Pore-cleansing agent

Abstract

To provide a naturally derived and highly safe oral pore-shrinking agent (material) and the like that can shrink pores and can be taken orally continuously, in humans and the like.SOLUTION: Provided is an oral pore-shrinking agent containing ceramide (for example, ceramide derived from rice).SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an orally ingestible pore minimizing agent of natural origin that is highly safe and can reduce pores in humans and the like and is also suitable for continuous oral ingestion.

Background Art

[0002] In recent years, particularly among young women, concerns about the visibility of pores have been increasing, and there is a demand for skin external preparations that improve this visibility. As a method for improving the visibility of pores, measures such as astringent lotions and removal of comedones have become common. Alternatively, makeup foundations are often used to improve the appearance. However, for example, astringent lotions are intended to tighten the skin and act by temporarily lowering the skin surface temperature with alcohol or coagulating proteins with organic acids or the like. Therefore, the burden on the skin is large, and it does not provide a fundamental solution to the visibility of pores, and the effect is not sufficient.

[0003] Due to these reasons, there is a demand for an orally ingestible pore minimizing agent of natural origin that is highly safe and can be continuously orally ingested in humans, for example (Patent Document 1).

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Patent Document 3

Patent Document 4

Patent Document 5

Patent Document 6

Summary of the Invention

[0005] The present invention aims to provide a naturally derived, highly safe oral pore-reducing agent (material) that can reduce pore size in humans and other organisms, and that can be taken orally on a continuous basis. [Means for solving the problem]

[0006] This invention was made to solve the above problems, and the inventors invented this invention as a result of exploring the effects of an extract (containing ceramide) extracted from rice seeds with ethanol.

[0007] The present invention includes the following embodiments. (1) An orally administered pore-reducing agent containing ceramide (for example, ceramide derived from rice). (2) A method for producing an oral pore-reducing agent, comprising the step of extracting rice seeds with ethanol. (3) An oral composition containing the agent described in (1) or the agent manufactured by the manufacturing method of (2). [Effects of the Invention]

[0008] The agents of the present invention can, for example, be used by oral ingestion to reduce pore size in humans and other organisms. [Modes for carrying out the invention]

[0009] The present invention will be described in reference to embodiments.

[0010] (derived from) In the specification of this application, the phrase "derived from" is used with the intention of encompassing (1) to (3) below. (1) It is purified, (2) Being isolated, and / or (3) Modification [this includes low molecular weight treatment and high molecular weight treatment (polymerization)] or alteration

[0011] (Ceramide) Ceramides have a structure in which a fatty acid is bound to sphingosine, a long-chain base. Keratinocytes in the later stages of differentiation (granular layer) synthesize various ceramides, and the diversity of these molecules is due to the diversity of hydroxylation (non-hydroxy, 2-hydroxy, and terminal ω-hydroxy) of the fatty acid and sphingosine base that constitute ceramide. In addition to the diversity of hydroxylation, there is also diversity in the chain length of the fatty acid and sphingosine base. These ceramides are found in living organisms in addition to the skin, in the blood, brain, spinal cord, and nerve tissue, and in plants they are found in pineapple, peach, konjac, wheat, rice, soybean, millet, spinach, mushrooms, etc. (Patent Document 2). In the present invention, ceramide includes, for example, glucosylceramide (a type of sphingoglycolipid in which ceramide is bound to glucose).

[0012] Methods for extracting ceramides from plant materials include, for example, extracting them from plant materials such as seeds of pineapple, peach, konjac, yuzu, grapes, and cherries, wheat, rice, and soybeans using an alcohol-based solvent (e.g., ethanol) (Patent Document 3), and extracting them from plant materials such as wheat, soybeans, corn, and rice bran after hydrolysis with an alkaline ethanol solvent using a mixed solvent of hexane, acetone, and water (e.g., Patent Documents 4 and 5). Plant-derived ceramides have the advantage of being gentle on the body and less likely to cause irritation when incorporated into cosmetics and supplements because they are plant-derived, but their structure is subtly different from ceramides found in human skin.

[0013] Methods for extracting glucosylceramide from plant materials include, for example, extraction by the method described in Japanese Patent Publication No. 2001-097983, or by using commercially available rice-derived glucosylceramide (e.g., from Nagara Science Co., Ltd.).

[0014] (Rice and rice-derived extracts) Rice refers to the annual plant Oryza sativa (Oryza sativa LINNE), Oryza glaberrima, and their hybrids, which are cultivated varieties of the genus Oryza. The rice used in this invention may be Japonica, Javanica, or Indica varieties, and may be non-glutinous rice, glutinous rice, sake rice, or feed rice. The rice variety used in this invention is not particularly limited and is not limited to any variety that is commonly cultivated as a crop. The rice used in this invention may be rice bred using hybrid technology. Rice bred using hybrid technology is a first-generation hybrid obtained by crossing two different strains of rice varieties, and generally possesses hybrid vigor (generally resulting in increased yield potential, improved resistance to biological and abiotic stressors, etc.) which is superior to either of the parents. In this invention, to produce ceramide (a ceramide-containing agent), it is preferable to use rice seeds, taking into consideration the ceramide content.

[0015] For obtaining rice-derived extracts, organic solvents such as water, alcohols (e.g., anhydrous ethanol, ethanol, propylene glycol, 1,3-butylene glycol, etc.), ketones such as acetone, and esters such as diethyl ether, dioxane, and ethyl acetate can be used individually or in combination of two or more solvents. The solvent extracts can also be used in their combined state. However, the use of hexane as a solvent is undesirable because it may result in the inclusion of other lipid-soluble components such as ceramides in the extract. Ethanol is preferably used. The amount of solvent used is 1 to 100 parts by weight, preferably 10 to 100 parts by weight, per 1 part by weight of the plant material for extraction.

[0016] Alternatively, alkaline organic solvents can be used by adding potassium hydroxide, sodium hydroxide, etc., to these alcohol-based solvents to make them alkaline. The lower limit of the alkali concentration is preferably 0.01 N, and more preferably 0.1 N. The upper limit of the alkali concentration is preferably 1 N, more preferably 0.5 N, and even more preferably 0.4 N.

[0017] The extraction method is not particularly limited, but usually, it may be within the boiling point range of the solvent at normal temperature and normal pressure, and filtration may be performed after extraction. Ordinary means generally applied in the extraction process may be arbitrarily selected and carried out.

[0018] The extract derived from rice used in the present invention can be produced, for example, by the production method of Production Example 1 below. The extract derived from rice described in the following examples is the extract derived from rice produced by Production Example 1 below.

[0019] (Production Example 1) Production method of extract derived from rice 881 g of seeds of Oryza sativa Linne (Gramineae) are added with 0.2N potassium hydroxide-ethanol for extraction. The extract is purified by a silica gel column, neutralized, and desalted, and the purified solution is concentrated to obtain 20 g of a rice extract. 800 g of an excipient (dextrin) is added to 200 g of the rice extract and dried to obtain 1000 g of a white to pale yellow powder.

[0020] (Recommended intake) The daily intake (in the case of intake in an oral composition) of the extract derived from rice used in the present invention can be appropriately adjusted depending on the intake form, purpose of use, age, body weight, etc. However, in order to exert the desired effect (such as shrinking pores), for adult humans per day, in terms of the dry matter of the extract derived from rice, preferably 20 mg / day or more, more preferably 40 mg / day or more, still more preferably 60 mg / day or more, and from the viewpoint of safety in humans, etc. during such intake, preferably 480 mg / day or less, more preferably 360 mg / day or less, still more preferably 180 mg / day or less.

[0021] (Form of oral intake pore shrinking agent) The form of the agent (material for shrinking pores) according to the present invention is not particularly limited, and examples include a liquid form, a solid form, a powder form, etc.

[0022] (Oral composition) The oral compositions according to the present invention include, for example, foods and beverages (including functional foods, foods for specified health uses, supplements, etc.), pharmaceuticals, and the like.

[0023] For example, if the oral composition is a food or beverage, the form of the food or beverage may include various foods and beverages such as bread, cakes, noodles, confectionery, jellies, frozen foods, ice cream, dairy products, and beverages, as well as forms similar to those of the oral administration preparations described above (tablets, capsules, syrups, etc.). Foods in various forms can be prepared by using the active ingredient of the present invention alone, or by combining it with other food ingredients, solvents, softeners, oils, emulsifiers, preservatives, flavorings, stabilizers, colorants, antioxidants, humectants, thickeners, etc., as appropriate.

[0024] For example, if the oral composition is a pharmaceutical, it is generally easy to assemble a convenient daily dosing regimen that can be adjusted according to the degree of discomfort, but the form of the pharmaceutical may be, for example, a solid or a liquid. Examples of the solid form include powders, tablets, pills, capsules, cachets, lozenges, suppositories, and dispersible granules. For example, in the case of a powder, the carrier is generally a finely ground solid that is a mixture with the finely ground active ingredient. For example, in the case of a tablet, the active ingredient is generally mixed in an appropriate proportion with a carrier having the required binding ability and molded into the desired shape and size. Suitable carriers may, but are not limited to, magnesium carbonate, magnesium stearate, talc, sugars, lactose, pectin, dextrin, starch, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose, low-melting-point waxes, cocoa butter, etc. The pharmaceutical product may also contain, as necessary, excipients, stabilizers, preservatives, binders, disintegrants, hydrocarbons, fatty acids, alcohols, esters, pH adjusters, antiseptics, etc., to the extent that it does not impair the desired effect.

[0025] (pores) Pores, whose openings to the skin surface widen with age, are characterized by a reduction in the protruding edges of the uneven structure of the skin surface, resulting in a mortar-shaped, sloping surface from the edge of the opening to the center bottom. There is no specific age at which this occurs; rather, individuals may notice that their pores have become more noticeable with age. Pores vary from person to person, and aging, in particular, can cause the openings to widen on the skin surface, resulting in a mortar-shaped appearance, with a longer sloping surface and a wider bottom (Patent Document 6).

[0026] Facial pores are present in everyone, but how they appear, and whether or not people are concerned about them, varies greatly from person to person. However, for women, for example, noticeable pores are not seen as a positive thing, but rather as a negative, and there is a demand for effective makeup methods that make pores less visible (Patent Document 6).

[0027] As mentioned above, the visibility of pores varies from person to person, but one of the contributing factors is aging. Generally, with age, the opening of the pore on the skin surface tends to widen morphologically, and this is one of the reasons why pores become more noticeable with age. In younger people, the pore morphology is thought to consist of relatively cylindrical depressions that occur independently, but with age, the opening of the opening diminishes the edges of the convex structure in the uneven structure of the skin surface, resulting in the depressions becoming more noticeable. Morphologically comparing the pores of both age groups, in younger people, the skin surface is described as having a "fine texture," and the pores themselves tend to be small and inconspicuous, or if present, they tend to be vertically cylindrical. In contrast, with age, the opening of the pore on the skin surface widens, and it is thought that it takes on a slope towards the bottom center, like the slope of a mortar. Thus, since the morphology of pores differs with age, there is no single method for simply concealing pores, and the appropriate makeup methods for this also differ (Patent Document 6).

[0028] The present invention will now be described in more detail with reference to examples, but the present invention is not limited in any way to these examples. In the following examples, the unit % indicating the content of components contained in the agent of the present invention means mass %. [Examples]

[0029] The following describes embodiments of the present invention.

[0030] [Test 1: Confirmation of the components of the agent used in Test 2 (containing rice-derived extract)] The content of a predetermined glucosylceramide in a preparation containing rice-derived extract prepared according to the above-described manufacturing example 1 was measured. The composition of the preparation (powder) is 20% rice-derived extract and 80% dextrin.

[0031] Approximately 50 mg of the agent was accurately weighed, dissolved in 3 mL of water, and then 17 mL of methanol was gradually added while stirring. Chloroform was added to this solution to make exactly 50 mL, and the solution was filtered through a membrane filter (pore size 0.45 μm) to obtain the filtrate as the test solution. Separately, 6 mg of rice-derived glucosylceramide (Nagara Science) was precisely weighed, dissolved in a chloroform / methanol mixture (2:1), and the total volume was made exactly 50 mL to prepare the standard solution. 3 μL of the test solution and 1, 2, 3, 4, and 5 μL of the standard solutions were measured, and liquid chromatography was performed under the following operating conditions. Next, the peak area of ​​glucosylceramide in each standard solution was measured, and a calibration curve was created. The concentration of glucosylceramide in the test solution was determined from the calibration curve, and the glucosylceramide content in the product was measured.

[0032] Measurements taken under the following conditions confirmed that the agent contains 10.0% or more glucosylceramide.

[0033] Operating conditions: • Detector: Light scattering detector • Column packing material: 2.2 μm silica gel for liquid chromatography • Column tube: Stainless steel tube with an inner diameter of 3.0 mm and a length of 75 mm. • Column temperature: Constant temperature around 35°C ·Mobile phase 0 min → 5 min Chloroform / 95 vol% methanol solution mixture (99:1) → (75:25) 5 minutes → 6.5 minutes Chloroform / 95 vol% methanol solution mixture (75:25) → (10:90) 6.5 min → 8 min Chloroform / 95 vol% methanol solution mixture (10:90) → (99:1) ·Flow rate: 0.8mL / min

[0034] [Study 2: Human Monitor Study] The study was conducted between April 5, 2021 and April 20, 2021, with 10 healthy male and female subjects aged 30 to 50.

[0035] An oral composition (capsule) was prepared for use in this experiment 2. The composition of this capsule, per daily dose, is shown in Table 1 below.

[0036] [Table 1]

[0037] The subjects took the capsules listed in Table 1 once a day between meals. Skin analysis was performed using the ANTERA3D skin analyzer on day 0 (before intake), day 3 (3 days after the start of intake), day 7 (7 days after the start of intake), and day 14 (14 days after the start of intake). TM Using this method, the following parameters were measured on the face (both cheeks): total volume of pore openings, total pore area, and depth of the deepest part of the pores. The measurement results (numerical values) are shown in Table 2. The total volume of pore openings (cubic millimeters) is the total volume of rough areas related to pores in the selected area. The total pore area (square millimeters) is the total area of ​​the measurement target. The depth of the deepest part of the pores (millimeters) is the maximum depth of the pores in the area selected for measurement.

[0038] The values ​​listed in Table 2 were calculated as follows: First, measurements were taken of the relevant item for 10 individuals (both cheeks). After these measurements, for each of the 10 individuals, the value on day 0 was set to 100, and the values ​​on days 3, 7, and 14 were calculated as relative values. After calculating these relative values, the average of the values ​​on days 3, 7, and 14 was calculated. These average values ​​are listed in Table 2. Table 2 shows the significant difference for each measurement item compared to the mean value on day 0 (significant difference by Dunnett's test, * indicates p<0.01, ** indicates p<0.05).

[0039] [Table 2]

[0040] The results shown in Table 2 (results in which a decrease in values ​​over time was confirmed for each measurement item) indicate that pore reduction was confirmed by taking the capsules listed in Table 1.

[0041] Although embodiments of the present invention (including examples) have been described above with reference to the drawings, the specific configuration of the present invention is not limited thereto, and any design changes, etc., that do not depart from the spirit of the present invention are still included. [Industrial applicability]

[0042] The present invention provides a naturally derived, highly safe oral pore-reducing agent (material) that can reduce pore size in humans and other organisms, and is also suitable for continuous oral intake.

Claims

1. A method for producing an oral composition for pore reduction containing ceramide, The oral composition comprises an extract derived from rice and dextrin. The method for producing the rice-derived extract is as follows: The process includes extracting ceramide from the seeds of rice Oryza Sativa Linne (Gramineae) using a solvent. The solvent is ethanol containing 0.01 N to 1 N potassium hydroxide. A method for producing the oral composition for pore reduction.

2. The manufacturing method according to claim 1, wherein the solvent is solely ethanol containing 0.1 N to 0.5 N potassium hydroxide.

3. The manufacturing method according to claim 1 or 2, wherein the amount of solvent used is 1 to 100 parts by weight per 1 part by weight of the rice seeds.

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