Oral liquid for improving eyesight and preparation method thereof

Abstract

The invention relates to oral liquid for improving eyesight and a preparation method thereof, and belongs to the field of health care products and medicines. The oral liquid for improving eyesight is prepared from the following raw materials in parts by weight: 1 to 30 parts of lutein, 1 to 30 parts of lutein ester, 1 to 5 parts of zeaxanthin, 1 to 5 parts of astaxanthin, 3 to 10 parts of beta-carotene, 10 to 20 parts of bilberry extract, 10 to 30 parts of vitamin E, 1 to 10 parts of butyl hydroxy anisd, 200 to 1500 parts of Tween 80 and 30000 to 100000 parts of water. The Tween 80 increases the water solubility of the nutritional ingredients, the butylated hydroxyanisole improves the stability of the nutritional ingredients, the absorptivity and bioavailability of the nutritional ingredients are also improved, and the eyesight protection effect is far better than that of the prior art. Compared with other antioxidants, the butylated hydroxyanisole has a better antioxidation effect on the nutritional ingredients, so that the nutritional ingredients have an extremely good stabilizing effect.

Description

[0001] This application is a divisional application. The original application has the application number 201710557598.8, the application date is July 10, 2017, and the invention title is Functional Nutritional Fortifier Composition and Preparation Method. Technical Field

[0002] This invention belongs to the fields of health products and medicines, and particularly relates to an oral liquid for improving eyesight and its preparation method. Background Technology

[0003] As electronic products have become an integral part of people's lives, while bringing increasing convenience, they have also caused harm, particularly to the eyes. People rely heavily on televisions, computers, and especially mobile phones in their daily lives. Prolonged close-range viewing of electronic devices can cause excessive contraction of the ciliary muscles, leading to symptoms such as dry and painful eyes, eye strain, and even various eye diseases. Besides using electronic products reasonably and scientifically to protect eye health, we can also alleviate eye fatigue and improve vision through diet and the intake of eye-healthy nutrients.

[0004] However, most patented inventions related to eye protection contain nutrients with limited efficacy, resulting in only minor effects on vision protection. Lutein, lutein esters, zeaxanthin, beta-carotene, and astaxanthin belong to the carotenoid family. These five substances, along with vitamin E and bilberry extract, can act as antioxidants, offering excellent protection for eyesight. Except for bilberry extract, which is slightly soluble in water, the aforementioned five carotenoids and vitamin E are fat-soluble and poorly water-soluble. Furthermore, lutein, lutein esters, zeaxanthin, astaxanthin, beta-carotene, bilberry extract, and vitamin E exhibit poor stability, leading to low bioavailability during storage and human consumption. Currently, a common method to improve the stability of lutein, lutein esters, zeaxanthin, beta-carotene, astaxanthin, vitamin E, and bilberry extract is to encapsulate these poorly soluble components into solid powders. However, solid powders are not conducive to human absorption. Preparing them as oral solutions could improve absorption, addressing both the low water solubility of these nutrients and their poor stability—a problem that remains unsolved and extremely difficult to overcome. To improve the stability of nutrients in aqueous solutions, our researchers conducted numerous experiments. Initially, they attempted to enhance nutrient stability by adding one or more water-soluble antioxidants, pH adjusters, or metal complexing agents. However, these methods proved ineffective in stabilizing the aforementioned nutrients and are therefore not feasible. Therefore, developing a solution with both high water solubility and strong stability for these nutrients is a pressing research direction.

[0005] The development of convenient, portable, and readily available oral dosage forms has always been a key focus in the pharmaceutical and health product industries. A challenge in this field is converting insoluble lutein, lutein esters, zeaxanthin, β-carotene, astaxanthin, vitamin E, and bilberry extract into highly soluble and stable oral liquid formulations. Adding other functional ingredients (such as collagen, vitamin C, and enzymes) to these oral liquid formulations to create multifunctional beverages is another area of ​​research in this field. Summary of the Invention

[0006] The technical problem to be solved by the present invention is to provide a functional nutrient fortifier composition containing fat-soluble nutrients with good solubility and stability, and a method for preparing the same.

[0007] To achieve the above objectives, the present invention adopts the following technical solution: A functional nutrient fortifier composition, made from the following raw materials in parts by weight: Nutritional components 1-130 parts, functional components 0-245 parts, fat-soluble antioxidants 1-10 parts, emulsifiers 200-1500 parts, water 30000-100000 parts.

[0008] The preferred functional nutrient fortifier composition is made from the following raw materials in parts by weight: Nutritional components: 4-85 parts; functional components: 0-150 parts; fat-soluble antioxidants: 2-5 parts; emulsifiers: 500-1000 parts; water: 50,000-80,000 parts.

[0009] A more preferred functional nutrient fortifier composition is made from the following raw materials in parts by weight: Nutritional components: 6-57 parts; functional components: 0-100 parts; fat-soluble antioxidants: 2.4 parts; emulsifiers: 600 parts; water: 60,000 parts.

[0010] The nutritional components include one or both of lutein and lutein esters, with each component weighing 1 to 30 parts, preferably 4 to 20 parts, and more preferably 6 parts.

[0011] Furthermore, the nutritional components include one or more of the following: 1-5 parts zeaxanthin, 1-5 parts astaxanthin, 3-10 parts β-carotene, 10-20 parts blueberry extract, and 10-30 parts vitamin E.

[0012] Preferably, the nutritional components also include one or more of the following: 3 parts zeaxanthin, 2 parts astaxanthin, 5 parts beta-carotene, 15 parts blueberry extract, and 20 parts vitamin E.

[0013] In this invention, lutein possesses strong antioxidant properties, absorbing harmful light such as blue light, inhibiting the activity of reactive oxygen species (ROS), and preventing ROS from damaging normal cells. Lutein is a major component of the macular pigment in the human retina. Blue light has the highest energy among all visible light reaching the retina and has the strongest damaging effect on the macula; lutein can filter out blue light. High-energy blue light can also induce the generation of free radicals, damaging optic nerve cells; lutein can quench singlet oxygen and capture ROS, thus playing an antioxidant role. Because lutein can prevent damage to the eyes caused by blue light, it can protect retinal tissue, improve vision, make vision more accurate, protect the retina, reduce the occurrence of cataracts, and prevent retinitis pigmentosa. Lutein esters are degraded into lutein in the human body, where they exert their effects.

[0014] Zeaxanthin can increase macular pigment, thereby enhancing the macula's ability to resist harmful substances and light damage, protecting the cone cells in the center of the retina, and preventing and slowing down age-related macular degeneration. Lutein and zeaxanthin are the only two types of carotenoids in the eye, and they are highly concentrated in the macula, the area responsible for fine vision. They improve and protect vision, relieve eye strain, and are extremely important for eye health.

[0015] Astaxanthin, a highly effective natural antioxidant, primarily functions to scavenge free radicals and enhance the body's anti-aging capabilities. Natural astaxanthin can penetrate the three major human blood-brain barrier, blood-pancreas barrier, and blood-testis barrier, and is the only carotenoid capable of crossing the blood-brain barrier. Therefore, it is the only carotenoid that can potentially act on brain cells and the retina of the eye. Astaxanthin easily crosses the blood-brain barrier and cell membranes, effectively preventing retinal oxidation and damage to photoreceptor cells, especially showing a more significant effect than lutein in preventing macular degeneration.

[0016] Beta-carotene is an antioxidant with detoxifying properties and is an essential nutrient for maintaining human health. It plays a significant role in preventing cataracts and, consequently, preventing aging and various degenerative diseases caused by aging, such as degenerative eye diseases. Vision depends on the macula in the retina; without sufficient beta-carotene for protection and support, this area will develop degenerative changes, leading to vision decline. This disease is more common in the elderly and can be prevented by consuming enough beta-carotene. In addition, beta-carotene is a precursor to vitamin A and can prevent night blindness caused by vitamin A deficiency. Beta-carotene acts like natural eye drops, helping to maintain the lubrication and transparency of the cornea and promoting eye health.

[0017] Bilberries are rich in anthocyanins, which help maintain capillary integrity and stabilize collagen. Anthocyanins are also powerful antioxidants, protecting the body from free radical damage. They promote the regeneration of rhodopsin in retinal cells, stimulating rhodopsin and preventing retinopathy and severe myopia caused by heme iron and diabetes, thus improving vision. Therefore, bilberry extract can effectively improve retinal accommodation, reduce damage to vision caused by light pollution and light stimulation, and is used to prevent blindness, glaucoma, cataracts, retinal hemorrhage, improve myopia, macular degeneration, diabetic retinopathy, retinitis pigmentosa, and night blindness. Healthy individuals or those with visual impairments can significantly improve night vision by using bilberry extract alone or simultaneously with beta-carotene and vitamin E, experiencing faster reactions to darkness and quicker recovery of visual acuity after exposure to bright light.

[0018] Vitamin E is a powerful antioxidant that regulates lipid oxidation, scavenges free radicals, and protects cells from oxidative damage. Vitamin E can inhibit lipid peroxidation in the lens of the eye, dilate peripheral blood vessels, improve blood circulation, and prevent the occurrence and progression of myopia.

[0019] Furthermore, the functional components of the present invention are selected from one or more of collagen, vitamin C, enzymes, taurine, vitamin B1, vitamin B2, vitamin B6, vitamin B12, caffeine, metal gluconate, metal citrate, water-soluble amino acids, water-soluble oligosaccharides, resistant dextrin, and hydrophilic colloids. Collagen (0-40 parts by weight), Vitamin C (0-30 parts by weight), Enzymes (0-30 parts by weight), Taurine (0-30 parts by weight), Vitamin B1 (0-20 parts by weight), Vitamin B2 (0-20 parts by weight), Vitamin B6 (0-20 parts by weight), Vitamin B12 (0-20 parts by weight), Caffeine (0-35 parts by weight), Metal gluconate (0-50 parts by weight), Metal citrate (0-50 parts by weight), Water-soluble amino acids (0-200 parts by weight), Water-soluble oligosaccharides (0-1000 parts by weight), Resistant dextrin (0-3000 parts by weight), Hydrophilic colloids (0-1000 parts by weight). This invention incorporates collagen, vitamin C, enzymes, taurine, vitamin B1, vitamin B2, vitamin B6, vitamin B12, caffeine, metal gluconate, metal citrate, water-soluble amino acids, water-soluble oligosaccharides, resistant dextrin, and hydrophilic colloids to prepare a functional oral liquid formulation that can more comprehensively regulate the body and prevent and treat diseases.

[0020] Collagen is a biological macromolecule, a white, opaque, unbranched fibrous protein, and an essential nutrient for delaying aging. It is widely found in human skin, bones, muscles, cartilage, joints, and hair tissue, playing a triple anti-aging role of support, repair, and protection. It can replenish the nutrients needed by each layer of the skin, enhance collagen activity, and has moisturizing, anti-aging, beautifying, wrinkle-reducing, and hair-nourishing effects. Vitamin C is an essential nutrient for the human body. In the body, vitamin C is an antioxidant, protecting the body from free radical threats. It is also a coenzyme. The main functions of vitamin C include: promoting collagen synthesis (vitamin C deficiency leads to impaired collagen synthesis and scurvy); promoting neurotransmitter synthesis; promoting steroid hydroxylation; promoting antibody synthesis; promoting iron absorption; promoting tetrahydrofolate formation; maintaining the activity of sulfhydryl enzymes; detoxification; cancer prevention; and free radical scavenging. Enzymes are macromolecules with biocatalytic functions. Enzymes have the effects of regulating immune response, anti-cancer, lowering blood pressure, regulating the intestines, relieving constipation, resisting gout, fighting type 2 diabetes, weight loss, and anti-allergy. As a unique health product with vitality, enzymes have great potential for health preservation. Taurine is a sulfur-containing non-protein amino acid that does not participate in the biosynthesis of proteins in the body, but is closely related to the metabolism of cystine and cysteine. Taurine can promote the development of brain tissue and intelligence in infants and young children; improve nerve conduction and visual function; prevent cardiovascular disease; affect lipid absorption and inhibit the formation of cholesterol stones; improve endocrine status and enhance human immunity; taurine can bind to insulin receptors, accelerate glycolysis, and lower blood sugar concentration; inhibit the occurrence and development of cataracts; supplementing with appropriate amounts of taurine can improve memory and has an anti-aging effect on the nervous system; maintain normal reproductive function. Vitamin B1 can treat beriberi and peripheral neuritis; aid digestion and promote growth; improve mental state; maintain the normal function of nerve tissue, muscles, and heart; relieve pain after dental surgery; and help treat shingles. Vitamin B2 participates in cell growth and metabolism, promoting development and cell regeneration; it participates in biological oxidation and energy metabolism in the body, and is an essential nutrient for tissue metabolism and repair; it participates in the absorption, storage, and mobilization of iron in the body; it eliminates inflammation in the mouth, lips, and tongue; it improves vision and reduces eye fatigue; and it also has antioxidant activity. Vitamin B6 participates in protein synthesis and breakdown, carbohydrate metabolism, and nucleic acid and DNA synthesis; it participates in the synthesis of certain neurotransmitters (serotonin, taurine, dopamine, norepinephrine, and γ-aminobutyric acid); and it contributes to the conversion of homocysteine ​​to methionine, thus playing a role in reducing chronic diseases.Vitamin B12 promotes the development and maturation of red blood cells, ensuring normal hematopoietic function and preventing pernicious anemia. Existing as a coenzyme, it increases folic acid utilization and promotes the metabolism of carbohydrates, fats, and proteins. It activates amino acids and promotes nucleic acid biosynthesis, thus contributing to protein synthesis and playing a vital role in the growth and development of infants and young children. It is an essential vitamin for the healthy functioning of the nervous system, participating in the formation of a lipoprotein in nerve tissue. Caffeine, an alkaloid, can, when used moderately, refresh the mind, combat depression, promote digestion, control weight, act as a diuretic, relieve pain, and prevent gallstones. Clinically, it is used to treat neurasthenia and for coma resuscitation. Metal gluconate and metal citrate provide the body with essential trace elements to maintain health. Water-soluble amino acids are the basic building blocks of proteins required for human nutrition. Water-soluble oligosaccharides improve the body's microecological environment, enhance immune function, improve lipid metabolism, and lower cholesterol and triglyceride levels. They do not raise blood sugar, making them suitable for people with high blood sugar and diabetes. They do not form a matrix with cariogenic bacteria, thus preventing tooth decay. Resistant dextrin is a low-molecular-weight, water-soluble dietary fiber that can increase the fiber content of food and provide sustained energy to the body. Its hydrophilic colloids can inhibit the absorption of neutral fats.

[0021] The cyclodextrin is selected from one of hydroxypropyl-β-cyclodextrin, β-cyclodextrin, sulfonyl ether-β-cyclodextrin, α-cyclodextrin, γ-cyclodextrin, and methyl-β-cyclodextrin. Hydroxypropyl-β-cyclodextrin and β-cyclodextrin are preferred, and hydroxypropyl-β-cyclodextrin is even more preferred.

[0022] The composition also contains an organic solvent.

[0023] The organic solvent is selected from one or more of acetone, ethanol, propylene glycol, and glycerol.

[0024] The fat-soluble antioxidant is selected from one or more of butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), and rosemary extract.

[0025] The emulsifier is one or more of Tween 80, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, and polyethylene glycol 15-hydroxystearate.

[0026] Furthermore, this functional nutrient fortifier composition also contains one or more of the following: acidity regulator, thickener, flavoring agent, and preservative; the acidity regulator adjusts the pH of the solution to 2.5–8.0; the thickener is 150–3000 parts by weight; the flavoring agent is 50–2000 parts by weight; and the preservative is 10–400 parts by weight.

[0027] Furthermore, the acidity regulator is selected from one or more of hydrochloric acid, acetic acid, acetate-acetate buffer, sulfuric acid, maleic acid, citric acid, lactic acid, malic acid, borate-sodium carbonate buffer, phosphoric acid, sodium dihydrogen phosphate, succinic acid, and borate buffer.

[0028] Furthermore, the thickener is selected from one or more of the following: povidone, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, gelatin, agar, polyvinyl alcohol, glyceryl monostearate, dextran, gum arabic, carrageenan, guar gum, carrageenan, pectin, propylene glycol alginate, sodium alginate, astragalus gum, xanthan gum, sodium hydroxymethyl cellulose, hydroxyethyl cellulose, carbomer, and polyethylene glycol.

[0029] Furthermore, the flavoring agent is selected from one or more of the following: steviol glycosides, protein sugar, aspartame, sucralose, sodium saccharin, alitane, cyclamate, licorice, acesulfame potassium, asarazolidin, neotame, tagatose, disodium glycyrrhizate, glucose, fructose, sucrose, maltose, xylitol, monosaccharide syrup, fruit juice syrup, honey, glycerin, sorbitol, mannitol, vanillin, peppermint water, compound cardamom tincture, benzaldehyde, cinnamaldehyde, malonic acid ester, ethyl acetoacetate, ethyl acetate, sodium cyclohexane, citronellal, water-soluble natural flavorings, water-soluble synthetic flavorings, water-soluble natural equivalent flavorings, water-soluble fermented flavorings, natural fruit juice, natural vegetable juice, vegetable concentrate, fruit concentrate, and adenosine monophosphate.

[0030] Furthermore, the preservative is selected from one or more of benzoic acid, potassium phenylpropionate, sodium benzoate, sorbic acid, sodium sorbate, potassium sorbate, calcium sorbate, methylparaben, ethylparaben, propylparaben, butylparaben, sodium methylparaben, sodium propylparaben, thimerosal, chlorobutanol, benzalkonium chloride, benzalkonium bromide, benzyl alcohol, phenethyl alcohol, and hexidine.

[0031] A functional nutrient fortifier composition is made from the following raw materials in parts by weight: 6 parts lutein or lutein ester, 2.4 parts butylated hydroxytoluene, 600 parts Tween 80, and 60,000 parts water.

[0032] A functional nutritional fortifier composition is made from the following raw materials in parts by weight: 4 parts lutein, 4 parts lutein ester, 3 parts zeaxanthin, 2 parts astaxanthin, 5 parts β-carotene, 15 parts blueberry extract, 20 parts vitamin E, 5 parts butylated hydroxyanisole, 600 parts Tween 80, and 60,000 parts water.

[0033] Any of the functional nutrient fortifier compositions described in this invention is an oral liquid formulation.

[0034] In this invention, lutein, lutein ester, zeaxanthin, β-carotene, astaxanthin, vitamin E, and bilberry extract are all fat-soluble nutrients. The emulsifiers used not only increase the water solubility of the nutrients but also do not affect their efficacy; however, the stability of these nutrients remains a technical challenge. To improve the stability of the nutrients in aqueous solutions, our researchers conducted numerous experiments. Initially, one or more water-soluble antioxidants, pH adjusters, and metal complexing agents were added to improve the stability of the nutrients. However, these methods did not stabilize the aforementioned nutrients and were therefore not feasible. Typically, because fat-soluble antioxidants are poorly soluble in water, there is no precedent for using them in aqueous solutions. We creatively discovered that by adding specific fat-soluble antioxidants while emulsifying the nutrients with an emulsifier, the emulsifier solubilizes the specific fat-soluble antioxidants. When this is then applied to prepare the aforementioned nutrient solution, we surprisingly found that the stability of these nutrients was greatly improved. The specific fat-soluble antioxidants are one or more selected from butylated hydroxytoluene, butylated hydroxyanisole, and rosemary extract. The emulsifiers used to solubilize the fat-soluble antioxidants are one or more selected from Tween 80, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, and polyethylene glycol 15-hydroxystearate. The scientifically formulated emulsifiers and specific fat-soluble antioxidants exhibit good compatibility, and the solubilized fat-soluble antioxidants provide better stabilization for the nutrients. This invention synergistically uses nutrients, emulsifiers, and fat-soluble antioxidants to provide a functional nutritional fortifier composition with high water solubility, good stability, rapid absorption, high bioavailability, and effective treatment for various eye diseases.

[0035] A method for preparing a functional nutrient fortifier composition, comprising any of the following methods: Method 1: 1) First, thoroughly mix the nutrients, fat-soluble antioxidants, and emulsifiers to prepare a nutrient mixture; 2) Heat the nutrient mixture and water to 40-80°C, then slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution; 3) Functional ingredients and / or other excipients can also be added to the nutrient solution to obtain a functional nutrient fortifier composition.

[0036] Method 2: 1) First, dissolve the nutrients in an organic solvent, then add fat-soluble antioxidants and emulsifiers and mix thoroughly to prepare a nutrient mixture; 2) Heat the nutrient mixture and water to 40-80°C, then slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution; 3) Functional ingredients and / or other excipients can also be added to the nutrient solution to obtain a functional nutrient fortifier composition.

[0037] This invention utilizes seven nutrients—lutein, lutein ester, zeaxanthin, β-carotene, astaxanthin, vitamin E, and bilberry extract—which effectively protect eyesight. Lutein, lutein ester, zeaxanthin, β-carotene, and astaxanthin belong to the carotenoid family. These five substances, along with vitamin E and bilberry extract, can all act as antioxidants to protect eyesight. Except for bilberry extract, which is slightly soluble in water, the aforementioned five carotenoids and vitamin E are fat-soluble and poorly water-soluble. Furthermore, lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, bilberry extract, and vitamin E have poor stability, resulting in low bioavailability during storage and human consumption. The emulsifier used in this invention not only increases the water solubility of the nutrients but also does not affect their efficacy; however, the stability of these nutrients remains a technical challenge. To improve the stability of nutrients, almost all water-soluble antioxidants were used in the research process of this invention. However, none of the water-soluble antioxidants used contributed to the stability of the nutrients, and fat-soluble antioxidants were difficult to apply due to their insolubility in water. We creatively discovered that by adding specific fat-soluble antioxidants while emulsifying nutrients with emulsifiers, the emulsifiers solubilize the specific fat-soluble antioxidants. The solubilized fat-soluble antioxidants are then applied to prepare nutrient solutions, resulting in a significant improvement in the stability of these nutrients. The specific fat-soluble antioxidants are one or more of butylated hydroxytoluene, butylated hydroxyanisole, and rosemary extract. The emulsifiers used to solubilize the fat-soluble antioxidants are one or more of Tween 80, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, and polyethylene glycol 15-hydroxystearate. This scientific combination of emulsifiers and specific fat-soluble antioxidants ensures good compatibility, and the solubilized fat-soluble antioxidants have a better stabilizing effect on the nutrients. The rational combination of nutrients, fat-soluble antioxidants, and emulsifiers increases the stability and solubility of nutrients, thereby improving the rate of biological absorption and bioavailability of nutrients, resulting in a more significant effect on protecting eyesight.

[0038] The advantages of this invention are as follows: The nutrients in this invention are lutein and lutein esters, and also contain zeaxanthin, β-carotene, astaxanthin, vitamin E, and bilberry extract. Using appropriate amounts of these nutrients can effectively treat various eye diseases. This invention creatively combines emulsifiers and fat-soluble antioxidants, surprisingly finding that not only do emulsifiers increase the water solubility of the nutrients, but fat-soluble antioxidants are also solubilized by the emulsifiers. Furthermore, the solubilized fat-soluble antioxidants improve the stability of the nutrients. Extensive experimental verification by this invention shows that butylated hydroxytoluene, butylated hydroxyanisole, and rosemary extract, after being solubilized by emulsifiers, have an extremely good stabilizing effect on the nutrients in this invention. The increased water solubility and stability of the nutrients also improve their absorption rate and bioavailability, resulting in a far superior effect on protecting eyesight compared to existing technologies.

[0039] The present invention will be further described below with reference to specific embodiments, but this is not intended to limit the invention. All equivalent substitutions made in accordance with the disclosure of the present invention are within the scope of protection of the present invention. Detailed Implementation

[0040] Example 1

[0041] I. Raw Materials

[0042] Lutein 6g, butylated hydroxytoluene 2.4g, Tween 80 600g, water 60000g.

[0043] II. Manufacturing Method

[0044] 1. First, thoroughly mix lutein, butylated hydroxytoluene, and Tween 80 to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 60°C. At 60°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0045] Example 2

[0046] I. Raw Materials

[0047] Lutein ester 6g, acetone 10g, butylated hydroxytoluene 2.4g, Tween 80 600g, steviol glycosides 10g, water 60000g.

[0048] II. Manufacturing Method

[0049] 1. First, dissolve lutein ester in acetone, then add butylated hydroxytoluene and Tween 80 and mix thoroughly to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 40°C. At 40°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. Add steviol glycosides to the nutrient solution, filter through a 0.25μm sterile filter membrane to remove bacteria, and finally obtain the functional nutrient fortifier composition.

[0050] Example 3

[0051] I. Raw Materials

[0052] Lutein 6g, lutein ester 6g, butylated hydroxytoluene 2.4g, Tween 80 600g, water 60000g.

[0053] II. Manufacturing Method

[0054] 1. First, thoroughly mix lutein, lutein ester, butylated hydroxytoluene, and Tween 80 to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 50°C. At 50°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0055] Example 4

[0056] I. Raw Materials

[0057] Lutein 4g, lutein ester 4g, zeaxanthin 3g, astaxanthin 2g, beta-carotene 5g, blueberry extract 15g, vitamin E 20g, butylated hydroxyanisole 5g, Tween 80 600g, water 60000g.

[0058] II. Manufacturing Method

[0059] 1. Thoroughly mix lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, blueberry extract, vitamin E, butylated hydroxyanisole, and Tween 80 to prepare a nutrient mixture. 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0060] Example 5

[0061] I. Raw Materials

[0062] Lutein 4g, lutein ester 20g, butylated hydroxytoluene 2g, butylated hydroxyanisole 5g, polyoxyethylene castor oil 1000g, water 80000g.

[0063] II. Manufacturing Method

[0064] 1. First, thoroughly mix lutein, lutein ester, butylated hydroxytoluene, butylated hydroxyanisole, and polyoxyethylene castor oil to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0065] Example 6

[0066] I. Raw Materials

[0067] Lutein 30g, lutein ester 4g, zeaxanthin 3g, ethanol-acetone (1:1) 15g, rosemary extract 1g, Tween 80 1500g, water 100000g.

[0068] II. Manufacturing Method

[0069] 1. Dissolve lutein, lutein ester, and zeaxanthin in an ethanol-acetone (1:1) solution, then add rosemary extract and Tween 80 and mix thoroughly to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 70°C. At 70°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0070] Example 7

[0071] I. Raw Materials

[0072] Lutein 20g, lutein ester 1g, astaxanthin 2g, blueberry extract 15g, butylated hydroxytoluene 10g, Tween 80 500g, water 50000g.

[0073] II. Manufacturing Method

[0074] 1. Thoroughly mix lutein, lutein ester, astaxanthin, blueberry extract, butylated hydroxytoluene, and Tween 80 to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 40°C. At 40°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. Place the nutrient solution in an autoclave and sterilize it under vacuum at 160°C for 15 minutes to obtain the functional nutrient fortifier composition.

[0075] Example 8

[0076] I. Raw Materials

[0077] 1g lutein, 30g lutein ester, 30g acetone, 2g butylated hydroxyanisole, 200g polyoxyethylene hydrogenated castor oil, 30000g water.

[0078] II. Manufacturing Method

[0079] 1. First, dissolve lutein and lutein ester in acetone, then add butylated hydroxyanisole and polyoxyethylene hydrogenated castor oil and mix thoroughly to prepare a nutrient mixture. 2. Heat both the nutrient mixture and water to 80°C. At 80°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0080] Example 9

[0081] I. Raw Materials

[0082] Lutein 6g, lutein ester 4g, zeaxanthin 5g, astaxanthin 5g, beta-carotene 3g, blueberry extract 10g, vitamin E 10g, rosemary extract 10g, Tween 80 1000g, water 100000g.

[0083] II. Manufacturing Method

[0084] 1. Thoroughly mix lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, blueberry extract, vitamin E, rosemary extract and Tween 80 to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 60°C. At 60°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0085] Example 10

[0086] I. Raw Materials

[0087] Lutein 1g, Lutein Ester 1g, Zeaxanthin 1g, Astaxanthin 1g, β-Carotene 10g, Bilberry Extract 20g, Vitamin E 20g, Collagen 8g, Butylated Hydroxyanisole 5g, Polyethylene Glycol 15-Hydroxystearate 500g, Water 50000g.

[0088] II. Manufacturing Method

[0089] 1. Thoroughly mix lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, blueberry extract, vitamin E, butylated hydroxyanisole, and polyethylene glycol 15-hydroxystearate to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. Add collagen to the nutrient solution, filter it through a 0.25μm sterile filter membrane to remove bacteria, and finally obtain the functional nutrient fortifier composition.

[0090] Example 11

[0091] I. Raw Materials

[0092] Lutein 4g, lutein ester 20g, butylated hydroxytoluene 7g, Tween 80 900g, povidone 30g, water-soluble natural fragrance 50g, water 80000g.

[0093] II. Manufacturing Method

[0094] 1. First, thoroughly mix lutein, lutein ester, butylated hydroxytoluene, butylated hydroxyanisole, and polyoxyethylene castor oil to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. Add povidone and water-soluble natural fragrance to the solution, and filter the nutrient solution through a 0.25μm sterile filter membrane to remove bacteria, finally obtaining the functional nutrient fortifier composition.

[0095] Compare with Example 1

[0096] I. Raw Materials

[0097] Lutein 4g, lutein ester 4g, zeaxanthin 3g, astaxanthin 2g, beta-carotene 5g, blueberry extract 15g, vitamin E 20g, sodium sulfite 120g, Tween 80 600g, water 60000g.

[0098] II. Manufacturing Method

[0099] 1. Thoroughly mix lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, bilberry extract, vitamin E and Tween 80 to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. Add sodium sulfite to the nutrient solution, filter it through a 0.25μm sterile filter membrane to remove bacteria, and finally obtain the functional nutrient fortifier composition.

[0100] Compare with Example 2

[0101] I. Raw Materials

[0102] Lutein 4g, lutein ester 4g, zeaxanthin 3g, astaxanthin 2g, beta-carotene 5g, blueberry extract 15g, vitamin E 20g, Tween 80 600g, water 60000g.

[0103] II. Manufacturing Method

[0104] 1. Thoroughly mix lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, bilberry extract, vitamin E and Tween 80 to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water until it is completely dissolved to prepare a nutrient solution. 3. The nutrient solution is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0105] Compare with Example 3

[0106] I. Raw Materials

[0107] Lutein 4g, lutein ester 4g, zeaxanthin 3g, astaxanthin 2g, beta-carotene 5g, blueberry extract 15g, vitamin E 20g, butylated hydroxyanisole 5g, water 60000g.

[0108] II. Manufacturing Method

[0109] 1. Thoroughly mix lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, blueberry extract, vitamin E, and butylated hydroxyanisole to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water and mix to prepare a nutrient solution. 3. The nutrient mixture is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0110] Compare with Example 4

[0111] I. Raw Materials

[0112] Lutein 4g, lutein ester 4g, zeaxanthin 3g, astaxanthin 2g, beta-carotene 5g, blueberry extract 15g, vitamin E 20g, water 60000g.

[0113] II. Manufacturing Method

[0114] 1. Thoroughly mix lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, bilberry extract, and vitamin E to prepare a nutrient mixture; 2. Heat both the nutrient mixture and water to 45°C. At 45°C, slowly add the nutrient mixture to the water and mix to prepare a nutrient solution. 3. The nutrient mixture is sterilized by filtration through a 0.25μm sterile filter membrane to obtain the functional nutrient fortifier composition.

[0115] Control standard (used only for treatment efficacy testing)

[0116] I. Raw Materials

[0117] Lutein 4g, lutein ester 4g, zeaxanthin 3g, astaxanthin 2g, beta-carotene 5g, blueberry extract 15g, vitamin E 20g, water 60000g.

[0118] II. Manufacturing Method

[0119] 1. Dissolve lutein, lutein ester, zeaxanthin, astaxanthin, beta-carotene, bilberry extract, and vitamin E in water, and stir at room temperature for 30 minutes.

[0120] Detection experiment

[0121] I. Method: This invention determined the water solubility and stability of Examples 1-10 and Control Examples 1-4. Since blueberries are rich in anthocyanins, the blueberry extract involved in this invention mainly refers to anthocyanins; the anthocyanins detected during the testing process represent the blueberry extracts in the examples.

[0122] 1. Solubility test

[0123] Take 100 ml of each newly prepared example sample or control sample, and concentrate the sample solution to a saturated solution by evaporating the water in the sample under reduced pressure. Simultaneously, prepare saturated solutions of standard samples for lutein, lutein esters, zeaxanthin, astaxanthin, β-carotene, anthocyanins, and vitamin E; these are the reference standards. Determine the content of each nutrient component in the example samples, control samples, and reference standards using high-performance liquid chromatography (HPLC). Use the nutrient content of the reference standards as the baseline for the corresponding example samples or control samples (calculated in units of 1). Calculate the solubility ratio of each example sample or control sample to the corresponding reference standard.

[0124] 2. Stability testing

[0125] Accelerated testing was used to determine the drug stability of the example and control samples of this invention. The example and control samples were placed under UV irradiation at 75% ± 5% humidity and 60℃ ± 2℃ for 24 hours. The content of nutrients in each example and control sample was determined by high-performance liquid chromatography (HPLC) at 0 hours and 24 hours, and the degradation rate of each nutrient was calculated. Degradation rate = (M0 - M...) 24 ) / M0, where M0 represents the nutrient content at 0 hours of accelerated testing in the example, and M 24 The nutrient content was measured during an accelerated 24-hour test as an example. The stability of the samples was determined by comparing the degradation rate of nutrients during the accelerated test.

[0126] 3. Treatment efficacy testing

[0127] Evaluation of treatment efficacy: The visual acuity of patients before and after treatment was measured using an internationally recognized visual acuity chart, and a systematic fundus examination was performed. The treatment effect was evaluated according to the "Clinical Disease Diagnostic Criteria".

[0128] Significant effect: The patient's visual acuity improves by ≥0.3 (or the patient's visual acuity improves by ≥0.3, and symptoms such as macular hemorrhage and vitreous condyloma basically disappear); Improvement: The patient's visual acuity improves by 0.1 to 0.2 (or the patient's visual acuity improves by 0.1 to 0.2, and the symptoms of macular lesions improve to some extent, and the disease progression is slow); Ineffective: The patient's visual acuity and clinical symptoms show no significant improvement. Total effective rate = Significant effect + Improvement.

[0129] Sixty patients with age-related macular degeneration were selected as subjects for the clinical trial.

[0130] Sixty patients with age-related macular degeneration were randomly divided into two groups (Group 1 and Group 2), with 30 patients in each group (60 eyes). Patients in Group 1 received the sample from Example 4, while patients in Group 2 received a control product containing the same amount of nutrients and water as in Example 4, but without other excipients. Both products were administered once daily at a dose of 10 ml for three months. Changes in visual acuity and the macular region before and after treatment were analyzed.

[0131] II. Results

[0132] Table 1 records the solubility properties of the samples from the embodiments of the present invention and the control samples. Table 2 records the degradation rate of the nutrients in the samples from the embodiments of the present invention and the control samples, and compares the stability properties of the tested samples. Table 3 records the clinical trial results of the samples from the embodiments of the present invention.

[0133] 1. Solubility test results

[0134] Table 1. Solubility ratios of the example samples and the control samples.

[0135] Table 1 records the solubility ratios of each nutrient in the examples or control examples and their corresponding reference products. Examples 1-10 contain nutrients, fat-soluble antioxidants, and emulsifiers; Control Example 1 contains nutrients and emulsifiers, but no fat-soluble antioxidants and contains water-soluble antioxidants; Control Example 2 contains nutrients and fat-soluble antioxidants, but no emulsifiers; Control Example 3 contains only nutrients and no fat-soluble antioxidants or emulsifiers. The data in the table show that the examples containing fat-soluble antioxidants and emulsifiers have high solubility; while the control examples containing emulsifiers but no fat-soluble antioxidants (or containing water-soluble antioxidants) have solubility similar to the examples; while Control Example 3, containing fat-soluble antioxidants but no emulsifiers, has poor solubility, almost the same as Control Example 4, which contains only nutrients. This indicates that emulsifiers are crucial for the solubility of nutrients.

[0136] 2. Stability testing

[0137] Table 2. Degradation rates of the sample from the examples and the control examples.

[0138] Table 2 records the degradation rates of each nutrient component during accelerated testing of Examples 1-10 and Control Examples 1-4, thus comparing the stability of the samples. The data shows that the examples containing both fat-soluble antioxidants and emulsifiers had the lowest nutrient degradation rate, less than 20%. Control Example 1 contained both water-soluble antioxidants and emulsifiers; Control Example 2 contained emulsifiers but no fat-soluble antioxidants; Control Example 3 contained fat-soluble antioxidants but no emulsifiers; and Control Example 4 contained neither fat-soluble antioxidants nor emulsifiers. The nutrient degradation rates of the control examples were all greater than 60%. Analysis shows that the stability of the samples from the present invention is far higher than that of the control examples, indicating that only the fat-soluble antioxidants solubilized by emulsifiers play a crucial role in the stability of the nutrients, while water-soluble antioxidants and unsolidated fat-soluble antioxidants have no effect on the stability of the nutrients in solution.

[0139] 3. Treatment efficacy testing

[0140] Table 3 Clinical trial testing of the samples in the examples

[0141] Table 3 summarizes the clinical trial data of Example 4 and the reference product of this invention. Example 4 contains multiple nutrients, fat-soluble antioxidants, and emulsifiers in reasonable amounts, resulting in good clinical efficacy. The reference product contains only nutrients and water, lacking fat-soluble antioxidants and emulsifiers, thus exhibiting poor emulsification, instability of nutrients, and poor clinical effect. The data indicate that the sample with both fat-soluble antioxidants and emulsifiers added to the nutrients provides the best eye protection and is the ideal sample.

[0142] As can be seen from the above description, the embodiments of the present invention achieve the following technical effects: The nutritional components of this invention contain lutein and / or lutein esters, and may also contain zeaxanthin, β-carotene, astaxanthin, vitamin E, and bilberry extract. These nutrients are effective in protecting eyesight. Lutein, zeaxanthin, β-carotene, and astaxanthin belong to the carotenoid family. These four substances, along with vitamin E and bilberry extract, can all act as antioxidants to protect eyesight. Except for bilberry extract, which is slightly soluble in water, the above four carotenoids and vitamin E are fat-soluble substances with poor water solubility. Moreover, lutein, zeaxanthin, astaxanthin, β-carotene, bilberry extract, and vitamin E have poor stability and low bioavailability during storage and human consumption.

[0143] The functional nutrient fortifier composition of this invention is an oral solution comprising nutrients, a fat-soluble antioxidant, an emulsifier, and water. Lutein, lutein esters, zeaxanthin, β-carotene, astaxanthin, vitamin E, and bilberry extract in this invention are fat-soluble nutrients with poor stability. The emulsifier used in this invention not only increases the water solubility of the nutrients but also does not affect their efficacy; however, the stability of these nutrients remains a technical challenge. To improve the stability of the nutrients in aqueous solutions, our researchers conducted numerous experiments, adding one or more of water-soluble antioxidants, pH adjusters, and metal complexing agents. However, none of these methods had a stabilizing effect on the aforementioned nutrients. Typically, because fat-soluble antioxidants are poorly soluble in water, there is currently no precedent for using them in aqueous solutions. We creatively discovered that by adding specific fat-soluble antioxidants while emulsifying the nutrients with an emulsifier, the emulsifier solubilizes the specific fat-soluble antioxidants, and then applying this solution to the preparation of the nutrient solution, we surprisingly found that the stability of these nutrients was greatly improved. The specific fat-soluble antioxidants are one or more selected from butylated hydroxytoluene, butylated hydroxyanisole, and rosemary extract. The emulsifiers used to solubilize the fat-soluble antioxidants are one or more selected from Tween 80, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, and polyethylene glycol 15-hydroxystearate. The scientifically formulated emulsifiers and specific fat-soluble antioxidants exhibit good compatibility, and the solubilized fat-soluble antioxidants provide better stability for the nutrients. This solution can be effectively absorbed by the human body, enhancing its therapeutic effect. The combined use of fat-soluble antioxidants and emulsifiers increases the solubility and stability of nutrients in water, providing a functional nutritional fortifier composition with high water solubility, good stability, rapid absorption, high bioavailability, and even the ability to effectively treat various eye diseases.

[0144] This invention also incorporates functional ingredients (collagen, vitamin C, or enzymes) to prepare a functional oral liquid formulation, which can more comprehensively regulate the body and prevent and treat diseases.

[0145] The above description is merely a preferred embodiment of the present invention and is not intended to limit the invention. Various modifications and variations can be made to the present invention by those skilled in the art. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the scope of protection of the present invention.

Claims

1. An oral liquid for improving eyesight, characterized in that, It is made from the following raw materials in parts by weight: 1-30 parts lutein, 1-30 parts lutein ester, 1-5 parts zeaxanthin, 1-5 parts astaxanthin, 3-10 parts β-carotene, 10-20 parts blueberry extract, 10-30 parts vitamin E, 1-10 parts butylated hydroxyanisole, 200-1500 parts Tween 80, and 30,000-100,000 parts water.

2. The oral liquid according to claim 1, characterized in that, It is made from the following ingredients in parts by weight: 4 parts lutein, 4 parts lutein ester, 3 parts zeaxanthin, 2 parts astaxanthin, 5 parts beta-carotene, 15 parts blueberry extract, 20 parts vitamin E, 5 parts butylated hydroxyanisole, 600 parts Tween 80, and 60,000 parts water.

3. The method for preparing the oral liquid according to claim 1 or 2, characterized in that, Includes the following steps: (1) Lutein, lutein ester, zeaxanthin, astaxanthin, β-carotene, blueberry extract, vitamin E, butylated hydroxyanisole and Tween 80 are thoroughly mixed to prepare a nutrient mixture; (2) Heat the nutrient mixture and water to 40~80℃, slowly add the nutrient mixture to the water to make it completely dissolved, and prepare a nutrient solution; (3) The nutrient solution is filtered through a 0.25μm sterile filter membrane to remove bacteria, and finally an oral liquid for improving vision is obtained.

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