Active ingredient retention agent

Abstract

The purpose of the present invention is to provide a novel means capable of enhancing and / or maintaining the effect of an active ingredient for a long period of time. Provided is a retention agent for retaining an active ingredient, the retention agent comprising an oil-in-water emulsion containing water, a hydrophobic substance, a cyclodextrin, and a polysaccharide tackifier.

Description

Technical Field

[0001] The present invention relates to a retention agent for retaining an active ingredient, which comprises: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide. Background Art

[0002] Currently, an emulsified composition containing oil, water, cyclodextrin, and a water-soluble gelling agent is widely used in various fields such as pharmaceuticals, cosmetics, food and beverages.

[0003] Patent Document 1 discloses an emulsified composition containing water, an oily component, α-cyclodextrin, and any one or more of agar, low-strength agar, galactomannan or glucomannan combined with xanthan gum, carrageenan, furcellaran, gellan gum, and natural gellan gum as a gel-forming component, and also discloses pharmaceuticals, cosmetics, and chemical products using the same.

[0004] Patent Document 2 discloses an emulsified composition characterized by containing oil, a proteolysate, water, cyclodextrin, etc. In addition, it is disclosed that gums such as xanthan gum, guar gum, gum arabic CMC, carrageenan, and locust bean gum can be used as stabilizers.

[0005] Patent Document 3 discloses an emulsified cosmetic which is obtained by mixing an aqueous raw material in which a water-soluble polymer compound such as pectin, tragacanth gum, gelatin, casein, sodium alginate, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, sodium polyacrylate, and carboxyvinyl polymer is dissolved with an oily raw material for cosmetics, and adding cyclodextrin to emulsify it.

[0006] Patent Document 4 discloses a skin emulsified composition which comprises water, oil, cyclodextrin, and at least one water-soluble gelling agent selected from the group consisting of carboxymethyl cellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind polysaccharide gum, and gellan gum.

[0007] Non-Patent Document 1 records that xanthan gum and tragacanth gum are respectively added as emulsification stabilizers to an oil-in-water droplet type emulsion obtained by emulsifying a 1:1 volume ratio sample of soybean oil and cyclodextrin aqueous solution, and as a result, the emulsification stability increases.

[0008] Prior Art Documents

[0009] Patent Documents

[0010] Patent Document 1: Japanese Patent Application Laid-Open No. 2016-204311

[0011] Patent Document 2: Japanese Patent Application Laid-Open No. 10-262560

[0012] Patent Document 3: Japanese Patent Publication No. 61-038166

[0013] Patent Document 4: WO2022 / 064997 Gazette

[0014] Non-Patent Literature

[0015] Non-Patent Literature 1: Nippon Shokuhin Kogyo Gakkaishi, Vol. 38, No. 1, 16 - 20 (1991) Summary of the Invention

[0016] Problems to be Solved by the Invention

[0017] In the fields of medicine, cosmetics, food and beverages, etc., compared with the past, due to reasons such as reducing the burden on the subject and the improvement of consumers' health awareness, there is an urgent desire to reduce the content of agents as active ingredients, flavor components, etc. Therefore, means for enhancing and / or maintaining the effect of the active ingredient for a long time are sought. Accordingly, an object of the present invention is to provide a new means for enhancing and / or maintaining the effect of the active ingredient for a long time.

[0018] Solutions to the Problems

[0019] The present inventors conducted in-depth research to solve the above problems, and as a result, found that an oil-in-water emulsion prepared by blending a hydrophobic substance, water, cyclodextrin, and a thickening polysaccharide adheres to the tissue of an animal, and the active ingredient is retained therein by absorption / adsorption, whereby the active ingredient can be retained, and the effect brought by the active ingredient can be enhanced and / or maintained for a long time in the tissue.

[0020] The present invention is an invention based on these new insights and includes the following inventions.

[0021] [1] A retention agent for retaining an active ingredient, comprising: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide.

[0022] [2] The retention agent according to [1], wherein the hydrophobic substance is at least one selected from the group consisting of fats and oils, hydrophobic waxes, and hydrophobic resins.

[0023] [3] The retention agent according to [1] or [2], wherein the thickening polysaccharide is at least one selected from the group consisting of carboxymethyl cellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind polysaccharide gum, gellan gum, gum arabic, pectin, phosphoric acid cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphoric acid cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose.

[0024] [4] The retention agent according to any one of [1] to [3] is used by adding it to food and drink.

[0025] [5] The retention agent according to any one of [1] to [3] is used by adding it to pharmaceuticals.

[0026] [6] The retention agent according to any one of [1] to [3] is used by adding it to cosmetics.

[0027] [7] A method for manufacturing a retention agent for retaining an active ingredient, which includes a step of mixing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide to form an oil-in-water emulsion.

[0028] [8] A food and drink containing a retention agent for retaining an active ingredient, the retention agent including: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and the retention agent being 0.5% by mass to 55% by mass based on the amount of the hydrophobic substance.

[0029] [9] A pharmaceutical containing a retention agent for retaining an active ingredient, the retention agent including: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and the retention agent being 0.5% by mass to 55% by mass based on the amount of the hydrophobic substance.

[0030]

[10] A cosmetic containing a retention agent for retaining an active ingredient, the retention agent including: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and the retention agent being 0.5% by mass to 55% by mass based on the amount of the hydrophobic substance.

[0031]

[11] Use of an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide in a method for manufacturing a retention agent for retaining an active ingredient.

[0032] This specification includes the content described in the specification etc. of Japanese Patent Application No. 2022-211335 filed on December 28, 2022, which is the basis of the priority of this application.

[0033] All the publications, patents, and patent applications cited in this specification are directly incorporated herein by reference.

[0034] Effects of the Invention

[0035] According to the present invention, it is possible to provide a retention agent for an active ingredient, which can retain the active ingredient on the tissue of an animal and can enhance and / or maintain the effect brought by the active ingredient for a long time. Brief Description of the Drawings

[0036] Figure 1 It is a graph showing the results of evaluating the change in the intensity of taste within 1 minute by the Time Intensity (TI) method using the sensory evaluation software FIZZ (Biosystemes) after preparing each sample by blending components of various taste qualities in an aqueous solution of the oil-in-water emulsion of the present invention (1% O / W(+)) and an aqueous solution of a mixture of components constituting the oil-in-water emulsion (not forming an oil-in-water emulsion) (1% O / W(-)). (Sweet taste: N = 4, salty / bitter taste: N = 5, sour / umami taste: N = 3. The results represent the average value).

[0037] Figure 2 It is a graph showing the results of evaluating the change in the intensity of taste within 1 minute by the Time Intensity (TI) method using the sensory evaluation software FIZZ (Biosystemes) after ingesting an aqueous salt solution before (before attachment) and after (after attachment) attaching the aqueous solution of the oil-in-water emulsion of the present invention (10% O / W(+)) to the oral cavity. Detailed Description of the Invention

[0038] 1. Oil-in-water emulsion

[0039] The oil-in-water emulsion in the present invention contains water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide.

[0040] In the present invention, the "hydrophobic substance" is not particularly limited as long as it is insoluble in water and can form an oil-in-water emulsion together with water, the cyclodextrin described in detail below, and the thickening polysaccharide. Preferred examples include oils and fats, hydrophobic waxes, hydrophobic resins, etc. The hydrophobic substance can be used alone or in combination of different types of hydrophobic substances. For example, the hydrophobic substance can be one or more substances selected from the group consisting of oils and fats, hydrophobic waxes, and hydrophobic resins, and an appropriate substance can be selected according to the utilization mode of the retention agent of the present invention.

[0041] In the present invention, the "oil-in-water emulsion" refers to an emulsified composition in which a hydrophobic substance is dispersed in water, and cyclodextrin and the thickening polysaccharide contribute to the formation and stability of this emulsified state.

[0042] In the present invention, the "oil and fat" can be the oil and fat commonly used in the formation of oil-in-water emulsions, and both polar and non-polar ones can be used. Examples of such oil and fat include, for example, plant-derived oil and fat (such as canola oil, refined rapeseed oil, soybean oil, corn oil, cottonseed oil, peanut oil, sesame seed oil, rice oil, rice bran oil, camellia seed oil, safflower oil, olive fruit oil, linseed oil, perilla oil, perilla seed oil, sunflower oil, palm oil, tea oil, coconut oil, avocado oil, candlenut seed oil, grape seed oil, cocoa seed butter, coconut oil, wheat germ oil, almond oil, evening primrose oil, castor seed oil, Chilean hazelnut oil, macadamia nut oil, rosehip oil, grape oil, cocoa butter, jojoba seed oil, palm kernel oil, etc.), isostearyl alcohol, octanol, lauryl alcohol, stearyl alcohol, 2-octadecanol, myristyl alcohol, cetyl alcohol, phytosterol, cholesterol, stearic acid, isostearic acid, capric acid, lanolin acid, lauric acid, myristic acid, palmitic acid, behenic acid, linoleic acid, linolenic acid, glycerol monostearate, glycerol monopalmitate, glycerol monobehenate, glycerol monomyristate, glycerol monolaurate, glycerol monolanolate, glycerol monooleate, triisostearin, isopropyl myristate, tri-2-heptylundecanoin, tri-2-ethylhexanoin, 2-heptylundecyl palmitate, di-2-heptylundecyl adipate, cetyl isooctanoate, trimethylolpropane-2-triheptylundecanoate, propane-2-ethyl hexanoate, pentaerythritol-2-heptylundecanoate, pentaerythritol-2-ethylhexanoate, cholesteryl isostearate, diethyl phthalate, dibutyl phthalate and other synthetic ester oils, tallow, lard, lanolin, squalene, squalane and other animal-derived oil and fat, silicone oil, etc., but not limited to these. The oil and fat used in the present invention is preferably an oil and fat that is at least in a liquid state at normal temperature, and preferably an animal-derived or plant-derived oil and fat with high safety, and particularly preferably an edible vegetable oil with edible experience and high safety. The oil and fat can be used alone or in combination of different oil and fats, and an appropriate oil and fat can be selected according to the utilization mode of the retention agent of the present invention. It should be noted that in this specification, "normal temperature" refers to 5 to 35 °C, preferably 15 to 30 °C.

[0043] In the present invention, examples of the "hydrophobic wax" include natural hydrophobic waxes derived from animals, plants, petroleum or minerals, and synthetic hydrophobic waxes. Hydrophobic waxes with a melting point of 80°C or lower can be used, and preferably, hydrophobic waxes that are in a liquid state at least at normal temperature. Examples of such hydrophobic waxes include, but are not limited to, beeswax, spermaceti, lanolin, urushi wax, rosin (colophony), candelilla wax, carnauba wax, cocoa butter, paraffin wax, microcrystalline wax, ceresin wax, petrolatum wax, ozokerite wax, polyethylene wax, oxidized polyethylene wax, Fischer-Tropsch wax, alcohol-modified wax, maleic acid-modified oxidized polyethylene wax, amide wax, etc. As the hydrophobic wax used in the present invention, hydrophobic waxes derived from animals or plants with high safety are particularly preferred. Any one of the hydrophobic waxes can be used alone, or different hydrophobic waxes can be used in combination, and an appropriate hydrophobic wax can be selected according to the utilization mode of the retention agent of the present invention.

[0044] In the present invention, the "hydrophobic resin" refers to a resin that does not have a hydrophilic group or has a small content thereof and is insoluble in polar solvents such as water. In the present invention, hydrophobic resins that are in a liquid state at least at normal temperature can be preferably used. Examples of such hydrophobic resins include, but are not limited to, silicone resins (non-hydrophilized silicone resins), polyurethane resins, fluorine-containing resins, polyethylene resins, polypropylene resins, polyester resins, acrylic resins, polystyrene resins, polycarbonate resins, polyvinyl chloride resins, polysulfone resins, polyethersulfone resins, polyaramide resins, polyamide resins, polyether resins, polyacrylonitrile resins, polyetherimide resins, and copolymers of these polymers, etc. As the hydrophobic resin used in the present invention, hydrophobic resins with high safety that are confirmed to have biocompatibility and bioaffinity are particularly preferred. Any one of the hydrophobic resins can be used alone, or different hydrophobic resins can be used in combination, and an appropriate hydrophobic resin can be selected according to the utilization mode of the retention agent of the present invention.

[0045] In the present invention, the "hydrophobic substance" is preferably an oil and a hydrophobic wax, and particularly preferably an oil.

[0046] The oil-in-water emulsion of the present invention may contain a hydrophobic substance in any amount, for example, in an amount of 1% by mass or more, 3% by mass or more, 5% by mass or more, or 7% by mass or more, and the upper limit is not particularly limited. For example, it may be set to 50% by mass or less, 40% by mass or less, 30% by mass or less, 20% by mass or less, or 10% by mass or less. The range of the amount of the hydrophobic substance in the oil-in-water emulsion of the present invention can be represented by using two values selected from the foregoing lower limit and upper limit values respectively. For example, the oil-in-water emulsion of the present invention may contain a hydrophobic substance in an amount appropriately selected from the ranges of 1% by mass to 50% by mass, 1% by mass to 30% by mass, 1% by mass to 20% by mass, or 1% by mass to 10% by mass, preferably 5% by mass to 10% by mass, or 7% by mass to 10% by mass. When the amount of the hydrophobic substance is less than 1% by mass, emulsification may sometimes be insufficient. On the other hand, when the amount of the hydrophobic substance is more than 50% by mass, stickiness, greasiness, etc. may sometimes be strongly felt. In either case, there may be a situation where the active ingredient cannot be retained in the usage form for the intended purpose, or a situation where the desired feeling in use cannot be obtained.

[0047] It should be noted that in this specification, the amounts of the respective components contained in the oil-in-water emulsion of the present invention are described in terms of mass% with the total mass of the oil-in-water emulsion being set to 100% by mass.

[0048] In the oil-in-water emulsion of the present invention, water can be contained in any amount capable of emulsifying hydrophobic substances and forming an oil-in-water emulsion together with cyclodextrin and thickening polysaccharides. For example, the oil-in-water emulsion of the present invention contains water in an amount of 15% by mass or more, 20% by mass or more, 30% by mass or more, 40% by mass or more, 45% by mass or more, 50% by mass or more, 60% by mass or more, or 70% by mass or more. The upper limit is not particularly limited and can be set to 90% by mass or less or 85% by mass or less, for example. The range of the amount of water in the oil-in-water emulsion of the present invention can be represented by using two values selected from the aforementioned lower limit and upper limit values, respectively. For example, the oil-in-water emulsion of the present invention can contain water in an amount appropriately selected from the ranges of 15% to 90% by mass, 45% to 90% by mass, or 70% to 85% by mass. The amount of water contained in the oil-in-water emulsion of the present invention is preferably contained in a larger amount than the hydrophobic substance in terms of volume ratio. For example, the content of the hydrophobic substance and water can be set to an amount where (hydrophobic substance: water) exceeds 1:1 in terms of volume ratio, and can be set to 1:2 or more, 1:3 or more, 1:4 or more, 1:5 or more, 1:6 or more, 1:10 or more, 1:15 or more, or 1:20 or more, for example. The upper limit of the amount of water is not particularly limited and can be set to 1:90 or less, 1:80 or less, 1:70 or less, 1:60 or less, or 1:50 or less. By adjusting the amounts of water and hydrophobic substance contained in the oil-in-water emulsion of the present invention to the above ranges, stickiness, greasiness, etc. can be suppressed.

[0049] "Cyclodextrin" refers to cyclic non-reducing maltooligosaccharides having glucose as a structural unit, and examples include α-cyclodextrin having 6 glucose units, β-cyclodextrin having 7 glucose units, and γ-cyclodextrin having 8 glucose units. In the present invention, α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin and their derivatives, and any combination thereof can be used. Examples of cyclodextrin derivatives include ethyl cyclodextrin, methyl cyclodextrin, hydroxyethyl cyclodextrin, hydroxypropyl cyclodextrin, methylamino cyclodextrin, amino cyclodextrin, carboxyethyl cyclodextrin, carboxymethyl cyclodextrin, sulfonyloxyethyl cyclodextrin, sulfonyloxy cyclodextrin, acetyl cyclodextrin, branched cyclodextrin, cyclodextrin fatty acid ester, glucosyl cyclodextrin, maltosyl cyclodextrin, etc., but are not limited thereto. α-Cyclodextrin is preferably used. α-Cyclodextrin has high solubility in water and can obtain an oil-in-water emulsion with little roughness.

[0050] In the oil-in-water emulsion of the present invention, cyclodextrin can be contained in an amount that can contribute to the emulsification and stability of the oil-in-water emulsion together with the thickening polysaccharide and can provide a desired feeling in the intended use form. For example, in the oil-in-water emulsion of the present invention, cyclodextrin is contained in an amount of 0.5% by mass or more, 1% by mass or more, 2.5% by mass or more, 3% by mass or more, 4% by mass or more, 4.5% by mass or more, or 5% by mass or more. The upper limit is not particularly limited and can be set, for example, to 15% by mass or less, 10% by mass or less, 9% by mass or less, 8% by mass or less, 7% by mass or less, or 6% by mass or less. The range of the amount of cyclodextrin in the oil-in-water emulsion of the present invention can be represented by using two values selected from the aforementioned lower limit and upper limit values respectively. For example, in the oil-in-water emulsion of the present invention, cyclodextrin can be contained in an amount appropriately selected from the ranges of 0.5% by mass to 15% by mass, such as 1% by mass to 15% by mass, 2.5% by mass to 10% by mass, 2.5% by mass to 9% by mass, 3% by mass to 9% by mass, 4% by mass to 8% by mass, 4.5% by mass to 9% by mass, or 5% by mass to 7% by mass, preferably 2.5% by mass to 9% by mass, or 4.5% by mass to 9% by mass. When the amount of cyclodextrin is less than 0.5% by mass, the emulsification and stability of the oil-in-water emulsion may become insufficient. On the other hand, when the amount of cyclodextrin is more than 15% by mass, the viscosity of the oil-in-water emulsion may become too high and the astringent feeling may become stronger. In either case, there may be a situation where the active ingredient cannot be retained or the desired feeling cannot be obtained in the intended use form.

[0051] In the present invention, "thickening polysaccharide" generally refers to a polysaccharide that is soluble in water and imparts viscosity (sometimes also referred to as a thickening stabilizer, water-soluble paste, etc.). As the thickening polysaccharide that can be used in the present invention, components commonly used in the manufacture of food and beverages, pharmaceuticals (including quasi-drugs), cosmetics, etc. can be used, and there is no particular limitation. Any one of the thickening polysaccharides can be used alone, or different thickening polysaccharides can be used in combination, and an appropriate thickening polysaccharide can be selected according to the utilization mode of the retention agent of the present invention. In the present invention, "thickening polysaccharide" preferably includes carboxymethyl cellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind polysaccharide gum, gellan gum, gum arabic, pectin, phosphoric acid cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphoric acid cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, etc. Any one of them can be used alone, or two or more different types of thickening polysaccharides can be used in combination.

[0052] In the present invention, the "viscosity-increasing polysaccharides" are more preferably carboxymethyl cellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind polysaccharide gum, and gellan gum, and further preferably carboxymethyl cellulose (CMC), glucomannan, tamarind polysaccharide gum, and xanthan gum. These viscosity-increasing polysaccharides can particularly impart extremely high emulsion stability to the oil-in-water emulsion of the present invention.

[0053] In the oil-in-water emulsion of the present invention, the viscosity-increasing polysaccharides can be contained in an amount that can contribute to the emulsification and stability of the oil-in-water emulsion together with cyclodextrin and can provide a desired feeling of use in the form of use for the intended purpose. For example, the oil-in-water emulsion of the present invention contains the viscosity-increasing polysaccharides in an amount of 0.05% by mass or more, 0.1% by mass or more, 0.2% by mass or more, or 0.3% by mass or more, and the upper limit is not particularly limited. For example, it can be set to 1% by mass or less, 0.8% by mass or less, 0.7% by mass or less, 0.6% by mass or less, or 0.5% by mass or less. The range of the amount of the viscosity-increasing polysaccharides in the oil-in-water emulsion of the present invention can be represented by using two values selected from the aforementioned lower limit and upper limit values respectively. For example, the oil-in-water emulsion of the present invention can contain the viscosity-increasing polysaccharides in an amount appropriately selected from the ranges of 0.05% by mass to 1% by mass, 0.1% by mass to 1% by mass, 0.2% by mass to 0.8% by mass, or 0.2% by mass to 0.5% by mass. When the amount of the viscosity-increasing polysaccharides is less than 0.05% by mass, the emulsification and stability of the oil-in-water emulsion may become insufficient. On the other hand, when the amount of the viscosity-increasing polysaccharides is more than 1% by mass, the viscosity of the oil-in-water emulsion may become too high. In either case, there may be a situation where the active ingredient cannot be retained or a desired feeling of use cannot be obtained in the form of use for the intended purpose.

[0054] In the oil-in-water emulsion of the present invention, the emulsification and stability of the oil-in-water emulsion are imparted by using the above-mentioned cyclodextrin and the above-mentioned thickening polysaccharide in combination. The emulsification and stability of the oil-in-water emulsion brought about by using the above-mentioned cyclodextrin and the above-mentioned thickening polysaccharide in combination do not depend on a three-dimensional matrix gel formed by dissolving a general gelling agent in water and cooling it (preferably does not contain a three-dimensional matrix gel). As described in detail in the following examples, it is considered to be due to the existence of an interaction caused by a hydrogen bond generated between the above-mentioned cyclodextrin and the above-mentioned thickening polysaccharide. In addition, the oil-in-water emulsion of the present invention has emulsification and stability by using the above-mentioned cyclodextrin and the above-mentioned thickening polysaccharide in combination, and therefore can substantially not contain an emulsifier usually used in the production of conventional emulsifying compositions, and preferably substantially does not contain the emulsifier. In the present invention, "substantially free of emulsifier" means that in the oil-in-water emulsion of the present invention, the emulsifier is not contained in a manner that exhibits an emulsifying effect, and does not mean that the emulsifier is completely absent. By substantially not containing an emulsifier, the present invention can obtain, for example, an oil-in-water emulsion having high safety such as low irritation and low allergenicity when the oil-in-water emulsion of the present invention is applied. Examples of the "emulsifier usually used in the production of conventional emulsifying compositions" include, but are not limited to, proteins, peptides or their hydrolyzates, glycerol fatty acid esters, organic acid monoglycerides, polyglycerol fatty acid esters, polyoxyethylene glycerol fatty acid esters, sorbitan fatty acid esters, propylene glycol fatty acid esters, polyoxyethylene fatty acid esters, polyglycerol condensed ricinoleic acid esters, sorbitan fatty acid esters, polyoxyethylene sorbitol fatty acid esters, sucrose fatty acid esters, lecithin, enzyme-decomposed lecithin, polyethylene glycol, polypropylene glycol, etc.

[0055] The form of the oil-in-water emulsion of the present invention is not particularly limited. In addition to the form having the above-mentioned water content, it can also be provided in the form of a semi-solid / semi-liquid (gel, sol, etc.) or a dried body (such as powder, sheet, etc.) prepared by reducing the water content. Such forms of semi-solid / semi-liquid (gel, sol, etc.) or dried body (such as powder, sheet, etc.) can be obtained as follows: After obtaining the oil-in-water emulsion having the above-mentioned water content, it is subjected to a conventionally known drying means to reduce the water content of the oil-in-water emulsion, thereby obtaining the above-mentioned forms of semi-solid / semi-liquid (gel, sol, etc.) or dried body (such as powder, sheet, etc.). Examples of such drying means include freeze-drying, heat drying, air drying, spray drying, drum drying, hot air drying, vacuum drying, etc., but are not limited to these. The water content of the oil-in-water emulsion after being subjected to the drying means can be appropriately selected according to the target form. In the case of the form of a dried body, for example, it can be set to less than 15% by mass, 10% by mass or less, 5% by mass or less, or 1% by mass or less. The lower limit of the water content of the oil-in-water emulsion after being subjected to the drying means is not particularly limited and can be set to 0% by mass or more, more than 0% by mass, 0.1% by mass or more, 0.5% by mass or more, 0.6% by mass or more, 0.7% by mass or more, or 0.8% by mass or more. The range of the water content of the form of the dried body can be represented by using two values respectively selected from the aforementioned upper and lower limits. For example, the water content of the oil-in-water emulsion can be set to 0% by mass or more and less than 15% by mass, more than 0% by mass and less than 15% by mass, 0.1% by mass or more and less than 15% by mass, 0.1% - 10% by mass, 0.5% - 5% by mass, 0.5% - 1% by mass, 0.6% - 1% by mass, 0.7% - 1% by mass, or 0.8% - 1% by mass. The oil-in-water emulsion of the present invention after being subjected to the drying means does not undergo a phase change to produce a water-in-oil emulsion. Moreover, particularly in the form of a dried body, it has high heat resistance and moisture resistance such that it does not discolor or dissolve even after being subjected to high temperature (such as around 100°C - 200°C) conditions and / or high humidity (such as around 95% humidity).

[0056] In the oil-in-water emulsion of the present invention, in addition to the above components, components commonly used in the production of utilization forms for purposes such as food and drink, pharmaceuticals (including quasi-drugs), cosmetics, etc. (hereinafter referred to as "other components") can be appropriately blended in an amount corresponding to the desired utilization form, within the range that does not impair the effects of the present invention. Examples of such other components include excipients, disintegrants, lubricants, binders, diluents, buffers, suspending agents, thickeners, preservatives, antibacterial agents, antiseptics, antioxidants, ultraviolet absorbers, colorants, pigments, dyes, pigments, lubricants, plasticizers, solvents, cosolvents, isotonic agents, flavoring and odor-correcting agents, vitamins, surfactants, pH regulators, chelating agents, etc., but are not limited to these.

[0057] The oil-in-water emulsion of the present invention can be produced by mixing, stirring water, a hydrophobic substance, cyclodextrin, a thickening polysaccharide, and, if necessary, other components in the above-described amounts. All the components can be mixed and stirred together, or the components can be added separately or in any combination in sequence (the order is not limited) and then mixed and stirred. The obtained oil-in-water emulsion can be subjected to heat sterilization treatment.

[0058] In addition, the oil-in-water emulsion obtained by mixing and stirring can be further subjected to drying means, if necessary. The drying means can be carried out by the above-mentioned conventionally known drying means, and the water content of the oil-in-water emulsion can be appropriately adjusted according to the purpose shape of the semi-solid / semi-liquid (gel, sol, etc.) or the dried product. The obtained dried product can be further subjected to crushing, grinding or pulverizing treatment, if necessary, to form powders, flakes and other forms. In the oil-in-water emulsion obtained by subjecting to drying means, other components can be mixed and stirred in the above-described amounts, if necessary, and / or it can also be subjected to heat sterilization treatment.

[0059] 2. Uses

[0060] The oil-in-water emulsion of the present invention can be used as a retention agent for retaining an active ingredient.

[0061] In the present invention, the "retention agent" refers to being able to retain for a long time by holding or maintaining the active ingredient at a specified site, and thus, compared with the case where the retention agent is not used, the effect of the active ingredient can be enhanced and / or maintained for a long time. When the retention agent of the present invention is administered to an animal or ingested together with the active ingredient, the oil-in-water emulsion adheres to the tissue at the application site, and the active ingredient is held here and / or absorbed / adsorbed to hold the active ingredient, thereby being able to retain, and compared with the case where the retention agent is not used, the effect brought by the active ingredient can be enhanced and / or maintained for a long time.

[0062] In the present invention, the "animal" is not particularly limited and can be any animal, preferably a mammal, and examples include humans, domestic animals (such as cows, horses, sheep, pigs, goats, etc.), pet animals (such as dogs, cats, rabbits, hamsters, guinea pigs, etc.) (not limited to these), and more preferably humans.

[0063] In the present invention, the "tissue" includes various epithelial tissues visible in the skin, oral cavity, esophagus, anus, vagina, nasal cavity, trachea, bronchi, stomach, small intestine, large intestine, fallopian tubes, uterus, pleura, peritoneum, vascular endothelium, alveoli, thyroid (follicles), renal tubules, ureters, bladder, etc., hair, fingernails, toenails, teeth, etc., and can be appropriately selected according to the target application site. In the present invention, the "epithelial tissue" is preferably various epithelial tissues visible in the skin, oral cavity, esophagus, nasal cavity, trachea, bronchi, etc., and more preferably the epithelial tissue in the oral cavity.

[0064] In the present invention, "administered or ingested together with the active ingredient" means that as long as the oil-in-water emulsion of the present invention and the active ingredient can coexist in the tissue at the application site during the time of administration or ingestion. For example, the oil-in-water emulsion of the present invention and the active ingredient can be included in one composition and administered or ingested simultaneously, or the two can be administered or ingested simultaneously or successively (preferably in the order of the oil-in-water emulsion of the present invention, followed by the active ingredient) in different forms and / or different administration routes. "Administration" means that as long as the oil-in-water emulsion of the present invention and the active ingredient can be delivered to the tissue as the application site, it can be appropriately selected according to the form, amount, etc. of the oil-in-water emulsion of the present invention and the active ingredient. For example, "administration" includes oral administration, spray administration, inhalation, nasal administration, intraoral administration, rectal administration, transdermal administration, coating, etc., but is not limited to these. Preferably, "administration" is oral administration, spray administration, inhalation, intraoral administration or coating.

[0065] In the present invention, examples of the "active ingredient" include water-soluble ingredients or ingredients having an affinity for the above hydrophobic substances (such as lipophilic ingredients, etc.). It is considered that the water-soluble ingredients are preferably bonded to the thickening polysaccharides and / or cyclodextrins (for example, forming hydrogen bonds) and retained in the water phase of the oil-in-water emulsion of the present invention. On the other hand, the ingredients having an affinity for the above hydrophobic substances are retained in the hydrophobic substances of the oil-in-water emulsion of the present invention. Examples of the "active ingredient" in the present invention include ingredients of the taste quality in food and drink (salty ingredients such as sodium chloride and potassium chloride; sweet ingredients such as sugars (glucose, fructose, sucrose, maltose, oligosaccharides, isomerized sugars, etc.), sugar alcohols (xylitol, sorbitol, glycerol, erythritol, etc.), natural sweeteners (stevia, glycyrrhizin, thaumatin, etc.), artificial sweeteners (aspartame, acesulfame potassium, sucralose, etc.); sour ingredients such as citric acid, succinic acid, lactic acid, tartaric acid, acetic acid, fumaric acid, malic acid, gluconic acid, ascorbic acid; umami ingredients such as glutamic acid, inosinic acid, guanylic acid; bitter ingredients such as alkaloids (caffeine, quinine, strychnine, theobromine, etc.), terpenes (limonoids, limonin, obacunone, nomilin, cucurbitacin, humulone, cnidilide, etc.), glycosides (terpene glycosides, flavanone glycosides, naringin, neohesperidin, etc.), amino acids (tryptophan, phenylalanine, trypsin, arginine, valine, leucine, isoleucine, proline, etc.), casein, soy protein, etc.; spicy ingredients such as capsaicin, piperine, sanshool, gingerol, gingerol, diallyl disulfide, p-hydroxybenzyl, isothiocyanate, etc.; astringent ingredients such as tannins, catechins, theaflavins, thearubigins, etc. (not limited to these)), and ingredients of food materials, seasonings, spices, etc. containing them, ingredients for specified treatments / purposes in pharmaceuticals (including quasi-drugs) and cosmetics (hereinafter referred to as "pharmaceuticals, etc."), such as medicaments, bactericides, antibacterial agents, antibiotics, enzymes, antibodies, vitamins, minerals, amino acids, cooling agents, deodorants, moisturizing agents, fragrances, etc. (not limited to these)).

[0066] In order to retain the active ingredients in food and beverages, pharmaceuticals, etc., the retention agent of the present invention can be added to food and beverages, pharmaceuticals, etc. for use. The addition amount only needs to be an amount that can retain or maintain the active ingredients in food and beverages, pharmaceuticals, etc. at a specified site, and can retain them for a long time compared with the case where the retention agent is not used, and can enhance and / or maintain the effect of the active ingredient for a long time. It can be appropriately determined according to the type and amount of the active ingredient, and the type and form of food and beverages, pharmaceuticals, etc. For example, in food and beverages, pharmaceuticals, etc., the retention agent of the present invention can be contained in an amount of 0.1% by mass or more, 0.5% by mass or more, 1% by mass or more, 2.5% by mass or more, 5% by mass or more, or 7% by mass or more based on the amount of its hydrophobic substance. There is no particular limitation on the upper limit. For example, it can be set to 55% by mass or less, 50% by mass or less, 40% by mass or less, 30% by mass or less, 20% by mass or less, or 10% by mass or less. The range of the amount of the retention agent of the present invention in food and beverages, pharmaceuticals, etc. can be represented by using two values selected from the aforementioned lower limit and upper limit values respectively. For example, in food and beverages, pharmaceuticals, etc., the retention agent of the present invention can be contained in an amount appropriately selected from the ranges of 0.5% by mass to 55% by mass, 0.5% by mass to 50% by mass, 0.5% by mass to 40% by mass, 0.5% by mass to 20% by mass, or 0.5% by mass to 10% by mass based on the amount of its hydrophobic substance. When the amount of the retention agent of the present invention contained in food and beverages, pharmaceuticals, etc. is less than or more than the above range, there will be cases where the active ingredient cannot be retained in the utilization form in the intended use.

[0067] It should be noted that in this specification, the amounts of the respective components contained in food and beverages, pharmaceuticals, etc. are expressed as mass% amounts with the total mass of the solution of the food and beverages, pharmaceuticals, etc., the liquid part other than the solid part (for example, in the case of food and beverages, the amount of the liquid part such as sauce and soup other than the ingredients) set to 100% by mass. In the case where food and beverages, pharmaceuticals, etc. are in a liquid form or do not have a liquid part form, the amount can be set as the amount in a solution prepared by adding an appropriate solvent (such as water, hot water, physiological saline, buffer solution, etc.) when administered or ingested / added to an appropriate solvent, or the amount in a solution formed by dissolving the food and beverages, pharmaceuticals, etc. in the moisture in the tissue at the application site (such as body fluids such as saliva).

[0068] In food and beverages, pharmaceuticals, etc., the retention agent of the present invention and the active ingredient can be contained simultaneously (for example, can be contained in one composition), or the retention agent of the present invention and the active ingredient can be in different forms (for example, can be contained separately in two or more compositions administered or ingested simultaneously).

[0069] The forms of food products, pharmaceuticals, etc. can be appropriately selected according to the form of utilization in the intended use (e.g., the form of a specified product, etc.), and any form such as solid, powder, granule, flake, chewable tablet, tablet, film, chewing gum, liquid, emulsion, semi-solid / semi-liquid (gel, sol, cream, paste, custard, etc.), soft capsule, etc. (not limited to these) can be adopted. Among them, it is preferable that the retention agent of the present invention coexists with the active ingredient in an amount within the above range in the tissue at the application site. Food products, pharmaceuticals, etc. can, according to their forms, be added with an appropriate solvent (e.g., water, hot water, physiological saline, buffer solution, etc.) / added to an appropriate solvent when administered or ingested as needed, and the content of the retention agent of the present invention in the food products, pharmaceuticals, etc. is adjusted to the above range before administration or ingestion (Food products, pharmaceuticals, etc. in such forms include, but are not limited to, forms such as solid, powder, granule, flake, liquid, emulsion, semi-solid / semi-liquid (gel, sol, cream, paste, custard, etc.)). Alternatively, food products, pharmaceuticals, etc. can also dissolve the retention agent and the active ingredient of the present invention in the moisture (e.g., body fluids such as saliva) in the tissue at the application site, and the content of the retention agent of the present invention is within the above range to exert its effect (Food products, pharmaceuticals, etc. in such forms include, but are not limited to, forms such as powder, granule, chewable tablet, tablet, film, chewing gum, etc.).

[0070] In food products, pharmaceuticals, etc., in addition to the retention agent and the active ingredient of the present invention, components that are usually used in the production of the form of utilization in the intended use (e.g., the form of a specified product, etc.) corresponding to the desired form of utilization can be appropriately blended in an amount that does not impair the effects of the present invention as needed. Examples of such components include, but are not limited to, excipients, disintegrants, lubricants, binders, diluents, buffers, suspending agents, thickening agents, preservatives, antibacterial agents, antiseptics, antioxidants, ultraviolet absorbers, colorants, pigments, dyes, colorants, lubricants, plasticizers, solvents, cosolvents, isotonic agents, flavor and odor correctors, fragrances, sweeteners, flavor components, acidulants, seasonings, humectants, vitamins, surfactants, chelating agents, antibacterial agents, emulsifiers, water-soluble organic solvents, food ingredients, etc.

[0071] In one mode, the retention agent of the present invention is provided by being included in a food product. By consuming this food product, the oil-in-water emulsion in the retention agent of the present invention adheres to the epithelial tissue in the oral cavity, and while staying here, it retains the active ingredient ingested simultaneously, such as a flavor component, and / or the component that absorbs / adsorbs and retains the flavor, thereby making it stay. Compared with the case where this retention agent is not used, the effect brought by the active ingredient (e.g., the flavor and taste brought by the flavor component) can be enhanced and / or maintained for a long time. The retention agent of the present invention in such a mode of utilization is sometimes also referred to as a flavor enhancer, a taste enhancer, etc.

[0072] In addition, in another aspect, the "retention agent" of the present invention is provided by being included in an oral care product. By holding the product in the mouth, the oil-in-water emulsion of the retention agent of the present invention adheres to the epithelial tissue in the oral cavity, where a medicament as an active ingredient given simultaneously is retained (examples include, but are not limited to, caries prevention / repair agents (cetylpyridinium chloride (CPC), benzalkonium chloride, benzethonium chloride (BTC), sodium fluoride, sodium monofluorophosphate, etc.), gingivitis / periodontitis prevention / improvement agents (ε-aminocaproic acid, isopropylmethylphenol (methylisopropylbenzene-5-ol), allantoin, dipotassium glycyrrhizinate, β-glycyrrhetinic acid, cetylpyridinium chloride (CPC), hinokitiol, triclosan, tranexamic acid, benzalkonium chloride, benzethonium chloride (BTC), triclosan, sodium chloride, tocopheryl acetate, etc.), stomatitis prevention / improvement agents (allantoin, glycyrrhizic acid, tranexamic acid, etc.), sensory hypersensitivity prevention / inhibitors (aluminum lactate, potassium nitrate, etc.), plaque prevention / removers (dextranase, etc.), dental calculus prevention / removers (sodium polyphosphate, sodium pyrophosphate, etc.), stain prevention / removers (sodium polyphosphate, polyethylene glycol, etc.), halitosis prevention / removers (isopropylmethylphenol (methylisopropylbenzene-5-ol), sodium lauroyl sarcosinate, etc.), oral dryness prevention / inhibitors (hyaluronic acid, milk protein extract, lactoperoxidase, glucose oxidase, lysozyme, lactoferrin, dipotassium phosphate, potassium chloride, calcium chloride hydrate, sodium chloride, magnesium chloride, pilocarpine hydrochloride, cevimeline hydrochloride hydrate, anethol trithione, etc.)), and / or absorbs / adsorbs and retains the medicament, thereby making it stay. Compared with the case where the retention agent is not used, the effects brought by the medicament can be enhanced and / or maintained for a long time. Such oral care products can be in the generally known forms in the past, such as mouthwashes, mouth rinses, mouthwashes, liquid toothpastes, toothpastes, powdered toothpastes, gels, films, chewing gums, sprays, liquids, etc.

[0073] In another aspect, the "retention agent" of the present invention is provided by being included in a hair care product. By applying this product to the hair, the oil-in-water emulsion in the retention agent of the present invention adheres to the hair, where it retains the active ingredients given simultaneously, such as hair protection ingredients (hydrolyzed eggshell membrane, hydrolyzed keratin, hydrolyzed collagen, hydrolyzed silk, hydrolyzed wheat, hydrolyzed wheat protein, hydrolyzed soy protein, glutamic acid, arginine, pyrrolidone carboxylic acid, polydimethylsiloxane, amino-terminated dimethyl polysiloxane, polyquaternium-10, chitosan, etc.), hair quality improving ingredients (stearyl trimethyl ammonium bromide, cetrimonium bromide, stearyl trimethyl ammonium chloride, etc.), hair repair ingredients (olive fruit oil, jojoba seed oil, avocado oil, squalane, isopropyl myristate, isostearyl alcohol, oleyl alcohol, egg yolk fatty oil, adsorbed and purified lanolin, wild soybean sterols, cholesterol, ceramides, etc.), and moisturizing ingredients (hyaluronic acid, glycerin, hydrolyzed eggshell membrane, hydrolyzed keratin, hydrolyzed collagen, hydrolyzed silk, hydrolyzed wheat, hydrolyzed wheat protein, hydrolyzed soy protein, glutamic acid, arginine, pyrrolidone carboxylic acid, egg yolk fatty oil, adsorbed and purified lanolin, wild soybean sterols, cholesterol, ceramides, etc. (not limited to these)), and / or absorbs and adsorbs them to retain them, thereby making them stay. Compared with the case where the retention agent is not used, the effects brought by the active ingredients can be enhanced and / or maintained for a long time. Such hair care products can be in the general forms known in the past, such as shampoos, hair conditioners, hair conditioners, hair treatments, etc.

[0074] Hereinafter, the present invention will be described by way of examples, but the present invention is not limited to these examples.

[0075] Examples

[0076] Experiment 1: Evaluation of the Emulsion Stability of the Oil-in-Water Emulsion

[0077] (1) Preparation of the oil-in-water emulsion

[0078] According to the composition in Table 1 below, each component was added and mixed to prepare an oil-in-water emulsion. As the hydrophobic substance, an oil (canola oil) was used, and as the thickening polysaccharide, any one of carboxymethyl cellulose (CMC), glucomannan, guar gum, κ-carrageenan, tamarind polysaccharide gum, gellan gum, xanthan gum, ι-carrageenan, locust bean gum, λ-carrageenan was blended. As a control, any one of carboxyvinyl polymer and sodium polyacrylate, which are non-polysaccharide thickeners, was blended.

[0079] The mixing of each component is carried out once, and it is carried out by stirring with a manual stirrer at 20,000 rpm for 10 minutes. The obtained oil-in-water emulsion (50 mL) is transferred to a conical tube (Falcon (registered trademark) conical tube 50 mL) and centrifuged at 3,000 rpm for 1 minute. Then, visually observe the thickness (depth) of the aqueous phase, micelles, and oil phase, measure the ratio (%) of each phase, and evaluate the emulsification stability of each composition. The case where the ratio of micelles is 100% is evaluated as "◎", the case where the ratio of micelles is 70% or more and less than 100% is evaluated as "〇", and the case where the ratio of micelles is less than 70% is evaluated as "×".

[0080] It should be noted that the amounts of each component in the tables described below are expressed as mass % amounts based on setting the amount of the obtained oil-in-water emulsion to 100 mass %. Fats and oils, α-cyclodextrin, and thickening polysaccharides are all used as food additives (food grade).

[0081] [Table 1]

[0082]

[0083] (2) Results

[0084] The thickening polysaccharides added to the oil-in-water emulsion, the measured ratio of each phase, and the evaluation results are shown in Table 2. By adding and mixing thickening polysaccharides together with water, hydrophobic substances, and α-cyclodextrin, an oil-in-water emulsion can be formed. From the above results, it can be seen that when using carboxymethyl cellulose (CMC), glucomannan, guar gum, κ-carrageenan, tamarind polysaccharide gum, gellan gum, xanthan gum, ι-carrageenan, locust bean gum, λ-carrageenan as thickening polysaccharides, it is confirmed that the micelle phase of the oil-in-water emulsion is maintained even under the above conditions, showing particularly high emulsification stability. In particular, when adding CMC, glucomannan, tamarind polysaccharide gum, and xanthan gum separately, no separation of the aqueous phase and the oil phase is found, and significantly high emulsification stability is confirmed. On the other hand, it is confirmed that due to the addition of a non-polysaccharide thickener, the separation of the aqueous phase and the oil phase is large under the above conditions, and the emulsification stability is relatively low.

[0085] [Table 2]

[0086]

[0087] According to the composition of Table 3 below, each component is added and mixed to prepare an oil-in-water emulsion. As the hydrophobic substance, any one of carnauba wax, petrolatum wax (white petrolatum), rosin, and silicone oil containing 1% of oil red is used. As the thickening polysaccharide, xanthan gum is compounded. The amounts of each component in the table are expressed as mass % amounts based on setting the amount of the obtained oil-in-water emulsion to 100 mass %.

[0088] By mixing and stirring each component in the same manner as described above, transfer the obtained oil-in-water emulsion (50 mL) to a conical tube (Falcon (registered trademark) conical tube 50 mL) and centrifuge at 3000 rpm for 1 minute. Then, visually observe the thickness (depth) of the aqueous phase, micelles, and oil phase, measure the proportion (%) of each phase, and evaluate the emulsification stability of each composition in the same manner as described above.

[0089] [Table 3]

[0090]

[0091] The hydrophobic substances added to the oil-in-water emulsion, the measured proportion of each phase, and the evaluation results are shown in Table 4. From this result, it was confirmed that not only in the case of using fats and oils, but also in the case of using other hydrophobic substances, an oil-in-water emulsion can be formed. In addition, even under the above conditions, the micelle phase of the oil-in-water emulsion is maintained, and high emulsification stability is obtained.

[0092] [Table 4]

[0093]

[0094] Experiment 2: Evaluation of the interaction between α-cyclodextrin and thickening polysaccharides in an oil-in-water emulsion

[0095] To evaluate the interaction between α-cyclodextrin and thickening polysaccharides in an aqueous solution, the enthalpy change (ΔH) was determined by isothermal titration calorimetry (ITC) according to a conventionally known method. That is, using an isothermal titration calorimeter (NANO ITC SV; TA Instruments), 10 μL of an aqueous solution of thickening polysaccharide (0.05 g / 100 mL) was added dropwise to an aqueous solution of α-cyclodextrin (25 g / 100 mL) every 180 seconds for 25 times (75 minutes), and the enthalpy value (μJ) was determined from the area of the 25th (final) titration peak. As a control, carboxyvinyl polymer and sodium polyacrylate, which are thickeners that are not polysaccharides, were used, and the enthalpy value (μJ) was determined in the same manner.

[0096] The results are shown in Table 5. In the case of using thickening polysaccharides (CMC and xanthan gum) that showed particularly high emulsion stability in Experiment 1 above, a positive enthalpy value, that is, an endothermic reaction, was confirmed. This result suggests the existence of an interaction via hydration water between the thickening polysaccharide and α-cyclodextrin. For example, it is considered that a part of the water molecules hydrated with the thickening polysaccharide forms a hydrogen bond with α-cyclodextrin. Generally, the hydrogen bond formed between water molecules has a shorter distance and a higher energy value compared to the hydrogen bond formed between the thickening polysaccharide and α-cyclodextrin where intermolecular repulsion is caused by charged sites. Therefore, it is considered that when a part of the water molecules hydrated with the thickening polysaccharide forms a hydrogen bond with α-cyclodextrin, an endothermic reaction occurs as a result of subtracting the energy value. The movement of heat (positive enthalpy value) suggests the existence of an interaction generated between the thickening polysaccharide and α-cyclodextrin, and it is considered that this interaction is the main reason for the high emulsion stability of the oil-in-water emulsion in Experiment 1 above.

[0097] [Table 5]

[0098]

[0099] Experiment 3: Performance evaluation of oil-in-water emulsion (flavor enhancement)

[0100] (1) Flavor evaluation of the oil-in-water emulsion itself

[0101] According to the composition of Table 6 below, each component was added and mixed to prepare an oil-in-water emulsion. The mixing of each component was carried out at one time, and it was stirred with a manual stirrer at 20000 rpm for 10 minutes.

[0102] It should be noted that the amounts of each component in the table are expressed as mass % amounts with the amount of the obtained oil-in-water emulsion being set to 100 mass%.

[0103] As a control, a mixture was prepared by mixing the components other than the oil according to the composition of Table 6 below, adding the oil, and manually mixing without applying a shear force (that is, not making an oil-in-water emulsion).

[0104] The obtained oil-in-water emulsion and the control mixture were each added to water in an amount of 1 mass%, and a sensory evaluation of the presence or absence of flavor in each solution was carried out by a trained professional panelist, etc.

[0105] [Table 6]

[0106]

[0107] As a result, no difference in odor was found between the oil-in-water emulsion and the control mixture compared to water without adding any substance.

[0108] When ingesting the control mixture, a rich feeling derived from the oil was slightly felt compared to water, but no difference in taste was felt.

[0109] When ingesting the oil-in-water emulsion, compared to water, it was felt that the entire oral cavity was widely covered (coated with the oil-in-water emulsion), but no difference in taste was felt. The amount of oil contained in the 1% oil-in-water emulsion solution was only about 0.13% by mass, and it was confirmed that no taste or odor derived from the oil was felt.

[0110] (2) Effect I of flavor enhancement brought about by the combined use of the oil-in-water emulsion

[0111] In the 1% oil-in-water emulsion solution and the 1% control mixture solution obtained above, the components of each taste substance described in Table 7 below were added to each solution in a specified amount to prepare samples for flavor evaluation (hereinafter, the sample containing the 1% oil-in-water emulsion solution is referred to as "1% O / W(+)", and the sample containing the 1% control mixture solution is referred to as "1% O / W(-)"). As a control, an aqueous solution prepared by adding only the same amount of the components of each taste substance to water (hereinafter, referred to as "control aqueous solution") was further used.

[0112] Each sample (10 mL) was ingested in the evaluation order described in Table 7 below, and a trained professional panelist etc. evaluated the intensity of each taste on a 10-point scale with the evaluation of the control aqueous solution set as 5. Gargling was performed twice with 20 mL of water.

[0113] [Table 7]

[0114]

[0115] The evaluation results of the intensity of each taste of each sample are shown in Table 8 below (sweetness, umami, sourness, bitterness: N = 4, saltiness: N = 3).

[0116] [Table 8]

[0117]

[0118] Based on the above results, it was confirmed that by containing the components of the taste substance in the oil-in-water emulsion (1% O / W(+)), the intensity of each taste was significantly increased. Even when the components of the taste substance were contained in a mixture that did not form an oil-in-water emulsion (1% O / W(-)), a tendency for a slight increase in the intensity of the taste was also confirmed, but the degree was small.

[0119] Furthermore, for 1% O / W (+) and 1% O / W (-), after ingestion of each sample, a well-trained panel of experts evaluated the change in taste intensity within 1 minute using the Time Intensity (TI) method using the sensory evaluation software FIZZ (Biosystemes). The results are shown in Figure 1 (Sweetness: N=4, Saltiness / bitterness: N=5, Sourness / umami: N=3, Figure 1 The results show the average value of the results of each evaluation).

[0120] Depend on Figure 1 The results confirmed that, compared with 1% O / W(-), 1% O / W(+) provided higher values for at least one of the rise in taste immediately after consumption, intensity, mid-range body, and persistence of aftertaste.

[0121] (3) Flavor enhancement effect of combined use of oil-in-water emulsion II

[0122] According to the composition shown in Table 9 below, the components were added and mixed to prepare an oil-in-water emulsion. As thickening polysaccharides, xanthan gum, gum arabic, pectin, cross-linked starch phosphate, hydroxypropyl starch, hydroxypropylated cross-linked starch phosphate, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose were used. The components were mixed at once using a hand mixer at 20,000 rpm for 10 minutes.

[0123] In addition, the amount of each component in a table|surface is shown as the amount by mass % with the amount of the obtained oil-in-water emulsion being 100 mass %.

[0124] As a control, a mixture was prepared by mixing the components other than the oil and fat according to the composition in Table 9 below, adding the oil and fat, and mixing manually without applying a shearing force (ie, not forming an oil-in-water emulsion).

[0125] [Table 9]

[0126]

[0127] The resulting mixture of the oil-in-water emulsion and the control was added to water in an amount of 1% by mass, thereby preparing a 1% by mass oil-in-water emulsion solution and a 1% by mass control mixture solution. Salt was added to the mixture in an amount of 0.6% by mass to prepare samples for flavor evaluation (hereinafter, the sample containing the 1% by mass oil-in-water emulsion solution is referred to as "1% O / W(+)", and the sample containing the 1% by mass control mixture solution is referred to as "1% O / W(-)"). As the control aqueous solution, an aqueous solution prepared by adding salt to water in an amount of 0.6% by mass was further used.

[0128] Each sample (10 mL) was taken in the evaluation order described in Table 7 above, and professional reviewers who had been fully trained evaluated the intensity of each taste on a 10-point scale with the evaluation of the control aqueous solution set at 5. Gargling was performed twice with 20 mL of water.

[0129] The evaluation results of the intensity of each taste of each sample are shown in Table 10 below (N = 3).

[0130] [Table 10]

[0131]

[0132] From the above results, it was confirmed that regardless of the type of thickening polysaccharide used, the intensity of the taste was significantly increased by containing an oil-in-water emulsion (1% O / W(+)).

[0133] (4) Effect of enhanced flavor brought about by the combined use / repeated intake of an oil-in-water emulsion

[0134] 1% O / W(+) (10 mL each) containing a flavor component (0.6 mass% of sodium chloride or 0.2 mass% of caffeine) prepared by the same method as in (2) above was taken 4 times in succession (without gargling in between), and the intensity of each taste in each intake was evaluated on a 10-point scale with the evaluation of the first intake set at 5. The evaluation was carried out by professional reviewers who had been fully trained.

[0135] The evaluation results of the intensity of each taste of each sample are shown in Table 11 below (salty taste: N = 4, bitter taste: N = 3).

[0136] [Table 11]

[0137]

[0138] Based on the above results, it was confirmed that in any case, the intensity of the taste was gradually increased by repeatedly taking samples containing an oil-in-water emulsion. It is considered that this is because the components of the flavor and the oil-in-water emulsion adhere to the oral cavity together and are accumulated.

[0139] (5) Effect of enhanced flavor brought about by additional use of an oil-in-water emulsion I

[0140] The oil-in-water emulsion prepared in (1) above was added to water in an amount to make 10 mass% respectively, to obtain a 10 mass% aqueous solution of an oil-in-water emulsion without a flavor component (hereinafter, referred to as "10% O / W(+)"). An aqueous solution containing a flavor component (hereinafter, referred to as "flavor aqueous solution"). A 0.6 mass% sodium chloride aqueous solution was used.

[0141] For evaluation, the participants ingested a flavor aqueous solution (10 mL) and evaluated the intensity of the taste (before attachment). The participants then rinsed their mouths (rinsed their mouths with 20 mL of water twice). Subsequently, 10% O / W (+) (10 mL) was placed in the mouth for 30 seconds, allowed to adhere, and then expelled. The participants then rinsed their mouths (rinsed their mouths with 20 mL of water twice). The participants then ingested the flavor aqueous solution (10 mL) again and evaluated the intensity of the taste (after attachment). The evaluation was conducted by a panel of trained professionals using a 10-point scale, with the flavor aqueous solution before attachment being rated at 5.

[0142] The obtained evaluation results are shown in the following Table 12 (N=4).

[0143] [Table 12]

[0144]

[0145] Furthermore, the flavor intensity changes within 1 minute after ingestion of each sample of the aqueous flavor solution before and after the oil-in-water emulsion was applied were evaluated by a well-trained panel of experts using the Time Intensity (TI) method using the sensory evaluation software FIZZ (Biosystemes). The results are shown in FIG. Figure 2 (N=4).

[0146] These results confirmed that even if only the flavor aqueous solution is ingested, the flavor intensity is enhanced when the oil-in-water emulsion is applied to the oral cavity without mixing the flavor components in advance. Figure 2 As shown, it was confirmed that when the flavor aqueous solution is ingested after the oil-in-water emulsion is attached, high values are achieved in terms of the flavor rise immediately after consumption, intensity, intermediate body, and persistence of the aftertaste. This is believed to be due to the flavor components adhering to and accumulating in the attached oil-in-water emulsion, exerting their effects.

[0147] (6) Flavor enhancement effect II by additional use of oil-in-water emulsion

[0148] Each flavor component listed in Table 13 below was added to water in a predetermined amount to prepare a flavor aqueous solution. The flavor aqueous solution was evaluated for each flavor intensity before and after application in the oral cavity at 10% O / W (+) using the same evaluation method as described in (5) above. The evaluation was performed by a well-trained panel of experts using a 10-point scale, with the flavor aqueous solution before application being rated at 5.

[0149] The obtained evaluation results are shown in the following Table 13 (N=2).

[0150] [Table 13]

[0151]

[0152] From the above results, it was confirmed that for all 5 basic tastes, without pre-mixing the components of the taste substances in the aqueous solution of the oil-in-water emulsion, when the oil-in-water emulsion adheres to the oral cavity and only the aqueous solution of the taste substances is ingested, the intensity of the taste is increased.

[0153] (7) Effect of enhancing the flavor of spicy components brought about by the combined use of oil-in-water emulsions

[0154] All of the above 5 basic tastes are perceived through the taste nerves. On the other hand, spiciness, astringency, etc. are not perceived through the taste nerves but through pain sensation and temperature sensation, and thus are distinguished from the components of the above taste substances. Therefore, for components different from the components of the taste substances, it was also confirmed whether the same effect could be obtained by the combined use of oil-in-water emulsions.

[0155] According to the composition of Table 14 below, each component was added and mixed, and an oil-in-water emulsion containing a spicy component in the oil was prepared. As the thickening polysaccharides, xanthan gum, gum arabic, pectin, phosphoric acid cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphoric acid cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose were used. The mixing of each component was carried out at one time, and stirring was carried out for 1 minute at 20,000 rpm using a Polytron homogenizer.

[0156] It should be noted that the amounts of the respective components in the table are expressed as mass % amounts based on setting the amount of the obtained oil-in-water emulsion to 100 mass %.

[0157] Chili oil was used as a control.

[0158] Regarding the evaluation, trained professional reviewers, etc. ingested each sample (10 mL), and evaluated the intensity of each taste on a 10-point scale with the evaluation of the control set to 5. The results are shown in Table 14, and each value shows the average value (N = 3).

[0159] [Table 14]

[0160]

[0161] As a result, it was confirmed that regardless of the type of thickening polysaccharide used, the intensity of spiciness of the oil-in-water emulsion containing a spicy component was increased compared to the control. In addition, it was confirmed that the spiciness of the oil-in-water emulsion containing a spicy component continued for more than 10 minutes after ingestion, but the spiciness felt after ingesting the control disappeared after about 2 minutes.

[0162] From this result, it was confirmed that for components different from the components of the taste substances or components in the oil, the effect (intensity) and persistence can also be improved by the combined use of oil-in-water emulsions.

[0163] (8) Comparative Example

[0164] According to the composition of Table 15 below, each component was added and mixed, and an emulsified composition was prepared. The mixing of each component was carried out by stirring with a Polytron homogenizer at 20,000 rpm for 1 minute.

[0165] At the time of evaluation, it was carried out in groups of Comparative Example A and Comparative Example B. Compared with the emulsified compositions (A-1, B-1) containing no α-cyclodextrin and thickening polysaccharide (xanthan gum), it was confirmed whether a high-intensity salty taste was felt in the emulsified compositions (A-2, B-2).

[0166] Regarding the evaluation, well-trained professional reviewers, etc. (N = 3) ingested each emulsified composition (A-1, B-1) (10 mL), evaluated the intensity of the taste, then rinsed their mouths (gargled with 20 mL of water × 2 times), and then ingested each emulsified composition (A-2, B-2) to evaluate and compare the intensity of the taste.

[0167] [Table 15]

[0168]

[0169] In Comparative Example A, both Comparative Example A-1 and Comparative Example A-2 had a buttery shape and hardly any salty taste was felt. Comparing Comparative Example A-1 with Comparative Example A-2, no difference in the intensity of the salty taste was found between the two.

[0170] In Comparative Example B, the emulsification of Comparative Example B-1 and Comparative Example B-2 was insufficient, and floating oil was confirmed. Both Comparative Example B-1 and Comparative Example B-2 felt a salty taste, but there was no remaining feeling afterwards, and no difference in the intensity of the salty taste was found between the two.

[0171] Experiment 4: Performance Evaluation of Oil-in-Water Emulsion (Enhancement of Hair Care Effect)

[0172] According to the composition of Table 16 below, each component was added and mixed, and an oil-in-water emulsion was prepared. The mixing of each component was carried out at one time, and it was carried out by stirring with a manual stirrer at 20,000 rpm for 10 minutes. It should be noted that the amounts of each component in the table are expressed as mass percentages with the amount of the obtained oil-in-water emulsion being set as 100% by mass.

[0173] [Table 16]

[0174]

[0175] The obtained oil-in-water emulsion was added to a commercial hair conditioner (TSUBAKIPREMIUM MOIST HAIR CONDITIONER (FineToday Holdings Co., Ltd.)) in an amount of 25% by mass to prepare a hair conditioner containing the oil-in-water emulsion. As a control, the commercial hair conditioner without the oil-in-water emulsion was used.

[0176] After washing the hair with shampoo, the hair was thoroughly rinsed with hot water at approximately 40°C. Approximately 10 g of a hair conditioner or a control hair conditioner mixed with an oil-in-water emulsion was applied to the entire hair by hand and allowed to sit for approximately 1 minute. The hair was then thoroughly rinsed with hot water at approximately 40°C, the moisture was removed with a towel, and the hair was dried with a hair dryer. The hair texture was then sensorily evaluated by panelists (N=3).

[0177] As a result, when the control hair conditioner was used, the hair was very smooth and shiny, but there was little aggregation of the hair due to electrostatic repulsion, and frizziness was observed.

[0178] On the other hand, when the hair conditioning agent containing the oil-in-water emulsion was used, the hair felt very smooth and shiny, and furthermore, felt moisturized and well-groomed, with no static frizzing or other issues observed, similar to the case of the control hair conditioning agent. This result is believed to indicate that the inclusion of the oil-in-water emulsion allows the active ingredients in the hair conditioning agent to be further retained on the hair, thereby enhancing and / or maintaining the effects of the active ingredients for a longer period of time. This, in turn, improves the moisturizing effect, reduces the surface potential of the hair that can affect frizzing, and further reduces repulsion between hair strands.

[0179] As described above, the oil-in-water emulsion of the present invention can adhere to a predetermined site, retain the active ingredient, and / or absorb, adsorb, and maintain the active ingredient to cause it to be retained, thereby enhancing and / or maintaining the effect of the active ingredient for a long period of time. As a retention agent for the active ingredient, it is expected to be used in various fields such as food and beverages, pharmaceuticals, and cosmetics.

Claims

1. A retention agent for retaining an active ingredient, comprising: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide.

2. The retention agent according to claim 1, wherein, The hydrophobic substance is one or more selected from the group consisting of oils, hydrophobic waxes, and hydrophobic resins.

3. The retention agent according to claim 1, wherein, The thickening polysaccharide is one or more selected from the group consisting of carboxymethyl cellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind polysaccharide gum, gellan gum, gum arabic, pectin, phosphoric acid cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphoric acid cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose.

4. The retention agent according to claim 1, which is used by adding it to food and drink.

5. The retention agent according to claim 1, which is used by adding it to pharmaceuticals.

6. The retention agent according to claim 1, which is used by adding it to cosmetics.

7. A method for manufacturing a retention agent for retaining an active ingredient, comprising the step of mixing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide to form an oil-in-water emulsion.

8. A food and drink containing a retention agent for retaining an active ingredient, the retention agent comprising: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and the retention agent being 0.5% by mass to 55% by mass based on the amount of its hydrophobic substance.

9. A pharmaceutical containing a retention agent for retaining an active ingredient, the retention agent comprising: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and the retention agent being 0.5% by mass to 55% by mass based on the amount of its hydrophobic substance.

10. A cosmetic containing a retention agent for retaining an active ingredient, the retention agent comprising: an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and the retention agent being 0.5% by mass to 55% by mass based on the amount of its hydrophobic substance.

11. Use of an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide in a method for manufacturing a retention agent for retaining an active ingredient.

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