WO2023112664A1 - Composition pharmaceutique pour application externe contenant du peroxyde de benzoyle - Google Patents

Composition pharmaceutique pour application externe contenant du peroxyde de benzoyle Download PDF

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Publication number
WO2023112664A1
WO2023112664A1 PCT/JP2022/044017 JP2022044017W WO2023112664A1 WO 2023112664 A1 WO2023112664 A1 WO 2023112664A1 JP 2022044017 W JP2022044017 W JP 2022044017W WO 2023112664 A1 WO2023112664 A1 WO 2023112664A1
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mass
acid
parts
oil
benzoyl peroxide
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PCT/JP2022/044017
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English (en)
Japanese (ja)
Inventor
純子 丸川
綾子 林
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ロート製薬株式会社
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Publication of WO2023112664A1 publication Critical patent/WO2023112664A1/fr

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    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • 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
    • A61K31/327—Peroxy compounds, e.g. hydroperoxides, peroxides, peroxyacids
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels

Definitions

  • B1 benzoyl peroxide
  • B1 glycyrrhetinic acid, its derivatives and/or salts thereof
  • B2 allantoin External composition.
  • the present inventors found that when benzoyl peroxide is added to the base of the composition for external use, the viscosity decreases over time.
  • the decrease in viscosity due to the addition of benzoyl peroxide is suppressed.
  • a decrease in viscosity affects the amount of drug released from the formulation, so it should be avoided in order to ensure the quality of the drug. Since the external pharmaceutical composition of the present invention has a reduced decrease in viscosity over time, it can be applied in a predetermined amount without particular consideration.
  • the external pharmaceutical composition of the present invention contains a component selected from glycyrrhetinic acids and allantoin in addition to benzoyl peroxide, so that it can be spread smoothly when applied to the skin. There is If it cannot be applied smoothly, it cannot be used comfortably. Since the purpose of topical pharmaceutical preparations is to treat a target disease, QOL deterioration such as discomfort during or after use tends to be neglected compared to topical cosmetic preparations and the like. However, if the feeling of use of the external pharmaceutical preparation is bad, it becomes a psychological hurdle to continuous use, and compliance or adherence decreases. Since the topical pharmaceutical composition of the present invention can be spread smoothly with little friction between the skin when applied, it has a good feeling in use and can avoid a decrease in compliance or adherence.
  • the external pharmaceutical composition of the present invention contains at least one component selected from (A) benzoyl peroxide, (B) (B1) glycyrrhetinic acid, derivatives thereof, and/or salts thereof, and (B2) allantoin.
  • the content of benzoyl peroxide relative to the total amount of the composition is 0.05-10% by mass, 0.05-7% by mass, 0.05-5% by mass, 0.05-3.5% by mass, 0.05-3.5% by mass, and 0.05-3.5% by mass.
  • the total concentration of at least one component selected from component (B) glycyrrhetinic acids and allantoin is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, and 0.1% by mass or more, based on the total amount of the composition. 5% by mass or more is more preferable. Also, it is preferably 1.5% by mass or less, more preferably 1% by mass or less, and even more preferably 0.7% by mass or less. Within this range, a sufficient anti-inflammatory action can be obtained, a decrease in viscosity over time can be suppressed, and smooth application can be achieved.
  • Glycyrrhetinic acid which is a glycoside of glycyrrhetinic acid, and glycyrrhizic acid esters such as methyl glycyrrhizinate and stearyl glycyrrhizinate are also examples of derivatives of glycyrrhetinic acid.
  • Glycyrrhizin can also be formulated in the form of licorice or licorice extract.
  • Salts of glycyrrhetic acid or glycyrrhetic acid derivatives are preferably ammonium salts and alkali metal salts, more preferably ammonium salts, potassium salts and sodium salts, and particularly preferably monoammonium salts, dipotassium salts and trisodium salts.
  • glycyrrhetinic acids glycyrrhetinic acid, stearyl glycyrrhetinate, glycyrrhizic acid, and salts thereof are preferred, and glycyrrhizic acid and glycyrrhizinate are more preferred.
  • Preferred glycyrrhizinates are monoammonium glycyrrhizinate, dipotassium glycyrrhizinate, and trisodium glycyrrhizinate.
  • Glycyrrhetinic acids can be used alone or in combination of two or more.
  • the concentration of glycyrrhetinic acids is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, more preferably 0.2% by mass, relative to the total amount of the composition. % by mass or more is more preferable. Moreover, 1 mass % or less is preferable, 0.75 mass % or less is preferable, and 0.5 mass % or less is more preferable. Within this range, a sufficient anti-inflammatory action can be obtained, a decrease in viscosity over time can be suppressed, and smooth application can be achieved.
  • the concentration of glycyrrhetinic acids relative to the total amount of the composition is 0.05 to 1% by mass, 0.05 to 0.75% by mass, 0.05 to 0.5% by mass, 0.1 to 1% by mass, 0.05% to 0.75% by mass, 0.05% to 0.5% by mass, 0.1% to 1% by mass. 1 to 0.75% by mass, 0.1 to 0.5% by mass, 0.2 to 1% by mass, 0.2 to 0.75% by mass, and 0.2 to 0.5% by mass.
  • the concentration of allantoin is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, relative to the total amount of the composition. Also, it is preferably 5% by mass or less, more preferably 2% by mass or less, more preferably 1% by mass or less, more preferably 0.5% by mass or less, and more preferably 0.2% by mass or less. Within this range, a sufficient anti-inflammatory action can be obtained, a decrease in viscosity over time can be suppressed, and smooth application can be achieved.
  • the content of allantoin is preferably 0.005 parts by mass or more, more preferably 0.01 parts by mass or more with respect to 1 part by mass of the content of benzoyl peroxide. is more preferable, 0.02 parts by mass or more is preferable, and 0.03 parts by mass or more is more preferable.
  • 0.8 mass part or less is preferable, 0.4 mass part or less is more preferable, 0.2 mass part or less is preferable, and 0.08 mass part or less is more preferable.
  • the ratio of the allantoin content to 1 part by mass of the benzoyl peroxide content is 0.005 to 0.8 parts by mass, 0.005 to 0.4 parts by mass, 0.005 to 0.2 parts by mass, 0.01 to 0.8 parts by mass, 0.01 to 0.4 parts by mass, 0.01 to 0.2 parts by mass, 0.02 to 0.8 parts by mass, 0.02 to 0.4 parts by mass, 0.02 to 0.2 parts by mass, 0.03 to 0.8 parts by mass, 0.03 to 0.4 parts by mass, and 0.03 to 0.2 parts by mass.
  • component (B1) and component (B2) are blended include glycyrrhetinic acid and allantoin, stearyl glycyrrhetinate and allantoin, glycyrrhizic acid and allantoin, monoammonium glycyrrhizinate and allantoin, dipotassium glycyrrhizinate and allantoin, and glycyrrhizin. acid trisodium salt and allantoin.
  • the composition of the present invention desirably contains water.
  • the concentration of water is preferably 25% by mass or more, more preferably 28% by mass or more, and even more preferably 40% by mass or more, relative to the total amount of the composition.
  • 90 mass % or less is preferable, and 80 mass % or less is more preferable. Within this range, destabilization of the composition due to benzoyl peroxide can be avoided, and the effects of the present invention can be sufficiently obtained.
  • the concentration of water relative to the total amount of the composition includes 25 to 90% by mass, 25 to 80% by mass, 28 to 90% by mass, 28 to 80% by mass, 40 to 90% by mass, and 40 to 80% by mass.
  • Higher alcohols include higher alcohols with 12 to 22 carbon atoms.
  • linear saturated alcohols such as lauryl alcohol, myristyl alcohol, cetanol, cetostearyl alcohol, stearyl alcohol, arachyl alcohol, behenyl alcohol; unsaturated alcohols such as oleyl alcohol, selachyl alcohol; hexyldecanol, isostearyl alcohol, octyldodeca decyltetradecanol, lanolin alcohol, branched alcohols such as isostearyl glyceryl ether, and the like.
  • sterols examples include animal sterols such as cholesterol, ergosterol and lanosterol; plant sterols (phytosterols) such as sitosterol, campesterol, stigmasterol, spinasterol and brassicasterol; and sterol derivatives such as phytosteryl hydroxystearate. .
  • animal sterols such as cholesterol, ergosterol and lanosterol
  • plant sterols such as sitosterol, campesterol, stigmasterol, spinasterol and brassicasterol
  • sterol derivatives such as phytosteryl hydroxystearate.
  • silicone oils include methylpolysiloxane, dimethylpolysiloxane, methylphenylpolysiloxane, decamethyltetrasiloxane, methylcyclopentasiloxane, highly polymerized methylpolysiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, and methylhydrogenpolysiloxane.
  • the base used in the present invention is preferably a combination of water and a polyhydric alcohol and/or an oil agent. 1 type selected from the group consisting of linear saturated or unsaturated alcohols of number 12 to 22, etc.) and ester oils (esters of fatty acids with 12 to 22 carbon atoms such as isopropyl myristate and fatty alcohols, etc.) A combination of the above is preferred.
  • sorbitan fatty acid esters propylene glycol fatty acid esters such as propylene glycol monostearate; polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hydrogenated castor Hydrogenated castor oil derivatives such as oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80; polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), polyoxyethylene (20) sorbitan monostearate (polysorbate 60) ), polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (20) sorbitan monooleate (polysorbate 80), polyoxyethylene (20) sorbitan isostearate; polyoxyethylene monococonut oil fatty acid glyceryl; glycerin alkyl ether; stearin Glycerin fatty acid esters such as glyceryl acid, glyceryl myristate, glyceryl oleate,
  • Moisturizing agents include, for example, hyaluronic acid, salts thereof, or derivatives thereof (e.g., sodium hyaluronate, zinc hyaluronate, low-molecular-weight hyaluronic acid, acetylated hyaluronic acid, crosslinked hyaluronic acid derivatives, cationized hyaluronic acid, etc.); chondroitin; Sulfuric acid or its salts; Amino acids such as heparinoids, alanine, serine, aspartic acid, glycine, arginine and derivatives thereof; Polyhydric alcohols such as glycerin, dipropylene glycol and 1,3-butanediol; Sorbitol, xylitol, erythritol, Sugar alcohols such as maltose/sucrose condensate (glucooligosaccharide), hydrolyzed xylan (xylo-
  • Antioxidants include dibutylhydroxytoluene, butylhydroxyanisole, p-hydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, ascorbic acid derivatives (ascorbyl stearate, ascorbyl palmitate, ascorbyl dipalmitate, ascorbyl acid monophosphate, ascorbyl diphosphate, ascorbate triphosphate, ascorbate sulfate, etc.), tocopherol, tocopherol derivatives (tocopherol acetate, tocopherol succinate, tocopherol calcium succinate, etc.), erythorbic acid, L-cysteine hydrochloride etc.
  • thickeners examples include polyvinyl alcohol, polyvinyl pyrrolidone, polyvinyl methyl ether, carboxyvinyl polymer, alkyl acrylate copolymer, alkyl acrylate methacrylate copolymer, and vinyl-based thickeners such as sodium polyacrylate.
  • Thickeners such as methyl cellulose, ethyl cellulose, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose, hydrophobized hydroxypropyl methyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone, polyvinyl methyl ether , guar gum, sclerotium gum, tamarind gum, xanthan gum, dextran, pectin, pullulan, gelatin, locust bean gum, carrageenan, agar, biosaccharide gum, alkyl acrylate methacrylate copolymer, sodium polyacrylate, bentonite, dextrin Fatty acid ester, dimethyldistearylammonium hectorite, sodium alginate, propylene glycol alginate, polyethylene glycol, macrogol, trimethylammonium
  • carboxyvinyl polymer is preferable from the viewpoint of exhibiting remarkable effects of the invention.
  • concentration of the total amount of thickening agent relative to the total amount of the composition may be 0.01 to 0.8% by mass, 0.05 to 0.5% by mass, and 0.1 to 0.2% by mass.
  • Antiseptics or preservatives include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl parahydroxybenzoate, isopropyl parahydroxybenzoate, butyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, parahydroxybenzoic acid.
  • pH adjusters examples include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide, sodium hydroxide, etc.). ), organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, arginine, glycine, etc.), and the like.
  • inorganic acids hydroochloric acid, sulfuric acid, etc.
  • organic acids lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.
  • inorganic bases potassium hydroxide, sodium hydroxide, etc.
  • organic bases triethanolamine, diisopropanolamine, triisopropanolamine, arginine, glycine, etc.
  • Chelating agents include ethylenediaminetetraacetic acid (edetic acid), ethylenediaminetetraacetate (sodium salt (edetate sodium: Japanese Pharmacopoeia, EDTA-2Na, etc.), potassium salt, etc.), phytic acid, gluconic acid, polyphosphoric acid, metalin acids and the like.
  • coloring agents examples include pigments listed in the legal pigment handbook (edited by the Japan Cosmetic Industry Association (2004)).
  • Bioactive or pharmacologically active ingredient Biologically active or pharmacologically active ingredients other than benzoyl peroxide, glycyrrhetinic acids, and allantoin include anti-inflammatory agents (other than glycyrrhetinic acids and allantoin), antipruritic agents (including antihistamines), local anesthetics, and disinfectants (other than benzoyl peroxide). , cooling agents, vitamins, keratin softening ingredients (chemical peeling ingredients), astringent ingredients, and the like. Among them, anti-inflammatory agents, anti-allergic agents, antibacterial agents, keratin softening ingredients, and vitamins are ingredients that are recommended to be used in combination with benzoyl peroxide.
  • Steroidal anti-inflammatory agents include prednisolone, hydrocortisone, cortisone, dexamethasone, triamcinolone, triamcinolone acetonide, difluprednate, mometasone, diflucortolone, fluocinonide, beclomethasone, deprodone, alclomethasone, flumethasone, amcinonide, clobetasone, diflorazone, and derivatives thereof.
  • Antihistamines include diphenhydramine, diphenhydramine hydrochloride, bromodiphenhydramine hydrochloride, clemastine fumarate, chlorphenoxamine hydrochloride, chlorpheniramine, chlorpheniramine maleate, promethazine hydrochloride, cetirizine hydrochloride, meclizine hydrochloride, ketotifen fumarate, olopatadine hydrochloride, fexofenadine hydrochloride, antazoline hydrochloride, azatadine dimaleate, epinastine hydrochloride and the like.
  • Antipruritic agents include crotamiton, ictamol, and moktar.
  • Local anesthetics include lidocaine, lidocaine hydrochloride, dibucaine hydrochloride, benzocaine, bupivacaine hydrochloride, tetracaine hydrochloride, and the like.
  • Bactericides other than benzoyl peroxide include isopropylmethylphenol, phenoxyethanol, benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, cetylpyridinium chloride, sodium benzoate, ethanol, chlorobutanol, sorbic acid, sorbin potassium salt, sodium dehydroacetate, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, butyl parahydroxybenzoate, oxyquinoline sulfate, phenethyl alcohol, benzyl alcohol, salicylic acid, cresol, triclosan and the like.
  • Vitamins include retinol, retinol acetate, retinol palmitate, retinol propionate, retinol derivatives such as retinol linoleate, retinal, retinoic acid, methyl retinoate, ethyl retinoate, retinol retinoate, d- ⁇ -tocopheryl retino Vitamin A such as ate, ⁇ -tocopheryl retinoate, ⁇ -tocopheryl retinoate; , Vitamin E such as (ascorbyl/tocopheryl) potassium phosphate; riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, riboflavin tetranicotinate, etc.
  • Keratin softening ingredients include salicylic acid, salicylic acid derivatives (macrogol salicylate, ethanol salicylate, etc.), glycolic acid, fruit acid, phytic acid, sulfur, urea, resorcinol, phytic acid, lactic acid, lactate, sodium hydroxide, potassium hydroxide. etc.
  • Astringent components include zinc paraphenolsulfonate, zinc oxide, menthol, and ethanol.
  • the formulation form of the composition for external use of the present invention is not particularly limited. Examples include spray agents, aerosol agents, pump foam agents, sheet agents obtained by impregnating a sheet such as nonwoven fabric with a chemical liquid, and stick agents.
  • gel formulations gel formulations
  • emulsion formulations emulsion formulations
  • cream formulations are preferable because they are easy to spread on the skin and have a good feeling in use.
  • the composition of the present invention is smooth, it can be easily spread over a wide area even in the form of a bulky preparation such as a stick type.
  • a stick-type formulation is preferable because the formulation does not stick to the hands.
  • emulsified formulations such as emulsions, creams and emulsion ointments
  • oil-in-water type water-in-oil type may be used. oil-in-water type is preferred.
  • the pH of the pharmaceutical composition of the present invention can be pH 3 to 7.5, preferably pH 3 to 7, more preferably pH 3 to 6.5, and pH 3.5 to 6. is even more preferred, and pH 3.8 to 5.5 is particularly preferred.
  • This pH can be adjusted, for example, by using a pH adjuster. However, this does not apply to formulation forms for which pH measurement is impossible or difficult.
  • the external pharmaceutical composition of the present invention can be used for treating or improving acne and pimples.
  • acnes acne vulgaris is preferred.
  • an anti-inflammatory agent selected from glycyrrhetinic acids and allantoin, it can be used to treat or improve acne and pimples while suppressing irritation caused by benzoyl peroxide.
  • the external pharmaceutical composition of the present invention may be applied to the affected area 1 to 3 times, 1 to 2 times, or once a day.
  • about 0.5 g may be applied to the entire face.
  • the external pharmaceutical composition of the present invention is preferably applied to the skin, and more preferably the skin of the face (especially forehead, chin, cheeks, around the mouth, nose), neck and back.
  • the container for containing the external pharmaceutical composition of the present invention includes bottle type, tube type, jar type, roll-on type, dropper type, spray type, dispenser type, stick type, pouch bag, chia pack and the like.
  • Roll-on type, dropper type, spray type, and dispenser type containers tend to leave part of the contents in the container or clog the discharge port, but the composition of the present invention is smooth, Even relatively hard or highly viscous formulations can flow smoothly from such containers.
  • the material of the container containing the external pharmaceutical composition of the present invention is not particularly limited as long as it can be used as a container for external pharmaceutical preparations.
  • container materials include polyolefin resins, acrylic acid resins, polyesters, polycarbonates, fluororesins, polyvinyl chloride, polyamides, and ABS, which are partially or entirely, preferably entirely, in contact with the external pharmaceutical composition for skin.
  • a container made of at least one material selected from the group consisting of resin, AS resin, polyacetal, modified polyphenylene ether, polyarylate, polysulfone, polyimide, cellulose acetate, aluminum, and glass.
  • polyethylene high density polyethylene (HDPE), low density polyethylene (LDPE), ultra-low density polyethylene, linear low-density polyethylene (LLDPE), ultra-high molecular weight polyethylene, etc.
  • polypropylene PP
  • polyolefin resins such as ethylene/propylene copolymer, polymethylpentene, polybutene-1,1,2-polybutadiene, polyester resins such as polyethylene terephthalate, polybutylene terephthalate, and polyethylene naphthalate are preferred, and polyethylene, polypropylene, and polyethylene terephthalate are preferred.
  • PE polyethylene
  • HDPE high density polyethylene
  • LDPE low density Polyethylene
  • LLDPE linear low density polyethylene
  • polypropylene aluminum
  • container materials can be used. When two or more materials are used, when two or more materials are mixed, when layers containing two or more different materials are laminated, different parts of the container (receiving part, lid, nozzle, etc.) This includes cases where different materials are included.
  • a topical pharmaceutical composition containing benzoyl peroxide is selected from (B) (B1) glycyrrhetinic acid, derivatives thereof, and/or salts thereof, and (B2) allantoin. It includes a method for suppressing a decrease in viscosity over time of a composition for external use, comprising at least one component of the composition for external use. The type and content of each component, the properties of the composition, etc. are as described for the topical pharmaceutical composition of the present invention.
  • the present invention provides (A) a topical pharmaceutical composition containing benzoyl peroxide, (B) (B1) glycyrrhetinic acid, derivatives thereof, and/or salts thereof, and (B2) allantoin.
  • the type and content of each component, the properties of the composition, etc. are as described for the topical pharmaceutical composition of the present invention.
  • the topical pharmaceutical composition of the present invention has little friction with the skin during application and can be spread smoothly, thus avoiding situations such as unapplied or excessive application.
  • Ability to spread smoothly includes less squeaking, less snagging, or less stickiness.
  • composition for external use was prepared so as to have the composition shown in Table 1.
  • the carboxyvinyl polymer was dispersed in water.
  • dipotassium glycyrrhizinate or allantoin was added, it was added in advance.
  • An aqueous solution of triethanolamine was added to this to neutralize it.
  • This mixture was dispersed in 1,3-propylene glycol and finally benzoyl peroxide hydrate was added.
  • the dosage form of the resulting composition is a gel.
  • Table 1 shows the results.
  • benzoyl peroxide Comparative Example 1
  • a composition containing only a base that does not contain benzoyl peroxide Reference Example 1
  • the viscosity ratio decreased.
  • allantoin Comparative Example 1
  • dipotassium glycyrrhizinate Comparative Example 2
  • recovery of the viscosity ratio was observed.
  • both allantoin and dipotassium glycyrrhizinate were blended (Example 3)
  • the viscosity ratio was remarkably recovered.
  • composition for external use of the present invention contains benzoyl peroxide, the decrease in viscosity during storage is suppressed, so no special consideration is required for distribution and storage.
  • external pharmaceutical composition of the present invention can be applied smoothly, it is easy to apply a predetermined amount, and therefore, a predetermined medicinal effect can be obtained. In addition, since it can be applied smoothly, it can be used comfortably.

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Abstract

Une composition pharmaceutique pour application externe qui comprend (A) du peroxyde de benzoyle et (B) au moins un composant choisi parmi l'acide (B1) glycyrrhétinique ainsi que ses dérivés et ses sels et (B2) de l'allantoïne ne subit pas de diminution de viscosité au fil du temps et peut être appliquée et étalée avec douceur sur la peau.
PCT/JP2022/044017 2021-12-14 2022-11-29 Composition pharmaceutique pour application externe contenant du peroxyde de benzoyle WO2023112664A1 (fr)

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