Retention agent for active ingredients
Patent Information
- Application Number
- JP2023514389
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2022-12-28
- Filing Date
- 2023-02-03
- Publication Date
- 2026-01-27
- Estimated Expiration
- 2043-02-03
AI Technical Summary
There is a need to enhance and prolong the effects of active ingredients in fields such as medicine, cosmetics, and food and beverages, particularly to reduce the content of drugs and taste components for patient comfort and health consciousness.
An oil-in-water emulsion comprising a hydrophobic substance, water, cyclodextrin, and a thickening polysaccharide is used to adhere to and retain active ingredients in animal tissues, enhancing and prolonging their effects.
The emulsion effectively retains active ingredients on tissues, thereby enhancing and prolonging their effects.
Smart Images

Figure 0007806385000017 
Figure 0007806385000018 
Figure 0007806385000001
Abstract
Description
[Technical Field]
[0001] The present invention relates to a retention agent used to retain an active ingredient, comprising an oil-in-water emulsion containing water, a hydrophobic material, a cyclodextrin, and a thickening polysaccharide. [Background technology]
[0002] BACKGROUND ART Nowadays, emulsion compositions comprising fats and oils, water, cyclodextrin, and a water-soluble gelling agent are widely used in various fields such as medicine, cosmetics, and food and beverages.
[0003] Patent Document 1 discloses an emulsion composition containing water, an oily component, α-cyclodextrin, and one or more of agar, low-strength agar, a combination of galactomannan or glucomannan with xanthan gum, carrageenan, furcellaran, gellan gum, and native gellan gum as a gel-forming component, and also discloses pharmaceuticals, cosmetics, and chemical products that use this emulsion composition.
[0004] Patent Document 2 discloses an emulsion composition characterized by containing fats and oils, protein hydrolysates, water, cyclodextrin, etc., and also discloses that gums such as xanthan gum, guar gum, gum arabic (CMC), carrageenan, and locust bean gum may be used as stabilizers.
[0005] Patent Document 3 discloses an emulsified cosmetic product obtained by mixing an aqueous raw material in which a water-soluble polymer compound such as pectin, gum tragacanth, gelatin, casein, sodium alginate, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, sodium polyacrylate, or carboxyvinyl polymer has been dissolved with an oily raw material for cosmetics, and emulsifying the mixture by adding cyclodextrin.
[0006] Patent Document 4 discloses an emulsion composition for skin containing water, oil, cyclodextrin, and at least one water-soluble gelling agent selected from the group consisting of carboxymethylcellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind gum, and gellan gum.
[0007] Non-Patent Document 1 describes that the addition of xanthan gum and tragacanth gum as emulsion stabilizers to an oil-in-water emulsion prepared by emulsifying a 1:1 volumetric ratio sample of soybean oil and an aqueous cyclodextrin solution increases emulsion stability. [Prior art documents] [Patent documents]
[0008] [Patent Document 1] Japanese Patent Application Laid-Open No. 2016-204311 [Patent Document 2] Japanese Patent Application Publication No. 10-262560 [Patent Document 3] Special Publication No. 61-038166 [Patent Document 4] WO2022 / 064997 publication [Non-patent literature]
[0009] [Non-Patent Document 1] Nippon Shokuhin Kogyo Gakkaishi, Vol. 38, No. 1, 16-20 (1991) Summary of the Invention [Problem to be solved by the invention]
[0010] In the fields of medicine, cosmetics, food and beverages, etc., there has long been a strong desire to reduce the content of active ingredients such as drugs and taste components for reasons such as reducing the burden on patients and increasing health consciousness among consumers, and therefore there has been a demand for means that can enhance and / or prolong the effects of the active ingredients. Therefore, an object of the present invention is to provide a new means that can enhance and / or prolong the effects of the active ingredients. [Means for solving the problem]
[0011] As a result of extensive research into solving the above problems, the present inventors have found that an oil-in-water emulsion comprising a hydrophobic substance, water, cyclodextrin, and a thickening polysaccharide can adhere to animal tissues and retain the active ingredient therein, and / or can absorb, adsorb, and retain the active ingredient, thereby allowing it to remain there, thereby enhancing and / or prolonging the effect of the active ingredient in the tissues.
[0012] The present invention is based on these new findings and includes the following inventions. [1] A retention agent used to retain an active ingredient, comprising an oil-in-water emulsion containing water, a hydrophobic material, a cyclodextrin, and a thickening polysaccharide. [2] The retention agent according to [1], wherein the hydrophobic substance is one or more selected from the group consisting of oils and fats, hydrophobic waxes, and hydrophobic resins. [3] A retention agent according to [1] or [2], wherein the thickening polysaccharide is one or more selected from the group consisting of carboxymethylcellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind gum, gellan gum, gum arabic, pectin, phosphate cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphate cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methylcellulose, hydroxypropylmethylcellulose, and hydroxyethylcellulose. [4] A retention agent according to any one of [1] to [3], which is added to food and beverages. [5] A retention agent selected from any of [1] to [3], which is added to a pharmaceutical. [6] A retention agent selected from [1] to [3] and used in cosmetics. [7] A method for producing a retention agent used to retain an active ingredient, comprising the step of mixing water, a hydrophobic substance, a cyclodextrin, and a thickening polysaccharide to form an oil-in-water emulsion. [8] A food or beverage containing a retention agent used to retain an active ingredient, the retention agent including an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, in an amount of 0.5% by mass to 55% by mass of the hydrophobic substance. [9] A pharmaceutical comprising a retention agent used to retain an active ingredient, the retention agent comprising an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, in an amount of 0.5% by mass to 55% by mass of the hydrophobic substance.
[10] A cosmetic product comprising a retention agent used to retain an active ingredient, the retention agent comprising an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, in an amount of 0.5% by mass to 55% by mass of the hydrophobic substance.
[11] Use of an oil-in-water emulsion containing water, a hydrophobic substance, a cyclodextrin, and a thickening polysaccharide in a method for producing a retention agent used to retain an active ingredient. This specification includes the contents described in the specification, etc. of Japanese Patent Application No. 2022-211335, filed on December 28, 2022, which is the priority basis of this application. All publications, patents, and patent applications cited herein are hereby incorporated by reference in their entirety. [Effects of the Invention]
[0013] 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, thereby enhancing and / or prolonging the effect of the active ingredient. [Brief explanation of the drawings]
[0014] [Figure 1] FIG. 1 is a graph showing the results of evaluation of the change in taste intensity over one minute after ingestion of samples prepared by blending components of each taste quality into an aqueous solution of the oil-in-water emulsion of the present invention (1% O / W(+)) and an aqueous solution of a mixture of the components that make up the oil-in-water emulsion (which does not form an oil-in-water emulsion) (1% O / W(-)), using the time intensity (TI) method with the sensory evaluation software FIZZ (Biosystemes) (sweetness: N=4, saltiness / bitterness: N=5, sourness / umami: N=3. Results are shown as average values). [Figure 2] FIG. 2 is a graph showing the results of evaluation of the change in taste intensity over 1 minute after ingesting saline solution before (before application) and after (after application) application of an aqueous solution of the oil-in-water emulsion (10% O / W(+)) according to the present invention to the oral cavity, using the Time Intensity (TI) method with sensory evaluation software FIZZ (Biosystemes) (N=4). DETAILED DESCRIPTION OF THE INVENTION
[0015] 1. Oil-in-water emulsion The oil-in-water emulsion of the present invention contains water, a hydrophobic substance, a cyclodextrin, and a thickening polysaccharide.
[0016] In the present invention, the term "hydrophobic substance" refers to any substance that is insoluble in water and capable of forming an oil-in-water emulsion together with water, a cyclodextrin, and a thickening polysaccharide, as described in detail below. The term is not particularly limited, but preferred examples include fats and oils, hydrophobic waxes, and hydrophobic resins. The hydrophobic substance may be any substance used alone, or different types of hydrophobic substances may be used in combination. For example, the hydrophobic substance may be one or more substances selected from the group consisting of fats and oils, hydrophobic waxes, and hydrophobic resins, and appropriate substances may be selected and used depending on the mode of use of the retention agent of the present invention.
[0017] In the present invention, the term "oil-in-water emulsion" refers to an emulsified composition in which a hydrophobic substance is dispersed in water, and the cyclodextrin and thickening polysaccharides contribute to the formation and stability of this emulsified state.
[0018] In the present invention, the term "oils and fats" refers to oils and fats that are commonly used in the formation of oil-in-water emulsions, and both polar and non-polar oils and fats can be used. Examples of such oils and fats include vegetable-derived oils (e.g., canola oil, rapeseed oil, soybean oil, corn oil, cottonseed oil, peanut oil, sesame oil, rice oil, rice bran oil, camellia oil, safflower oil, olive oil, linseed oil, perilla oil, perilla oil, sunflower oil, palm oil, tea oil, coconut oil, avocado oil, kukui nut oil, grapeseed oil, cocoa butter, coconut oil, wheat germ oil, almond oil, evening primrose oil, castor oil, hazelnut oil, macadamia nut oil, rosehip oil, grapeseed oil). , cocoa oil, jojoba oil, palm kernel oil, etc.), isostearyl alcohol, caprylic alcohol, lauryl alcohol, stearyl alcohol, 2-octadecyl alcohol, myristyl alcohol, cetyl alcohol, phytosterols, cholesterol, stearic acid, isostearic acid, capric acid, lanolinic acid, lauric acid, myristic acid, palmitic acid, behenic acid, linoleic acid, linolenic acid, glyceryl monostearate, glyceryl monopalmitate, mono Glyceryl Behenate, Glyceryl Monomyristate, Glyceryl Monolaurate, Glyceryl Monolanolate, Glyceryl Monolinolenate, Glyceryl Monolinolenate, Glyceryl Monooleate, Glyceryl Triisostearate, Isopropyl Myristate, Glycerol Tri-2-heptylundecanoate, Glycerol Tri-2-ethylhexanoate, 2-Heptylundecyl Palmitate, Di-2-heptylundecyl Adipate, Cetyl Isooctadecyl Examples of the oils include, but are not limited to, synthetic ester oils such as trimethylolpropane-2-trimethylolheptylundecanoate, propane-2-ethylhexanoate, pentaerythritol-2-heptylundecanoate, pentaerythritol-2-ethylhexanoate, cholesterol isostearate, diethyl phthalate, and dibutyl phthalate; animal-derived oils and fats such as beef tallow, lard, lanolin, squalene, and squalane; and silicone oil.The fats and oils used in the present invention are preferably liquid at least at room temperature, and are preferably highly safe animal- or plant-derived fats and oils, with edible vegetable oils that have been used in food and are highly safe being particularly preferred. The fats and oils may be used alone or in combination, and appropriate fats and oils can be selected and used depending on the application of the retention agent of the present invention. In this specification, "room temperature" means 5 to 35°C, preferably 15 to 30°C.
[0019] In the present invention, "hydrophobic wax" refers to natural hydrophobic waxes derived from animals, plants, petroleum, or minerals, as well as synthetic hydrophobic waxes. Those having a melting point of 80°C or less can be used, and those that are liquid at least at room temperature are preferred. Examples of such hydrophobic waxes include, but are not limited to, beeswax, spermaceti wax, wool wax, Japan wax, rosin (pine resin), candelilla wax, carnauba wax, cocoa butter, paraffin wax, microcrystalline wax, ceresin wax, petrolatum wax, ozokenitite wax, polyethylene wax, oxidized polyethylene wax, Fischer-Tropsch wax, alcohol-modified wax, maleic acid-modified oxidized polyethylene wax, and amide wax. Highly safe hydrophobic waxes derived from animals or plants are particularly preferred as the hydrophobic wax used in the present invention. The hydrophobic waxes may be used alone or in combination, and appropriate waxes may be selected and used depending on the application of the retention agent of the present invention.
[0020] In the present invention, the term "hydrophobic resin" refers to a resin that does not have hydrophilic groups or has a small content of hydrophilic groups and is insoluble in polar solvents such as water. In the present invention, those that are in a liquid state at least at room temperature are preferably used. Examples of such hydrophobic resins include, but are not limited to, silicone resins (unhydrophilized), polyurethane resins, fluorine-containing resins, polyethylene resins, polypropylene resins, polyester resins, acrylic resins, polystyrene resins, polycarbonate resins, polyvinyl chloride resins, polysulfone resins, polyethersulfone resins, polyaramid resins, polyamide resins, polyether resins, polyacrylonitrile resins, polyetherimide resins, and copolymers of these polymers. The hydrophobic resins used in the present invention are particularly preferably those that have been confirmed to be biocompatible and biocompatible and are highly safe. The hydrophobic resins may be used alone or in combination, and appropriate ones may be selected and used depending on the intended use of the retention agent of the present invention.
[0021] In the present invention, the "hydrophobic substance" is preferably a fat or oil and a hydrophobic wax, and particularly preferably a fat or oil.
[0022] The oil-in-water emulsion of the present invention can contain a hydrophobic substance in any amount, for example, 1% by mass or more, 3% by mass or more, 5% by mass or more, or 7% by mass or more. The upper limit is not particularly limited, but can be, for example, 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 hydrophobic substance in the oil-in-water emulsion of the present invention can be expressed using two numerical values selected from the above-mentioned lower and upper numerical values. For example, the oil-in-water emulsion of the present invention can contain a hydrophobic substance in an amount appropriately selected from the range 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. If the amount of hydrophobic substance is less than 1% by mass, emulsification may be insufficient, whereas if the amount of hydrophobic substance is more than 50% by mass, the product may feel very sticky or slimy. In either case, the active ingredient may not be retained in the intended application, or the desired feel may not be achieved.
[0023] In this specification, the amount of each component contained in the oil-in-water emulsion of the present invention is expressed in mass % with the total mass of the oil-in-water emulsion being 100 mass %.
[0024] In the oil-in-water emulsion of the present invention, water can be contained in any amount that is capable of emulsifying the hydrophobic substance and forming an oil-in-water emulsion together with the cyclodextrin and thickening polysaccharide. 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 of the water content is not particularly limited, but can be, for example, 90% by mass or less or 85% by mass or less. The range of the amount of water in the oil-in-water emulsion of the present invention can be expressed using two numerical values selected from the above-mentioned lower and upper limits, respectively. For example, the oil-in-water emulsion of the present invention can contain water in an amount appropriately selected from the range of 15% by mass to 90% by mass, 45% by mass to 90% by mass, or 70% by mass to 85% by mass. The amount of water contained in the oil-in-water emulsion of the present invention is preferably greater than the amount of hydrophobic substance in terms of volume ratio, and for example, the content of hydrophobic substance to water can be greater than 1:1 in terms of volume ratio (hydrophobic substance:water), for example, 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, and the upper limit of the amount of water is not particularly limited, but can be 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 within the above ranges, stickiness, sliminess, etc. can be suppressed.
[0025] "Cyclodextrin" refers to a cyclic non-reducing maltooligosaccharide whose constituent unit is glucose, and examples thereof include α-cyclodextrin, which has 6 glucose units, β-cyclodextrin, which has 7 glucose units, and γ-cyclodextrin, which has 8 glucose units. In the present invention, α-, β-, and γ-cyclodextrin, as well as derivatives thereof, and any combination thereof may be used. Examples of cyclodextrin derivatives include, but are not limited to, ethyl cyclodextrin, methyl cyclodextrin, hydroxyethyl cyclodextrin, hydroxypropyl cyclodextrin, methylamino cyclodextrin, amino cyclodextrin, carboxyethyl cyclodextrin, carboxymethyl cyclodextrin, sulfoxyethyl cyclodextrin, sulfoxyl cyclodextrin, acetyl cyclodextrin, branched cyclodextrin, cyclodextrin fatty acid ester, glucosyl cyclodextrin, and maltosyl cyclodextrin. α-Cyclodextrin is preferred. α-Cyclodextrin is highly soluble in water, allowing the preparation of oil-in-water emulsions with minimal graininess.
[0026] The cyclodextrin in the oil-in-water emulsion of the present invention can be contained in an amount that contributes to the emulsification and stability of the oil-in-water emulsion together with the thickening polysaccharide and that allows the desired feel when used in the intended application. For example, the oil-in-water emulsion of the present invention contains cyclodextrin 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 of the amount is not particularly limited, and can be, for example, 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 expressed using two numerical values selected from the above-mentioned lower and upper limits, respectively. For example, the oil-in-water emulsion of the present invention can contain cyclodextrin in an amount appropriately selected from the range of 0.5% by mass to 15% by mass, for example, 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. If the amount of cyclodextrin is less than 0.5% by mass, the emulsification and stability of the oil-in-water emulsion may be insufficient, whereas if the amount is more than 15% by mass, the oil-in-water emulsion may become too viscous or have a strong squeaky feeling. In either case, the active ingredient may not be retained or the desired feel may not be obtained when used in the intended application.
[0027] In the present invention, "thickening polysaccharide" generally refers to a polysaccharide that dissolves in water and imparts viscosity (sometimes also referred to as a thickening stabilizer, water-soluble paste, etc.). Thickening polysaccharides that can be used in the present invention include ingredients that are commonly used in the production of foods and beverages, pharmaceuticals (including quasi-drugs), cosmetics, etc., and are not particularly limited. Any thickening polysaccharide may be used alone, or different thickening polysaccharides may be used in combination, and appropriate ones can be selected and used depending on the usage mode of the retention agent of the present invention. In the present invention, the "thickening polysaccharide" preferably includes carboxymethylcellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind gum, gellan gum, gum arabic, pectin, phosphate cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphate cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, and the like, and any of these may be used alone or two or more different types may be used in combination.
[0028] In the present invention, the "thickening polysaccharide" is more preferably carboxymethylcellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind gum, or gellan gum, and even more preferably carboxymethylcellulose (CMC), glucomannan, tamarind gum, or xanthan gum. These thickening polysaccharides can particularly impart high emulsion stability to the oil-in-water emulsion of the present invention.
[0029] The thickening polysaccharide in the oil-in-water emulsion of the present invention can be contained in an amount that contributes to the emulsification and stability of the oil-in-water emulsion together with cyclodextrin and that allows the desired feel when used in the intended application. For example, the oil-in-water emulsion of the present invention contains the thickening polysaccharide 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, with the upper limit not being particularly limited, but can be, for example, 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 thickening polysaccharide in the oil-in-water emulsion of the present invention can be expressed using two numerical values selected from the above-mentioned lower and upper limits, respectively. For example, the oil-in-water emulsion of the present invention can contain thickening polysaccharide in an amount appropriately selected from the range of 0.05% to 1% by mass, 0.1% to 1% by mass, 0.2% to 0.8% by mass, or 0.2% to 0.5% by mass. If the amount of thickening polysaccharide is less than 0.05% by mass, the emulsification and stability of the oil-in-water emulsion may be insufficient. On the other hand, if the amount is more than 1% by mass, the viscosity of the oil-in-water emulsion may be too high. In either case, it may be impossible to retain the active ingredient or obtain the desired feel when used in the intended application.
[0030] In the oil-in-water emulsion of the present invention, the emulsification and stability of the oil-in-water emulsion are imparted by the combined use of the cyclodextrin and the thickening polysaccharide. The emulsification and stability of the oil-in-water emulsion imparted by the combined use of the cyclodextrin and the thickening polysaccharide do not depend on the three-dimensional matrix gel formed by dissolving a typical gelling agent in water and cooling (preferably, does not include a three-dimensional matrix gel). Rather, as will be described in detail in the Examples below, it is believed to be due to the presence of hydrogen-bonding interactions between the cyclodextrin and the thickening polysaccharide. Furthermore, since the oil-in-water emulsion of the present invention is emulsified and stable by the combined use of the cyclodextrin and the thickening polysaccharide, it may be substantially free of emulsifiers commonly used in the production of conventional emulsion compositions, and preferably is substantially free of such emulsifiers. In the present invention, "substantially free of emulsifiers" means that the oil-in-water emulsion of the present invention does not contain an emulsifier in a form that exerts an emulsifying effect, and does not intend that no emulsifier is contained at all. By being substantially free of emulsifiers, the present invention can obtain an advantageous oil-in-water emulsion that is highly safe, for example, with low irritation and low allergenicity, when the oil-in-water emulsion of the present invention is applied. Examples of "emulsifiers commonly used in the production of conventional emulsion compositions" include, but are not limited to, proteins, peptides or hydrolysates thereof, glycerin fatty acid esters, organic acid monoglycerides, polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, sorbitan fatty acid esters, propylene glycol fatty acid esters, polyoxyethylene fatty acid esters, polyglycerin condensed ricinoleic acid esters, sorbitan fatty acid esters, polyoxyethylene sorbit fatty acid esters, sucrose fatty acid esters, lecithin, enzymatically hydrolyzed lecithin, polyethylene glycol, and polypropylene glycol.
[0031] The form of the oil-in-water emulsion of the present invention is not particularly limited. In addition to forms having the above-mentioned water contents, the emulsion can be provided in the form of a semi-solid / semi-liquid (gel, sol, etc.) or a dried form (e.g., powder, flakes, etc.) prepared by reducing the water content. Such semi-solid / semi-liquid (gel, sol, etc.) or dried form (e.g., powder, flakes, etc.) can be obtained by obtaining an oil-in-water emulsion having the above-mentioned water content and then subjecting it to a conventionally known drying method to reduce the water content of the oil-in-water emulsion. Examples of such drying methods include, but are not limited to, freeze drying, heat drying, air drying, spray drying, drum drying, hot air drying, and vacuum drying. The water content of the oil-in-water emulsion after drying can be appropriately selected depending on the desired form. In the case of a dried form, the water content can be, for example, 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 drying is not particularly limited, and may be 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 in the dried form can be expressed using two numerical values selected from the above upper and lower numerical values. For example, the water content of the oil-in-water emulsion can be 0% by mass to less than 15% by mass, more than 0% by mass to less than 15% by mass, 0.1% by mass to less than 15% by mass, 0.1% by mass to 10% by mass, 0.5% by mass to 5% by mass, 0.5% by mass to 1% by mass, 0.6% by mass to 1% by mass, 0.7% by mass to 1% by mass, or 0.8% by mass to 1% by mass. The oil-in-water emulsion of the present invention after being subjected to a drying means does not undergo a phase transition to form a water-in-oil emulsion, and in particular, the dried form has high heat resistance and moisture resistance, and does not discolor or dissolve even after being subjected to high temperature conditions (e.g., about 100°C to 200°C) and / or high humidity conditions (e.g., about 95% humidity).
[0032] In addition to the above components, the oil-in-water emulsion of the present invention may further contain, as needed, ingredients commonly used in the production of intended uses such as foods and beverages, pharmaceuticals (including quasi-drugs), and cosmetics (hereinafter referred to as "other ingredients") in amounts appropriate to the desired use form, provided that the effects of the present invention are not impaired. Examples of such other ingredients include, but are not limited to, excipients, disintegrants, lubricants, binders, diluents, buffers, suspending agents, thickeners, preservatives, antibacterial agents, antiseptics, antioxidants, UV absorbers, colorants, pigments, dyes, pigments, lubricants, plasticizers, solvents, solubilizers, isotonicity agents, flavorings, vitamins, surfactants, pH adjusters, and chelating agents.
[0033] The oil-in-water emulsion of the present invention can be produced by mixing and stirring the water, hydrophobic substance, cyclodextrin, thickening polysaccharide, and other ingredients, as needed, in the amounts described above. All of the ingredients may be mixed and stirred together, or the ingredients may be added separately or in any combination sequentially (in any order) and mixed and stirred. The oil-in-water emulsion obtained by mixing and stirring may be subjected to heat sterilization.
[0034] Furthermore, the oil-in-water emulsion obtained by mixing and stirring may be further subjected to drying means, if necessary. Drying means can be carried out by the conventionally known drying means described above, and the water content of the oil-in-water emulsion can be appropriately adjusted depending on the desired shape of the semi-solid / semi-liquid (gel, sol, etc.) or dried product. The obtained dried product can be further subjected to crushing, pulverization, or grinding treatment, if necessary, to form powder, flakes, etc. The oil-in-water emulsion obtained by drying means may be mixed and stirred with other components in the amounts described above, if necessary, and / or may be subjected to heat sterilization treatment.
[0035] 2.Applications The oil-in-water emulsion of the present invention can be used as a retention agent for retaining an active ingredient.
[0036] In the present invention, a "retention agent" is an agent that can retain or maintain an active ingredient at a predetermined site for a longer period of time, thereby enabling the effect of the active ingredient to be enhanced and / or maintained for a longer period of time compared to when the retention agent is not used. When the retention agent of the present invention is administered or ingested together with an active ingredient to an animal, the oil-in-water emulsion adheres to the tissue at the application site, where it retains the active ingredient and / or absorbs and adsorbs the active ingredient and retains it, thereby enabling the effect of the active ingredient to be enhanced and / or maintained for a longer period of time compared to when the retention agent is not used.
[0037] In the present invention, the term "animal" is not particularly limited and may refer to any animal, but is preferably a mammal, such as (but not limited to) humans, livestock animals (cows, horses, sheep, pigs, goats, etc.), and pets (dogs, cats, rabbits, hamsters, guinea pigs, etc.), more preferably humans.
[0038] In the present invention, "tissue" refers to various epithelial tissues found in the skin, oral cavity, esophagus, anus, vagina, nasal cavity, trachea, bronchi, stomach, small intestine, large intestine, fallopian tube, uterus, pleura, peritoneum, vascular endothelium, alveoli, thyroid gland (follicles), renal tubules, ureter, bladder, etc., as well as hair, nails, teeth, etc., and can be appropriately selected depending on the intended application site. In the present invention, "epithelial tissue" preferably refers to various epithelial tissues found in the skin, oral cavity, esophagus, nasal cavity, trachea, bronchi, etc., and more preferably refers to epithelial tissue within the oral cavity.
[0039] In the present invention, "administered or ingested together with an active ingredient" means that the oil-in-water emulsion of the present invention and the active ingredient are administered or ingested within a time period that allows them to coexist in the tissue at the application site. For example, the oil-in-water emulsion of the present invention and the active ingredient may be administered or ingested simultaneously in a single composition, or they may be administered or ingested in separate forms and / or via separate administration routes, simultaneously or one after the other (preferably, the order of the oil-in-water emulsion of the present invention, followed by the active ingredient). "Administration" is sufficient as long as it delivers the oil-in-water emulsion of the present invention and the active ingredient to the tissue at the application site, and can be appropriately selected depending on the form and amount of the oil-in-water emulsion of the present invention and the active ingredient. For example, "administration" includes, but is not limited to, oral administration, spray administration, inhalation, nasal administration, buccal administration, rectal administration, transdermal administration, and application. Preferably, "administration" is oral administration, spray administration, inhalation, buccal administration, or application.
[0040] In the present invention, the "active ingredient" may be a water-soluble ingredient or an ingredient having affinity for the above-mentioned hydrophobic substance (e.g., lipophilic ingredient, etc.). It is believed that the water-soluble ingredient is retained in the water in the oil-in-water emulsion of the present invention, preferably by bonding (e.g., hydrogen bonding) with the thickening polysaccharide and / or cyclodextrin. On the other hand, it is believed that the ingredient having affinity for the above-mentioned hydrophobic substance is retained in the hydrophobic substance in the oil-in-water emulsion of the present invention. The "active ingredient" in the present invention may be any ingredient that contributes to the taste of food or drink (salty ingredients such as sodium chloride and potassium chloride; sweet ingredients such as sugars (glucose, fructose, sucrose, maltose, oligosaccharides, isomerized sugar, etc.), sugar alcohols (xylitol, sorbitol, glycerin, erythritol, etc.), natural sweeteners (stevia, glycyrrhizin, thaumatin, etc.), artificial sweeteners (aspartame, acesulfame potassium, sucralose, etc.), etc. Flavor components: sour components such as citric acid, succinic acid, lactic acid, tartaric acid, acetic acid, fumaric acid, malic acid, gluconic acid, and ascorbic acid; umami components such as glutamic acid, inosinic acid, and guanylic acid; alkaloids (caffeine, quinine, strychnine, theobromine, etc.), terpenes (limonoids, limonin, obacunone, nomilin, cucurbitacin, humulone, lupulone, etc.), glycosides (terpene glycosides, flavanone glycosides, nari Examples of the active ingredient include (but are not limited to) amino acids (tryptophan, phenylalanine, trypsin, arginine, valine, leucine, isoleucine, proline, etc.), bitter components such as casein and soy protein; pungent components such as capsaicin, piperine, sanshool, shogaol, gingerol, diallyl disulfide, p-hydroxybenzyl isothiocyanate; and astringent components such as tannins, catechin, theaflavin, and thearubigin), as well as food ingredients, seasonings, spices, etc. containing these ingredients, and ingredients used for specified treatments and purposes in pharmaceuticals (including quasi-drugs) and cosmetics (hereinafter referred to as "pharmaceuticals, etc.") (for example, but not limited to, drugs, disinfectants, antibacterial agents, antibiotics, enzymes, antibodies, vitamins, minerals, amino acids, cooling agents, deodorants, moisturizers, fragrances, etc.).
[0041] The retention agent of the present invention can be added to foods, beverages, pharmaceuticals, etc. to retain the active ingredients of the foods, beverages, pharmaceuticals, etc. The amount of the retention agent added may be any amount that can retain or maintain the active ingredients of the foods, beverages, pharmaceuticals, etc. in a predetermined location for a longer period than when the retention agent is not used, thereby enhancing and / or prolonging the effect of the active ingredient, and can be appropriately determined depending on the type and amount of the active ingredient and the type and form of the foods, beverages, pharmaceuticals, etc. For example, the retention agent of the present invention can be contained in foods, beverages, pharmaceuticals, etc. 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, calculated based on the amount of the hydrophobic substance. The upper limit of the amount is not particularly limited, and can be, for example, 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 foods, beverages, pharmaceuticals, etc. can be expressed using two numerical values selected from the above-mentioned lower and upper limits, and for example, the retention agent of the present invention can be contained in foods, beverages, pharmaceuticals, etc. 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 hydrophobic substance. If the amount of the retention agent of the present invention contained in foods, beverages, pharmaceuticals, etc. is less or more than the above range, it may not be possible to retain the active ingredient in the form of use for the intended application.
[0042] In this specification, the amount of each component contained in a food, drink, medicine, etc. is expressed in mass %, where the total mass of the liquid portion excluding the solution or solid portion of the food, drink, medicine, etc. (for example, in the case of a food, drink, the amount of the liquid portion such as sauce or soup excluding ingredients) is taken as 100 mass %. When the food, drink, medicine, etc. is in a liquid form or in a form without a liquid portion, the amount can be the amount in a solution prepared by adding / adding to an appropriate solvent (for example, water, hot water, physiological saline, buffer solution, etc.) at the time of administration or ingestion, or in a solution in which the food, drink, medicine, etc. is dissolved in water in the tissue at the application site (for example, body fluids such as saliva).
[0043] Foods, beverages, pharmaceuticals, etc. may contain the retention agent of the present invention and the active ingredient together (for example, they may be contained in a single composition), or the retention agent of the present invention and the active ingredient may be in separate forms (for example, they may be contained in two or more compositions that are administered or ingested together).
[0044] The form of the food, beverage, pharmaceutical, etc. can be appropriately selected depending on the form of use in the intended application (e.g., the form of a specified product, etc.), and can take any form, including, but not limited to, solid, powder, granules, flakes, chewable tablets, sheets, films, chewing gums, liquids, emulsions, semi-solid / semi-liquid (gels, sols, creams, pastes, mousses, etc.), soft capsules, etc. However, it is preferable that the retention agent of the present invention coexists with the active ingredient in the tissue at the application site in an amount within the above-mentioned range. Depending on the form, the food, beverage, pharmaceutical, etc. can be administered or ingested after adding / adding an appropriate solvent (e.g., water, hot water, physiological saline, buffer solution, etc.) to adjust the content of the retention agent of the present invention in the food, beverage, pharmaceutical, etc. to the above-mentioned range (such forms of food, beverage, pharmaceutical, etc. include, but are not limited to, solids, powders, granules, flakes, liquids, emulsions, semi-solid / semi-liquid (gels, sols, creams, pastes, mousses, etc.)). Alternatively, the food, beverage, medicine, etc. may be allowed to act by dissolving the retention agent of the present invention and the active ingredient 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 may be set within the above-mentioned range (such forms of food, beverage, medicine, etc. include, but are not limited to, powder, granules, chewable tablets, sheets, films, chewing gum, etc.).
[0045] In addition to the retention agent and active ingredient of the present invention, foods, beverages, pharmaceuticals, etc., can further contain, as needed, ingredients commonly used in the production of the intended use form (e.g., the form of a specified product, etc.) in amounts appropriate to the desired use form, within a range that does not impair the effects of the present invention. Examples of such ingredients include, but are not limited to, excipients, disintegrants, lubricants, binders, diluents, buffers, suspending agents, thickeners, preservatives, antibacterial agents, antiseptics, antioxidants, UV absorbers, colorants, pigments, dyes, pigments, lubricants, plasticizers, solvents, solubilizers, isotonicity agents, flavorings, fragrances, sweeteners, taste components, acidulants, seasonings, humectants, vitamins, surfactants, chelating agents, antibacterial agents, emulsifiers, water-soluble organic solvents, and foodstuffs.
[0046] In one embodiment, the retention agent of the present invention is provided as a food or beverage. When the food or beverage is consumed, the oil-in-water emulsion in the retention agent of the present invention adheres to the epithelial tissue in the oral cavity, where it retains the active ingredients ingested therein, such as taste components, and / or absorbs and adsorbs the taste components and retains them, thereby retaining them. This allows the effects of the active ingredients (e.g., the flavor and taste brought about by the taste components) to be enhanced and / or maintained for a longer period of time than when the retention agent is not used. The retention agent of the present invention in this usage embodiment may also be referred to as a flavor enhancer or taste enhancer.
[0047] In another embodiment, the "retention agents" of the present invention are provided in oral care products. By placing the product in the mouth, the oil-in-water emulsion in the retention agent of the present invention adheres to the epithelial tissues in the oral cavity, where it releases the active ingredients of the drugs administered thereto (for example, caries prevention / restoration agents (cetylpyridinium chloride (CPC), benzalkonium chloride, benzethonium chloride (BTC), sodium fluoride, sodium monofluorophosphate, etc.), gingivitis / periodontitis prevention / improvement agents (ε-aminocaproic acid, isopropylmethylphenol (cymen-5-ol), allantoin, dipotassium glycyrrhizinate, β-glycyrrhetinic acid, cetylpyridinium chloride (CPC), hinokitiol, triclosan, tranexamic acid, benzalkonium chloride, benzethonium chloride (BTC), triclosan, sodium chloride, tocopherol acetate, etc.), stomatitis prevention / improvement agents (allantoin, glycyrrhizinic acid, tranexamic acid, etc.), and hypersensitivity prevention / suppression agents (aluminum lactate, potassium nitrate, etc.)). By retaining and / or absorbing / adsorbing and retaining drugs, the effect of the drug can be enhanced and / or maintained for a longer period of time compared to when the retention agent is not used, and the effect of the drug can be enhanced and / or maintained for a longer period of time compared to when the retention agent is not used. Such oral care products may be in conventionally known forms, such as mouth rinses, mouthwashes, liquid dentifrices, toothpastes, powdered dentifrices, gels, films, chewing gums, sprays, liquids, etc.
[0048] In another embodiment, the "retention agent" of the present invention is provided as being contained in a hair care product. By applying the product to hair, the oil-in-water emulsion in the retention agent of the present invention adheres to the hair, and the co-administered active ingredients, 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, dimethicone, amodimethicone, polyquaternium-10, chitosan, etc.), hair quality improving ingredients (stearyltrimonium bromide, cetrimonium bromide, stearyltrimonium chloride, etc.), hair repair ingredients (olive oil, jojoba oil, avocado oil, squalane, isopropyl myristate, isostearyl alcohol, oleyl alcohol, egg yolk fatty oil, adsorbed refined lanolin, soybean extract, etc.), and the like, are then absorbed into the hair. The retention agent retains and / or absorbs or adsorbs and retains active ingredients, such as (but not limited to) 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 purified lanolin, soybean sterol, cholesterol, ceramide, etc.), and the effects of the active ingredients can be enhanced and / or maintained for a longer period of time compared to when the retention agent is not used. Such hair care products can be in the conventional, general forms known in the art, such as shampoos, rinses, conditioners, treatments, etc.
[0049] The present invention will be described below with reference to examples, but the present invention is not limited to these examples. [Example]
[0050] Experiment 1: Evaluation of emulsion stability of oil-in-water emulsions (1) Preparation of oil-in-water emulsion Oil-in-water emulsions were prepared by adding and mixing each ingredient according to the composition in Table 1. Oil (canola oil) was used as the hydrophobic substance, and the thickening polysaccharides used were carboxymethylcellulose (CMC), glucomannan, guar gum, κ-carrageenan, tamarind gum, gellan gum, xanthan gum, ι-carrageenan, locust bean gum, and λ-carrageenan, and as a control, either a carboxyl vinyl polymer or sodium polyacrylate, which are non-polysaccharide thickeners.
[0051] Each component was mixed at once and stirred using a hand blender at 20,000 rpm for 10 minutes. Each resulting oil-in-water emulsion (50 mL) was transferred to a conical tube (Falcon® conical tube 50 mL) and centrifuged at 3,000 rpm for 1 minute. The thickness (depth) of the aqueous phase, micelles, and oil phase was then visually observed, and the proportion (%) of each phase was measured to evaluate the emulsion stability of each composition. Evaluation was performed using a 100% micelle proportion as "◎," a micelle proportion of 70% or more but less than 100% as "◯," and a micelle proportion of less than 70% as "×."
[0052] The amount of each component in the tables below is shown in mass % with the amount of the obtained oil-in-water emulsion being 100 mass %. Food additives (food grade) were used for the fats and oils, α-cyclodextrin, and thickening polysaccharides.
[0053] [Table 1]
[0054] (2) Results The thickening polysaccharides added to the oil-in-water emulsions, the measured proportions of each phase, and the evaluation results are shown in Table 2. Oil-in-water emulsions can be formed by adding and mixing thickening polysaccharides with water, hydrophobic substances, and α-cyclodextrin. As is clear from the results above, when carboxymethylcellulose (CMC), glucomannan, guar gum, κ-carrageenan, tamarind gum, gellan gum, xanthan gum, ι-carrageenan, locust bean gum, or λ-carrageenan was used as the thickening polysaccharide, the micellar phase of the oil-in-water emulsion was maintained even under the above conditions, demonstrating particularly high emulsion stability. In particular, when CMC, glucomannan, tamarind gum, or xanthan gum was added, no separation of the aqueous and oil phases was observed, demonstrating significantly high emulsion stability. On the other hand, it was confirmed that the addition of a non-polysaccharide thickener resulted in significant separation of the aqueous and oil phases under the above conditions, resulting in relatively low emulsion stability.
[0055] [Table 2]
[0056] Each component was added and mixed according to the composition shown in Table 3 below to prepare an oil-in-water emulsion. The hydrophobic substance used was either carnauba wax, petrolatum wax (white petrolatum), rosin, or silicone oil, containing 1% of Oil Red, and xanthan gum was used as the thickening polysaccharide. The amount of each component in the table is shown in % by mass, with the amount of the resulting oil-in-water emulsion being 100% by mass.
[0057] The components were mixed and stirred in the same manner as above, and the resulting oil-in-water emulsions (50 mL) were transferred to conical tubes (Falcon® conical tubes, 50 mL) and centrifuged at 3,000 rpm for 1 minute. The thicknesses (depths) of the aqueous, micelle, and oil phases were then visually observed, and the proportions (%) of each phase were measured. The emulsion stability of each composition was evaluated in the same manner as above.
[0058] [Table 3]
[0059] The hydrophobic substances added to the oil-in-water emulsions, the measured proportions of each phase, and the evaluation results are shown in Table 4. These results confirm that oil-in-water emulsions can be formed using not only oils and fats but also other hydrophobic substances, and that the micellar phase of the oil-in-water emulsion is maintained even under the above conditions, resulting in high emulsion stability.
[0060] [Table 4]
[0061] Experiment 2: Evaluation of the interaction between α-cyclodextrin and thickening polysaccharides in oil-in-water emulsions To evaluate the interaction between α-cyclodextrin and polysaccharide thickeners in aqueous solution, the enthalpy change (ΔH) was determined by isothermal titration calorimetry (ITC) according to a conventional method. Specifically, using an isothermal titration calorimeter (NANO ITC SV; TA Instruments), 10 μL of a polysaccharide thickener solution (0.05 g / 100 mL) was added dropwise to an α-cyclodextrin aqueous solution (25 g / 100 mL) every 180 seconds for 25 times (75 min), and the enthalpy value (μJ) was calculated from the area of the 25th (final) titration peak. As controls, enthalpy values (μJ) were similarly determined using non-polysaccharide thickeners, carboxyl vinyl polymer and sodium polyacrylate.
[0062] The results are shown in Table 5. When thickening polysaccharides (CMC and xanthan gum), which demonstrated particularly high emulsion stability in Experiment 1, were used, a positive enthalpy value, i.e., an endothermic reaction, was observed. This result suggests the existence of an interaction between the thickening polysaccharide and α-cyclodextrin via hydration water. For example, it is thought that some of the water molecules hydrated in the thickening polysaccharide form hydrogen bonds with α-cyclodextrin. Typically, hydrogen bonds formed between water molecules are shorter in distance and have a higher energy value than hydrogen bonds formed between thickening polysaccharides and α-cyclodextrin, which are caused by intermolecular repulsion due to charged sites. Therefore, when some of the water molecules hydrated in the thickening polysaccharide form hydrogen bonds with α-cyclodextrin, it is thought that an endothermic reaction occurs as a result of the subtraction of energy values. The heat transfer (positive enthalpy value) suggests the existence of an interaction between the thickening polysaccharide and α-cyclodextrin, and this interaction is thought to be the factor that produces high emulsion stability in the oil-in-water emulsion in Experiment 1 above.
[0063] [Table 5]
[0064] Experiment 3: Performance evaluation of oil-in-water emulsions (flavor enhancement) (1) Taste evaluation of the oil-in-water emulsion itself An oil-in-water emulsion was prepared by adding and mixing each component according to the composition in Table 6. Each component was mixed at once and stirred at 20,000 rpm for 10 minutes using a hand blender.
[0065] The amount of each component in the table is shown in mass % with the amount of the obtained oil-in-water emulsion being 100 mass %.
[0066] As a control, a mixture was used which was prepared by mixing ingredients other than oil and fat according to the composition in Table 6 below, then adding oil and fat, and mixing by hand without applying shear force (i.e., not forming an oil-in-water emulsion).
[0067] The obtained oil-in-water emulsion and the control mixture were each added to water in an amount of 1% by mass, and the presence or absence of flavor in each solution was evaluated by a panel of well-trained experts through sensory testing.
[0068] [Table 6]
[0069] As a result, neither the oil-in-water emulsion nor the control mixture had any noticeable difference in odor compared to plain water.
[0070] When the control mixture was ingested, a slight thickening sensation due to the oil was felt compared to water, but no difference in taste was detected.
[0071] When the oil-in-water emulsion was ingested, it felt like the entire oral cavity was more widely covered (as if the oil-in-water emulsion was adhering) than when water was ingested, but no difference in taste was detected.The amount of oil contained in the 1% by mass oil-in-water emulsion solution was only about 0.13% by mass, and it was confirmed that there was no detectable taste or smell derived from the oil.
[0072] (2) Flavor enhancement effect of oil-in-water emulsion To the 1% by mass oil-in-water emulsion solution obtained above and the 1% by mass control mixture solution, a predetermined amount of each taste component listed in Table 7 below was added to each solution to prepare samples for flavor evaluation (hereinafter, the sample containing 1% by mass oil-in-water emulsion solution will be referred to as "1% O / W(+)", and the sample containing 1% by mass control mixture solution will be referred to as "1% O / W(-)"). Furthermore, as a control, an aqueous solution in which only the same amount of each taste component was added to water (hereinafter, referred to as "control aqueous solution") was used.
[0073] Each sample (10 mL) was ingested in the order shown in Table 7 below, and the intensity of each taste was evaluated by a panel of well-trained experts on a 10-point scale, with the control aqueous solution being given a rating of 5. Rinsing was performed twice with 20 mL of water.
[0074] [Table 7]
[0075] The evaluation results for the intensity of each taste for each sample are shown in Table 8 below (sweetness, umami, sourness, bitterness: N=4, saltiness: N=3).
[0076] [Table 8]
[0077] These results confirmed that the inclusion of taste components in an oil-in-water emulsion (1% O / W(+)) significantly enhanced the intensity of each taste. When taste components were included in a mixture that did not form an oil-in-water emulsion (1% O / W(-)), a slight increase in taste intensity was also observed, but the degree of this increase was slight.
[0078] Furthermore, for the 1% O / W(+) and 1% O / W(-) samples, the change in taste intensity over one minute after ingestion was evaluated by well-trained expert panelists using the time intensity (TI) method with the sensory evaluation software FIZZ (Biosystemes). The results are shown in Figure 1 (sweetness: N=4, saltiness / bitterness: N=5, sourness / umami: N=3; the results in Figure 1 represent the average of the results for each panelist).
[0079] The results in Figure 1 confirm that, compared to 1% O / W(-), 1% O / W(+) achieved higher values in one or more of the following: onset of each flavor immediately after ingestion, intensity, thickness of the middle note, and persistence of the aftertaste.
[0080] (3) Flavor enhancement effect of oil-in-water emulsion II Oil-in-water emulsions were prepared by adding and mixing the ingredients according to the formulations in Table 9. The thickening polysaccharides used were xanthan gum, gum arabic, pectin, phosphate cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphate cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose. The ingredients were mixed together and stirred at 20,000 rpm for 10 minutes using a hand blender.
[0081] The amount of each component in the table is shown in mass % with the amount of the obtained oil-in-water emulsion being 100 mass %.
[0082] As a control, a mixture was used which was prepared by mixing ingredients other than oil and fat according to the composition in Table 9 below, then adding oil and fat, and mixing by hand without applying shear force (i.e., not forming an oil-in-water emulsion).
[0083] [Table 9]
[0084] The resulting oil-in-water emulsion and the control mixture were each added to water in an amount of 1% by mass to prepare a 1% by mass oil-in-water emulsion solution and a 1% by mass control mixture solution. Salt was added to each solution in an amount of 0.6% by mass to prepare samples for flavor evaluation (hereinafter, the sample containing 1% by mass of the oil-in-water emulsion solution will be referred to as "1% O / W(+)," and the sample containing 1% by mass of the control mixture solution will be referred to as "1% O / W(-)"). An aqueous solution prepared by adding salt to water in an amount of 0.6% by mass was also used as a control aqueous solution.
[0085] Each sample (10 mL) was ingested in the order shown in Table 7, and the intensity of each taste was evaluated by a panel of well-trained experts on a 10-point scale, with the control aqueous solution being rated as 5. Rinsing was performed twice with 20 mL of water.
[0086] The evaluation results for the intensity of each taste of each sample are shown in Table 10 below (N=3).
[0087] [Table 10]
[0088] From the above results, it was confirmed that regardless of the type of thickening polysaccharide used, the taste intensity was significantly increased by including an oil-in-water emulsion (1% O / W(+)).
[0089] (4) Flavor enhancement by combined and repeated ingestion of oil-in-water emulsion The subjects were given 1% O / W(+) containing taste components (0.6% by mass of salt or 0.2% by mass of caffeine) prepared in the same manner as in (2) above, and 10 mL of each was taken four times consecutively (without rinsing), and the intensity of each taste was evaluated on a 10-point scale, with the first intake being evaluated as 5. The evaluation was carried out by well-trained expert panelists.
[0090] The evaluation results for the intensity of each taste of each sample are shown in Table 11 below (salty: N=4, bitter: N=3).
[0091] [Table 11]
[0092] These results confirmed that in all cases, repeated ingestion of samples containing oil-in-water emulsions gradually increased the intensity of the taste, which is thought to be due to the fact that the taste components adhere to and accumulate in the oral cavity along with the oil-in-water emulsion.
[0093] (5) Effect of flavor enhancement by separate use of oil-in-water emulsion I The oil-in-water emulsions prepared in (1) above were each added to water in an amount of 10% by mass to obtain a 10% by mass aqueous solution of the oil-in-water emulsion that did not contain flavor components (hereinafter referred to as "10% O / W(+)"). A 0.6% by mass saline solution was used as the aqueous solution to which the flavor components were added (hereinafter referred to as "aqueous flavor solution").
[0094] For the evaluation, the taste solution (10 mL) was ingested, and the taste intensity was evaluated (before application), followed by mouth rinsing (rinsing twice with 20 mL of water). Next, 10 mL of 10% O / W(+) was held in the mouth for 30 seconds, allowed to adhere to the oral cavity, then spat out, the mouth was rinsed (rinsing twice with 20 mL of water), and then the taste solution (10 mL) was ingested again and the taste intensity was evaluated (after application). The evaluation was carried out by well-trained expert panelists on a 10-point scale, with 5 being the rating of the taste solution before application.
[0095] The evaluation results obtained are shown in Table 12 below (N=4).
[0096] [Table 12]
[0097] Furthermore, for the taste solutions before and after application of the oil-in-water emulsion, the change in taste intensity over 1 minute after ingestion of each sample was evaluated by well-trained expert panelists using the Time Intensity (TI) method with the sensory evaluation software FIZZ (Biosystemes). The results are shown in Figure 2 (N=4).
[0098] These results confirmed that the intensity of the taste was enhanced simply by applying the oil-in-water emulsion to the oral cavity without premixing the taste components into the oil-in-water emulsion solution. Furthermore, as shown in Figure 2, when the taste aqueous solution was ingested after applying the oil-in-water emulsion, high values were obtained for the onset of the taste immediately after ingestion, the intensity, the thickness of the middle part, and the persistence of the aftertaste. This is thought to be because the taste components adhere to and accumulate in the applied oil-in-water emulsion, and then act.
[0099] (6) Flavor enhancement effect of separate use of oil-in-water emulsion II The taste components listed in Table 13 below were added to water in the specified amounts to prepare taste solutions, and the taste intensity of each taste solution was evaluated before and after application of 10% O / W(+) to the oral cavity in the same manner as in the evaluation method described in (5) above. The evaluation was carried out by well-trained expert panelists on a 10-point scale, with 5 being the rating of the taste solution before application.
[0100] The evaluation results obtained are shown in Table 13 below (N=2).
[0101] [Table 13]
[0102] From the above results, it was confirmed that for all five basic tastes, the intensity of the taste was increased by simply ingesting the taste aqueous solution after applying the oil-in-water emulsion to the oral cavity, without premixing the taste components into the aqueous solution of the oil-in-water emulsion.
[0103] (7) Enhancement of the flavor of pungent components by using oil-in-water emulsion The above five basic tastes are all sensed by the gustatory nerves. On the other hand, spiciness, astringency, etc. are sensed not by the gustatory nerves but by pain and temperature sensations, and are therefore distinct from the above taste components. Therefore, we investigated whether the use of an oil-in-water emulsion in combination with other components other than taste components would have the same effect.
[0104] An oil-in-water emulsion containing a pungent component in an oil was prepared by adding and mixing each component according to the composition in Table 14. The thickening polysaccharides used were xanthan gum, gum arabic, pectin, phosphate cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphate cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose. Each component was mixed at once and stirred for 1 minute at 20,000 rpm using a Polytron homogenizer.
[0105] The amount of each component in the table is shown in mass % with the amount of the obtained oil-in-water emulsion being 100 mass %. Chili oil was used as a control.
[0106] Well-trained expert panelists ingested each sample (10 mL) and evaluated the intensity of each flavor on a 10-point scale, with the control being rated as 5. The results are shown in Table 14, and each value represents the average (N=3).
[0107] [Table 14]
[0108] The results confirmed that all oil-in-water emulsions containing pungent ingredients had a stronger pungent taste than the control, regardless of the type of thickening polysaccharide used. Furthermore, it was confirmed that the pungent taste of the oil-in-water emulsions containing pungent ingredients lasted for more than 10 minutes after ingestion, while the pungent taste felt after ingestion of the control disappeared within about 2 minutes.
[0109] These results confirmed that the effect (strength) and duration of effects can be increased by using oil-in-water emulsions in combination with ingredients other than taste ingredients, as well as ingredients in oils and fats.
[0110] (8) Comparative Example An emulsion composition was prepared by adding and mixing each component according to the composition in Table 15. The components were mixed using a Polytron homogenizer at 20,000 rpm for 1 minute.
[0111] The evaluation was carried out by dividing the samples into sets of Comparative Example A and Comparative Example B, and it was confirmed whether the emulsion compositions (A-2, B-2) had a stronger salty taste than the emulsion compositions (A-1, B-1) that did not contain α-cyclodextrin or a thickening polysaccharide (xanthan gum).
[0112] For the evaluation, well-trained expert panelists (N=3) ingested each emulsion composition (A-1, B-1) (10 mL), evaluated the intensity of the taste, then washed their mouths (rinsed twice with 20 mL of water), and then ingested each emulsion composition (A-2, B-2), evaluated and compared the intensity of the taste.
[0113] [Table 15]
[0114] In Comparative Example A, both Comparative Example A-1 and Comparative Example A-2 had a butter-like shape and had almost no salty taste. Comparing Comparative Example A-1 and Comparative Example A-2, no difference was observed in the strength of the salty taste between the two.
[0115] In Comparative Example B, both Comparative Example B-1 and Comparative Example B-2 were insufficiently emulsified, and oil floating was observed. In both Comparative Example B-1 and Comparative Example B-2, a salty taste was felt, but it did not linger, and no difference in the strength of the salty taste was observed between the two.
[0116] Experiment 4: Performance evaluation of oil-in-water emulsions (enhancing hair care effects) Each component was added and mixed according to the composition shown in Table 16 below to prepare an oil-in-water emulsion. Each component was mixed at once and stirred for 10 minutes at 20,000 rpm using a hand blender. The amount of each component in the table is shown in mass % with the amount of the resulting oil-in-water emulsion being 100 mass %.
[0117] [Table 16]
[0118] The obtained oil-in-water emulsion was added to a commercially available hair conditioner (TSUBAKI Premium Moist Hair Conditioner (Fine Today Co., Ltd.) in an amount of 25% by mass to prepare a hair conditioner containing the oil-in-water emulsion. As a control, the same commercially available hair conditioner containing no oil-in-water emulsion was used.
[0119] After washing the hair with hair shampoo, the hair was rinsed thoroughly with hot water of about 40°C. Approximately 10 g of the oil-in-water emulsion hair conditioner or the control hair conditioner was taken in the palm of the hand and applied thoroughly to the entire hair and left for about 1 minute. The hair was then rinsed thoroughly with hot water of about 40°C, the moisture was removed with a towel, and the hair was dried with a hair dryer. After that, the hair texture was evaluated by a panel of 3 people (N=3).
[0120] As a result, when the control hair conditioner was used, the hair felt very smooth and shiny, but due to static electricity repulsion, the hair was less manageable and flyaways were observed.
[0121] On the other hand, when the hair conditioner containing the oil-in-water emulsion was used, the hair felt very smooth and shiny, just like when the control hair conditioner was used, but it also felt moisturized and smooth, and the hair was easy to manage and no static flyaways were observed. This result is thought to be due to the fact that the inclusion of the oil-in-water emulsion allows the active ingredients contained in the hair conditioner to remain in the hair longer, thereby enhancing and / or prolonging the effects of the active ingredients, thereby enhancing the moisturizing effect, reducing the surface potential of the hair that affects flyaways, and further reducing the repulsion between hair strands.
[0122] As described above, the oil-in-water emulsion of the present invention can adhere to a predetermined site and retain and / or absorb / adsorb the active ingredient, thereby enhancing and / or prolonging the effect of the active ingredient. It is therefore expected that the emulsion will be used as a retention agent for active ingredients in various fields, such as food and beverages, pharmaceuticals, and cosmetics.
Claims
1. A retention agent comprising an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, used to adhere the oil-in-water emulsion to an application site and retain an active ingredient therein, wherein the application site is an animal epithelial tissue other than skin, hair, nails, or teeth.
2. The retention agent according to claim 1, wherein the hydrophobic substance is at least one selected from the group consisting of oils and fats, hydrophobic waxes, and hydrophobic resins.
3. 2. The retention agent according to claim 1, wherein the thickening polysaccharide is one or more selected from the group consisting of carboxymethylcellulose (CMC), xanthan gum, locust bean gum, guar gum, glucomannan, κ-carrageenan, ι-carrageenan, λ-carrageenan, tamarind gum, gellan gum, gum arabic, pectin, phosphate cross-linked starch, hydroxypropyl starch, hydroxypropylated phosphate cross-linked starch, tragacanth gum, hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, and hydroxyethyl cellulose.
4. 2. The retention agent according to claim 1, which is added to food and drink and the application site is the epithelial tissue of the oral cavity or esophagus, or teeth.
5. The retention agent according to claim 1, which is added to a pharmaceutical product.
6. The retention agent according to claim 1, which is added to cosmetics and is applied to hair, nails, or teeth.
7. 1. A method for producing a retention agent, which comprises the step of mixing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide to form an oil-in-water emulsion, and is used to adhere the oil-in-water emulsion to an application site and retain an active ingredient therein, wherein the application site is an animal epithelial tissue other than skin, hair, nails, or teeth.
8. A food or drink comprising an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and a retention agent used to adhere the oil-in-water emulsion to an application site and retain the active ingredient, in an amount of 0.5% by mass to 55% by mass in terms of the amount of the hydrophobic substance, wherein the application site is the epithelial tissue of the oral cavity or esophagus, or teeth.
9. A pharmaceutical comprising an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and a retention agent used to adhere the oil-in-water emulsion to an application site and retain the active ingredient, in an amount of 0.5% by mass to 55% by mass in terms of the amount of the hydrophobic substance, wherein the application site is an animal epithelial tissue other than skin, hair, nails, or teeth.
10. A cosmetic product comprising an oil-in-water emulsion containing water, a hydrophobic substance, cyclodextrin, and a thickening polysaccharide, and a retention agent used to adhere the oil-in-water emulsion to an application site and retain the active ingredient, in an amount of 0.5% by mass to 55% by mass in terms of the amount of the hydrophobic substance, wherein the application site is hair, nails, or teeth.
11. 1. Use of an oil-in-water emulsion containing water, a hydrophobic substance, a cyclodextrin, and a thickening polysaccharide in a method for producing a retention agent used to attach the oil-in-water emulsion to an application site and retain an active ingredient therein, wherein the application site is an animal epithelial tissue other than skin, hair, nails, or teeth.
Citation Information
Patent Citations
Valve type tubular water turbine generator
JP1986038166A
Odor masking and stabilizing composition for treating keratinous tissue, skin conditions and promoting wound healing
JP1993503071A
Emulsified composition and its production
JP1998262560A
Emulsion composition
JP2016204311A
Topical skin care formulations comprising plant extracts
US20210220254A1