Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
  • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
  • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
  • A61K31/355—Tocopherols, e.g. vitamin E
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
  • A61K31/4164—1,3-Diazoles
  • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
  • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Definitions

• the present invention relates to a skin external preparation composition containing an ester steroid.
• Ester steroids represented by prednisolone valerate acetate, have excellent anti-inflammatory effects and can be used externally to treat eczema/dermatitis, prurigo, insect bites, psoriasis, palmoplantar pustulosis, etc. It is widely used as a disease treatment drug. It is known that the ester steroids are susceptible to hydrolysis and require formulation measures to suppress decomposition in order to be stably blended, and they also do not dissolve in vaseline, which is known as an ointment base. There is a problem.
• Patent Document 1 there are techniques to prepare ointments by blending lactic acid esters in addition to steroids and medium-chain fatty acid triglycerides (Patent Document 1), and techniques to produce liquid preparations by blending a large amount of ethanol in addition to steroids and medium-chain fatty acid triglycerides.
• Patent Document 2 and a technique for preparing an external preparation by blending polypropylene glycol in addition to steroids and polar oils (Patent Document 3) has been reported.
• gamma oryzanol is a component contained in rice bran, and has been known to have sebum secretion promoting effects, skin temperature increasing effects, and blood flow increasing effects. It is also used in cosmetics as a whitening agent.
• gamma oryzanol has low solubility in oil agents, and it is difficult to stably incorporate it at a high concentration into external preparations containing oil agents.
• Patent Document 4 As an attempt to improve the solubility of gamma oryzanol, a technique for preparing a topical preparation by blending gamma oryzanol with N-lauroyl-L-glutamic acid-2-octyldodecyl diester (Patent Document 4), A technique has been reported in which a diester consisting of a fatty acid having 8 to 18 carbon atoms and a dihydric alcohol is blended to form an external preparation (Patent Document 5).
• the skin external preparations containing ester steroids or gamma oryzanol use special surfactants and solvents such as ethanol, which soften the intercellular lipids in the stratum corneum of the epidermis and destroy the skin barrier. If a solvent with insufficient solubility is used, these poorly soluble ingredients will precipitate during long-term storage, and if the product is not applied to the skin, there is a concern that In some cases, there is a concern that the feeling of use may be deteriorated, such as a feeling of roughness, and furthermore, the preparation may become non-uniform.
• ester steroids and gamma oryzanol have low solubility in oils, and no external preparation for skin containing these two has been commercialized. Therefore, the object of the present invention is to contain an ester steroid and gamma oryzanol, completely dissolve both components, maintain formulation stability and component stability even after long-term storage, suppress skin irritation, and improve the feeling of use. An object of the present invention is to provide an excellent skin external preparation composition.
• the present inventor conducted various studies to solve the above-mentioned problems.
• the solubility of ester steroids was improved, which made it possible to reduce the amount of medium chain fatty acid triglycerides.
• a skin external preparation composition can be obtained in which the two components are completely dissolved, the formulation stability and component stability are maintained even after long-term storage, and the skin irritation is suppressed and the feel is excellent. It has also been found that the stability of the formulation after long-term storage and the feeling of use can be further improved by adding a higher alcohol to the formulation.
• a skin external preparation composition containing the following components (A) to (C).
• (B) Ester steroid
• C) Medium chain fatty acid triglyceride
• the mass ratio (B/A) of component (B) to component (A) is 2 or more and 100 or less
• Description skin external preparation composition [3] The skin external preparation composition according to [1] or [2], wherein the mass ratio (C/B) of component (C) to component (B) is 6 or more and 30 or less.
• the content of component (A) is 0.01% by mass or more and 0.5% by mass or less
• the content of component (B) is 0.1% by mass or more and 3% by mass or less
• the content of component (C) is The skin external preparation composition according to any one of [1] to [3], wherein the amount is 3% by mass or more and 30% by mass or less.
• Component (A) is one or more selected from dexamethasone acetate, prednisolone acetate, prednisolone valerate acetate, hydrocortisone butyrate, hydrocortisone acetate, cortisone acetate, and betamethasone valerate.
• the skin external preparation composition according to any one of [1] to [6].
• [8] The skin external preparation composition according to any one of [1] to [6], wherein component (A) is prednisolone valerate acetate.
• component (D) is a chain aliphatic monohydric alcohol having 12 or more and 22 or less carbon atoms.
• the skin external preparation composition according to any one of [1] to [9], further containing one or more selected from tocopherols, bactericides, local anesthetics, allantoin, and antihistamines. [11] Any of [1] to [10] further contains one or more selected from oils, emulsifiers, buffers, chelating agents, polyhydric alcohols, and water other than component (C) and component (D).
• the skin external preparation composition described in is described in .
• both the ester steroid and gamma oryzanol are dissolved and maintained stably for a long period of time, and the composition has a good feel when used.
• the present invention is a skin external preparation composition containing an ester steroid and gamma oryzanol, and one embodiment thereof is a skin external preparation composition containing the following components (A) to (C).
• Component (A) is an ester steroid.
• Ester steroids are compounds in which at least one hydroxy group present in a synthetic or natural steroid skeleton is esterified with a fatty acid or the like, and have excellent anti-inflammatory effects. Since the skin external preparation composition of the present invention contains the ester steroid, it is useful as a therapeutic agent for skin diseases such as eczema/dermatitis, prurigo, insect bites, psoriasis, and palmoplantar pustulosis.
• the ester steroid may be any ester steroid used as an external skin preparation, such as clobetasol propionate, diflorasone acetate, mometasone furoate, betamethasone butyrate propionate, fluocinonide, difluprednate.
• component (A) one or more selected from these ester steroids can be used.
• dexamethasone acetate, prednisolone acetate, prednisolone valerate acetate, hydrocortisone butyrate, hydrocortisone acetate, cortisone acetate, and betamethasone valerate are preferred; Grass acid ester is more preferred, and prednisolone valerate acetate is even more preferred.
• the content of component (A) in the skin external preparation composition of the present invention is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and 0.01% by mass or more, more preferably 0.05% by mass or more, from the viewpoint of the effectiveness of component (A). .1 mass% or more is more preferable, and from the viewpoint of solubility of component (A) in the composition, 0.5 mass% or less is preferable, 0.4 mass% or less is more preferable, and 0.3 mass% or less. % or less is more preferable.
• the content is preferably 0.01% by mass or more and 0.5% by mass or less, more preferably 0.05% by mass or more and 0.4% by mass or less, and even more preferably 0.1% by mass or more and 0.3% by mass or less.
• Component (B) is gamma oryzanol.
• Gamma oryzanol is a general term for esters that are a condensation of ferulic acid and sterol, which are contained in the lipids of rice bran.
• the main components include oryzanol A (cycloartol ferulate ester), oryzanol C (24-methylene cycloartanol ferulate ester), campesterol ferulate, etc. Since the skin external preparation composition of the present invention contains gamma oryzanol, its sebum secretion promoting effect improves and reinforces the pharmacological effect of component (A).
• gamma oryzanol surprisingly contributes to improving the solubility of component (A) together with component (C).
• component (A) e.g., gamma oryzanol
• gamma oryzanol is also found in rice germ oil, corn oil, and various grain oils, so it can be extracted from these oils.
• commercially available products can also be used.
• the content of component (B) in the skin external preparation composition of the present invention is preferably 0.1% by mass or more, more preferably 0.4% by mass or more, and 0.1% by mass or more, more preferably 0.4% by mass or more, from the viewpoint of the effectiveness of component (B). It is more preferably 5% by mass or more, and from the viewpoint of the solubility of component (B) in the composition, it is preferably 3% by mass or less, more preferably 2% by mass or less, and even more preferably 1.5% by mass or less. .
• the content is preferably 0.1% by mass or more and 3% by mass or less, more preferably 0.4% by mass or more and 2% by mass or less, and even more preferably 0.5% by mass or more and 1.5% by mass or less.
• Component (C) is a medium chain fatty acid triglyceride.
• component (C) mainly contributes to improving the solubility of component (A) and component (B), but it also improves the storage stability of component (A) and component (B), and the storage stability of the formulation. It also contributes to improving the feeling of use of the composition.
• Medium chain fatty acid triglyceride usually refers to fatty acid triglyceride having 6 or more and 12 or less carbon atoms.
• the content of component (C) in the skin external preparation composition of the present invention is determined based on the solubility of component (A) and component (B) in the composition, the storage stability of component (A) and component (B), From the viewpoint of storage stability of the formulation, it is preferably 3% by mass or more, more preferably 6% by mass or more, even more preferably 8% by mass or more, and from the viewpoint of the feel of the composition, 30% by mass or less, It is more preferably 20% by mass or less, and even more preferably 15% by mass or less.
• the content is preferably 3% by mass or more and 30% by mass or less, more preferably 6% by mass or more and 20% by mass or less, and even more preferably 8% by mass or more and 15% by mass or less.
• component (B) contributes to improving the solubility of component (A) in the composition.
• the mass ratio (B/A) of component (B) to component (A) is preferably 2 or more and 100 or less, preferably 3 or more and 50 or less, and preferably 4 or more and 15 or less. is even more preferable.
• component (B) and component (C) also contribute to improving the solubility of component (A) in the composition.
• the mass ratio (C/B) of component (C) to component (B) is preferably 6 or more and 30 or less, more preferably 8 or more and 20 or less, and 10 or more and 15 or less. It is even more preferable.
• the skin external preparation composition of the present invention further contains component (D) higher alcohol to improve long-term storage stability in the composition of component (A) and component (B). It is preferable from the viewpoint of improving the solubility of component (B) and the long-term storage stability of the formulation, and improving the feeling of use of the composition.
• Higher alcohol usually refers to a long chain alcohol with 6 or more carbon atoms, but in the present invention, it is preferable to use a chain aliphatic monohydric alcohol with 8 or more and 24 carbon atoms, and a chain with 12 or more and 22 or less carbon atoms. More preferably, an aliphatic monohydric alcohol of the formula is used. Specific examples include lauryl alcohol, myristyl alcohol, cetanol, stearyl alcohol, arachidyl alcohol, behenyl alcohol, and oleyl alcohol.
• the content of component (D) in the skin external preparation composition of the present invention is determined to improve the long-term storage stability of the component (A) and component (B) in the composition, and to dissolve component (A) and component (B).
• the content is preferably 2% by mass or more, more preferably 4% by mass or more, even more preferably 6% by mass or more, and from the viewpoint of improving the feel of the composition, 15% by mass or more. It is preferably at most 12% by mass, more preferably at most 10% by mass, and even more preferably at most 10% by mass.
• the content is preferably 2% by mass or more and 15% by mass or less, more preferably 4% by mass or more and 12% by mass or less, and even more preferably 6% by mass or more and 10% by mass or less.
• the skin external preparation composition of the present invention includes other active ingredients such as local anesthetics, bactericides, tocopherols, allantoin, and antihistamines; oils other than the above-mentioned components (C) and (D); Emulsifiers, buffering agents, chelating agents, polyhydric alcohols, amino acids, water, etc. can be added.
• active ingredients such as local anesthetics, bactericides, tocopherols, allantoin, and antihistamines
• Emulsifiers Emulsifiers, buffering agents, chelating agents, polyhydric alcohols, amino acids, water, etc. can be added.
• Examples of local anesthetics include lidocaine, dibucaine, tetracaine, oxydibucaine, bupivacaine, mepivacaine, propitocaine, diethylaminoethyl parabutylaminobenzoate, and the like, with lidocaine and dibucaine being preferred, and lidocaine being more preferred. Hydrochloride salts of these lidocaine, dibucaine, tetracaine, etc. can also be used.
• the content of the local anesthetic in the skin external preparation composition of the present invention is 0.1% by mass or more and 4% by mass or less, from the viewpoint of solubility and stability of component (A) and component (B), and local anesthetic action. It is preferably 0.2% by mass or more and 3% by mass or less, more preferably 0.5% by mass or less and 3% by mass or less.
• the disinfectant examples include isopropylmethylphenol, methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate, sodium dehydroacetate, p-cresol, and the like.
• isopropylmethylphenol is preferably blended as a disinfectant.
• Other parabens and the like are preferably added as preservatives.
• These disinfectants are preferably contained in the skin external preparation composition of the present invention in an amount of 0.02% by mass or more and 1.0% by mass or less, more preferably 0.05% by mass or more and 0.5% by mass or less. preferable.
• tocopherols examples include tocopherol, tocopherol acetate, and tocopherol nicotinate.
• the content of tocopherols in the skin external preparation composition of the present invention is preferably 0.1% by mass or more and 2% by mass or less, and preferably 0.1% by mass or more and 1% by mass or less.
• Allantoin whose chemical name is 5-ureidohydantoin, is used as a skin protective agent because it has tissue recovery effects.
• the content of allantoin in the skin external preparation composition of the present invention is preferably 0.1% by mass or more and 1% by mass or less, more preferably 0.1% by mass or more and 0.8% by mass or less, from the viewpoint of the effects of allantoin. It is preferably 0.1% by mass or more and 0.5% by mass or less.
• antihistamines examples include diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine, chlorpheniramine maleate, diphenylimidazole, and the like.
• the content of the antihistamine in the skin external preparation composition of the present invention is preferably 0.05% by mass or more and 5% by mass or less, more preferably 0.1% by mass or more and 3% by mass or less, and 0.2% by mass or more and 2% by mass. % or less is more preferable.
• oils other than component (C) and component (D) include petrolatum, squalane, plastibase, paraffin, liquid paraffin, white beeswax, and silicone oil.
• the content of these oils in the skin external preparation composition of the present invention is preferably 1% by mass or more and 80% by mass or less, more preferably 3% by mass or more and 80% by mass or less, and 5% by mass or more and 80% by mass. It is more preferable to contain the following.
• emulsifiers include nonionic ones such as polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, glycerin fatty acid ester, polyoxyethylene fatty acid ester, polyoxyethylene alkyl ether, sorbitan fatty acid ester, and polyoxyethylene polyoxypropylene glycol.
• examples include surfactants and ionic surfactants such as sodium lauryl sulfate and sodium cetyl sulfate, among which it is preferable to use nonionic surfactants.
• the content of the emulsifier in the skin external preparation composition of the present invention is preferably 0.5% by mass or more and 10% by mass or less, more preferably 0.5% by mass or more and 8% by mass or less.
• the buffering agent a combination of an aliphatic hydroxy acid such as lactic acid, citric acid, malic acid, or tartaric acid and an alkali metal salt thereof is preferred.
• the content of the buffer in the skin external preparation composition of the present invention is preferably 0.1% by mass or more and 3% by mass or less, more preferably 0.2% by mass or more and 2% by mass or less, from the viewpoint of pH adjustment effect. More preferably 0.3% by mass or more and 1.5% by mass or less.
• the content of the chelating agent in the skin external preparation composition of the present invention is preferably 0.1% by mass or more and 2% by mass or less, more preferably 0.2% by mass or more and 1% by mass or less, and 0.2% by mass or more and 0% by mass or less. More preferably, the content is .8% by mass or less.
• polyhydric alcohols examples include glycerin, 1,3-butylene glycol, propylene glycol, dipropylene glycol, and polyethylene glycol. These polyhydric alcohols are preferably contained in the skin topical composition of the present invention in an amount of 2% by mass to 20% by mass, and more preferably 4% by mass to 10% by mass.
• the content of water in the skin external preparation composition of the present invention is preferably 0% by mass or more and 70% by mass or less, more preferably 0% by mass or more and 60% by mass or less.
• the form of the skin external preparation composition of the present invention is an oil-based ointment, it does not substantially contain water, and when it is a cream (including both water-in-oil emulsions and oil-in-water emulsions), it contains water. It is preferable to contain.
• the skin external preparation composition of the present invention contains thickeners such as polyvinylpyrrolidone, carboxymethylcellulose, colloidal hydrated aluminum silicate, xanthan gum, locust bean gum, tragacanth gum, guar gum, gelatin, gum arabic, alginic acid, and albumin. You can also.
• thickeners such as polyvinylpyrrolidone, carboxymethylcellulose, colloidal hydrated aluminum silicate, xanthan gum, locust bean gum, tragacanth gum, guar gum, gelatin, gum arabic, alginic acid, and albumin. You can also.
• the skin preparation composition outside the present invention may be an oil-based ointment or a cream as described above, but in the case of a cream, the pH should be 4 or more and 6 or less in terms of skin irritation and component stability. is preferable, 4.5 or more and 5.6 or less are more preferable, and 4.8 or more and 5.4 or less are still more preferable.
• the pH is adjusted by the buffer.
• the skin external preparation composition of the present invention can be manufactured by uniformly mixing the above-mentioned components according to a conventional method.
• the skin external preparation composition of the present invention which is a cream
• the skin external preparation composition of the present invention can be prepared by heating and dissolving the lipophilic component and the hydrophilic component to which an emulsifier has been added separately in a lipophilic base or water, adding the latter to the former, and then adding the latter to the former and adding it to the homomixer. It is preferable to produce the emulsified product by stirring and emulsifying the emulsified product using, for example, a solvent, and then cooling it to room temperature.
• the skin external preparation composition of the present invention contains component (A) ester steroid, it is mainly used to treat skin diseases such as eczema/dermatitis group, prurigo group, insect bites, psoriasis, and palmoplantar pustulosis. It is useful as It can be used by applying an appropriate amount to the area where these skin diseases occur.
• the skin external preparation composition of the present invention has component (A) and component (B) stably dissolved in the composition, and the composition is stable for a long period of time.
• the usability is also good.
• the stability of component (A) and component (B) is determined by measuring the presence or absence of decomposition of component (A) and component (B) in the composition after long-term storage using high performance liquid chromatography (HPLC). It can be determined from this.
• HPLC high performance liquid chromatography
• the long-term storage stability of the formulation can be determined by visual observation and microscopic observation of the composition after long-term storage to determine the emulsified state and the presence or absence of precipitates.
• the feeling of use can be determined by applying the composition after long-term storage to the skin and performing a sensory evaluation of the presence or absence of roughness, ease of spreading, and ease of application.
• Examples 1 to 15 and Comparative Examples 1 to 5 Oily ointments and creams were manufactured according to the conventional methods using the formulations shown in Tables 1 to 3. The resulting formulation was evaluated for (1) component stability, (2) formulation stability, and (3) usability using the following methods. In addition, (4) comprehensive evaluation of these evaluations was also performed. The results are shown in Tables 1 to 3.
• Component stability is determined by storing the formulation under harsh conditions (50°C for 1 month) in order to predict chemical changes during long-term storage, and determining whether or not components (A) and (B) in the formulation decompose. was evaluated using the following criteria by measuring with high performance liquid chromatography (HPLC).
• Formulation stability was determined by conducting a so-called temperature cycle test in which the storage temperature was rapidly changed every 12 hours, with a low temperature of 5°C and a high temperature of 40°C, and visual inspection of the composition after one month of storage. The emulsified state and the presence or absence of precipitates were evaluated by microscopic observation using the following criteria.
• the skin external preparation composition of the present invention containing (A) ester steroid, (B) gamma oryzanol, and (C) medium chain fatty acid triglyceride can dissolve components (A) and (B). It can be seen that the composition has good properties, is stable for a long period of time, and has a good usability.

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