derivative described above in the above step (2) can be dissolved in the mixed extract of the step (1), and it is preferred that the mixed extract is a fat-soluble component.
- the solubilizer is LRI (PPG-26 butanol-26, PEG-40 hydrogenated castor oil).
- the invention also provides a gel for treating hair loss, comprising the following steps:
- the peony bark extract, the oriental arborvitae leaf extract, the rosemary extract, the tea tree extract, the angelica extract, the Eclipta extract, the sage extract, Saw palmetto extract, hop extract, noni extract, peppermint extract, biotin, inositol, hydrolyzed wheat protein, oat dextran, zinc gluconate, tocopheryl acetate are all prepared by the prior art or Market purchase.
- the oriental arborvitae leaf extract In order to better exert the beneficial effects of the present invention, it is preferable to include the oriental arborvitae leaf extract, the oriental arborvitae leaf extract, the rosemary extract, the tea tree extract, the angelica extract, and the sage extract respectively as the volatile oil component, that is, the side.
- Tar rosemary essential oil, tea tree oil, angelica essential oil, sage essential oil, scutellaria essential oil.
- the peony bark extract, the Eclipta extract, the saw palmetto extract, the hop extract, and the noni extract are respectively water extracts, such as water-frying Cooking liquid.
- the combination of Chinese and Western medicine theory is adopted, and the scientific and rational combination of the components is combined with the gel dosage form which is beneficial to the full effect of the composition to realize effective treatment for seborrheic alopecia.
- the peony bark extract water extract, has anti-inflammatory effect, antibacterial, anti-inflammatory, anti-oxidation, anti-dandruff, itching.
- the Angelica extract Angelica essential oil, hematopoiesis, anti-oxidation, scavenging free radicals, anti-inflammatory analgesia.
- the extract of Astragalus membranaceus essential oil of scutellaria, qi and solid table, diuretic toxic, pus, and sore muscle.
- the noni extract noni fruit powder, can activate cells and nourish the brain.
- the arborvitae leaf extract tar tar can reduce dandruff, relieve skin inflammation, eczema, mold infection, regulate scalp greasy secretion, reduce hair loss.
- the rosemary extract rosemary essential oil has a strong astringent effect, regulates greasy and unclean skin, and promotes blood circulation.
- the Eclipta prostrata extract water extract, improve cellular immunity and humoral immunity, nourish liver and kidney, cool blood to stop bleeding.
- the sage extract sage essential oil calms tension, improves headaches and migraine, and relieves anxiety.
- the saw palmetto extract water extract, effectively inhibits 5a-reductase activity, reduces dihydrotestosterone production and antagonizes the binding of androgen to androgen receptor in prostate tissue, and promotes liver and kidney.
- the hop extract Jianweixiaoshi, soothe the diuretic, and effectively inhibit 5a-reductase activity.
- the tea tree extract tea tree oil, acne anti-inflammatory, oil control convergence, inhibition of bacteria, strengthen immunity.
- the fullerene is a hollow fullerene and/or a fullerene derivative; the hollow fullerene comprises one or more of C 60 , C 70 , C 76 , C 84 , preferably C 60 or C 70 Or a mixture of C 60 and C 70 ; the fullerene derivatives include, but are not limited to, C 60 -(OH)n, C 70 -(OH)n, C 60 -(COOH)n, C 70 -(COOH ) n, (n is 4-30).
- Seborrheic alopecia mostly related to excessive accumulation of androgen in the scalp, rosemary, Eclipta, sage, saw palmetto, hops are sebum regulators, and can inhibit 5a-reductase activity very well To relieve seborrheic alopecia. Seborrheic alopecia is often accompanied by severe dermatitis. Tea tree oil and peppermint oil have antibacterial, anti-inflammatory and soothing effects on the skin.
- the nutrition comes from blood
- the liver is the main blood
- the kidney is the main bone
- its glory is in the hair
- the production and shedding and the rise and fall of the kidney and liver
- the drip is closely related, so the extract of Platycladus orientalis in the prescription is the medicinal yin and yin, the peony bark, the scutellaria extract, the angelica extract are the medicinal herbs, the qi and blood is added, and the noni is the adjuvant to strengthen the anti-inflammatory and antibacterial The effect of activating cells.
- the addition of fullerenes enhances the effect of the anti-inflammatory activated cells of the composition on the activation of hair follicles.
- Fullerenes are long-acting antioxidants, free radical scavengers, and complexed with a variety of essential oil extracts to stabilize essential oils.
- the ingredients also remove free radicals from the scalp and activate the hair follicles.
- the side through the qi and blood circulation combined with sebum regulating ingredients, and a long-acting free radical scavenger, to ensure the stability of the active ingredients, and thus ensure the efficacy.
- the dosage form of the invention can be used quantitatively according to the needs of the patient.
- patients with hair loss should clean the scalp with a clean towel, then apply a hot towel to the scalp for 20-30 minutes (temperature control is about 40 °C).
- the hot hole can make the pores open for the penetration of drugs.
- the water-soluble fullerene derivative used in the present invention is a hollow fullerol or a metal fullerol, which can effectively activate hair follicles for treating hair loss, can achieve the purpose of rapid hair growth; at the same time, can grow The hair is brighter, firmer and stronger.
- the invention solves the problem that some commercialized hair water has a long period in the process of treating hair loss, and the effect is obvious after two weeks of administration, and the purpose of rapid hair growth is achieved.
- fullerene olive oil, amino fullerene, hydroxy fullerene can effectively promote the expression of VEGFR-2 in the hair follicles of the head, thereby promoting hair growth, treating hair loss, safe and effective, no side effects, not easy relapse.
- alopecia areata, seborrheic alopecia more obvious.
- a composition for treating seborrheic alopecia which is capable of treating not only baldness but also seborrheic dermatitis alopecia, especially for androgen-dependent hereditary episodes.
- the composition not only eliminates itching and dandruff, but also treats bacterial infective hair loss and promotes hair loss in patients.
- the products of the fullerene and the fullerene derivative thereof of the present invention can be rapidly produced, and have obvious hair growth effects after one week of use.
- Figure 1 shows an amino fullerene infrared absorption spectrum of Example 1 and Example 2 of the aminofullerene according to the present invention
- Example 2 shows an amino fullerene electron beam probe of Example 1 and Example 2 of the amino fullerene according to the present invention. Analysis result
- Figure 3 shows the amino fullerene hydrated particle size (Figure 3a) and zeta potential ( Figure 3b) of Example 1 and Example 2 of the aminofullerene according to the present invention
- Figure 4 shows the infrared absorption spectrum of C 60 (O) 5 (OH) 12 prepared according to the hydroxy fullerene of the present invention
- Figure 5 is a graph showing the X-ray photoelectron spectroscopy C1s peak fitting curve of C 60 (O) 5 (OH) 12 prepared according to the hydroxy fullerene of the present invention
- Figure 6 shows the hydrated particle size (Figure 6a) and zeta potential (Figure 6b) of C 60 (O) 5 (OH) 12 prepared according to the present invention for hydroxyfullerene Example 1.
- Fig. 7 is a graph showing the growth of the back hair of the mouse in the test hair growth of the aqueous solution of fullerol; wherein, Figs. 7A, 7B, 7C and 7D are photographs before use of the drugs of Figs. 7E, 7F, 7G and 7H, respectively. 7E, 7F, and 7G are photographs of hair growth when the concentrations of fullerol are 800 ppm, 1000 ppm, and 1500 ppm, respectively, and Fig. 7H is a photograph of hair growth when physiological saline is used.
- Fig. 8 is a graph showing the results of histological evaluation of the number of mouse hair follicles of H&E staining in Test Example 1, wherein Fig. 8A, Fig. 8B, Fig. 8C, and Fig. 8D are respectively used when physiological saline is used, and the concentrations of fullerol are 800 ppm, 1000 ppm, and 1500 ppm, respectively. the result of.
- Figure 9 is a graph showing the VEGFR-2 content of the C 60 - olive oil group Western Blot according to the test example of the present invention.
- FIG 10 is a C 60 Test Example Two of the present invention - olive oil group detected by RT-PCR VEGFR-2 content map, wherein the A: C 60 - Olive Oil; B: Olive Oil; C: Minoxidil; D: Saline.
- Figure 11 is a graph showing the content of mouse VEGFR-2, Western Blot, of the test example diaminofullerene according to the present invention.
- Figure 12 is a graph showing the content of mouse VEGFR-2 of diamino fullerene according to the present invention, RT-PCR.
- Figure A Aminofullerene; B minoxidil; C; physiological saline.
- Figure 13 is a graph showing the content of mouse VEGFR-2, Western Blot, of the test dihydroxy fullerene according to the present invention.
- Figure 14 is a graph showing the content of mouse VEGFR-2 of dihydroxy fullerene according to the present invention, RT-PCR.
- Figure A hydroxyfullerene
- C physiological saline.
- Figure 15 is a photograph of H&E staining of back samples of mice in seven groups of experiments according to the third test example of the present invention, showing the condition of hair follicles in the back fur of mice of different experimental groups a) blank group, b) the present patent composition, c Pure purulene group, d) plant extract (without fullerenes), e) minoxidil, f) normal saline, g) model group (not administered).
- Figure 16 is a H&E staining picture of a back case of mice in seven experimental experiments according to the present invention, wherein a) blank group, b) the patented composition, c) pure fullerene group, d) plant extract ( Does not contain fullerenes), e) minoxidil, f) saline, g) model group (no administration).
- Figure 17 is a statistical graph of germinal development after trial use in different age groups.
- the fullerene powder C 70 was ball-milled and refined to 0.05-1 ⁇ m, and then 1 g of the refined fullerene powder was mixed with 20 g of soybean oil, placed in a ball mill at 500 rpm, and ball-milled for 8 hours to obtain fullerene oil.
- the suspension was heated to 40 ° C, and protected with nitrogen. After stirring for 12 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- the fullerene powder C 60 was ball-milled and refined to 0.05-1 ⁇ m, and 5 g of the refined fullerene powder was mixed with 100 g of soybean oil, placed in a ball mill at 700 rpm, and ball-milled for 12 hours to obtain fullerene oil.
- the suspension was heated to 50 ° C, and protected with nitrogen. After stirring for 24 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- the fullerene powder C 76 was ball-milled and refined to 0.05-1 ⁇ m, and the refined fullerene powder 0.1 was mixed with 10 g of green thorn fruit oil, placed in a ball mill at 1000 rpm, and ball-milled for 20 hours to obtain Fuller.
- the olefin oil suspension was heated to 60 ° C, and protected with nitrogen. After stirring for 36 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- the fullerene powder Gd@C 82 is ball milled and refined to 0.05-1 ⁇ m, and 10 g of the refined fullerene powder is mixed with 40 g of olive oil, placed in a ball mill at 500-1000 rpm, and ball milled for 8-20 h.
- a fullerene oil suspension is obtained, and the fullerene oil suspension is heated to 40-60 ° C, protected with nitrogen, stirred for 12-72 hours, centrifuged, and filtered to obtain a fullerene oil solution.
- fullerene powder was ball milled 0.05-1 refinement, then the fullerene powder was mixed with 3g refined olive oil 30g, placed in a ball mill for 500 revolutions / minute, 80h ball milling, to give an oil fullerene
- the suspension was heated to 40 ° C, and protected with nitrogen. After stirring for 12 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- the fullerene powder C 70 was ball-milled and refined to 0.05-1 ⁇ m, and then 3 g of the refined fullerene powder was mixed with 30 g of olive oil, placed in a ball mill at 500 rpm, and ball-milled for 80 hours to obtain fullerene oil.
- the suspension was heated to 40 ° C, and protected with nitrogen. After stirring for 12 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- the fullerene powder C 76 was ball-milled and refined to 0.05-1 ⁇ m, and then 3 g of the refined fullerene powder was mixed with 20 g of olive oil, placed in a ball mill at 500 rpm, and ball-milled for 80 hours to obtain fullerene oil.
- the suspension was heated to 40 ° C, and protected with nitrogen. After stirring for 12 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- the fullerene powder C 60 was ball-milled and refined to 0.05-1 ⁇ m, and 5 g of the refined fullerene powder was mixed with 25 g of olive oil, placed in a ball mill at 500 rpm, and ball-milled for 80 hours to obtain fullerene oil.
- the suspension was heated to 40 ° C, and protected with nitrogen. After stirring for 12 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- Fullerene powder C 70 was ball-milled and refined to 0.05-1 ⁇ m, and 1 g of the refined fullerene powder was mixed with 15 g of olive oil, placed in a ball mill at 500 rpm, and ball-milled for 80 hours to obtain fullerene oil.
- the suspension was heated to 40 ° C, and protected with nitrogen. After stirring for 12 hours, it was centrifuged and filtered to obtain a fullerene oil solution.
- step (b) Add the solution obtained in step (a) to a 250 ml round bottom flask and use a rotary evaporator (Model: IKA) RV10 basic) The filtrate was spin-dried completely (temperature: 70 ° C, rotation speed: 80 r/min). Diluted hydrochloric acid (concentration: 1 mol/L) was placed in a round bottom flask, and the flask was shaken to dissolve the dried product on the inner wall in dilute hydrochloric acid to obtain a brown-red clear solution.
- Diluted hydrochloric acid concentration: 1 mol/L
- step (c) The solution obtained in the step (b) is neutralized with a pH test paper using an aqueous NaOH solution (concentration: 10 mol/L) to be weakly acidic (pH is about 5) to ensure that excess ethylenediamine exists as a chloride salt. It can be sufficiently removed in the subsequent dialysis step.
- the neutralized solution was placed in a dialysis bag (cutoff molecular weight: 3,500) and dialyzed in ultrapure water, and the conductivity of the dialysis to ultrapure water was less than 1 ⁇ s/cm.
- the brown-red solution was dropped on a silver mirror and naturally dried for infrared spectroscopy (IR) testing.
- IR infrared spectroscopy
- the infrared characteristic absorption of the sample at around 3300 nm proves that the ethylene diamine is bonded to the fullerene carbon cage while the infrared characteristic absorption at 800-1500 nm (carbon cage)
- the sample solution was dropped on an electron probe station to which a carbon conductive paste was adhered, and dried for electron beam probe analysis (EPMA). The test results are shown in Fig.
- Example 2 The reaction conditions and procedures were the same as in Example 1, except that 50 mg of metal fullerene Gd@C 82 solid (purity: 99%, Xiamen Funa New Material Technology Co., Ltd.) was used instead of C 60 . A clear brownish black solution containing Gd@C 82 (EDA) 8 was finally obtained.
- the obtained product was subjected to component detection by the same test method and conditions as in Example 1. As shown in Fig. 1, the infrared characteristic absorption (-NH 2 stretching vibration absorption peak) of the sample at about 3300 nm proved that ethylenediamine was bonded.
- the hydrated particle size was about 100 nm and the surface was positively charged, which was suitable for cell capture and phagocytosis.
- the sample was freeze-dried for CHN elemental analysis (EA), and two positions were randomly selected in the sample.
- EA CHN elemental analysis
- the analysis results are shown in Table 2.
- the concentration of the sample in the solution can be determined by measuring the Gd 3+ ion concentration in the sample by inductively coupled plasma atomic emission spectroscopy (ICP-AES) (the sample is treated with concentrated nitric acid and the Gd acid in the sample is decomposed into Gd 3+ ions).
- ICP-AES inductively coupled plasma atomic emission spectroscopy
- reaction conditions and procedures were the same as in Example 1, except that 50 mg of Y@C 82 , Ho@C 82 or Lu@C 82 solid (purity: 99%, Xiamen Funa New Material Technology Co., Ltd.) was used instead of C 60 .
- reaction conditions and procedures are the same as in Example 1, except that 50 mg of Sc 3 N@C 80 , Y 3 N@C 80 or Lu 3 N@C 80 solid (purity: 99%, Xiamen Funa New Material Technology Co., Ltd.) is used. Company) replaces C 60 .
- step (b) The solution obtained in the step (a) is added to a 50 ml centrifuge tube, and an excess of 95% ethanol (analytical grade, Sinopharm reagent) is added. After centrifugation (rotation speed: 10000 r/min, time: 4 min), the upper colorless solution was removed, and the collected precipitate was dissolved in ultrapure water to obtain a yellow clear solution.
- 95% ethanol analytical grade, Sinopharm reagent
- step (c) The solution obtained in the step (b) was placed in a dialysis bag (cutoff molecular weight: 3,500) and dialyzed in ultrapure water, and the conductivity of the dialysis to ultrapure water was less than 1 ⁇ s/cm to obtain a yellow solution.
- step (d) The solution after the dialysis in step (c) is placed in a 50 mL plastic centrifuge tube, frozen in liquid nitrogen, and placed in a freeze dryer to freeze-dry (temperature: -29 ° C, vacuum: 55 Pa, time: 48 h). The resulting yellow solid was placed in a brown vial for later use.
- IR infrared spectroscopy
- the solid sample was directly used for X-ray photoelectron spectroscopy.
- the photoelectron spectroscopy of the C element in the sample was subjected to peak fitting.
- the peak of 285.91eV belongs to CO
- the chemical composition of the sample is C60(O) 5 (OH) 12 .
- the sample solution was directly used for dynamic light scattering (DLS) test. As shown in Fig.
- the sample had a hydrated particle size of about 145 nm and a negatively charged surface, which was stably present in the aqueous solution for a long period of time.
- a solid sample was used for CHN elemental analysis (EA) and two random positions (1# and 2#) in the sample were taken for elemental analysis. The results are shown in Table 3.
- the hydroxyl group-modified C60 in the sample can be quantified according to the C content in Table 3.
- the preparation method and preparation conditions were the same as those in Example 1, except that in the step (a), C 60 , C 76 , C 78 and C 84 were used instead of C 60 .
- step (a) The preparation method and preparation conditions were the same as those in Example 1. The difference is that in step (a), Y@C 82 , Ho@C 82 , and Lu@C 82 are used instead of C 60 .
- step (a) is, respectively Y 3 N @ C 82, Sc 3 N @ C 82, and Lu 3 N @ C 82 alternative C 60.
- a composition against head infection, anti-itch and anti-de-stabilization occurs from linseed oil 200g, sea buckthorn oil 200g, camellia oil 200g, juniper oil 150g, geranium oil g, menthol 100g, licorice extract 50g, Jujube extract 70g, peony bark extract 50g, pan pomegranate extract 50g, Centella asiatica extract 40g, Chuanxiong extract 50g, black tea extract 50g, plant sterol 30g, pepper extract 0.7g, glutinous rice extract 30g Ginger extract 20g, aloe extract 30g, hop extract 30g, Eclipta extract 30g, Angelica extract 40g, Ginkgo biloba extract 30g, Noni extract 30g, oat glucan 10g, inositol 40g, fertility 30 g of phenol acetate, 0.7 g of biotin, and 15 g of fullerene.
- a solubilizing agent is added to the oil phase, and after sufficiently stirring so that the oil phase is completely solubilized, the aqueous phase is added thereto, and the mixture is uniformly mixed to obtain the composition of the present invention.
- the invention relates to a composition for combating head infection, anti-itch and anti-de-solidification, which is prepared from the following raw materials by weight: flaxseed oil 500g, sea buckthorn oil 500g, camellia oil 500g, juniper oil 500g, geranium 500g 500 ml of menthol, 400 g of licorice extract, 400 g of jujube extract, 400 g of peony bark extract, 400 g of pan pomegranate extract, 400 g of Centella asiatica extract, 400 g of Rhizoma Chuanxiong extract, 400 g of black tea extract, 200 g of phytosterol, and pepper 200 g of extract, 200 g of glutinous rice extract, 200 g of ginger extract, 200 g of aloe extract, 200 g of hop extract, 200 g of Eclipta prostrata extract, 200 g of angelica extract, 200 g of ginkgo extract, 200 g of noni extract, oats 200 g of
- the invention relates to a composition for combating head infection, anti-itch and anti-de-stabilization, which is prepared from the following raw materials by weight: linseed oil 10 g, sea buckthorn oil 10 g, camellia oil 10 g, juniper oil 10 g, geranium oil 10 g, menthol 30 g, licorice extract 1 g, jujube extract 1 g, peony bark extract 1 g, pan pomegranate extract 1 g, centella asiatica extract 1 g, Chuanxiong extract 1 g, black tea extract 1 g, phytosterol 1 g, Capsicum extract 0.1g, glutinous rice extract 1g, ginger extract 1g, aloe extract 1g, hop extract 1g, Eclipta extract 1g, Angelica extract 1g, Ginkgo biloba extract 1g, Noni extract 1g, 1 g of oat dextran, 10 g of inositol, 10 g of tocophe
- the invention relates to a composition for combating head infection, anti-itch and anti-de-stabilization, which is prepared from the following raw materials by weight: linseed oil 50g, sea buckthorn oil 50g, camellia oil 50g, juniper oil 50g, geranium oil 50 g, menthol 50 g, licorice extract 5 g, jujube extract 5-g, peony bark extract 5 g, pan pomegranate extract 5 g, centella asiatica extract 5 g, Chuanxiong extract 5 g, black tea extract 5 g, plant sterol 5 g, capsicum extract 0.5 g, glutinous rice extract 5 g, ginger extract 5 g, aloe extract 5 g, hop extract 5 g, Eclipta prostrata extract 5 g, angelica extract 5 g, ginkgo extract 5 g, noni extract 5 g, oat glucan 5 g, inositol 20 g, tocopheryl
- the invention relates to a composition for combating head infection, anti-itch and anti-de-solidification, which is prepared from the following raw materials by weight: flaxseed oil 400g, sea buckthorn oil 400g, camellia oil 400g, juniper oil 400g, geranium oil 400g, menthol 400 g, licorice extract 200 g, jujube extract 200 g, peony bark extract 200 g, pan pomegranate extract 200 g, centella asiatica extract 200 g, Chuanxiong extract 200 g, black tea extract 200 g, plant sterol 100 g, pepper extract 100 g 100 g of glutinous rice extract, 100 g of ginger extract, 100 g of aloe extract, 100 g of hop extract, 100 g of Eclipta prostrata extract, 100 g of angelica extract, 100 g of ginkgo extract, 100 g of noni extract, 100 g of oat glucan 200 g of inositol, 100
- the invention relates to a composition for combating head infection, anti-itch and anti-de-stabilization, which is prepared from the following raw materials by weight: linseed oil 100g, sea buckthorn oil 100g, camellia oil 100g, juniper oil 100g, geranium oil 100 g, menthol 70 g, licorice extract 10 g, jujube extract 10 g, peony bark extract 10 g, pan pomegranate extract 10 g, centella asiatica extract 10 g, Chuanxiong extract 10 g, black tea extract 10 g, plant sterol 10 g, 10 g of capsicum extract, 10 g of glutinous rice extract, 10 g of ginger extract, 10 g of aloe extract, 10 g of hop extract, 10 g of Eclipta prostrata extract, 10 g of angelica extract, 10 g of ginkgo extract, 10 g of noni extract, oatmeal 5 g of dextran, 30 g of inos
- the invention relates to a composition for combating head infection, anti-itch and anti-de-stabilization, which is prepared from the following raw materials by weight: linseed oil 300g, sea buckthorn oil 300g, camellia oil 300g, juniper oil 300g, geranium oil 300 g, 200 ml of menthol, 100 g of licorice extract, 100 g of jujube extract, 100 g of peony bark extract, 100 g of pan pomegranate extract, 100 g of Centella asiatica extract, 100 g of Rhizoma Chuanxiong extract, 100 g of black tea extract, 50 g of phytosterol, 10 g of capsicum extract, 50 g of glutinous rice extract, 50 g of ginger extract, 50 g of aloe extract, 50 g of hop extract, 50 g of Eclipta prostrata extract, 50 g of angelica extract, 50 g of ginkgo extract, 50 g of noni extract, oatmeal 20
- the invention relates to a composition for combating head infection, anti-itch and anti-de-solidification, which is prepared from the following raw materials by weight: linseed oil 150g, sea buckthorn oil 150g, camellia oil 150g, juniper oil 130g, geranium oil 150 g, menthol 100 g, licorice extract 20 g, jujube extract 20 g, peony bark extract 20 g, pan pomegranate extract 20 g, centella asiatica extract 20 g, Chuanxiong extract 20 g, black tea extract 20 g, plant sterol 20 g, Capsicum extract 0.5g, glutinous rice extract 10g, ginger extract 10g, aloe extract 10g, hop extract 10g, Eclipta extract 10g, Angelica extract 10g, Ginkgo biloba extract 10g, Noni extract 10g, 50 g of oat dextran, 30 g of inositol, 20 g of tocopheryl a
- the invention relates to a composition for combating head infection, anti-itch and anti-de-stabilization, which is prepared from the following raw materials by weight: flaxseed oil 250g, sea buckthorn oil 250g, camellia oil 250g, juniper oil 180g, geranium oil 250 g, menthol 150 g, licorice extract 70 g, jujube extract 70 g, peony bark extract 70 g, pan pomegranate extract 70 g, centella asiatica extract 70 g, Chuanxiong extract 70 g, black tea extract 70 g, plant sterol 40 g, 2 g of capsicum extract, 50 g of glutinous rice extract, 50 g of ginger extract, 50 g of aloe extract, 50 g of hop extract, 50 g of Eclipta prostrata extract, 50 g of angelica extract, 50 g of ginkgo extract, 50 g of noni extract, oatmeal 20 g of dextran, 100 g of inosi
- composition of any of the embodiments 1-9 is formulated into an emulsion comprising the following steps:
- the mixed oil phase is stirred at a temperature of 40 degrees for 1 hour under reduced pressure, so that the components are better dissolved in the oil phase to be an oil phase;
- a composition for treating seborrheic alopecia which is prepared by the following parts by weight:
- Peony skin extract 0.1g arborvitae leaf extract 0.1g, rosemary extract 0.1g, tea tree extract 0.1g, angelica extract 0.1g, astragalus extract 0.1g, Eclipta prostrata extract 0.1g, rat Sage extract 0.01g, saw palmetto extract 0.01g, hop extract 0.01g, Noni extract 0.01g, biotin 0.01g, inositol 0.1g, hydrolyzed wheat protein 0.1g, oat dextran 0.1g, Zinc gluconate 0.1 g, peppermint 0.1 g, biophenol phenol acetate 0.01 g, fullerene and its corresponding derivative 0.001 g.
- step (2) Dissolving fullerenes and their corresponding derivatives in the mixed extract of step (1), adding tocopherol acetate and menthol to obtain a fullerene mixture, and then compatibilizing with a solubilizing agent to fully compatibilize After well, place it overnight, filter, and take the supernatant I for use;
- a composition for treating seborrheic alopecia which is prepared by the following parts by weight:
- Mudan peel extract 5g oriental arborvitae leaf extract 5g, rosemary extract 5g, tea tree extract 5g, angelica extract 5g, astragalus extract 5g, Eclipta prostrata extract 5g, sage extract 2g, saw Palm extract 2g, hop extract 2g, Noni extract 2g, biotin 0.05g, inositol 2g, hydrolyzed wheat protein 1g, oat dextran 1g, zinc gluconate 5g, mint 5g, biophenol acetate 1g , fullerene and its corresponding derivative fullerene 3g.
- step (2) Dissolving fullerenes and their corresponding derivatives in the mixed extract of step (1), adding tocopherol acetate and menthol to obtain a fullerene mixture, and then compatibilizing with a solubilizing agent to fully compatibilize After well, place it overnight, filter, and take the supernatant I for use;
- a composition for treating seborrheic alopecia which is prepared from the following raw materials by weight: 0.3 g of peony bark extract, 0.3 g of arborvitae leaf extract, 0.2 g of rosemary extract, 0.1 g of tea tree extract, Angelica extract 0.2g, Astragalus membranaceus extract 0.2g, Eclipta prostrata extract 0.2g, sage extract 0.1g, Saw palmetto extract 0.05g, hop extract 0.05g, Noni extract 0.1g, biotin 0.01 g, inositol 0.1 g, hydrolyzed wheat protein 0.1 g, oat dextran 0.1 g, zinc gluconate 0.5 g, mint 1 g, tocopheryl acetate 0.03 g, fullerene and its corresponding derivative 0.01 g.
- step (2) Dissolving fullerenes and their corresponding derivatives in the mixed extract of step (1), adding tocopherol acetate and menthol to obtain a fullerene mixture, and then compatibilizing with a solubilizing agent to fully compatibilize After well, place it overnight, filter, and take the supernatant I for use;
- a composition for treating seborrheic alopecia which is prepared from the following raw materials by weight: 3 g of peony bark extract, 3 g of arborvitae leaf extract, 3 g of rosemary extract, 3 g of tea tree extract, 2 g of angelica extract 2, Astragalus membranaceus extract 2g, Eclipta prostrata extract 2g, sage extract 2g, Saw palmetto extract 1.5g, hop extract 1.5g, Noni extract 1g, biotin 0.03g, inositol 1g, hydrolyzed wheat Protein 0.5 g, oat dextran 0.5 g, gluconic acid 3 g, peppermint 3 g, tocopheryl acetate 0.06 g, fullerene and its corresponding derivative 2 g.
- step (2) Dissolving fullerenes and their corresponding derivatives in the mixed extract of step (1), adding tocopherol acetate and menthol to obtain a fullerene mixture, and then compatibilizing with a solubilizing agent to fully compatibilize After well, place it overnight, filter, and take the supernatant I for use;
- a composition for treating seborrheic alopecia which is prepared from the following raw materials by weight: 0.3 g of peony bark extract, 0.3 g of arborvitae leaf extract, 0.2 g of rosemary extract, 0.1 g of tea tree extract, Angelica extract 0.2g, Astragalus membranaceus extract 0.2g, Eclipta prostrata extract 0.2g, sage extract 0.1g, Saw palmetto extract 0.08g, hop extract 0.08g, Noni extract 0.08g, biotin 0.01 g, inositol 0.1 g, hydrolyzed wheat protein 0.2 g, oat dextran 0.2 g, zinc gluconate 2 g, mint 1 g, tocopheryl acetate 0.03 g, fullerene and its corresponding derivative 0.01 g.
- step (2) Dissolving fullerenes and their corresponding derivatives in the mixed extract of step (1), adding tocopherol acetate and menthol to obtain a fullerene mixture, and then compatibilizing with a solubilizing agent to fully compatibilize After well, place it overnight, filter, and take the supernatant I for use;
- a composition for treating seborrheic alopecia is 2.5 g of peony bark extract, 2.5 g of arborvitae leaf extract, 2.5 g of rosemary extract, 2 g of tea tree extract, 1.5 g of angelica extract, and astragalus extract 1.5.
- Eclipta prostrata extract 1.5g is 2.5 g of peony bark extract, 2.5 g of arborvitae leaf extract, 2.5 g of rosemary extract, 2 g of tea tree extract, 1.5 g of angelica extract, and astragalus extract 1.5.
- Eclipta prostrata extract 1.5g is 2.5 g of peony bark extract, 2.5 g of arborvitae leaf extract, 2.5 g of rosemary extract, 2 g of tea tree extract, 1.5 g of angelica extract, and astragalus extract 1.5.
- Eclipta prostrata extract 1.5g is 2.5 g of peony bark extract
- 2.5 g of arborvitae leaf extract 2.5 g of rosemary extract
- 2 g of tea tree extract 1.5 g of angelica extract
- astragalus extract 1.5 is
- a composition for treating seborrheic alopecia is 0.5 g of peony bark extract, 0.5 g of arborvitae leaf extract, 0.5 g of rosemary extract, 0.3 g of tea tree extract, 0.3 g of angelica extract, and astragalus extract.
- Example 1 Eclipta prostrata extract 0.3 g, sage extract 0.3 g, saw palmetto extract 0.1 g, hop extract 0.1 g, noni extract 0.5 g, biotin 0.01 g, inositol 0.1 g, hydrolysis Wheat protein 0.3 g, oat dextran 0.3 g, zinc gluconate 1 g, peppermint 2 g, biophenol phenol acetate 0.05 g, fullerene and its corresponding derivative 0.03 g were prepared according to the method of Example 1.
- a composition for treating seborrheic alopecia is 2 g of peony bark extract, 2 g of arborvitae leaf extract, 2 g of rosemary extract, 1 g of tea tree extract, 1 g of angelica extract, 1 g of astragalus extract, and Eclipta prostrata 1 g of extract, 1 g of sage extract, 1 g of saw palmetto extract, 1 g of hop extract, 1 g of noni extract, 0.01 g of biotin, 0.1 g of inositol, 0.3 g of hydrolyzed wheat protein, 0.3 g of oat dextran Zinc gluconate 1 g, mint 2 g, biophenol phenol acetate 0.05 g, fullerene and its derivative 0.6 g were prepared according to the method of Example 1.
- a hydrogel for treating seborrheic alopecia includes 0.5% of peony skin extract, 0.5% of arborvitae leaf extract, 0.5% of rosemary plant extract, 0.3% of tea plant extract, and 0.3 of angelica plant extract. %, saw palmetto plant extract 0.15%, Eclipta plant extract 0.3%, sage plant extract 0.3%, hop plant extract 0.1%, biotin 0.01%, inositol 0.1%, hydrolyzed wheat protein 0.3% , oat dextran 0.3%, zinc gluconate 1%, 1,3-butanediol 4%, hydroxyethyl cellulose 0.05%, citric acid 0.3%, hyaluronic acid 3%, mint 2%, biophenol B
- the main active materials such as acid ester 0.5%, LRI-80 30%, EDTA-2Na 1%, Tween-80 35%, EDTA-2Na 0.5%, fullerene and its corresponding derivative 6%, are added to deionized water. 100%.
- the invention relates to a method for treating a seborrheic alopecia hydrogel comprising the following components: the formula comprises 0.3% of the plant extract of Shouwu, 0.3% of the extract of peony bark, 0.15% of the plant extract of Platycladus orientalis, and 0.15 of the extract of Astragalus membranaceus.
- Noni plant extract 0.15% Noni plant extract 0.15%, Angelica plant extract 0.15%, saw palmetto plant extract 0.15%, aloe plant extract 0.05%, biotin 0.01%, inositol 0.1%, hydrolyzed wheat protein 0.3%, oats Glycan 0.3%, zinc gluconate 1%, 1,3-butanediol 4%, hydroxyethyl cellulose 0.05%, citric acid 0.3%, hyaluronic acid 3%, mint 2%, biophenol acetate 0.5 %, LRI-80 20%, EDTA-2Na 1%, fullerenes and their corresponding derivatives 4% and other main active materials, 100% of deionized water.
- a hydrogel for treating seborrheic alopecia comprises the following components: 0.5-2 parts of peony bark extract, arborvitae leaves 0.5-2 parts of extract, 0.5-2 parts of rosemary extract, 0.3-1 part of tea tree extract, 0.3-1 part of angelica extract, 0.3-1 part of Astragalus membranaceus extract, 0.3-1 part of Eclipta extract , sage extract 0.3-1 part, saw palmetto extract 0.1-1 part, hop extract 0.1-1 part, noni extract 0.5-1 part, biotin 0.01 part, inositol 0.1 part, hydrolyzed wheat protein 0.3 parts, 0.3 parts of oat dextran, 1 part of zinc gluconate, 2 parts of menthol, 0.05 part of biophenol phenol acetate, and 0.03-0.6 parts of fullerene and its corresponding derivatives.
- a composition for treating seborrheic alopecia which is prepared from the following raw materials by weight: peony bark extract 1 g, arborvitae leaf extract 1 g, rosemary extract 1 g, tea tree extract 1 g, angelica extract 1 g, 1 kg of Astragalus membranaceus extract, 1 g of Eclipta prostrata extract, 1 g of sage extract, 0.3 g of Saw palmetto extract, 0.7 g of hop extract, 0.8 g of Noni extract, 0.01 g of biotin, 0.1 mg of inositol g, hydrolyzed wheat protein 0.3 g, oat dextran 0.3 g, zinc gluconate 1 g, mint 2 g, biophenol phenol acetate 0.05 g, fullerene and its corresponding derivative 0.01 g, the preparation method is as in Example 1.
- a composition for treating seborrheic alopecia which is prepared from the following parts by weight: peony bark extract 5g, arborvitae leaf extract 5g, rosemary extract 5g, tea tree extract 5g, angelica extract 5g 5g of Astragalus membranaceus L., 5g of Eclipta prostrata extract, 2g of sage extract, 2g of Saw Palmetto extract, 2g of hop extract, 2g of Noni extract, 0.05g of biotin, 2g of inositol, 1g of hydrolyzed wheat protein , oat glucan 1 g, zinc gluconate 5 g, mint 5 g, biophenol phenol acetate 1 g, fullerenes and their corresponding derivatization 10 g, the preparation method is as in Example 1.
- a composition for treating seborrheic alopecia is 2.5 g of peony bark extract, 2.5 g of arborvitae leaf extract, 2.5 g of rosemary extract, 2 g of tea tree extract, 1.5 g of angelica extract, and astragalus extract 1.5.
- Eclipta prostrata extract 1.5g is 2.5 g of peony bark extract, 2.5 g of arborvitae leaf extract, 2.5 g of rosemary extract, 2 g of tea tree extract, 1.5 g of angelica extract, and astragalus extract 1.5.
- Eclipta prostrata extract 1.5g is 2.5 g of peony bark extract, 2.5 g of arborvitae leaf extract, 2.5 g of rosemary extract, 2 g of tea tree extract, 1.5 g of angelica extract, and astragalus extract 1.5.
- Eclipta prostrata extract 1.5g is 2.5 g of peony bark extract
- 2.5 g of arborvitae leaf extract 2.5 g of rosemary extract
- 2 g of tea tree extract 1.5 g of angelica extract
- astragalus extract 1.5 is
- the control group was replaced with physiological saline in place of the aqueous solution of fullerol, and the other treatments were the same.
- the difference between the blank group, the control group and the experimental group was compared every other week, and the administration time was two weeks.
- a C 60 (OH) 22 aqueous solution was prepared at a concentration of 1000 ppm.
- the control group was replaced with physiological saline in place of the aqueous solution of fullerol, and the other treatments were the same.
- the difference between the blank group, the control group and the experimental group was compared every other week, and the administration time was two weeks.
- Fig. 8A and Fig. 8C The results of histological evaluation of the number of mouse hair follicles stained with H&E are shown in Fig. 8.
- the present invention was treated with a C 60 (OH) 22 solution having a concentration of 1000 ppm as compared with the blank group.
- the number of hair follicles in the skin is significantly increased, indicating that the fullerol of the present invention has an effect of promoting hair growth.
- a C 60 (OH) 22 aqueous solution was prepared at a concentration of 1500 ppm.
- the control group was replaced with physiological saline in place of the aqueous solution of fullerol, and the other treatments were the same.
- the difference between the blank group, the control group and the experimental group was compared every other week, and the administration time was two weeks.
- Fig. 8A and Fig. 8D The results of histological evaluation of the number of mouse hair follicles stained with H&E are shown in Fig. 8.
- the present invention was treated with a C 60 (OH) 22 solution having a concentration of 1500 ppm as compared with the blank group.
- the number of hair follicles in the skin is significantly increased, indicating that the fullerol of the present invention has an effect of promoting hair growth.
- Test Example 1 Accelerator containing fullerene oil
- mice C57BL/6 black mice were 8 weeks old. After ether anesthesia, the rosin paraffin mixed in a 1:1 ratio was heated and thawed and applied to the back of the mouse. After it was cooled and hardened, it was peeled off, and all the terminating hair was removed. Highly synchronized hair growth during growth, the hair follicles are morphologically indistinguishable from spontaneously formed hair follicles. After 9 days, the back hair grew completely. The mice were divided into 4 groups: C 60 - olive oil group, olive oil group, minoxidil group, and saline group. 150 ⁇ l of the back was applied every day. After 14 days, the back skin of the mice was taken, using Western Blot. The VEGFR-2 content was detected by RT-PCR.
- the fullerene oil promoter of the present invention can up-regulate VEGFR-2 content, treat hair loss, and is superior to minoxidil for androgenetic alopecia and alopecia areata.
- mice C57BL/6 black mice were 8 weeks old. After ether anesthesia, the rosin paraffin mixed in a 1:1 ratio was heated and thawed and applied to the back of the mouse. After it was cooled and hardened, it was peeled off, and all the terminating hair was removed. Highly synchronized hair growth during growth, the hair follicles are morphologically indistinguishable from spontaneously formed hair follicles. After 9 days, the back hair grew completely. The mice were divided into three groups, the aminofullerene group, the minoxidil group and the saline group. 150 ⁇ l of the back was applied to the back every day. After 14 days, the back skin of the mice was taken and Western Blot and RT-PCR methods were used.
- VEGFR-2 content was measured.
- RESULTS Figure 11
- Western Blot test of the aminofullerene group showed that the content of VEGFR-2 in the mice coated with amino fullerenes was significantly higher than that in the other groups.
- Figure 12 RT-PCR analysis showed that Mice with a fullerene on the back had significantly higher levels of VEGFR-2 than the other groups.
- the amino fullerene promoter of the present invention can up-regulate VEGFR-2 content, treat hair loss, and is superior to minoxidil for androgenetic alopecia and alopecia areata.
- mice C57BL/6 black mice were 8 weeks old. After ether anesthesia, the rosin paraffin mixed in a 1:1 ratio was heated and thawed and applied to the back of the mouse. After it was cooled and hardened, it was peeled off, and all the terminating hair was removed. Highly synchronized hair growth during growth, the hair follicles are morphologically indistinguishable from spontaneously formed hair follicles. After 9 days, the back hair grew completely. The mice were divided into three groups: hydroxyfullerene group, minoxidil group and saline group. 150 ⁇ l of the back was applied every day. After 14 days, the back skin of the mice was taken and Western Blot and RT-PCR methods were used. The VEGFR-2 content was measured.
- Figure 13 shows that Western Blot assay showed that the VEGFR-2 content of the mice with hydroxyfullerene on the back was significantly higher than that of the other groups.
- Figure 14 shows that RT-PCR can be seen that the back is coated with hydroxyl rich. The content of VEGFR-2 in the mice was significantly higher than that in the other groups.
- the hydroxyfullerene promoter of the present invention can up-regulate VEGFR-2 content, treat hair loss, and is superior to minoxidil in the treatment of androgenetic alopecia and alopecia areata.
- the experimental model is a seborrheic alopecia model. Unlike the common seborrheic alopecia model, this example greatly increases the injection dose of testosterone propionate and increases the number of injection days in order to cause serious infection in the back of the mouse.
- C57/B6 black rats except for the blank group, were injected subcutaneously with testosterone propionate parallel to the spinal region at the back of the mouse at a concentration of 25 mg/ml, an injection dose of 7 mg/kg/day, and an injection time of 6 weeks. .
- the back hair of the mice showed different degrees of shedding.
- the test area of the testosterone in the dorsal skin of the mice showed severe erythema, erosion, skin lesions in some areas, and agglomeration of hair. From the 42nd day, it was administered by external application. The way to treat. The experiment is divided into seven groups.
- the blank group is not administered: normal feeding, no treatment
- the model group is not administered: the model is performed according to the above-mentioned seborrheic alopecia model step, and no drug is administered.
- the composition (a composition of the composition against the head infection, anti-itch and anti-de-stabilization of the composition of the fullerene C 60 ) once a day in the hair removal area: according to the above-mentioned seborrheic alopecia model step modeling After topical administration, smear on the back of the mouse
- the fourth group of pure fullerenes once a day in the hair removal area after the above-mentioned seborrheic alopecia model step modeling, topical administration. Since fullerenes are in a powder state and have poor solubility and cannot be directly applied to the back of a mouse, in order to apply fullerene to the back of a small genus, a C 60 -PVP complex is prepared by the method of Patent Application No. 200580049615.2. It is known that fullerenes are active substances in this complex, and PVP is inert and has no external irritancy. Apply C 60 -PVP aqueous solution to the back hair removal area of mice to verify the efficacy of pure fullerenes
- Plant extract mixture (only containing fullerenes and their derivatives) once a day in the hair removal area: tocopherol acetate and menthol, plant sterols are dissolved in linseed oil, sea buckthorn oil, camellia oil, In a mixture of juniper oil and geranium oil, solubilized by a solubilizing agent, and then the solubilized aqueous solution and plant extract (licorice extract, jujube extract, peony bark extract, pan pomegranate extract, centella asiatica) Extract, Chuanxiong extract, black tea extract, phytosterol, capsicum extract, glutinous rice extract, ginger extract, aloe extract, hop extract, Eclipta extract, angelica extract, ginkgo extract, Nori extract) mixed with an aqueous solution of oat dextran, inositol, and biotin, and the mixture was applied to the back hair removal area of the mouse.
- plant extract licorice
- the composition of the present invention has the effect of lowering testosterone levels and preventing or treating hair loss.
- the composition of the present invention has a synergistic effect on lowering testosterone hormone levels than the pure fullerene group and the plant extract group, and fully demonstrates the remarkable effect of the composition of the present invention on seborrheic alopecia. .
- Example 3 of the present composition product after 15 days, the scalp pustule was atrophied, the hair loss part re-grows hair, and the patient was physically and mentally pleasing.
- the above test examples 1, 2 can be seen that the addition of fullerenes has a synergistic effect on the extract of traditional Chinese medicine, and the effect of activating hair follicles in the anti-inflammatory activated cells is obvious.
- the composition of the present invention has a synergistic effect on lowering testosterone hormone levels, and the effect is significantly higher than that of the pure fullerene group and the plant extract group, which fully demonstrates that the composition of the present invention is remarkable for seborrheic alopecia. effect.
- the composition of the present invention fights head infections, relieves itching and prevents hair loss.
- the composition not only eliminates itching and dandruff, but also treats bacterial infectious hair loss and promotes hair loss in patients.
- the experimental model was a model of seborrheic alopecia: C57/B6 black mice, except for the blank group, the other groups were injected subcutaneously with testosterone propionate parallel to the spinal region on the back of the mouse at a concentration of 25 mg/ml, and the injection dose was 5 mg/ Kg/day, the injection time is five weeks. After the fifth week, the back hair of the mice showed different degrees of shedding, and the erythema, erosion, and hair agglomeration appeared in the test area of the testosterone in the back skin of the mice. From the 36th day, the treatment was performed by external administration. At the 9th week, the experiment was stopped, and blood and mouse back skin were taken for biochemical indicators and pathological analysis.
- the blank group is not administered: normal feeding, without any treatment;
- the model group is not administered: the model is performed according to the above-mentioned seborrheic alopecia model step, and no drug is administered;
- the third group. A composition for treating seborrheic alopecia.
- the composition of Example 7 is once a day in the hair removal area: after the model is established according to the above-mentioned seborrheic alopecia model, external application is applied to the back hair removal area of the mouse;
- the fourth group of pure fullerenes once a day in the hair removal area after the above-mentioned seborrheic alopecia model step modeling, topical administration. Since fullerenes are in a powder state and have poor solubility and cannot be directly applied to the back of the mouse, in order to apply fullerene to the back of the mouse, a C 60 -PVP complex is prepared by the method of Patent Application No. 200580049615.2. It is known that fullerenes are active substances in this complex, and PVP is inert and has no external irritancy. The C 60 -PVP aqueous solution was applied to the back hair removal area of the mouse to verify the efficacy of pure fullerenes;
- Plant extract mixture (excluding fullerenes and their derivatives fullerene C60) once a day in the hair removal area: dissolve tocopherol acetate and menthol in side tar, rosemary essential oil, tea tree oil , a mixture of angelica essential oil and sage essential oil, solubilized with a solubilizing agent, and then the solubilized aqueous solution and plant extract (peony extract, Eclipta extract, saw palmetto extract, hop extract) , the aqueous solution of Noni extract dispersed in water is mixed, and then mixed with biotin, inositol, hydrolyzed wheat protein, oat glucan, zinc gluconate aqueous solution;
- the saline group is once a day in the hair removal area
- the hair follicle has high melanin content, a large number of hair follicles, and the health condition is close to that of the blank group, and the effect is far superior to the pure fullerene group, the plant extract group, and the minoxidil group, which fully demonstrates that the composition of the present invention is
- the addition of fullerenes has a synergistic effect on the extract of traditional Chinese medicine, and the effect of activating hair follicles in germinal anti-inflammatory activated cells is obvious.
- Testosterone T ( ⁇ mol/L) Blank group 10 0.6528 ⁇ 0.0201 Patent group 9 1.3339 ⁇ 0.0291 Pure fullerene group 9 1.9739 ⁇ 0.0311 Plant extract group (excluding fullerenes) 8 2.9327 ⁇ 0.0373 Minoxidil group 10 3.1119 ⁇ 0.0300 Saline group 8 3.2003 ⁇ 0.0391 Model group (not administered) 8 3.1339 ⁇ 0.0311
- the testosterone levels in the mice of the patent composition group were significantly lower than those in the model group and the minoxidil group, indicating that the composition of the present invention has a testosterone-lowering level and can prevent or treat hair loss. effect.
- the composition of the present invention has a synergistic effect on lowering testosterone hormone levels than the pure fullerene group and the plant extract group, and fully demonstrates the remarkable effect of the composition of the present invention on seborrheic alopecia. .
- the patient has baldness for about 5 years.
- Family hereditary hair loss due to personal work pressure, staying up late to work overtime, eating more meat, eating alcohol, no more effect after using more methods, the hair grows 7 days after the trial of the agent of the invention (Example 3), After 15 days, it was apparent that the hair in the bald area became black and thick.
- the patient's information is improved, the work schedule is actively adjusted, the sleep is performed on time, the outdoor exercise is performed, the meat intake is reduced, and the drinking is stopped.
- the compositions of the invention have a therapeutic hereditary alopecia effect.
- bald hair has hair growth, 30 After a day, the baldness area becomes black and thick, and the night is good, the spirit is full, and the mood is good.
- the composition of the present invention has an anti-inflammatory effect and is effective for seborrheic alopecia.
- Collecting androgenetic alopecia has a family history, that is, androgen-dependent hereditary off-law. After passing statistics on people of different ages, see Figure 17: 50 people aged between 40-50 years old (implementation) Example 8) After 7-15 days of trial, 47 people successfully developed new hair; 40 people aged between 50 and 60 years old tried it, and after 7-15 days of trial, 35 people successfully developed new hair; 40 people aged 60 or older try it after 7-15 days After use, 30 people successfully developed new hair; it can be seen that for hereditary hair loss, the overall efficiency of the composition of the present invention is over 86%.
- the scalp stratum corneum is generally thick, and has a large barrier effect on the penetration of the drug.
- the drug is not easily transdermally absorbed, so there is a difference in the penetration of the drug.
- they can be achieved by increasing the amount of medication.
- the results of the above test examples 1-3 show that the addition of fullerenes has a synergistic effect on the extract of traditional Chinese medicine, and the effect of activating hair follicles in germinal anti-inflammatory activated cells is obvious.
- the composition of the present invention has a synergistic effect on lowering testosterone hormone levels, and the effect is significantly higher than that of the pure fullerene group and the plant extract group, which fully demonstrates that the composition of the present invention is remarkable for seborrheic alopecia. effect.
- For androgen-dependent hereditary episodes new ones can be developed 1 week after administration.
- hereditary alopecia the hair grew 7 days after administration, and it became apparent after 15 days that the hair in the bald area became black and thick.
- the present invention discloses the use of a fullerene and a derivative thereof for producing a product for promoting hair growth, which can promote the expression of vascular endothelial cell growth factor in hair follicles of the head.
- the hair growth promoting product is at least one of a hair follicle vascular endothelial cell growth factor promoter, a hair growth agent, a hair conditioner, an anti-release agent and a hair growth agent, and the fullerene and the derivative thereof are oil, an aqueous solution or And in any one of the compositions of the extract of the Chinese herbal medicine, the vascular endothelial growth factor promoter of the head hair follicle is one or more of fullerene oil, amino fullerene, and hydroxy fullerene, and is water-soluble.
- Fullerene derivatives are hollow fullerol and / or metal fullerol, amino fullerene, hydroxy fullerene; also disclosed a fight against head infection, itching and anti-deformation and a treatment of seborrheic Hair loss of a traditional Chinese medicine composition containing fullerenes and derivatives thereof.
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Abstract
一种富勒烯及其衍生物在制备促进毛发生长产品中的应用。一种对抗头部感染,止痒防脱固发生发和一种治疗脂溢性脱发的含有富勒烯及其衍生物的中药组合物。所述富勒烯及其衍生物治疗毛囊血管内皮细胞生长因子下降所导致的脱发,尤其是雄激素性脱发、斑秃、脂溢性脱发。富勒烯及其衍生物为油、水溶液和/或与中药提取物的组合物中任一种形式。
Description
交叉引用
本发明要求2016年10月9日向中国专利局提交的、申请号为CN201610881557.X、发明名称为“水溶性富勒烯衍生物在促进毛发生长中的应用”的中国专利申请的优先权,该申请的全部内容通过引用结合在本发明中。
本发明还要求2016年12月14日向中国专利局提交的、申请号CN201611155549.3、发明名称为“一种对抗头部感染,止痒防脱的组合物及其制备方法和应用”的中国专利申请的优先权,该申请的全部内容通过引用结合在本发明中。
本发明还要求2016年12月14日向中国专利局提交的、申请号201611155550.6、发明名称“一种治疗脂溢性脱发的组合物”的中国专利申请的优先权,该申请的全部内容通过引用结合在本发明中。
本发明属于生物医药领域,具体涉及一种富勒烯及其衍生物在制备促进毛发生长产品中的应用。
自从1985年发现以来,富勒烯就因其特殊的物理和化学性能而倍受关注。近些年,富勒烯分子及其衍生物、复合物、包合物,更是被发现具有优异的抗氧化活性、抗菌性和抗癌性等生理活性。在诸多水溶性富勒烯中,由于富勒醇(C60(OH)n)优异的生理活性和稳定性而备受关注。有关富勒醇的制备方法,也已经发展了不少包括:1、四丁基氢氧化铵(TBAH)催化碱法合成(J.Chem.Soc.Chem.Commun.,1993,(23):1784-1785);2、聚乙二醇(PEG)催化合成([J].J.Cent.South Univ.T.,1999,6(1):35-3);3、酸法(浓硫酸或浓硝酸)([J].Chin.J.Chem.,2004,22(9):1000-1011)合成;4、富勒烯氯化物强碱水解法(如中国发明专利申请号:01109496.6,发明人:陈滇宝,陈红蕾,刘青,章裕华);5、富勒烯水悬液水解法(辐射研究与辐射工艺学报,2010.28(1),张晓敏等)。6、低羟基数富勒醇深度水解法(ACSNANO,2008,vol(2),327-333)。
脱发(alopecia)是临床常见毛发病,随着生活水平的提高,人们对美容美发的要求日益迫切,现代医学和传统医学对此的研究也越来越受到重视。脱发,虽不属严重疾病,但却对人们的精神、心理产生较大的影响。目前临床常见的脱发有以下几种:1、雄激素性脱发(AGA)有家族史,是雄激素依赖性的遗传性脱发病,病理特点是生长期毛囊与休止期毛囊的比例由正常的12:1降低到5:1,毛囊逐渐缩小及毛囊密度由正常成年人的326个cm2,减少到278个cm2。2、斑秃(alopecia areata)一种功能性疾病,可突然发生于身体任何部位的局限性斑状脱发,神经系统紊乱是重要因素。3、脂溢性脱发也被称为早秃,主要发病机理与遗传、雄性素、皮脂溢出等相关。由于头部油脂分泌过多,头发油腻,从而导致头皮潮湿油腻,空气中的尘埃与头皮屑混杂,几天不洗头就很脏,并散发臭味。
目前,市场上治疗脱发的药物有多种,大体可分为合成药、中药及混合药剂,现有的治疗脱发的产品由于其制备成本高、生发配方合理性方面有缺陷、不能够快速的促进头发的生长,达不到立竿见影的效果。有的药物在使用时还具有一定的疗效,但是患者一旦停药,病情就会复发。大多配方只是涉及防脱生发的一个方面或两个方面,而防脱生发是需要多方面的共同作用才能产生良好的效果,不单单是将几种能生发的活性物质加在一起就能产生。例如专利CN200910071736公开了一种治疗脱发的中药组合物,包括熟地、当归、川芎、白术、夜交藤、女贞子、菟丝子、鸡血藤、首乌、鸡内金、山萸肉、仙灵脾、五味子、茯苓、白芍、丹参、侧柏叶、旱莲草、黑芝麻、桑葚子、远志、酸枣仁、合欢皮、羌活、紫草、黄连、黄芪、桃仁、生甘草等组成,治疗斑秃、普秃、全秃及脂溢性脱发有较好疗效。CN201310347018公开一种治疗脱发的中药组合物,其包括15种原料,熟地黄、何首乌、生地黄、山茱萸、墨旱莲、山药、侧柏叶、人参、党参、茯苓、牡丹皮、泽泻、知母、地骨皮、银柴胡。专利201610482648公开一种再出发滋养露及其制备方法,通过从啤酒花、桑椹、何首乌、毛喉鞘蕊花、藏红花、牡丹皮按照合理配比组成的混合料中提取有效成分,改善脱发及改善发质的作用。CN201510025222一种防脱发的洗发护发组合物,含有锯棕榈提取物和柠檬草精作为主要成分,所述组合物有效防止或减少脱发。上述专利起效慢,停止用药后容易复发。不能彻底解决脱发患者的困扰。同时上述专利对感染导致的头屑增多及掉发脱发没有效果,对改善雄激素依赖性的遗传性脱发病疗效不明显。目前被FDA批准外用治疗雄激素源性脱发的一种局部外用药米诺地尔可以有效抑制毛发脱落和促进毛发再生,但米诺地尔现有的治疗脱发的方法起效慢、副作用大。
因此一种起效快,毒副作用小的药物急需解决的问题。
发明内容
本发明的目的是提供一种富勒烯及其衍生物促进毛发生长中的应用。
本发明还提供富勒烯及其衍生物在制备促进毛发生长产品中的应用。上述应用中,所述促进毛发生长产品为头部毛囊血管内皮细胞生长因子促进剂、养发剂、护发剂、防脱剂和生发剂中的至少一种。
所述促进毛发生长产品为富勒烯及其衍生物的油形式、水溶液和与中药提取物组成的组合物中任一种。
本发明通过下述技术方案实现的:
本发明的一种技术方案,本发明的富勒烯及其衍生物在促进毛发生长中的应用。
本发明的富勒烯及其衍生物能够促进头部毛囊血管内皮细胞生长因子表达。
本发明的富勒烯及其衍生物能够治疗毛囊血管内皮细胞生长因子下降所导致的脱发。
本发明的富勒烯及其衍生物能够上调毛囊血管内皮细胞生长因子VEGF含量,尤其是上调毛囊血管内皮细胞生长因子VEGFR-2含量。
本发明所述的脱发包括雄激素性脱发、斑秃、脂溢性脱发,优选雄激素性脱发和斑秃。
本发明所述富勒烯衍生物为水溶性富勒烯衍生物包括羟基富勒烯、氨基富勒烯、空心富勒醇和/或金属富勒醇。
本发明一种实施方式,所述水溶性富勒烯衍生物为氨基富勒烯,将固体富勒烯与有机胺溶液混合反应,获得所述氨基富勒烯,例如Cm(EDA)n;M@Cm(EDA)n,(M=Gd、Y、Ho、Lu);M3N@Cm(EDA)n(M=Sc、Y、Lu);其中m=60、70、76、78、82、84,n=5-9。
具体所述氨基富勒烯是通过下述方法制备得到:
(a)将有机胺溶液与固体富勒烯混合,在室温搅拌或加热搅拌回流条件下进行反应,其中,有机胺包括乙二胺、丙胺、丙醇胺、对苯二胺和二乙醇胺的至少之一;固体富勒烯包括空心富勒烯C2n、金属富勒烯M@C2n、M2@C2n、MA@C2n、M3N@C2n、M2C2@C2n、M2S@C2n、M2O@C2n和MxA3-xN@C2n中的至少之一,其中,M和A分别独立的选自Sc、Y和镧系金属元素,30≤n≤60,0≤x≤3;
(b)将步骤(a)得到的溶液旋转干燥,用稀酸溶液溶解旋转干燥后的剩余固体,其
中,稀酸溶液为无机酸溶液,稀酸溶液的浓度为0.5~1.5mmol/L;
(c)调节步骤(b)得到的溶液的pH值为4~6,透析至溶液的电导率小于1μs/cm;
(d)利用阴离子交换树脂处理步骤(c)得到的溶液,透析至溶液的电导率小于1μs/cm。
本发明一种实施方式,所述水溶性富勒烯衍生物为羟基富勒烯,将固体富勒烯与过氧化氢溶液以及碱溶液混合反应获得的。例如Cm(O)5(OH)n;M3N@Cm(O)5(OH)n,(M=Sc、Y、Lu);M@Cm(O)5(OH)n,(M=Gd、Y、Ho、Lu);其中m=60、70、76、78、84,n=16-30。
具体所述羟基富勒烯是由下述方法制备得到:
将固体富勒烯与过氧化氢溶液以及碱溶液混合反应,其中,碱溶液包括氢氧化钠水溶液、氢氧化钾水溶液以及四丁基氢氧化铵水溶液的至少之一,固体富勒烯包括空心富勒烯C2n、M@C2n、M2@C2n、MA@C2n、M3N@C2n、M2C2@C2n、M2S@C2n、M2O@C2n和MxA3-xN@C2n中的至少之一,其中,M和A分别独立的选自Sc、Y和镧系金属元素,30≤n≤60,0≤x≤3;所述碱溶液中碱的含量为8~15wt%;基于所述过氧化氢溶液的总质量,所述过氧化氢溶液中过氧化氢的含量为20~40wt%;所述混合溶液中所述过氧化氢以及所述碱溶液的体积比为7:(1~4);所述反应是在加热搅拌处理下进行的,所述加热搅拌处理的加热温度为50~80摄氏度,搅拌速率为600~1500rpm/min,时间为15~36小时,对经过所述反应的所述混合溶液进行提纯处理。
进一步优选,羟基富勒烯的制备是通过下述方法得到的:
(a)将质量百分含量为30%的过氧化氢水溶液和质量百分含量为40%的氢氧化钠溶液按照体积比为7:3加入100mL圆底烧瓶,加入200mg富勒烯固体,使用磁力搅拌器搅拌24h,温度:70℃,转速:1000r/min,过滤,保留滤液;
(b)将滤液加离心管中,再加入过量的浓度为95%的乙醇,经过离心后收集沉淀,离心转速:10000r/min,离心时间:4min,将沉淀溶于水;
(c)将(b)步骤得到的溶液进行透析处理,透析至溶液的电导率小于1μs/cm;
(d)将透析后的溶液冷冻干燥,以便获得羟基富勒烯固体,冻干温度:-29℃,真空度:55Pa,冻干时间:48h。
本发明一种实施方式,所述水溶性富勒烯衍生物为空心富勒醇和/或金属富勒醇;所述空心富勒醇的本体材料为C2n;所述金属富勒醇的本体材料为M@C2n、M2@C2n和MA@C2n中的任一种,其中,M和A均为金属元素,所述M和A均选自Sc、Y和镧系金属元素中的任意一种;30≤n≤60。
进一步优选,所述空心富勒醇的本体材料可为C60;所述金属富勒醇的本体材料可为Gd@C82。
所述空心富勒醇和/或金属富勒醇中的羟基可为15~35个,具体可为22。所述的空心富勒醇和/或金属富勒醇仅是羟基修饰,例如,C60(OH)22。
毛囊研究的主要方向是毛囊真表皮间相互调控作用,涉及多个基因、生长因子、形态发生分子家族及信号通路等如:转化生长因子(TGF)、成纤维细胞生长因子(FGF)/Wnt通路、BMP家族,以及表皮生长因子、血管内皮细胞生长因子、干细胞生长因子等。这些家族、因子都由相应的受体、配体、胞质内递质及核转录因子等组成。近年来发现血管内皮细胞生长因子(VEGF)家族对毛囊的生长具有调控作用,而且在生长期毛囊的毛乳头细胞、毛囊外毛根鞘细胞上均发现有VEGF表达。生长期毛囊周围的血管明显增强,进入退行期后毛囊周围的血管开始退化,而休止期则血管化现象停止,这一现象与外毛根鞘细胞表达VEGF有关。VEGF家族成员通过结合位于血管内皮细胞特异性的VEGF受体介导微血管增生、增强血管通透性及内皮细胞增殖等作用,VEGF受体分为VEGFR-1、VEGFR-2和VGEGFR-3,在内皮细胞中VEGF的增殖主要由VEGFR-2介导。由于VEGF仅在生长期的毛囊中表达,并且在雄激素源性脱发和斑秃患者的毛囊肿VEGF表达减弱甚至消失。
本发明的另一种技术方案,本发明富勒烯及其衍生物在制备促进毛发生长产品中的应用。
本发明一种实施方式,所述促进毛发生长产品为所述水溶性富勒烯衍生物空心富勒醇和/或金属富勒醇的水溶液。
所述水溶性富勒烯衍生物水溶液的质量浓度可为100~10000ppm,具体可为800~1500ppm、800ppm、1000ppm或1500ppm。
本发明一种实施方式,本发明所述促进毛发生长产品为一种头部毛囊血管内皮细胞生长因子促进剂,其包含富勒烯与油的组合即富勒烯油、氨基富勒烯水溶液、羟基富勒烯水溶液中的一种或几种。本发明的促进剂能够促进头部毛囊血管内皮细胞生长因子表达;上调毛囊血管内皮细胞生长因子VEGF含量,尤其是上调毛囊血管内皮细胞生长因子VEGFR-2含量,从而能够治疗毛囊血管内皮细胞生长因子下降所导致的脱发。
本发明的一种头部毛囊血管内皮细胞生长因子促进剂的使用方法:富勒烯油可以为涂抹使用,氨基富勒烯水溶液、羟基富勒烯水溶液可以为涂抹或口服使用。
上述富勒烯油,其中富勒烯在富勒烯油中浓度为0.01-20mg/ml;进一步优选所述
富勒烯油中富勒烯浓度0.1mg/mL-15mg/mL;进一步优选,所述富勒烯油中富勒烯浓度1-10mg/ml。
本发明所述的富勒烯油中富勒烯为空心富勒烯和/或金属富勒烯。包括但不限于富勒烯C2n、M@C2n、M2@C2n、MA@C2n、M3N@C2n、M2C2@C2n、M2S@C2n、M2O@C2n和MxA3-xN@C2n中的任一种,其中,M和A均为金属元素,所述M和A均选自Sc、Y和镧系金属元素中的任意一种;30≤n≤60;0≤x≤3;进一步优选所述富勒烯选择C60、C70、C76、C84,Gd@C82,SC3N@C80一种或以上的混合物。
所述的油包括但不限于植物种子,花朵,根茎等的提取物,例如橄榄油,大豆油、亚麻籽油,青刺果油,油菜籽油,甜杏仁油,葵花油,红花籽油,葡萄籽油,月见草油,琉璃苣籽油,当归油,生姜油,荷荷巴油,核桃油,鳄梨油,芒果油,蓖麻油,杏仁油,乳木果油,玫瑰果油,椰子油,棕榈油,谷糠油,小麦胚芽油,金盏花油,芦荟油,棕榈油,甜杏仁油,玉米油,葡萄籽油等一种或几种的混合物;进一步优选富勒烯油为富勒烯橄榄油。
所述富勒烯油的制备:将富勒烯末与油充分混合均匀后,置于球磨机中,超声、搅拌、加热,使富勒烯在油中充分溶解,过滤得到富勒烯油。
进一步优选,将富勒烯粉末进行球磨细化0.05-1μm,再将细化后的富勒烯粉末与油进行混合,置于球磨机中500-1000转/分钟,球磨8-20h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到40-60℃,氮气保护,搅拌12-72h后,离心、过滤,得到富勒烯油溶液。
进一步优选,将富勒烯粉末球磨细化0.05-1μm,与油充分混合均匀后,置于球磨机中500-700转/分钟,球磨6-10h,得到富勒烯油混悬液,然后将混悬液加热到40-50℃超声、氮气保护,搅拌加热10-15h,使富勒烯在油中充分溶解,离心、过滤得到富勒烯油。
本发明的一种头部毛囊血管内皮细胞生长因子促进剂可用于保健品或药品或食品或护肤品或发用品的有效成分之一,与药学上可接受的载体或与中药提取物组成组合物,其填加量为0.01-99.99%。
本发明另一实施方式,本发明所述促进毛发生长产品为一种对抗头部感染,止痒防脱固发生发的组合物;该组合物不仅能够消除瘙痒和头屑,还能治疗细菌感染性脱发,促进脱发患者生出新发。
进一步优选,一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量
份的原料制得:亚麻籽油10-500份、沙棘油10-500份、山茶油10-500份、杜松油10-500份、天竺葵油10-500份、薄荷醇30-500份、甘草提取物1-400份、红枣提取物1-400份、牡丹皮提取物1-400份、潘石榴提取物1-400份、积雪草提取物1-400份、川穹提取物1-400份、红茶提取物1-400份、植物甾醇1-200份、辣椒提取物0.1-200份、槐米提取物1-200份、生姜提取物1-200份、芦荟提取物1-200份、啤酒花提取物1-200份、墨旱莲提取物1-200份、当归提取物1-200份、银杏提取物1-200份、诺丽提取物1-200份、燕麦葡聚糖1-200份、肌醇10-300份、生育酚乙酸酯10-300份、生物素0.1-5份、富勒烯1-50份。
进一步优选,一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油50-400份、沙棘油50-400份、山茶油50-400份、杜松油50-400份、天竺葵油50-400份、薄荷醇50-400份、甘草提取物5-200份、红枣提取物5-200份、牡丹皮提取物5-200份、潘石榴提取物5-200份、积雪草提取物5-200份、川穹提取物5-200份、红茶提取物5-200份、植物甾醇5-100份、辣椒提取物0.5-100份、槐米提取物5-100份、生姜提取物5-100份、芦荟提取物5-100份、啤酒花提取物5-100份、墨旱莲提取物5-100份、当归提取物5-100份、银杏提取物5-100份、诺丽提取物5-100份、燕麦葡聚糖5-100份、肌醇20-200份、生育酚乙酸酯10-100份、生物素0.3-3份、富勒烯5-30份。
进一步优选,一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油100-300份、沙棘油100-300份、山茶油100-300份、杜松油100-300份、天竺葵油100-300份、薄荷醇70-200份、甘草提取物10-100份、红枣提取物10-100份、牡丹皮提取物10-100份、潘石榴提取物10-100份、积雪草提取物10-100份、川穹提取物10-100份、红茶提取物10-100份、植物甾醇10-50份、辣椒提取物0.5-10份、槐米提取物10-50份、生姜提取物10-50份、芦荟提取物10-50份、啤酒花提取物10-50份、墨旱莲提取物10-50份、当归提取物10-50份、银杏提取物10-50份、诺丽提取物10-50份、燕麦葡聚糖5-20份、肌醇30-100份、生育酚乙酸酯20-70份、生物素0.5-2份、富勒烯10-20份。
更进一步优选,一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油150-250份、沙棘油150-250份、山茶油150-250份、杜松油130-180份、天竺葵油150-250份、薄荷醇100-150份、甘草提取物20-70份、红枣提取物20-70份、牡丹皮提取物20-70份、潘石榴提取物20-70份、积雪草提取
物20-70份、川穹提取物20-70份、红茶提取物20-70份、植物甾醇20-40份、辣椒提取物0.5-2份、槐米提取物10-50份、生姜提取物10-50份、芦荟提取物10-50份、啤酒花提取物10-50份、墨旱莲提取物10-50份、当归提取物10-50份、银杏提取物10-50份、诺丽提取物10-50份、燕麦葡聚糖5-20份、肌醇30-100份、生育酚乙酸酯20-70份、生物素0.5-2份、富勒烯10-20份。
最佳,一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油200份、沙棘油200份、山茶油200份、杜松油150份、天竺葵油150份、薄荷醇100份、甘草提取物50份、红枣提取物70份、牡丹皮提取物50份、潘石榴提取物50份、积雪草提取物40份、川穹提取物50份、红茶提取物50份、植物甾醇30份、辣椒提取物0.7份、槐米提取物30份、生姜提取物20份、芦荟提取物30份、啤酒花提取物30份、墨旱莲提取物30份、当归提取物40份、银杏提取物30份、诺丽提取物30份、燕麦葡聚糖10份、肌醇40份、生育酚乙酸酯30份、生物素0.7份、富勒烯15份。
本发明的一个实施方式,本发明所述止痒防脱固发生发组合物与药剂上可接受的载体制成可接受的剂型。药学上可接受的载体以重量计可以是制剂总重量0.1-99.9%。药物组合物以适合药用的制剂形式存在。药用的制剂为片剂、胶囊剂、颗粒剂、丸剂、散剂、膏剂、混悬剂、注射剂、粉针剂、栓剂、霜剂、滴剂或贴剂。其中,所述片剂为糖衣片剂、薄膜衣片剂、肠溶衣片剂或缓释片剂;所述胶囊剂为硬胶囊剂、软胶囊剂、缓释胶囊剂;所述粉针剂为冻干粉针剂。
所述药物可接受的的载体选自:甘露醇、山梨醇、山梨酸或钾盐、焦亚硫酸钠、亚硫酸氢钠、硫代硫酸钠、盐酸半胱氨酸、巯基乙酸、蛋氨酸、维生素A、维生素C、维生素E、维生素D、氮酮、EDTA二钠、EDTA钙钠,一价碱金属的碳酸盐、醋酸盐、磷酸盐或其水溶液、盐酸、醋酸、硫酸、磷酸、氨基酸、氯化钠、氯化钾、乳酸钠、木糖醇、麦芽糖、葡萄糖、果糖、右旋糖苷、甘氨酸、淀粉、蔗糖、乳糖、甘露糖醇、硅衍生物、纤维素及其衍生物、藻酸盐、明胶、聚乙烯吡咯烷酮、甘油、丙二醇、乙醇、土温60-80、司班-80、蜂蜡、羊毛脂、液体石蜡、十六醇、没食子酸酯类、琼脂、三乙醇胺、碱性氨基酸、尿素、尿囊素、碳酸钙、碳酸氢钙、表面活性剂、聚乙二醇、环糊精、β-环糊精、磷脂类材料、高岭土、滑石粉、硬脂酸钙、硬脂酸镁等。
本发明的组合物,作为制剂形式,每剂中含有的发明化合物的有效量为0.1~1000mg,所述每剂指的是,每一制剂单位,如片剂的每片,胶囊的每粒,也可指每次
服用剂量,如每次服用100mg。虽然剂量单位形式中所含活性成分的量可以变化,但一般根据所选择活性成分的效力,调节在1~1000mg范围内。
本发明的组合物在制备成粉剂、片剂、可分散粉剂、胶囊、胶囊剂、栓剂和软膏形式的固体或半固体药物制剂时,可使用固体载体。可使用的固体载体优选为选自稀释剂、调味剂、增溶剂、润滑剂、悬浮剂、粘合剂、膨胀剂等中的一种或多种物质,或可为包封物质。在粉状制剂中,在载体中含有5~70%的微粒化活性成分。适宜的固体载体包括碳酸镁、硬脂酸镁、滑石粉、蔗糖、乳糖、果胶、糊精、淀粉、明胶、甲基纤维素、羧甲基纤维素钠、低沸点蜡、可可脂等。由于它们易于给药,片剂,粉剂、扁囊剂和胶囊等代表最有利的口服固体制剂。
本发明的液体制剂包括溶液、悬液和乳液。例如,非胃肠道给药的注射制剂可为水或水-丙二醇溶液形式,调节其等渗度,pH等使适于活体的生理条件。液体制剂还可制成在聚乙二醇、水溶液中的溶液形式。可通过将活性成分溶解在水中,再加入适量的着色剂、调味剂、稳定剂和增稠剂,来制备口服水溶液。可将微粒化的活性成分分散在粘性物质如天然和合成胶、甲基纤维素、羧甲基纤维素钠和其它已知悬浮剂中制备适于口服的水悬液。
为了易于给药及剂量均一,将上述药物制剂配制成剂量单位形式是特别有利的。制剂的剂量单位形式指适于作为单一剂量的物理分离单位,每个单位含有产生所期望的治疗效果的计算好的预定量的活性成分。这种剂量单位形式可为包装形式,如片剂、胶囊或装在小管或小瓶中的粉剂,或装在管或瓶中的软膏、凝胶或霜剂。
将上述组合物制成药剂时,可以根据制剂工艺要求,将组合物中某一成分拆分出来与辅料混合。例如,当制剂为乳剂或膏剂时,水溶性成分如甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物、燕麦葡聚糖、肌醇、生物素加入到水相中,而亚麻籽油、沙棘油、山茶油、百里香油、杜松油、天竺葵油、薄荷醇、生育酚乙酸酯、富勒烯等加入到油相中。
本发明优选剂型为乳剂、喷雾剂,其组合物与辅料重量比(1-5):(5-10)。
本发明的一个实施方式优选乳剂,由止痒防脱固发生发组合物与水、乳化剂制备而成。
上述所述的乳化剂包括但不限于乳剂的形成需要机械力的作用,另一个加入适应
的乳化剂,所述的乳化剂包括天然乳化剂、合成乳化剂、固体粉末乳化剂。所述天然乳化剂包括但不限于阿拉伯胶、西黄芪胶、甘油、豆磷脂、明胶、卵黄、琼脂、海藻酸钠、白芨胶、果胶、套脚、胆固醇等。所述的合成乳化剂包括但不限于十二烷基硫酸钠、十六烷基硫酸钠、鲸蜡醇、溴化十六烷基三甲铵或溴化十四烷基三甲胺、吐温、司盘、纤维素及其衍生物、甲基纤维素羧甲基纤维素等。所述固体粉末乳化剂包括但不限于硅藻土、氢氧化镁、氢氧化铝、二氧化硅、二氧化铝、白陶土、氢氧化钙、氢氧化锌、硬脂酸镁等。
本发明的一种对抗头部感染,止痒防脱固发生发乳剂的制备方法,包括如下步骤:
(1)将亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、生育酚乙酸酯充分混合均匀,将富勒烯粉末适度研磨后加入上述混合油相中,然后将加热融化后的薄荷醇加入其中,将混合好的油相40摄氏度条件下,减压搅拌1h,使各组分更好的在油相中溶解,为油相;
(2)取去离子水,向其中加入甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物、燕麦葡聚糖、肌醇、生物素,溶解搅拌均匀后超声,离心,取上清液,然后向上清液中加入EDTA-2Na,静置24h,离心取上清液备用,为水相;
(3)将油相和水相混合后,加入增溶乳化剂LRI和磷脂,充分搅拌均质后形成乳液。
本发明的一个实施方式优选喷雾剂,由止痒防脱固发生发组合物与水、增溶剂制备而成。具体步骤为:
(1)将亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、植物甾醇,生育酚乙酸酯充分混合均匀,将富勒烯粉末适度研磨后加入上述混合油相中,然后将加热融化后的薄荷醇加入其中,将混合好的油相40摄氏度条件下,减压搅拌1h,使各组分更好的在油相中溶解,为油相;
(2)取去离子水,向其中加入甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物、燕麦葡聚糖、肌醇、生物素,溶解搅拌均匀后超声,离心,取上清液,然后向上清液中加入EDTA-2Na,静置24h,离心取上清液备用,为水相;
(3)向油相中加入增溶剂,充分搅拌使得油相被完全增溶后,将水相加入其中,充分均质后得到均匀透明的稳定液体,将此液体灌装入喷雾瓶中使用。
上述组合物,制备方法及制剂中,所述的亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、薄荷醇、甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物、燕麦葡聚糖、水解小麦蛋白、燕麦葡聚糖、葡糖酸锌、生育酚乙酸酯均为现有技术制备或者市购。
为了更好的发挥本发明的有益效果,优选包括甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物分别为水提取物,例如用水煎煮液。
本发明组合物中,将中西医理论相结合,将各组分科学合理的结合。其中所述亚麻籽油:不饱和脂肪酸含量高,对皮肤具有优良的亲和力和渗透力,其所含的多种脂肪酸容易被皮肤吸收,用来补充皮肤所需要的脂质成分,消炎和抗增生作用,对减轻由紫外线引起的红斑症及炎症反应有很好的效果,对于治疗皮肤过敏症、湿疹有明显的效果。所述沙棘油:其中的挥发油类化合物的消炎功效,促进毛细血管血液循环,沙棘中卵磷脂等磷脂类化合物是一种生物活性较高的成分,可促进细胞代谢,是多种维生素和生物活性物质的复合体;它能滋养皮肤、促进新陈代谢、抗过敏,杀菌消炎,促进上皮细胞再生,对皮肤有修复作用,能保持皮肤的酸性环境,具有较强的渗透性。所述山茶油:活血化瘀,治疗湿疹,治疗皮癣。所述杜松油:油性充血皮肤的帮手,还能改善头皮的皮脂,净化的特性可改善粉刺、毛孔阻塞、皮肤炎、流行的湿疹、干癣。所述天竺葵油:平衡皮脂分泌,可治疗湿疹,皮癣。所述薄荷醇:具有消炎止痛,清凉止痒的功效。所述甘草提取物:补脾益气,清热解毒,吸收紫外线。所述红枣提取物:富含蛋白质、脂肪、糖类、胡萝卜素、B族维生素、维生素C、维生素P以及钙、磷、铁和环磷酸腺苷等营养成分。所述牡丹皮提取物:镇痛、止血、抗菌,能去屑,止痒,调理头发,保湿,柔软,光亮,促进头发生长。所述番石榴提取物:治皮肤湿疹,瘙痒,热痱,富含各种维生素及微量元素。所述积雪草提取物:抗菌消炎,治疗因病毒或者细菌引起的带状疱疹,活血化瘀。所述当归提取物:当归精油,造血作用,抗氧化、清除自由基,抗炎镇痛。所述诺丽提取物:诺丽果粉,可活化细胞,
滋养脑部。所述墨旱莲提取物:水浸提物,提高细胞免疫和体液免疫,养肝益肾、凉血止血。所述鼠尾草提取物:鼠尾草精油,镇定紧张情绪,改善头疼和偏头痛,舒缓焦虑的心情。所述锯棕榈提取物:水浸提物,有效抑制5a—还原酶活性,减少双氢睾酮生成拮抗前列腺组织中的雄激素与雄激素受体结合,利肝肾。所述啤酒花提取物:健胃消食,安神利尿,有效抑制5a—还原酶活性。所述富勒烯为空心富勒烯和/或富勒烯衍生物。所述空心富勒烯包含C60、C70、C76、C84中一种或几种,优选C60或C70或C60和C70的混合物;所述富勒烯衍生物包括但不限于C60-(OH)n,C70-(OH)n,C60-(COOH)n,C70-(COOH)n(n为4-30)。所述川穹提取物:具有活血行气,祛风止痛的作用。所述红茶提取物:具有抗菌消炎的作用,可用于清除自由基,能够抑制病毒。所述植物甾醇:具有较强的抗炎作用,能够抑制胆固醇的吸收,促进胆固醇的降解。所述辣椒提取物:具有抗炎镇痛、散寒燥湿。所述槐米提取物:具有抗炎作用,抑制浮肿和炎症的发生。所述生姜提取物:含有6-姜酚活动成分,具有抗炎抗氧化等多种功效,用6-姜酚处理头发毛囊,能够引起毛囊真皮乳头细胞的凋亡,从而抑制头发的生长。所述芦荟提取物:保湿作用,头发顺滑,能过减少皮屑的产生。
人体毛发生长分为三个周期,生长期,退行期,休止期,三个周期一次循环。当某些干扰因素扰乱了正常毛发的循环周期,使得生长期缩短,毛发变细,由长毛变为毫毛,大毛囊变为小毛囊,渐渐形成脱发严重的感染。脂溢性脱发,多数是雄性激素在头皮部位的过多聚集有关。本发明组合物中墨旱莲,鼠尾草,锯棕榈,啤酒花为皮脂调节剂,并可以很好的抑制5a—还原酶活性,缓解脂溢性脱发。脂溢性脱发多伴随严重的皮炎,亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油和薄荷油具有抑菌消炎舒缓皮肤的作用。同时,根据中医学基础知识,发之营养来源于血,肝主血气,生根于肾气,肾主骨,其荣在发,因此发的生产与脱落,与肾和肝的精气盛衰及其疏泄息息相关,因此组方中牡丹皮提取物为君药滋阴升发,番石榴、积雪草、川穹、当归提取物为臣药,行气补血功效,生姜、诺丽等为佐药,加强消炎抑菌活化细胞之功效并刺激毛囊真皮乳头细胞的凋亡,从而抑制头发的生长。加入富勒烯更能增强组合物生发抗炎活化细胞激活毛囊的作用。富勒烯是一种长效抗氧化剂,自由基清除剂,与多种精油类植提物复配,可以稳定精油类活性成分的功效,同时还可以清除头皮部位的自由基,激活毛囊。本方通过补气活血结合皮脂调节成分,又加以一款长效自由基清除剂,保证了活性成分的稳定性,进而保证了功效,避免了副作用的产生。
本发明剂型可根据患者需要进行定量使用。脱发患者在使用本产品前,先用干净
毛巾对头皮进行清洁,再用干净热毛巾对头皮进行热敷20-30分钟(温度控制40℃左右),通过热敷能够让毛孔张开有利于药物的渗透,用手指蘸取少许生发产品,于脱发部位进行均匀涂抹按摩,作用脱发部位一定时间后用清水将脱皮清洗干净,每天早晚各一次,经过7-15天后,会发现原来的脱发部位有不同程度的新发长出。由于个体差异的问题,患者在使用的时候应根据自己使用的情况,对所需浓度有一定的调动,是因为脱发部位经过长年暴露在外面,头皮角质层普遍偏厚,对药物的渗透有较大的屏障作用,药物不易透皮吸收,因此对于药物的渗透产生的差异。建议脱发史长的患者使用浓度较高的产品,有利于头发的再生。
本发明另一实施方试,本发明所述促进毛发生长产品为一种治疗脂溢性脱发的组合物,该组合物不仅能够治疗秃发,还能治疗脂溢性皮炎性脱发,尤其是对雄激素依赖性的遗传性脱发病有疗效。
本发明一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物0.1-5份、侧柏叶提取物0.1-5份、迷迭香提取物0.1-5份、茶树提取物0.1-5份、当归提取物0.1-5份、黄芪提取物0.1-5份,墨旱莲提取物0.1-5份、鼠尾草提取物0.01-2份、锯棕榈提取物0.01-2份、啤酒花提取物0.01-2份、诺丽提取物0.01-2份、生物素0.01-0.05份、肌醇0.1-2份、水解小麦蛋白0.1-1份、燕麦葡聚糖0.1-1份、葡萄酸锌0.1-5份、薄荷0.1-5份、生物酚乙酸酯0.01-1份、富勒烯及其相应衍生物0.001-10份。
进一步优选,一种治疗脂溢性脱发的组合物,是由下述重量份的原料制得:牡丹皮提取物0.3-3份、侧柏叶提取物0.3-3份、迷迭香提取物0.2-3份、茶树提取物0.1-3份、当归提取物0.2-2份、黄芪提取物0.2-2份,墨旱莲提取物0.2-2份、鼠尾草提取物0.1-2份、锯棕榈提取物0.05-1.5份、啤酒花提取物0.05-1.5份、诺丽提取物0.1-1份、生物素0.01-0.03份、肌醇0.1-1份、水解小麦蛋白0.1-0.5份、燕麦葡聚糖0.1-0.5份、葡萄酸锌0.5-3份、薄荷1-3份、生育酚乙酸酯0.03-0.06份、富勒烯及其相应衍生物0.01-5份。
进一步优选,一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物0.3-2.5份、侧柏叶提取物0.3-2.5份、迷迭香提取物0.2-2.5份、茶树提取物0.1-2份、当归提取物0.2-1.5份、黄芪提取物0.2-1.5份,墨旱莲提取物0.2-1.5份、鼠尾草提取物0.1-1.5份、锯棕榈提取物0.08-1.5份、啤酒花提取物0.08-1.5份、诺丽提取物0.08-1份、生物素0.01-0.03份、肌醇0.1-0.5份、水解
小麦蛋白0.2-0.4份、燕麦葡聚糖0.2-0.4份、葡萄酸锌2-3份、薄荷1-3份、生育酚乙酸酯0.03-0.06份、富勒烯及其相应衍生物0.01-2份。
进一步优选,一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物0.5-2份、侧柏叶提取物0.5-2份、迷迭香提取物0.5-2份、茶树提取物0.3-1份、当归提取物0.3-1份、黄芪提取物0.3-1份,墨旱莲提取物0.3-1份、鼠尾草提取物0.3-1份、锯棕榈提取物0.1-1份、啤酒花提取物0.1-1份、诺丽提取物0.5-1份、生物素0.01份、肌醇0.1份、水解小麦蛋白0.3份、燕麦葡聚糖0.3份、葡萄酸锌1份、薄荷2份、生物酚乙酸酯0.05份、富勒烯及其相应衍生物0.03-0.6份。
进一步优选,一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物1份、侧柏叶提取物1份、迷迭香提取物1份、茶树提取物1份、当归提取物1份、黄芪提取物1份,墨旱莲提取物1份、鼠尾草提取物1份、锯棕榈提取物0.3份、啤酒花提取物0.7份、诺丽提取物0.8份、生物素0.01份、肌醇0.1份、水解小麦蛋白0.3份、燕麦葡聚糖0.3份、葡萄酸锌1份、薄荷2份、生物酚乙酸酯0.05份、富勒烯及其相应衍生物0.01份。
本发明另一个技术方案是该治疗脂溢性脱发的组合物与药剂上可接受的载体制成可接受的剂型。本发明的组合物,在制成药剂时,单位剂量的药剂可含有本发明的药物活性物质0.1-1000mg,其余为药学上可接受的载体。药学上可接受的载体以重量计可以是制剂总重量的0.1-99.9%。
本发明治疗脱发的组合物,优选的是单位剂量的药物制剂形式,在制成药物制剂时可以制成任何可药用的剂型。
根据本发明的实施方式之一,本发明的组合物是外用剂型,如凝胶剂、软膏剂、乳剂、敷剂、膏剂等。
本发明的组合物,根据需要可以加入一些药物可接受的载体,可以采用制剂学常规技术制备该药物制剂,如将药物活性物质与药物可接受的载体混合。所述药物可接受的的载体选自:甘露醇、山梨醇、山梨酸或钾盐、焦亚硫酸钠、亚硫酸氢钠、硫代硫酸钠、盐酸半胱氨酸、巯基乙酸、蛋氨酸、维生素A、维生素C、维生素E、维生素D、氮酮、EDTA二钠、EDTA钙钠,一价碱金属的碳酸盐、醋酸盐、磷酸盐或其水溶液、盐酸、醋酸、硫酸、磷酸、氨基酸、氯化钠、氯化钾、乳酸钠、木糖醇、麦芽糖、葡萄糖、果糖、右旋糖苷、甘氨酸、淀粉、蔗糖、乳糖、甘露糖醇、硅衍生物、纤维
素及其衍生物、藻酸盐、明胶、聚乙烯吡咯烷酮、甘油、丙二醇、乙醇、土温60-80、司班-80、蜂蜡、羊毛脂、液体石蜡、十六醇、没食子酸酯类、琼脂、三乙醇胺、碱性氨基酸、尿素、尿囊素、碳酸钙、碳酸氢钙、表面活性剂、聚乙二醇、环糊精、β-环糊精、磷脂类材料、高岭土、滑石粉、硬脂酸钙、硬脂酸镁等。
本发明优选所述剂型为水凝胶剂,其组合物与基质重量比(1-5):(5-10),优选3-5:5-7。
所述的基质包括1,3-丁二醇、甲基纤维素,羟乙基纤维素、柠檬酸、透明质酸、LRI(PPG-26丁醇聚醚-26、PEG-40氢化蓖麻油)、EDTA-2Na、卡波姆、阿拉伯胶,安息香胶,琼脂,糊精,明胶,果胶,海藻酸钠,聚丙烯酸、聚乙烯醇、玻璃酸钠中一种或几种。
本发明治疗脂溢性脱发水凝胶剂,其包括下述重量份的原料制成:牡丹皮提取物0.1-5份、侧柏叶提取物0.1-5份、迷迭香提取物0.1-5份、茶树提取物0.1-5份、当归提取物0.1-5份、黄芪提取物0.1-5份,墨旱莲提取物0.1-5份、鼠尾草提取物0.01-2份、锯棕榈提取物0.01-2份、啤酒花提取物0.01-2份、诺丽提取物0.01-2份、生物素0.01-0.05份、肌醇0.1-2份、水解小麦蛋白0.1-1份、燕麦葡聚糖0.1-1份、葡萄酸锌0.1-5份、薄荷0.1-5份、生物酚乙酸酯0.01-1份、富勒烯及其相应衍生物0.001-10份、1,3-丁二醇0.1%-10份、羟乙基纤维素0.01-1份、柠檬酸0.01-1份、透明质酸0.1-10份、LRI 3-20份、EDTA-2Na 0.01-1份,去离子水补充至100%。
进一步优选,本发明治疗脂溢性脱发水凝胶剂,其包括下述重量份的原料:牡丹皮提取物0.3-3份、侧柏叶提取物0.3-3份、迷迭香提取物0.2-3份、茶树提取物0.1-3份、当归提取物0.2-2份、黄芪提取物0.2-2份,墨旱莲提取物0.2-2份、鼠尾草提取物0.1-2份、锯棕榈提取物0.05-1.5份、啤酒花提取物0.05-1.5份、诺丽提取物0.1-1份、生物素0.01-0.03份、肌醇0.1-1份、水解小麦蛋白0.1-0.5份、燕麦葡聚糖0.1-0.5份、葡萄酸锌0.5-3份、薄荷1-3份、生育酚乙酸酯0.03-0.06份、富勒烯及其相应衍生物0.01-2份,1,3-丁二醇0.1%-10份、羟乙基纤维素0.01-1份、柠檬酸0.01-1份、透明质酸2-6份、LRI 4-15份、EDTA-2Na 0.5-1份,去离子水补充至100%。
进一步优选,本发明治疗脱发水凝胶剂,其包括下述重量份的原料药制成:牡丹皮提取物0.5-2份、侧柏叶提取物0.5-2份、迷迭香提取物0.5-2份、茶树提取物0.3-1份、当归提取物0.3-1份、黄芪提取物0.3-1份,墨旱莲提取物0.3-1份、鼠尾草提
取物0.3-1份、锯棕榈提取物0.1-1份、啤酒花提取物0.1-1份、诺丽提取物0.5-1份、生物素0.01份、肌醇0.1份、水解小麦蛋白0.3份、燕麦葡聚糖0.3份、葡萄酸锌1份、薄荷2份、生物酚乙酸酯0.05份、富勒烯及其相应衍生物0.03-0.6份。1,3-丁二醇4份、羟乙基纤维素0.1份、柠檬酸0.3份、透明质酸1.5份、LRI 7份、EDTA-2Na 1份、去离子水补充至100%。
本发明的一种治疗脂溢性脱发组合物的制备方法,包括如下步骤:
(1)取侧柏叶提取物,迷迭香提取物,茶树提取物,当归提取物,鼠尾草提取物,黄芪提取物混合均匀得混合物提取物;
(2)将富勒烯及其相应衍生物加入步骤(1)混合提取物中,再加入生育酚乙酸酯和薄荷醇得富勒烯混合物,然后用增溶剂进行增溶,充分增溶好后,放置过夜,过滤,取上清液I备用;
(3)将牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物混合均匀后,用水超声提取,然后离心过滤,上清液II备用;
(4)将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌溶解于水得溶液III;
(5)将上述上清液I、上清液II、溶液III混合均匀即得组合物。
上述步骤(2)中上所述的富勒烯及其衍生物可溶解于步骤(1)混合提取物中,优选混合提取物为脂溶性成分。所述增溶剂为LRI(PPG-26丁醇聚醚-26、PEG-40氢化蓖麻油)。
本发明还提供一种治疗脱发的凝胶剂,包括步骤如下:
(1)将羟乙基纤维素先溶于水中充分溶胀;
(2)将上述组合物中加入上述羟乙基纤维素水溶液中,加入柠檬酸、EDTA-2Na和透明质酸,充分均质,充分陈化后形成凝胶。
上述组合物,制备方法及制剂中,所述的牡丹皮提取物、侧柏叶提取物、迷迭香提取物、茶树提取物、当归提取物、墨旱莲提取物、鼠尾草提取物、锯棕榈提取物、啤酒花提取物、诺丽提取物、薄荷提取物,生物素、肌醇、水解小麦蛋白、燕麦葡聚糖、葡糖酸锌、生育酚乙酸酯均为现有技术制备或者市购。
为了更好的发挥本发明的有益效果,优选包括侧柏叶提取物、侧柏叶提取物、迷迭香提取物、茶树提取物、当归提取物、鼠尾草提取物分别为挥发油成分即侧柏油,迷迭香精油,茶树油,当归精油,鼠尾草精油,黄芪精油。优选牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物分别为水提取物,例如用水煎
煮液。
本发明组合物中,将中西医理论相结合,将各组分科学合理的结合,配合利于组合物功效充分发挥的凝胶剂型,实现对脂溢性脱发的有效治疗。其中所述牡丹皮提取物:水浸提物,有抗炎作用,抗菌、抗炎、抗氧化,去屑,止痒。所述当归提取物:当归精油,造血作用,抗氧化、清除自由基,抗炎镇痛。所述黄芪提取物:黄芪精油,补气固表,利尿托毒,排脓,敛疮生肌。用于气虚乏力,食少便溏,中气下陷,久泻脱肛,便血崩漏,表虚自汗,气虚水肿,痈疽难溃,久溃不敛,血虚痿黄,内热消渴。所述诺丽提取物:诺丽果粉,可活化细胞,滋养脑部。所述侧柏叶提取物:侧柏油,可减少头屑、缓解皮肤炎症、湿疹、霉菌感染、调理头皮油腻分泌、减少掉头发。所述迷迭香提取物:迷迭香精油,具有较强的收敛作用,调理油腻不洁的肌肤,促进血液循环。所述墨旱莲提取物:水浸提物,提高细胞免疫和体液免疫,养肝益肾、凉血止血。所述鼠尾草提取物:鼠尾草精油,镇定紧张情绪,改善头疼和偏头痛,舒缓焦虑的心情。所述锯棕榈提取物:水浸提物,有效抑制5a—还原酶活性,减少双氢睾酮生成拮抗前列腺组织中的雄激素与雄激素受体结合,利肝肾。所述啤酒花提取物:健胃消食,安神利尿,有效抑制5a—还原酶活性。所述茶树提取物:茶树油,祛痘消炎,控油收敛,抑菌,强化免疫力。所述薄荷:薄荷脑,调理阻塞肌肤,舒缓肌肤,收缩微血管。所述富勒烯为空心富勒烯和/或富勒烯衍生物;所述空心富勒烯包含C60、C70、C76、C84中一种或几种,优选C60或C70或C60和C70的混合物;所述富勒烯衍生物包括但不限于:C60-(OH)n,C70-(OH)n,C60-(COOH)n,C70-(COOH)n,(n为4-30间)。
人体毛发生长分为三个周期,生长期,退行期,休止期,三个周期一次循环。当某些干扰因素扰乱了正常毛发的循环周期,使得生长期缩短,毛发变细,由长毛变为毫毛,大毛囊变为小毛囊,渐渐形成脱发。脂溢性脱发,多数是雄性激素在头皮部位的过多聚集有关,迷迭香,墨旱莲,鼠尾草,锯棕榈,啤酒花为皮脂调节剂,并可以很好的抑制5a—还原酶活性,缓解脂溢性脱发。脂溢性脱发多伴随严重的皮炎,茶树油和薄荷油具有抑菌消炎舒缓皮肤的作用。同时,根据中医学基础知识,发之营养来源于血,肝主血气,生根于肾气,肾主骨,其荣在发,因此发的生产与脱落,与肾和肝的精气盛衰及其疏泄息息相关,因此组方中侧柏叶提取物为君药滋阴升发,牡丹皮、黄芪提取物、当归提取物为臣药,补气补血功效,诺丽为佐药,加强消炎抑菌活化细胞之功效。加入富勒烯更能增强组合物生发抗炎活化细胞激活毛囊的作用。富勒烯是一种长效抗氧化剂,自由基清除剂,与多种精油类植提物复配,可以稳定精油类活性
成分的功效,同时还可以清除头皮部位的自由基,激活毛囊。本方通过补气活血结合皮脂调节成分,又加以一款长效自由基清除剂,保证了活性成分的稳定性,进而保证了功效。
本发明剂型可根据患者需要进行定量使用。脱发患者在使用本产品前,先用干净毛巾对头皮进行清洁,再用干净热毛巾对头皮进行热敷20-30分钟(温度控制40℃左右),通过热敷能够让毛孔张开有利于药物的渗透,用手指蘸取少许生发产品,于脱发部位进行均匀涂抹按摩,作用脱发部位一定时间后用清水将脱皮清洗干净,每天早晚各一次,经过7-15天后,会发现原来的脱发部位有不同程度的新发长出。由于个体差异的问题,患者在使用的时候应根据自己使用的情况,对所需用量有一定的调动,是因为脱发部位经过长年暴露在外面,头皮角质层普遍偏厚,对药物的渗透有较大的屏障作用,因此对于药物的渗透产生的差异。建议脱发史长的患者使用浓度较高的产品或者增加使用量和使用次数,有利于头发的再生。
1、本发明采用的水溶性富勒烯衍生物为空心富勒醇或金属富勒醇,它能有效激活毛囊,用于治疗脱发,能达到了快速生发的目的;同时,可以使长出的毛发更光亮、坚挺柔顺、粗壮。本发明解决了一些商品化的生发水在治疗脱发的过程中周期长的问题,用药两周后效果很明显,达到了快速生发的目的。
2、富勒烯橄榄油、氨基富勒烯、羟基富勒烯能够有效促进VEGFR-2在头部毛囊部位的表达,从而起到促进毛发生长、治疗脱发的目的,安全有效,无副作用,不易复发。尤其是对雄激素性脱发、斑秃、脂溢性脱发效果更明显。
3、一种治疗脂溢性脱发的组合物,该组合物不仅能够治疗秃发,还能治疗脂溢性皮炎性脱发,尤其是对雄激素依赖性的遗传性脱发病有疗效。
4、一种对抗头部感染,止痒防脱固发生发的组合物。该组合物不仅能够消除瘙痒和头屑,还能治疗细菌感染性脱发,促进脱发患者生出新发。
5、本发明的富勒烯及其富勒烯衍生物的产品均能快速生发,使用一周后即有明显生发效果。
图1显示了根据本发明氨基富勒烯实施例1以及实施例2的氨基富勒烯红外吸收谱;
图2显示了根据本发明氨基富勒烯实施例1以及实施例2的氨基富勒烯电子束探针分
析结果;
图3显示了根据本发明氨基富勒烯实施例1以及实施例2的氨基富勒烯水合粒径(图3a)和zeta电位(图3b);
图4显示了根据本发明羟基富勒烯实施例1制备的C60(O)5(OH)12的红外吸收谱;
图5显示了根据本发明羟基富勒烯实施例1制备的C60(O)5(OH)12的X射线光电子能谱C1s峰拟合曲线;
图6显示了根据本发明羟基富勒烯实施例1制备的C60(O)5(OH)12的水合粒径(图6a)和zeta电位(图6b);
图7显示了试验例一富勒醇水溶液生发中小鼠背部毛发生长图;其中,图7A、图7B、图7C和图7D分别为图7E、图7F、图7G和图7H使用药物前的照片,图7E、图7F和图7G分别为使用富勒醇浓度为800ppm、1000ppm和1500ppm时的毛发生长照片,图7H为使用生理盐水时的毛发生长照片。
图8显示了试验例一H&E染色的小鼠毛囊数量的组织学评价结果,其中,图8A、图8B、图8C和图8D分别为使用生理盐水、富勒醇浓度为800ppm、1000ppm和1500ppm时的结果。
图9是根据本发明试验例二C60-橄榄油组Western Blot检测VEGFR-2含量图。
图10是根据本发明的试验例二C60-橄榄油组RT-PCR检测检测VEGFR-2含量图,其中A:C60-橄榄油;B:橄榄油;C:米诺地尔;D:生理盐水。
图11是根据本发明的试验例二氨基富勒烯的小鼠VEGFR-2,Western Blot检测含量图。
图12是根据本发明的试验例二氨基富勒烯的小鼠VEGFR-2,RT-PCR检测含量图A:氨基富勒烯;B米诺地尔;C;生理盐水。
图13是根据本发明的试验例二羟基富勒烯的小鼠VEGFR-2,Western Blot检测含量图。
图14是根据本发明的试验例二羟基富勒烯的小鼠VEGFR-2,RT-PCR检测含量图A:羟基富勒烯;B米诺地尔;C:生理盐水。
图15是根据本发明试验例三,七组实验的小鼠背部病例H&E染色图片,可以看出不同实验组的小鼠背部毛皮内毛囊的状况a)空白组,b)本专利组合物,c)纯富勒烯组,d)植提物(不含富勒烯),e)米诺地尔,f)生理盐水,g)模型组(不给药)。
图16是根据本发明试验例四,七组实验的小鼠背部病例H&E染色图片,其中,a)空白组,b)本专利组合物,c)纯富勒烯组,d)植提物(不含富勒烯),e)米诺地尔,
f)生理盐水,g)模型组(不给药)。
图17不同年龄段人群试用后生发统计图。
下面结合附图,对本发明的具体实施方式进行详细描述,但应当理解本发明的保护范围并不受具体实施方式的限制。
实施例 富勒烯油
实施例1 C70富勒烯油
将富勒烯粉末C70进行球磨细化0.05-1μm,再将细化后的富勒烯粉末1g与大豆油20g进行混合,置于球磨机中500转/分钟,球磨8h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到40℃,氮气保护,搅拌12h后,离心、过滤,得到富勒烯油溶液。
实施例2 C60富勒烯油
将富勒烯粉末C60进行球磨细化0.05-1μm,再将细化后的富勒烯粉末5g与大豆油100g进行混合,置于球磨机中700转/分钟,球磨12h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到50℃,氮气保护,搅拌24h后,离心、过滤,得到富勒烯油溶液。
实施例3 C76富勒烯油
将富勒烯粉末C76进行球磨细化0.05-1μm,再将细化后的富勒烯粉末0.1与青刺果油10g进行混合,置于球磨机中1000转/分钟,球磨20h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到60℃,氮气保护,搅拌36h后,离心、过滤,得到富勒烯油溶液。
实施例4 Gd@C82富勒烯油
将富勒烯粉末Gd@C82进行球磨细化0.05-1μm,再将细化后的富勒烯粉末10g与橄榄油40g进行混合,置于球磨机中500-1000转/分钟,球磨8-20h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到40-60℃,氮气保护,搅拌12-72h后,离心、过滤,得到富勒烯油溶液。
实施例5 C60富勒烯油
将富勒烯粉末C60进行球磨细化0.05-1μm,再将细化后的富勒烯粉末3g与橄榄油30g进行混合,置于球磨机中500转/分钟,球磨80h,得到富勒烯油混悬液,再将
富勒烯油混悬液加热到40℃,氮气保护,搅拌12h后,离心、过滤,得到富勒烯油溶液。
实施例6 C70富勒烯油
将富勒烯粉末C70进行球磨细化0.05-1μm,再将细化后的富勒烯粉末3g与橄榄油30g进行混合,置于球磨机中500转/分钟,球磨80h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到40℃,氮气保护,搅拌12h后,离心、过滤,得到富勒烯油溶液。
实施例7 C76富勒烯油
将富勒烯粉末C76进行球磨细化0.05-1μm,再将细化后的富勒烯粉末3g与橄榄油20g进行混合,置于球磨机中500转/分钟,球磨80h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到40℃,氮气保护,搅拌12h后,离心、过滤,得到富勒烯油溶液。
实施例8 C60富勒烯油
将富勒烯粉末C60进行球磨细化0.05-1μm,再将细化后的富勒烯粉末5g与橄榄油25g进行混合,置于球磨机中500转/分钟,球磨80h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到40℃,氮气保护,搅拌12h后,离心、过滤,得到富勒烯油溶液。
实施例9 C70富勒烯油
将富勒烯粉末C70进行球磨细化0.05-1μm,再将细化后的富勒烯粉末1g与橄榄油15g进行混合,置于球磨机中500转/分钟,球磨80h,得到富勒烯油混悬液,再将富勒烯油混悬液加热到40℃,氮气保护,搅拌12h后,离心、过滤,得到富勒烯油溶液。
实施例 氨基富勒烯
实施例1:制备C60(EDA)9
(a)将50mL乙二胺(分析纯,国药试剂)加入100mL具塞锥形瓶,加入50mg固体富勒烯C60(纯度:99%,厦门福纳新材料科技有限公司),再加入磁力搅拌子,使用磁力搅拌器搅拌24h(温度:室温,转速:1000r/min),使用溶剂过滤器(容积:1L,滤膜孔径:200nm,津腾公司)将反应物抽滤后得到棕红色溶液。溶液的成分主要是未参加反应的乙二胺和C60(EDA)9。
(b)将(a)步骤得到的溶液加入250ml的圆底烧瓶中,再使用旋转蒸发仪(型号:IKA
RV10 basic)将滤液旋转干燥完全(温度:70摄氏度,转速:80r/min)。将稀盐酸(浓度:1mol/L)加入到圆底烧瓶中,振荡烧瓶使其内壁上的蒸干物溶解在稀盐酸中,得到棕红色澄清溶液。
(c)将(b)步骤得到的溶液使用NaOH水溶液(浓度:10mol/L)中和pH试纸检测为弱酸性(pH为5左右),以保证过量的乙二胺以氯化盐形式存在,能够在后续的透析步骤充分除去。将中和后溶液装入透析袋(截止分子量为3500)放入超纯水中透析,透析至超纯水的电导率小于1μs/cm即可。
(d)将(c)步骤透析后的溶液流经装有阴离子交换树脂(Ambersep900(OH),伊诺凯试剂公司)的层析柱,重复3次。将离子交换后溶液装入透析袋(截止分子量为3500)放入超纯水中透析透析至超纯水的电导率小于1μs/cm。溶液呈澄清的棕红色。
将棕红色溶液滴于银镜上,自然干燥后用于红外光谱(IR)测试。如图1所示,样品在3300nm左右的红外特征吸收(-NH2的伸缩振动吸收峰)证明乙二胺被键合到富勒烯的碳笼,同时在800-1500nm红外特征吸收(碳笼上C-C和C=C的伸缩振动峰)的变化也佐证乙二胺已经键合到碳笼上。将样品溶液滴于粘有碳导电胶的电子探针台上,自然干燥后用于电子束探针分析(EPMA),测试结果如图2(a)所示,经过阴离子交换后的样品中只存在CN元素(H无法被检测),说明键合的乙二胺是以本体形式而不是以氯化盐形式存在。将样品溶液直接用于动态光散射(DLS)测试,如图3所示,其水合粒径在100nm左右且表面带正电荷,适合被细胞捕获、吞噬。将样品冷冻干燥用于CHN元素分析(EA),随机在样品中选择2个位置,分析结果见表1,由N:C比例可以确定其化学组成为C60(EDA)9。通过调整(a)步骤中乙二胺和富勒烯的反应时间,可以调控键合的乙二胺的数量,获得C60(EDA)n,n=5-9。
表1:C60(EDA)9元素分析结果
实施例2:制备Gd@C82(EDA)8
反应条件以及步骤同实施例1,所不同的是,采用50mg金属富勒烯Gd@C82固体
(纯度:99%,厦门福纳新材料科技有限公司)替代C60。最终获得含有Gd@C82(EDA)8的澄清棕黑色溶液。采用与实施例1中相同的测试方法以及条件对获得的产品进行成分检测,如图1所示,样品在3300nm左右的红外特征吸收(-NH2的伸缩振动吸收峰)证明乙二胺被键合到富勒烯的碳笼,同时在800-1500nm红外特征吸收(碳笼上C-C和C=C的伸缩振动峰)的变化也佐证乙二胺已经键合到碳笼上。将样品溶液滴于粘有碳导电胶的电子探针台上,自然干燥后用于电子束探针分析(EPMA),测试结果如图2(b)所示,经过阴离子交换后的样品中只存在C、N、Gd元素(H无法被检测),说明键合的乙二胺是以本体形式而不是以氯化盐形式存在。将样品溶液直接用于动态光散射(DLS)测试,如图3所示,其水合粒径在100nm左右且表面带正电荷,适合被细胞捕获、吞噬。将样品冷冻干燥用于CHN元素分析(EA),随机在样品中选择2个位置,分析结果见表2,由N:C比例可以确定其化学组成为Gd@C82(EDA)8。通过调整乙二胺和金属富勒烯的反应时间,可以调控键合的乙二胺的数量,获得Gd@C82(EDA)n,n=6-8。使用等电感耦合等离子体原子发射光谱(ICP-AES)测试样品中Gd3+离子浓度(使用浓硝酸处理样品,将样品内的Gd酸解成Gd3+离子),可以确定溶液中样品浓度。
表2:Gd@C82(EDA)8元素分析结果
实施例3:制备Cm(EDA)9(m=70、76、78、84)
反应条件以及步骤同实施例1,所不同的是,采用50mg C70、C76、C78或者C84固体(纯度:99%,厦门福纳新材料科技有限公司)替代C60。
实施例4:制备M@C82(EDA)8(M=Y、Ho、Lu)
反应条件以及步骤同实施例1,所不同的是,采用50mg Y@C82、Ho@C82或者Lu@C82固体(纯度:99%,厦门福纳新材料科技有限公司)替代C60。
实施例5:制备M3N@C80(EDA)8(M=Sc、Y、Lu)
反应条件以及步骤同实施例1,所不同的是,采用50mg Sc3N@C80、Y3N@C80或
者Lu3N@C80固体(纯度:99%,厦门福纳新材料科技有限公司)替代C60。
实施例 羟基富勒烯
实施例1:制备羟基修饰的C60
(a)将7mL质量百分含量为30%的过氧化氢(分析纯,购于国药试剂)水溶液和3mL质量百分含量为40%的氢氧化钠(分析纯,国药试剂)加入100mL圆底烧瓶,加入200mg富勒烯C60固体(纯度:99%,厦门福纳新材料科技有限公司),再加入磁力搅拌子(型号:B200),使用磁力搅拌器搅拌24h(温度:70℃,转速:1000r/min),使用溶剂过滤器(容积:1L,滤膜孔径:200nm,津腾公司)过滤得到棕黄色溶液。
(b)将(a)步骤得到的溶液加入50ml的离心管中,再加入过量的浓度为95%的乙醇(分析纯,国药试剂)。经过离心(转速:10000r/min,时间:4min)后去除上层无色溶液,将收集的沉淀溶于超纯水中,得到黄色澄清溶液。
(c)将(b)步骤得到的溶液装入透析袋(截止分子量为3500)放入超纯水中透析,透析至超纯水的电导率小于1μs/cm,得到黄色溶液。
(d)将(c)步骤透析后的溶液装入50mL塑料离心管中,使用液氮冷冻后放入冷冻干燥机中冷冻干燥(温度:-29℃,真空度:55Pa,时间:48h),将得到的黄色固体装入棕色样品瓶中备用。
将固体样品溶于超纯水再滴于银镜上,自然干燥后用于红外光谱(IR)测试,如图4所示,样品在3400nm左右的红外特征吸收(-OH的伸缩振动吸收峰)证明羟基被键合到碳笼;同时在800-1500nm红外特征吸收(碳笼上C-C和C=C的伸缩振动峰)属于富勒烯碳笼的特征振动吸收峰;特征振动峰为1750nm-1归属于-C=O伸缩振动,这是由于-C-OH过度氧化或者频哪醇重排产生的。将固体样品直接用于X射线光电子能谱分析,如图5所示,对样品中C元素光电子能谱进行分峰拟合,键能为284.68eV的峰属于C-C和C=C,键能为285.91eV的峰属于C-O,键能为288.58eV的峰属于C=O,根据积分面积可以确定样品的化学组成是C60(O)5(OH)12。将样品溶液直接用于动态光散射(DLS)测试,如图6所示,样品水合粒径在145nm左右且表面带负电荷,能够长期稳定地存在于水溶液中。将固体样品用于CHN元素分析(EA),取样品中两个随机位置(1#以及2#)进行元素分析。结果见表3。根据表3中的C含量可以对样品中的羟基修饰的C60进行定量。
表3:羟基修饰的C60元素分析结果
通过调整(a)步骤中过氧化氢和C60的反应温度和反应时间,可以调控键合的羟基的数量(C60(O)5(OH)n,n=16-30)。
实施例2:制备羟基修饰的Cn(n=70、76、78、84)
制备方法和制备条件同实施例1,所不同的是,在步骤(a)中,分别采用C70、C76、C78以及C84替代C60。
实施例3:制备羟基修饰的金属富勒烯M@C82
制备方法和制备条件同实施例1。所不同的是,在步骤(a)中,分别采用Y@C82、Ho@C82、以及Lu@C82替代C60。
实施例4:制备羟基修饰的M3N@C80
制备方法和制备条件同实施例1。所不同的是,在步骤(a)中,分别采用Y3N@C82、Sc3N@C82、以及Lu3N@C82替代C60。
实施例:一种对抗头部感染,止痒防脱固发生发的组合物
实施例1:
一种对抗头部感染,止痒防脱固发生发的组合物是由亚麻籽油200g、沙棘油200g、山茶油200g、杜松油150g、天竺葵油g、薄荷醇100g、甘草提取物50g、红枣提取物70g、牡丹皮提取物50g、潘石榴提取物50g、积雪草提取物40g、川穹提取物50g、红茶提取物50g、植物甾醇30g、辣椒提取物0.7g、槐米提取物30g、生姜提取物20g、芦荟提取物30g、啤酒花提取物30g、墨旱莲提取物30g、当归提取物40g、银杏提取物30g、诺丽提取物30g、燕麦葡聚糖10g、肌醇40g、生育酚乙酸酯30g、生物素0.7g、富勒烯15g。
(1)将亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、生育酚乙酸酯充分混合均匀,将富勒烯粉末适度研磨后加入上述混合油相中,然后将加热融化后的薄荷醇加入其中,将混合好的油相40度条件下,减压搅拌,使各组分更好的在油相中溶解,为油相;
(2)取去离子水,向素,溶解搅拌均匀后超声,离心,取上清液,为水相;
(3)向油相中加入增溶剂,充分搅拌使得油相被完全增溶后,将水相加入其中,混合均匀即得本发明组合物。
实施例2
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油500g、沙棘油500g,山茶油500g、杜松油500g、天竺葵500g、薄荷醇500g、甘草提取物400g、红枣提取物400g、牡丹皮提取物400g、潘石榴提取物400g、积雪草提取物400g、川穹提取物400g、红茶提取物400g、植物甾醇200g、辣椒提取物200g、槐米提取物200g、生姜提取物200g、芦荟提取物200g、啤酒花提取物200g、墨旱莲提取物200g、当归提取物200g、银杏提取物200g、诺丽提取物200g、燕麦葡聚糖200g、肌醇300g、生育酚乙酸酯300g、生物素5g、富勒烯50g。制备方法按照实施例1。
实施例3
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油10g、沙棘油10g,山茶油10g、杜松油10g、天竺葵油10g、薄荷醇30g、甘草提取物1g、红枣提取物1g、牡丹皮提取物1g、潘石榴提取物1g、积雪草提取物1g、川穹提取物1g、红茶提取物1g、植物甾醇1g、辣椒提取物0.1g、槐米提取物1g、生姜提取物1g、芦荟提取物1g、啤酒花提取物1g、墨旱莲提取物1g、当归提取物1g、银杏提取物1g、诺丽提取物1g、燕麦葡聚糖1g、肌醇10g、生育酚乙酸酯10g、生物素0.1g、富勒烯1g。制备方法按照实施例1。
实施例4
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油50g、沙棘油50g、山茶油50g、杜松油50g、天竺葵油50g、薄荷醇50g、甘草提取物5g、红枣提取物5-g、牡丹皮提取物5g、潘石榴提取物5g、积雪草提取物5g、川穹提取物5g、红茶提取物5g、植物甾醇5g、辣椒提取物0.5g、槐米提取物5g、生姜提取物5g、芦荟提取物5g、啤酒花提取物5g、墨旱莲提取物5g、当归提取物5g、银杏提取物5g、诺丽提取物5g、燕麦葡聚糖5g、肌醇20g、生育酚乙酸酯10g、生物素0.3g、富勒烯5g。按照实施例1的方法制备。
实施例5
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油400g、沙棘油400g、山茶油400g、杜松油400g、天竺葵油400g、薄荷醇
400g、甘草提取物200g、红枣提取物200g、牡丹皮提取物200g、潘石榴提取物200g、积雪草提取物200g、川穹提取物200g、红茶提取物200g、植物甾醇100g、辣椒提取物100g、槐米提取物100g、生姜提取物100g、芦荟提取物100g、啤酒花提取物100g、墨旱莲提取物100g、当归提取物100g、银杏提取物100g、诺丽提取物100g、燕麦葡聚糖100g、肌醇200g、生育酚乙酸酯100g、生物素3g、富勒烯30g。制备方法按照实施例1。
实施例6
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油100g、沙棘油100g,山茶油100g、杜松油100g、天竺葵油100g、薄荷醇70g、甘草提取物10g、红枣提取物10g、牡丹皮提取物10g、潘石榴提取物10g、积雪草提取物10g、川穹提取物10g、红茶提取物10g、植物甾醇10g、辣椒提取物10g、槐米提取物10g、生姜提取物10g、芦荟提取物10g、啤酒花提取物10g、墨旱莲提取物10g、当归提取物10g、银杏提取物10g、诺丽提取物10g、燕麦葡聚糖5g、肌醇30g、生育酚乙酸酯20g、生物素0.5g、富勒烯10g。制备方法按照实施例1。
实施例7
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油300g、沙棘油300g、山茶油300g、杜松油300g、天竺葵油300g、薄荷醇200g、甘草提取物100g、红枣提取物100g、牡丹皮提取物100g、潘石榴提取物100g、积雪草提取物100g、川穹提取物100g、红茶提取物100g、植物甾醇50g、辣椒提取物10g、槐米提取物50g、生姜提取物50g、芦荟提取物50g、啤酒花提取物50g、墨旱莲提取物50g、当归提取物50g、银杏提取物50g、诺丽提取物50g、燕麦葡聚糖20g、肌醇100g、生育酚乙酸酯70g、生物素2g、富勒烯20g。按照实施例1方法制备。
实施例8
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油150g、沙棘油150g、山茶油150g、杜松油130g、天竺葵油150g、薄荷醇100g、甘草提取物20g、红枣提取物20g、牡丹皮提取物20g、潘石榴提取物20g、积雪草提取物20g、川穹提取物20g、红茶提取物20g、植物甾醇20g、辣椒提取物0.5g、槐米提取物10g、生姜提取物10g、芦荟提取物10g、啤酒花提取物10g、墨旱莲提取物10g、当归提取物10g、银杏提取物10g、诺丽提取物10g、燕麦葡聚糖50g、肌醇30g、生育酚乙酸酯20g、生物素0.5g、富勒烯10g。按照实施例1方法制备。
实施例9
一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油250g、沙棘油250g、山茶油250g、杜松油180g、天竺葵油250g、薄荷醇150g、甘草提取物70g、红枣提取物70g、牡丹皮提取物70g、潘石榴提取物70g、积雪草提取物70g、川穹提取物70g、红茶提取物70g、植物甾醇40g、辣椒提取物2g、槐米提取物50g、生姜提取物50g、芦荟提取物50g、啤酒花提取物50g、墨旱莲提取物50g、当归提取物50g、银杏提取物50g、诺丽提取物50g、燕麦葡聚糖20g、肌醇100g、生育酚乙酸酯70g、生物素2g、富勒烯20g。按照实施例1方法制备。
实施例10
取实施例1-9任意一项实施例的组合物制成乳剂,包括如下步骤:
(1)将亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、生育酚乙酸酯充分混合均匀,将富勒烯粉末适度研磨后加入上述混合油相中,然后将加热融化后的薄荷醇加入其中,将混合好的油相40度条件下,减压搅拌1h,使各组分更好的在油相中溶解,为油相;
(2)取去离子水,向其中加入甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物、燕麦葡聚糖、肌醇、生物素,溶解搅拌均匀后超声,离心,取上清液,然后向上清液中加入EDTA-2Na,静置24h,离心取上清液备用,为水相;
(3)将油相和水相混合后,加入增溶乳化剂LRI和磷脂,充分搅拌均质后形成乳液。
实施例11
取实施例1-9任意一个组合物制成喷雾剂,包括如下步骤:
1)将亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、植物甾醇,生育酚乙酸酯充分混合均匀,将富勒烯粉末适度研磨后加入上述混合油相中,然后将加热融化后的薄荷醇加入其中。将混合好的油相40度条件下,减压搅拌1h,使各组分更好的在油相中溶解,为油相;
(2)取去离子水,向其中加入甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏
提取物、诺丽提取物、燕麦葡聚糖、肌醇、生物素,溶解搅拌均匀后超声,离心,取上清液,然后向上清液中加入EDTA-2Na,静置24h,离心取上清液备用,为水相;
(3)向油相中加入增溶剂,充分搅拌使得油相被完全增溶后,将水相加入其中,充分均质后得到均匀透明的稳定液体,将此液体灌装入喷雾瓶中使用。
实施例 一种治疗脂溢性脱发的组合物
实施例1
一种治疗脂溢性脱发的组合物,取由下述重量份的原料备用:
牡丹皮提取物0.1g、侧柏叶提取物0.1g、迷迭香提取物0.1g、茶树提取物0.1g、当归提取物0.1g、黄芪提取物0.1g、墨旱莲提取物0.1g、鼠尾草提取物0.01g、锯棕榈提取物0.01g、啤酒花提取物0.01g、诺丽提取物0.01g、生物素0.01g、肌醇0.1g、水解小麦蛋白0.1g、燕麦葡聚糖0.1g、葡萄酸锌0.1g、薄荷0.1g、生物酚乙酸酯0.01g、富勒烯及其相应衍生物0.001g。
(1)取侧柏叶提取物,迷迭香提取物,茶树提取物,当归提取物,鼠尾草提取物,黄芪提取物混合均匀得混合物提取物;
(2)将富勒烯及其相应衍生物溶解于步骤(1)混合提取物中,再加入生育酚乙酸酯和薄荷醇得富勒烯混合物,然后用增溶剂进行增容,充分增容好后,放置过夜,过滤,取上清液I备用;
(3)将牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物混合均匀后,用水超声提取,然后离心过滤,上清液II备用;
(4)将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌溶解于水得溶液III;
(5)将上述上清液I、上清液II、溶液III混合均匀即可。
实施例2
一种治疗脂溢性脱发的组合物,取由下述重量份的原料备用:
牡丹皮提取物5g、侧柏叶提取物5g、迷迭香提取物5g、茶树提取物5g、当归提取物5g、黄芪提取物5g、墨旱莲提取物5g、鼠尾草提取物2g、锯棕榈提取物2g、啤酒花提取物2g、诺丽提取物2g、生物素0.05g、肌醇2g、水解小麦蛋白1g、燕麦葡聚糖1g、葡萄酸锌5g、薄荷5g、生物酚乙酸酯1g、富勒烯及其相应衍生物富勒烯3g。
(1)取侧柏叶提取物,迷迭香提取物,茶树提取物,当归提取物,鼠尾草提取物,黄芪提取物混合均匀得混合物提取物;
(2)将富勒烯及其相应衍生物溶解于步骤(1)混合提取物中,再加入生育酚乙酸酯和薄荷醇得富勒烯混合物,然后用增溶剂进行增容,充分增容好后,放置过夜,过滤,取上清液I备用;
(3)将牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物混合均匀后,用水超声提取,然后离心过滤,上清液II备用;
(4)将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌溶解于水得溶液III;
(5)将上述上清液I、上清液II、溶液III混合均匀即可。
实施例3
一种治疗脂溢性脱发的组合物,取由下述重量份的原料备用:牡丹皮提取物0.3g、侧柏叶提取物0.3g、迷迭香提取物0.2g、茶树提取物0.1g、当归提取物0.2g、黄芪提取物0.2g,墨旱莲提取物0.2g、鼠尾草提取物0.1g、锯棕榈提取物0.05g、啤酒花提取物0.05g、诺丽提取物0.1g、生物素0.01g、肌醇0.1g、水解小麦蛋白0.1g、燕麦葡聚糖0.1g、葡萄酸锌0.5g、薄荷1g、生育酚乙酸酯0.03g、富勒烯及其相应衍生物0.01g。
(1)取侧柏叶提取物,迷迭香提取物,茶树提取物,当归提取物,鼠尾草提取物,黄芪提取物混合均匀得混合物提取物;
(2)将富勒烯及其相应衍生物溶解于步骤(1)混合提取物中,再加入生育酚乙酸酯和薄荷醇得富勒烯混合物,然后用增溶剂进行增容,充分增容好后,放置过夜,过滤,取上清液I备用;
(3)将牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物混合均匀后,用水超声提取,然后离心过滤,上清液II备用;
(4)将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌溶解于水得溶液III;
(5)将上述上清液I、上清液II、溶液III混合均匀即可。
实施例4
一种治疗脂溢性脱发的组合物,取由下述重量份的原料备用:牡丹皮提取物3g、侧柏叶提取物3g、迷迭香提取物3g、茶树提取物3g、当归提取物2g、黄芪提取物2g、墨旱莲提取物2g、鼠尾草提取物2g、锯棕榈提取物1.5g、啤酒花提取物1.5g、诺丽提取物1g、生物素0.03g、肌醇1g、水解小麦蛋白0.5g、燕麦葡聚糖0.5g、葡萄酸3g、薄荷3g、生育酚乙酸酯0.06g、富勒烯及其相应衍生物2g。
(1)取侧柏叶提取物,迷迭香提取物,茶树提取物,当归提取物,鼠尾草提取物,
黄芪提取物混合均匀得混合物提取物;
(2)将富勒烯及其相应衍生物溶解于步骤(1)混合提取物中,再加入生育酚乙酸酯和薄荷醇得富勒烯混合物,然后用增溶剂进行增容,充分增容好后,放置过夜,过滤,取上清液I备用;
(3)将牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物混合均匀后,用水超声提取,然后离心过滤,上清液II备用;
(4)将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌溶解于水得溶液III;
(5)将上述上清液I、上清液II、溶液III混合均匀即可。
实施例5
一种治疗脂溢性脱发的组合物,取由下述重量份的原料备用:牡丹皮提取物0.3g、侧柏叶提取物0.3g、迷迭香提取物0.2g、茶树提取物0.1g、当归提取物0.2g、黄芪提取物0.2g,墨旱莲提取物0.2g、鼠尾草提取物0.1g、锯棕榈提取物0.08g、啤酒花提取物0.08g、诺丽提取物0.08g、生物素0.01g、肌醇0.1g、水解小麦蛋白0.2g、燕麦葡聚糖0.2g、葡萄酸锌2g、薄荷1g、生育酚乙酸酯0.03g、富勒烯及其相应衍生物0.01g。
(1)取侧柏叶提取物,迷迭香提取物,茶树提取物,当归提取物,鼠尾草提取物,黄芪提取物混合均匀得混合物提取物;
(2)将富勒烯及其相应衍生物溶解于步骤(1)混合提取物中,再加入生育酚乙酸酯和薄荷醇得富勒烯混合物,然后用增溶剂进行增容,充分增容好后,放置过夜,过滤,取上清液I备用;
(3)将牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物混合均匀后,用水超声提取,然后离心过滤,上清液II备用;
(4)将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌溶解于水得溶液III;
(5)将上述上清液I、上清液II、溶液III混合均匀即可。
实施例6
一种治疗脂溢性脱发的组合物是由牡丹皮提取物2.5g、侧柏叶提取物2.5g、迷迭香提取物2.5g、茶树提取物2g、当归提取物1.5g、黄芪提取物1.5g,墨旱莲提取物1.5g、鼠尾草提取物1.5g、锯棕榈提取物1.5g、啤酒花提取物1.5g、诺丽提取物1g、生物素0.03g、肌醇0.5g、水解小麦蛋白0.4g、燕麦葡聚糖0.4g、葡萄酸锌3g、薄荷3g、生育酚乙酸酯0.06g、富勒烯及其相应衍生物1g,制备方法按照实施例1。
实施例7
一种治疗脂溢性脱发的组合物是由牡丹皮提取物0.5g、侧柏叶提取物0.5g、迷迭香提取物0.5g、茶树提取物0.3g、当归提取物0.3g、黄芪提取物0.3g,墨旱莲提取物0.3g、鼠尾草提取物0.3g、锯棕榈提取物0.1g、啤酒花提取物0.1g、诺丽提取物0.5g、生物素0.01g、肌醇0.1g、水解小麦蛋白0.3g、燕麦葡聚糖0.3g、葡萄酸锌1g、薄荷2g、生物酚乙酸酯0.05g、富勒烯及其相应衍生物0.03g,按照实施例1方法制备。
实施例8
一种治疗脂溢性脱发的组合物是由牡丹皮提取物2g、侧柏叶提取物2g、迷迭香提取物2g、茶树提取物1g、当归提取物1g、黄芪提取物1g,墨旱莲提取物1g、鼠尾草提取物1g、锯棕榈提取物1g、啤酒花提取物1g、诺丽提取物1g、生物素0.01g、肌醇0.1g、水解小麦蛋白0.3g、燕麦葡聚糖0.3g、葡萄酸锌1g、薄荷2g、生物酚乙酸酯0.05g、富勒烯及其衍生物0.6g,按照实施例1方法制备。
实施例9:
一种治疗脂溢性脱发水凝胶剂包括牡丹皮植提物0.5%、侧柏叶植提物0.5%、迷迭香植提物0.5%、茶树植提物0.3%、当归植提物0.3%、锯棕榈植提物0.15%、墨旱莲植提物0.3%、鼠尾草植提物0.3%、啤酒花植提物0.1%、生物素0.01%、肌醇0.1%、水解小麦蛋白0.3%、燕麦葡聚糖0.3%、葡萄酸锌1%、1,3-丁二醇4%、羟乙基纤维素0.05%、柠檬酸0.3%、透明质酸3%、薄荷2%、生物酚乙酸酯0.5%、LRI-80 30%、EDTA-2Na 1%、吐温-80 35%、EDTA-2Na 0.5%、富勒烯及其相应衍生物6%等主要活性原料,去离子水补充到100%。
实施例10:
一种治疗脂溢性脱发水凝胶剂包括以下组分:所述配方包首乌植提物0.3%、牡丹皮植提物0.3%、侧柏叶植提物0.15%、黄芪植提物0.15%、诺丽植提物0.15%、当归植提物0.15%、锯棕榈植提物0.15%、芦荟植提物0.05%、生物素0.01%、肌醇0.1%、水解小麦蛋白0.3%、燕麦葡聚糖0.3%、葡萄酸锌1%、1,3-丁二醇4%、羟乙基纤维素0.05%、柠檬酸0.3%、透明质酸3%、薄荷2%、生物酚乙酸酯0.5%、LRI-80 20%、EDTA-2Na 1%、富勒烯及其相应衍生物4%等主要活性原料,去离子水补充到100%。
实施例11
一种治疗脂溢性脱发水凝胶剂包括下述组分:牡丹皮提取物0.5-2份、侧柏叶提
取物0.5-2份、迷迭香提取物0.5-2份、茶树提取物0.3-1份、当归提取物0.3-1份、黄芪提取物0.3-1份,墨旱莲提取物0.3-1份、鼠尾草提取物0.3-1份、锯棕榈提取物0.1-1份、啤酒花提取物0.1-1份、诺丽提取物0.5-1份、生物素0.01份、肌醇0.1份、水解小麦蛋白0.3份、燕麦葡聚糖0.3份、葡萄酸锌1份、薄荷2份、生物酚乙酸酯0.05份、富勒烯及其相应衍生物0.03-0.6份。1,3-丁二醇4份、羟乙基纤维素0.1份、柠檬酸0.3份、透明质酸1.5份、LRI 7份、EDTA-2Na 1份、去离子水补充至100%。
实施例12
一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物1g、侧柏叶提取物1g、迷迭香提取物1g、茶树提取物1g、当归提取物1g、黄芪提取物1g,墨旱莲提取物1g、鼠尾草提取物1g、锯棕榈提取物0.3g、啤酒花提取物0.7g、诺丽提取物0.8g、生物素0.01g、肌醇0.1g、水解小麦蛋白0.3g、燕麦葡聚糖0.3g、葡萄酸锌1g、薄荷2g、生物酚乙酸酯0.05g、富勒烯及其相应衍生物0.01g,制备方法按照实施例1。
实施例13
一种治疗脂溢性脱发的组合物,取由下述重量份的原料备用:牡丹皮提取物5g、侧柏叶提取物5g、迷迭香提取物5g、茶树提取物5g、当归提取物5g、黄芪提取物5g,墨旱莲提取物5g、鼠尾草提取物2g、锯棕榈提取物2g、啤酒花提取物2g、诺丽提取物2g、生物素0.05g、肌醇2g、水解小麦蛋白1g、燕麦葡聚糖1g、葡萄酸锌5g、薄荷5g、生物酚乙酸酯1g、富勒烯及其相应衍生10g,制备方法按照实施例1。
实施例14
一种治疗脂溢性脱发的组合物是由牡丹皮提取物2.5g、侧柏叶提取物2.5g、迷迭香提取物2.5g、茶树提取物2g、当归提取物1.5g、黄芪提取物1.5g,墨旱莲提取物1.5g、鼠尾草提取物1.5g、锯棕榈提取物1.5g、啤酒花提取物1.5g、诺丽提取物1g、生物素0.03g、肌醇0.5g、水解小麦蛋白0.4g、燕麦葡聚糖0.4g、葡萄酸锌3g、薄荷3g、生育酚乙酸酯0.06g、富勒烯及其相应衍生物5g,制备方法按照实施例1。
试验例一 富勒醇水溶液的生发试验
试验例1
药品:配制浓度为800ppm的C60(OH)22的水溶液。
方法:实验组取100微升上述配置的富勒醇水溶液均匀涂抹于C57雄鼠背部,并采取微针促渗的方式促渗,直至小鼠背部没有明显的药物残留。对照组用生理盐水代替富勒醇水溶液,其他处理相同。每隔一周比较空白组、对照组和实验组的差别,用药时间为两周。
结果:两周后小鼠背部毛发生长图如图7中图7E所示。由该图可以看出,实验组比对照组的毛发更茂盛、浓密、黑亮,效果良好;与空白组(图7H)对比,小鼠背部毛发数量明显增多。H&E染色的小鼠毛囊数量的组织学评价结果如图8所示,由图8A和图8B可以看出,与空白组相比,本发明采用浓度为800ppm的C60(OH)22溶液作用后的皮肤内毛囊数量明显增多,说明本发明富勒醇起到了促进毛发生长的效果。
试验例2
药品:配制浓度为1000ppm的C60(OH)22水溶液。
方法:实验组取100微升上述配置的富勒醇水溶液均匀涂抹于C57雄鼠背部,并采取微针促渗的方式促渗,直至小鼠背部没有明显的药物残留。对照组用生理盐水代替富勒醇水溶液,其他处理相同。每隔一周比较空白组、对照组和实验组的差别,用药时间为两周。
结果:两周后小鼠背部毛发生长图如图7中图7F所示。由该图可以看出,实验组比对照组的毛发更茂盛、浓密、黑亮,效果良好;与空白组(图7H)对比,小鼠背部毛发数量明显增多。
H&E染色的小鼠毛囊数量的组织学评价结果如图8所示,由图8A和图8C可以看出,与空白组相比,本发明采用浓度为1000ppm的C60(OH)22溶液作用后的皮肤内毛囊数量明显增多,说明本发明富勒醇起到了促进毛发生长的效果。
试验例3
药品:配制浓度为1500ppm的C60(OH)22水溶液。
方法:实验组取100微升上述配置的富勒醇水溶液均匀涂抹于C57雄鼠背部,并采取微针促渗的方式促渗,直至小鼠背部没有明显的药物残留。对照组用生理盐水代替富勒醇水溶液,其他处理相同。每隔一周比较空白组、对照组和实验组的差别,用药时间为两周。
结果:两周后小鼠背部毛发生长图如图7中图7G所示。由该图可以看出,实验组比对照组的毛发更茂盛、浓密、黑亮,效果良好;与空白组(图7H)对比,小鼠背部毛发数量明显增多。
H&E染色的小鼠毛囊数量的组织学评价结果如图8所示,由图8A和图8D可以看出,与空白组相比,本发明采用浓度为1500ppm的C60(OH)22溶液作用后的皮肤内毛囊数量明显增多,说明本发明富勒醇起到了促进毛发生长的效果。
由上述试验例1-3可以看出,富勒醇能够用于治疗脱发,用药两周后效果很明显,达到了快速生发的目的。
试验例二 头部毛囊血管内皮细胞生长因子促进剂的毛发生长试验
试验例1:含富勒烯油的促进剂
C57BL/6小黑鼠8周大,乙醚麻醉后,将按1:1比例混合的松香石蜡加热融化后涂抹于小鼠背部,待其冷却变硬后剥去,拔掉所有终止期毛发,诱导高度同步的生长期毛发发育,该毛囊与自发形成的生长期毛囊在形态上无差别。9天后其背部毛发生长完全。将小鼠分为4组,分别为C60-橄榄油组、橄榄油组、米诺地尔组、生理盐水组,每天背部涂抹150微升,14天后,取小鼠背部皮肤,采用Western Blot和RT-PCR方法检测VEGFR-2含量。
结果:图9 Western Blot检测可以看出,背部涂抹C60的小鼠VEGFR-2含量明显高于其他组;图10 RT-PCR检测可以看出,背部涂抹C60的小鼠,VEGFR-2含量明显高于其他组。
结论:本发明的富勒烯油的促进剂能够上调VEGFR-2含量,治疗脱发,对于雄性激素源性脱发及斑秃效果明显优于米诺地尔。
试验例2:氨基富勒烯促进剂
C57BL/6小黑鼠8周大,乙醚麻醉后,将按1:1比例混合的松香石蜡加热融化后涂抹于小鼠背部,待其冷却变硬后剥去,拔掉所有终止期毛发,诱导高度同步的生长期毛发发育,该毛囊与自发形成的生长期毛囊在形态上无差别。9天后其背部毛发生长完全。将小鼠分为3组,分别为氨基富勒烯组、米诺地尔组、生理盐水组,每天背部涂抹150微升,14天后,取小鼠背部皮肤,采用Western Blot和RT-PCR方法检测VEGFR-2含量。结果:附图11,氨基富勒烯组的Western Blot检测可以看出,背部涂抹氨基富勒烯的小鼠VEGFR-2含量明显高于其他组;附图12:RT-PCR检测可以看出,背部涂抹氨基富勒烯的小鼠,VEGFR-2含量明显高于其他组。
结论:本发明的氨基富勒烯促进剂能够上调VEGFR-2含量,治疗脱发,对于雄性激素源性脱发及斑秃效果明显优于米诺地尔。
试验例3:羟基富勒烯促进剂
C57BL/6小黑鼠8周大,乙醚麻醉后,将按1:1比例混合的松香石蜡加热融化后涂抹于小鼠背部,待其冷却变硬后剥去,拔掉所有终止期毛发,诱导高度同步的生长期毛发发育,该毛囊与自发形成的生长期毛囊在形态上无差别。9天后其背部毛发生长完全。将小鼠分为3组,分别为羟基富勒烯组、米诺地尔组、生理盐水组,每天背部涂抹150微升,14天后,取小鼠背部皮肤,采用Western Blot和RT-PCR方法检测VEGFR-2含量。结果:附图13说明:Western Blot检测可以看出,背部涂抹羟基富勒烯的小鼠VEGFR-2含量明显高于其他组;附图14说明:RT-PCR检测可以看出,背部涂抹羟基富勒烯的小鼠,VEGFR-2含量明显高于其他组。
结论:本发明的羟基富勒烯的促进剂能够上调VEGFR-2含量,治疗脱发,对于雄性激素源性脱发及斑秃效果明显优于米诺地尔。
由上述试验例1-3可以看出,富勒烯油、氨基富勒烯、羟基富勒烯能够用于治疗脱发,用药9天后效果很明显,达到了快速生发的目的,且能够上调VEGFR-2含量治疗脱发,对于雄性激素源性脱发及斑秃效果明显优于米诺地尔。
试验例三 感染性脂溢性脱发
试验例1动物实验
1.1实验方法
实验模型为脂溢性脱发模型,与普通脂溢性脱发模型不同的是,该实施例为了造成小鼠背部严重的感染,将丙酸睾酮的注射剂量大大提高,注射天数也相应延长。
C57/B6黑鼠,除空白组外,其余各组在小鼠背部平行于脊柱区的皮下注射丙酸睾酮造模,浓度为25mg/ml,注射计量7mg/kg/day,注射时间为6周。第五周后小鼠背部毛发出现不同程度的脱落,小鼠背部皮肤丙酸睾酮注射区出现严重红斑,糜烂,部分区域出现皮癣,毛发结块现象,从第42天开始,通过外用给药的方式进行治疗。实验分七组,
第一组.空白组不给药:正常喂养,不进行任何处理
第二组.模型组不给药:按上述脂溢性脱发模型步骤进行造模,不给予任何药物
第三组.组合物(一种对抗头部感染,止痒防脱固发生发的组合物的实施例1富勒烯C60)每天一次于脱毛区域:按上述脂溢性脱发模型步骤造模后,外用给药,涂抹于小鼠背部脱毛区域
第四组.纯富勒烯每天一次于脱毛区域:按上述脂溢性脱发模型步骤造模后,外用给药。由于富勒烯是粉末状态,并且溶解性较差,不能直接涂抹在小鼠背部,为了
将富勒烯能涂抹于小属背部,参考专利申请号200580049615.2的方法制备了C60-PVP复合物,已知的是富勒烯在此复合物中是活性物质,PVP是惰性的且无外用刺激性。将C60-PVP水溶液涂抹于小鼠背部脱毛区域来验证纯富勒烯的功效
第五组.植提物混合物(仅不含有富勒烯及其衍生物)每天一次于脱毛区域:将生育酚乙酸酯和薄荷醇,植物甾醇溶解于亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油的混合物中,利用增溶剂进行增溶,然后将增溶后的水溶液和植提物(甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物)和燕麦葡聚糖、肌醇、生物素的水溶液混合,将混合物涂抹于小鼠背部脱毛区域
第六组.3%米诺地尔(阳性对照组)每天一次于脱毛区域
第七组.生理盐水组每天一次于脱毛区域
第10周时停止实验,取血及小鼠背部皮肤进行生化指标及病理分析
2、结果
2.1病理分析:由图15七组实验的小鼠背部病例H&E染色图片可以看出,本专利组合物的在给模型小鼠使用后,小鼠背部毛皮的毛囊黑色素含量高,毛囊数量多,健康状况和空白组接近,效果远远优于纯富勒烯组、植提物组、米诺地尔组,充分说明了本发明的组合物的也就是加入富勒烯后对中药提取物产生了协调作用,在生发抗炎活化细胞激活毛囊的作用效果明显。
2.2用睾酮试剂盒对各组小鼠血清中激素水平测定,结果见表4
表4各组小鼠血清测试结果,用睾酮试剂盒进行测试各组激素水平
分组 | N | T(μmol/L) |
空白组 | 10 | 0.6928±0.0211 |
本专利组合物组 | 9 | 1.9039±0.0231 |
纯富勒烯组 | 9 | 2.3739±0.0331 |
植提物组(不含富勒烯) | 10 | 3.9327±0.0303 |
米诺地尔组 | 10 | 3.5119±0.0311 |
生理盐水组 | 10 | 4.2003±0.0291 |
模型组(不给药) | 8 | 4.1339±0.0211 |
从表4中可以得知本专利组合物组的小鼠睾酮激素水平要明显低于模型组和米诺地尔组,说明本发明的组合物具有降低睾酮激素水平,可预防或治疗脱发的作用。本发明的组合物降低睾酮激素水平的作用明显高于纯富勒烯组、植提物组的降低睾酮激素水平作用具有协同作用,充分说明了本发明的组合物对于脂溢性脱发的显著效果。
试验例2:临床病例
付某,男,37岁,多年头皮脓包导致头皮感染,引起局部脱发,平时以药物缓解,但是副作用较大,故停药。使用本组合物产品实施例3,15天后,起到明显效果,头皮脓包萎缩,脱发部位重新长出毛发,患者身心愉悦。
岳某,50岁,常年头皮屑较多,头皮瘙痒,头顶部毛发稀少,使用几款纯中药配方后,效果不明显,遂放弃治疗,严重影响患者精神面貌。使用本产品(实施例6)14天后,瘙痒症状明显减轻,20天后,头屑基本不再有,头顶部毛发变黑变多变粗。
综上所述,上述试验例1,2可见,加入富勒烯后对中药提取物产生了协调作用,在生发抗炎活化细胞激活毛囊的作用效果明显。本发明的组合物具有降低睾酮激素水平,作用明显高于纯富勒烯组、植提物组的降低睾酮激素水平作用具有协同作用,充分说明了本发明的组合物对于脂溢性脱发的显著效果。本发明的组合物对抗头部感染,止痒防脱生发,该组合物不仅能够消除瘙痒和头屑,还能治疗细菌感染性脱发,促进脱发患者生出新发。
试验例四 遗传性脂溢性脱发的治疗
试验例1脂溢性脱发的治疗
1.1实验方法
实验模型为脂溢性脱发模型:C57/B6黑鼠,除空白组外,其余各组在小鼠背部平行于脊柱区的皮下注射丙酸睾酮造模,浓度为25mg/ml,注射计量5mg/kg/day,注射时间为五周。第五周后小鼠背部毛发出现不同程度的脱落,小鼠背部皮肤丙酸睾酮注射区出现红斑,糜烂,毛发结块现象,从第36天开始,通过外用给药的方式进行治疗。第9周时停止实验,取血及小鼠背部皮肤进行生化指标及病理分析。
1.2实验分组
第一组.空白组不给药:正常喂养,不进行任何处理;
第二组.模型组不给药:按上述脂溢性脱发模型步骤进行造模,不给予任何药物;
第三组.一种治疗脂溢性脱发的组合物实施例7组合物每天一次于脱毛区域:按上述脂溢性脱发模型步骤造模后,外用给药,涂抹于小鼠背部脱毛区域;
第四组.纯富勒烯每天一次于脱毛区域:按上述脂溢性脱发模型步骤造模后,外用给药。由于富勒烯是粉末状态,并且溶解性较差,不能直接涂抹在小鼠背部,为了将富勒烯能涂抹于小鼠背部,参考专利申请号200580049615.2的方法制备了C60-PVP复合物,已知的是富勒烯在此复合物中是活性物质,PVP是惰性的且无外用刺激性。将C60-PVP水溶液涂抹于小鼠背部脱毛区域来验证纯富勒烯的功效;
第五组.植提物混合物(不含有富勒烯及其衍生物富勒烯C60)每天一次于脱毛区域:将生育酚乙酸酯和薄荷醇溶解于侧柏油,迷迭香精油,茶树油,当归精油,鼠尾草精油的混合物中,利用增溶剂进行增溶,然后将增溶后的水溶液和植提物(牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物分散于水中)的水溶液混合,再与将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌水溶液混合即可;
第六组.3%米诺地尔(阳性对照组)每天一次于脱毛区域;
第七组.生理盐水组每天一次于脱毛区域;
3结果
3.1病理分析:由图16七组实验的小鼠背部病例H&E染色图片,可以看出不同实验组的小鼠背部毛皮内毛囊的状况,组合物的在给模型小鼠使用后,小鼠背部毛皮的毛囊黑色素含量高,毛囊数量多,健康状况和空白组接近,效果远远优于纯富勒烯组、植提物组、米诺地尔组,充分说明了本发明的组合物的也就是加入富勒烯后对中药提取物产生了协调作用,在生发抗炎活化细胞激活毛囊的作用效果明显。
3.2用睾酮试剂盒对各组小鼠血清中激素水平测定,结果见表5
表5各组小鼠血清测试结果,用睾酮试剂盒进行测试各组激素水平
分组 | N | 睾酮T(μmol/L) |
空白组 | 10 | 0.6528±0.0201 |
本专利组合物组 | 9 | 1.3339±0.0291 |
纯富勒烯组 | 9 | 1.9739±0.0311 |
植提物组(不含富勒烯) | 8 | 2.9327±0.0373 |
米诺地尔组 | 10 | 3.1119±0.0300 |
生理盐水组 | 8 | 3.2003±0.0391 |
模型组(不给药) | 8 | 3.1339±0.0311 |
从表5中可以得知,本专利组合物组的小鼠睾酮激素水平要明显低于模型组和米诺地尔组,说明本发明的组合物具有降低睾酮激素水平,可预防或治疗脱发的作用。本发明的组合物降低睾酮激素水平的作用明显高于纯富勒烯组、植提物组的降低睾酮激素水平作用具有协同作用,充分说明了本发明的组合物对于脂溢性脱发的显著效果。
试验例2临床病例:
固某,男,48岁。患者秃发5年左右。家族遗传性脱发,并因个人工作压力大,熬夜加班,饮食偏肉食较多,喜饮酒,采用较多方法后无明显效果,通过试用本发明药剂(实施例3)后7天头发长出,15天后明显看出秃发部位所长头发变黑变粗。见效后,提高了患者的信息,主动调节工作作息时间,按时睡眠,多做室外运动,减少肉的摄入,不再饮酒。本发明的组合物具有治疗遗传性脱发作用。
孙某,男,50岁,患者秃发10年左右。为典型的油性皮肤。其前额和头顶为甚,毛发干枯,伴面色少华,神疲乏力,爪甲不荣,失眠多梦,试用本发明药剂(实施例5)后11天观察,秃发有头发长出,30天后秃发部位变黑变粗,并且夜寐安,精神足,心情悦。本发明的组合物具有抗炎作用,对脂溢性脱发有疗效。
试验例3雄激素依赖性的遗传性脱发病的治疗
收集雄激素性脱发(AGA)有家族史即雄激素依赖性的遗传性脱发病例,经过通过对不同年龄段人群进行了统计见附图17:年龄在40-50岁之间50人试用(实施例8),经过7-15天试用后,有47人成功长出新发;年龄在50-60岁之间40人试用,经过7-15天试用后,有35人成功长出新发;年龄在60以上岁40人试用,经过7-15天试
用后,有30人成功长出新发;可见,对于遗传性脱发,本发明组合物整体有效率达到86%以上。从中我们可以得出,脱发部位经过长年暴露在外面,头皮角质层普遍偏厚,对药物的渗透有较大的屏障作用,药物不易透皮吸收,因此对于药物的渗透产生差异。对于没有达到预期的患者可以通过增加用药量来得以实现。
综上所述,上述试验例1-3结果可见,加入富勒烯后对中药提取物产生了协调作用,在生发抗炎活化细胞激活毛囊的作用效果明显。本发明的组合物具有降低睾酮激素水平,作用明显高于纯富勒烯组、植提物组的降低睾酮激素水平作用具有协同作用,充分说明了本发明的组合物对于脂溢性脱发的显著效果。对于雄激素依赖性的遗传性脱发病,用药后1周即可长出新发。对于遗传性脱发,用药后7天头发长出,15天后明显看出秃发部位所长头发变黑变粗。
本发明权利要求书范围及所有实施例都具有上述试验例效果,具有治疗脂溢性脱发及遗传性脱发作用,促进毛发生长的作用。
本发明公开一种富勒烯及其衍生物在制备促进毛发生长产品中的应用,所述富勒烯及其衍生物能够促进头部毛囊血管内皮细胞生长因子表达。治疗毛囊血管内皮细胞生长因子下降所导致的脱发,尤其是雄激素性脱发、斑秃、脂溢性脱发。所述促进毛发生长产品为头部毛囊血管内皮细胞生长因子促进剂、养发剂、护发剂、防脱剂和生发剂中的至少一种,富勒烯及其衍生物为油、水溶液或和与中药提取物的组合物中任一种形式,所述头部毛囊血管内皮细胞生长因子促进剂为富勒烯油、氨基富勒烯、羟基富勒烯中一种或几种,水溶性富勒烯衍生物为空心富勒醇和/或金属富勒醇、氨基富勒烯、羟基富勒烯;还公开一种对抗头部感染,止痒防脱固发生发和一种治疗脂溢性脱发的的含有富勒烯及其衍生物的中药组合物。
Claims (42)
- 一种富勒烯及其衍生物在制备促进毛发生长产品中的应用。
- 如权利要求1所述的应用,其特征在于,所述促进毛发生长产品为治疗脱发的促进毛发生长产品。
- 如权利要求2所述的应用,其特征在于,所述脱发包括雄激素性脱发、斑秃、脂溢性脱发,优选雄激素性脱发和斑秃。
- 如权利要求2所述的应用,其特征在于,所述脱发是由头部毛囊血管内皮细胞生长因子下降导致的。
- 如权利要求4所述的应用,其特征在于,所述富勒烯及其衍生物上调毛囊血管内皮细胞生长因子VEGF含量,优选上调毛囊血管内皮细胞生长因子VEGFR-2含量。
- 如权利要求1所述的应用,其特征在于,富勒烯衍生物为水溶性富勒烯衍生物。
- 如权利要求1所述的应用,其特征在于,所述促进毛发生长产品为头部毛囊血管内皮细胞生长因子促进剂、养发剂、护发剂、防脱剂和生发剂中的至少一种。
- 如权利要求1所述的应用,其特征在于,所述促进毛发生长产品为水溶性富勒烯衍生物的水溶液。
- 如权利要求6或8所述的应用,其特征在于,所述水溶性富勒烯衍生物,包括羟基富勒烯、氨基富勒烯、空心富勒醇和/或金属富勒醇。
- 如权利要求8所述的应用,其特征在于,所述水溶性富勒烯衍生物的水溶液的质量浓度可为100~10000ppm;优选800~1500ppm;更优选800ppm、1000ppm或1500ppm。
- 如权利要求8所述的应用,其特征在于,所述促进毛发生长产品为空心富勒醇和/或金属富勒醇的水溶液。
- 如权利要求11所述的应用,所述空心富勒醇和/或金属富勒醇的水溶液质量浓度可为100~10000ppm;优选800~1500ppm;更优选800ppm、1000ppm或1500ppm。
- 如权利要求11所述的应用,其特征在于,所述空心富勒醇的本体材料为C2n;所述金属富勒醇的本体材料为M@C2n、M2@C2n和MA@C2n中的任一种,其中,M和A均为金属元素,所述M和A均选自Sc、Y和镧系金属元素中的任意一种;30≤n≤60。
- 如权利要求11所述的应用,其特征在于,所述空心富勒醇和/或金属富勒醇中的羟基可为15~35个,优选22个。
- 如权利要求1所述的应用,其特征在于,所述促进毛发生长产品为一种头部毛囊血管内皮细胞生长因子促进剂,其包含富勒烯油、氨基富勒烯水溶液、羟基富勒烯水溶液一种或几种。
- 如权利要求15所述的应用,其特征在于,所述富勒烯油是由富勒烯与油组成。
- 如权利要求15所述的应用,其特征在于,氨基富勒烯是Cm(EDA)n;M@Cm(EDA)n,(M=Gd、Y、Ho、Lu);M3N@Cm(EDA)n(M=Sc、Y、Lu)中的任一种;其中m=60、70、76、78、82、84,n=5-9。
- 如权利要求15所述的应用,其特征在于,所述羟基富勒烯是Cm(O)5(OH)n;M3N@Cm(O)5(OH)n,(M=Sc、Y、Lu);M@Cm(O)5(OH)n,(M=Gd、Y、Ho、Lu)中的任一种;其中m=60、70、76、78、84,n=16-30。
- 如权利要求16所述的应用,其特征在于,所述富勒烯油,其中富勒烯在富勒烯油中浓度为0.01-20mg/ml;进一步优选所述富勒烯油中富勒烯浓度0.1mg/mL-15mg/mL;进一步优选,所述富勒烯油中富勒烯浓度1-10mg/ml。
- 如权利要求16所述的应用,其特征在于,所述的富勒烯油中富勒烯为空心富勒烯和/或金属富勒烯,包括富勒烯C2n、M@C2n、M2@C2n、MA@C2n、M3N@C2n、M2C2@C2n、M2S@C2n、M2O@C2n和MxA3-xN@C2n中的任一种,其中,M和A均为金属元素,所述M和A均选自Sc、Y和镧系金属元素中的任意一种;30≤n≤60;0≤x≤3;进一步优选所述富勒烯选择C60、C70、C76、C84,Gd@C82,SC3N@C80一种或以上的混合物。
- 如权利要求16所述的应用,其特征在于,所述的油包括植物种子,花朵,根茎等的提取物,包括橄榄油,大豆油、亚麻籽油,青刺果油,油菜籽油,甜杏仁油,葵花油,红花籽油,葡萄籽油,月见草油,琉璃苣籽油,当归油,生姜油,荷荷巴油,核桃油,鳄梨油,芒果油,蓖麻油,杏仁油,乳木果油,玫瑰果油,椰子油,棕榈油,谷糠油,小麦胚芽油,金盏花油,芦荟油,棕榈油,甜杏仁油,玉米油,葡萄籽油等一种或几种的混合物;进一步优选油为橄榄油。
- 如权利要求15所述的应用,其特征在于,所述富勒烯油的制备:将富勒烯末与油充分混合均匀后,置于球磨机中,超声、搅拌、加热,使富勒烯在油中充分溶解,过滤得到富勒烯油。
- 如权利要求9或17所述的应用,其特征在于所述氨基富勒烯是通过下述方法制 备得到:(a)将有机胺溶液与固体富勒烯混合,在室温搅拌或加热搅拌回流条件下进行反应,其中,有机胺包括乙二胺、丙胺、丙醇胺、对苯二胺和二乙醇胺的至少之一;固体富勒烯包括空心富勒烯C2n、金属富勒烯M@C2n、M2@C2n、MA@C2n、M3N@C2n、M2C2@C2n、M2S@C2n、M2O@C2n和MxA3-xN@C2n中的至少之一,其中,M和A分别独立的选自Sc、Y和镧系金属元素,30≤n≤60,0≤x≤3;(b)将步骤(a)得到的溶液旋转干燥,用稀酸溶液溶解旋转干燥后的剩余固体,其中,稀酸溶液为无机酸溶液,稀酸溶液的浓度为0.5~1.5mmol/L;(c)调节步骤(b)得到的溶液的pH值为4~6,透析至溶液的电导率小于1μs/cm;(d)利用阴离子交换树脂处理步骤(c)得到的溶液,透析至溶液的电导率小于1μs/cm。
- 如权利要求9或18所述的应用,其特征在于,所述羟基富勒烯是由下述方法制备得到:将固体富勒烯与过氧化氢溶液以及碱溶液混合反应,其中,碱溶液包括氢氧化钠水溶液、氢氧化钾水溶液以及四丁基氢氧化铵水溶液的至少之一,固体富勒烯包括空心富勒烯C2n、M@C2n、M2@C2n、MA@C2n、M3N@C2n、M2C2@C2n、M2S@C2n、M2O@C2n和MxA3-xN@C2n中的至少之一,其中,M和A分别独立的选自Sc、Y和镧系金属元素,30≤n≤60,0≤x≤3;所述碱溶液中碱的含量为8~15wt%;基于所述过氧化氢溶液的总质量,所述过氧化氢溶液中过氧化氢的含量为20~40wt%;所述混合溶液中所述过氧化氢以及所述碱溶液的体积比为7:(1~4);所述反应是在加热搅拌处理下进行的,所述加热搅拌处理的加热温度为50~80摄氏度,搅拌速率为600~1500rpm/min,时间为15~36小时,对经过所述反应的所述混合溶液进行提纯处理。
- 如权利要求24所述的应用,其特征在于,所述羟基富勒烯是由下述方法制备得到:(a)将质量百分含量为30%的过氧化氢水溶液和质量百分含量为40%的氢氧化钠溶液按照体积比为7:3加入100mL圆底烧瓶,加入200mg富勒烯固体,使用磁力搅拌器搅拌24h,温度:70℃,转速:1000r/min,过滤,保留滤液;(b)将滤液加离心管中,再加入过量的浓度为95%的乙醇;经过离心后收集沉淀,离心转速:10000r/min,离心时间:4min,将沉淀溶于水;(c)将(b)步骤得到的溶液进行透析处理,透析至溶液的电导率小于1μs/cm;(d)将透析后的溶液冷冻干燥,以便获得羟基富勒烯固体;冻干温度:-29℃,真 空度:55Pa,冻干时间:48h。
- 如权利要求1所述的应用,其特征在于,所述促进毛发生长产品一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油10-500份、沙棘油10-500份、山茶油10-500份、杜松油10-500份、天竺葵油10-500份、薄荷醇30-500份、甘草提取物1-400份、红枣提取物1-400份、牡丹皮提取物1-400份、潘石榴提取物1-400份、积雪草提取物1-400份、川穹提取物1-400份、红茶提取物1-400份、植物甾醇1-200份、辣椒提取物0.1-200份、槐米提取物1-200份、生姜提取物1-200份、芦荟提取物1-200份、啤酒花提取物1-200份、墨旱莲提取物1-200份、当归提取物1-200份、银杏提取物1-200份、诺丽提取物1-200份、燕麦葡聚糖1-200份、肌醇10-300份、生育酚乙酸酯10-300份、生物素0.1-5份、富勒烯1-50份。
- 如权利要求26所述的应用,其特征在于,所述一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油50-400份、沙棘油50-400份,山茶油50-400份、杜松油50-400份、天竺葵油50-400份、薄荷醇50-400份、甘草提取物5-200份、红枣提取物5-200份、牡丹皮提取物5-200份、潘石榴提取物5-200份、积雪草提取物5-200份、川穹提取物5-200份、红茶提取物5-200份、植物甾醇5-100份、辣椒提取物0.5-100份、槐米提取物5-100份、生姜提取物5-100份、芦荟提取物5-100份、啤酒花提取物5-100份、墨旱莲提取物5-100份、当归提取物5-100份、银杏提取物5-100份、诺丽提取物5-100份、燕麦葡聚糖5-100份、肌醇20-200份、生育酚乙酸酯10-100份、生物素0.3-3份、富勒烯5-30份。
- 如权利要求27所述的应用,其特征在于,所述一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油100-300份、沙棘油100-300份、山茶油100-300份、杜松油100-300份、天竺葵油100-300份、薄荷醇70-200份、甘草提取物10-100份、红枣提取物10-100份、牡丹皮提取物10-100份、潘石榴提取物10-100份、积雪草提取物10-100份、川穹提取物10-100份、红茶提取物10-100份、植物甾醇10-50份、辣椒提取物0.5-10份、槐米提取物10-50份、生姜提取物10-50份、芦荟提取物10-50份、啤酒花提取物10-50份、墨旱莲提取物10-50份、当归提取物10-50份、银杏提取物10-50份、诺丽提取物10-50份、燕麦葡聚糖5-20份、肌醇30-100份、生育酚乙酸酯20-70份、 生物素0.5-2份、富勒烯10-20份。
- 如权利要求28所述的应用,其特征在于,所述一种对抗头部感染,止痒防脱固发生发的组合物,其是由下述重量份的原料制得:亚麻籽油150-250份、沙棘油150-250份、山茶油150-250份、杜松油130-180份、天竺葵油150-250份、薄荷醇100-150份、甘草提取物20-70份、红枣提取物20-70份、牡丹皮提取物20-70份、潘石榴提取物20-70份、积雪草提取物20-70份、川穹提取物20-70份、红茶提取物20-70份、植物甾醇20-40份、辣椒提取物0.5-2份、槐米提取物10-50份、生姜提取物10-50份、芦荟提取物10-50份、啤酒花提取物10-50份、墨旱莲提取物10-50份、当归提取物10-50份、银杏提取物10-50份、诺丽提取物10-50份、燕麦葡聚糖5-20份、肌醇30-100份、生育酚乙酸酯20-70份、生物素0.5-2份、富勒烯10-20份。
- 如权利要求26-29任意一项所述的应用,其特征在于,所述组合物可以制成药学或保健或日化可接受的剂型。
- 如权利要求30所述的应用,其特征在于,所述剂型为乳剂、喷雾剂,其组合物与辅料重量比(1-5):(5-10)。
- 如权利要求31所述的应用,其特征在于,所述一种对抗头部感染,止痒防脱固发生发乳剂是通过下述方法制备得到:(1)将亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、生育酚乙酸酯充分混合均匀,将富勒烯粉末适度研磨后加入上述混合油相中,然后将加热融化后的薄荷醇加入其中,将混合好的油相40摄氏度条件下,减压搅拌1h,使各组分更好的在油相中溶解,为油相;(2)取去离子水,向其中加入甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物、燕麦葡聚糖、肌醇、生物素,溶解搅拌均匀后超声,离心,取上清液,然后向上清液中加入EDTA-2Na,静置24h,离心取上清液备用,为水相;(3)将油相和水相混合后,加入增溶乳化剂LRI和磷脂,充分搅拌均质后形成乳液。
- 如权利要求31所述的应用,其特征在于,一种对抗头部感染,止痒防脱固发生 发喷剂是由下述方法制备得到:(1)将亚麻籽油、沙棘油、山茶油、杜松油、天竺葵油、植物甾醇,生育酚乙酸酯充分混合均匀,将富勒烯粉末适度研磨后加入上述混合油相中,然后将加热融化后的薄荷醇加入其中;将混合好的油相40摄氏度条件下,减压搅拌1h,使各组分更好的在油相中溶解,为油相;(2)取去离子水,向其中加入甘草提取物、红枣提取物、牡丹皮提取物、潘石榴提取物、积雪草提取物、川穹提取物、红茶提取物、植物甾醇、辣椒提取物、槐米提取物、生姜提取物、芦荟提取物、啤酒花提取物、墨旱莲提取物、当归提取物、银杏提取物、诺丽提取物、燕麦葡聚糖、肌醇、生物素,溶解搅拌均匀后超声,离心,取上清液,然后向上清液中加入EDTA-2Na,静置24h,离心取上清液备用,为水相;(3)向油相中加入增溶剂,充分搅拌使得油相被完全增溶后,将水相加入其中,充分均质后得到均匀透明的稳定液体,将此液体灌装入喷雾瓶中使用。
- 如权利要求26-29任意一项所述的应用,其特征在于,所述组合物在制备预防或治疗脂溢性脱发产品、治疗头皮炎症产品、治疗止痒止屑产品中的应用。
- 如权利要求1所述的应用,其特征在于,所述促进毛发生长产品是一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物0.1-5份、侧柏叶提取物0.1-5份、迷迭香提取物0.1-5份、茶树提取物0.1-5份、当归提取物0.1-5份、黄芪提取物0.1-5份,墨旱莲提取物0.1-5份、鼠尾草提取物0.01-2份、锯棕榈提取物0.01-2份、啤酒花提取物0.01-2份、诺丽提取物0.01-2份、生物素0.01-0.05份、肌醇0.1-2份、水解小麦蛋白0.1-1份、燕麦葡聚糖0.1-1份、葡萄酸锌0.1-5份、薄荷0.1-5份、生物酚乙酸酯0.01-1份、富勒烯及其相应衍生物0.001-10份。
- 如权利要求35所述的应用,其特征在于,一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物0.3-2.5份、侧柏叶提取物0.3-2.5份、迷迭香提取物0.2-2.5份、茶树提取物0.1-2份、当归提取物0.2-1.5份、黄芪提取物0.2-1.5份,墨旱莲提取物0.2-1.5份、鼠尾草提取物0.1-1.5份、锯棕榈提取物0.08-1.5份、啤酒花提取物0.08-1.5份、诺丽提取物0.08-1份、生物素0.01-0.03份、肌醇0.1-0.5份、水解小麦蛋白0.2-0.4份、燕麦葡聚糖0.2-0.4份、葡萄酸锌2-3份、薄荷1-3份、生育酚乙酸酯0.03-0.06份、富勒烯 及其相应衍生物0.01-2份。
- 如权利要求36所述的应用,其特征在于,一种治疗脂溢性脱发的组合物,其是由下述重量份的原料制得:牡丹皮提取物0.5-2份、侧柏叶提取物0.5-2份、迷迭香提取物0.5-2份、茶树提取物0.3-1份、当归提取物0.3-1份、黄芪提取物0.3-1份,墨旱莲提取物0.3-1份、鼠尾草提取物0.3-1份、锯棕榈提取物0.1-1份、啤酒花提取物0.1-1份、诺丽提取物0.5-1份、生物素0.01份、肌醇0.1份、水解小麦蛋白0.3份、燕麦葡聚糖0.3份、葡萄酸锌1份、薄荷2份、生物酚乙酸酯0.05份、富勒烯及其相应衍生物0.03-0.6份。
- 如权利要求35-37任意一项所述的应用,其特征在于,所述组合物可以制成药学或保健或日化可接受的剂型。
- 如权利要求38所述的应用,其特征在于,所述剂型为水凝胶剂,其组合物与基质重量比(1-5):(5-10),优选3-5:5-7。
- 如权利要求39所述的应用,其特征在于,一种治疗脂溢性脱发水凝胶剂,其包括下述重量份的原料制成:牡丹皮提取物0.1-5份、侧柏叶提取物0.1-5份、迷迭香提取物0.1-5份、茶树提取物0.1-5份、当归提取物0.1-5份、黄芪提取物0.1-5份,墨旱莲提取物0.1-5份、鼠尾草提取物0.01-2份、锯棕榈提取物0.01-2份、啤酒花提取物0.01-2份、诺丽提取物0.01-2份、生物素0.01-0.05份、肌醇0.1-2份、水解小麦蛋白0.1-1份、燕麦葡聚糖0.1-1份、葡萄酸锌0.1-5份、薄荷0.1-5份、生物酚乙酸酯0.01-1份、富勒烯及其相应衍生物0.001-10份、1,3-丁二醇0.1%-10份、羟乙基纤维素0.01-1份、柠檬酸0.01-1份、透明质酸0.1-10份、LRI 3-20份、EDTA-2Na 0.01-1份,去离子水补充至100%。
- 如权利要求35-37任意一项所述的应用,其特征在于,所述组合物是由下述制备方法得到的:(1)取侧柏叶提取物,迷迭香提取物,茶树提取物,当归提取物,鼠尾草提取物,黄芪提取物混合均匀得混合物提取物;(2)将富勒烯及其相应衍生物加入步骤(1)混合提取物中,再加入生育酚乙酸酯和薄荷醇得富勒烯混合物,然后用增溶剂进行增容,放置过夜,过滤,取上清液I备用;(3)将牡丹皮提取物,墨旱莲提取物,锯棕榈提取物,啤酒花提取物,诺丽提取物混合均匀后,用水超声提取,然后离心过滤,上清液II备用;(4)将生物素,肌醇,水解小麦蛋白,燕麦葡聚糖,葡糖酸锌溶解于水得溶液III;(5)将上述上清液I、上清液II、溶液III混合均匀即可。
- 如权利要求35-37任意一项所述的应用,其特征在于,所述的组合物在制备预防或治疗脂溢性脱发产品、雄激素依赖性的遗传性脱发产品中的应用。
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CN201611155549.3A CN106474447A (zh) | 2016-12-14 | 2016-12-14 | 一种对抗头部感染,止痒防脱的组合物及其制备方法和应用 |
CN201611155549.3 | 2016-12-14 | ||
CN201611155550.6A CN107334894A (zh) | 2016-12-14 | 2016-12-14 | 一种治疗脂溢性脱发的组合物 |
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