WO2013061588A1 - Préparation absorbée par voie transdermique - Google Patents

Préparation absorbée par voie transdermique Download PDF

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Publication number
WO2013061588A1
WO2013061588A1 PCT/JP2012/006829 JP2012006829W WO2013061588A1 WO 2013061588 A1 WO2013061588 A1 WO 2013061588A1 JP 2012006829 W JP2012006829 W JP 2012006829W WO 2013061588 A1 WO2013061588 A1 WO 2013061588A1
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WO
WIPO (PCT)
Prior art keywords
acid
adhesive layer
sensitive adhesive
imidafenacin
carbon atoms
Prior art date
Application number
PCT/JP2012/006829
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English (en)
Japanese (ja)
Inventor
勝幸 猪尾
大樹 高野
渡邉　正人
範洋 金山
Original Assignee
杏林製薬株式会社
帝國製薬株式会社
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Application filed by 杏林製薬株式会社, 帝國製薬株式会社 filed Critical 杏林製薬株式会社
Priority to JP2013540656A priority Critical patent/JP5995112B2/ja
Publication of WO2013061588A1 publication Critical patent/WO2013061588A1/fr

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    • 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
    • A61K9/7061—Polyacrylates
    • 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
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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 percutaneous absorption preparation containing 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyramide or a pharmaceutically acceptable salt thereof as an active ingredient.
  • imidafenacin is a compound with selective M1 / M3 muscarinic receptor antagonistic activity, for example, frequent urination and urine associated with overactive bladder Known as an incontinence drug.
  • transdermal preparations have been proposed (for example, Patent Documents 1 and 2).
  • imidafenacin can be easily administered even to elderly people.
  • a temporary increase in blood concentration which may occur in the case of oral administration, can be suppressed.
  • the absorbability of drugs by transdermal administration is lower than that of oral administration, etc. It is often difficult to ensure the necessary blood concentration. Therefore, the drugs that can be administered in the dosage form of the transdermal preparation are limited. Imidafenacin also has very low absorbability from the skin, and therefore, improvement in transdermal absorbability when administered as a transdermally absorbable preparation is required.
  • the present invention has been made based on such circumstances, and has excellent transdermal absorbability with respect to 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyramide or a pharmaceutically acceptable salt thereof. It aims at providing the percutaneous absorption type formulation which shows this.
  • transdermally absorbable preparation according to any one of 1) to 3), wherein the acrylic pressure-sensitive adhesive layer further contains an ester of a fatty acid having 6 to 20 carbon atoms.
  • another embodiment of the present invention provides 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyl containing an acrylic pressure-sensitive adhesive, oleic acid, and a carboxylic acid having 2 to 10 carbon atoms
  • the present invention relates to a composition that promotes transdermal absorption of an amide or a pharmaceutically acceptable salt thereof.
  • the said composition can be used as a composition which comprises the adhesive layer of a percutaneous absorption type formulation, for example.
  • a percutaneous absorption preparation having excellent percutaneous absorption for 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyramide or a pharmaceutically acceptable salt thereof. can do.
  • the percutaneous absorption type preparation of this embodiment has a support and an acrylic pressure-sensitive adhesive layer (hereinafter also simply referred to as a pressure-sensitive adhesive layer) containing an acrylic pressure-sensitive adhesive formed on the surface of the support.
  • the pressure-sensitive adhesive layer contains 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyramide or a pharmaceutically acceptable salt thereof as an active ingredient.
  • the transdermal preparation refers to a pharmaceutical dosage form that is affixed to the skin and absorbs the drug into the body through the skin. Drugs introduced into the body through the skin are absorbed, for example, into capillaries and delivered to the site of action according to blood flow.
  • blended with an acrylic adhesive layer other than the imidafenacin which is an active ingredient is generally called an additive.
  • Additives include oleic acid, carboxylic acids having 2 to 10 carbon atoms, and other ingredients (capric acid and crotamiton, esters of fatty acids having 6 to 20 carbon atoms, and / or as required) Or other ingredients).
  • the ratio of each component contained in the pressure-sensitive adhesive layer to the total components of the pressure-sensitive adhesive layer is based on the total mass of the pressure-sensitive adhesive layer composed of the acrylic pressure-sensitive adhesive, imidafenacin, and additives. It means that. However, the total mass of the reference pressure-sensitive adhesive layer does not include an organic solvent that may be used during production.
  • Acrylic adhesive which comprises an adhesive layer
  • Acrylic pressure-sensitive adhesives are, for example, acrylic ester homopolymers formed from one type of acrylic ester, copolymers formed from two or more types of acrylic ester, acrylic esters and other functional monomers. It can be formed from a copolymer with a monomer, or a mixture thereof.
  • Acrylic acid esters are, for example, (meth) acrylic acid methyl ester, (meth) acrylic acid ethyl ester, (meth) acrylic acid butyl ester, (meth) acrylic acid pentyl ester, (meth) acrylic acid hexyl ester, (meth) Acrylic heptyl ester, (meth) acrylic acid octyl ester, (meth) acrylic acid nonyl ester, (meth) acrylic acid decyl ester, or the like can be used.
  • Functional monomers capable of forming a copolymer with an acrylic ester include, for example, hydroxyl group-containing monomers such as (meth) acrylic acid hydroxyethyl ester, (meth) acrylic acid hydroxypropyl ester, (meth) Amide group-containing monomers such as acrylamide and dimethyl (meth) acrylamide, or carboxyl group-containing monomers such as (meth) acrylic acid, itaconic acid, and maleic acid can be used.
  • acrylic adhesive acrylic acid / octyl acrylate ester copolymer, 2-ethylhexyl acrylate / 2-ethylhexyl methacrylate / dodecyl methacrylate copolymer, or 2-ethylhexyl acrylate / vinyl pyrrolidone acrylate A copolymer or the like can be used.
  • the ratio of the acrylic pressure-sensitive adhesive with respect to all components blended in the pressure-sensitive adhesive layer is not particularly limited, but can be, for example, 50 to 90% by mass (preferably 50 to 80% by mass).
  • the pressure-sensitive adhesive layer contains imidafenacin as an active ingredient, specifically, 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyramide or a pharmaceutically acceptable salt thereof.
  • Imidafenacin may be blended either in a dissolved form or in a mixture of a dissolved form and a non-dissolved form.
  • the dissolved type means a state in which imidafenacin is completely dissolved in the pressure-sensitive adhesive layer, and specifically refers to a state in which imidafenacin crystals are not observed visually or with an optical microscope in the pressure-sensitive adhesive layer.
  • the non-dissolving type means that imidafenacin is present in the pressure-sensitive adhesive layer in a crystalline or non-crystalline state.
  • the dissolved form of imidafenacin is absorbed into the body through the skin.
  • Insoluble imidafenacin is not directly absorbed into the body, but changes into dissolved form as the dissolved imidafenacin decreases with percutaneous absorption. That is, undissolved imidafenacin acts as a source of dissolved imidafenacin.
  • imidafenacin contained in the pressure-sensitive adhesive layer is preferably a dissolution type from the viewpoint of quality stability such as rapid transdermal absorbability and skin adhesiveness.
  • Examples of pharmaceutically acceptable salts of 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyramide include inorganic acid salts such as hydrochloride, sulfate, or hydrobromide, Or organic acid salts such as maleate, fumarate, acetate, oxalate, tartrate, or benzenesulfonic acid.
  • the ratio of imidafenacin to the total components blended in the pressure-sensitive adhesive layer is not particularly limited, but can be, for example, 1 to 30% by mass (preferably 2 to 20% by mass).
  • the pressure-sensitive adhesive layer contains oleic acid and a carboxylic acid having 2 to 10 carbon atoms.
  • the transdermal absorbability of imidafenacin can be enhanced.
  • Oleic acid acts, for example, as a solubilizer that dissolves imidafenacin in an acrylic adhesive.
  • the carboxylic acid having 2 to 10 carbon atoms acts as a solubilizer, for example, like oleic acid.
  • Examples of the carboxylic acid having 2 to 10 carbon atoms include acetic acid, propionic acid, butyric acid, pentanoic acid, and heptanoic acid.
  • a hydroxy acid which is a carboxylic acid having an alcoholic or phenolic hydroxyl group can also be used.
  • the hydroxy acid include lactic acid, tartaric acid, and citric acid. In this embodiment, it is preferable to use a hydroxy acid, and it is more preferable to use lactic acid from the viewpoint of the solubility of imidafenacin.
  • the ratio of oleic acid and carboxylic acid having 2 to 10 carbon atoms to the total components blended in the adhesive layer is not particularly limited.
  • the proportion of oleic acid can be 2 to 20% by mass (preferably 5 to 15% by mass) with respect to the total components blended in the pressure-sensitive adhesive layer.
  • the proportion of the carboxylic acid having 2 to 10 carbon atoms can be 0.5 to 30% by mass (preferably 1 to 20% by mass) with respect to all the components blended in the pressure-sensitive adhesive layer.
  • the acrylic adhesive layer containing imidafenacin further contains capric acid and crotamiton in addition to oleic acid and carboxylic acid having 2 to 10 carbon atoms. It is preferable to do.
  • Capric acid acts as a solubilizer, for example, like oleic acid and carboxylic acids having 2 to 10 carbon atoms.
  • crotamiton acts as an absorption promoter for imidafenacin into the body, for example.
  • the transdermal absorbability of imidafenacin can be further enhanced by containing capric acid and crotamiton in the adhesive layer.
  • the pressure-sensitive adhesive layer of the transdermal preparation containing imidafenacin is described later in addition to carboxylic acid having 2 to 10 carbon atoms such as oleic acid and lactic acid, capric acid and crotamiton. It further contains an ester of a fatty acid having 6 to 20 carbon atoms, such as isopropyl myristate.
  • the ratio of capric acid and crotamiton to the total component blended in the pressure-sensitive adhesive layer is not particularly limited.
  • the ratio of capric acid is 0.1 to 20% by mass (preferably, the total component blended in the pressure-sensitive adhesive layer). 0.5 to 15% by mass).
  • the ratio of crotamiton can be 0.1 to 10% by mass (preferably 0.5 to 10% by mass) with respect to the total components blended in the pressure-sensitive adhesive layer.
  • an ester of a fatty acid having 6 to 20 carbon atoms contains imidafenacin.
  • the physical properties of the pressure-sensitive adhesive layer can be optimized, and the transdermal absorbability of imidafenacin can be further increased.
  • An ester of a fatty acid having 6 to 20 carbon atoms acts, for example, as a softening agent that increases the tackiness of an acrylic pressure-sensitive adhesive.
  • Examples of the fatty acid ester having 6 to 20 carbon atoms include isopropyl myristate, isopropyl palmitate, and oleyl oleate. In this embodiment, it is preferable to use isopropyl myristate.
  • the ratio of the fatty acid ester having 6 to 20 carbon atoms to the total components blended in the pressure-sensitive adhesive layer can be 2 to 50% by mass, preferably 5 to 40% by mass.
  • the pressure-sensitive adhesive layer may further contain other components as additives.
  • other components include one or more of other solubilizers, other softeners, other absorption enhancers, skin irritation mitigators, and antioxidants.
  • Soluble agents include higher fatty acid esters (such as isopropyl palmitate or oleyl oleate), higher alcohols (such as lauryl alcohol, isopropanol, isostearyl alcohol, octyldodecanol, or oleyl alcohol), fatty acids (isostearic acid, lauric acid, Adipic acid, sebacic acid, or myristic acid), dibasic acid diesters (diethyl sebacate, diisopropyl sebacate, diisopropyl adipate, etc.), triacetin, benzyl alcohol, cetyl lactate, octyldodecyl lactate, liquid paraffin, or these The mixture of 2 or more types of these can be mentioned.
  • higher fatty acid esters such as isopropyl palmitate or oleyl oleate
  • higher alcohols such as lauryl alcohol, isopropanol, isostearyl alcohol, oc
  • paraffin oil such as liquid paraffin
  • animal oil such as squalane and squalene
  • almond oil olive oil
  • camellia oil castor oil
  • tall oil peanut oil and other vegetable oils
  • silicone oil polybutene
  • medium chain fatty acid triglyceride Mention may be made of glyceryl monostearate, isopropyl myristate, diisopropyl adipate, dipropylene glycol or mixtures of two or more thereof.
  • Absorption accelerators include triacetin, fatty acids or fatty alcohols (lauric acid, myristic acid, oleyl alcohol, isopropanol, lauryl alcohol, dipropylene glycol, propylene glycol, etc.), fatty acid esters (glyceryl monolaurate, glyceryl monoole) Cetyl lactate, octyl dodecyl lactate, glycerol monolaurate, glycerol monooleate, propylene glycol monolaurate, propylene glycol monooleate, sorbitan monolaurate, or sorbitan monooleate), or a mixture of two or more of these Can be mentioned.
  • fatty acids or fatty alcohols lauric acid, myristic acid, oleyl alcohol, isopropanol, lauryl alcohol, dipropylene glycol, propylene glycol, etc.
  • fatty acid esters glyceryl monolaurate, glyce
  • Examples of the skin irritation mitigating agent include glycerin, allantoin, antihistamines (diphenhydramine, etc.), anti-inflammatory agents (glycyrrhetinic acid, etc.), steroids, or a mixture of two or more of these.
  • antioxidant examples include dibutylhydroxytoluene (BHT), DL- ⁇ -tocopherol, ascorbyl palmitate, or a mixture of two or more thereof.
  • BHT dibutylhydroxytoluene
  • DL- ⁇ -tocopherol DL- ⁇ -tocopherol
  • ascorbyl palmitate or a mixture of two or more thereof.
  • additives may also be included as additives.
  • petroleum resin Quinton or Alcon etc.
  • surfactant polyoxyethylene hydrogenated castor oil 20, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene sorbite fatty acid ester (polysorbate 20, polysorbate 60, Polysorbate 80 or polyoxyethylene sorbitan monolaurate), polyoxyethylene fatty acid ester (polyoxyl 40 stearate), sorbitan fatty acid ester (sorbitan monooleate, sorbitan trioleate, sorbitan monolaurate, or sorbitan sesquioleate) Etc.), self-emulsifying type glyceryl monostearate, glyceryl monostearate, sorbitan monostearate, sucrose fatty acid ester, macrogol 400, lauromacro Sodium phosphate, polyoxyethylene lauryl ether, polyoxyethylene oleyl ether, polyoxyethylene nonylphenyl ether, polyoxy
  • the transdermal preparation of this embodiment can be produced by forming an acrylic pressure-sensitive adhesive layer on a support.
  • the pressure-sensitive adhesive layer is preferably covered with a release liner for the purpose of protecting the pressure-sensitive adhesive layer until it is used.
  • the manufacturing method of the transdermally absorbable preparation of the present embodiment is not particularly limited, and can be appropriately selected by those skilled in the art.
  • the transdermally absorbable preparation of this embodiment can be produced by a method generally called a hot melt method or a method called a solvent method. When based on the hot melt method, for example, a mixture (base component) of imidafenacin, an additive, and an acrylic pressure-sensitive adhesive is melted by heat and applied to a release film or a support to form a pressure-sensitive adhesive layer.
  • a transdermal preparation is obtained by bonding the formed pressure-sensitive adhesive layer to a support or a release film.
  • a mixture of imidafenacin, an additive, and an acrylic pressure-sensitive adhesive is dissolved in an organic solvent such as methanol, ethanol, ethyl acetate, chloroform, or hexane, and a release film or a support is obtained. Extend and apply on the body. Next, the solvent is removed by drying to form an adhesive layer. Subsequently, a transdermal preparation is obtained by bonding the formed pressure-sensitive adhesive layer to a support or a release film.
  • size and thickness of an adhesive layer are not specifically limited, Those skilled in the art can set suitably.
  • the material for the support of the transdermal preparation of the present embodiment is not particularly limited, and can be appropriately set by those skilled in the art.
  • a stretchable or non-stretchable support can be used.
  • it can be selected from cloth, non-woven fabric, polyurethane, polyester, polyvinyl acetate, polyvinylidene chloride, polyethylene, polyethylene terephthalate (PET), aluminum sheet, or a composite material thereof.
  • the material of the release film is not particularly limited and can be appropriately selected by those skilled in the art.
  • Specific examples include a polyethylene film, a PET film, or a polypropylene film obtained by silicon coating.
  • the transdermally absorbable preparation of the present embodiment includes, for example, frequent urination / urinary incontinence associated with overactive bladder (OAB), asthma, chronic obstructive pulmonary disease (COPD), Alternatively, it is useful as a preventive and / or therapeutic agent for irritable bowel syndrome (IBS).
  • OAB overactive bladder
  • COPD chronic obstructive pulmonary disease
  • IBS irritable bowel syndrome
  • the affixing site is not particularly limited, and is, for example, the back of the ear, the abdomen such as the arm or lower abdomen, the chest, the back, the waist, the buttocks, the inner side of the thigh, or the legs such as the calf.
  • the amount of imidafenacin contained in the pressure-sensitive adhesive layer is not particularly limited, and the disease to be prevented or treated, the size of the pressure-sensitive adhesive layer, the administration time, or the target blood concentration of imidafenacin
  • about 0.1 mg to about 30 mg can be blended in the preparation or in a single dose.
  • the transdermal absorbability of imidafenacin can be improved by containing oleic acid and a carboxylic acid having 2 to 10 carbon atoms in addition to imidafenacin in the acrylic adhesive layer. it can. Moreover, the transdermal absorbability of imidafenacin can be further improved by containing capric acid and crotamiton in the adhesive layer. Furthermore, the transdermal absorption of imidafenacin can be further enhanced by containing an ester of a fatty acid having 6 to 20 carbon atoms in the adhesive layer.
  • the transdermal preparation of this embodiment for example, imidafenacin can be efficiently absorbed into the circulating blood through the skin. .
  • side effects that can occur with the rapid increase in blood concentration seen in oral administration can be avoided. Therefore, the transdermally absorbable preparation of this embodiment is very useful as a preventive and / or therapeutic drug for frequent urination / urinary incontinence associated with overactive bladder (OAB), asthma, COPD, IBS, and the like.
  • OAB overactive bladder
  • transdermally absorbable preparation of the present invention is not limited to the form described in the examples.
  • Example 1 9 g of 4- (2-methyl-1-imidazolyl) -2,2-diphenylbutyramide, 3 g of lactic acid, 7 g of oleic acid and 0.9 g of capric acid were dissolved in 100 g of methanol. To this solution, 17 g of isopropyl myristate and 2 g of crotamiton were added and mixed well to obtain a main agent solution. Thereafter, the main agent solution was added to 305.5 g of an acrylic acid / octyl acrylate copolymer / ethyl acetate solution having a solid concentration of 20% (61.1 g as the weight of the adhesive) and mixed well to prepare an adhesive solution.
  • Example 1 Apply the adhesive solution to a 75um PET film using a comma doctor so that the weight of the paste after drying is about 80g / m 2 and dry for 10 minutes at a temperature of about 80 ° C. A layer was formed. The formed pressure-sensitive adhesive layer and a support (15 ⁇ m thick PET film) were bonded together to obtain a transdermal absorption preparation of Example 1.
  • Example 2 to 4 and Comparative Examples 1 to 14 Transdermal absorption preparations of Examples 2 to 4 and Comparative Examples 1 to 14 were prepared in the same manner as in Example 1, except that the ratio of the components contained was changed. The amounts of components contained in the pressure-sensitive adhesive layer in Examples and Comparative Examples are shown in FIG.
  • [In vitro rat skin permeability test method] Franz-type cell in which the abdominal skin ( ⁇ 15mm) of HWY male hairless rats (10-11 weeks old) (weight 260-280g) was peeled off, and 37 ° C hot water was circulated around the outer periphery with the dermis side as the receptor layer side (Open area: 1.77 cm 2 ). Next, the percutaneous absorption preparations ( ⁇ 14 mm) of Examples and Comparative Examples were attached to the stratum corneum side of the skin. A PBS buffer solution (pH 7.4) was used as the receptor solution, and the receptor solution was sampled over time. The concentration of imidafenacin in the sampled receptor fluid was measured by the UPLC (Ultra Performance Liquid Chromatography) method under the following measurement conditions.
  • UPLC Ultra Performance Liquid Chromatography
  • the cumulative drug permeation amount per 1 cm 2 of the preparation at each sampling point was calculated ( ⁇ g / cm 2 ), and the relationship between time and cumulative drug permeation amount was graphed. Thereafter, a correlation line of the cumulative drug permeation amount was calculated from the graph, and the slope thereof was defined as a FLUX value that is a drug permeation rate.
  • FLUX Amount of transdermal drug absorbed per hour that is transdermally absorbed from an area of 1 cm 2 of the formulation after application
  • the obtained FLUX value is shown in FIG.
  • the percutaneous absorption preparations of Examples 1 to 4 all showed higher imidafenacin percutaneous absorption than the percutaneous absorption preparation of the comparative example.
  • the percutaneous absorption preparation of Example 1 containing capric acid and crotamiton was confirmed to have a higher percutaneous absorption than the other Examples.
  • the transdermally absorbable preparation of the present invention can prevent, for example, frequent urination / urinary incontinence associated with overactive bladder (OAB), asthma, chronic obstructive pulmonary disease (COPD), and irritable bowel syndrome (IBS). Useful for treatment.
  • OAB overactive bladder
  • COPD chronic obstructive pulmonary disease
  • IBS irritable bowel syndrome

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Abstract

L'invention a pour objet une préparation absorbée par voie transdermique ayant une excellente absorbabilité transdermique de 4-(2-méthyl-1-imidazolyl)-2,2-diphénylbutylamide ou d'un sel pharmaceutiquement acceptable contenu dans celle-ci. La préparation absorbée par voie transdermique selon l'invention comprend un support et une couche d'agent adhésif acrylique qui est formée sur la surface du support et contient du 4-(2-méthyl-1-imidazolyl)-2,2-diphénylbutylamide ou un sel pharmaceutiquement acceptable de celui-ci, la couche d'agent adhésif acrylique contenant de plus de l'acide oléique et un acide carboxylique ayant 2-10 atomes de carbone.
PCT/JP2012/006829 2011-10-26 2012-10-25 Préparation absorbée par voie transdermique WO2013061588A1 (fr)

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JP2013540656A JP5995112B2 (ja) 2011-10-26 2012-10-25 経皮吸収型製剤

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014214109A (ja) * 2013-04-24 2014-11-17 杏林製薬株式会社 貼付剤

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1652523A1 (fr) * 2003-08-04 2006-05-03 Kyorin Pharmaceutical Co., Ltd. Preparation pour absorption transdermique
EP1844773A1 (fr) * 2005-02-03 2007-10-17 Kyorin Pharmaceutical Co., Ltd. Preparation pour absorption percutanee
WO2012057212A1 (fr) * 2010-10-28 2012-05-03 久光製薬株式会社 Formule pour absorption percutanée

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1652523A1 (fr) * 2003-08-04 2006-05-03 Kyorin Pharmaceutical Co., Ltd. Preparation pour absorption transdermique
EP1844773A1 (fr) * 2005-02-03 2007-10-17 Kyorin Pharmaceutical Co., Ltd. Preparation pour absorption percutanee
WO2012057212A1 (fr) * 2010-10-28 2012-05-03 久光製薬株式会社 Formule pour absorption percutanée

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014214109A (ja) * 2013-04-24 2014-11-17 杏林製薬株式会社 貼付剤

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JPWO2013061588A1 (ja) 2015-04-02
TW201332592A (zh) 2013-08-16

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