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WO2020116570A1 - Préparation topique pour la peau - Google Patents

Préparation topique pour la peau Download PDF

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Publication number
WO2020116570A1
WO2020116570A1 PCT/JP2019/047652 JP2019047652W WO2020116570A1 WO 2020116570 A1 WO2020116570 A1 WO 2020116570A1 JP 2019047652 W JP2019047652 W JP 2019047652W WO 2020116570 A1 WO2020116570 A1 WO 2020116570A1
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Prior art keywords
group
steroid
skin
resolvin
external preparation
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Ceased
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PCT/JP2019/047652
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English (en)
Japanese (ja)
Inventor
健治 椛島
本田　哲也
雄宇 澤田
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Lydia O'leary Memorial Pias Dermatological Foundation
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Lydia O'leary Memorial Pias Dermatological Foundation
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Priority to JP2020560012A priority Critical patent/JP7309215B2/ja
Publication of WO2020116570A1 publication Critical patent/WO2020116570A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/202—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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 skin external preparation.
  • Steroids have been widely used as pharmaceuticals since they have many actions such as anti-inflammatory, anti-allergic, or immunosuppression.
  • injections Steroid preparations having various dosage forms such as oral preparations, suppositories, and external preparations are known.
  • the widespread use of steroid preparations is due to the strong activity of steroids.
  • side effects also strongly appear in proportion to this activity. Therefore, clinically, steroids are currently used in consideration of their efficacy and side effects.
  • steroid external preparations used for the treatment of eczema are classified into 5 groups (group I: strongest, group II: very strong, group III: strong, group IV: medium, group V: weak) depending on the strength of anti-inflammatory action. Often classified into. Since the occurrence of side effects is almost parallel to the strength of drug efficacy, this classification is extremely useful when used in actual patients.
  • Patent Document 1 in the oil containing the long-chain ⁇ -3 polyunsaturated fatty acid extracted from organisms such as fish and crustaceans, a specific inflammation converging mediator (Specialized Proresolving Mediator: SPM) and It contains an SPM precursor, and the SPM contains Resolvin E1 (5S,12R,18R-trihydroxy-eicosa-6Z,8E,10E,14Z,16E-pentaenoic acid).
  • SPM Specific inflammation converging mediator
  • Resolvin E1 5S,12R,18R-trihydroxy-eicosa-6Z,8E,10E,14Z,16E-pentaenoic acid.
  • Patent Document 1 does not describe how much resolvin E1 exerts an anti-inflammatory effect on the skin.
  • the present invention has been made in view of the above-mentioned conventional state of the art, and an object thereof is to provide a skin external preparation. Further, a preferred object of the present invention is to provide an external preparation for skin having an excellent anti-inflammatory effect. Further, a preferred object of the present invention is to provide an external preparation for skin which has excellent anti-inflammatory effect, particularly excellent durability, and has few side effects.
  • the present inventors have conducted intensive studies to achieve the above-mentioned object, and as a result, by combining resolvin E1 and a steroid drug classified as a glucocorticoid receptor agonist, the anti-inflammatory effect of both is enhanced and , Found that sustainability is enhanced.
  • the steroid drug is classified as a V group (weak) in terms of classification, when used in combination with Resolvin E1, it has the same level as a steroid drug classified as a III group (strong). It has been found that a strong anti-inflammatory effect is obtained, and further, a decrease in the anti-inflammatory effect over time is suppressed, and a good anti-inflammatory effect lasts for a long time. Since steroids classified into group V (weak) have low side effects corresponding to the degree of drug efficacy, it can be said that it is desirable that the combination with resorbin E1 enhances the anti-inflammatory effect and maintains it.
  • the present invention has been completed by further research based on these findings, and has the following embodiments.
  • External preparation for skin An external preparation for skin which is a combination of resolvin E1 and a glucocorticoid receptor agonist.
  • I-2 A composition (combination drug) in which the combination of resolvin E1 and a glucocorticoid receptor agonist contains resolvin E1 and a glucocorticoid receptor agonist, or a preparation containing resolvin E1 (for example, skin
  • the external preparation for skin according to (I-1) which is a combination product (kit, set) of a preparation (external preparation) and a preparation containing a glucocorticoid receptor agonist (for example, external preparation for skin).
  • V group steroid drug a steroid drug classified into V group (weak)
  • IV group a steroid drug classified into IV group (medium)
  • An external preparation for skin which is a combination with a group IV steroid.
  • composition (combined preparation) containing the resolvin E1 and a group V steroid agent or a group IV steroid agent containing the resolvin E1 and a group V steroid agent or a group IV steroid agent, or resolvin E1 A combination product (kit, set) of a preparation containing (for example, a skin external preparation) and a preparation containing a group V steroid agent or a preparation containing a group IV steroid agent (for example, a skin external preparation), (I -3) External preparation for skin.
  • Group V steroid is selected from the group consisting of prednisolone, prednisolone acetate, fradiomycin sulfate, dexamethasone, hydrocortisone acetate, fludoxycortide, betamethasone, a mixture of betamethasone and chlordeniramine maleate, and hydrocortisone.
  • the at least one group IV steroid is at least one selected from the group consisting of valeric acid/prednisolone acetate, hydrocortisone butyrate, clobetasone butyrate, alclomethasone propionate, triamcinolone acetonide, and flumethasone pivalate.
  • the external preparation for skin according to I-3) or (I-4).
  • the glucocorticoid receptor agonist, or the group V or IV steroid is prednisolone, prednisolone acetate, valeric acid/prednisolone acetate, hydrocortisone, hydrocortisone acetate, hydrocortisone butyrate, dexamethasone, betamethasone, betamethasone and malein.
  • the glucocorticoid receptor agonist or the V-group steroid is at least one selected from the group consisting of prednisolone and prednisolone acetate.
  • the external preparation for skin according to any one of items.
  • the resolvin E1 and the glucocorticoid receptor agonist or the steroid drug are used in a molar ratio of 1:1000 to 1:2, preferably 1:100 to 1:10, more preferably 1:50 to
  • (I-10) For treating or preventing at least one skin disease selected from the group consisting of eczema, dermatitis, psoriasis, prurigo group, palmoplantar pustulosis, pruritus cutis, erythema, and erythroderma
  • the external preparation for skin according to any one of (I-1) to (I-9), which is a pharmaceutical.
  • (II) Method of using external preparation for skin (II-1)
  • a step of applying an effective amount of the external preparation for skin according to any one of (I-1) to (I-10) above to the skin of mammals A method for reducing inflammation of the skin, comprising: (II-2)
  • the mammal has at least one skin disease selected from the group consisting of eczema, dermatitis, psoriasis, prurigo group, palmoplanter pustulosis, pruritus cutaneus, erythema, and erythroderma.
  • (II-1) which is an affected animal, and which has a step of applying an effective amount of the external preparation for skin according to any one of (I-1) to (I-10) to the affected area How to list.
  • (II-3) A combination of resolvin E1 and a glucocorticoid receptor agonist, or a combination of resolvin E1 and a group V or group IV steroid drug, which is used for the prevention or treatment of skin inflammation.
  • (II-4) Use for prevention or treatment of at least one skin disease selected from the group consisting of eczema, dermatitis, psoriasis, prurigo group, palmoplanter pustulosis, pruritus cutis, erythema, and erythroderma
  • Prophylactic or therapeutic agent for at least one skin disease selected from the group consisting of eczema, dermatitis, psoriasis, prurigo group, palmoplanter pustulosis, pruritus cutis, erythema, and erythroderma
  • An external preparation for skin comprising a combination of resolvin E1 which is one aspect of the present invention and a steroid drug classified as a glucocorticoid receptor agonist exhibits a high anti-inflammatory effect and is durable when used in combination. It is useful as an anti-inflammatory agent.
  • a skin external preparation comprising a combination of the resolvin E1 which is one embodiment of the present invention and a steroid agent (group V steroid agent or group IV steroid agent) classified into V group (weak) or IV group (medium) in classification. By including both, it is possible to obtain an anti-inflammatory effect equivalent to that of the class III (strong) steroid drug in terms of classification.
  • the external preparation for skin of the present invention can reduce the side effects that may occur due to the use of steroids. Therefore, the external preparation for skin is useful as an anti-inflammatory agent that exerts a high anti-inflammatory effect while suppressing the occurrence of side effects. Furthermore, the external preparation for skin which is a combination of Resolvin E1 and a group V or group IV steroid, preferably a group V steroid, has a long-lasting efficacy in addition to the above-mentioned effects, while suppressing the occurrence of side effects. It is also useful as a long-lasting anti-inflammatory agent that exerts a high anti-inflammatory effect.
  • External preparation for skin is an external preparation for skin obtained by combining resolvin E1 and a glucocorticoid receptor agonist.
  • Resolvin E1 is 5S,12R,18R-trihydroxy-eicosa-6Z,8E,10E,14Z,16E-pentaenoic acid, which is a compound known as a specific inflammatory converging mediator (SPM).
  • SPM specific inflammatory converging mediator
  • RvE1 can be produced according to a known production method, for example, the production method described in Ogawa N, Kobayashi Y. Tetrahedron lett. 2009; 50:6079-6082.
  • RvE1 is a natural component contained in oil containing long-chain ⁇ -3 polyunsaturated fatty acids extracted from fish, crustaceans, algae, or molluscs, It can also be extracted and isolated from an oil containing a polyunsaturated fatty acid (for example, Patent Document 1 described above).
  • the RvE1 used in the present invention may be a synthetic product or a naturally derived product as long as it has the effect. Further, it may be a purified product or a crudely purified product. Examples of the crude product include, but are not limited to, the aforementioned long-chain ⁇ -3 polyunsaturated fatty acid-containing oil, or its RvE1-containing fraction.
  • a glucocorticoid receptor agonist is a drug that exerts a medicinal effect including an anti-inflammatory action by binding to a glucocorticoid receptor.
  • Examples of the steroid drug classified as a glucocorticoid receptor agonist include, but are not limited to, the following (Nippon Pharmacologic Journal, Folia Pharmacol. Jpn. 128, 411-415, 2006).
  • Clobetasol propionate diftrazone acetate; mometasone furoate, betamethasone butyrate propionate, fluocinonide, betamethasone dipropionate, difluprednate, putesonide, amcinonide, diflucortron valerate, hydrocortisone butyrate propionate dexamethasone oxalate, dexamethasone valerate, , Betamethasone valerate, beclomethasone propionate, fluocinolone acetonide; prednisolone valerate acetate, triamcinolone acetonide, flumethasone pivalate, alclomethasone propionate, clobetasone butyrate hydrocortisone butyrate, dexamethasone; prednisolone, hydrocortisone acetate.
  • glucocorticoid receptor agonists compounds that are preferably classified as group V steroids or compounds that are classified as group IV steroids, and more preferably compounds that are classified as group V steroids.
  • These compounds have the advantage of low side effects, as described below, while their efficacy is relatively low or mild.
  • the combined use of RvE1 significantly enhances the drug effect (particularly the anti-inflammatory effect), and thus has an advantage that the benefit (merit) obtained by using RvE1 in combination is high.
  • the combined use of a compound classified as a V group or IV group steroid with RvE1 is also useful in that the durability of the anti-inflammatory effect is improved. That is, the external preparation for skin of this aspect is useful as a minimally invasive, persistent anti-inflammatory agent.
  • Examples of the glucocorticoid receptor agonist used in combination with RvE1 include preferably prednisolone and its salts, which are preferably classified into Group V. Among them, prednisolone acetate is preferable. By combining these, a long-lasting anti-inflammatory effect and/or a high side effect reducing effect can be obtained.
  • the ratio contained in the final preparation of RvE1 used in combination with the glucocorticoid receptor agonist is within a range in which the effect of the present invention is exerted. Although it is good, a range of 0.0001 to 0.1% by mass can be usually mentioned. It is preferably about 0.0005 to 0.01% by mass, and more preferably about 0.001 to 0.002% by mass. Further, the combination ratio of RvE1 and the glucocorticoid receptor agonist can be exemplified by a molar ratio in the range of 1:1000 to 1:2. It is preferably 1:100 to 1:10, more preferably 1:50 to 1:5.
  • Another aspect of the present invention is an external preparation for skin, which is a combination of RvE1 and a group V steroid or a group IV steroid.
  • the external preparation for skin of this embodiment contains RvE1 and a group V steroid agent or a group IV steroid agent to obtain an anti-inflammatory effect equivalent to that of a group III (strong) steroid agent (group III steroid agent).
  • group III strong
  • group III steroid agent group III steroid agent
  • group III steroid agent group III steroid agent
  • group V steroids and group IV steroids have fewer side effects than group III steroids, while suppressing and reducing side effects caused by the use of steroids, an anti-inflammatory effect equivalent to that of group III steroids can be obtained.
  • the external preparation for skin of this aspect is also useful in that the durability of the anti-inflammatory effect is better than that of the group III steroid. That is, the external preparation for skin of this aspect is useful as a minimally invasive, persistent anti-inflammatory agent.
  • the Group V steroids include, but are not limited to, prednisolone, prednisolone acetate, fradiomycin, dexamethasone sulfate, hydrocortisone, hydrocortisone acetate, fludoxycortide, betamethasone, and a mixture of betamethasone and chlordeniramine maleate. These can be used in combination with RvE1 either alone or in combination of two or more, and optionally in combination with a group IV steroid.
  • prednisolone and its salts are preferable because of their excellent anti-inflammatory effect persistence and large side effect reducing effect, and among them, prednisolone acetate is more preferable.
  • group IV steroids include, but are not limited to, valeric acid/prednisolone acetate, clobetasone butyrate, alclomethasone propionate, hydrocortisone butyrate, triamcinolone acetonide, and flumethasone pivalate. These can be used in combination with RvE1 alone or in combination of two or more, and optionally in combination with a Group V steroid.
  • the ratio contained in the final preparation of RvE1 used in combination with the steroid agent may be within the range that produces the effect of the present invention, Usually, the range of 0.0001 to 0.1 mass% can be mentioned. It is preferably about 0.0005 to 0.01% by mass, and more preferably about 0.001 to 0.002% by mass.
  • the combination ratio of RvE1 and the steroid agent can be exemplified in the range of 1:1000 to 1:2 as a molar ratio. It is preferably 1:100 to 1:10, more preferably 1:50 to 1:5.
  • “combination” means that the external preparation for skin of the present invention is (I) When RvE1 and a glucocorticoid receptor agonist or a group V or group IV steroid agent are contained in the same preparation in a mixed state (combined preparation), (Ii) A preparation containing RvE1 and a preparation containing a glucocorticoid receptor agonist or a group V or group IV steroid agent are packaged as separate preparations, and both are sold as a combination (kit).
  • a preparation containing RvE1 and a preparation containing a glucocorticoid receptor agonist or a group V or group IV steroid are each individual preparations, which are sold as one package in combination.
  • a formulation containing RvE1 and a formulation containing a glucocorticoid receptor agonist or a group V or group IV steroid are present in the market as separate formulations through separate distribution channels, It is used in the meaning including the case of being used in combination at the time of use.
  • the term “combination product” or “skin external preparation consisting of a combination” means that the administration of the preparation containing RvE1 to the skin of the subject (mammal) means that the drug is a glucocorticoid receptor agonist or group V or IV.
  • Administration of a preparation containing a group steroid agent may be carried out at different times, simultaneously or in parallel, and RvE1, a glucocorticoid receptor agonist or a group V or IV group steroid agent in a distribution stage including sales The form is not specifically asked.
  • both formulations are administered at the same time, it is preferable that the user or practitioner use the formulation containing RvE1 and the formulation containing a glucocorticoid receptor agonist or group V or group IV steroid at the time of use.
  • a method may be mentioned in which the compounded ingredients are mixed to prepare a compounded ingredient containing both, and the prepared compounded ingredient is applied to the skin of the subject.
  • the “formulation containing RvE1” as used herein means a preparation in which RvE1 is combined with other components
  • the “formulation containing a glucocorticoid receptor agonist” refers to a glucocorticoid receptor agonist other than It means a preparation in which components are combined
  • a preparation containing a group V or group IV steroid agent means a preparation in which a group V or group IV steroid agent is combined with another component.
  • These formulations include those in the form of external preparations for skin.
  • the other components include carriers or additives for pharmaceutical preparations that are usually used for external medicines.
  • the “combination product” is preferably the compounding agent described in (i) above.
  • the external preparation for skin includes an oily component, an aqueous component, an anti-inflammatory component other than RvE1, an anti-acne component, a whitening component, a preservative, a pH adjusting agent, and A sticking agent, a stabilizer and the like can be added as necessary.
  • oil component examples include cetostearyl alcohol, medium chain fatty acid triglyceride, polyoxyethylene hydrogenated castor oil, glycerin stearate, liquid paraffin, petrolatum, squalane, beeswax, palmitic acid and the like.
  • aqueous component examples include water, propylene glycol, glycerin, polyethylene glycol, 1,3-butylene glycol and the like.
  • anti-inflammatory component other than RvE1 examples include components derived from plants (for example, comfrey), allantoin, glycyrrhizic acid or derivatives thereof, tranexamic acid, zinc oxide, pyridoxine hydrochloride, tocopherol acetate, salicylic acid or derivatives thereof, ⁇ - Examples thereof include aminocaproic acid, pantothenyl alcohol, laurel extract, psyllium extract, quince extract, izayoi extract, and age extract.
  • the anti-acne component is a component effective against acne, and includes, for example, clindamycin, nadifloxacin, sulfur, isopropylmethylferrol, pionine (photosensitizer 201), allantoin, dipotassium glycyrrhizinate, pyridoxine hydrochloride, calamine, guaiazulene sulfone.
  • Antibacterial, antibacterial and anti-inflammatory components such as sodium acidate and stearyl glycyrrhetinate; components with chemical peeling effect such as glycolic acid, lactic acid, salicylic acid, macrogol salicylate, trichloroacetic acid, ascorbic acid, ascorbic acid glucoside, ascorbyl tetrahexyldecanoate, etc. Antioxidants and the like.
  • para-aminobenzoic acid derivatives As whitening ingredients, para-aminobenzoic acid derivatives, salicylic acid derivatives, coumarin derivatives, amino acid compounds, benzotriazole derivatives, tetrazole derivatives, imidazoline derivatives, pyrimidine derivatives, dioxane derivatives, camphor derivatives, furanic acid derivatives, pyrone derivatives, nucleic acid derivatives, allantoin Derivatives, nicotinic acid derivatives, vitamin C or its derivatives (vitamin C phosphate magnesium salt, vitamin C glucoside, etc.), vitamin D or its derivatives, vitamin E or its derivatives, kojic acid or its derivatives, oxybenzone, benzophenone, arbutin, Examples thereof include tranexamic acid, guaiazulene, shikonin, baicalin, baicalein, berberine, placenta extract, ellagic acid, and rucinol.
  • antiseptics examples include parabens and the like.
  • pH adjusters examples include phosphoric acid, citric acid, sodium hydroxide, potassium hydroxide, organic amines and the like.
  • thickener examples include crystalline cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, carboxyvinyl polymer, acrylic acid-alkyl methacrylate copolymer, carmellose sodium, polyvinyl alcohol and the like.
  • stabilizer examples include tocopherol, BHT (dibutylhydroxytoluene), sodium edetate hydrate and the like.
  • the dosage form of the external preparation for skin of the present invention is not particularly limited. Examples of dosage forms include lotions, creams, gels, ointments and the like.
  • the external preparation for skin of the present invention can be prepared according to the usual method for producing an external preparation for skin (16th revised Japanese Pharmacopoeia Manual 2011, A126 to A149).
  • the external preparation for skin of the present invention exerts an anti-inflammatory effect by being applied to a subject's skin, specifically, mammalian skin, preferably human skin in an effective amount, and reduces inflammation in the skin. , Useful for healing and improvement.
  • the external preparation for skin of the present invention exerts an anti-inflammatory effect, so that eczema, dermatitis (including atopic dermatitis and the like), psoriasis, prurigo group, palmoplantar pustulosis, pruritus cutis, erythema. , And/or can be usefully used for treating or preventing skin diseases such as erythroderma.
  • the present invention is a method for reducing inflammation of the skin, which comprises a step of applying an effective amount of the external preparation for skin to the skin of mammals.
  • the mammal preferably includes a human.
  • the mammal also includes at least one skin disease selected from the group consisting of eczema, dermatitis, psoriasis, prurigo group, palmoplantar pustulosis, pruritus cutis, erythema, and erythroderma.
  • the number of applications (the number of applications) and the dose (the amount of application) to the affected area are not limited as long as the effects of the present invention are exhibited.
  • the effective daily amount that exerts an anti-inflammatory effect can be applied once or a plurality of times a day to the affected area.
  • the drugs used are as follows.
  • Vaseline Propeto (registered trademark), manufactured by Maruishi Pharmaceutical Co., Ltd.
  • Predonin eye ointment 0.25% prednisolone acetate ester-containing preparation, manufactured by Shionogi Pharmaceutical Co., Ltd.
  • RvE 1:1 mg RvE1 with ethanol 100 times Prepared by diluting (ethanol containing 1% RvE1)
  • Boala Ointment 0.12% dexamethasone valerate-containing preparation, manufactured by Maruho Co., Ltd.
  • predonin ophthalmic ointment is a steroid drug classified into Group V (weak), and Boala ointment is classified into Group III (strong) It is a steroid drug.
  • DNFB 1-Fluoro-2,4-dinitrobenzene
  • Sensitization induction was performed by applying 0.5% DNFB solution (25 ⁇ l) once to the abdomen of each group of mice (groups 1 to 5) with shaved abdomen and chest. ..

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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne une préparation topique pour la peau qui possède un effet anti-inflammatoire, qui combine de la résolvine E1 à un agoniste du récepteur des glucocorticoïdes, ou qui combine de la résolvine E1 à un stéroïde catégorisé comme appartenant au groupe V (faible) ou à un stéroïde catégorisé comme appartenant au groupe IV (modéré).
PCT/JP2019/047652 2018-12-05 2019-12-05 Préparation topique pour la peau Ceased WO2020116570A1 (fr)

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JP2020560012A JP7309215B2 (ja) 2018-12-05 2019-12-05 皮膚外用剤

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JP2018227868 2018-12-05
JP2018-227868 2018-12-05

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WO2020116570A1 true WO2020116570A1 (fr) 2020-06-11

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PCT/JP2019/047652 Ceased WO2020116570A1 (fr) 2018-12-05 2019-12-05 Préparation topique pour la peau

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JP (1) JP7309215B2 (fr)
WO (1) WO2020116570A1 (fr)

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
ARITA, MAKOTO ET AL.: "Novel chemical mediators in the resolution of inflammation, Resorbin and protectin derived from omega-3 fatty acids", PROTEIN, NUCLEIC ACID AND ENZYME, vol. 52, no. 4, 2007, pages 348 - 354 *
KIM, T. ET AL.: "Omega-3 fatty acid-derived mediator, Resolvin E1, ameliorates 2, 4- dinitrofluorobenzene-induced atopic dermatitis in NC/Nga mice", INTERNATIONAL IMMUNOPHARMACOLOGY, vol. 14, no. 4, 2012, pages 384 - 391, XP055715330, ISSN: 1567-5769 *
SAWADA, Y. ET AL.: "Resolvin E1 attenuates murine psoriatic dermatitis", SCIENTIFIC REPORTS, vol. 8, no. 1, 8 August 2018 (2018-08-08), pages 11873, XP055715331, ISSN: 2045-2322, DOI: 10.1038/s41598-018-30373-1 *
WATANABE, TOSHIYUKI: "Treatment of atopic dermatitis with a new external medicine containing DHA/EPA", ALLERGY IN PRACTICE, vol. 27, no. 12, 2007, pages 972 - 975 *

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JPWO2020116570A1 (ja) 2021-10-28
JP7309215B2 (ja) 2023-07-18

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