Composition for eye care

Abstract

An object of the present invention is to provide an eye care composition which can be produced with a reduced risk of failure during production by not using a bilberry extract raw material, has good formulation stability, and can be reduced in dosage.SOLUTION: The above object can be achieved by an eye care composition comprising a Haematococcus alga extract, a marigold extract, a propolis extract and vitamin A as active ingredients, and an eye care composition comprising astaxanthin, lutein, zeaxanthin, a propolis extract and vitamin A as active ingredients.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to eye care compositions. [Background technology]

[0002] Antioxidant components such as polyphenols such as anthocyanins and carotenoid pigments such as lutein are used as active ingredients in eye care compositions, and eye care compositions are used to protect the eyes from various types of oxidative stress.

[0003] Some eye care compositions, such as "Blueberry Eye PRO" (manufactured by Wakasa Seikatsu Co., Ltd.), use bilberry-derived anthocyanin (hereinafter referred to as VMA) as an active ingredient. "Blueberry Eye PRO" contains 40 mg of VMA (160 mg of bilberry extract raw material) (see, for example, Non-Patent Document 1).

[0004] VMA is widely used in eye care compositions. However, the effective dose of VMA is as high as 40 mg or more per day, and the VMA content in bilberry extract raw materials is only about 36% by mass even in highly purified forms. Therefore, to obtain an effective amount of VMA, it is necessary to produce an eye care composition containing 111 mg or more of bilberry extract raw materials per day. Therefore, when VMA is combined with excipients and other ingredients in the formulation, problems arise, such as the number of formulations to be taken increasing and the size of each formulation increasing.

[0005] Furthermore, VMA has the property of reacting or polymerizing with other ingredients combined with it, impairing the stability of the formulation. In particular, in soft capsule formulations, VMA reacts with gelatin molecules derived from the capsule coating, which is known to cause delayed disintegration of the formulation and decay of the ingredients (see, for example, Patent Document 1).

[0006] Other known eye care components besides VMA include astaxanthin, lutein, and zeaxanthin. Astaxanthin has physiological effects such as improving eye fatigue, reducing shoulder and lower back strain associated with eye fatigue, and improving eye focusing ability. Some foods containing astaxanthin have functional claims. Lutein and zeaxanthin also have physiological effects such as regulating eye condition, increasing human macular pigmentation dose (MPOD) concentration-dependently (e.g., Non-Patent Document 2), and improving contrast sensitivity. Some foods containing lutein or zeaxanthin have functional claims. Astaxanthin is contained in Haematococcus algae extract, and lutein and zeaxanthin are contained in marigold extract.

[0007] Known eye care compositions containing VMA, astaxanthin, and lutein include an agent for relieving stiff shoulders and an agent for relieving eye congestion that contain astaxanthin, lutein, black soybean husk extract, bilberry extract, and DHA (see, for example, Patent Document 2). [Prior art documents] [Patent documents]

[0008] [Patent Document 1] Japanese Patent Application Laid-Open No. 2011-079786 [Patent Document 2] Japanese Patent Application Laid-Open No. 2016-183121 [Non-patent literature]

[0009] [Non-Patent Document 1] Wakasa Life Shopping Website [URL] https: / / shop.wakasa.jp / shop / blueberry%EF%BC%8Dsupplements / g / g111000131-00 / ; Searched July 2024 [Non-patent document 2] Richard A. Bone et al., Arch Biochem Biophys. 2010 Dec 1; 504(1): 50-55. Summary of the Invention [Problem to be solved by the invention]

[0010] The shoulder stiffness alleviating agent and eye congestion alleviating agent described in Patent Document 2 combine astaxanthin with bilberry extract and black soybean husk extract. However, while astaxanthin is an oil raw material, VMA is a powder raw material. When an eye care composition is formulated as a soft capsule, using VMA, which is a powder raw material, increases the risk of defects during manufacturing. In this regard, the shoulder stiffness alleviating agent and eye congestion alleviating agent described in Patent Document 2 contain VMA, which results in poor formulation stability and a large daily intake (number of capsules), i.e., a large single dose.

[0011] Therefore, an object of the present invention is to provide an eye care composition that can be produced without using VMA, i.e., bilberry extract raw material, thereby reducing the risk of defects during production, has good formulation stability, and can be made in a smaller dosage. [Means for solving the problem]

[0012] The present inventors have conducted extensive research to solve the above problems and have concluded that an eye care composition that combines antioxidant ingredients other than VMA would have good formulation stability and could be reduced in dosage, leading to a reduction in the burden of ingestion.

[0013] Therefore, by replacing VMA with astaxanthin, the inventors created an eye care composition that not only provides the "eye fatigue reduction" and "eye focus adjustment" functions claimed by VMA-containing eye care compositions, but also "shoulder and lower back strain reduction." Specifically, by incorporating an effective amount of astaxanthin, it becomes possible to claim that the product reduces eye fatigue, shoulder and lower back strain, and improves functional eye focus adjustment. Furthermore, by incorporating effective amounts of lutein and zeaxanthin, it becomes possible to claim that the product has the effects of regulating eye condition, supplementing macular pigment levels, and improving contrast sensitivity.

[0014] The effective dose of astaxanthin is only 6 mg per day, but by using a highly concentrated raw material, the amount can be reduced to 30 mg per day, less than one-third of the amount required when using VMA raw materials. This allows for a smaller dosage than VMA-containing eye care compositions, while still combining many antioxidant ingredients such as lutein, zeaxanthin, propolis, and vitamin A.

[0015] According to Non-Patent Document 2, MPOD increases in a concentration-dependent manner between 0 mg, 5 mg, 10 mg, and 20 mg of lutein. Since it has been reported that lutein increases the amount of macular pigment in a concentration-dependent manner, increasing the amount of lutein will lead to increased added value of eye care compositions.

[0016] VMA is a powdered ingredient, while astaxanthin is an oil. The contents of soft capsules are blended, crushed, and sieved while heated, but to prevent decomposition and deterioration of the ingredients, it is desirable to add the active ingredient as far downstream as possible in the blending process. VMA, a powdered ingredient, must be added before the crushing process to disperse it, but by replacing VMA with astaxanthin, it can be added after the crushing process, minimizing the heat history.

[0017] When a powder ingredient such as VMA is added to a soft capsule, it can remove moisture from the coating, leading to formulation defects such as capsule cracking, leakage, and powder getting caught during molding. However, by replacing VMA with astaxanthin, an oil ingredient, it is possible to reduce the risk of these defects.

[0018] The applicant's current product containing VMA, "Kukkiri iBee (registered trademark)," contains an effective amount of VMA, but the lutein content is only 6 mg, with the recommended daily intake being two tablets. By replacing VMA with astaxanthin, the amount of lutein can be significantly increased to 20 mg while maintaining the existing antioxidants of Brazilian propolis powder (50 mg) and vitamin A (231 μg). Furthermore, it is possible to add 2 mg of zeaxanthin, a carotenoid pigment. Like lutein, zeaxanthin is a component present in the eye as a macular pigment with antioxidant properties, and adding it can protect the eyes from light stress.

[0019] Furthermore, the daily liquid volume can be significantly reduced, making it possible to formulate the recommended daily intake as a single tablet. This not only reduces the burden on supplement users, but also contributes to reducing formulation processing costs, simplifying the filling process, and miniaturizing packaging materials. However, because astaxanthin is a fat-soluble pigment, it is difficult to formulate it at high concentrations when formulated in forms other than soft capsules, such as tablets or granules. For example, the content is about 20% for oil raw materials and about 2% for powder raw materials.

[0020] The present invention has been completed based on the findings and successful examples first discovered by the present inventors.

[0021] Thus, the following aspects of the present invention are provided: [1] An eye care composition containing Haematococcus algae extract, marigold extract, propolis extract, and vitamin A as active ingredients. [2] An eye care composition containing astaxanthin, lutein, zeaxanthin, propolis extract, and vitamin A as active ingredients. [3] The eye care composition according to item [1] or [2], which is in the form of a soft capsule formulation. [Effects of the Invention]

[0022] The eye care composition of one embodiment of the present invention can protect the eyes of the user by the active ingredient contained therein. By not using VMA, the eye care composition of one embodiment of the present invention can be produced with a reduced risk of defects during production, has good formulation stability, and can be formulated in small doses. The eye care composition of one embodiment of the present invention can be stored well due to its formulation stability, and the small doses can reduce the burden on the user. The eye care composition of one embodiment of the present invention can be added after the grinding process during production, so it can be produced with minimal thermal history. DETAILED DESCRIPTION OF THE INVENTION

[0023] Each aspect of the present invention will be described in detail below, but the present invention can take various forms as long as it achieves its object.

[0024] The term "composition" is not particularly limited to the meaning normally used, but may refer to, for example, a substance made by combining two or more components (raw materials). "Food and beverage" is a generic term meaning food, beverages, or both. "And / or" means any one or any or all combinations of two or more of the associated listed items. "Content" is synonymous with concentration and amount added (amount used), and refers to the ratio of the amount of a component to the total amount of the composition. However, the total amount of the components does not exceed 100%. When a commercially available product is used, the content of the component is preferably the amount of the component contained in the commercially available product, but may also be the amount of the commercially available product itself. "Comprise," "contain," and "include" mean that elements other than those explicitly stated as included may be added (same meaning as "comprise at least"), but also encompass "consist of" and "essentially consist of." That is, "comprise" can mean including the explicitly stated elements and any one or more elements, consisting of the explicitly stated elements, or essentially consisting of the explicitly stated elements. Elements include limitations such as ingredients, steps, conditions, and parameters. The use of "to" in a numerical range includes both the preceding and following numerical values, and also includes ranges excluding either of the included limits. For example, "0% to 100%" means 0% or more, 100% or less, or 0% or more and 100% or less. "About" means an amount within ±10% of the quantity following the term. For example, "about 100" means 100±10%, i.e., 90 to 110.

[0025] One aspect of the present invention is an eye care composition. The eye care composition is used to improve symptoms caused by the eyes. Specifically, the eye care composition has one, two, three, or all four of the following effects on the user: reducing eye fatigue, adjusting eye focus, reducing shoulder strain associated with eye fatigue, and reducing lower back strain. These physiological effects of the eye care composition are sometimes collectively referred to as eye care effects.

[0026] Eye care compositions are broadly divided into two aspects. The eye care composition of the first aspect of the present invention contains, as active ingredients, Haematococcus algae extract, marigold extract, propolis extract, and vitamin A. The eye care composition of the second aspect of the present invention contains, as active ingredients, astaxanthin, lutein, zeaxanthin, propolis extract, and vitamin A.

[0027] [Haematococcus algae extract and astaxanthin] Haematococcus algae extract and astaxanthin are included as functional ingredients in the eye care composition.

[0028] Haematococcus algae extract, also known as Haematococcus algae pigment, is an extract of Haematococcus algae such as Haematococcus pluvialis, Haematococcus lacustris, Haematococcus capensis, Haematococcus deroebakensis, and Haematococcus zimbabwiensis. Haematococcus algae extract can be obtained, for example, by culturing Haematococcus algae and subjecting the resulting culture to an extraction treatment.

[0029] The Haematococcus algae extract contains approximately 1% to 40% by mass of astaxanthin. Astaxanthin can be obtained by subjecting the Haematococcus algae extract to a purification treatment. The Haematococcus algae extract may be used as one containing an equivalent amount of astaxanthin. For example, if the Haematococcus algae extract contains 20% by mass of astaxanthin, 100 mg of the Haematococcus algae extract may be used as one containing 20 mg of astaxanthin.

[0030] The Haematococcus algae extract and astaxanthin may be commercially available from BGG Japan, Oryza Oil & Fat Chemical, Fuji Chemical Industry, Biogenic, and the like.

[0031] The content of Haematococcus algae extract is, for example, preferably 5% by mass to 7% by mass, more preferably 5.7% by mass to 6.7% by mass, and even more preferably approximately 6.1% by mass, based on the total amount of the eye care composition.

[0032] The astaxanthin content is, for example, preferably 0.5% to 2% by mass, more preferably 1.1% to 1.4% by mass, and even more preferably about 1.2% by mass, based on the total amount of the eye care composition. For example, when the eye care composition is a 500 mg soft capsule, the astaxanthin content may be 5.5 mg to 7.0 mg per capsule.

[0033] In a paper by Yasunori Nagaki et al. (Clinical Medicine, Vol. 22, No. 1 (January) 2006, pp. 41-54), it is stated that in a double-blind study comparing astaxanthin administration and non-administration, the astaxanthin group showed a significant improvement in the accommodative ability of people complaining of tired eyes, and that the astaxanthin group also showed significantly better symptoms of "blurred vision" and "stiff shoulders and lower back." Furthermore, in a paper by Nagaki et al. (J.Trad.Med. 19, 170-173, 2002), it is stated that the group taking 5 mg of astaxanthin showed a significant improvement in eye fatigue symptoms (p<0.05) compared to the placebo group.

[0034] The eye care composition of one embodiment of the present invention contains a large amount of astaxanthin compared to the shoulder stiffness relief agent and eye congestion relief agent (2 mg of astaxanthin / granule) described in Patent Document 2, and therefore has excellent effects on eye focusing, relief of "blurred vision" and "stiff shoulders and lower back," and relief of eye fatigue symptoms.

[0035] [Marigold extract, lutein and zeaxanthin] Marigold extract, lutein and zeaxanthin are included as functional ingredients in eye care compositions.

[0036] Marigold extract, also known as marigold pigment, is an extract of marigold, and can be obtained, for example, by subjecting marigold petals to an extraction treatment.

[0037] Marigold extract contains approximately 1% to 50% by mass of lutein and / or 1% to 20% by mass of zeaxanthin. Purification of the marigold extract yields lutein, zeaxanthin, or a mixture thereof. The marigold extract may be used as one containing equivalent amounts of lutein and / or zeaxanthin. For example, if the marigold extract contains 20% by mass of lutein and 2% by mass of zeaxanthin, 100 mg of the marigold extract may contain 20 mg of lutein and 2 mg of zeaxanthin.

[0038] Marigold extract, lutein, and zeaxanthin may be commercially available from BGG Japan, DSM Nutrition Japan, Koyo Sho, Kyowa Hakko Bio, Inabata Fragrance, and the like.

[0039] The content of marigold extract is, for example, preferably 15% by mass to 25% by mass, more preferably 19.2% by mass to 22.2% by mass, and even more preferably approximately 20.4% by mass, based on the total amount of the eye care composition.

[0040] The lutein content of the eye care composition is preferably 3% to 5% by mass, more preferably 3.8% to 4.5% by mass, and even more preferably about 4.1% by mass. For example, when the eye care composition is a 500 mg soft capsule, the lutein content may be 19.0 mg to 22.5 mg per capsule.

[0041] The content of zeaxanthin is, for example, preferably 0.1% by mass to 1% by mass, more preferably 0.3% by mass to 0.6% by mass, and even more preferably about 0.4% by mass, based on the total amount of the eye care composition. For example, when the eye care composition is a 500 mg soft capsule, the content of zeaxanthin may be 1.5 mg to 3.0 mg per capsule.

[0042] [Propolis extract] Propolis extract is included as an antioxidant ingredient in eye care compositions.

[0043] Propolis is a resinous or waxy substance that forms the walls of beehives and is made by mixing the buds and resins of plants that bees have collected with their saliva. Propolis can be obtained, for example, as a beekeeping product in the usual way.

[0044] The propolis extract is an extract of propolis and is obtained by subjecting propolis to an extraction treatment. The propolis extract may be commercially available from Yamada Bee Farm or the like.

[0045] The content of the propolis extract is, for example, preferably 9% by mass to 12% by mass, more preferably 9.6% by mass to 11.7% by mass, and even more preferably approximately 10.2% by mass, based on the total amount of the eye care composition.

[0046] [Vitamin A] Vitamin A is included in eye care compositions as an antioxidant and nutritional fortifier.

[0047] Vitamin A is a general term for retinol, retinal, and retinoic acid. Vitamin A may be produced by a conventional method or may be commercially available from Riken Vitamin Co., Ltd.

[0048] The content of vitamin A is, for example, preferably 0.01% by mass to 0.1% by mass, more preferably 0.04% by mass to 0.07% by mass, and even more preferably about 0.05% by mass, based on the total amount of the eye care composition.

[0049] [Eye care composition] The eye care composition of one embodiment of the present invention is used to improve symptoms caused by the eyes of a user.

[0050] The eye care composition is administered to, for example, a mammal, preferably a human, to improve symptoms caused by the eye, and is preferably administered orally.

[0051] The dosage of an eye care composition for oral administration can be determined as appropriate depending on the active ingredient, the form of the composition, and the application method and amount, but for example, for an adult weighing 60 kg, the daily dose, calculated on a dry solids basis, is preferably 100 mg to 3,000 mg, more preferably 200 mg to 1,000 mg, even more preferably 300 mg to 600 mg, and even more preferably about 500 mg. However, these dosages can be increased or decreased as appropriate depending on factors such as the health condition of the recipient, the administration method, the type of active ingredient, and the combination with other compositions.

[0052] As long as the daily dose is within the above-mentioned range, the eye care composition may be administered once a day or in divided doses such as twice or three times a day. Although the eye care composition is expected to be effective in a relatively short period of time after administration, continuous administration for one to four weeks, one month or more, six months or more, or one year or more is expected to further sustain or enhance the effect, and therefore continuous administration is preferred.

[0053] The eye care composition can be used as, or as a part of, a food or drink or a pharmaceutical product, and is preferably used as, or as a part of, a food or drink used for eye care.

[0054] The eye care composition can be used as a food or drink, preferably a food or drink intended for health maintenance, health promotion, etc., more preferably a health food, functional food, nutritional composition, dietary supplement, supplement, health food, food for specified health uses, nutrient functional food, food with functional claims, pharmaceutical product, etc. The eye care composition can also be used as an additive that imparts an eye care effect.

[0055] Foods, beverages, and pharmaceuticals containing the eye care composition as an ingredient can be produced, for example, by adding the eye care composition to intermediate products in the manufacturing process of these products.

[0056] In addition to the active ingredient, foods and beverages contain other ingredients, such as minerals, vitamins, flavonoids, quinones, polyphenols, amino acids, nucleic acids, essential fatty acids, cooling agents, binders, sweeteners, disintegrants, lubricants, colorants, flavorings, stabilizers, gelling agents, preservatives, sustained-release regulators, surfactants, solubilizers, and humectants.

[0057] The method for producing the food or drink is not particularly limited as long as it contains the active ingredient and / or the eye care composition, and any known method can be used as appropriate.

[0058] When the eye care composition is used as a supplement, the dosage unit form is not particularly limited and can be selected as appropriate. Examples include pills, chewable tablets, troches, and other tablets, capsules (hard capsules, soft capsules), granules, liquids, powders, syrups, pastes, drinks, gummies, and the like. However, because astaxanthin is an oil-based ingredient and lutein is also a fat-soluble component, soft capsules are preferred.

[0059] Pharmaceuticals contain other ingredients in addition to the active ingredient, such as vitamins, herbal medicines, etc. The active ingredient and other ingredients can also be mixed with other pharmaceutical ingredients listed in the Japanese Pharmacopoeia before use.

[0060] When preparing an eye care composition as a pharmaceutical, the active ingredient, together with ingredients acceptable for pharmaceuticals, may be prepared into a pharmaceutical formulation in the form of a tablet (including plain tablets, sugar-coated tablets, effervescent tablets, film-coated tablets, chewable tablets, troches, etc.), capsule (hard capsule, soft capsule), pill, powder (powder), fine granules, granules, liquid, suspension, emulsion, syrup, paste, injection (including the case where the composition is mixed with distilled water or an infusion such as an amino acid infusion or an electrolyte infusion at the time of use to prepare a liquid), or the like.

[0061] The pharmaceutical agent may be administered topically, preferably orally.

[0062] In addition to the active ingredient, pharmaceuticals may contain, as appropriate, pharmaceutically acceptable ingredients such as excipients, binders, disintegrants, lubricants, colorants, suspending agents, thickeners, antioxidants, absorption enhancers, pH adjusters, preservatives, antiseptics, stabilizers, surfactants, sweeteners, flavoring agents, and fragrances.

[0063] The eye care composition may also be used as a quasi-drug.

[0064] The eye care composition of one embodiment of the present invention is applied to eye care of mammals including humans (preferably humans).

[0065] Furthermore, the eye care composition according to one embodiment of the present invention contains active ingredients that have traditionally been used as food ingredients, and therefore can be used as a highly safe product overall.

[0066] A specific example of an eye care composition according to one embodiment of the present invention is a 500 mg soft capsule containing active ingredients consisting of 5.7% by mass to 6.7% by mass of Haematococcus algae extract, 19.2% by mass to 22.2% by mass of marigold extract, 9.6% by mass to 11.7% by mass of propolis extract, and 0.4% by mass to 0.8% by mass of vitamin A, and 58.8% by mass to 64.9% by mass of excipients and other ingredients. By taking one soft capsule at a time once a day, the user's eye fatigue can be alleviated, the eye focusing function can be adjusted, and strain on the shoulders and lower back can be reduced.

[0067] Another specific example of an eye care composition according to one embodiment of the present invention is a 500 mg soft capsule containing active ingredients consisting of 1.1 to 1.4% by mass of astaxanthin, 3.8 to 4.5% by mass of lutein, 0.3 to 0.6% by mass of zeaxanthin, 9.6 to 11.7% by mass of propolis extract, and 0.4 to 0.8% by mass of vitamin A, and 81.9 to 85.0% by mass of excipients and other ingredients. By taking one soft capsule at a time once a day, the user can reduce eye fatigue, adjust the eye focusing function, reduce shoulder strain, and reduce strain on the lower back.

[0068] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples, and the present invention can take various forms as long as the object of the present invention can be achieved. [Example]

[0069] The eye care composition of Example 1, which is a soft capsule, was produced by blending, pulverizing, sieving, molding, and filling the commercially available ingredients shown in Table 1. Similarly, the eye care composition of Example 2 and the eye care composition of Comparative Example 1 were produced using the commercially available ingredients shown in Tables 2 and 3.

[0070] As shown in Tables 1 to 3, the eye care compositions of Examples 1 and 2 had a higher content of eye care functional ingredients and a lower dosage compared to the eye care composition of Comparative Example 1, and were manufactured as soft capsules that allowed the intake of an effective amount in one capsule.

[0071] [Table 1]

[0072] [Table 2]

[0073] [Table 3] [Industrial Applicability]

[0074] The eye care composition of one embodiment of the present invention can be used to protect the eyes of a user due to the active ingredients contained therein, and since it can be easily produced, it can be produced in large quantities on an industrial scale.

Claims

1. An eye care composition comprising Haematococcus algae extract, marigold extract, propolis extract and vitamin A as active ingredients.

2. An eye care composition comprising astaxanthin, lutein, zeaxanthin, propolis extract and vitamin A as active ingredients.

3. 3. The eye care composition according to claim 1, which is in the form of a soft capsule formulation.

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