CN116139226B

CN116139226B - Eye protection composition for relieving asthenopia and application thereof

Info

Publication number: CN116139226B
Application number: CN202211694012.XA
Authority: CN
Inventors: 王小宇; 张洁
Original assignee: Heilongjiang Wusuli River Pharmaceutical Co ltd
Current assignee: Heilongjiang Wusuli River Pharmaceutical Co ltd
Priority date: 2022-12-28
Filing date: 2022-12-28
Publication date: 2024-03-29
Anticipated expiration: 2042-12-28
Also published as: CN116139226A

Abstract

The invention relates to an eye-protecting composition for relieving visual fatigue and application thereof, wherein the eye-protecting composition for relieving visual fatigue comprises lutein ester, zeaxanthin, beta-carotene and plant extracts; the plant extract comprises herba Setariae extract, blackcurrant extract, and grape seed extract. The invention creatively selects the combination of three specific plant extracts comprising the grass extract, the blackcurrant extract and the grape seed extract to be matched with lutein ester, zeaxanthin and beta-carotene, thereby comprehensively improving the effects of the composition in relieving visual fatigue, improving eyesight and improving eyesight persistence; wherein the three components of the cordgrass extract, the blackcurrant extract and the grape seed extract complement each other, and the cordgrass extract and the grape seed extract have unexpected potential synergistic effect on the promotion effect.

Description

Eye protection composition for relieving asthenopia and application thereof

Technical Field

The invention belongs to the technical field of eye protection products, relates to an eye protection composition for relieving visual fatigue and application thereof, and in particular relates to an eye protection composition for relieving visual fatigue and application thereof in preparation of a preparation with the effects of relieving visual fatigue and improving vision.

Background

The eye is the most important organ in human perception, and about 80% of knowledge and memory in the brain is acquired through the eye. People can feel beauty of the world through eyes, and any work needs eyes to cooperate, and the work is completed through eyes whether a computer is used or a user writes, drives and walks. Due to popularization of electronic products in modern society, eyes are overused, eyes cannot fully rest due to working pressure and insufficient sleep, a series of eye diseases are generated, eyes are dry, eyes are unsmooth, eye fatigue is caused, eyes are affected by long-time reading, computer and television watching and the like, harmful light injury is caused due to aging, and fundus retina macula area is gradually changed. Patients with asthenopia gradually increase, and symptoms such as eye discomfort, vision disorder, eye corresponding lesions, headache, nausea, stomach discomfort and the like after the total body symptom is combined seriously.

CN112715729a discloses a blueberry lutein ester tablet candy for relieving visual fatigue and a preparation method thereof, which comprises the following components: lutein ester, blueberry powder, D-mannitol, maltodextrin, microcrystalline cellulose, citric acid and magnesium stearate; the preparation method comprises the steps of sieving, mixing, preparing soft materials, granulating, mixing, tabletting and the like.

CN112022938A discloses a hydrogel eye patch for relieving asthenopia and preventing myopia, which is prepared from the following raw materials in percentage by weight: 0.1 to 1.0 percent of traditional Chinese medicine compound essential oil, 1.0 to 5.0 percent of traditional Chinese medicine compound extract, 0.2 to 0.6 percent of water-soluble lutein microcapsule powder, 0.1 to 0.5 percent of water-soluble zeaxanthin microcapsule powder, 10 to 25 percent of high polymer material, 20 to 30 percent of propylene glycol, 0.1 to 0.5 percent of citric acid, 0.1 to 0.3 percent of aluminum hydroxide and 40 to 60 percent of purified water.

The main functional components of the oral eye-protection product disclosed in the prior art are zeaxanthin and lutein ester, the functional components are single, the absorption is limited, and the bioavailability is not high. The external eye-protection patch can only temporarily relieve asthenopia, and can not fundamentally solve the eye-protection problem. Therefore, the development of a product which has multiple functional components, high bioavailability, high biological safety and can effectively relieve asthenopia and improve eyesight is very significant.

Disclosure of Invention

Aiming at the defects of the prior art, the invention aims to provide an eye protection composition for relieving visual fatigue and application thereof, in particular to an eye protection composition for relieving visual fatigue and application thereof in preparation of a preparation with the effects of relieving visual fatigue and improving vision.

In order to achieve the aim of the invention, the invention adopts the following technical scheme:

in a first aspect, the present invention provides an eye-care composition for relieving asthenopia comprising lutein ester, zeaxanthin, β -carotene, plant extracts; the plant extract comprises herba Setariae extract, blackcurrant extract, and grape seed extract.

The lutein ester is an important carotenoid fatty acid ester, can supplement the macular pigment density in the macular area of the retina of human eyes, protect the macula and promote the development of the macula; protecting eyes from being damaged by light, delaying aging of the eyes and preventing lesions; protecting vision and relieving asthenopia symptoms; preventing macular degeneration and retinitis pigmentosa, and reducing drusen. Wherein zeaxanthin is a novel oil-soluble natural pigment, and often coexists with lutein, beta-carotene, cryptoxanthin and the like in nature to form carotenoid mixtures. Zeaxanthin is a powerful antioxidant in humans and protects the biological system from potentially deleterious effects of excessive oxidation by quenching oxidation-resistant actions such as singlet oxygen, scavenging free radicals, etc. Wherein, beta-carotene has good effect on eye development, because the carotene can synthesize vitamin A in vivo, and the carotene can not only promote eye part development, but also prevent night blindness.

The invention creatively selects the combination of three specific plant extracts comprising the grass extract, the blackcurrant extract and the grape seed extract to be matched with lutein ester, zeaxanthin and beta-carotene, thereby comprehensively improving the effects of the composition in relieving visual fatigue, improving eyesight and improving eyesight persistence; wherein the three components of the cordgrass extract, the blackcurrant extract and the grape seed extract complement each other, and the cordgrass extract and the grape seed extract have unexpected potential synergistic effect on the promotion effect.

Preferably, the eye protection composition for relieving asthenopia comprises, by mass, 1-10 parts of lutein ester, 0.5-3 parts of zeaxanthin, 0.2-5 parts of beta-carotene and 0.1-10 parts of plant extract.

When the plant extract is matched with lutein ester, zeaxanthin and beta-carotene in the specific mass ratio, the effects of relieving visual fatigue, improving eyesight and improving eyesight persistence are more remarkable.

The lutein ester may be 1 part, 2 parts, 3 parts, 4 parts, 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, 10 parts, etc.

The zeaxanthin may be 0.5 parts, 1 part, 1.2 parts, 1.5 parts, 1.8 parts, 2 parts, 2.2 parts, 2.5 parts, 2.8 parts, 3 parts, etc.

The beta-carotene may be 0.2 parts, 0.5 parts, 1 part, 1.5 parts, 2 parts, 2.5 parts, 3 parts, 3.5 parts, 4 parts, 5 parts, etc.

The mass fraction of the plant extract may be 0.1 part, 1 part, 2 parts, 3 parts, 4 parts, 5 parts, 6 parts, 8 parts, 9 parts, 10 parts, etc.

Preferably, the mass ratio of the small grass extract, the blackcurrant extract and the grape seed extract in the plant extract is (2-5): 1-3): 1.

When the grass extract, the blackcurrant extract and the grape seed extract are combined in the specific mass ratio, the potential synergistic effect is more remarkable, so that the effects of the product in the aspects of relieving visual fatigue, improving eyesight and improving eyesight persistence are better promoted.

Wherein the specific point value in (2-5) may be selected from 2, 2.5, 3, 3.5, 4, 4.5, 5, etc.

Wherein the specific point value in (1-3) may be selected from 1, 1.5, 2, 2.5, 3, etc.

Other specific point values in the numerical ranges are selectable, and will not be described in detail herein.

The grass extract in the eye-care composition according to the present invention can be obtained either by using a commercially available product or by self-making, and more preferably by the extraction method described below.

Preferably, the herba Setariae extract is prepared by a preparation method comprising the following steps:

pulverizing herba Setariae, mixing with ethanol water solution, ultrasonic treating, microwave extracting, filtering, and lyophilizing the filtrate.

The invention more preferably adopts an ultrasonic-microwave synergistic extraction method to obtain the herba euphorbiae lathyris extract, can improve the extraction rate of flavonoid substances to a greater extent, and simultaneously ensures the stability of the efficacy of the flavonoid substances, thereby achieving better efficacy in the eye-protecting composition.

Preferably, the aqueous ethanol solution is an aqueous ethanol solution having a volume fraction of 60-80% (e.g., 60%, 65%, 70%, 75%, 80%, etc.).

The invention more preferably uses ethanol aqueous solution with volume fraction of 60-80% as extraction reagent, because flavonoids in the extract can be extracted efficiently and stably.

Preferably, the ratio of the aqueous ethanol solution to the millet grass is 1 (20-60) g/mL, such as 1:20g/mL, 1:30g/mL, 1:40g/mL, 1:50g/mL, 1:60g/mL, etc.

Preferably, the sonication is performed at a power of 300-600W (e.g., 300W, 350W, 400W, 450W, 500W, 550W, 600W, etc.) at 40-60 ℃ (e.g., 40 ℃, 45 ℃, 50 ℃, 55 ℃, 60 ℃, etc.) for 3-10min (e.g., 3min, 4min, 5min, 6min, 7min, 8min, 9min, 10min, etc.).

Preferably, the microwave extraction is performed at a power of 250-400W (e.g., 250W, 300W, 350W, 400W, etc.) for 1-5min (e.g., 1min, 2min, 3min, 4min, 5min, etc.).

The invention preferably uses the specific ultrasonic process parameters and microwave process parameters, can improve the extraction rate of the flavonoid substances to a greater extent, ensures the stability of the efficacy of the flavonoid substances, and further has better efficacy in the eye-protection composition.

Preferably, the plant extract further comprises any one or a combination of at least two of safflower extract, chrysanthemum extract or rice germ extract.

The present invention has also found that the efficacy of the product can be further improved to some extent if any one or a combination of at least two of safflower extract, chrysanthemum extract or rice germ extract is added to the eye care composition product.

Preferably, the eye-care composition for relieving asthenopia further comprises a vitamin component.

Preferably, the vitamin component comprises any one or a combination of at least two of vitamin C, vitamin a or vitamin B6.

In a second aspect, the invention provides the use of an eye protection composition for relieving asthenopia according to the first aspect for preparing a preparation having the efficacy of relieving asthenopia and improving vision.

The eye protection composition can be combined with other auxiliary materials such as functional auxiliary materials (blueberry concentrated juice, blueberry powder, dried orange peel concentrated juice, dried orange peel powder, high fructose corn syrup, vitamins and the like), excipient, flavoring agent, pH regulator, cosolvent, suspending agent, thickener, solvent and the like according to the requirement, and is used for preparing preparations with the effects of relieving visual fatigue and improving vision in various dosage forms, and the adaptation degree is very high.

Preferably, the dosage form of the formulation comprises a solution, a powder, a granule, a tablet or a capsule.

Preferably, the preparation with the effects of relieving asthenopia and improving vision also contains auxiliary materials.

Preferably, the auxiliary materials comprise any one or a combination of at least two of blueberry concentrated juice, blueberry powder, dried orange peel concentrated juice, dried orange peel powder or high fructose syrup.

Compared with the prior art, the invention has the following beneficial effects:

Detailed Description

In order to further describe the technical means adopted by the present invention and the effects thereof, the following describes the technical scheme of the present invention in combination with the preferred embodiments of the present invention, but the present invention is not limited to the scope of the embodiments.

The following examples and comparative examples relate to the partial sources of raw materials as follows:

raw materials	Purchase source	Model number
			Lutein ester	Siami Biotechnology Co Ltd	Food grade
Zeaxanthin	Siami Biotechnology Co Ltd	Food grade
			Beta-carotene	Shandong Runchun Biotech Co.Ltd	Food grade
Herba Setariae extract	Siami Biotechnology Co Ltd	Food grade
			Blackcurrant extract	Siami Biotechnology Co Ltd	Food grade
Grape seed extract	Siami Biotechnology Co Ltd	Food grade
			Safflower extract	Siami Biotechnology Co Ltd	Food grade
Chrysanthemum extract	Siami Biotechnology Co Ltd	Food grade
			High fructose syrup	Jinan Yi chemical Co Ltd	Food grade
Blueberry juice	Siam Qian grass extract bioengineering Co.Ltd	Food grade

Preparation example 1

The preparation example provides a herba Setariae extract, which is prepared by the following steps:

pulverizing herba Setariae, mixing with 40 times of 70% ethanol water solution, ultrasonic treating at 50deg.C under 500W for 7min, microwave extracting at 280W for 3min, filtering, and freeze drying.

Preparation example 2

pulverizing herba Setariae, mixing with 65% ethanol water solution of 50 times mass, ultrasonic treating at 55deg.C under 400W for 5min, microwave extracting at 350W for 2min, filtering, and freeze drying.

Preparation example 3

pulverizing herba Setariae, mixing with 30 times of 75% ethanol water solution, ultrasonic treating at 45deg.C under 600W for 10min, microwave extracting at 250W for 4min, filtering, and freeze drying.

Preparation example 4

The present preparation provides a herba Setariae extract, and the preparation method is different from that of preparation 1 only in that 50% volume fraction ethanol water solution is used, and other conditions are kept unchanged.

Preparation example 5

The present preparation provides a herba Setariae extract, and the preparation method is different from that of preparation 1 only in that 90% volume fraction ethanol water solution is used, and other conditions are kept unchanged.

Preparation example 6

The present preparation provides a herba Setariae extract, and the preparation method is different from that of preparation 1 only in that the power of microwave extraction is 500W, and other conditions are kept unchanged.

Preparation example 7

The preparation example provides a herba Setariae extract, and the preparation method is different from that of preparation example 1 only in that the power of microwave extraction is 200W, and other conditions are kept unchanged.

Preparation example 8

pulverizing herba Setariae, mixing with 40 times of 70% ethanol water solution, microwave extracting at 280W for 3min, filtering, and freeze drying.

Example 1

The embodiment provides an eye-protecting composition, which comprises the following components in parts by mass: 6 parts of lutein ester, 0.5 part of zeaxanthin, 1 part of beta-carotene, 0.5 part of herba euphorbiae humifusae extract, 0.3 part of blackcurrant extract and 0.2 part of grape seed extract, wherein the herba euphorbiae humifusae extract uses the product prepared in preparation example 1, and the other parts are all commercial products. The preparation method comprises the following steps: mixing the above materials, and stirring.

Example 2

The embodiment provides an eye-protecting composition, which comprises the following components in parts by mass: 4.5 parts of lutein ester, 1 part of zeaxanthin, 2 parts of beta-carotene, 0.4 part of herba euphorbiae humifusae extract, 0.4 part of blackcurrant extract and 0.2 part of grape seed extract, wherein the herba euphorbiae humifusae extract uses the product prepared in preparation example 2, and the other parts are all commercial products. The preparation method comprises the following steps: mixing the above materials, and stirring.

Example 3

The embodiment provides an eye-protecting composition, which comprises the following components in parts by mass: lutein ester 5 parts, zeaxanthin 1.5 parts, beta-carotene 1 part, herba Euphrasiae Regelii extract 0.4 parts, blackcurrant extract 0.45 parts, grape seed extract 0.15 parts, wherein the herba Euphrasiae Regelii extract is prepared from the product prepared in preparation example 3, and the other products are all commercial products. The preparation method comprises the following steps: mixing the above materials, and stirring.

Examples 4 to 8

This example provides five eye care compositions whose formulations differ from example 1 only in the use of the products of preparations 4-8, respectively, for the herba Setariae extract. The preparation is described in example 1.

Example 9

This example provides an eye care composition whose formulation differs from example 1 only in that the herba Euphrasiae Regelii extract is used in the commercial products listed in the table above. The preparation is described in example 1.

Comparative example 1

This comparative example provides an eye protection composition whose formulation differs from example 1 only in that it does not contain the herb extract, and the missing parts by mass are proportioned to the parts by mass of the blackcurrant extract and the grape seed extract, with the other conditions remaining unchanged. The preparation is described in example 1.

Comparative example 2

This comparative example provides an eye protection composition whose formulation differs from example 1 only in that it does not contain blackcurrant extract, and the missing parts by mass are proportioned to the parts by mass of the eyebright extract and grape seed extract, with the other conditions remaining unchanged. The preparation is described in example 1.

Comparative example 3

This comparative example provides an eye protection composition whose formulation differs from example 1 only in that it does not contain grape seed extract, and the missing parts by mass are proportioned to the parts by mass of the pongamia pinnata extract and blackcurrant extract, with the other conditions remaining unchanged. The preparation is described in example 1.

Comparative example 4

This comparative example provides an eye care composition whose formulation differs from example 1 only in that it does not contain a plant extract component, and the missing parts by mass are proportioned to the parts by mass of lutein ester, zeaxanthin, beta-carotene, with the other conditions remaining unchanged. The preparation is described in example 1.

Comparative example 5

This comparative example provides an eye protection composition whose formulation differs from example 1 only in that it does not contain lutein ester, zeaxanthin, beta-carotene, and the missing mass fraction is proportionally divided over the mass fraction of the herb extract, blackcurrant extract, grape seed extract, with the other conditions remaining unchanged. The preparation is described in example 1.

Example 10

The embodiment provides an eye-protecting composition, which comprises the following components in parts by mass: 6 parts of lutein ester, 0.5 part of zeaxanthin, 1 part of beta-carotene, 0.4 part of herba eupatorii extract, 0.2 part of blackcurrant extract, 0.1 part of grape seed extract, 0.1 part of safflower extract and 0.2 part of chrysanthemum extract, wherein the herba eupatorii extract is prepared from the product prepared in preparation example 1, and the other parts are all commercial products. The preparation method comprises the following steps: mixing the above materials, and stirring.

Application examples 1 to 15

20mg of the compositions prepared in examples 1-10 and comparative examples 1-5 were homogenized with 4g of high fructose syrup and 2mL of blueberry juice, sterilized, and packaged for subsequent testing, respectively.

Test case

Voluntary subjects with long-term eye and asthenopia are selected, with ages between 18 and 50 years, excluding subjects not meeting the inclusion age criteria, those suffering from eye diseases, and no products related to the tested functions within 6 months. The test groups are grouped according to random and double-blind requirements, and symptoms and food levels of each test group are balanced according to symptoms and vision examination conditions during grouping, and meanwhile, the test groups are comparable in terms of age, sex and other factors. The test is divided into 16 groups, each group comprises 20 people, and the 20 people have various symptoms such as symptoms of eye distension and photophobia, symptoms of dry eyes and blurred vision, and single eye pain. And the number of people distributed at each symptom level is relatively uniform.

The products of application examples 1-15 were taken in 1-15 groups, 100mL each day, and the 16 groups were placebo controlled groups, and the test was performed for 60 days. After the test, the improvement of asthenopia symptoms (symptoms such as eye distension, eye pain, photophobia, blurred vision, and dry eyes) of each group of individuals was evaluated.

Wherein the symptom classification and scoring of asthenopia symptoms are as follows:

the even sense is 1-2 times/day; sometimes it means 3-4 times/day; often more than 4 times per day.

Wherein the product efficacy decision criteria are as follows:

improvement of symptoms: any symptom improvement (1 minute or more in symptom level decrease) and other symptoms without deterioration are judged as the symptom improvement;

the method is effective: the symptoms are improved, and the difference between the front and back of the photopic persistence is more than or equal to 10 percent, so that the effect is achieved;

invalidation: other cases are invalid.

Photopic duration= (photopic time/total time of fixation) ×100%, total time of fixation 180s.

The results of the improvement rate of each symptom are shown in table 1:

TABLE 1

Improvement rate% = number of active people/total number of people.

As can be seen from the data in table 1: the eye-protecting composition has excellent effect of relieving asthenopia, wherein each component of the plant extract has potential synergistic effect, and the source mode and the extraction mode of the plant extract can influence the effects of the product.

The test also evaluates the vision improvement effect of the groups, and the improvement of the vision is achieved by increasing the definition of the vision chart on the standard vision chart by 1 line or more than 1 line after the test is finished. The statistical results are shown in table 2:

TABLE 2

Group of	Improvement rate
		1	25％
2	25％
		3	15％
4	25％
		5	10％
6	20％
		7	25％
8	25％
		9	20％
10	35％
		11	5％
12	20％
		13	20％
14	15％
		15	5％
16	0

As can be seen from the data in table 2: the eye-protecting composition has excellent eyesight improving effect, and the components of the plant extract have potential synergistic effect, so that the source mode and the extraction mode of the plant extract can influence the effects of the product.

The applicant states that the present invention is described by way of the above examples as an eye protection composition for relieving asthenopia and its use, but the present invention is not limited to the above examples, i.e. it is not meant that the present invention must be practiced by relying on the above examples. It should be apparent to those skilled in the art that any modification of the present invention, equivalent substitution of raw materials for the product of the present invention, addition of auxiliary components, selection of specific modes, etc., falls within the scope of the present invention and the scope of disclosure.

The preferred embodiments of the present invention have been described in detail above, but the present invention is not limited to the specific details of the above embodiments, and various simple modifications can be made to the technical solution of the present invention within the scope of the technical concept of the present invention, and all the simple modifications belong to the protection scope of the present invention.

In addition, the specific features described in the above embodiments may be combined in any suitable manner, and in order to avoid unnecessary repetition, various possible combinations are not described further.

Claims

1. The eye protection composition for relieving the asthenopia is characterized by comprising, by mass, 1-10 parts of lutein ester, 0.5-3 parts of zeaxanthin, 0.2-5 parts of beta-carotene and 0.1-10 parts of plant extract;

the plant extract is a small grass extract, a blackcurrant extract and a grape seed extract with the mass ratio of (2-5) to (1-3) 1;

the herba Setariae extract is prepared by a preparation method comprising the following steps:

pulverizing herba Setariae, mixing with ethanol water solution, ultrasonic treating, microwave extracting, filtering, and freeze drying the filtrate;

the microwave extraction is carried out for 1-5min at the power of 250-400W;

the ethanol aqueous solution is ethanol aqueous solution with volume fraction of 60-80%;

the ultrasonic treatment is carried out at 40-60 ℃ for 3-10min with power of 300-600W.

2. The eyeshield composition for relieving visual fatigue as claimed in claim 1, characterized in that the ratio of feed liquid of the eyeshield to aqueous solution of ethanol is 1 (20-60) g/mL.

3. The eye-care composition for alleviating asthenopia according to claim 1, wherein the plant extract further comprises safflower extract and chrysanthemum extract.

4. Use of the eyeshield composition for relieving asthenopia according to any one of claims 1-3 in preparation of a formulation having asthenopia relieving and vision improving effects;

the dosage forms of the preparation comprise solutions, powders, granules, tablets or capsules.

5. The use according to claim 4, wherein the preparation having the efficacy of relieving asthenopia and improving eyesight further comprises an auxiliary material.

6. The use according to claim 5, wherein the auxiliary materials comprise blueberry juice concentrate and high fructose syrup.