Moisturizing and eye-moistening composition as well as preparation method and application thereof

Abstract

The invention belongs to the technical field of compositions, and provides a moisture-retaining and eye-moistening composition as well as a preparation method and application thereof. According to the moisturizing eye-moistening composition provided by the invention, the soybean lecithin, the retinol palmitate lipidosome, the xanthophyll, the oligomeric hyaluronic acid and the ethylenediamine tetraacetic acid in a specific ratio are combined, and all the components can play a good synergistic effect, so that the effects of relieving asthenopia symptoms, protecting eyesight and maintaining normal vision are improved; the eye drops can improve and relieve eye dryness and eye astringency symptoms caused by various reasons (such as fatigue, wearing of contact lenses, use of electronic products, excessive use of eyes and the like).

Description

Technical Field

[0001] The present invention relates to the technical field of compositions, and more particularly, to a moisturizing eye care composition, a preparation method thereof, and an application thereof. Background Art

[0002] The "light" damage caused by insufficient intake or excessive consumption of lutein is the main cause of myopia, amblyopia, etc. At present, ophthalmic products for dry eyes and dryness caused by fatigue, wearing contact lenses, using electronic products, excessive eye use, etc. can only relieve the symptoms of dry eyes and dryness, and have no function of relieving visual fatigue symptoms, protecting eyesight, and maintaining normal vision.

[0003] Therefore, there is an urgent need to develop an eye care product that can not only relieve dry eyes and dryness, but also relieve visual fatigue, protect eyesight, and maintain normal vision. Summary of the Invention

[0004] The present invention aims to solve at least one of the technical problems existing in the above-mentioned prior art. For this purpose, the present invention provides a moisturizing eye care composition, a preparation method thereof, and an application thereof. The moisturizing eye care composition provided by the present invention can not only relieve the symptoms of dry eyes and dryness, but also relieve visual fatigue symptoms, protect eyesight, and maintain normal vision.

[0005] The first aspect of the present invention provides a moisturizing eye care composition.

[0006] Specifically, a moisturizing eye care composition, calculated by weight, comprises the following components:

[0007] 0.1 - 10 parts of soy lecithin, 1 - 5 parts of retinol palmitate liposome, 1.2 - 5 parts of lutein, 0.1 - 10 parts of oligomeric hyaluronic acid (oligomeric HA), and 0.01 - 10 parts of ethylenediaminetetraacetic acid (EDTA).

[0008] Lutein plays an important protective role in the macula of the retina, can effectively relieve visual fatigue symptoms and protect eyesight. The permeability of retinyl palmitate liposome is improved. The liposome is similar and compatible with the skin, and its sensitivity to light, temperature, oxygen, etc. is reduced, which can effectively maintain normal visual function. Oligomeric HA is itself a component of human skin, is an acidic mucopolysaccharide most widely distributed in the human body, exists in the matrix of connective tissue, has good moisturizing effect, and is used to relieve dry eye syndrome. The present invention adopts a combination of soybean lecithin, retinyl palmitate liposome, lutein, oligomeric hyaluronic acid and ethylenediaminetetraacetic acid in a specific ratio. Among them, the retinyl palmitate liposome reduces the sensitivity of the eyes to light, temperature, oxygen, etc., maintains normal visual function, thereby protecting eyesight, and lutein relieves visual fatigue symptoms and protects eyesight. The functions of retinyl palmitate liposome and lutein complement each other, and can not only relieve dryness and astringency of the eyes caused by fatigue, wearing contact lenses, using electronic products, overuse of eyes, etc., but also significantly improve the effects of relieving visual fatigue symptoms, protecting eyesight and maintaining normal vision.

[0009] Preferably, the moisturizing eye care composition further comprises at least one of a lubricant, a humectant, a pH buffer, menthol, and water.

[0010] More preferably, by weight, the moisturizing eye care composition further comprises 0.2 - 5 parts of a lubricant, 1 - 10 parts of a humectant, 0.02 - 15 parts of a pH buffer, 0.12 - 10 parts of menthol, and 80 - 100 parts of water.

[0011] Preferably, the lubricant is polyoxyethylene 40 hydrogenated castor oil.

[0012] Preferably, the humectant is polyethylene glycol 400 (PEG400) and / or glycerol.

[0013] Preferably, the pH buffer is sodium dihydrogen phosphate and / or disodium hydrogen phosphate.

[0014] More preferably, by weight, the components of the moisturizing eye care composition include: 0.1 - 10 parts of soybean lecithin, 1 - 5 parts of retinyl palmitate liposome, 1.2 - 5 parts of lutein, 0.1 - 10 parts of oligomeric hyaluronic acid, 0.01 - 10 parts of ethylenediaminetetraacetic acid, 0.2 - 5 parts of polyoxyethylene 40 hydrogenated castor oil, 0.2 - 5 parts of polyethylene glycol 400, 1 - 5 parts of glycerol, 0.042 - 3 parts of sodium dihydrogen phosphate, 0.25 - 10 parts of disodium hydrogen phosphate, 0.12 - 10 parts of menthol, and 80 - 100 parts of water.

[0015] PEG400, glycerol and water can be miscible in any proportion and are not easily volatile. They are used as humectants to absorb and retain moisture. Sodium dihydrogen phosphate and disodium hydrogen phosphate are used to adjust the acidity and alkalinity of the product, making the acidity and alkalinity, and osmotic pressure of the product close to the pH value and intraocular pressure of the eye environment. After using the product, no dehydration or water absorption occurs, so as to cause the intraocular pressure to increase or decrease. Sodium dihydrogen phosphate and disodium hydrogen phosphate act as pH buffers to jointly maintain the pH value of the product at neutral, maintain the stability of the product, do not cause irritation to the eyelids, and are gentle to the skin. Menthol is used as an irritant, acting on the skin or mucous membrane, having a cooling and antipruritic effect. A moisturizing product can be obtained without adding menthol, and a cooling product can be obtained after adding menthol.

[0016] The second aspect of the present invention provides a method for preparing a moisturizing eye composition.

[0017] A method for preparing a moisturizing eye composition includes the following steps:

[0018] (1) Take a solution containing soy lecithin as solution A;

[0019] (2) Add retinyl palmitate liposome, lutein, oligomeric hyaluronic acid and ethylenediaminetetraacetic acid to water in sequence, and mix to obtain solution B;

[0020] (3) Mix solution A and solution B to obtain the moisturizing eye composition.

[0021] Preferably, in step (1), the preparation method of the solution containing soy lecithin is: add water to soy lecithin, heat and stir at 80-90 °C for 10-20 min to obtain a solution containing soy lecithin. Heating helps soy lecithin dissolve faster.

[0022] Preferably, in step (2), add retinyl palmitate liposome, polyethylene glycol 400, lutein, oligomeric hyaluronic acid, ethylenediaminetetraacetic acid, glycerol, sodium dihydrogen phosphate and disodium hydrogen phosphate to water in sequence, and stir until completely dissolved to obtain solution B; or; add retinyl palmitate liposome, polyethylene glycol 400, lutein, oligomeric hyaluronic acid, menthol, ethylenediaminetetraacetic acid, glycerol, sodium dihydrogen phosphate and disodium hydrogen phosphate to water in sequence, and stir until completely dissolved to obtain solution B.

[0023] The third aspect of the present invention provides an application of a moisturizing eye composition.

[0024] An application of a moisturizing eye composition in the preparation of ophthalmic products.

[0025] The fourth aspect of the present invention provides an ophthalmic spray product.

[0026] An ophthalmic spray product includes the moisturizing eye composition.

[0027] Preferably, the ophthalmic spray product is used by spraying it on the surface of the eyelid after closing the eyes.

[0028] Currently, most ophthalmic products are used by directly dropping the liquid onto the eyeball, but many groups, especially children, are quite resistant to it. Moreover, due to the entry of foreign objects into the eyeball, the eyeball will reflexively protect itself and blink, resulting in waste of the liquid and a decline in the therapeutic effect. However, the ophthalmic spray product provided by the present invention can not only relieve dry eyes and dryness and discomfort in the eyes, but also relieve symptoms of visual fatigue, protect eyesight and maintain normal vision. Moreover, by spraying it onto the eyeball, it is mild and non-irritating, improving acceptance, not easily causing waste of the liquid, and also ensuring a good therapeutic effect.

[0029] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0030] The moisturizing eye care composition provided by the present invention adopts a combination of soybean lecithin, retinol palmitate liposome, lutein, oligomeric hyaluronic acid and ethylenediaminetetraacetic acid in a specific ratio. Each component can play a good synergistic effect, improving the effects of relieving visual fatigue, protecting eyesight and maintaining normal vision, and can improve the symptoms of dry eyes and dryness and discomfort in the eyes caused by various reasons (such as fatigue, wearing contact lenses, using electronic products, overusing eyes, etc.). Detailed implementation manners

[0031] In order to make those skilled in the art more clearly understand the technical solutions described in the present invention, the following examples are listed for illustration. It should be noted that the following examples do not limit the scope of protection required by the present invention.

[0032] Unless otherwise specified, the raw materials, reagents or devices used in the following examples can all be obtained from conventional commercial channels or can be obtained by existing known methods.

[0033] The main raw material sources used in the examples and comparative examples of the present invention are as follows:

[0034] Soybean lecithin: Produced by Henan Siwei Biotechnology Co., Ltd., peroxide value ≤5.

[0035] Retinol palmitate liposome: Produced by Guangzhou Zhongkang Medical Technology Co., Ltd., pH value (1% aqueous solution, 20 °C) is 6 - 7.

[0036] Lutein: Produced by Guangzhou Baoyi Biotechnology Co., Ltd., water-soluble, pH value 4.0 - 8.0.

[0037] Oligomeric HA: Produced by Dongying First Biotechnology Co., Ltd., average relative molecular mass <10KDa.

[0038] PEG400: Produced by Xi'an Taihua Pharmaceutical Technology Co., Ltd., with an average molecular weight of 380 - 420 and an acidity of 4.0 - 7.0.

[0039] Polyoxyl 40 Hydrogenated Castor Oil: BASF(China)Co., Ltd., Shanghai, with a maximum acid value of 0.8 mg KOH / g.

[0040] EDTA: Produced by Chengdu Huayi Pharmaceutical Excipients Manufacturing Co., Ltd., with a pH value of 4.0 - 5.0.

[0041] Menthol: Produced by Guangzhou Fuyou New Material Technology Co., Ltd., water-soluble, with a pH value (1% aqueous solution, 20 °C) of 5.5 - 8.5.

[0042] Example 1 (Moisturizing Type)

[0043] A moisturizing eye care composition, by weight, includes the components shown in Table 1.

[0044] The preparation method of the above moisturizing eye care composition includes the following steps:

[0045] (1) Take water and add it to soy lecithin, heat and stir at 85 ± 2 °C for 15 min to obtain Solution A;

[0046] (2) Add retinyl palmitate liposome, PEG400, lutein, oligomeric HA, EDTA, glycerol, sodium dihydrogen phosphate monohydrate, and disodium hydrogen phosphate dodecahydrate to water in sequence and stir until completely dissolved to obtain Solution B;

[0047] (3) Mix Solution A and Solution B to obtain the moisturizing eye care composition, and the product performance is stable.

[0048] Example 2 (Moisturizing Type)

[0049] A moisturizing eye care composition, by weight, includes the components shown in Table 1.

[0050] The above moisturizing eye care composition is the same as that in Example 1.

[0051] Example 3 (Moisturizing Type)

[0052] A moisturizing eye care composition, by weight, includes the components shown in Table 1.

[0053] The above moisturizing eye care composition is the same as that in Example 1.

[0054] Example 4 (Refreshing Type)

[0055] A moisturizing eye care composition, which is different from that in Example 1 in that 0.12 parts of menthol are added.

[0056] The preparation method of the above-mentioned moisturizing eye care composition comprises the following steps:

[0057] (1) Add water to soy lecithin, heat and stir at 85 ± 2 °C for 15 min to obtain liquid A;

[0058] (2) Add retinyl palmitate liposome, PEG400, lutein, oligomeric HA, menthol, EDTA, glycerol, sodium dihydrogen phosphate monohydrate, and disodium hydrogen phosphate dodecahydrate to water in sequence and stir until completely dissolved to obtain liquid B;

[0059] (3) Mix liquid A and liquid B to obtain the product, and the product has stable performance.

[0060] Example 5 (refreshing type)

[0061] A moisturizing eye care composition, which is different from Example 2 in that 10 parts of menthol are added. The preparation method is the same as that of Example 4.

[0062] Comparative Example 1

[0063] A composition, which is different from Example 1 in that it does not contain lutein.

[0064] Comparative Example 2

[0065] A composition, which is different from Example 1 in that it does not contain retinyl palmitate liposome.

[0066] Comparative Example 3

[0067] A composition, which is different from Example 1 in that the amount of soy lecithin is reduced to 0.05 part.

[0068] Comparative Example 4

[0069] A composition, which is different from Example 1 in that PEG400 is replaced with an equal weight part of PEG200.

[0070] Comparative Example 5

[0071] A composition, which is different from Example 1 in that it does not contain oligomeric HA.

[0072] Comparative Example 6

[0073] A composition, which is different from Example 1 in that the amount of soy lecithin is increased to 15 parts.

[0074] Comparative Example 7

[0075] A composition, which is different from Example 1 in that oligomeric hyaluronic acid is replaced with an equal weight part of hyaluronic acid.

[0076] Comparative Example 8

[0077] A composition, which is different from that in Example 1 in that the preparation method is changed to:

[0078] (1) Take water and add it to soy lecithin, heat and stir at 85 °C for 15 min, then add retinyl palmitate liposome and lutein to obtain Solution A;

[0079] (2) Add PEG400, oligomeric HA, EDTA, glycerol, sodium dihydrogen phosphate monohydrate, and disodium hydrogen phosphate dodecahydrate to water in sequence and stir until completely dissolved to obtain Solution B;

[0080] (3) Mix Solution A and Solution B to obtain the composition.

[0081] The components and their dosages of each example are shown in Table 1 below:

[0082] Table 1 Components and Dosages of Each Example (parts by weight)

[0083]

[0084]

[0085] Product effect test

[0086] Screen 130 patients with dry eyes, dry and astringent eyes, and eye fatigue caused by video terminals. They meet the diagnostic criteria of "Expert Consensus on the Diagnosis and Treatment of Visual Fatigue (2014)", and all have eye itching, dry eyes, dry and astringent eyes and other eye symptoms after long-term use of electronic products such as computers, mobile phones, and TVs. Randomly divide them into 13 groups, with 10 people in each group, and test the effects of the products of different examples and comparative examples respectively. The patients are aged 18 - 40 years old, and the continuous use time of the video terminal is > 5 h per day. The patients are informed and consent. Exclusion criteria: (1) Patients with eye fatigue caused by other reasons; (2) Patients with other eye diseases; (3) Those who have received relevant treatment 2 weeks before enrollment; (4) Those who are allergic to the ingredients of this product; (5) Patients with mental disorders; (6) Women in pregnancy or lactation.

[0087] Product usage method: Use with eyes closed, keep a distance of about 10 cm with eyes closed, spray the product on the eyelids, spray 1 - 2 times each time, 3 - 4 times a day.

[0088] Eye symptom scoring criteria: Before treatment and 4 weeks after treatment, the eye symptoms (including dry eyes, dry and astringent eyes, and eye fatigue) of each group of patients are scored at 4 levels according to the severity. Among them, no symptoms are 0 points, mild symptoms are 2 points, moderate symptoms are 4 points, and severe symptoms are 6 points.

[0089] Vision test: Test the vision of the patients before and after treatment. The treatment time is 4 weeks. The specific method is: Dilate the pupils with the drug compound tropicamide, and after half an hour, perform refractive detection with an optometry device.

[0090] Statistical methods were used to analyze the data with SPSS 22.0; measurements were expressed as , and chi-square and t-tests were performed respectively; P < 0.05 was considered statistically significant.

[0091] Table 2 Results of the efficacy tests for each example and comparative example

[0092]

[0093]

[0094] As can be seen from the above table, the moisturizing eye care compositions provided in Examples 1-5 of the present invention have a significant effect of alleviating dry eyes, dry and astringent eyes, and eye fatigue, which helps to relieve eye symptoms and increase the eye comfort of patients. They can be used for symptoms such as dry eyes and dry and astringent eyes caused by fatigue, wearing contact lenses, using electronic products, overusing eyes, etc. Moreover, they can protect eyesight, maintain the function of normal vision, have a certain protective effect on eyesight, and even can achieve a certain improvement effect (the naked eye vision after treatment is improved). In addition, they are easy to use, low in price, good in safety, and can be widely promoted.

[0095] Compared with Example 1, Comparative Example 1 and Comparative Example 2 do not contain lutein and retinol palmitate liposomes respectively, resulting in a significant decrease in the effect of alleviating dry eyes, dry and astringent eyes, and eye fatigue, and the effect on protecting eyesight is not obvious.

[0096] Compared with Example 1, in Comparative Example 3, the amount of soy lecithin was reduced, making it difficult to interact with other components, resulting in a significant decrease in the effect of alleviating dry eyes, dry and astringent eyes, and eye fatigue, and it did not play a role in protecting eyesight. Long-term use of the composition of Comparative Example 3, without alleviating the uncomfortable eye symptoms (dry eyes, dry and astringent eyes, and eye fatigue), continuous eye use may even lead to a decrease in eyesight.

[0097] Compared with Example 1, in Comparative Example 4, PEG400 was replaced with an equal weight of PEG200, resulting in a significant decrease in the effect of alleviating dry eyes, dry and astringent eyes, and eye fatigue, and it could not play a role in protecting eyesight.

[0098] Compared with Example 1, Comparative Example 5 does not contain oligomeric HA, resulting in a significant decrease in the effect of alleviating dry eyes, dry and astringent eyes, and eye fatigue, and it could not play a role in protecting eyesight.

[0099] Compared with Example 1, in Comparative Example 6, the amount of soy lecithin was increased, resulting in the inability to quickly penetrate the skin and play a role. Therefore, the effect of alleviating dry eyes, dry and astringent eyes, and eye fatigue was significantly decreased, and it could not play a role in protecting eyesight.

[0100] Compared with Example 1, in Comparative Example 7, the oligomeric HA was replaced with an equal weight of HA, resulting in a significant decrease in the effects of alleviating dry eyes, dry and astringent eyes, and eye fatigue. HA has a large molecular weight (the weight-average molecular weight of HA is 500 - 730 KDa, and the average relative molecular weight of oligomeric HA < 10 KDa), while the oligomeric HA used in Example 1 has a much smaller molecular weight. It can not only eliminate the reactive oxygen free radicals induced by sunlight irradiation, improve the cellular antioxidant capacity, but also enhance the skin's defense against UVB. It also has biological activity, can be better absorbed through the eyelid, has a good moisturizing effect, and can synergize with other components to improve the effects of alleviating dry eyes, dry and astringent eyes, and eye fatigue. Moreover, it does not play a role in protecting eyesight. Long-term use of the composition in Comparative Example 7 may even lead to a decline in eyesight when the discomfort symptoms of the eyes (dry eyes, dry and astringent eyes, and eye fatigue) are not alleviated and continuous eye use persists.

[0101] Compared with Example 1, in Comparative Example 8, the mixing method of the components was changed. Since retinol palmitate liposomes and lutein are not heat-resistant and will be degraded at this temperature, losing their original properties, the effects of the composition in alleviating dry eyes, dry and astringent eyes, and eye fatigue were significantly decreased, and it also did not play a role in protecting eyesight.

Claims

1. A moisturizing eye-moistening composition, characterized in that: According to parts by weight, it includes the following components: 0.1-10 parts of soybean lecithin, 1-5 parts of retinol palmitate liposome, 1.2-5 parts of lutein, 0.1-10 parts of oligomeric hyaluronic acid, and 0.01-10 parts of ethylenediaminetetraacetic acid.

2. The moisturizing eye-moistening composition according to claim 1, characterized in that: The moisturizing eye-moistening composition further comprises at least one of a lubricant, a humectant, a pH buffer, menthol and water.

3. The moisturizing eye-moistening composition according to claim 2, characterized in that: In parts by weight, the moisturizing eye-moistening composition further comprises 0.2-5 parts of lubricant, 1-10 parts of moisturizing agent, 0.02-15 parts of pH buffer, 0.12-10 parts of menthol and 80-100 parts of water.

4. The moisturizing eye-moistening composition according to claim 3, characterized in that: The lubricant is polyoxyethylene 40 hydrogenated castor oil.

5. The moisturizing eye-moistening composition according to claim 4, characterized in that: The moisturizing agent is polyethylene glycol 400 and / or glycerol.

6. The moisturizing eye-moistening composition according to claim 5, characterized in that: The pH buffer is sodium dihydrogen phosphate and / or disodium hydrogen phosphate.

7. The moisturizing eye-moistening composition according to claim 6, characterized in that: In parts by weight, the components of the moisturizing eye-moistening composition include: 0.1-10 parts of soy lecithin, 1-5 parts of retinol palmitate liposomes, 1.2-5 parts of lutein, 0.1-10 parts of oligomeric hyaluronic acid, 0.01-10 parts of ethylenediaminetetraacetic acid, 0.2-5 parts of polyoxyethylene 40 hydrogenated castor oil, 0.2-5 parts of polyethylene glycol 400, 1-5 parts of glycerol, 0.042-3 parts of sodium dihydrogen phosphate, 0.25-10 parts of disodium hydrogen phosphate, 0.12-10 parts of menthol and 80-100 parts of water.

8. The method for preparing the moisturizing eye-moistening composition according to any one of claims 1 to 7, characterized in that: The steps include: (1) taking a solution containing soybean lecithin as solution A; (2) adding retinol palmitate liposomes, lutein, oligomeric hyaluronic acid and ethylenediaminetetraacetic acid to water in sequence and mixing to obtain liquid B; (3) Mixing liquid A and liquid B to obtain the moisturizing eye-moistening composition.

9. The preparation method according to claim 8, characterized in that: In step (1), the preparation method of the solution containing soybean lecithin is: adding water to soybean lecithin, heating and stirring at 80-90° C. for 10-20 minutes to obtain a solution containing soybean lecithin.

10. The preparation method according to claim 8, characterized in that: In step (2), retinol palmitate liposomes, polyethylene glycol 400, lutein, oligomeric hyaluronic acid, ethylenediaminetetraacetic acid, glycerol, sodium dihydrogen phosphate and disodium hydrogen phosphate are added to water in sequence and stirred until completely dissolved to obtain liquid B; or; retinol palmitate liposomes, polyethylene glycol 400, lutein, oligomeric hyaluronic acid, menthol, ethylenediaminetetraacetic acid, glycerol, sodium dihydrogen phosphate and disodium hydrogen phosphate are added to water in sequence and stirred until completely dissolved to obtain liquid B.

11. Use of the moisturizing eye-moistening composition according to any one of claims 1 to 7 in the preparation of ophthalmic products.

12. An ophthalmic spray product comprising the moisturizing eye-moistening composition according to any one of claims 1 to 7.

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