Composition for relieving pseudomyopia of eyes and preparation process thereof

Abstract

The invention provides a composition for relieving pseudomyopia of eyes and a preparation process thereof, and relates to the technical field of traditional Chinese medicine compositions.The composition is prepared from borneol, L-menthol, plants rich in flavone, plants rich in amino acid, pollen typhae, radix salviae miltiorrhizae, radix angelicae sinensis and / or polysorbate-80. The invention also provides a preparation process. The preparation process comprises the following steps: mixing and crushing the flavone-rich plants and the pollen typhae, and performing alcohol extraction to obtain an extracting solution 1; crushing plants rich in amino acid and angelica sinensis, and performing enzymolysis to obtain an extracting solution 2; soaking radix salviae miltiorrhizae powder with water to obtain an extracting solution 3; carrying out lipidosome treatment; and mixing the liposome solution, borneol, L-menthol and / or polysorbate-80 to obtain the composition. The composition disclosed by the invention is good in permeability, good in drug effect and strong in targeting property when being applied to the myopia treatment process.

Description

Technical Field

[0001] The invention relates to the technical field of traditional Chinese medicine compositions, and in particular to a composition for alleviating eye pseudomyopia and a preparation process thereof. Background Art

[0002] As the pace of life in modern society accelerates, people spend more time using their eyes, especially young people, who spend a long time in close contact with books, electronic devices, and other close-up scenes, and their eye problems are becoming increasingly prominent. Among them, the incidence of pseudomyopia has been increasing year by year, becoming one of the important factors affecting vision health.

[0003] Pseudomyopia, also known as accommodative myopia, is mainly caused by long-term close-up use of the eyes, which leads to continuous contraction and spasm of the ciliary muscle and increased thickness of the lens, thus changing the refractive power of the eye and causing temporary vision loss. If not intervened in time, pseudomyopia can easily develop into true myopia, causing long-term vision problems for patients.

[0004] At present, there are various treatment methods for pseudomyopia, but they all have certain limitations. Although the traditional correction method of fitting glasses can temporarily improve the clarity of vision, it cannot fundamentally solve the problem of ciliary muscle spasm and is not effective in delaying the development of myopia. Some eye drops contain mydriatic ingredients, which can relax the ciliary muscle in the short term, but long-term use may cause eye discomfort, such as dryness, photophobia and other adverse reactions, and there is a risk of drug dependence; some eye drops simply stimulate the eyes through cooling ingredients, and the soothing effect is short-lived, making it difficult to achieve the purpose of continuously relieving ciliary muscle tension.

[0005] In terms of physical therapy, eye exercises have certain health-care effects, can promote blood circulation in the eyes, and relieve some fatigue, but the operation techniques are strict, and teenagers often find it difficult to perform them in a standardized manner, and the effects vary. Eye massagers stimulate eye acupoints by massaging, and have certain effects in relaxing eye muscles, but the instruments are inconvenient to carry, the use scenarios are limited, and the massage intensity and accuracy of the parts are difficult to guarantee, so the degree of relief for pseudomyopia is limited.

[0006] In the field of pharmaceutical compositions, although some existing traditional Chinese medicine prescriptions claim to be effective for eye diseases, most of them lack accurate component analysis and modern process optimization, have low extraction rates of effective ingredients, and poor formulation stability, resulting in unstable actual application effects and failure to meet clinical needs. Western medicine compositions also face problems such as large side effects and weak targeting, making it difficult to accurately act on the ciliary muscles of the eye and achieve long-term relief.

[0007] Topical eye patches are very common items for relieving pseudomyopia, but during the application process the drug must pass through the skin barrier in order to be effective, so the drug ingredients in common eye patches have poor permeability.

[0008] The compositions or drugs used to treat pseudomyopia in the prior art have poor effects, weak targeting and poor permeability. Summary of the invention

[0009] The invention provides a composition for alleviating pseudomyopia of the eye and a preparation process thereof, so as to solve the technical problems in the prior art of poor permeability, poor drug effect and weak targeting of external dressings used for treating pseudomyopia.

[0010] In order to achieve the above-mentioned invention object, the technical solution provided by the present invention is as follows:

[0011] A preparation process of the composition for alleviating ocular pseudomyopia as described above comprises the following steps:

[0012] S1, mixing and crushing the flavonoid-rich plants and Pollen Typhae to obtain an alcohol-extracted powder, and putting the alcohol-extracted powder into ethanol at a ratio of 1 g to 20-25 mL for alcohol extraction, filtering and concentrating until the volume of the alcohol-extracted solution is reduced by 2 / 3-4 / 5, to obtain an extract 1;

[0013] S2, crushing the amino acid-rich plants and angelica to obtain enzymolysis powder, adding the enzymolysis powder to acetic acid-sodium acetate buffer at a ratio of 1 g: 12-15 mL, adjusting the pH value to 4.5-6.0, and then adding cellulase and pectinase to perform the first enzymolysis, wherein the temperature of the first enzymolysis is 40-50° C., and the time is 2-4 h, to obtain a first reaction solution;

[0014] S3, adding disodium hydrogen phosphate to the first reaction solution to adjust the pH value to 6, adding papain and ficin for a second enzymolysis, wherein the mass ratio of papain to ficin is 1:1-2, the temperature of the second enzymolysis is 50-55°C, the time is 3-5h, and the volume of the enzymolysis solution is reduced by 2 / 3 through enzyme inactivation, filtration and concentration, to obtain extract 2;

[0015] S4, crushing Danshen to obtain Danshen powder, adding Danshen powder to water at a solid-liquid ratio of 1g:10-12mL, keeping warm at 90-100°C for 1-2 hours, filtering to obtain an extraction solution, and concentrating to reduce the volume of the extraction solution by 2 / 3 to obtain extract 3;

[0016] S5. Dissolve the phospholipid in an ethanol-water solution, remove the ethanol and water by rotary evaporation in a round-bottom flask, form a phospholipid film on the inner wall of the round-bottom flask, and then add the extract 1, extract 2, and extract 3 in a mass ratio of 1-10:10:2.5-3.2, and perform ultrasonic dispersion at 35-45° C. to disperse the phospholipid film to obtain a liposome solution.

[0017] Ultrasonic dispersion in S5 allows the phospholipid film to interact with a specific liquid (a mixture of extract 1, extract 2, and extract 3), causing the phospholipid molecules to absorb water again and disperse. From a molecular level, phospholipid molecules have a hydrophilic head and a hydrophobic tail. When added to the mixed liquid, the hydrophilic head interacts with the water molecules and other polar components in the liquid, causing the phospholipid molecules to gradually disperse from the film state.

[0018] S6. Mixing the liposome solution, borneol, L-menthol and / or polysorbate 80 to obtain the composition.

[0019] Preferably, the mass ratio of the flavonoid-rich plant to the pollen of Typha aquatica in S1 is 10:2-4, and the average particle size of the alcohol-extracted powder is 180-250 microns.

[0020] Preferably, the alcohol extraction time in S1 is 24-48 hours and the temperature is 35-45°C.

[0021] Preferably, the mass ratio of the amino acid-rich plant to Angelica sinensis in S2 is 10:2-3, and the average particle size of the enzymatic hydrolysis powder is 100-150 microns.

[0022] Preferably, the concentration of the ethanol aqueous solution in S5 is 55-70wt%.

[0023] Preferably, in S6, the liposome solution is 80-90 parts by mass, borneol is 0.1-1 part by mass, L-menthol is 0.1-1 part by mass, and polysorbate 80 is 0.5-2 parts by mass.

[0024] Preferably, the flavonoid-rich plants are one or more of Chuanxiong, ginseng, cassia seed, mulberry, blueberry, angelica, and ginkgo.

[0025] Preferably, the plants rich in amino acids are one or more of soybeans and nuts.

[0026] The present invention also provides a composition for alleviating eye pseudomyopia prepared according to the above preparation process.

[0027] An application of the composition as described above, wherein the composition, carbomer and sodium hyaluronate are mixed for preparing eye dressing, wherein the mass ratio of the composition, carbomer and sodium hyaluronate is 100:0.1-1:0.01-1.

[0028] Pseudomyopia is usually caused by excessive use of the eyes, which leads to continuous contraction and spasm of the ciliary muscle, lengthening of the lens axis distance and increasing thickness. When the eyes need to see close objects, nerve signals regulate the contraction of the ciliary muscle by releasing acetylcholine. Long-term close-range use of the eyes causes the continuous release of acetylcholine, which keeps the ciliary muscle in a contracted state, causing disorders in the release and metabolic regulation mechanism of acetylcholine. For example, abnormal activity of acetylcholinesterase (an enzyme that breaks down acetylcholine) causes acetylcholine to be unable to be broken down in time, and the ciliary muscle will continue to receive contraction signals, making it difficult to recover from the spasm.

[0029] When the excitation of the presynaptic neuron reaches the terminal of its axon branch, the presynaptic membrane responds to Ca 2+ The permeability of Ca 2+ Influx causes synaptic vesicles to move to the presynaptic membrane and fuse with it, releasing acetylcholine in the form of exocytosis. After acetylcholine is released into the synaptic cleft, it binds to the acetylcholine receptor on the postsynaptic membrane, causing the ion channels on the postsynaptic membrane to open, causing changes in the activity of the postsynaptic neuron, and then producing specific neural effects.

[0030] The effective ingredients in the flavonoid-rich plants and the water candle pollen can be extracted through the alcohol extraction process, and the extract 1 contains rich flavonoid compounds. Flavonoid compounds are a natural antioxidant. It can inhibit the generation of free radicals in the body and reduce the damage of free radicals to vascular endothelial cells. First, the phenolic hydroxyl structure of flavonoids can combine with thromboxane A2 (TXA2) to reduce the aggregation of platelets. When the vascular endothelial cells are in a good state, it helps the normal relaxation of blood vessels, which is more conducive to blood flow. After flavonoids improve the blood circulation of the eyes, it helps to relieve the tension of the ciliary muscles. Secondly, the phenolic hydroxyl structure of flavonoids can interact with the calcium ion channel protein on the cell membrane, control the calcium ions in and out of the cells, and then reduce the release of acetylcholine, so as to achieve the purpose of relaxing the ciliary muscles.

[0031] In addition, cellulase and pectinase are selected to destroy the cell wall structure for plants and angelica containing amino acids, so that the effective ingredients in the cells are more easily released. At the same time, trypsin and papain are added to hydrolyze the protein in the plant to release amino acids. The composition of the present invention is rich in amino acids, acetylcholine is a neurotransmitter synthesized by choline and acetyl coenzyme A under the catalysis of choline acetyltransferase, there is a quaternary ammonium group with a positive charge in the molecule, and the acidic structure of amino acids is negatively charged at the same time, and the two are like "lock and key", combined together by the effect of ionic bonds, thereby blocking the combination of acetylcholine and the acetylcholine receptor on the postsynaptic membrane, and achieving the effect of relaxing the ciliary muscle.

[0032] In order to improve the permeability and effect of the effective substances in the composition in the eye, the flavonoids, amino acids and salvia miltiorrhiza extracts in the present invention are compounded into the liposome solution. There are many barriers in the eye tissue, such as corneal barriers, conjunctival barriers, etc. The cornea is composed of a multilayer structure, and its epithelial layer is the main barrier to prevent foreign substances from entering the eye. Under normal circumstances, many drug molecules are difficult to penetrate these barriers to reach the target tissue in the eye due to their size, hydrophilicity and hydrophobicity. The nanometer particle size of the liposome (generally between 100-500nm) enables it to match the cell gap size of the eye barrier. For example, the tight junction gap between corneal epithelial cells is about 2-5nm, and the liposome can enter the deep tissue of the cornea through these gaps. The liposome is mainly composed of a phospholipid bilayer, with a hydrophilic head and a hydrophobic tail. This structure enables it to have good compatibility with the cell membrane of the eye tissue. For hydrophilic effective ingredients, the internal aqueous core of the liposome can wrap them; for lipophilic ingredients, the phospholipid bilayer of the liposome can accommodate them. When liposomes come into contact with ocular tissues, based on the principle of like dissolves like, they can better fuse with the cell membrane, thereby promoting the penetration of active ingredients. For example, liposomes containing lipophilic flavonoids can fuse with the phospholipid layer of the corneal cell membrane and deliver flavonoids directly into the corneal cells.

[0033] Different tissues in the eye have different importance in treating pseudomyopia, such as ciliary muscle, which is a key tissue for regulating vision. Liposomes can be modified on their surface (such as connecting specific antibodies or ligands) to enable them to specifically recognize and bind to receptors on the surface of ciliary muscle cells, thereby achieving precise targeted drug delivery. For example, small molecule ligands that can bind to acetylcholine receptors on ciliary muscle cells are connected to the surface of liposomes, so that liposomes can carry active ingredients and preferentially gather around the ciliary muscles, thereby increasing the concentration of active ingredients in the ciliary muscles and enhancing the effect of relieving the tension of the ciliary muscles.

[0034] Liposomes can slowly release active ingredients in ocular tissues. This is because the interaction between liposomes and ocular tissues is a gradual process, and their phospholipid bilayers will gradually degrade in the tissues, allowing the encapsulated active ingredients to be continuously released. For example, after entering the perivascular tissues of the eye, liposomes containing Danshen extract will continue to release the active ingredients in the extract for hours or even days, maintaining the state of ocular vasodilation and improved blood circulation, and providing lasting support for relieving eye fatigue and pseudomyopia.

[0035] Polysorbate-80 can increase the permeability of the stratum corneum of the skin. They can interact with skin lipids, disrupt the orderly arrangement of lipids, and thus create channels for the absorption of amino acids. At the same time, polysorbate-80 can wrap amino acid molecules, allowing them to be better dispersed on the skin surface and increase the contact area with the skin. L-Menthol has a strong ability to form hydrogen bonds, and can compete for hydrogen bonding sites in the stratum corneum, allowing the drug to be freed from the stratum corneum and transported to penetrate into the deep layers of the skin. The two substances used together can affect the permeability of different layers of the skin to drugs, namely the stratum corneum and the substratum corneum. When the two substances are used together, they act together on the skin to overcome the barrier function of the entire cortex and allow the drug to penetrate into the eyes. This effect reduces the retention of drugs in the skin.

[0036] The mixed use of water candle pollen, angelica and salvia can enrich the microvascular circulation in the choroid, improve the local blood supply, and inhibit the progressive thinning of the retina, choroid and sclera. At the same time, it can inhibit the progression of pseudomyopia by regulating the related expressions of MMP-2 and HIF-1α in the choroid and sclera.

[0037] The technical solution of the present invention has at least the following beneficial effects compared with the prior art:

[0038] (1) The composition of the present invention is rich in flavonoids and amino acids, which can reduce the release of acetylcholine, thereby achieving the purpose of relaxing the ciliary muscle and effectively preventing pseudomyopia;

[0039] (2) By modifying flavonoids and encapsulating the active ingredients in liposomes, the permeability of the active ingredients is enhanced and the therapeutic effect is improved;

[0040] (3) Adding polysorbate-80 and L-menthol overcomes the barrier function of the entire cortex, allowing the drug to penetrate into the eye and improve the targeting of the drug;

[0041] (4) Use different extraction methods for different ingredients to improve the dissolution of effective substances, realize the small molecule size of effective substances, and promote the absorption of effective substances. DETAILED DESCRIPTION

[0042] In order to make the purpose, technical scheme and advantages of the embodiments of the present invention clearer, the technical scheme of the embodiments of the present invention will be clearly and completely described below. Obviously, the described embodiments are part of the embodiments of the present invention, not all of them. Based on the described embodiments of the present invention, all other embodiments obtained by ordinary technicians in the field without creative labor are within the scope of protection of the present invention. Sodium hyaluronate: Article No.: Q-0174810, molecular weight: 0.8-1.5Milliion Da, Xi'an Qiyue Biology. Cellulase: enzyme activity parameter 50,000 U / g. Pectinase: enzyme activity parameter 50,000 U / g. Papain: enzyme activity parameter 100,000 U / g. Fig protease: enzyme activity parameter 100,000 U / g.

[0043] Example 1

[0044] The present embodiment provides a composition for alleviating pseudomyopia of the eye, and the raw materials thereof include: borneol, L-menthol, Chuanxiong, ginseng, soybean, pollen pollen, salvia miltiorrhiza, angelica sinensis and polysorbate 80.

[0045] A preparation process of the composition for alleviating ocular pseudomyopia in this embodiment comprises the following steps:

[0046] S1. Mix and crush Chuanxiong, ginseng and pollen pollen in a mass ratio of 5:5:2 to obtain an alcohol-extracted powder with an average particle size of 180 μm, and put the alcohol-extracted powder into ethanol at a solid-liquid ratio of 1 g:20 mL for alcohol extraction. The extraction time is 24 h at a temperature of 45° C., and the filtrate is concentrated at a temperature of 50° C. and a pressure of 0.01 MPa until the volume of the alcohol-extracted solution is reduced by 4 / 5 to obtain an extract 1.

[0047] S2, soybean and angelica were mixed and crushed in a mass ratio of 10:2 to obtain an enzymatic hydrolysis powder with an average particle size of 100 microns, and the enzymatic hydrolysis powder was added to an acetic acid-sodium acetate buffer in a ratio of 1g:12mL of solid-liquid ratio, and the pH value was adjusted to 4.5, and then cellulase and pectinase (the mass ratio of the two was 1:1) were added for the first enzymatic hydrolysis, the sum of the mass of the cellulase and the pectinase was 1% of the mass of the enzymatic hydrolysis powder, the temperature of the first enzymatic hydrolysis was 40°C, and the time was 4h, to obtain a first reaction solution;

[0048] S3, adding disodium hydrogen phosphate to the first reaction solution to adjust the pH value to 6, adding papain and ficin for a second enzymolysis, wherein the mass ratio of papain to ficin is 1:1, and the total amount of papain and ficin added is 0.5% of the mass of the enzymolysis powder, the temperature of the second enzymolysis is 50°C, the time is 5h, the enzyme is inactivated, filtered, and concentrated under reduced pressure at 60°C and 0.005MPa to reduce the volume of the enzymolysis solution by two thirds, to obtain extract 2;

[0049] S4, crushing Danshen to obtain Danshen powder, adding Danshen powder to water at a solid-liquid ratio of 1g:10mL, keeping warm at 90°C for 1 hour, filtering, and concentrating under reduced pressure at 60°C and 0.005MPa until the volume of the extraction solution is reduced by two thirds, to obtain extract 3;

[0050] S5, dissolving soybean lecithin in an ethanol aqueous solution at 45°C (the added mass of the ethanol aqueous solution is 35 times the mass of the phospholipids, and the concentration of the ethanol aqueous solution is 60wt%), removing ethanol and water by rotary evaporation in a round-bottom flask, forming a phospholipid film on the inner wall of the round-bottom flask, and then adding the extract 1, extract 2 and extract 3 in a mass ratio of 1:10:2.5, the total mass of extract 1, extract 2 and extract 3 is 5 times the mass of soybean lecithin, and ultrasonically dispersing at 100W for 25min at a temperature of 35°C to disperse the phospholipid film to obtain a liposome solution;

[0051] S6. Mix 80 parts of the liposome solution, 0.1 parts of borneol, 0.1 parts of L-menthol, and 0.5 parts of polysorbate 80 by mass to obtain the composition.

[0052] An application of the composition as described above, wherein the composition, carbomer 940 and sodium hyaluronate are mixed and used to prepare an eye dressing, wherein the mass ratio of the composition, carbomer 940 and sodium hyaluronate is 100:0.1:0.01.

[0053] Example 2

[0054] This embodiment provides a composition for alleviating pseudomyopia of the eye, and its raw materials include: borneol, L-menthol, cassia seed, mulberry, peanut, pollen pollen, salvia miltiorrhiza, angelica sinensis and polysorbate 80.

[0055] A preparation process of the composition for alleviating ocular pseudomyopia in this embodiment comprises the following steps:

[0056] S1. Mix Cassia seed, mulberry and Pollen Typhae in a mass ratio of 5:5:4, crush them to obtain an alcohol-extracted powder with an average particle size of 250 μm, put the alcohol-extracted powder into ethanol in a solid-liquid ratio of 1 g:25 mL for alcohol extraction, the extraction time is 48 h, the temperature is 35° C., filter, and concentrate the filtrate at a temperature of 50° C. and a pressure of 0.01 MPa until the volume of the alcohol-extracted solution is reduced by 2 / 3 to obtain an extract 1;

[0057] S2. Peanuts and angelica are mixed and crushed in a mass ratio of 10:3 to obtain an enzymatic hydrolysis powder with an average particle size of 150 microns. The enzymatic hydrolysis powder is added to an acetic acid-sodium acetate buffer in a ratio of 1 g:15 mL of a solid-liquid ratio. After the pH value is adjusted to 6.0, cellulase and pectinase (the mass ratio of the two is 1:1) are added to perform the first enzymatic hydrolysis. The sum of the mass of the cellulase and the pectinase is 1% of the mass of the enzymatic hydrolysis powder. The temperature of the first enzymatic hydrolysis is 50° C. and the time is 2 h to obtain a first reaction solution.

[0058] S3, adding disodium hydrogen phosphate to the first reaction solution to adjust the pH value to 6, adding papain and ficin for a second enzymolysis, wherein the mass ratio of papain to ficin is 1:2, and the total amount of papain and ficin added is 0.5% of the mass of the enzymolysis powder, the temperature of the second enzymolysis is 55°C, the time is 3h, the enzyme is inactivated, filtered, and concentrated under reduced pressure at 60°C and 0.005MPa to reduce the volume of the enzymolysis solution by two thirds, to obtain extract 2;

[0059] S4, crushing Danshen to obtain Danshen powder, adding Danshen powder to water at a solid-liquid ratio of 1g:12mL, keeping warm at 100°C for 1 hour, filtering, and concentrating under reduced pressure at 60°C and 0.005MPa until the volume of the extraction solution is reduced to one third of the original volume, to obtain extract 3;

[0060] S5, dissolving soybean lecithin in an ethanol aqueous solution at 45°C (the added mass of the ethanol aqueous solution is 35 times the mass of the phospholipids, and the concentration of the ethanol aqueous solution is 60wt%), removing ethanol by rotary evaporation in a round-bottom flask, the ambient temperature is 40°C, forming a phospholipid film on the inner wall of the round-bottom flask, and then adding the extract 1, extract 2 and / or extract 3 in a mass ratio of 5:10:3.2, the total mass of extract 1, extract 2 and extract 3 is 5 times the mass of soybean lecithin, and ultrasonically dispersing at 100W for 25min at a temperature of 45°C to disperse the phospholipid film to obtain a liposome solution;

[0061] S6. Mix 90 parts of the liposome solution, 1 part of borneol, 1 part of L-menthol, and 2 parts of polysorbate 80 by mass to obtain the composition.

[0062] An application of the composition as described above, wherein the composition, carbomer 940 and sodium hyaluronate are mixed for preparing eye dressing, wherein the mass ratio of the composition, carbomer 940 and sodium hyaluronate is 100:1:1.

[0063] Example 3

[0064] The present embodiment provides a composition for alleviating pseudomyopia, wherein the raw materials include: borneol, L-menthol, bilberry, spatholobi, ginkgo, peanut, pollen pollen, salvia miltiorrhiza, angelica sinensis and / or polysorbate 80.

[0065] A preparation process of the composition for alleviating ocular pseudomyopia in this embodiment comprises the following steps:

[0066] S1, mixing blueberry, millet chrysanthemum, ginkgo and pollen pollen in a mass ratio of 3:3:4:3, crushing to obtain an alcohol-extracted powder with an average particle size of 200 μm, and putting the alcohol-extracted powder into ethanol in a ratio of 1 g:23 mL of solid-liquid ratio for 30 h at a temperature of 40° C., filtering, and concentrating the filtrate at a temperature of 50° C. and a pressure of 0.01 MPa until the volume of the alcohol-extracted solution is reduced by 3 / 4 to obtain an extract 1;

[0067] S2. Peanuts and angelica are mixed and crushed in a mass ratio of 10:2.5 to obtain an enzymolysis powder with an average particle size of 140 microns. The enzymolysis powder is added to an acetic acid-sodium acetate buffer in a ratio of 1 g:13 mL of a solid-liquid ratio. After the pH value is adjusted to 5.0, cellulase and pectinase (the mass ratio of the two is 1:1) are added to perform the first enzymolysis. The sum of the mass of the cellulase and the pectinase is 1% of the mass of the enzymolysis powder. The temperature of the first enzymolysis is 45° C. and the time is 3 h to obtain a first reaction solution.

[0068] S3, adding disodium hydrogen phosphate to the first reaction solution to adjust the pH value to 6, adding papain and ficin for a second enzymolysis, wherein the mass ratio of papain to ficin is 1:2, and the total amount of papain and ficin added is 0.5% of the mass of the enzymolysis powder, the temperature of the second enzymolysis is 53° C., the time is 4 h, the enzyme is inactivated, filtered, and concentrated under reduced pressure at 60° C. and 0.005 MPa to reduce the volume of the enzymolysis solution by two thirds, to obtain extract 2;

[0069] S4, crushing Danshen to obtain Danshen powder, adding Danshen powder to water at a solid-liquid ratio of 1g:11mL, keeping warm at 95°C for 1.5 hours, filtering, and concentrating under reduced pressure at 60°C and 0.005MPa until the volume of the extraction solution is reduced to one third of the original volume, to obtain extract 3;

[0070] S5, dissolving soybean lecithin in an ethanol aqueous solution at 45°C (the added mass of the ethanol aqueous solution is 35 times the mass of the phospholipids, and the concentration of the ethanol aqueous solution is 60wt%), the ambient temperature is 40°C, and the ethanol is removed by rotary evaporation in a round-bottom flask to form a phospholipid film on the inner wall of the round-bottom flask, and then adding the extract 1, extract 2 and / or extract 3 in a mass ratio of 10:10:3, the total mass of extract 1, extract 2 and extract 3 is 5 times the mass of soybean lecithin, and ultrasonically dispersing at 80W for 25min at a temperature of 35°C to disperse the phospholipid film to obtain a liposome solution;

[0071] S6. Mix 85 parts of the liposome solution, 0.5 parts of borneol, 0.5 parts of L-menthol, and 1 part of polysorbate 80 by mass to obtain the composition.

[0072] An application of the composition as described above, wherein the composition, carbomer 940 and sodium hyaluronate are mixed for preparing eye dressing, wherein the mass ratio of the composition, carbomer 940 and sodium hyaluronate is 100:0.8:0.6.

[0073] Comparative Example 1

[0074] This comparative example is similar to Example 1, except that in this comparative example,

[0075] Dissolve soybean lecithin in an ethanol aqueous solution at 45° C. (the added mass of the ethanol aqueous solution is 35 times the mass of the phospholipids, and the concentration of the ethanol aqueous solution is 60wt%), remove ethanol and water by rotary evaporation in a round-bottom flask, form a phospholipid film on the inner wall of the round-bottom flask, then add the extract 1 and the extract 2 at a mass ratio of 1:10, the total mass of the extract 1 and the extract 2 is 5 times the mass of the soybean lecithin, and ultrasonically disperse at 100W for 25 minutes at a temperature of 35° C. to disperse the phospholipid film to obtain a liposome solution;

[0076] S6. Mix the liposome solution, extract 3 (the total amount of the liposome solution and extract 3 is 80 parts, and the mass ratio of the liposome solution to the extract 3 is (16.3-2.5):2.5, i.e., 5.52:1), 0.1 part of borneol, 0.1 part of L-menthol, and 0.5 part of polysorbate-80 to obtain the composition.

[0077] Comparative Example 2

[0078] This comparative example is similar to Example 1, except that in this comparative example, an equal amount of papain is replaced by ficin.

[0079] Comparative Example 3

[0080] This comparative example is similar to Example 1, except that in this comparative example, an equal amount of ficin is replaced by papain.

[0081] Comparative Example 4

[0082] This comparative example is similar to Example 1, except that in this comparative example, the mass ratio of papain to ficin is 1:0.2.

[0083] Comparative Example 5

[0084] This comparative example is similar to Example 1, except that in this comparative example, the mass ratio of papain to ficin is 1:5.

[0085] Comparative Example 6

[0086] This comparative example is similar to Example 1, except that in this comparative example, an equal amount of Radix Notoginseng is replaced by Radix Notoginseng. Radix Notoginseng has the effects of stopping bleeding, dispersing blood stasis, and reducing swelling, and its medicinal effect is similar to that of Radix Notoginseng.

[0087] The eye structure and physiological function of guinea pigs are similar to those of humans, especially in terms of axial development and refractive state. By inducing a myopia model in guinea pigs, the development process of human myopia can be simulated, and the effect of eye patches can be tested. Usually, the form deprivation method is used, such as wearing a translucent eye mask on one or both eyes of the guinea pig to limit its visual input and make the eye develop in the direction of myopia.

[0088] 45 ordinary tricolor guinea pigs, 2 weeks old and weighing 120 g, were purchased from Beijing Keyu Animal Breeding Center. The breeding environment was maintained at a humidity of 50%, a room temperature of 20-26°C, fluorescent lighting, and a light cycle of 12h / 12h alternating light and dark. The animals had free access to water and food.

[0089] The guinea pigs were randomly divided into 9 groups, 5 in each group, and the results were calculated and the average value was taken.

[0090] Group 1 served as the normal control group, in which the guinea pigs were kept normally for 14 days without any intervention on their eyes;

[0091] Group 2 was the model group, in which the right eye was used as the form-deprived eye. The right eye of the guinea pig was covered with a semi-transparent eye for 14 consecutive days, and the left eye was not treated.

[0092] Group 3 used the right eye as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days), and applied the eye dressing in Example 1 for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied within 15 minutes each time), and the left eye was not treated;

[0093] Group 4 used the right eye as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days) and applied the eye dressing of Example 2 for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied continuously within 15 minutes each time), and the left eye was not treated;

[0094] Group 5 used the right eye as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days) and applied the eye dressing of Example 3 for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied within 15 minutes each time), and the left eye was not treated;

[0095] Group 6 used the right eye as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days), and applied the eye dressing in Comparative Example 1 for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied within 15 minutes each time), and the left eye was not treated;

[0096] Group 7 used the right eye as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days), and applied the eye dressing in Comparative Example 2 for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied within 15 minutes each time), and the left eye was not treated;

[0097] In group 8, the right eye was used as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days), and the eye dressing in Comparative Example 3 was applied for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied continuously within 15 minutes each time), and the left eye was not treated.

[0098] In group 9, the right eye was used as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days), and the eye dressing in Comparative Example 4 was applied for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied continuously within 15 minutes each time), and the left eye was not treated.

[0099] In group 10, the right eye was used as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days), and the eye dressing in Comparative Example 5 was applied for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied continuously within 15 minutes each time), and the left eye was not treated.

[0100] In group 11, the right eye was used as the form-deprived eye (the guinea pig's right eye was covered with a translucent eye for 14 consecutive days), and the eye dressing in Comparative Example 6 was applied for 15 minutes every day (the application amount was 25 g / eye, the application was selected when the guinea pig was sleeping, and a total of 25 g was applied continuously within 15 minutes each time), and the left eye was not treated.

[0101] The refraction of the guinea pigs was measured every 0, 7, and 14 days. Tropicamide eye drops were instilled into the eyes of the guinea pigs once every 5 minutes, 1 drop each time, for a total of 4 times. After 20 minutes, the refraction of each guinea pig was measured using a strip retinoscope. The measurement results are shown in Table 1.

[0102] Table 1 Refractive power statistics

[0103]

[0104]

[0105] By comparing the data of Example 1 and Comparative Example 1, it can be seen that the extract 3 has no obvious promoting effect on flavonoids if it is not encapsulated in liposomes. If it is not encapsulated in liposomes, the extract 3 will be randomly distributed in the body or reaction system, resulting in a low effective concentration in the target area. Liposomes can concentrate the extract 3 in the target area through specific recognition with target cells or passive physical processes, such as permeation through capillary walls. In this way, a higher concentration is formed locally, which is more conducive to interaction with flavonoids and enhances the promoting effect on flavonoids.

[0106] Comparing the relevant data of Examples 1-3 and Comparative Examples 2-5, it can be seen that papain and ficin achieve a good synergistic effect, and only when the ratio of the two is within the scope of the present invention can the best effect be achieved.

[0107] Comparing the relevant data of Example 1 and Comparative Example 6, it can be seen that the effect of using Panax notoginseng instead of Radix Puhuang to treat myopia is not good.

[0108] The above are only specific embodiments of the present invention, but the protection scope of the present invention is not limited thereto. The protection scope of the present invention shall be based on the protection scope of the claims.

Claims

1. A preparation process of a composition for alleviating pseudomyopia of the eye, characterized in that: The following steps are involved: S1, mixing and crushing the flavonoid-rich plants and Pollen Typhae to obtain an alcohol-extracted powder, and putting the alcohol-extracted powder into ethanol at a ratio of 1 g to 20-25 mL for alcohol extraction, filtering and concentrating until the volume of the alcohol-extracted solution is reduced by 2 / 3-4 / 5, to obtain an extract 1; S2, crushing the amino acid-rich plants and angelica to obtain enzymolysis powder, adding the enzymolysis powder to acetic acid-sodium acetate buffer at a ratio of 1 g: 12-15 mL, adjusting the pH value to 4.5-6.0, and then adding cellulase and pectinase to perform the first enzymolysis, wherein the temperature of the first enzymolysis is 40-50° C., and the time is 2-4 h, to obtain a first reaction solution; S3, adding disodium hydrogen phosphate to the first reaction solution to adjust the pH value to 6, adding papain and ficin for a second enzymolysis, wherein the mass ratio of papain to ficin is 1:1-2, the temperature of the second enzymolysis is 50-55°C, the time is 3-5h, and the volume of the enzymolysis solution is reduced by 2 / 3 through enzyme inactivation, filtration and concentration, to obtain extract 2; S4, crushing Danshen to obtain Danshen powder, adding Danshen powder to water at a solid-liquid ratio of 1g:10-12mL, keeping warm at 90-100°C for 1-2 hours, filtering to obtain an extraction solution, and concentrating to reduce the volume of the extraction solution by 2 / 3 to obtain extract 3; S5, dissolving the phospholipid in an ethanol aqueous solution, removing the ethanol and water by rotary evaporation in a round-bottom flask, forming a phospholipid film on the inner wall of the round-bottom flask, and then adding the extract 1, extract 2, and extract 3 in a mass ratio of 1-10:10:2.5-3.2, and performing ultrasonic dispersion at 35-45° C. to disperse the phospholipid film to obtain a liposome solution; S6. Mixing the liposome solution, borneol, L-menthol and / or polysorbate 80 to obtain the composition.

2. The preparation process according to claim 1, characterized in that: The mass ratio of the flavonoid-rich plant to the pollen of Typha aquatica in S1 is 10:2-4, and the average particle size of the alcohol-extracted powder is 180-250 microns.

3. The preparation process according to claim 1, characterized in that: The alcohol extraction time in S1 is 24-48h, and the temperature is 35-45°C.

4. The preparation process according to claim 1, characterized in that: The mass ratio of the amino acid-rich plant to Angelica sinensis in S2 is 10:2-3, and the average particle size of the enzymatic hydrolysis powder is 100-150 microns.

5. The preparation process according to claim 1, characterized in that: In S6, the liposome solution is 80-90 parts, borneol is 0.1-1 parts, L-menthol is 0.1-1 parts, and polysorbate 80 is 0.5-2 parts by mass.

6. The preparation process according to claim 1, characterized in that: The flavonoid-rich plants are one or more of Chuanxiong, ginseng, cassia seed, mulberry, blueberry, angelica, and ginkgo.

7. The process according to claim 1, characterized in that The amino acid-rich plants are one or more of soybeans and nuts.

8. A composition for alleviating ocular pseudomyopia prepared by the preparation process according to any one of claims 1 to 7.

9. Use of the composition according to claim 8, wherein the composition, carbomer and sodium hyaluronate are mixed for preparing eye dressing, wherein the mass ratio of the composition, carbomer and sodium hyaluronate is 100:0.1-1:0.01-1.

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