Oily formulations

Abstract

To provide an oily formulation that can easily dispense the appropriate amount and has excellent resistance to liquid leakage. [Solution] An oily preparation containing at least one selected from the group consisting of diphenhydramine and salts thereof, wherein the oily preparation is housed in a container in which part or all of the part in contact with the oily preparation is made of plastic.

Description

Technical Field

[0001] The present invention relates to an oily preparation. The present invention also relates to a liquid dripping improvement agent for an oily preparation housed in a container formed of plastic, and a method for imparting a liquid dripping improvement effect to an oily preparation.

Background Art

[0002] Suppression of skin barrier damage due to dryness and accompanying itching is an issue for improving quality of life (QOL), and hitherto, solubilized compositions, emulsified compositions, ointment compositions, etc. have been used (for example, Patent Document 1).

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0004] However, the emulsified composition has a problem of insufficient emolliency, and the ointment composition has a problem of being unpleasant due to stickiness caused by the residue of solid oil on the skin. Therefore, it has been required to suppress skin dryness that causes scratching by using a base having a high emollient effect mainly composed of an oily component. However, skin external preparations mainly composed of oily components are excellent in elongation and conformity, but have problems such as difficulty in discharging an appropriate amount of use, such as too little or too much discharge, and poor liquid dripping.

[0005] Therefore, an object of the present invention is to provide an oily preparation that can easily discharge an appropriate discharge amount and is excellent in liquid dripping.

Means for Solving the Problems

[0006] The inventors of the present invention have found that an oily formulation containing diphenhydramine and housed in a plastic container can solve the above problems, and have completed the present invention.

[0007] The present invention provides, for example, the following inventions: [1] An oily preparation containing at least one selected from the group consisting of diphenhydramine and salts thereof, wherein the oily preparation is housed in a container in which part or all of the part in contact with the oily preparation is made of plastic. [2] The oily formulation according to [1], wherein the plastic is at least one selected from the group consisting of polyolefin resins and polyester resins. [3] The oily preparation according to [1] or [2], wherein the total content of diphenhydramine and its salts is 0.01 to 5.0% by mass, based on the total amount of the oily preparation. [4] An oily preparation according to any one of [1] to [3], comprising at least one antioxidant selected from lipid-soluble antioxidants. [5] A liquid flow improver for oily formulations, contained in a plastic container, comprising at least one selected from the group consisting of diphenhydramine and its salts as an active ingredient. [6] A method for imparting an effect of improving liquid flow to an oily formulation, The oily formulation is housed in a container in which part or all of the part that comes into contact with the oily formulation is made of plastic. A method comprising incorporating at least one substance selected from the group consisting of diphenhydramine and its salts into an oily preparation. [7] A method for filling a container with an oily preparation containing at least one selected from the group consisting of diphenhydramine and its salts, A filling method wherein the container is a container in which part or all of the part that comes into contact with the oily preparation is made of plastic. [Effects of the Invention]

[0008] According to the present invention, it is possible to provide an oily formulation that can easily dispense an appropriate amount and has excellent liquid-free properties. [Brief explanation of the drawing]

[0009] [Figure 1] This figure shows an overview of the release and slipperiness tests for resin surfaces. [Modes for carrying out the invention]

[0010] The embodiments for carrying out the present invention will be described in detail below. However, the present invention is not limited to the following embodiments.

[0011] [Oily-based formulations] The oily formulation according to the present invention contains at least one substance selected from the group consisting of diphenhydramine and its salts, and is housed in a container in which part or all of the part in contact with the oily formulation is made of plastic. Because the oily formulation according to the present invention employs such a configuration, it is possible to easily dispense an appropriate amount, and it also has excellent liquid-free properties. In this embodiment, the oily formulation refers to a formulation in which the water content is a certain amount or less, and is usually 5% by mass or less, preferably 3% by mass or less, and more preferably 1% by mass or less, based on the total amount of the oily formulation.

[0012] ((A) Diphenhydramine and its salts) The diphenhydramine and its salts used in the oily formulation according to this embodiment (hereinafter sometimes referred to as "component (A)") are not particularly limited as long as they are acceptable in the fields of pharmaceuticals, quasi-drugs, or cosmetics. The diphenhydramine or its salts may also be in the form of a hydrate.

[0013] Examples of diphenhydramine salts include organic acid salts, inorganic acid salts, salts with organic bases, salts with metals, and ammonium salts.

[0014] Examples of the organic acid salts of diphenhydramine include monocarboxylic acid salts such as acetate, trifluoroacetate, butyrate, palmitate, and stearate; polyvalent carboxylate salts such as fumarate, maleate, succinate, and malonate; oxycarboxylate salts such as lactate, tartrate, and citrate; and organic sulfonate salts such as lauryl sulfate, methanesulfonate, and toluenesulfonate.

[0015] Examples of the inorganic acid salts of diphenhydramine include hydrochloride, sulfate, nitrate, hydrobromide, and phosphate.

[0016] Examples of the salts of diphenhydramine with organic bases include salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, and picoline.

[0017] Examples of the salts of diphenhydramine with metals include salts with alkali metals such as sodium and potassium, salts with alkaline earth metals such as calcium and magnesium, and salts with aluminum.

[0018] From the viewpoint of more significantly exhibiting the effects according to the present invention, diphenhydramine and its inorganic acid salts are preferred as diphenhydramine and its salts, diphenhydramine and diphenhydramine hydrochloride are more preferred, and diphenhydramine is even more preferred.

[0019] Commercially available diphenhydramine and its salts can also be used. Diphenhydramine and its salts may be used alone or in combination of two or more.

[0020] The content of component (A) in the oily formulation according to this embodiment is not particularly limited and is set appropriately depending on the type of component (A), the types and content of other blending components, the use and formulation form of the oily formulation, etc. As for the content of component (A), from the viewpoint of more significantly exhibiting the effects of the present invention, for example, the total content of component (A) is preferably 0.01 to 5% by mass, more preferably 0.05 to 4% by mass, even more preferably 0.1 to 2% by mass, and particularly preferably 0.2 to 1.0% by mass, based on the total amount of the oily formulation.

[0021] ((B) Antioxidants) The oily formulation according to this embodiment may further contain an antioxidant (hereinafter sometimes referred to as "component (B)"). By combining component (A) and component (B) and incorporating them into the oily formulation, the effects of the present invention are more pronounced.

[0022] The antioxidant used in the oily formulation according to this embodiment is not particularly limited, as long as it is permissible in the pharmaceutical, quasi-drug, or cosmetic fields.

[0023] Antioxidants include lipid-soluble antioxidants and water-soluble antioxidants. Lipid-soluble antioxidants include lipid-soluble phenols, specifically dibutylhydroxytoluene (hereinafter sometimes referred to as "BHT"), butylhydroxyanisole (hereinafter sometimes referred to as "BHA"), and their derivatives. Specific examples of water-soluble antioxidants include ascorbic acid, its derivatives, and their salts (e.g., ascorbic acid, disodium ascorbic acid-2-sulfate, sodium ascorbate, magnesium ascorbic acid-2-phosphate, sodium ascorbic acid-2-phosphate, ascorbic acid palmitate, ascorbic acid stearate, aminopropyl ascorbic acid phosphate, tocopherol ascorbic acid phosphate, ascorbic acid triphosphate, ascorbic acid palmitate), ethylenediaminetetraacetic acid (EDTA), ethylenediaminetetraacetic acid salts (sodium salt (sodium edetate: Japanese Pharmacopoeia, EDTA-2Na), potassium salt, etc.).

[0024] As for antioxidants, from the viewpoint of more significantly exhibiting the effects of the present invention, lipid-soluble antioxidants are preferred, lipid-soluble phenols are more preferred, dibutylhydroxytoluene, butylhydroxyanisole and their derivatives are even more preferred, dibutylhydroxytoluene and butylhydroxyanisole are even more preferred, and dibutylhydroxytoluene is particularly preferred. By using dibutylhydroxytoluene as an antioxidant, the effects of the present invention are more significantly exhibited, and the odor change of oily formulations is more significantly suppressed.

[0025] Antioxidants can be commercially available. Antioxidants may be used individually or in combination of two or more types.

[0026] The content of component (B) in the oily formulation according to this embodiment is not particularly limited and is set as appropriate depending on the type of component (B), the types and content of other blending components, the use and formulation form of the oily formulation, etc. As for the content of component (B), from the viewpoint of more significantly exhibiting the effects of the present invention, for example, the total content of component (B) is preferably 0.0001 to 3% by mass, more preferably 0.0005 to 1% by mass, even more preferably 0.001 to 0.5% by mass, and particularly preferably 0.02 to 1% by mass, based on the total amount of the oily formulation.

[0027] In the oily formulation according to this embodiment, the content ratio of component (B) to component (A) is not particularly limited and is set appropriately depending on the types of component (A) and component (B), the types and content of other blending components, the use and formulation form of the oily formulation, etc. As for the content ratio of component (B) to component (A), from the viewpoint of more significantly exhibiting the effects of the present invention, for example, the total content of component (B) in the oily formulation according to this embodiment is preferably 0.0005 to 1 part by mass, more preferably 0.001 to 0.5 parts by mass, even more preferably 0.005 to 0.2 parts by mass, and even more preferably 0.01 to 0.1 parts by mass, per 1 part by mass of the total content of component (A) contained in the oily formulation according to this embodiment.

[0028] (Oily components) The oily formulation according to this embodiment may contain an oily component. The oily component is not particularly limited as long as it is permissible in the fields of pharmaceuticals, quasi-drugs, or cosmetics.

[0029] Examples of oily components include oils and fats, hydrocarbon oils, ester oils, silicone oils, higher alcohols, and higher fatty acids.

[0030] Examples of fats and oils include esters of fatty acids and glycerol, and these may be naturally derived or synthetic. Specific examples of fats and oils include avocado oil, linseed oil, almond oil, olive oil, cocoa oil, beef tallow, tung oil, wheat germ oil, sesame oil, rice germ oil, rice bran oil, safflower oil, soybean oil, evening primrose oil, camellia oil, corn oil, rapeseed oil, horse fat, peach kernel oil, palm oil, palm kernel oil, castor oil, sunflower oil, lard, grape oil, jojoba oil, macadamia nut oil, mink oil, cottonseed oil, Japanese wax, coconut oil, hydrogenated coconut oil, peanut oil, lanolin, egg yolk oil, rosehip oil, and medium-chain triglycerides.

[0031] Examples of hydrocarbon oils include paraffinic hydrocarbons and olefinic hydrocarbons. Specific examples of paraffinic hydrocarbons include paraffin, liquid paraffin, light liquid paraffin, liquid isoparaffin, light isoparaffin, heavy liquid isoparaffin, petrolatum, squalane, squalene, vegetable squalane, ceresin, microcrystalline wax, and pristane. Specific examples of olefinic hydrocarbons include straight-chain olefin compounds such as hexene, octene, decene, dodecene, and tetradecene; branched-chain olefin compounds such as diisobutylene and triisobutylene; and cyclic olefin compounds such as cyclohexene and dicyclopentene. Other hydrocarbon oils include acetylene hydrocarbons (alkynes containing one triple bond), hydrocarbons containing two or more double and / or triple bonds, and cyclic hydrocarbons such as aromatic hydrocarbons and alicyclic hydrocarbons.

[0032] Examples of ester oils include synthetic esters and esters of higher alcohols and higher fatty acids. Specific examples of ester oils include, for example, diisopropyl adipate, diisobutyl adipate, 2-hexyldecyl adipate, di-2-heptylundecyl adipate, isostearyl isostearate, hexadecyl isostearate, trimethylolpropane triisostearate, cetyl 2-ethylhexanoate, neopentyl glycol di-2-ethylhexanoate, trimethylolpropane tri-2-ethylhexanoate, pentaerythritol tetra-2-ethylhexanoate, cetyl octanoate, oleyl oleate, octyldodecyl oleate, decyl oleate, neopentyl glycol dicaprate, and 2-ethylhexyl succinate. Examples include isocetyl stearate, butyl stearate, diethyl sebacate, diisopropyl sebacate, cetyl lactate, tetradecyl lactate, isopropyl myristate, octyldodecyl myristate, cetyl myristate, myristyl myristate, isopropyl palmitate, octyl palmitate, 2-ethylhexyl palmitate, 2-hexyldecyl palmitate, 2-heptylundecyl palmitate, cholesteryl 12-hydroxystearate, phytosteryl oleate, diisostearyl malate, caprylic / capric triglyceride, paramethoxycinnamate, and pentaerythritol tetralosinate.

[0033] Examples of silicone oils include dimethylpolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, octamethylcyclotetrasiloxane, octamethylcyclopentasiloxane, decamethylcyclohexasiloxane, stearoxysilicone, and other higher alkoxy-modified silicones, alkyl-modified silicones, and higher fatty acid ester-modified silicones.

[0034] Examples of higher alcohols include octyldodecanol, isostearyl alcohol, and oleyl alcohol.

[0035] Higher fatty acids include saturated or unsaturated straight-chain or branched-chain fatty acids with 12 to 22 carbon atoms. Specific examples of higher fatty acids include isostearic acid, oxystearic acid, oleic acid, stearic acid, palmitic acid, behenic acid, myristic acid, lauric acid, lanolinic acid, linoleic acid, and linolenic acid.

[0036] Oily components can be commercially available. Oily components may be used individually or in combination of two or more types.

[0037] As the oily component, hydrocarbon oils are preferred, paraffinic hydrocarbons are more preferred, and liquid paraffin and light liquid paraffin are even more preferred.

[0038] The content of oily components in the oily formulation according to this embodiment is not particularly limited and is set appropriately depending on the type of oily component, the type and content of other compounding components, the use and formulation form of the oily formulation, etc. As for the content of oily components, for example, based on the total amount of the oily formulation, the total content of oily components may be 50% by mass or more, 60% by mass or more, 70% by mass or more, or 80% by mass or more. There is no particular upper limit on the content of oily components, but for example, it may be 99% by mass or less.

[0039] In the oily formulation according to this embodiment, known additives permitted in the fields of pharmaceuticals, quasi-drugs, or cosmetics may be added, either individually or in combination of two or more, as long as they do not impair the effects of the present invention. For example, vitamins, steroids, local anesthetic components, antipruritic components, antibacterial components, cooling agents, preservatives, pH adjusters, irritation reducers, colorants, fragrances, pearlescent luster imparters, anti-inflammatory components, and astringent components may be added.

[0040] Examples of vitamins include vitamin A derivatives (retinol derivatives such as retinol, retinyl acetate, and retinyl palmitate, retinal, retinoic acid, methyl retinoate, ethyl retinoate, retinyl retinoate, vitamin A oil, vitamin A fatty acid esters, alpha-carotene, beta-carotene, gamma-carotene, delta-carotene, lycopene, zeaxanthin, cryptoxanthin, astaxanthin, echinenone, etc.) and vitamin K derivatives (phylloquinone, phylloquinone, etc.). Fat-soluble vitamins such as vitamin D (methyl hesperidin, ergocalciferol, cholecalciferol, etc.), vitamin E (dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate, etc.), and vitamin B2 (riboflavin, flavin mononucleotide, flavin adenine dinucleotide sodium, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5') Examples of water-soluble vitamins include: vitamin B1 (thiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate phosphate, thiamine monophosphate, thiamine diphosphate, thiamine diphosphate hydrochloride, thiamine triphosphate, thiamine triphosphate monophosphate, etc.), vitamin B6 (pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5'-pyridoxal phosphate, pyridoxamine hydrochloride, etc.), vitamin B12 (cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin, etc.), and vitamin C (ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbate phosphate, magnesium ascorbate phosphate, etc.). As for the vitamins, fat-soluble vitamins are preferred, vitamin A and vitamin E are more preferred, vitamin E is even more preferred, and tocopherol acetate is even more preferred.The vitamin content in the oily formulation according to this embodiment is not particularly limited and is set appropriately depending on the type of vitamin, the type and content of other ingredients, and the intended use. From the viewpoint of achieving the effects of the present invention more significantly, the vitamin content is preferably 0.01 to 5% by mass, more preferably 0.1 to 2% by mass, even more preferably 0.1 to 1% by mass, and even more preferably 0.2 to 0.5% by mass, based on the total amount of the oily formulation. If the vitamin is vitamin A, it is preferably 1,000 to 1,000,000 IU / 100g, and more preferably 5,000 to 500,000 IU / 100g, based on the total amount of the oily formulation. IU refers to the International Unit determined by the method described in the 17th edition of the Japanese Pharmacopoeia, Vitamin A Quantitative Determination Method, etc.

[0041] Examples of steroids include prednisolone, hydrocortisone, cortisone, dexamethasone, and their derivatives, as well as their salts. More specifically, examples include dexamethasone propionate, difluprednate, hydrocortisone propionate butyrate, prednisolone acetate valerate (prednisolone valerate acetate), prednisolone, beclomethasone dipropionate, dexamethasone valerate, hydrocortisone butyrate, hydrocortisone acetate, dexamethasone, hydrocortisone, dexamethasone acetate, hydrocortisone, cortisone acetate, and prednisolone acetate. The steroid content in the oily formulation according to this embodiment is not particularly limited and is set as appropriate depending on the type of steroid, the type and content of other ingredients, and the application. From the viewpoint of achieving the effects of the present invention more significantly, the steroid content is preferably 0.01 to 0.5 w / w%, for example, based on the total amount of the oily formulation.

[0042] Examples of local anesthetic components include lidocaine, lidocaine hydrochloride, dibucaine, dibucaine hydrochloride, ethyl aminobenzoate, eucalyptus oil, eugenol, and chlorobutanol. The content of local anesthetic components in the oily formulation according to this embodiment is not particularly limited and is set as appropriate depending on the type of local anesthetic component, the types and content of other components, and the application. From the viewpoint of achieving the effects of the present invention more significantly, the content of local anesthetic components is preferably 0.01 to 5 w / w%, for example, based on the total amount of the oily formulation.

[0043] Examples of antipruritic ingredients include crotamiton, chlorpheniramine, chlorpheniramine maleate, nonyl vanillylamide, mequitazine, thymol, eugenol, polyoxyethylene lauryl ether, and perilla extract. The content of the antipruritic ingredient in the oily formulation according to this embodiment is not particularly limited and is set as appropriate depending on the type of antipruritic ingredient, the type and content of other ingredients, and the application. From the viewpoint of achieving the effects of the present invention more significantly, the content of the antipruritic ingredient is preferably 0.1 to 15 w / w%, for example, based on the total amount of the oily formulation.

[0044] Examples of antibacterial components include isopropylmethylphenol, chlorhexidine gluconate, chlorhexidine hydrochloride, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium bromide, decalinium chloride, triclosan, and trichlorocarbanilide. The content of antibacterial components in the oily formulation according to this embodiment is not particularly limited and is set as appropriate depending on the type of antibacterial component, the type and content of other components, and the application. From the viewpoint of achieving the effects of the present invention more significantly, the content of antibacterial components is preferably 0.01 to 1 w / w% based on the total amount of the oily formulation.

[0045] Examples of cooling agents include menthol, menthoxypropanediol, monomenthyl glyceryl ether, menthyl lactate, camphor, eugenol, eucalyptus oil, cineole, mint oil, and peppermint oil. The content of the cooling agent in the oily formulation according to this embodiment is not particularly limited and is set as appropriate depending on the type of cooling agent, the type and content of other ingredients, and the application. From the viewpoint of achieving the effects of the present invention more significantly, the content of the cooling agent is preferably 0.01 to 10 w / w%, for example, based on the total amount of the oily formulation.

[0046] Examples of preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl parahydroxybenzoate, isopropyl parahydroxybenzoate, butyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, benzyl parahydroxybenzoate, methyl parahydroxybenzoate, phenoxyethanol, benzyl alcohol, chlorobutanol, sorbic acid and its salts, chlorhexidine gluconate, alkanediol, and glycerin fatty acid esters.

[0047] Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, phosphoric acid, polyphosphate, and boric acid, etc.), organic acids (lactic acid, sodium lactate, acetic acid, citric acid, sodium citrate, tartaric acid, malic acid, succinic acid, sodium succinate, oxalic acid, gluconic acid, fumaric acid, propionic acid, aspartic acid, epsilonaminocaproic acid, glutamic acid, and aminoethylsulfonic acid, etc.), gluconolactone, ammonium acetate, inorganic bases (sodium bicarbonate, sodium carbonate, potassium hydroxide, sodium hydroxide, calcium hydroxide, and magnesium hydroxide, etc.), and organic bases (monoethanolamine, triethanolamine, diisopropanolamine, lysine, triisopropanolamine, etc.).

[0048] Examples of irritation-reducing agents include licorice extract, sodium alginate, and 2-methacryloyloxyethyl phosphorylcholine.

[0049] Examples of colorants include inorganic pigments and natural dyes.

[0050] Examples of pearlescent luster imparting agents include ethylene glycol distearate, ethylene glycol monostearate, and triethylene glycol distearate.

[0051] Examples of anti-inflammatory ingredients include glycyrrhetinic acid, glycyrrhizic acid derivatives, allantoin, azulene, and aminocaproic acid.

[0052] Examples of astringent components include zinc oxide, zinc sulfate, allantoin dihydroxyaluminum, allantoin chlorohydroxyaluminum, aluminum chloride, zinc sulfocarbonate, and tannic acid.

[0053] The viscosity of the oily formulation according to this embodiment may be, for example, 1 mPa·s or more, preferably 10 mPa·s or more, more preferably 15 mPa·s or more, even more preferably 20 mPa·s, and even more preferably 30 mPa·s or more. Furthermore, the viscosity of the oily formulation according to this embodiment may be, for example, 500 mPa·s or less, preferably 200 mPa·s or less, more preferably 100 mPa·s or less, even more preferably 80 mPa·s or less, and even more preferably 70 mPa·s or less. The viscosity of the oily formulation is the viscosity at 20°C measured by filling a 100 mL glass container (SV-100; Nichiden Rika Glass) with the oily formulation using a rotational viscometer (RB80L type viscometer, manufactured by Toki Sangyo Co., Ltd., rotor; M1 rotor, 60 rpm).

[0054] The form of the oily formulation according to this embodiment may be solid, liquid, gel, or sherbet. The oily formulation of this embodiment is preferably liquid because it has excellent spreadability and compatibility, can be easily dispensed in the appropriate amount, and has excellent liquid-free properties.

[0055] The oily formulation according to this embodiment may be a pharmaceutical, a quasi-drug, or a cosmetic. The oily formulation of this embodiment is preferable as a topical preparation, and more preferable as a topical skin preparation, because it has excellent spreadability and compatibility, can be easily dispensed in the appropriate amount, and has excellent liquid drainage. Furthermore, because it can be easily dispensed in the appropriate amount, it is suitable for quasi-drugs and pharmaceuticals, and more suitable for pharmaceuticals.

[0056] (container) The oily formulation according to this embodiment is provided in a container in which part or all of the part that comes into contact with the oily formulation is made of plastic (filled, injected, sealed). The container may be any packaging having a part that comes into contact with the oily formulation, and may consist of, for example, a container body portion that contains the oily formulation, a portion including the dispensing part of the container (e.g., a nozzle, an inner stopper), a suction tube, a cap, etc.

[0057] Examples of plastics used to form the container include polyolefin resins, polyester resins, polystyrene resins, vinyl chloride resins, and fluororesins. Among these, polyolefin resins and polyester resins are preferred, polyolefin resins are more preferred, and polyethylene and polypropylene are particularly preferred.

[0058] Polyolefin resins may be polymers obtained by polymerizing a single olefin or polymers obtained by copolymerizing two or more olefins. These polymers may also contain other polymerizable monomers as constituent components. Specific examples of polyolefin resins include polyethylene (including low-density polyethylene, medium-density polyethylene, high-density polyethylene, etc.), polypropylene (including isotactic polypropylene, syndiotactic polypropylene, and atactic polypropylene), ethylene-propylene copolymers, and polymethylpentene.

[0059] The polyester resin may be a polymer obtained by condensation polymerization of one or more polycarboxylic acids and one or more polyalcohols. The polymer may also contain other polymerizable monomers as constituent components. Specific examples of polyester resins include polyethylene terephthalate, polyethylene naphthalate, polybutylene terephthalate, and polycarbonate.

[0060] Polystyrene resins may be polymers obtained by polymerizing styrene, or copolymers of styrene with other polymerizable monomers. Specific examples of polystyrene resins include polystyrene, acrylonitrile-styrene copolymers, and acrylonitrile-butadiene-styrene copolymers.

[0061] The vinyl chloride resin may be either a polymer obtained by polymerizing vinyl chloride, or a copolymer of vinyl chloride with another polymerizable monomer. Specific examples of vinyl chloride resins include polyvinyl chloride, ethylene-vinyl chloride copolymer, and vinyl acetate-vinyl chloride copolymer.

[0062] Fluororesins may be polymers obtained by polymerizing a single fluorine-containing olefin, or polymers obtained by copolymerizing two or more fluorine-containing olefins. These polymers may also contain other polymerizable monomers as constituent components. Specific examples of fluororesins include polytetrafluoroethylene, polychlorotrifluoroethylene, polyvinylidene fluoride, polyvinyl fluoride, and perfluoroalkoxy fluororesins.

[0063] In this embodiment, the container for holding the oily formulation is made of plastic in part or all of the part that comes into contact with the oily formulation. For example, if the container has a perforated stopper (nozzle), only the perforated stopper portion may be made of plastic, or the other parts of the container, etc., may be made of plastic, or the entire container may be made of plastic. Alternatively, for example, a film or layer made of plastic may be formed on the inner surface of the container, or the container itself may be made of plastic.

[0064] The container for containing the oily formulation according to this embodiment may have its constituent parts (container body, part including the dispenser opening (nozzle, inner stopper), suction tube, cap, etc.) made of plastic, or the entire container may be made of plastic. From the viewpoint of more significantly achieving the effects of the present invention, it is preferable that at least the part including the dispenser opening (nozzle, inner stopper) of the container for containing the oily formulation according to this embodiment is made of plastic, and it is more preferable that the container body, the part including the dispenser opening (nozzle, inner stopper), and the suction tube are made of plastic.

[0065] The shape of the container for containing the oily formulation according to this embodiment, the shape of the dispensing part, and the capacity are not particularly limited and may be set as appropriate depending on the application, etc. Specifically, for example, it may be a bottle type (for example, one in which the dispensing part shape is a hinge cap and an inner stopper type), a jar type, a tube type, a dropper type, a dispenser type, a spray type, a roll-on type, a mist type, or an enamel bottle type.

[0066] The oily formulation according to this embodiment may also be provided as an oily formulation in a container according to this embodiment. The present invention can also be considered as an external product (hand care product, body care product, face care product, etc.) in which the oily formulation according to the present invention is contained in a container according to this embodiment.

[0067] [Method for imparting liquid flow-improving effects to liquid flow-improving agents and oily formulations] The present invention is based on the fact that an oily formulation containing diphenhydramine and housed in a plastic container can be easily dispensed in an appropriate amount and has excellent liquid flow. Therefore, in one aspect, the present invention can be considered as a liquid flow improving agent for an oily formulation housed in a plastic container, in which at least one selected from the group consisting of diphenhydramine and its salts is the active ingredient. Furthermore, in another aspect, the present invention can be considered as a method for imparting a liquid flow improving effect to an oily formulation, wherein the oily formulation is housed in a container in which part or all of the part in contact with the oily formulation is made of plastic, and the oily formulation contains at least one selected from the group consisting of diphenhydramine and its salts.

[0068] Detailed embodiments of the liquid flow improving agent and the method for imparting a liquid flow improving effect to an oily formulation according to this embodiment are as described for the oily formulation.

[0069] [Method for filling oil-based formulations] One aspect of the present invention relates to a method for filling a container with an oily formulation containing at least one selected from the group consisting of diphenhydramine and its salts, wherein the container is formed of plastic in part or all of the portion that comes into contact with the oily formulation. Detailed embodiments of the filling method are as described for the oily formulation. [Examples]

[0070] The present invention will be described in detail below based on test examples, but the present invention is not limited to these.

[0071] [Test Example 1: Release and Slipperiness Test on Resin Surface (1) - High Viscosity Formulation] Formulas were prepared with the compositions shown in Table 1 and subjected to release and slipperiness tests on resin surfaces. A schematic of the release and slipperiness tests on resin surfaces is shown in Figure 1. A cylindrical bottle made of injection-blow molded plastic (PET, PP, or PE) was cut in half lengthwise to create test piece 2, which was placed on an inclined surface 1 at an angle of 30° to the horizontal plane. 30 μL of each formula was dispensed onto test piece 2 from a vertical direction using a micropipette, and the time required for each formula to travel a certain distance (6 cm) on test piece 2 was measured.

[0072] The average travel speed (cm / s) of each formulation was calculated from the measured time and travel distance, and the rate of increase in speed (%) of the formulations in the examples was calculated according to the following formula (A). In Test Example 1, the "average travel speed of the standard formulation" is the average travel speed of the formulation of Comparative Example 1 on a test piece of the same material. The results are also shown in Table 1. Speed ​​increase rate (%) = {(Average movement speed of the formulation solution in the example / Average movement speed of the standard formulation solution) - 1} × 100 ... Equation (A)

[0073] [Table 1]

[0074] As shown in Table 1, it was confirmed that the addition of diphenhydramine increased the average migration speed in both PE and PP resins, improving the release and slipperiness of the formulation solution from these resin surfaces.

[0075] [Test Example 2: Release and Slipperiness Test on Resin Surface (2) - Low Viscosity Formulation] Formulas were prepared with the compositions shown in Table 2 and subjected to release and slipperiness tests on resin surfaces. The release and slipperiness tests on resin surfaces were carried out using the same procedure as in Test Example 1. In Test Example 2, the "average migration speed of the standard formula" in formula (A) is the average migration speed of the formula of Comparative Example 2 on a test piece of the same material. The results are also shown in Table 2.

[0076] [Table 2]

[0077] As shown in Table 2, even with low-viscosity formulations, the inclusion of diphenhydramine increased the average migration speed in both PE and PP resins, and improved the release and slipperiness of the formulation liquid from these resin surfaces.

[0078] [Test Example 3: Release and Slipperiness Test on Resin Surface (3) - Antioxidant Blending] Formulas were prepared with the compositions shown in Table 3 and subjected to release and slipperiness tests on resin surfaces. The release and slipperiness tests on resin surfaces were carried out using the same procedure as in Test Example 1. In Test Example 3, the "average migration speed of the standard formula" in formula (A) is the average migration speed of the formula of Comparative Example 3 on a test piece of the same material. The results are also shown in Table 3.

[0079] [Table 3]

[0080] As shown in Table 3, in formulations containing an antioxidant (BHT), the addition of diphenhydramine significantly increased the average migration speed in PET, PE, and PP resins, and significantly improved the release and slipperiness of the formulation solution from these resin surfaces.

[0081] [Test Example 4: Release and Slipperiness Test on Resin Surface (4)] Formulas were prepared with the compositions shown in Table 4 and subjected to release and slipperiness tests on resin surfaces. For the release and slipperiness tests on resin surfaces, test specimens were made by cutting plates of each type of plastic (PET, PP, or PE) to a size sufficient for the area required for the test, and the time required for each formula to move a certain distance (5 cm) on the test specimen was measured using the same procedure as in Test Example 1.

[0082] [Table 4]

[0083] [Test Example 5: Sensory Test (1)] The formulations for Example 3 and Comparative Example 3 shown in Table 3 were prepared and filled into plastic containers (container material: bottle - PET resin, nozzle - PE resin) to obtain the formulations. The sensory experience during actual use was evaluated by a sensory test conducted by four subjects. The sensory test was conducted using the Visual Analog Scale (VAS) method for (1) ease of dispensing, (2) ease of controlling the dispensing volume, and (3) clean liquid release. For each question item, the VAS was calculated by measuring the length from the left end of a 10 cm line segment to the shaded position of the answer, and this was used as the answer value. For the "ease of dispensing" item, "difficult to dispensing" was 0, which is the worst state, and "easy to dispensing" was 100, which is the best state. For "ease of controlling the dispensing volume," "difficult to control" was 0, which is the worst state, and "easy to control" was 100, which is the best state. For "clean liquid release," "poor liquid release" was 0, which is the worst state, and "good liquid release" was 100, which is the best state. The sensory test was conducted with the subjects unable to identify the contents of the formulation.

[0084] From the obtained VAS scores, the percentage increase in score for Example 3 compared to Comparative Example 3 was calculated according to the following formula. The results of the sensory evaluation are shown in Table 5. Score improvement rate of Example 3 compared to Comparative Example 3 (%) = {(VAS score of Example 3 / VAS score of Comparative Example 3) - 1} × 100 [Table 5]

[0085] As shown in Table 5, the inclusion of diphenhydramine improved the scores for all items related to ease of dispensing, ease of dispensing volume control, and liquid release, which were challenges in the design of conventional oily formulations. In particular, the scores for ease of dispensing volume control and liquid release were significantly improved.

[0086] [Test Example 6: Sensory Test (2)] A sensory evaluation of the ease of controlling the discharge volume was conducted using the same procedure as in Test Example 5, except that the material of the dispensing nozzle of the plastic container was changed from PE resin to PP resin. The results of the sensory evaluation are shown in Table 6.

[0087] [Table 6]

[0088] As shown in Table 6, even when the material of the dispensing nozzle of the plastic container is made of PP resin, it was confirmed that the inclusion of diphenhydramine improves the ease of controlling the dispensing volume, which was a challenge in the design of conventional oily formulations.

[0089] The oily formulation of the present invention offers improved release and slipperiness of the formulation liquid from resin surfaces, and in actual use, it improves ease of control of the discharge volume, ease of discharge, and clean liquid flow, thus solving the problems of conventional oily formulations. Furthermore, the improved release and slipperiness of the formulation liquid from resin surfaces prevents liquid residue in the container.

[0090] [Test Example 7: Effect of light irradiation on suppressing odor change of diphenhydramine (1) - Odor measurement] Formulas were prepared with the compositions shown in Table 7, and 15 mL was filled into 20 mL glass containers (SV-20; Nichiden Rika Glass). The odor of each sample before light irradiation was measured using an odor sensor (portable odor sensor mini, P-329m; Shin-Cosmos Electric Co., Ltd.). Next, each sample container was irradiated with a light irradiation device, Suntester (SUNTEST XLS+; Toyo Seiki Seisakusho), at an irradiance of 765 w / m². 2 The light was irradiated for 1 hour (2754 kJ / m³). 2 This corresponds to [the above]. The odor of each sample after light irradiation was measured in the same manner. From the obtained measurements, the odor increase rate (times) was calculated according to the following formula. The results are also shown in Table 7. Odor increase rate (times) = Odor sensor reading after light irradiation / Odor sensor reading before light irradiation

[0091] [Test Example 8: Effect of light irradiation on suppressing odor change of diphenhydramine (2) - Sensory evaluation] Formulas were prepared with the compositions shown in Table 7, and 15 mL was filled into 20 mL glass containers (SV-20; Nichiden Rika Glass Co., Ltd.). The containers were then separated into light-irradiated and unirradiated samples. For the light-irradiated samples, each sample container was irradiated using a light irradiation device, Suntester (SUNTEST XLS+; Toyo Seiki Seisakusho Co., Ltd.), at an irradiance of 765 w / m². 2 Irradiated for 1 hour (2754 kJ / m³). 2 (This corresponds to...). Light-irradiated and unirradiated samples were subjected to sensory testing. The sensory testing was conducted by three testers using the Visual Analog Scale (VAS) method to assess the degree of unpleasant odor. For each question item, the length from the left end of a 10 cm line segment to the shaded position of the answer was measured and used as the answer value. An answer value of 0 indicates no unpleasant odor at all, and 100 indicates a strong unpleasant odor, with lower values ​​indicating better results. The sensory testing was conducted in a manner that prevented the subjects from identifying the contents of the formulation.

[0092] The odor suppression rate (%) was calculated from the obtained VAS scores according to the following formula. The results of the sensory evaluation are also shown in Table 7. Odor suppression rate (%) = [1 - {(VAS score of the light-irradiated sample in Example 3 - VAS score of the unirradiated sample in Example 3) / (VAS score of the light-irradiated sample in Example 1 - VAS score of the unirradiated sample in Example 1)}] × 100

[0093] [Table 7]

[0094] As shown in Table 7, oily formulations containing dibutylhydroxytoluene (BHT) in addition to diphenhydramine showed significantly suppressed odor, as confirmed by both instrumental measurements and sensory tests.

[0095] [Examples of formulations] Tables 8 to 11 illustrate representative examples of the oily formulations of the present invention. All units in the tables are w / w%.

[0096] Formulation Examples 1 to 32 were prepared and filled into containers A and B, respectively. [Table 8]

[0097] [Table 9]

[0098] [Table 10]

[0099] [Table 11] [Explanation of Symbols]

[0100] 1…Slope, 2…Test specimen.

Claims

[Claim 1] An oily preparation containing at least one selected from the group consisting of diphenhydramine and salts thereof, wherein the oily preparation is housed in a container in which part or all of the part in contact with the oily preparation is made of plastic.

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