WO2021107106A1 - 経口組成物 - Google Patents

経口組成物 Download PDF

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Publication number
WO2021107106A1
WO2021107106A1 PCT/JP2020/044249 JP2020044249W WO2021107106A1 WO 2021107106 A1 WO2021107106 A1 WO 2021107106A1 JP 2020044249 W JP2020044249 W JP 2020044249W WO 2021107106 A1 WO2021107106 A1 WO 2021107106A1
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WO
WIPO (PCT)
Prior art keywords
lutein
mass
oral composition
eye
lipoic acid
Prior art date
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PCT/JP2020/044249
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English (en)
French (fr)
Japanese (ja)
Inventor
敬 石川
良宏 高井
菜採 羽渕
千晶 小倉
Original Assignee
ロート製薬株式会社
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Application filed by ロート製薬株式会社 filed Critical ロート製薬株式会社
Priority to JP2021561552A priority Critical patent/JPWO2021107106A1/ja
Publication of WO2021107106A1 publication Critical patent/WO2021107106A1/ja

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    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L27/00Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L27/00Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
    • A23L27/20Synthetic spices, flavouring agents or condiments
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/46Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention relates to an oral composition. More specifically, it relates to an oral composition comprising lutein and ⁇ -lipoic acid, lutein and seaberry, or ⁇ -lipoic acid.
  • Eye strain and discomfort include overuse of the eyes such as reading, gazing work, and observation work, mental tension, and aging, but the number has increased rapidly with the spread of personal computers and smartphones. Eye strain and upset due to VDT (Visual Display Computer) work are also increasing. Patients who complain of eye strain or discomfort generally also have symptoms such as pain in the back of the eyes, blurred vision, dry eyes, stiff shoulders, and heavy head. It has been pointed out that these symptoms are caused by the ciliary muscles becoming excessively tense due to long-term gaze work and the like, and the accommodation function of the eyes deteriorates.
  • presbyopia cataracts, glaucoma, and age-related macular degeneration may be the cause, but deterioration or dysfunction of visual function is not caused by such symptoms or diseases. But it can happen.
  • the decline in visual function causes a decrease in QOL (Quality of Life), and it is necessary to maintain or improve the function.
  • astaxanthin and anthocyanins are also known as components used in compositions for aiming eye health and components having an excellent effect of improving eye strain (for example, Patent Document 2). ⁇ 3).
  • An object of the present invention is to provide an oral composition having an effect of alleviating various eye disorders.
  • ⁇ -lipoic acid has a function of improving focus adjustment and a function of maintaining short-range visual acuity. Furthermore, they have found that ⁇ -lipoic acid and seaberry have an effect of improving the flavor of lutein, and have completed the present invention.
  • Item 1 An oral composition containing lutein and ⁇ -lipoic acid.
  • Item 2. Item 2.
  • Item 3. A composition for improving the flavor of lutein containing ⁇ -lipoic acid.
  • Item 4. A method for improving the flavor of an oral composition, which comprises coexisting ⁇ -lipoic acid with the oral composition containing lutein.
  • a method for suppressing aggregation of an oral composition which comprises coexisting lutein with an oral composition containing ⁇ -lipoic acid.
  • Item 6. Contains ⁇ -lipoic acid to maintain the amount of pigment in the yellow spots of the eye (eye), maintain the ability to see, improve the contrast sensitivity of the eye, improve the accommodation of the eye, alleviate eye troubles, improve the condition of the eye, and fatigue the eye.
  • Item 8. The oral composition according to Item 6 or 7, further containing lutein.
  • Item 9. Item 6.
  • Item 10. An oral composition containing lutein and sea berries.
  • Item 11. Item 10.
  • Item 12. A composition for improving the flavor of lutein containing seaberries.
  • Item 13 A method for improving the flavor of an oral composition, which comprises coexisting seaberries with an oral composition containing lutein.
  • flavor refers to any perception of an oral composition, such as aroma, odor, odor, taste, etc., when the oral composition is brought close to the nose or in the mouth.
  • odor also includes an unpleasant odor felt after eating or drinking the oral composition, such as a return odor.
  • flavor improvement means preventing deterioration of the flavor over time, maintaining the flavor over time, improving the flavor as compared with lutein alone, or comparing with lutein alone. Includes either to improve the flavor.
  • “Lutein” ( ⁇ , ⁇ -carotene-3,3'-diol) used in the present invention is a kind of carotenoid present in leaves, flowers, fruits and the like of plants.
  • the lutein used in the present invention is not limited, but a plant-derived lutein, particularly a marigold-derived lutein can be used. Lutein can also be contained by using the marigold pigment itself.
  • lutein derived from chloroplasts such as spinach, kale, and komatsuna can also be used.
  • the lutein may be artificially synthesized, may be obtained by genetic recombination, or a commercially available product may be used. Lutein may be in the form of a pharmaceutically acceptable salt.
  • Lutein is a red-orange pigment that accumulates in the macula of the retina and has antioxidant power. Light energy is concentrated in the macula, and the cells are dense and oxidative stress associated with its activity tends to accumulate. However, it is the macula pigment that protects the visual function by protecting against the light exposure and oxidative stress. , Zeaxanthin, mesozeaxanthin and the like. Therefore, administration of lutein suppresses the oxidative stress accumulated in the retinal nerve cells, contributes to the survival and visual function of the nerve cells, and causes abnormal enhancement of cell activity due to excessive light irradiation and oxidative stress of the retinal photoreceptor cells. Suppresses cell death due to accumulation and DNA damage.
  • Ingestion of lutein reduces the risk of developing age-related macular degeneration and also reduces the risk of developing cataracts.
  • Administration of retina improves contrast sensitivity in mesopic vision in high glare environments, improves contrast sensitivity in high mesopic vision, and improves visual function in low illumination; eye aging. It is possible to delay the function of the eye and suppress the occurrence of retinal diseases such as age-related macular degeneration, retinal pigment degeneration, central retinal chorioretinosis, macular hole retinal epithelial plasty, and macular hole. Etc. are also expected.
  • Lutein is a component having excellent functions as described above, but it is easily decomposed by light or heat. Lutein also has an unpleasant taste or odor. In the case of a preparation containing lutein, deterioration of flavor after storage and unpleasant taste at the time of eating and drinking are particularly problematic. Even in soft capsules and the like that stably contain lutein, the return odor and unpleasant taste after eating and drinking have become problems.
  • ⁇ -lipoic acid used in the present invention is represented by the following chemical formula.
  • the ⁇ -lipoic acid in the present invention is any of R, S- (+/-)- ⁇ -lipoic acid, R- (+)- ⁇ -lipoic acid, and S-(-)- ⁇ -lipoic acid. It may be salt or salt.
  • the ⁇ -lipoic acid in the present invention may be an extract derived from a synthetic product or a natural product component, or may be a commercially available product.
  • the form of ⁇ -lipoic acid may be powder, emulsion, or dispersion.
  • the ⁇ -lipoic acid of the present invention may also be an inclusion body of cyclodextrin from the viewpoint of significantly exerting the effect of the present invention, but is not limited thereto.
  • aggregation is a phenomenon in which ⁇ -lipoic acid is not dispersed, and for example, a phenomenon in which a component that precipitates is generated by centrifugation.
  • oral composition may be used as it is as a food or drink, an oral drug, or an oral quasi-drug, or as a raw material for the production thereof. It may be used.
  • food and drink refers to foods with functional claims, foods for specified health use, foods with nutritional function, foods for the elderly, special purpose foods, health supplements, food preparations such as confectionery tablets, and beverages. Including. These may be in the form of supplement preparations; packaged beverages; instant powdered beverages, instant granulated beverages, carbonated beverages, nutritional beverages, fruits for dissolution in water (hot water), milk, fruit juice, green juice, etc.
  • the pH is not particularly limited, but is preferably 2.0 to 2.0 from the viewpoint of improving the flavor. It is 8.0, more preferably 2.5 to 7.0, and even more preferably 3.0 to 6.0.
  • a first aspect of the present invention relates to an oral composition containing lutein and ⁇ -lipoic acid.
  • the content of lutein in the oral composition containing lutein and ⁇ -lipoic acid of the present invention is generally preferably 0.01% by mass or more, preferably 0.1% by mass, based on the total amount of the composition.
  • the above is more preferable, and 1% by mass or more is even more preferable.
  • a reasonably ingestible amount of oral composition will contain lutein sufficient to produce the desired effect.
  • the content of lutein in the oral composition is preferably 30% by mass or less, more preferably 20% by mass or less, still more preferably 10% by mass or less, based on the total amount of the composition. Within this range, it is easy to formulate and relatively easy to take.
  • the content of lutein in the oral composition containing lutein and ⁇ -lipoic acid of the present invention is generally preferably 0.01 to 30% by mass, preferably 0.1 to 30% by mass, based on the total amount of the composition. 20% by mass is more preferable, and 1 to 10% by mass is even more preferable.
  • the content of lutein is preferably 0.001% by mass or more based on the total amount, and 0. More preferably, it is 003% by mass or more.
  • the content of lutein in the packaged beverage or liquid is preferably 0.1% by mass or less, more preferably 0.025% by mass or less, based on the total amount of the composition.
  • lutein When the oral composition containing lutein and ⁇ -lipoic acid of the present invention is a packaged beverage or a liquid preparation, lutein may be contained in an amount of 0.001 to 0.1% by mass based on the total amount. It is preferably contained in an amount of 0.003 to 0.025% by mass, more preferably 0.003 to 0.025% by mass.
  • Lutein should also be an effective amount to tone the eyes. For example, 0.1 mg to 50 mg, more preferably 1 mg to 30 mg, and even more preferably 6 mg to 25 mg per day.
  • the content of ⁇ -lipoic acid in the oral composition containing lutein and ⁇ -lipoic acid of the present invention is generally preferably 0.001% by mass or more based on the total amount of the composition, and 0. 01% by mass or more is more preferable, and 0.1% by mass or more is even more preferable. Within this range, a reasonably ingestible amount of oral composition will contain enough ⁇ -lipoic acid to produce the desired effect.
  • the content of ⁇ -lipoic acid in the oral composition is preferably 90% by mass or less, more preferably 50% by mass or less, and even more preferably 40% by mass or less, based on the total amount of the composition. Within this range, it is easy to formulate and relatively easy to take.
  • the content of ⁇ -lipoic acid in the oral composition containing lutein and ⁇ -lipoic acid of the present invention is generally preferably 0.001 to 90% by mass, preferably 0, based on the total amount of the composition. 0.01 to 50% by mass is more preferable, and 0.1 to 40% by mass is even more preferable.
  • the content of ⁇ -lipoic acid is preferably 0.001% by mass or more based on the total amount. , 0.005% by mass or more is more preferable.
  • the content of ⁇ -lipoic acid in the packaged beverage or liquid is preferably 1% by mass or less, more preferably 0.1% by mass or less, based on the total amount of the composition.
  • ⁇ -lipoic acid may be contained in an amount of 0.001 to 1% by mass based on the total amount. It is preferably contained in an amount of 0.005 to 0.1% by mass, more preferably 0.005 to 0.1% by mass.
  • the amount of ⁇ -lipoic acid may be sufficient as long as it is sufficient for improving the flavor of lutein, but it may also be contained in an amount having a function of adjusting the condition of the eyes, which will be described later.
  • the content of ⁇ -lipoic acid with respect to 1 part by mass of lutein is not particularly limited, but the effect of improving the flavor of lutein and suppressing the aggregation of ⁇ -lipoic acid. From the viewpoint of remarkably playing, preferably 0.01 to 100 parts by mass, more preferably 0.05 to 50 parts by mass, still more preferably 0.1 to 10 parts by mass, and particularly preferably 0.5 to 5 parts by mass. is there.
  • the oral composition containing lutein and ⁇ -lipoic acid of the present invention can be used for foods and drinks, pharmaceuticals and quasi-drugs other than lutein and ⁇ -lipoic acid as long as the effects of the present invention are not impaired. It may contain known components. These include, for example, various pigments such as pH adjusters, preservatives, antioxidants (vitamin C, vitamin E, extracted tocopherol, etc.), thickeners, stabilizers, caramel pigments, emulsifiers, pastes and other additives. Contains but not limited to shaping agents and active ingredients primarily derived from plants.
  • the type of emulsifier that can be used in the oral composition containing the lecithin and ⁇ -lipoic acid of the present invention is not particularly limited, but is, for example, sucrose fatty acid ester, glycerin fatty acid ester (for example, monoglycerin fatty acid ester, polyglycerin fatty acid).
  • emulsifiers may be used alone or in combination of two or more.
  • excipient used in the oral composition containing lutein and ⁇ -lipoic acid of the present invention is not particularly limited, but for example, processed starch, starch decomposition products (dextrin, powdered candy, etc.), cellulose and the like.
  • Sugars Sugars, sugars (monosaccharides (glucose, fructos, etc.), disaccharides (eg, sucrose, lactose, maltose, trehalose, etc.), oligosaccharides (cellooligosaccharides, maltooligosaccharides, fructooligosaccharides, etc.), sugar alcohols (xylitol, sorbitol, etc.) Lactitol, maltose, etc.), reduced saccharified products, etc.), dietary fiber (for example, indigestible dextrin, polydextrose, guar gum enzymatic decomposition products, etc.) and the like. These excipients may be used alone or in combination of two or more.
  • the oral composition containing lutein and ⁇ -lipoic acid of the present invention can also contain carotenoids other than lutein.
  • carotenoids include crocetin, pharmaceutically acceptable salt of crocetin, cutinashi extract (Yamabiko), cutinashi pigment, saffron extract, germinated broccoli extract, broccoli sprout extract, paprika extract, ⁇ -carotene, zeaxanthin, astaxanthin. , Marigold extract, red paprika, paprika pigment, western ginseng extract, capsicum extract, tochu leaf extract, benibana extract, rafuma extract and the like.
  • the numbers in parentheses are aliases. These carotenoids may be used alone or in combination of two or more.
  • the oral composition containing lutein and ⁇ -lipoic acid of the present invention may also contain polyphenols.
  • the polyphenols contained in the oral composition containing lutein and ⁇ -lipoic acid of the present invention include ginkgo biloba extract, mangostin extract, strawberry seed extract, walnut polyphenol, galana extract, Javanese ginger extract, nobiletin, blueberry leaf extract and cassis. Examples thereof include extracts, curcumin, white curcuminoid, parsley extract, makiberry extract, polymethoxyflavonoid (PMF) and the like. These polyphenols may be used alone or in combination of two or more.
  • the oral composition containing lutein and ⁇ -lipoic acid of the present invention may also contain haskap juice, bilberry fruit extract, grape young shoot extract, ginger extract and the like. These may be used individually by 1 type, or may be used in combination of 2 or more type.
  • An oral composition containing lutein and ⁇ -lipoic acid is an oral composition in which the unfavorable flavor caused by lutein is improved or the flavor is improved and it is easy to take. Furthermore, for example, in foods with functional claims and health foods, the amount of pigment in the yellow spot of the eye (eye) is maintained, the ability to see is maintained, the contrast sensitivity of the eye is improved, the focus of the eye is improved, and the eye is not limited. It can be used to relieve worries, improve eye condition, relieve eye fatigue, improve accommodation, protect the eyes (eyes) from light stimuli, or take measures against blue light and liquid crystal lights.
  • the oral composition of the present invention can be ingested regardless of gender or age, and can also be used by sick persons, but it is particularly desirable to ingest it by healthy persons who are concerned about the condition of their eyes. For example, it is desirable for people who use their eyes for a long time to take it on a personal computer, desk work, reading, etc.
  • the oral composition of the present invention can also be used for middle-aged and elderly eye disorders, and maintains the amount of pigment in the yellow spot that decreases with aging, maintains the ability to see that decreases with aging, and reduces the contrast sensitivity of the eye with aging.
  • the form of the oral composition of the present invention includes, for example, capsule preparation, tablet, orally disintegrating tablet, granule, fine granule, round agent, paste-like agent, cream-like agent, caplet-like agent, gel-like agent, chewable form. In addition to supplements, it can be prepared as a normal food or drink in a solid form such as an agent or a liquid form such as a syrup or suspension.
  • a solid dosage form in a capsule formulation is preferable from the viewpoint of administration and flavor.
  • the oral composition of the present invention when used as a capsule preparation, examples thereof include hard capsules, soft capsules, microcapsules, and seamless capsules.
  • the capsule film is preferably composed of one or more of pig skin gelatin, pork bone gelatin, fish gelatin or natural hydrophilic polymer. These capsule coatings can be prepared by well-known and conventional methods.
  • thickening polysaccharides, etc., fats and oils, polyhydric alcohols, surfactants, antioxidants, pigments, fragrances, etc. can be optionally added to the capsule film used for capsule preparations. May contain.
  • the oral composition of the present invention can be contained in one container or divided into a plurality of containers, for example, 2 to 3 for one day in order to adjust the daily intake.
  • the method for producing an oral composition containing lutein and ⁇ -lipoic acid of the present invention includes a step of adding lutein and ⁇ -lipoic acid.
  • lutein and ⁇ -lipoic acid may be contained at the same time or separately. The order in which they are contained separately does not matter.
  • the production of the oral composition of the present invention can further include a heat sterilization step, a container filling step, and the like.
  • composition for improving the flavor of lutein containing ⁇ -lipoic acid A second aspect of the present invention is a composition for improving the flavor of lutein containing ⁇ -lipoic acid.
  • the lutein flavor-improving composition of the present invention contains ⁇ -lipoic acid.
  • the content of ⁇ -lipoic acid is not particularly limited, but from the viewpoint of significantly exerting the effect of the present invention, it is preferably 0. It is 001% by mass or more, more preferably 0.005% by mass or more, further preferably 0.01% by mass or more, particularly preferably 0.05% by mass or more, and most preferably 0.1% by mass or more.
  • the content of ⁇ -lipoic acid is not particularly limited, but from the viewpoint of significantly exerting the effect of the present invention, it is preferably 100% by mass with respect to the total amount of the flavor-improving composition. It may be%, and may contain other components as the case may be.
  • the content of ⁇ -lipoic acid is generally preferably 0.001 to 100% by mass, preferably 0.005 to 100% by mass, based on the total amount of the composition. More preferably, 0.01 to 100% by mass is further preferable, 0.05 to 100% by mass is particularly preferable, and 0.1 to 100% by mass is most preferable.
  • the flavor-improving composition of the present invention can be used in coexistence with an oral composition containing lutein.
  • the amount of ⁇ -lipoic acid may be sufficient as long as it is sufficient for improving the flavor of lutein, but it may also be contained in an amount having a function of adjusting the condition of the eyes, which will be described later.
  • composition for improving the flavor of lutein containing ⁇ -lipoic acid of the present invention can be mainly used as a raw material for the production of foods and drinks, pharmaceuticals, or quasi-drugs in order to coexist with lutein.
  • the form of the flavor improving composition of the present invention is not particularly limited. It may be liquid, solid or semi-solid, and may be tablets, orally disintegrating tablets, capsules, granules, fine granules, rounds, pastes, creams, caplets, gels, chewables. It can be used as a material for preparing a supplement in a solid dosage form such as a pharmaceutical product or in a liquid dosage form such as a syrup and a suspension.
  • Methods for improving the flavor of oral compositions containing lutein are used in an oral composition containing lutein, and comprises adding ⁇ -lipoic acid to the composition.
  • the method for suppressing aggregation of the present invention is used for an oral composition containing ⁇ -lipoic acid, and comprises incorporating lutein in the composition.
  • the present invention is also an oral composition containing ⁇ -lipoic acid, which is used to tone the eyes.
  • ⁇ -lipoic acid which is used to tone the eyes.
  • maintenance of the amount of pigment in the yellow spot of the eye (eye) maintenance of viewing ability, improvement of contrast sensitivity of the eye, improvement of accommodation of the eye, alleviation of eye trouble, It can be used to improve eye condition, relieve eye fatigue, improve accommodation, protect the eye (eye) from light stimulation, or take measures against blue light and liquid crystal light.
  • the oral composition of the present invention can be ingested regardless of gender or age, and can also be used by sick persons, but it is particularly desirable to ingest it by healthy persons who are concerned about the condition of their eyes. For example, it is desirable for people who use their eyes for a long time to take it on a personal computer, desk work, reading, etc.
  • the oral composition of the present invention can also be used for middle-aged and elderly eye disorders, and maintains the amount of pigment in the yellow spot that decreases with aging, maintains the ability to see that decreases with aging, and reduces the contrast sensitivity of the eye with aging.
  • the content of ⁇ -lipoic acid in the oral composition containing ⁇ -lipoic acid of the present invention is generally preferably 0.001% by mass or more, preferably 0.01% by mass, based on the total amount of the composition. % Or more is more preferable, and 0.1% by mass or more is even more preferable. Within this range, a reasonably ingestible amount of oral composition will contain enough ⁇ -lipoic acid to produce the desired effect.
  • the content of ⁇ -lipoic acid in the oral composition is preferably 90% by mass or less, more preferably 50% by mass or less, and even more preferably 40% by mass or less, based on the total amount of the composition. Within this range, it is easy to formulate and relatively easy to take.
  • ⁇ -Lipoic acid may also be in an amount effective for conditioning the eyes.
  • the content of ⁇ -lipoic acid in the oral composition containing ⁇ -lipoic acid of the present invention is generally preferably 0.001 to 90% by mass, preferably 0.01, based on the total amount of the composition. It is more preferably from 50% by mass, and even more preferably from 0.1 to 40% by mass.
  • the content of ⁇ -lipoic acid is preferably 0.001% by mass or more based on the total amount, and is 0. More preferably .005% by mass or more.
  • the content of ⁇ -lipoic acid in the packaged beverage or liquid is preferably 1% by mass or less, more preferably 0.1% by mass or less, based on the total amount of the composition.
  • ⁇ -lipoic acid is contained in an amount of 0.001 to 1% by mass based on the total amount in terms of dry mass. It is preferable, and it is more preferable that it is contained in an amount of 0.005 to 0.1% by mass.
  • the amount of ⁇ -lipoic acid is, for example, preferably 1 mg to 1000 mg, more preferably 5 mg to 800 mg, and further preferably 10 mg to 600 mg per day.
  • the oral composition containing ⁇ -lipoic acid of the present invention may further contain lutein.
  • lutein it is possible to further delay the aging of the eye and maintain the function of the eye.
  • the content of lutein in the oral composition containing ⁇ -lipoic acid of the present invention is generally preferably 0.01% by mass or more, preferably 0.1% by mass or more, based on the total amount of the composition. More preferably, 1% by mass or more is even more preferable. Within this range, a reasonably ingestible amount of oral composition will contain lutein sufficient to produce the desired effect.
  • the content of lutein in the oral composition is preferably 30% by mass or less, more preferably 20% by mass or less, still more preferably 10% by mass or less, based on the total amount of the composition. Within this range, it is easy to formulate and relatively easy to take.
  • the content of lutein in the oral composition containing ⁇ -lipoic acid of the present invention is generally preferably 0.01 to 30% by mass, preferably 0.1 to 20% by mass, based on the total amount of the composition. % Is more preferable, and 1 to 10% by mass is even more preferable.
  • the content of lutein is preferably 0.001% by mass or more, preferably 0.003% by mass, based on the total amount. % Or more is more preferable.
  • the content of lutein in the packaged beverage or liquid is preferably 0.1% by mass or less, more preferably 0.025% by mass or less, based on the total amount of the composition.
  • the oral composition containing lutein and ⁇ -lipoic acid of the present invention is a packaged beverage or a liquid preparation
  • lutein is contained in an amount of 0.001 to 0.1% by mass based on the total amount in terms of dry mass. It is more preferable that the content is 0.003 to 0.025% by mass.
  • Lutein should also be an effective amount to tone the eyes. For example, 0.1 mg to 50 mg, more preferably 1 mg to 30 mg, and even more preferably 6 mg to 25 mg per day can be contained.
  • the content of ⁇ -lipoic acid with respect to 1 part by mass of lutein is not particularly limited, but from the viewpoint of significantly exerting the effect of the present invention. It is preferably 0.01 to 100 parts by mass, more preferably 0.05 to 50 parts by mass, still more preferably 0.1 to 10 parts by mass, and particularly preferably 0.5 to 5 parts by mass.
  • a third aspect of the present invention relates to an oral composition containing lutein and seaberry.
  • the content of lutein in the oral composition containing lutein and seaberry of the present invention is generally preferably 0.01% by mass or more, more preferably 0.1% by mass or more, based on the total amount of the composition. Preferably, 1% by mass or more is even more preferable. Within this range, a reasonably ingestible amount of oral composition will contain lutein sufficient to produce the desired effect.
  • the content of lutein in the oral composition is preferably 30% by mass or less, more preferably 20% by mass or less, still more preferably 10% by mass or less, based on the total amount of the composition. Within this range, it is easy to formulate and relatively easy to take.
  • the content of lutein in the oral composition containing lutein and seaberry of the present invention is generally preferably 0.01 to 30% by mass, preferably 0.1 to 20% by mass, based on the total amount of the composition. Is more preferable, and 1 to 10% by mass is even more preferable.
  • the content of lutein is preferably 0.001% by mass or more, preferably 0.003% by mass, based on the total amount. The above is more preferable.
  • the content of lutein in the packaged beverage or liquid is preferably 0.1% by mass or less, more preferably 0.025% by mass or less, based on the total amount of the composition.
  • lutein When the oral composition containing lutein and seaberry of the present invention is a packaged beverage or a liquid preparation, lutein may be contained in an amount of 0.001 to 0.1% by mass based on the total amount in terms of dry mass. More preferably, it is further preferably contained in an amount of 0.003 to 0.025% by mass.
  • Lutein should also be an effective amount to tone the eyes. For example, 0.1 mg to 50 mg, more preferably 1 mg to 30 mg, and even more preferably 6 mg to 25 mg per day.
  • Seaberry used in the oral composition of the present invention is also called sea buckthorn and is a plant of the family Elaeagnaceae.
  • the sea berry is not particularly limited, but includes a crushed sea berry product, a sea berry extract and the like.
  • the sea berries are derived from fruits including pericarp, pulp and seeds.
  • Seaberry can be at least one selected from the group consisting of Hippophae rhhamnoides Leikora and Hippophae rhhamnoides Havego.
  • the term "seaberry extract” is not limited as long as it is derived from a natural product component, but in the present specification, it is a concept including oil obtained from the fruit of seaberry of a plant, and is an oil. It preferably contains a soluble component.
  • a commercially available product such as seaberry fruit oil (oriza oiling) can also be used.
  • the oil obtained from the seaberry fruit can be obtained by squeezing the crushed fruit as it is, filtering the crude oil obtained by centrifugation, and then vacuum drying.
  • the seaberry extract is also a concept that includes a product obtained by extracting seaberry fruits and fruit juice.
  • seaberry extract P oriza oiling
  • seaberry extract-WSP oriza oiling
  • seaberry extract J oriza
  • Commercial products such as oiling) and seaberry extract oil (manufactured by Puredia) can also be used.
  • the obtained product obtained by extracting the seaberry fruit is obtained by extracting the crushed dried fruit with a solvent (for example, hydrous ethanol, water, hexane, etc.) in an amount several times the weight thereof at about room temperature, and solid-liquid. It can also be obtained separately.
  • a solvent for example, hydrous ethanol, water, hexane, etc.
  • the form of "sea berry” may be any of liquid, emulsion, paste, solid and powder.
  • Seaberry oil is rich in fatty acids.
  • fatty acids include palmitoleic acid, palmitic acid, oleic acid, linoleic acid, ⁇ -linolenic acid, and stearic acid.
  • the content of palmitoleic acid is preferably 10 to 60% by mass, more preferably 15 to 55% by mass, further preferably 20 to 50% by mass, particularly preferably 25 to 45% by mass, and 30 to 40% by mass. % Is the most preferable.
  • the content of palmitic acid is preferably 10 to 60% by mass, more preferably 15 to 55% by mass, further preferably 20 to 50% by mass, particularly preferably 25 to 45% by mass, and particularly preferably 30 to 40% by mass. % Is the most preferable.
  • the content of oleic acid is preferably 5 to 55% by mass, more preferably 10 to 50% by mass, further preferably 15 to 45% by mass, particularly preferably 20 to 40% by mass, and 25 to 35% by mass. % Is the most preferable.
  • the content ratio of palmitoleic acid, palmitic acid and oleic acid is not particularly limited as long as the effect of the present invention is obtained, but the mass ratio is, for example, 1: 0.5 to 2: 0. It is preferably 2 to 2, more preferably 1: 0.8 to 1.5: 0.5 to 1.5, and more preferably 1: 0.8 to 1.2: 0.5 to 1.2. Is more preferable.
  • the content of seaberries (including seaberry extract) in the oral composition containing lutein and seaberry of the present invention may vary depending on the form of the oral composition. Generally, in terms of dry weight, 0.01% by mass or more is preferable, 0.05% by mass or more is more preferable, and 0.1% by mass or more is even more preferable with respect to the total amount of the composition. Within this range, a reasonably ingestible amount of the oral composition will contain a seaberry extract sufficient to produce the desired effect.
  • the content of ⁇ -lipoic acid in the oral composition is preferably 50% by mass or less, more preferably 30% by mass or less, and 10% by mass or less, based on the total amount of the composition in terms of dry weight. Is even more preferable. Within this range, it is easy to formulate and relatively easy to take.
  • the seaberry extract is preferably 0.005% by mass or more, more preferably 0.02% by mass or more, further preferably 0.07% by mass or more, and 0.15% by mass or more, based on the total amount of the composition. Even more preferable. Within this range, a reasonably ingestible amount of oral composition will contain enough seaberries to produce the desired effect.
  • the content of the seaberry extract in the oral composition is preferably 40% by mass or less, more preferably 20% by mass or less, and more preferably 15% by mass or less, based on the total amount of the composition in terms of dry weight. Even more preferable. Within this range, it is easy to formulate and relatively easy to take.
  • seaberry those obtained as "seaberry oil” can also be used, and 0.005% by mass or more is preferable, 0.02% by mass or more is more preferable, and 0.07% by mass is based on the total amount of the composition. % Or more is even more preferable, and 0.15% by mass or more is even more preferable. Within this range, a reasonably ingestible amount of oral composition will contain enough seaberries to produce the desired effect.
  • the content of seaberry oil in the oral composition is preferably 40% by mass or less, more preferably 20% by mass or less, and further preferably 15% by mass or less, based on the total amount of the composition in terms of dry weight. More preferred. Within this range, it is easy to formulate and relatively easy to take.
  • the content of seaberry in the oral composition containing lutein and seaberry of the present invention is generally preferably 0.01 to 50% by mass based on the total amount of the composition in terms of dry weight. 0.05 to 30% by mass is more preferable, and 0.1 to 10% by mass is even more preferable.
  • the content of the seaberry extract in the oral composition containing lutein and seaberry of the present invention is generally 0.005 to 40% by mass based on the total amount of the composition in terms of dry weight.
  • 0.02 to 15% by mass is more preferable, 0.07 to 10% by mass is further preferable, and 0.15 to 5% by mass is even more preferable.
  • the content of seaberry oil in the oral composition containing lutein and seaberry of the present invention is generally preferably 0.005 to 40% by mass based on the total amount of the composition in terms of dry weight. , 0.02 to 15% by mass is more preferable, 0.07 to 10% by mass is further preferable, and 0.15 to 5% by mass is even more preferable.
  • the content of seaberry is 0.0001% by mass or more based on the total amount in terms of dry weight. Preferably, it is 0.0002% by mass or more, more preferably 0.001% by mass or more.
  • the content of seaberries in the packaged beverage or liquid is preferably 10% by mass or less, more preferably 5% by mass or less, and 1% by mass or less, based on the total amount of the composition in terms of dry weight. More preferred.
  • the content of the seaberry extract is preferably 0.00005% by mass or more, preferably 0.0001% by mass, based on the total amount. % Or more is more preferable, and 0.0005% by mass or more is further preferable.
  • the content of seaberries in the packaged beverage or liquid is preferably 10% by mass or less, more preferably 5% by mass or less, and 1% by mass or less, based on the total amount of the composition in terms of dry weight. More preferred.
  • the content of seaberry oil is preferably 0.00005% by mass or more, preferably 0.0001% by mass, based on the total amount.
  • the above is more preferable, and 0.0005% by mass or more is further preferable.
  • the content of seaberries in the packaged beverage or liquid is preferably 10% by mass or less, more preferably 5% by mass or less, and 1% by mass or less, based on the total amount of the composition in terms of dry weight. More preferred.
  • the amount of seaberry may be sufficient as long as it is sufficient for improving the flavor of lutein, but it may also be contained in an amount that also has the function of adjusting the tone of the eyes, which will be described later.
  • 0.1 mg to 200 mg more preferably 0.5 mg to 100 mg, and even more preferably 1 mg to 10 mg per day.
  • the amount of seaberry may be sufficient as long as it is sufficient for improving the flavor of lutein, but it may also be contained in an amount that also has the function of adjusting the tone of the eyes, which will be described later.
  • the seaberry extract is preferably 0.1 mg to 200 mg, more preferably 0.5 mg to 100 mg, and even more preferably 1 mg to 10 mg per day.
  • the amount of seaberry may be sufficient as long as it is sufficient for improving the flavor of lutein, but it may also be contained in an amount that also has the function of adjusting the tone of the eyes, which will be described later.
  • the amount of seaberry oil per day is preferably 0.1 mg to 200 mg, more preferably 0.5 mg to 100 mg, and even more preferably 1 mg to 10 mg.
  • the content of seaberry with respect to 1 part by mass of lutein is not particularly limited, but from the viewpoint of significantly improving the flavor of lutein and suppressing the aggregation of ⁇ -lipoic acid.
  • Dry mass equivalent or as seaberry oil usually 0.01 to 100 parts by mass, preferably 0.1 to 100 parts by mass, more preferably 0.1 to 50 parts by mass, still more preferably 0.1 to 10 parts by mass. , Particularly preferably 0.5 to 5 parts by mass.
  • oral composition containing lutein and seaberry of the present invention are all described in the above section [Oral composition containing lutein and ⁇ -lipoic acid].
  • the present invention also includes the following aspects. (1) Maintaining the amount of pigment in the yellow spot of the eye (eye), maintaining the ability to see, improving the contrast sensitivity of the eye, improving the focus adjustment of the eye, alleviating eye troubles, improving the condition of the eye, alleviating the feeling of fatigue of the eye, adjusting Use of ⁇ -lipoic acid to improve deficiency, protect the eyes from light irritation, or produce oral compositions for blue light or liquid crystal light control or symptom relief.
  • Example 1 Flavor improving effect of lutein The taste improving effect of lutein was evaluated.
  • the oral compositions of Example 1 and Comparative Example 1 shown in Table 1 were mixed and prepared.
  • Five taste judges evaluated the taste felt immediately after taking about 50 mg of each oral composition with a spatula.
  • the taste score was evaluated on a scale of 0 to 15 with "I can't take it” as 15 and "I can take it” as 0, and the average of the values of 5 people was taken.
  • which of the oral compositions of Examples and Comparative Examples was evaluated was evaluated so that the judge could not recognize it.
  • the recognition of numerical values was standardized among the judges according to the following criteria.
  • Test results The test results are shown in Table 2.
  • Example 2 Effect of lutein on agglutination of ⁇ -lipoic acid After collecting 10 mg each of the oral compositions of Example 2 and Comparative Example 2 shown in Table 3, fill a glass bottle (screw cap) with a capacity of 30 mL and add 10 mL of safflower oil to disperse. I let you. Centrifugation (3100 rpm; 10 minutes) was performed using a cooling centrifuge (EX-126: manufactured by Tomy Seiko Co., Ltd.), and 1 mL each of the supernatants before and after the centrifugation was collected. Further, each sample was diluted to a measurable concentration, and the content of ⁇ -lipoic acid was measured by HPLC.
  • EX-126 manufactured by Tomy Seiko Co., Ltd.
  • Test results The test results are also shown in Table 3.
  • Example 3 The effect of ⁇ -lipoic acid on alleviating eye disorders was evaluated. The effect of ⁇ -lipoic acid on alleviating eye disorders was evaluated.
  • the oral compositions of Example 3 and Reference Examples shown in Table 4 were mixed to prepare soft capsules. These were taken once a day for 4 weeks, and the change value of short-distance visual acuity (average of 8 people) and the change value of near point (average of 4 people) after and before taking were evaluated.
  • the short-distance visual acuity is measured using the Hiragana Universal Near-Point Inspection Table (Short-distance Visual Acuity Table) (Handa-ya Shoten), and the short-distance visual acuity is judged from the size of characters that the subject can read at a distance of 30 cm. did.
  • the near point was measured using Triiris C9000 (Hamamatsu Photonics Co., Ltd.), and the position where the optotype appeared blurry to the subject was recorded as the near point. In all the measurements, the subjects were subjected to a visual acuity test in advance and the visual acuity was corrected.
  • the mass% ratio of cyclodextrin to ⁇ -lipoic acid in the R- ⁇ -lipoic acid-CD clathrate used is 88.5: 11.5.
  • Table 4 shows the results of short-distance visual acuity and perigee change values. From this result, it was found that ⁇ -lipoic acid improves short-distance visual acuity and is useful for focus adjustment.
  • Example 4 Flavor improving effect of lutein The taste improving effect of lutein was evaluated.
  • the oral compositions of Example 5 and Comparative Example 3 shown in Table 6 were mixed and prepared.
  • Five taste judges evaluated the taste felt immediately after taking about 50 mg of each oral composition with a spatula.
  • the taste score was evaluated on a scale of 0 to 15 with "I can't take it” as 15 and "I can take it” as 0, and the average of the values of 5 people was taken. That is, in the grade evaluation from 0 to 15, the recognition of numerical values was standardized among the judges according to the following criteria. The numerical value indicates that the larger the value, the stronger the unpleasant flavor is felt, and the greater the degree of difficulty in taking the drug.
  • palmitoleic acid was 30.1% by mass
  • palmitic acid was 30% by mass
  • oleic acid was 28.6% by mass
  • linoleic acid was 2.8% by mass
  • ⁇ -linolenic acid was 1.00% by mass
  • Stearic acid was 0.6% by mass.
  • the following is a pharmaceutical example of an oral composition containing lutein and ⁇ -lipoic acid, lutein and seaberry, or ⁇ -lipoic acid of the present invention. All of these maintain the amount of pigment in the yellow spots of the eye (eye), maintain the ability to see, improve the contrast sensitivity of the eye, improve the focus adjustment of the eye, alleviate eye troubles, improve the condition of the eye, and alleviate the feeling of fatigue of the eye. It can be used as an oral composition for improving accommodation, protecting the eyes (eyes) from light stimuli, or taking measures against blue light and liquid crystal light.
  • maintenance of the amount of pigment in the yellow spot that decreases with aging maintenance of viewing power that decreases with aging, improvement of decrease in contrast sensitivity of the eye due to aging, improvement of decrease in focus adjustment function of the eye due to aging, eye due to aging It can be used as an oral composition for alleviating the worries of aging, improving the condition of the eyes due to aging, alleviating the feeling of fatigue of the eyes due to aging, or improving dysregulation due to aging. It is also desirable for those who have difficulty seeing small letters and things, those who have difficulty seeing the letters and things at hand, those who have difficulty seeing in dimly lit places, and those who take time to focus on things at different distances.
  • the powdered beverage means a powder for dissolving 3 g in 100 to 200 ml.

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PCT/JP2020/044249 2019-11-29 2020-11-27 経口組成物 WO2021107106A1 (ja)

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Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050112210A1 (en) * 2003-09-12 2005-05-26 Terry Grossman Eye nutritional supplement
US20070082064A1 (en) * 2005-10-12 2007-04-12 Krawitz Paul L Nutritional or dietary supplement for the treatment of macular degeneration
JP2007529450A (ja) * 2004-03-19 2007-10-25 ネステク ソシエテ アノニム 機能性成分の送達
US20080181972A1 (en) * 2007-01-29 2008-07-31 Valentina Amico Compositions and Methods for Maintaining, Strengthening, Improving, or Promoting Eye Health
US20090252796A1 (en) * 2008-04-07 2009-10-08 Mazed Mohammad A Nutritional supplement for the prevention of cardiovascular disease, alzheimer's disease, diabetes, and regulation and reduction of blood sugar and insulin resistance
CN101670019A (zh) * 2008-09-11 2010-03-17 郑侠慧 一种具有抗辐射和保护视力功能的复合制剂
CN101843784A (zh) * 2010-02-08 2010-09-29 崔晓廷 一种强效保护视力的多维叶黄素制剂
CN104824644A (zh) * 2015-05-13 2015-08-12 宁波北仑戌鸿农业科技有限公司 适合保护视力的食品
WO2019168185A1 (ja) * 2018-03-02 2019-09-06 ロート製薬株式会社 後眼部異常の予防及び/又はリスク軽減用食品組成物

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050112210A1 (en) * 2003-09-12 2005-05-26 Terry Grossman Eye nutritional supplement
JP2007529450A (ja) * 2004-03-19 2007-10-25 ネステク ソシエテ アノニム 機能性成分の送達
US20070082064A1 (en) * 2005-10-12 2007-04-12 Krawitz Paul L Nutritional or dietary supplement for the treatment of macular degeneration
US20080181972A1 (en) * 2007-01-29 2008-07-31 Valentina Amico Compositions and Methods for Maintaining, Strengthening, Improving, or Promoting Eye Health
US20090252796A1 (en) * 2008-04-07 2009-10-08 Mazed Mohammad A Nutritional supplement for the prevention of cardiovascular disease, alzheimer's disease, diabetes, and regulation and reduction of blood sugar and insulin resistance
CN101670019A (zh) * 2008-09-11 2010-03-17 郑侠慧 一种具有抗辐射和保护视力功能的复合制剂
CN101843784A (zh) * 2010-02-08 2010-09-29 崔晓廷 一种强效保护视力的多维叶黄素制剂
CN104824644A (zh) * 2015-05-13 2015-08-12 宁波北仑戌鸿农业科技有限公司 适合保护视力的食品
WO2019168185A1 (ja) * 2018-03-02 2019-09-06 ロート製薬株式会社 後眼部異常の予防及び/又はリスク軽減用食品組成物

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