CN110755286A - Hairline filling composition helpful for hair growth - Google Patents
Hairline filling composition helpful for hair growth Download PDFInfo
- Publication number
- CN110755286A CN110755286A CN201911128427.9A CN201911128427A CN110755286A CN 110755286 A CN110755286 A CN 110755286A CN 201911128427 A CN201911128427 A CN 201911128427A CN 110755286 A CN110755286 A CN 110755286A
- Authority
- CN
- China
- Prior art keywords
- hairline
- raw material
- filling composition
- hair growth
- percent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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Abstract
The invention provides a hairline filling composition helpful for hair growth, which comprises the following raw materials in percentage by weight: 1 to 5 percent of minoxidil, 45 to 98 percent of powdery raw material or oily raw material or a mixture of the powdery raw material and the oily raw material, 0.1 to 40 percent of permeation enhancer and 0.1 to 10 percent of functional additive. The invention can perform targeted treatment and modification on the hair loss area, thereby promoting the hair growth, and is very convenient and portable in use.
Description
Technical Field
The invention relates to the field of cosmetics, in particular to a hairline filling composition for promoting hair growth.
Background
Minoxidil is currently the only recognized drug that can be used to treat hair loss. It was first applied to hypertension, is a potassium channel agonist, and can relax vascular smooth muscle, dilate arterioles, decrease peripheral resistance, and thus lower blood pressure. Minoxidil is found to make hair (beard) longer and thicker in the treatment of hypertension. Therefore, the compound is developed and applied as a medicine for treating male pattern baldness. The exact mechanism by which it promotes hair growth is not known and may be by way of enhancing skin blood flow, affecting keratinocyte growth, and the like. The minoxidil preparation on the market is mainly liniment or gel, needs to be used every day, needs 3 months for use, and has the possibility of relapse after stopping the use.
The first generation solvent of the minoxidil hair-growing liquid is mainly ethanol and propylene glycol, the two solvents can dissolve active ingredients minoxidil and have the effect of promoting transdermal drug delivery efficiency, the product contains ethanol and propylene glycol with large dose, part of patients are stimulated to have allergic manifestations such as dandruff, scalp itch, redness and the like, and the second generation solvent of the minoxidil hair-growing liquid is improved to be a non-propylene glycol solvent, so that the side effect of propylene glycol allergy is avoided. But is easy to flow to the non-affected parts such as the hairless forehead when in use. Moreover, the hair restorer needs to be additionally used in daily life and is easy to forget.
The minoxidil-containing cosmetic is mainly shampoo, is inconvenient to use every day, has long hair washing dry time and limited use scene, cannot be used in a targeted manner, and is easy to act on the face and neck where vigorous hair is not expected.
Disclosure of Invention
Aiming at the defects of the prior art, the hairline filling composition beneficial to hair growth is provided, and can be applied by powder or paste, so that the medicine can be accurately quantified, positioned and uniformly administered, and the poor effect or side effect caused by waste and uneven application is avoided. And the effect of modifying the hair loss and hair loss area is achieved by smearing and using the medicine, the compliance of patients and the safety of medicine application are improved, and the treatment effect is realized.
The technical scheme provided by the invention is as follows: a hairline filling composition for promoting hair growth comprises the following raw materials in percentage by weight: 1 to 5 percent of minoxidil, 45 to 98 percent of powdery raw material or oily raw material or a mixture of the powdery raw material and the oily raw material, 0.1 to 40 percent of permeation enhancer and 0.1 to 10 percent of functional additive.
Furthermore, the hairline filling composition also comprises 0.1-0.5% of essence, 0.5-15% of pigment and 0.02-1% of preservative.
Further, the powdery raw material is any one of inorganic powdery raw materials such as talcum powder, kaolin, zinc white powder, titanium dioxide, bentonite, calcium carbonate and calcium bicarbonate, or organic powdery raw materials such as zinc stearate, magnesium stearate and polyethylene powder, or a mixture of any two or more of the inorganic powdery raw materials and the organic powdery raw materials.
Further, the oily raw material is any one of grease, wax, higher fatty acid, alcohol and ester or a mixture of any two or more of the grease, the wax, the higher fatty acid, the alcohol and the ester.
Further, the permeation enhancer is any one of or a mixture of any two or more of sulfoxides, pyrrolidones, Azone (laurocapram) and analogues thereof, soft permeation enhancers, fatty acids and esters thereof, surfactants, terpenes, amines, amides, cyclodextrins, amino acids, macrocyclic compounds, phospholipids and water.
Further, the functional additive includes a glue; one or more additives with microcirculation promoting, metabolism promoting, antiinflammatory, and antibacterial effects are selected from lactic acid, sodium lactate, PCA-Na, hyaluronic acid, hydrolyzed collagen, chitin and its derivatives, plant humectant, vitamin E, vitamin D, bioactive polypeptide, and human epidermal growth factor.
The hairline line filling composition has the beneficial effects that the hairline filling composition contains the minoxidil component, 1) a hair loss patient can play a role in treating hair loss during daily hairline modification, the condition that the existing minoxidil solution prepared on the basis of ethanol has large stimulation on the use of the hair loss patient is avoided, and the hairline filling composition is suitable for people allergic to the ethanol; 2) the situation that the application interval is long, the single use is matched with long hair washing time and the targeted application characteristics are lacked when the minoxidil is used for washing and protecting hair in daily use, and the minoxidil-containing hair conditioner is suitable for people who want to be operated simply and conveniently, consumes short time and strengthens the use of targeted hair loss areas; 3) the hairline-filling composition is suitable for daily use; 4) the targeted therapy can be performed on the area with few hairs and alopecia, so that the hair growth is promoted; 5) is very convenient and portable in use. The effect of promoting hair growth can be achieved when the alopecia area is locally modified by a patient, so that the invention provides great convenience for the alopecia patient, and 6) the functional additive is added, so that the hair-growing liquid has the effects of moisturizing, promoting microcirculation, promoting metabolism, diminishing inflammation and sterilizing.
Detailed Description
The present invention will be further described with reference to the following specific examples.
In the following description of the examples, the powdery raw material is any one of inorganic powdery raw materials such as talc, kaolin, zinc white, titanium dioxide, bentonite, mica, calcium carbonate, and calcium bicarbonate, or organic powdery raw materials such as zinc stearate, magnesium stearate, and polyethylene powder, or a mixture of any two or more of them.
The oily raw material is any one or mixture of two or more of oil, wax, higher fatty acid, alcohol and ester.
The permeation enhancer is any one of or a mixture of any two or more of sulfoxides, pyrrolidones, Azone and analogues thereof, soft permeation enhancers, fatty acids and esters thereof, surfactants, terpenes, amines, amides, cyclodextrins, amino acids, macrocyclic compounds, phospholipids and water.
The functional additive is a glue; one or more additives with microcirculation promoting, metabolism promoting, antiinflammatory, and antibacterial effects are selected from lactic acid, sodium lactate, PCA-Na, hyaluronic acid, hydrolyzed collagen, chitin and its derivatives, plant humectant, vitamin E, vitamin D, bioactive polypeptide, and human epidermal growth factor.
Example 1 (with powdery raw material as main material):
the following substances are prepared according to weight percentage: 5% of minoxidil, 42% of talcum powder, 29.4% of mica, 6.9% of kaolin, 7% of zinc stearate, 1% of vitamin E, 6% of isopropyl palmitate, 0.1% of essence, 0.6% of preservative, 1% of carbon black and 1% of lecithin.
Mixing the components uniformly, and pressing and forming in a tray. The powder cake or sponge can be dipped and pressed for use.
Example 2 (with oily raw materials as the main material):
the following substances are prepared according to weight percentage: 2% of minoxidil, 17% of beeswax, 11% of insect wax, 9% of vaseline, 10% of lanolin, 7% of liquid paraffin, 20% of paraffin, 11.4% of pigment, 1% of tocopherol acetate, 1% of essence, 0.6% of preservative, 5% of ultramarine and 5% of 2-n-nonyl-1, 3-dioxolane.
Grinding the components except essence, such as pigment, petrolatum, liquid paraffin and the like into uniform pigment slurry, heating and melting the residual grease and wax, mixing the pigment slurry into the melted grease and wax pigment, fully stirring, and cooling to 45 ℃ to add the essence. The powder cake or sponge can be dipped and pressed for use.
Example 3 (mixing of powder raw material and oily raw material as main material):
1.4 percent of minoxidil, 6 percent of carbon black, 7 percent of titanium dioxide, 45 percent of hardened oil, 7 percent of cocoa butter, 4 percent of beeswax, 6 percent of castor oil, 12 percent of lanolin, 10 percent of 2-n-nonyl-1, 3-dioxolane, 1 percent of essence and 0.6 percent of preservative.
Mixing the powder materials, adding hardened oil and lanolin, mixing, grinding, and press forming. The powder cake or sponge can be dipped and pressed for use.
Example 4 (mixing of powder raw material and oily raw material as main material):
the composition comprises, by weight, 2% of minoxidil, 22% of polyvinylpyrrolidone, 25% of black iron oxide, 5% of propylene glycol, 0.3% of tragacanth, 15% of polyacrylate, 10% of 2-n-nonyl-1, 3-dioxolane, 19.55% of deionized water, 1% of essence and 0.15% of methylparaben.
Mixing the powder material and pigment in a ball mill, grinding, adding propylene glycol, tragacanth, essence, minoxidil, etc., grinding, mixing with water, stirring, and packaging. The powder cake or sponge can be dipped and pressed for use.
Example 4 is a paste formulation. Unlike current minoxidil hair restorer such as cranberry and dafei, which contains 95% -98% of propylene glycol and ethanol, the propylene glycol in example 4 contains only 5%. Example 4 the addition of other permeation enhancers such as water, 2-n-nonyl-1, 3-dioxolane, to increase minoxidil permeability, reduce the amount of propylene glycol required, and synergistically with other ingredients improve the long-lasting performance of the product after use, suitable for use by the group of the habitual use of the ointment.
The following studies illustrate the beneficial effects of the present invention:
first, quantitative, uniform dosing control test index and method (example 1):
total coating area per gram of product: four samples were taken and prepared into a cake (area S)0) Precision weighing (W)1). Preparing 4 sponges with the same material and size, and measuring the bottom area S1(S1Less than S0) Precision weighing of W2. Preparation area of 10S14 pieces of test paper, precisely weighing W3. The sponge is pressed on the sample and the test paper with the same strength, the pressed parts on the test paper are not overlapped, and the pressing is carried out for 10 times. Precision weighing test paper (W)4) Sponge weight (W)5) The remaining sample size (W)6). The total area of application per gram was calculated as follows: s0*(W1-W6)/(W4-W3+W5-W1)/W1The content of main drugs per square centimeter is as follows: applying a 100-square-centimeter test paper according to the pressure of 1 to the product, extracting the main drug by absolute ethyl alcohol, drying at low temperature, adding 60ml of hydrochloric acid solution (9 → 1000), transferring to a 100ml measuring flask, oscillating to dissolve minoxidil, adding hydrochloric acid solution (9 → 1000) to dilute to a scale, shaking up, precisely absorbing 2ml of the diluted solution, placing in another measuring flask, diluting to a scale by using hydrochloric acid solution (9 → 1000), and measuring the absorbance of 281nm wavelength by using an ultraviolet-visible spectrophotometer (appendix IVA of the second part of the year edition of Chinese pharmacopoeia); and taking the minoxidil reference substance, precisely weighing, adding a hydrochloric acid solution (9 → 1000) to dissolve and dilute into a solution containing about 5 mu g of minoxidil in each 1ml, performing open hair measurement, and calculating to obtain the minoxidil. The main content per square centimeter is 80-120% of the measured content.
Content determination: precisely weighing 1g of the product in a 100ml measuring flask, and extracting the main drug by using absolute ethyl alcohol. Drying the crude extract of main drug at low temperature, adding 60ml of hydrochloric acid solution (9 → 1000), transferring to a 100ml measuring flask, oscillating to dissolve minoxidil, adding hydrochloric acid solution (9 → 1000) to dilute to scale, shaking up, precisely absorbing 2ml of diluted solution, placing in another measuring flask, diluting to scale with hydrochloric acid solution (9 → 1000), and measuring absorbance of 281nm wavelength according to ultraviolet-visible spectrophotometer (appendix of second part of 2015 edition of Chinese pharmacopoeia); and taking the minoxidil reference substance, precisely weighing, adding a hydrochloric acid solution (9 → 1000) to dissolve and dilute into a solution containing about 5 mu g of minoxidil in each 1ml, performing open hair measurement, and calculating to obtain the minoxidil. The content of minoxidil in each gram of the product is 90.0-110.0% of the measured content.
Stability detection index and method
1. Influence factor test: the method is operated according to the second edition of Chinese pharmacopoeia 2015 and the standard inspection method of the product, the sample is irradiated by strong light of 4500LX +/-500 LX for 10 days, placed in a high-temperature water bath at 60 ℃ for 10 days, and placed in a low-temperature refrigerator at 4 ℃ for 10 days, so that the appearance, the shape, the content of the main drug per square centimeter and the inspection index of minoxidil are not obviously changed, and the quality is stable.
2. Accelerated destruction test: the method is operated according to the second edition of Chinese pharmacopoeia 2015 and the standard inspection method of the product, and the sample is placed for 6 months at the temperature of 30 +/-2 ℃ and the relative humidity of 65 +/-5 percent, so that the appearance, the shape, the content of the main drug per square centimeter and the inspection index of minoxidil are not obviously changed, and the quality is stable.
3. Long-term sample retention observation experiment: the method is operated according to the second edition of Chinese pharmacopoeia 2015 and the standard inspection method of the product, and the sample is placed for 24 months at 25 +/-2 ℃ and at a relative humidity of 60 +/-5%, so that the appearance, the shape, the content of the main drug per square centimeter and the inspection index of minoxidil are not obviously changed, and the quality is stable.
Third, safety study
1. Acute toxicity test: minoxidil mouse intravenous injection administration LD5050mg/kg, rat intravenous administration LD5029mg/kg, mice were orally administered LD501321-3492 mg/kg, oral administration LD for vole502457-2648 mg/kg.
2. Safety of topical application: the product is administered for a single time or repeatedly, has no obvious stimulation to rabbit skin integrity, and has slight stimulation to rabbit damaged skin; has no obvious allergy to the whole skin of the guinea pig.
3. Carcinogenesis: the teratogenicity research result of the skin administration of minoxidil on the field mice and rats for 24 hours shows that no carcinogenesis is found at the doses of 8.25 and 80 mg/kg/day.
4. Teratogenic effect: the research result of teratogenicity of subcutaneous administration of minoxidil pregnant mice shows that no teratogenicity is generated at the dose of 80 mg/kg/day.
Four, main pharmacodynamic study
Minoxidil as a classical antihypertensive drug can deploy vascular smooth muscle and reduce peripheral vascular resistance, and is suitable for various types of hypertension, and the main adverse reaction is hirsutism. The action mechanism of minoxidil for local external application to stimulate hair growth is not clear.
Fifth, pharmacokinetic study
The minoxidil is only absorbed in a micro-amount when being locally applied, and the normal scalp administration absorption rate is 0.3-4.2%. The 1% minoxidil solution was administered topically 2 times a day, 1ml each time (maximum dose was recommended for topical administration), with a peak concentration of blood drug administered normally to the intact scalp of 5.8% of that administered orally (2.5 mg/time twice a day).
After topical administration of minoxidil, the drug absorbed in vivo is cleared within 95% of four days, but there is no means for small measures of metabolic conversion.
Sixth, clinical research
Clinical study results show that the hairline filling composition has 100% of effectiveness for hairline burst modification and 79% of total effectiveness for treating hairline baldness.
While the invention has been described in detail with respect to specific embodiments thereof, it will be understood that the invention is not limited to the specific forms disclosed, but is capable of use in various other combinations, modifications, and environments and is intended to cover such modifications, equivalents, and improvements as may be made by those skilled in the art.
Claims (6)
1. A hairline filling composition for helping hair growth is characterized by comprising the following raw materials in percentage by weight: 1 to 5 percent of minoxidil, 45 to 98 percent of powdery raw material or oily raw material or a mixture of the powdery raw material and the oily raw material, 0.1 to 40 percent of permeation enhancer and 0.1 to 10 percent of functional additive.
2. The hairline filling composition helping hair growth according to claim 1, characterized in that: the hairline filling composition also comprises 0.1-0.5% of essence, 0.5-15% of pigment and 0.02-1% of preservative.
3. The hairline filling composition helping hair growth according to claim 1, characterized in that: the powdery raw material is any one or a mixture of any two or more of talcum powder, kaolin, zinc white powder, titanium dioxide, bentonite, calcium carbonate, calcium bicarbonate, mica, zinc stearate, magnesium stearate and polyethylene powder.
4. The hairline filling composition helping hair growth according to claim 1, characterized in that: the oily raw material is any one or a mixture of any two or more of grease, wax, higher fatty acid, alcohol and ester.
5. The hairline filling composition helping hair growth according to claim 1, characterized in that: the permeation enhancer is any one of or a mixture of any two or more of sulfoxides, pyrrolidones, azones and analogues thereof, soft permeation enhancers, terpenes, amines, amides, cyclodextrins, amino acids and esters thereof, macrocyclic compounds, phospholipids and water.
6. The hairline filling composition helping hair growth according to claim 1, characterized in that: the functional additive comprises one or more additives with effects of promoting microcirculation, metabolism, diminishing inflammation and sterilizing, such as adhesive, lactic acid, sodium lactate, PCA-Na, hyaluronic acid, hydrolyzed collagen, chitin and its derivatives, plant humectant, vitamin E, vitamin D, bioactive polypeptide and human epidermal growth factor.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN115475168A (en) * | 2022-10-18 | 2022-12-16 | 湖北工业大学 | Minoxidil-containing pharmaceutical composition, and preparation method and application thereof |
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| CN115475168B (en) * | 2022-10-18 | 2024-02-13 | 湖北工业大学 | Minoxidil-containing pharmaceutical composition and preparation method and application thereof |
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