CN114099551B - Asthenopia-relieving and eye-moistening composition - Google Patents
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/30—Zinc; Compounds thereof
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- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7032—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a polyol, i.e. compounds having two or more free or esterified hydroxy groups, including the hydroxy group involved in the glycosidic linkage, e.g. monoglucosyldiacylglycerides, lactobionic acid, gangliosides
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
- A61K35/56—Materials from animals other than mammals
- A61K35/618—Molluscs, e.g. fresh-water molluscs, oysters, clams, squids, octopus, cuttlefish, snails or slugs
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
Abstract
The invention provides a composition for relieving asthenopia and moistening eyes, and relates to the technical field of daily necessities. The composition for relieving asthenopia and moistening eyes comprises glycerol glucoside, zinc sulfate, tea polyphenol, taurine, dipotassium glycyrrhizinate, menthol, borneol and other main components. The composition for relieving eye fatigue and moistening eyes can be used for eye moistening spray and eye washing liquid type aqueous products, has the effects of relieving eye fatigue, eye pruritus, dry eye circumference, dry eyes, improving eyesight and the like, and is good in moisturizing effect, natural, safe, non-irritating and good in application prospect.
Description
Technical Field
The invention relates to the technical field of daily necessities, in particular to an eye moistening composition for relieving visual fatigue.
Background
With the change of life style and working environment, electronic products such as computers, mobile phones and the like are used at high frequency, more and more people, especially the young generation, have eyes in a sub-health state, wherein asthenopia and dry eyes are the most common. The asthenopia is also called asthenopia syndrome, and is a group of syndromes that visual disturbance, discomfort of eyes or accompanied general symptoms and the like are caused after eyes are used, so that the visual operation cannot be normally carried out due to the fact that the load which can be borne by the visual function of human eyes is exceeded when human eyes look at objects by various causes. Epidemiological studies have shown that 23% of school-age children, 64% to 90% of computer users, and 71.3% of dry eye patients all have symptoms of asthenopia of varying degrees. The main reasons for dry eyes are chronic inflammations including conjunctivitis, keratitis and the like, and tear reduction, which are common; the pathological causes include dry eye and Sjogren's syndrome, which is a systemic disease and can cause dry eyes. Long-term asthenopia and dry eyes are the important causes of myopia.
The common treatment means for asthenopia is drug therapy, such as naphazoline eyedrops for improving pseudomyopia and relieving asthenopia, compound asparaguim eyedrops, pearl eyesight improving eyedrops, esculin eyedrops, artificial tear sodium hyaluronate eyedrops, polyvinyl alcohol eyedrops and the like. Based on the above, the development of eye washing liquid or eye spraying agent which can effectively clean eyes and improve the eye environment and asthenopia has certain market prospect, but many eye washing liquid or eye spraying agent disclosed in the prior art have the defects of complex components, limited asthenopia relieving effect, easy generation of eye irritation and the like.
Disclosure of Invention
The invention aims to solve the technical problems and provides the eye moistening composition which can effectively relieve visual fatigue, eye pruritus, eye periphery dryness, dry eyes, vision improvement and the like, has good moisturizing effect, simple components, safety and no stimulation, and has good application prospect.
The technical scheme of the invention is realized as follows: the invention provides an eye-moistening composition for relieving asthenopia, which comprises the following raw materials in percentage by mass:
preferably, the material comprises the following raw materials in percentage by mass:
further preferably, the material comprises the following raw materials in percentage by mass:
the invention discloses a composition for relieving asthenopia and moistening eyes, which comprises glycerol glucoside, zinc sulfate, tea polyphenol, taurine, dipotassium glycyrrhizinate, pearl extract, menthol and borneol, and can be used for relieving asthenopia, eye pruritus, eye circumference dryness, eye dryness, vision improvement and the like, and specifically comprises the following components:
the invention particularly selects glycerol glucoside, which is a glucoside compound formed by connecting glycerol molecules and glucose molecules through glycosidic bonds and is a natural product with high purity and single 2 alpha molecular configuration obtained by natural spirulina through an algal cell endophytic biosynthesis technology. The inventor finds out through intensive research that on one hand, asthenopia is mainly caused by the fact that metabolic waste oxygen free radicals are accumulated and increased to cause the structural damage and the function reduction of myocytes, excessive loss of nutrient substances of the visual cells, untimely supply of required nutrient substances and prolonged recovery time of macula lutea and retina, while glycerol glucoside in the composition for moistening eyes of the invention plays a good role in resisting inflammation and removing oxygen free radicals after entering eyes, and is matched with zinc sulfate to supplement trace mineral zinc element of nutrient substances of the visual cells after entering eyes, so that asthenopia is rapidly relieved under the combined action of the glycerol glucoside and the zinc sulfate; on the other hand, the glycerol glucoside serving as a natural polymer humectant has a synergistic effect after being compounded with the humectant sodium hyaluronate, so that the moisturizing performance of the compounded humectant is effectively improved, the eye surface can be lubricated for a long time, and the symptoms of eye dryness, swelling pain and the like caused by asthenopia are improved. Specifically, the addition amount of the glycerol glucoside is controlled to be 0.001-5%, preferably 0.5-5%, the effect cannot be achieved when the content of the glycerol glucoside is too low, but the content is not as high as possible, and experiments show that the content of the glycerol glucoside is too high, so that the irritation feeling can be brought to eyes, and the moisturizing effect of the eye moisturizing composition can be influenced.
Zinc sulfate: has antiinflammatory and astringent effects. Zinc ions can precipitate protein, can form a very thin protein film with the protein on the eyeball surface, necrotic tissues and secretions, can prevent cell sap from extravasation, and has the functions of astringency, hemostasis and weak antibiosis. The addition amount of zinc sulfate is 0.001% -1%, preferably 0.001% -0.1%.
Borneol: pungent, bitter and slightly cold. It enters heart, spleen and lung meridians. Induce resuscitation and refresh mind, clear heat and alleviate pain. Can be used for treating block syndrome such as unconsciousness, conjunctival congestion, swelling and pain, sore throat, aphtha, sore and ulcer, swelling and pain, and unhealing after ulceration. Modern pharmacology: the borneol has slight stimulation to sensory nerves when being locally applied, and has certain pain relieving and mild antiseptic effects. The higher concentration (0.5%) has inhibitory effect on Staphylococcus, streptococcus, diplococcus pneumoniae, escherichia coli and some pathogenic dermatophytes.
Menthol: is extracted from leaf and stem of herba Menthae, and is white crystal, which is the main ingredient of herba Menthae and Mentha Piperita officinalis essential oil. It can be used as irritant in medicine, and has effects in refreshing and relieving itching.
Pearl extract: improving eyesight, removing toxic substances, and resisting oxidation. Can make skin healthy, fine, moist, smooth and white, and can restore skin elasticity and increase luster to the maximum extent for aging and rough skin. It can obviously reduce wrinkles, eliminate black spots, and has the functions of filling and smoothing facial sores and furuncles, whelks, wounds and the like, healing, diminishing inflammation and promoting tissue regeneration.
Dipotassium glycyrrhizinate: has antibacterial, antiinflammatory, toxic materials clearing away, antiallergic, and deodorant effects, and can be used in eye drop for activating corticosteroid (inhibiting metabolic enzyme). Indirectly enhance the action of corticosteroid compounds, can be used in all cosmetics such as cream, water, lotion, milk, honey, etc., and can neutralize or reduce toxic substances in cosmetics and prevent allergic reaction in some cosmetics.
Taurine: also called beta-aminoethanesulfonic acid, is a sulfur-containing non-protein amino acid, exists in a free state in vivo, and does not participate in the biosynthesis of proteins in vivo. Taurine also has important functions of regulating the osmotic pressure of the crystal, resisting oxidation and the like, and the concentration of taurine which is an important substance for regulating the osmotic pressure is obviously reduced, the anti-oxidation function is weakened, and the protein in the crystal is excessively oxidized. The supplement of taurine can inhibit the occurrence and development of cataract.
Tea polyphenol: also called "Yioling", wei polyphenol "and Fang Ha Ling", which are polyhydroxy compounds contained in tea leaves, abbreviated as TP, and mainly comprise complexes of catechins (flavanols), flavones, flavonols, anthocyanidins, phenolic acids, depside acids, polymeric phenols and the like as chemical components. The tea polyphenols can remove facial greasiness and astringe follicular orifice, and have effects of sterilizing, resisting skin aging, and reducing skin injury caused by ultraviolet radiation in sunlight.
Further, a pH regulator and an osmotic pressure regulator are also included, and the pH of the composition is regulated to 6-8 by adding the pH regulator; the osmolality of the composition is adjusted to 280-320mOsm/L by the addition of an osmolality adjusting agent.
The pH regulator is disodium hydrogen phosphate or sodium dihydrogen phosphate, and the osmotic pressure regulator is sodium chloride or potassium chloride.
The bacteriostatic agent is phenoxyethanol or benzalkonium chloride, and the chelating agent is EDTA disodium. The humectant comprises at least one of glycerin, butanediol and sodium hyaluronate.
The surfactant is at least one of polysorbate-20, polysorbate-60 and polysorbate-80.
The eye moistening composition also comprises a thickening agent, and the addition amount of the thickening agent can be controlled according to the viscosity requirement of a product. The viscous agent is at least one of polyvinyl alcohol, polyvinylpyrrolidone, cellulose derivative and polyethylene glycol.
The eye moistening composition is a water aqua, can be used as a daily eye moistening product, such as a spray or an eye washing liquid, can quickly relieve symptoms such as dry eyes, acid swelling eyes, visual double images and the like caused by visual fatigue in a long-acting manner, and has the advantages of simple components, naturalness, safety, no stimulation, long-term use and good application prospect.
Detailed Description
Examples 1 to 4: eye moistening spray for relieving asthenopia
The amounts of the raw materials for preparing the eye spray of examples 1 to 4 and comparative examples 1 to 2 are shown in table 1.
TABLE 1
Note: the glycerol glucoside is obtained from Kazuki Biotech development Inc. in Qingdao, and the Margarita extract is obtained from Ughai; biotech Inc.
The preparation method of the eye moistening spray for relieving asthenopia comprises the following steps:
(1) Heating Borneolum Syntheticum and Mentholum with polysorbate-80 to dissolve;
(2) Dispersing sodium hyaluronate with glycerol uniformly, adding a certain amount of deionized water, heating to dissolve completely, keeping the temperature, stirring for 10 minutes, and then cooling;
(3) When the temperature is reduced to below 45 ℃, adding zinc sulfate, EDTA disodium, dipotassium glycyrrhizinate, pearl extract, taurine, tea polyphenol, glycerol glucoside, phenoxyethanol and the rest deionized water, mixing and stirring for 10 minutes, adding a pH regulator and an osmotic pressure regulator, mixing and stirring for at least 20 minutes until the mixture is completely and uniformly mixed, and obtaining the eye moistening spray for relieving asthenopia.
Examples 5 to 7: preparation of eyewash for relieving asthenopia and moistening eyes
The amounts of the raw materials for preparing the eyewash of examples 5-7 are shown in Table 2.
TABLE 2
The preparation method of the eye lotion for relieving asthenopia and moistening eyes comprises the following steps:
(1) Heating and dissolving Borneolum Syntheticum and Mentholum with polysorbate-80;
(2) Uniformly dispersing sodium hyaluronate with glycerol, uniformly dispersing sodium carboxymethylcellulose with butanediol, adding a certain amount of deionized water, heating to completely dissolve the sodium hyaluronate, preserving heat, stirring for 10 minutes, and cooling;
(3) Cooling to below 45 deg.C, adding zinc sulfate, disodium EDTA, dipotassium glycyrrhizinate, margarita extract, taurine, tea polyphenols, glycerol glucoside, phenoxyethanol and the rest deionized water, mixing and stirring for 10 min, adding pH regulator and osmotic pressure regulator, mixing and stirring for at least 20 min until completely mixing to obtain eye lotion for relieving asthenopia and moistening eyes.
Safety evaluation tests were performed on the eye spray and eye lotion for relieving asthenopia prepared in examples 1 to 7, and effectiveness evaluation tests were performed on the eye spray and eye lotion for relieving asthenopia prepared in examples 1 to 7 and comparative examples 1 to 3:
1. acute eye irritation test
1. The test substance: the products prepared in the embodiments 1-6 of the invention comprise eye moistening spray and eye washing liquid for relieving asthenopia.
2. Animals: 3 common-grade New Zealand rabbits weighing 2-3Kg were provided by Shanghai Dry Biotechnology, inc. Producing license number of experimental animal: SCXK (Shanghai) 2015-0005. Quality certification: 20200006000175.
3. the test method comprises the following steps: the test samples were subjected to acute eye irritation testing in accordance with technical Specifications for cosmetic safety (2015 edition).
Both eyes of the test animals were examined (using a 2% sodium fluorescein examination) within 24h prior to the test. Animals found to have symptoms of eye irritation, corneal defects, and conjunctival damage were not used for the test specimens.
The lower eyelid of one side of the eye of the rabbit is slightly pulled open, 0.1ml of the test object is dripped into the conjunctival sac, and the upper eyelid and the lower eyelid are passively closed for 1s to prevent the test object from being lost. The other eye was not treated for self-control. Eyes are not washed within 24 hours after the test object is dripped.
The eyes of the animals were examined 1, 24, 48, and 72h and 4D and 7D after the instillation of the test substances. If no stimulus response occurs for 72 hours, the test is terminated. If corneal involvement or other ocular irritation is detected and the patient does not recover within 7D, the observation period is prolonged to determine the reversibility or irreversibility of the lesion, generally not exceeding 21D, and 7D, 14D and 21D observations are provided, and after 24h observation and recording are completed, the eyes of all animals are further examined using sodium fluorescein.
The eye irritation response was graded according to the technical Specification for cosmetic safety (2015 version) P494-495 Table 1, and according to P495 Table 3.
4. The specific results were evaluated as follows:
(not washing)
Test results show that the eye moistening spray and eye washing liquid for relieving asthenopia prepared by the embodiment of the invention have no stimulation to the eye stimulation of rabbits under the condition of no flushing.
2. Efficacy test for relieving asthenopia
Clinical trial evaluation of the asthenopia relieving effect is carried out on the eye moistening spray and the eye lotion prepared in the embodiment and the comparative example.
The first test method comprises the following steps: randomly selecting 70 asthenopia patients with symptoms of dry eyes and distending pain of eyes, wherein the age is 30-50 years, and the patients face the LED screen to overuse eyes every day. The eye moistening sprays prepared in examples 1-4 and the eye moistening sprays prepared in comparative examples 1-3 are respectively used in groups 1-4 and groups 5-7, and after the eye moistening sprays are sprayed twice to each eye in trial, the effect of relieving swelling pain and dry eyes and the use feeling of the eyes after trial are evaluated, and the results are shown in table 1.
TABLE 1 efficacy evaluation results of eye-moistening sprays for relieving asthenopia
And a second test method: randomly selecting 30 asthenopia patients with symptoms of dry eyes and distending pain of eyes when facing LED screen and having eyes overuse eyes every day, wherein the age is 30-50 years old. The eyes were randomly divided into 3 groups of 10 persons each, and the eye lotion prepared in examples 5 to 7 was used for washing the eyes with an eye washing instrument on trial, and after washing, the posture was maintained for 30 seconds, and then the effect of alleviating the symptoms of swelling pain and dryness of the eyes and the feeling of use after trial were evaluated, and the results are shown in table 2.
TABLE 2 evaluation results of efficacy of eyewash for relieving asthenopia
Clinical test result analysis shows that the eye moistening spray and the eye washing liquid prepared by the invention have slight cooling feeling after entering eyes, can refresh and restore consciousness, are safe and non-irritant after being tried out by a human body, can quickly relieve eye distending pain and eye dry visual fatigue symptoms, have good clinical use effect and have better market prospect.
Claims (3)
1. The eye moistening composition for relieving asthenopia is characterized by comprising the following raw materials in percentage by mass:
glycerol glucoside 0.001% -5%
0.001 to 0.5 percent of zinc sulfate
0.001% -5% of tea polyphenol
Taurine 0.001-5%
Dipotassium glycyrrhizinate 0.01-5%
0.01 to 5 percent of pearl extract
0.001% -1% of menthol
0.001 to 1 percent of borneol
0.1 to 10 percent of humectant
0.01 to 10 percent of surfactant
0.1 to 0.5 percent of bacteriostatic agent
0.01 to 0.1 percent of chelating agent
Adding deionized water to 100%;
also comprises a pH regulator and an osmotic pressure regulator, and the pH of the composition is regulated to 6-8 by adding the pH regulator; adjusting the osmolality of the composition to 280-320mOsm/L by adding an osmolality adjusting agent;
the pH regulator is disodium hydrogen phosphate or sodium dihydrogen phosphate, and the osmotic pressure regulator is sodium chloride or potassium chloride; the bacteriostatic agent is phenoxyethanol or benzalkonium chloride, and the chelating agent is EDTA disodium; the humectant is at least one of glycerin, butanediol and sodium hyaluronate; the surfactant is at least one of polysorbate-20, polysorbate-60 and polysorbate-80.
2. The composition for relieving asthenopia and moistening eyes according to claim 1, which comprises the following raw materials in percentage by mass:
glycerol glucoside 0.1% -5%
0.001 to 0.1 percent of zinc sulfate
0.001 to 1 percent of tea polyphenol
Taurine 0.001% -2%
Dipotassium glycyrrhizinate 0.01-2%
0.01 to 2 percent of pearl extract
Menthol 0.001-0.1%
0.001 to 0.1 percent of borneol
0.1 to 10 percent of humectant
0.01 to 10 percent of surfactant
0.1 to 0.5 percent of bacteriostatic agent
0.01 to 0.1 percent of chelating agent
Deionized water was added to 100%.
3. The composition for relieving asthenopia and moistening eyes according to claim 1 or 2, further comprising a viscous agent, wherein the viscous agent is at least one of polyvinyl alcohol, polyvinylpyrrolidone, cellulose derivatives and polyethylene glycol.
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