WO2013191293A1 - Composition pharmaceutique contenant du loxoprofène - Google Patents

Composition pharmaceutique contenant du loxoprofène Download PDF

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Publication number
WO2013191293A1
WO2013191293A1 PCT/JP2013/067223 JP2013067223W WO2013191293A1 WO 2013191293 A1 WO2013191293 A1 WO 2013191293A1 JP 2013067223 W JP2013067223 W JP 2013067223W WO 2013191293 A1 WO2013191293 A1 WO 2013191293A1
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Prior art keywords
pharmaceutical composition
oil
loxoprofen
silicate
magnesium
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PCT/JP2013/067223
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English (en)
Japanese (ja)
Inventor
博志 三浦
陽貴 中川
優花 石田
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興和株式会社
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Priority to JP2013547762A priority Critical patent/JP5450910B1/ja
Publication of WO2013191293A1 publication Critical patent/WO2013191293A1/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
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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

Definitions

  • the present invention relates to a pharmaceutical composition containing loxoprofen, which is also known as an active ingredient of Loxonin (registered trademark).
  • Loxoprofen is a kind of non-steroidal anti-inflammatory analgesic (NSAID) (Non-Patent Document 1), and it is effective in treating diseases such as osteoarthritis, myalgia, swelling / pain after trauma, and inflammation / analysis of symptoms. It is used as an active ingredient of external preparations such as gels, poultices and tapes (Non-patent Document 2).
  • terpenes such as menthol and mint oil are blended in external anti-inflammatory analgesics and the like for the purpose of giving a cooling feeling, and external preparations blended with loxoprofen are also known (Patent Documents 1 to 3).
  • polyhydric alcohols, such as polyvinyl alcohol, are mix
  • an object of the present invention is to provide a pharmaceutical composition in which the interaction between loxoprofen or a salt thereof and one or more selected from terpenes and polyhydric alcohols is suppressed.
  • the inventors of the present invention further studied to solve this problem, and as a result, by adding a silicic acid compound such as light anhydrous silicic acid to the loxoprofen or a salt thereof and the interactive component, the interaction was achieved.
  • the present invention has been completed by finding that it can be suppressed.
  • the present invention includes the following components (A), (B) and (C): (A) Loxoprofen or a salt thereof (B) One or more selected from the group consisting of the following components (B-1) and (B-2) (B-1) Terpenes (B-2) Polyhydric alcohol (C ) A pharmaceutical composition containing a silicic acid compound is provided.
  • the present invention provides a pharmaceutical composition containing one or more selected from loxoprofen or a salt thereof, and terpenes and a polyhydric alcohol with reduced interaction, without going through complicated steps. Can do.
  • loxoprofen or a salt thereof includes not only loxoprofen itself but also a pharmaceutically acceptable salt of loxoprofen, and further a solvate of loxoprofen or a pharmaceutically acceptable salt thereof with water, alcohol or the like. It is. These are known compounds, and can be produced by known methods, or commercially available products can be used.
  • loxoprofen or a salt thereof is preferably loxoprofen sodium hydrate (chemical name: Monosodium 2- [4-[(2-oxocyclopentyl) methyl] phenyl] propanoate dihydrate).
  • the content of loxoprofen or a salt thereof is not particularly limited and may be appropriately determined according to the desired anti-inflammatory analgesic effect, but is 0.01 to 45 relative to the total mass of the pharmaceutical composition in terms of loxoprofen sodium anhydride. % By mass is preferable, 0.1 to 40% by mass is more preferable, and 0.5 to 35% by mass is particularly preferable.
  • terpenes are not particularly limited, and examples thereof include monoterpenes and sesquiterpenes. Terpenes may be cyclic or chain type. Examples of such terpenes include, for example, isoborneol, iron, osimene, carveol, carbotanaseton, carbomenton, carvone, caren, caron, camphene, camphor, geraniol, sabinene, safranal, cyclocitral, citral, citronellal, citronellic acid, Citronellol, Cineol, Cymen, Silvestrene, Thymol, Isotjojol, Tujon, Terpineol, Terpinene, Terpinolene, Tricyclene, Nerol, Pinene, Pinoccampheol, Pinol, Piperithenone, Ferrandral, Ferrandrene, Fentchen, Fentyl Alcohol, Per
  • any optical isomer is included in the present invention, and it may be a single optical isomer or a mixture of various optical isomers.
  • camphor, geraniol, citronellal, thymol, terpineol, borneol, menthol, limonene and the like are preferable, d-camphor, dl-camphor, thymol, borneol, l-menthol, dl-menthol are more preferable, l-menthol, Particularly preferred is dl-camphor.
  • an essential oil containing the terpenes as described above may be used.
  • Such essential oils include, for example, anise oil, ylang ylang oil, iris oil, fennel oil, orange oil, cananga oil, chamomile oil, kayap oil, caraway oil, kubeb oil, grapefruit oil, cinnamon oil, coriander oil, saffron oil Oil, salamander oil, perilla oil, citriodora oil, citronella oil, ginger oil, gingergrass oil, gingergrass oil, spearmint oil, peppermint oil, geranium oil, geranium oil, clove oil, turpentine oil, spruce oil , Neroli oil, basil oil, peppermint oil, palmarosa oil, pimento oil, petitgren oil, bay oil, peniroyal oil, henoposi oil, bergamot oil, bored rose oil, pepper oil, marjolan oil, mandarin oil,
  • the content of terpenes is not particularly limited, but is preferably 0.01 to 45% by mass, more preferably 0.1 to 40% by mass, and 0.5 to 35% by mass with respect to the total mass of the pharmaceutical composition. Particularly preferred.
  • the essential oil is preferably 0.1 to 50% by mass, more preferably 0.5 to 40% by mass, and particularly preferably 1 to 35% by mass with respect to the total mass of the pharmaceutical composition.
  • the content ratio of loxoprofen or a salt thereof and terpenes contained in the pharmaceutical composition of the present invention is not particularly limited, but terpenes are added in an amount of 0.1 part by mass to 1 part by mass of loxoprofen or a salt thereof in terms of anhydrous loxoprofen sodium.
  • terpenes are added in an amount of 0.1 part by mass to 1 part by mass of loxoprofen or a salt thereof in terms of anhydrous loxoprofen sodium.
  • Those containing 01 to 15 parts by mass are preferred, those containing 0.1 to 10 parts by mass are more preferred, and those containing 0.5 to 7 parts by mass are particularly preferred.
  • loxoprofen or a salt thereof contains 0.1 to 40 parts by mass of essential oil, and 0.25 to 30 parts by mass with respect to 1 part by mass in terms of anhydrous loxoprofen sodium. Are more preferable, and those containing 0.5 to 20 parts by mass are particularly preferable.
  • polyhydric alcohol means an alcohol having two or more hydroxyl groups in the same molecule.
  • propylene glycol, glycerin, 1,3-butylene glycol, sorbitol, mannitol, dipropylene glycol, polyvinyl examples include alcohol and macrogol. Among these, glycerin, 1,3-butylene glycol, sorbitol, mannitol, dipropylene glycol, and polyvinyl alcohol are preferable, and polyvinyl alcohol is more preferable.
  • Polyvinyl alcohol is a polymer obtained by saponifying polyvinyl acetate, and can be produced by a known method, or a commercially available product can be used.
  • the degree of polymerization of vinyl acetate, which is a raw material for polyvinyl alcohol, can be adjusted as appropriate, and the degree of saponification can be adjusted as appropriate.
  • the polymerization degree and saponification degree of vinyl acetate are not particularly limited, and may be determined by appropriate examination.
  • the degree of polymerization is preferably about 200 to 3500, and particularly preferably about 300 to 2200.
  • the degree of saponification is preferably 65 to 100 mol%, more preferably 78 to 97 mol%.
  • those having a saponification degree of 78 to 96 mol% (referred to as polyvinyl alcohol (partially saponified product)) and those having 97 mol% or more (referred to as polyvinyl alcohol (completely saponified product)) are more preferable.
  • 78 to 96 mol% is particularly preferable.
  • the content of the polyhydric alcohol is not particularly limited, but is preferably 0.005 to 80% by mass, more preferably 0.01 to 70% by mass, and 0.02 to 60% by mass with respect to the total mass of the pharmaceutical composition. % Is more preferable, 0.1 to 50% by mass is even more preferable, and 0.2 to 40% by mass is particularly preferable.
  • the content ratio of loxoprofen or a salt thereof and a polyhydric alcohol contained in the pharmaceutical composition of the present invention is not particularly limited, but the polyhydric alcohol is 1 part by mass of loxoprofen or a salt thereof in terms of loxoprofen sodium anhydride. Is preferably 0.005 to 80 parts by mass, more preferably 0.01 to 70 parts by mass, further preferably 0.02 to 60 parts by mass, and 0.1 to 50 parts by mass Even more preferred are those containing 0.2 to 40 parts by weight.
  • examples of the “silicic acid compound” include silicate compounds and salts of silicate compounds.
  • a salt of such a silicic acid compound an inorganic salt is preferable.
  • examples of the inorganic salt include metal salts, and examples of the metal constituting the metal ion include alkaline earth metals such as magnesium and calcium; alkali metals such as sodium; and group 13 metals such as aluminum. It is done.
  • silicic acid compound as described above include hydrous silicic acid compounds such as hydrous silicon dioxide, hydrous magnesium silicate, hydrous magnesium silicate (natural) or salts thereof; light anhydrous silicic acid such as light anhydrous silicic acid; Salts thereof: Silicic acid such as silicon dioxide, synthetic aluminum silicate, synthetic sodium magnesium silicate, calcium silicate, magnesium silicate, magnesium aluminum silicate, magnesium aluminate silicate, magnesium magnesium silicate, or salts thereof Diatomaceous earth, bentonite, kaolin and the like. These may be used alone or in combination of two or more.
  • hydrous silicon dioxide, hydrous magnesium silicate, hydrous magnesium silicate (natural), light anhydrous silicic acid, silicon dioxide, calcium silicate, magnesium aluminate, magnesium metasilicate, and kaolin are preferable.
  • light anhydrous silicic acid is particularly preferable.
  • the said silicic acid compound is a well-known thing, besides being able to manufacture by a well-known method, a commercially available thing can be used.
  • the content of the silicate compound is not particularly limited, but is preferably 0.1 to 45% by mass, more preferably 0.5 to 40% by mass, based on the total mass of the pharmaceutical composition, from the viewpoint of the interaction inhibitory action. 1 to 35% by mass is particularly preferable.
  • the content ratio of loxoprofen or a salt thereof contained in the pharmaceutical composition of the present invention and a silicate compound is not particularly limited, and loxoprofen or a salt thereof is 1 in terms of loxoprofen sodium anhydride from the viewpoint of interaction inhibition action.
  • loxoprofen or a salt thereof is 1 in terms of loxoprofen sodium anhydride from the viewpoint of interaction inhibition action.
  • Those containing 0.1 to 45 parts by mass of silicate compound relative to parts by mass are preferred, those containing 0.5 to 40 parts by mass are more preferred, and those containing 1 to 35 parts by mass are particularly preferred.
  • the pharmaceutical composition of the present invention can be produced by, for example, a known method described in the 16th revised Japanese Pharmacopoeia General Rules for Preparations.
  • the dosage form is not particularly limited, and may be any of solid, semi-solid, and liquid shapes, and may be a shape usually used in pharmaceuticals depending on the purpose of use and the like. it can. Specifically, preparations for oral administration (tablets, capsules, granules, powders, oral solutions, syrups, oral jelly, etc.), preparations applied to the vagina (vagina tablets, vaginal suppositories, etc.), skin, etc.
  • a semi-solid or liquid preparation for example, a water-containing composition
  • an oral solution, syrup, external solution, spray, ointment, cream, gel, or patch is preferable, and in particular, an oral solution, syrup, external solution, spray, ointment, cream, gel, or patch.
  • it is a liniment, lotion, external aerosol, pump spray, ointment, cream, gel, tape or poultice.
  • Examples of the route of administration of the pharmaceutical composition of the present invention include oral, transdermal and parenteral such as transvaginal.
  • parenteral is preferred, and transdermal administration is particularly preferred.
  • a drug other than loxoprofen or a salt thereof, terpenes, polyhydric alcohol and silicate compound for example, analgesic ingredient, anti-inflammatory ingredient, antihistamine ingredient, bactericidal ingredient, astringent Protective ingredients, blood circulation promoting ingredients, warmth ingredients, local anesthetic ingredients, antitussives, noscapine, bronchodilators, expectorants, hypnotic sedatives, vitamins, anti-inflammatory agents, gastric mucosal protective agents, antacids, anticholinergics 1 type, or 2 or more types selected from the group consisting of herbal medicines, Chinese medicine prescriptions and the like may be included.
  • analgesic ingredient for example, analgesic ingredient, anti-inflammatory ingredient, antihistamine ingredient, bactericidal ingredient, astringent Protective ingredients, blood circulation promoting ingredients, warmth ingredients, local anesthetic ingredients, antitussives, noscapine, bronchodilators, expectorants, hypnotic sedative
  • analgesic component for example, aspirin, aspirin aluminum, acetaminophen, isopropylantipyrine, ibuprofen, ethenzamide, sazapyrine, salicylamide, salicylic acid, ethylene glycol salicylate, glycol salicylate, sodium salicylate, methyl salicylate, thiaramide hydrochloride, lactylphenetidine Etc.
  • the anti-inflammatory component include sodium guaiazulene sulfonate, glycyrrhizic acid, glycyrrhetinic acid, dipotassium glycyrrhizinate and the like.
  • Antihistamine components include, for example, azelastine hydrochloride, alimemazine tartrate, istipendil hydrochloride, iproheptin hydrochloride, epinastine hydrochloride, emedastine fumarate, ketotifen fumarate, triprolidine hydrochloride, tripelenamine hydrochloride, tondylamine
  • examples thereof include hydrochloride, phenetazine hydrochloride, promethazine hydrochloride, promethazine methylene disalicylate, mequitazine, methodirazine hydrochloride, and mebhydroline napadisilate.
  • Examples of the sterilizing component include benzalkonium chloride.
  • Examples of the astringent / protective component include zinc oxide.
  • Examples of the blood circulation promoting component include tocopherol acetate, benzyl nicotinate, heparin-like substances, sodium polyethylene sulfonate, and the like.
  • Examples of the warm sensation component include nonanoic acid vanillylamide, capsaicin, red pepper and the like.
  • Examples of the local anesthetic component include lidocaine, clove oil, belladonna extract and the like.
  • Antitussives include, for example, aloclamide hydrochloride, eprazinone hydrochloride, carbetapentane enoate, cloperastine hydrochloride, cloperastine phendizoate, dibutate sodium, dimemorphan phosphate, tipepidine citrate, And tipepidine hibenzate.
  • noscapine examples include noscapine hydrochloride and noscapine.
  • bronchodilator examples include trimethquinol hydrochloride, phenylephrine hydrochloride, methoxyphenamine hydrochloride and the like.
  • expectorants examples include ammonia, fennel, ammonium chloride and the like.
  • Vitamins include vitamin B 1 , vitamin B 2 , vitamin B 5 , vitamin B 6 , vitamin B 12 , vitamin C, hesperidin and derivatives thereof, and salts thereof (for example, thiamine, thiamine chloride hydrochloride, thiamine nitrification) , Dicetiamine hydrochloride, cetothiamine hydrochloride, fursultiamine, fursultiamine hydrochloride, octothiamine, chicotiamine, thiamine disulfide, bisbutiamine, bisbenchamine, prosultiamine, benfotiamine, riboflavin, riboflavin phosphate , Riboflavin butyrate, sodium riboflavin phosphate, panthenol, panthetin, sodium pantothenate, pyridoxine hydrochloride,
  • anti-inflammatory agent examples include glycyrrhizic acid and derivatives thereof and salts thereof (for example, dipotassium glycyrrhizinate and monoammonium glycyrrhizinate), seaprose, semi-alkaline proteinase, serrapeptase, proctase, pronase, bromelain and the like.
  • gastric mucosa protective agent examples include gefarnate, cetraxate hydrochloride, sofalcone, teprenone, methylmethionine sulfonium chloride and the like.
  • anticholinergic agents examples include oxyphencyclimine hydrochloride, dicyclomine hydrochloride, methixene hydrochloride, tipepidium bromide, methylbenactidium bromide, pirenzepine hydrochloride, isopropamide iodide, diphenylpiperidinomethyldioxolane iodide, etc. .
  • Herbal medicines include Akamegashiwa (red buds), Asenyaku (Asenyaku), Arnica, Yinakukaku (Oyakukan), Fennel (Yellow), Turmeric (Yongyin), Engosaku (Yankou), Ogon (Yellow), Ousei (Yellow) , Owaku (yellow cocoon), Spruce (cherry bark), Oulen (yellow ren), Onji (distant), Gajutsu (Iso), valerian grass (Chicken grass), Chamomile, Karonin (Karojin), Kyo-kyo (kikyo), Kyonin (Kyojin), Kukoshi (Birch), Kukoyo (Bamboo Leaves), Keigai (Kashiwagi), Keihi (Kinshikashi), Ketsumeishi (Keiko), Gentiana, Gennoshouko (Current Evidence), Kouka (Safflower), Koubushi (Kagoshi
  • Herbal formulas include Keishito (Keishaeyu), Kousosan (Kousosan), Psychokeito (Shibako Keiedo), Shosai Koto (Koshisaifuto), Bakumondou (Bakumon Fuyuto), Hangekou Bokuto (Hankatsu Koboku-yu).
  • the pharmaceutical composition of the present invention contains loxoprofen, which is a kind of NSAID, or a salt thereof, it can be used as a medical drug or an OTC drug.
  • loxoprofen which is a kind of NSAID, or a salt thereof
  • it can be used as a medical drug or an OTC drug.
  • osteoarthritis, myalgia and after trauma It is useful as an analgesic / anti-inflammatory agent, etc., because it has efficacy or effect such as anti-inflammatory / analgesic disease selected from swelling and pain.
  • Example 1-A Loxoprofen sodium hydrate (Daiwa Pharmaceutical Co., Ltd .: trade name: Japanese Pharmacopoeia Loxoprofen sodium hydrate) 2g and l-menthol (Takasago Fragrance: trade name: l-menthol) 2g were mixed, and this mixture was put in a glass bottle. Sample 1-A was obtained.
  • Example 1-B Loxoprofen sodium hydrate (manufactured by Daiwa Pharmaceutical Co., Ltd .: trade name, Japanese Pharmacopoeia Loxoprofen sodium hydrate) 2 g, l-menthol (trade name, l-menthol), 2 g of light anhydrous silicic acid (manufactured by Nippon Aerosil Co., Ltd .: product) No. Aerosil 300) 2 g was mixed, and this mixture was placed in a glass bottle to obtain Sample 1-B.
  • Example 2-A Loxoprofen sodium hydrate (Daiwa Pharmaceutical Co., Ltd .: trade name: Japanese Pharmacopoeia Loxoprofen sodium hydrate) 2g and polyvinyl alcohol (partially saponified product) (Nippon Synthetic Chemical Industry: trade name: Gohsenol EG-40) were mixed, This mixture was placed in a glass bottle to obtain Sample 2-A.
  • Example 2-B Loxoprofen sodium hydrate (manufactured by Daiwa Pharmaceutical Co., Ltd .: trade name: Japanese Pharmacopoeia Loxoprofen sodium hydrate) 2 g, polyvinyl alcohol (partially saponified product) (manufactured by Nippon Synthetic Chemical Industry Co., Ltd .: trade name: Gohsenol EG-40) and light anhydrous silica 2 g of acid (product name: Aerosil 300 manufactured by Nippon Aerosil Co., Ltd.) was mixed, and this mixture was placed in a glass bottle to obtain Sample 2-B.
  • the interaction between loxoprofen or a salt thereof and an interactive component can be suppressed. Therefore, it is possible to provide a pharmaceutical composition comprising loxoprofen or a salt thereof and an interactive component, which has excellent storage stability. Since the pharmaceutical composition of the present invention contains loxoprofen, which is a kind of NSAID, it is effective for, for example, diseases selected from osteoarthritis, myalgia and swelling / pain after trauma, as well as anti-inflammatory / analgesic symptoms. It can be suitably used as a pharmaceutical composition.
  • loxoprofen which is a kind of NSAID

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Abstract

La présente invention concerne une composition pharmaceutique dans laquelle l'interaction entre le loxoprofène ou son sel et un composant interactif est inhibée. L'invention porte plus particulièrement sur une composition pharmaceutique contenant les composants (A), (B) et (C) suivants : (A) du loxoprofène ou son sel ; (B) une ou plusieurs substances sélectionnées dans le groupe constitué des composants (B-1) terpènes et (B-2) alcools polyhydriques ; et (C) un composé d'acide silicique.
PCT/JP2013/067223 2012-06-22 2013-06-24 Composition pharmaceutique contenant du loxoprofène WO2013191293A1 (fr)

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JP2013547762A JP5450910B1 (ja) 2012-06-22 2013-06-24 ロキソプロフェンを含有する医薬組成物

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JP2012140972 2012-06-22
JP2012-140972 2012-06-22
JP2013-117460 2013-06-04
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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015083563A (ja) * 2013-09-18 2015-04-30 第一三共ヘルスケア株式会社 ロキソプロフェン配合皮膚外用液剤
EP2926810A1 (fr) * 2014-03-31 2015-10-07 Sanovel Ilac Sanayi ve Ticaret A.S. Formulations pharmaceutiques liquides orales de loxoprophène
EP2926832A1 (fr) * 2014-03-31 2015-10-07 Sanovel Ilac Sanayi ve Ticaret A.S. Formulations pharmaceutiques pour une utilisation topique du loxoprofène
JP2017200909A (ja) * 2016-04-27 2017-11-09 第一三共ヘルスケア株式会社 ロキソプロフェン配合皮膚用外用剤
JP2017226623A (ja) * 2016-06-23 2017-12-28 救急薬品工業株式会社 非水性貼付剤
JP2018065878A (ja) * 2013-04-25 2018-04-26 第一三共ヘルスケア株式会社 ロキソプロフェン含有外用剤組成物
JP2018123172A (ja) * 2013-03-29 2018-08-09 興和株式会社 ロキソプロフェン含有外用固形剤
KR20180098233A (ko) 2015-12-25 2018-09-03 코와 가부시키가이샤 록소프로펜을 함유하는 의약 제제
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JP2017137304A (ja) * 2016-01-29 2017-08-10 興和株式会社 ロキソプロフェンを含有する医薬製剤
JP7186026B2 (ja) * 2018-06-27 2022-12-08 小林製薬株式会社 外用医薬組成物
JP7186025B2 (ja) * 2018-06-27 2022-12-08 小林製薬株式会社 外用医薬組成物
JP7186024B2 (ja) * 2018-06-27 2022-12-08 小林製薬株式会社 外用医薬組成物
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JP2018123172A (ja) * 2013-03-29 2018-08-09 興和株式会社 ロキソプロフェン含有外用固形剤
JP2018065878A (ja) * 2013-04-25 2018-04-26 第一三共ヘルスケア株式会社 ロキソプロフェン含有外用剤組成物
JP2015083563A (ja) * 2013-09-18 2015-04-30 第一三共ヘルスケア株式会社 ロキソプロフェン配合皮膚外用液剤
EP2926810A1 (fr) * 2014-03-31 2015-10-07 Sanovel Ilac Sanayi ve Ticaret A.S. Formulations pharmaceutiques liquides orales de loxoprophène
EP2926832A1 (fr) * 2014-03-31 2015-10-07 Sanovel Ilac Sanayi ve Ticaret A.S. Formulations pharmaceutiques pour une utilisation topique du loxoprofène
KR20180098233A (ko) 2015-12-25 2018-09-03 코와 가부시키가이샤 록소프로펜을 함유하는 의약 제제
JP2017200909A (ja) * 2016-04-27 2017-11-09 第一三共ヘルスケア株式会社 ロキソプロフェン配合皮膚用外用剤
JP7325168B2 (ja) 2016-04-27 2023-08-14 第一三共ヘルスケア株式会社 ロキソプロフェン配合皮膚用外用剤
JP2017226623A (ja) * 2016-06-23 2017-12-28 救急薬品工業株式会社 非水性貼付剤
WO2020262057A1 (fr) * 2019-06-24 2020-12-30 帝國製薬株式会社 Timbre adhésif à base d'eau
CN114007594A (zh) * 2019-06-24 2022-02-01 帝国制药株式会社 水性贴剂
WO2022172915A1 (fr) * 2021-02-10 2022-08-18 コスメディ製薬株式会社 Préparation transdermique contenant un antioxydant

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