[go: up one dir, main page]

WO2018190294A1 - Composition médicinale comprenant de l'escitalopram - Google Patents

Composition médicinale comprenant de l'escitalopram Download PDF

Info

Publication number
WO2018190294A1
WO2018190294A1 PCT/JP2018/014919 JP2018014919W WO2018190294A1 WO 2018190294 A1 WO2018190294 A1 WO 2018190294A1 JP 2018014919 W JP2018014919 W JP 2018014919W WO 2018190294 A1 WO2018190294 A1 WO 2018190294A1
Authority
WO
WIPO (PCT)
Prior art keywords
escitalopram
salt
pharmaceutical composition
mannitol
coating
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP2018/014919
Other languages
English (en)
Japanese (ja)
Inventor
時任正和
本庄達哉
中村達郎
高橋京介
奥田豊
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Towa Pharmaceutical Co Ltd
Original Assignee
Towa Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Towa Pharmaceutical Co Ltd filed Critical Towa Pharmaceutical Co Ltd
Priority to JP2018540506A priority Critical patent/JP6423133B1/ja
Publication of WO2018190294A1 publication Critical patent/WO2018190294A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans

Definitions

  • the present invention belongs to the technical field of pharmaceutical compositions.
  • the present invention relates to a pharmaceutical composition containing escitalopram or a salt thereof as an active ingredient, and relates to a pharmaceutical composition that ensures storage stability as a pharmaceutical product.
  • Escitalopram is the general name for the S form of citalopram, and the chemical name: (S) -1- [3- (dimethylamino) propyl] -1- (4-fluorophenyl) -1,3-dihydroisobenzofuran-5 -Carbonitrile).
  • This has a selective serotonin reuptake inhibitory action (SSRI), and its oxalate (see the structural formula below) is marketed as an antidepressant under a trade name such as Lexapro (registered trademark, Lexapro). .
  • Patent Document 1 As invention regarding the pharmaceutical composition of escitalopram, patent document 1 and 2 can be mentioned, for example.
  • Patent Document 1 an object is to develop a pharmaceutical dosage form for escitalopram oxalate having high bioavailability and minimizing impurities generated during production, and the problem is an average of less than 100 ⁇ m.
  • Patent Document 1 describes that it is preferable to use titanium oxide as a pigment (see paragraph [0037]), but other specific pigments including Examples are not specifically mentioned.
  • various film forming agents that can be usually used in the pharmaceutical field are exemplified, and cellulose derivatives are also exemplified. Such film forming agents are for coating uncoated tablets.
  • Patent Document 2 describes a large crystalline particle of escitalopram oxalate suitable for direct compression and a method for producing the same.
  • Such crystalline particles have an average particle size (D 50 ) and a particle size of at least 40 ⁇ m.
  • Patent Document 3 discloses an orally disintegrating tablet with reduced unpleasant taste such as bitter taste, comprising drug-containing granules formed by coating a drug mixed with an excipient with ethyl cellulose.
  • drug-containing granules formed by coating a drug mixed with an excipient with ethyl cellulose.
  • escitalopram there is no description regarding the pharmaceutical composition of escitalopram.
  • the main object of the present invention is to provide a novel pharmaceutical composition containing escitalopram or a salt thereof as an active ingredient and ensuring storage stability (light stability, heat stability) as a pharmaceutical product.
  • the present inventors have included iron oxide in the pharmaceutical composition of escitalopram, and the average particle size (D 50 ) of escitalopram is 40 ⁇ m or less, and a mixture containing the escitalopram particles and mannitol.
  • the present invention was completed by finding that the above-mentioned problems can be solved by granulating the powder. Furthermore, the inventors have found that the above problem can also be solved by coating the core particles containing escitalopram and an excipient with ethyl cellulose, thereby completing the present invention.
  • Examples of the present invention include the following.
  • a pharmaceutical composition comprising escitalopram or a salt thereof and iron oxide.
  • the escitalopram or a salt thereof has an average particle diameter D 50 of 40 ⁇ m or less and is contained in granules containing D-mannitol. Pharmaceutical composition as described in any one of these.
  • a method for producing a pharmaceutical composition comprising a step of granulating a mixture containing particles of escitalopram or a salt thereof having an average particle size D 50 of 40 ⁇ m or less and D-mannitol.
  • a granule having a coating layer containing ethyl cellulose on the outside of a core particle containing escitalopram or a salt thereof and an excipient [10] The granule according to [9] above, wherein the excipient is D-mannitol or crystalline cellulose.
  • a pharmaceutical composition containing escitalopram or a salt thereof as an active ingredient it is possible to ensure storage stability (light stability, thermal stability) as a pharmaceutical product.
  • the experimental result which shows the thermal stability of a tablet is represented.
  • the vertical axis represents the amount (%) of total related substances produced, and the horizontal axis represents the amount (%) of ethyl cellulose relative to the amount of core particles.
  • the black circle line shows the results of tablets obtained from the formulation (containing mannitol) in Table 9 described later, and the black triangle line shows the results of tablets obtained from the formulation in Table 11 (containing crystalline cellulose) described later.
  • Each line shows the results of tablets obtained from the formulation (containing lactose) in Table 13 described later.
  • composition of the present invention contains escitalopram or a salt thereof as an active ingredient.
  • the escitalopram or a salt thereof according to the present invention (hereinafter also referred to simply as “escitalopram”) is a known compound, and can be easily produced or obtained.
  • the escitalopram may be a particle or a crystalline polymorph.
  • the salt of escitalopram is not particularly limited as long as it is a pharmaceutically acceptable acid addition salt, and examples thereof include salts with organic acids and salts with inorganic acids.
  • examples of the salt with an organic acid include salts with oxalic acid, acetic acid, citric acid, tartaric acid, maleic acid, succinic acid, fumaric acid, p-toluenesulfonic acid, benzenesulfonic acid, and methanesulfonic acid.
  • Examples of the salt with an inorganic acid include salts with hydrochloric acid, hydrobromic acid, hydroiodic acid, nitric acid, sulfuric acid, and phosphoric acid. Of these, salts with oxalic acid are preferred. Such salts include hydrates and solvates.
  • the escitalopram according to the present invention preferably has an average particle size of 40 ⁇ m or less or within a range of 5 to 40 ⁇ m, and more preferably an average particle size within a range of 10 to 40 ⁇ m.
  • the “average particle diameter” is a volume average particle diameter, and means a particle diameter (D 50 , median diameter) at which the cumulative distribution from the smaller one becomes 50% when measured by a laser diffraction method.
  • the content of escitalopram per unit form (formulation) in the composition of the present invention varies depending on the dosage form and the like, but the amount of escitalopram is suitably within the range of 1 to 50 mg, and within the range of 5 to 20 mg. preferable.
  • the composition of the present invention preferably contains iron oxide.
  • Inclusion of iron oxide can improve the light stability.
  • the iron oxide is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include yellow iron sesquioxide, iron sesquioxide, brown iron oxide, and black iron oxide. Among these, yellow iron sesquioxide and iron sesquioxide are preferable.
  • the content of iron oxide in the composition of the present invention varies depending on the content of escitalopram, the type of iron oxide, the dosage form, etc., but is suitably in the range of 0.01 to 15% by mass, It is preferably in the range of 10% by mass, more preferably in the range of 0.1 to 5% by mass. If it is less than 0.01% by mass, sufficient storage stability may not be obtained. If it exceeds 15% by mass, the powder physical properties may be deteriorated and the color may be uneven.
  • Unit Form and Additives examples include tablets, capsules, granules, fine granules, and powders. Of these, tablets are preferred. Examples of such tablets include ordinary tablets, film-coated tablets, sugar-coated tablets, multilayer tablets, enteric tablets, matrix tablets, orally disintegrating tablets, sustained-release tablets, dispersible tablets, chewable tablets, tongues, and the like. Mention may be made of tablets, troches and chewable tablets.
  • the hardness of the tablet is not particularly limited, but is preferably 35 to 130 N, for example.
  • composition of the present invention contains pharmaceutically acceptable additives in addition to the above-described iron oxide, if necessary.
  • additives include, but are not limited to, excipients, disintegrants or disintegration promoters, binders, lubricants or fluidizing agents (anti-adhesion agents), coating agents, plasticizers, colorants, taste masking, and the like.
  • the composition of the present invention can have an appropriate amount of these according to the dosage form and the like.
  • additives include excipients such as D-mannitol, lactose, crystalline cellulose, corn starch, agar, gelatin, precipitated calcium carbonate, calcium hydrogen phosphate, sucrose; carboxymethyl cellulose, carboxymethyl cellulose calcium, low substitution Degrading agents or disintegration accelerators such as hydroxypropylcellulose, sodium croscarmellose, sodium carboxymethyl starch, calcium carbonate, sodium carbonate, corn starch, carmellose calcium, crospovidone; sodium carboxymethylcellulose, methylcellulose, hypromellose, gelatin, polyvinyl Binders such as pyrrolidone, polyvinyl alcohol, povidone; colloidal silica, talc, magnesium stearate, Lubricants or fluidizing agents such as calcium teaate, stearic acid, hydrous silicon dioxide, light anhydrous silicic acid, macrogol; methylcellulose, ethylcellulose, hypromellose, hydroxypropylcellulose, hydroxyethyl
  • composition of the present invention is a tablet
  • the total escitalopram-related substance after storage for 1 month under an open condition of 40 ° C. and a relative humidity of 75% is 0.2% by weight or less. What is 0.15 weight% or less is more preferable. What is 0.1 weight% or less is still more preferable.
  • composition of the present invention can be produced by a conventional method according to the dosage form employed.
  • tablets are made into a powder mixture by adding excipients, disintegrants, etc., and then added with a dispersion in which coloring agents are dispersed, and granulated (for example, wet granulation) to be granulated or slugged.
  • granulated for example, wet granulation
  • the granulation may be dry granulation.
  • the production method of the composition (tablet) of the present invention preferably includes a step of granulating a mixture containing escitalopram particles and mannitol having an average particle size of 40 ⁇ m or less or in the range of 5 to 40 ⁇ m.
  • the average particle size of escitalopram particles in such a production method is more preferably in the range of 10 to 40 ⁇ m.
  • the granulation may be either wet granulation or dry granulation, but wet granulation is preferred.
  • the composition of the present invention produced by the production method is particularly excellent in improving the light stability.
  • composition (tablet) of the present invention is preferably produced using granules having a coating layer containing ethylcellulose on the outside of the core particles containing escitalopram and an excipient.
  • excipient include those described above, but D-mannitol and crystalline cellulose are preferable.
  • the composition of the present invention produced by such a production method is particularly excellent in improving thermal stability.
  • the granule can be produced by a conventional method. Specifically, for example, each compounding component is mixed, granulated (for example, wet granulation), sized and dried to produce the core particles, and the core particles are usually coated with a coating agent containing ethyl cellulose. It can be manufactured by coating by the method. An intermediate coating layer may be provided between the core particle and the coating layer containing ethylcellulose.
  • the core particles can include iron oxide and the like. Moreover, talc, iron oxide, etc. can be included in the coating layer containing ethyl cellulose.
  • the above-mentioned granule having a coating layer containing the core particles and ethyl cellulose, an excipient, a lubricant and the like are added and mixed, and then compressed (compressed) by a conventional method to obtain the composition (tablet) of the present invention.
  • composition of the present invention can be film-coated with a coating on the surface of the tablet, if necessary, and can be sugar-coated with sugar.
  • coating agent that can be used in such film coating include hypromellose, hydroxypropyl cellulose, ethyl cellulose, polyacrylate, and polymethacrylate (Eudragid (registered trademark)).
  • composition of the present invention varies depending on the dosage form, the content of escitalopram, the patient's condition, body weight, age, etc., for example, once to several times a day or at an interval of one day to several days, It can be administered as a depressant.
  • ⁇ Stability test> (1) Light Stability Test The light stability test was performed using an ATLAS light stability tester (model number: SUNTEST XLS +) under irradiation conditions of a total illumination of 1,200,000 lx (lux) ⁇ hr.
  • Thermal stability test The thermal stability test was performed by storing for one month under an open condition of 40 ° C. and a relative humidity of 75% RH.
  • sample solution 20 mL of the following mobile phase A was added to tablets (1) or granules (1) and shaken and sonicated. The obtained liquid was filtered through a membrane filter having a pore size of 0.45 ⁇ m or less, 5 mL of the first filtrate was removed, and 10 mL of the next filtrate was used as a sample solution.
  • Detector UV absorptiometer (measurement wavelength: 237 nm)
  • Column A stainless tube having an inner diameter of 4.6 mm and a length of 25 cm packed with 5 ⁇ m of octadecyl silica gel for liquid chromatography.
  • Column temperature constant temperature around 45 ° C.
  • Mobile phase A pH 3.0 phosphate buffer / acetonitrile mixture (17: 3)
  • Mobile phase B Acetonitrile / pH 3.0 phosphate buffer (4: 1)
  • Mobile phase liquid feed The mixing ratio of mobile phase A and mobile phase is adjusted as appropriate to control the concentration gradient. Flow rate: 1.0 mL per minute
  • the core particles were put into a fluidized bed granulator, and the coating liquid was sprayed onto the particles, dried, and sized to prepare a sized powder (coating particles).
  • the coated particles, D-mannitol, crystalline cellulose, light anhydrous silicic acid, croscarmellose sodium, talc, and magnesium stearate were mixed and tableted to obtain an uncoated tablet for testing. And the light stability test was done about each uncoated tablet for a test. The test results are shown in the subsequent stages of Tables 7 and 8.
  • talc was dispersed in a solution obtained by dissolving a coating agent (ethyl cellulose, hypromellose, or aminoalkyl methacrylate copolymer E) in a mixed solution of purified water and absolute ethanol to prepare a coating solution.
  • a coating agent ethyl cellulose, hypromellose, or aminoalkyl methacrylate copolymer E
  • Example 57 the above core particles were put into a fluidized bed granulator, and the above coating solution was sprayed thereon, dried and sized to prepare a sized powder (coating particles).
  • a sized powder coating particles
  • D-mannitol crystalline cellulose
  • croscarmellose sodium croscarmellose sodium
  • talc croscarmellose sodium
  • magnesium stearate magnesium stearate
  • tablets obtained from coated particles in which core particles are coated with ethyl cellulose are tablets obtained from coated particles in which core particles are coated with another coating agent or particles not coated with a coating agent.
  • the heat stability was better than that.
  • Example 66 Except for Example 66, the above core particles were put into a fluidized bed granulator, and the above coating solution was sprayed thereon, dried and sized to prepare a sized powder (coating particles).
  • This coated granule or uncoated granule (core particle), D-mannitol, crystalline cellulose, light anhydrous silicic acid, croscarmellose sodium, talc, magnesium stearate are mixed and tableted to obtain an uncoated tablet for testing. It was. And the thermal stability test was done about each uncoated tablet for a test. The test results are shown in Table 12.
  • Example 73 Except for Example 73, the above core particles were put into a fluidized bed granulator, and the above coating solution was sprayed, dried and sized to prepare a sized powder (coating granule).
  • This coated granule or uncoated granule (core particle), D-mannitol, crystalline cellulose, light anhydrous silicic acid, croscarmellose sodium, talc, magnesium stearate are mixed and tableted to obtain an uncoated tablet for testing. It was. And the thermal stability test was done about each uncoated tablet for a test. The test results are shown in Table 14.
  • tablets obtained from those containing mannitol or crystalline cellulose as the core particle excipient are more than tablets obtained from those containing lactose as the core particle excipient. Excellent thermal stability.
  • Example 74 According to the formulation shown in Table 15, escitalopram oxalate having an average particle diameter D 50 of 15 ⁇ m, D-mannitol, croscarmellose sodium, and hydroxypropylcellulose were mixed, and a colorant (yellow ferric oxide) was mixed with water. The dispersion liquid dispersed in was added, granulated, dried, and sized to prepare core particles. Separately, talc was dispersed in a solution obtained by dissolving hypromellose in purified water to prepare an intermediate layer coating solution.
  • a colorant yellow ferric oxide
  • the core particles were put in a fluidized bed granulator, and the intermediate layer coating solution was sprayed onto the core particles, dried and sized to prepare a sized powder (intermediate layer particles).
  • talc was dispersed in a solution obtained by dissolving a coating agent (ethylcellulose) in a mixed solution of purified water and absolute ethanol to prepare an ethylcellulose coating solution.
  • the sized powder (intermediate layer particles) was put in a fluidized bed granulator, and the ethyl cellulose coating solution was sprayed onto the dried powder, dried and sized to prepare sized powder (coating particles).
  • Example 75 According to the formulation shown in Table 16, talc and yellow ferric oxide were dispersed in a solution obtained by dissolving escitalopram oxalate and hydroxypropyl cellulose having an average particle size D 50 of 15 ⁇ m in a mixture of purified water and absolute ethanol. The coating solution was adjusted. D-mannitol spherical granules were put into a fluidized bed granulator, and the above coating solution was sprayed onto the granules, dried and sized to prepare sized powder (core particles).
  • talc was dispersed in a solution obtained by dissolving a coating agent (ethylcellulose) in a mixed solution of purified water and absolute ethanol to prepare an ethylcellulose coating solution.
  • a coating agent ethylcellulose
  • the above sized powder (core particles) was put into a fluidized bed granulator, and the ethyl cellulose coating solution was sprayed on this, dried and sized to prepare a sized powder (coating particles).
  • composition of the present invention is useful as a pharmaceutical because its storage stability is ensured.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention aborde principalement le problème de la fourniture d'une nouvelle composition médicinale qui comprend de l'escitalopram en tant que principe actif et a une stabilité sécurisée (stabilité à la lumière et stabilité thermique) en tant que médicament. La présente invention comprend, par exemple : une composition médicinale caractérisée en ce qu'elle comprend de l'escitalopram ou un sel de celui-ci et de l'oxyde de fer; un procédé de fabrication d'une composition médicinale, ledit procédé étant caractérisé en ce qu'il comprend une étape de granulation d'un mélange qui contient des particules d'escitalopram ou un sel de celui-ci ayant un diamètre moyen de particule D50 de 40 µm ou moins et du mannitol; et des granulés caractérisés en ce qu'ils comprennent une particule de noyau contenant de l'escitalopram ou un sel de celui-ci et un excipient et une couche de revêtement contenant de l'éthylcellulose.
PCT/JP2018/014919 2017-04-10 2018-04-09 Composition médicinale comprenant de l'escitalopram Ceased WO2018190294A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2018540506A JP6423133B1 (ja) 2017-04-10 2018-04-09 エスシタロプラム医薬組成物

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2017077345 2017-04-10
JP2017-077345 2017-04-10

Publications (1)

Publication Number Publication Date
WO2018190294A1 true WO2018190294A1 (fr) 2018-10-18

Family

ID=63792966

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2018/014919 Ceased WO2018190294A1 (fr) 2017-04-10 2018-04-09 Composition médicinale comprenant de l'escitalopram

Country Status (2)

Country Link
JP (3) JP6423133B1 (fr)
WO (1) WO2018190294A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022001562A (ja) * 2020-06-22 2022-01-06 東和薬品株式会社 エスシタロプラム錠剤
JP2023018887A (ja) * 2021-07-28 2023-02-09 共和薬品工業株式会社 エスシタロプラムシュウ酸塩含有錠剤
JP2023529499A (ja) * 2020-06-15 2023-07-10 ホワン イン ファーマシューティカル カンパニー リミテッド 医薬組成物
WO2024165628A1 (fr) 2023-02-07 2024-08-15 Kinast Lasse Forme pharmaceutique orale à libération immédiate d'escitalopram ou de racémate de celui-ci avec une teneur accrue en api

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018190294A1 (fr) * 2017-04-10 2018-10-18 東和薬品株式会社 Composition médicinale comprenant de l'escitalopram
JP7253776B2 (ja) * 2019-01-18 2023-04-07 株式会社大一商会 遊技機
JP7253774B2 (ja) * 2019-01-18 2023-04-07 株式会社大一商会 遊技機
JP7253772B2 (ja) * 2019-01-18 2023-04-07 株式会社大一商会 遊技機
JP7253775B2 (ja) * 2019-01-18 2023-04-07 株式会社大一商会 遊技機
JP7391521B2 (ja) * 2019-03-12 2023-12-05 東和薬品株式会社 勃起不全治療用医薬組成物

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005525993A (ja) * 2001-07-31 2005-09-02 ハー・ルンドベック・アクチエゼルスカベット エスシタロプラムを含む結晶性組成物
JP2009519969A (ja) * 2005-12-14 2009-05-21 ハー・ルンドベック・アクチエゼルスカベット エスシタロプラムの放出調節製剤およびパルス型放出製剤
JP2011126906A (ja) * 2004-02-20 2011-06-30 Eisai R & D Management Co Ltd ワルファリンカリウム含有医薬組成物とその製造方法
JP2011520798A (ja) * 2008-05-07 2011-07-21 へクサル アーゲー シュウ酸エスシタロプラムを含む粒状物
JP2015147821A (ja) * 2015-05-29 2015-08-20 大日本住友製薬株式会社 光安定性の向上した組成物
JP2015178482A (ja) * 2014-03-20 2015-10-08 日医工株式会社 ロスバスタチン含有医薬製剤
US20160008375A1 (en) * 2013-03-01 2016-01-14 Sanovel Ilac Sanayi Ve Ticaret A.S. Pharmaceutical formulations comprising quetiapine and escitalopram
CN106176691A (zh) * 2016-08-31 2016-12-07 齐鲁制药有限公司 一种草酸艾司西酞普兰口溶膜剂及其制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006123243A2 (fr) * 2005-05-20 2006-11-23 Aurobindo Pharma Limited Formes galeniques pharmaceutiques d'un antidepresseur
TWI347942B (en) 2005-06-22 2011-09-01 Lundbeck & Co As H Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base
US7834201B2 (en) 2005-06-22 2010-11-16 H. Lundbeck A/S Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base
EP2134325A2 (fr) * 2007-03-01 2009-12-23 Aurobindo Pharma Limited Formes posologiques solides stables d'un antidépresseur
US20090048336A1 (en) 2007-08-17 2009-02-19 Naveen Kumar Kolla Escitalopram oxalate powders
WO2009135646A2 (fr) * 2008-05-05 2009-11-12 Farmaprojects, Sa Compositions pharmaceutiques stables et procédés de préparation desdites compositions adaptés à l’échelle industrielle
GR20080100696A (el) 2008-10-23 2010-05-13 Genepharm �.�. Φαρμακοτεχνικη μορφη με βελτιωμενη γευση του φαρμακευτικα αποδεκτου αλατος εσιταλοπραμης
WO2018190294A1 (fr) 2017-04-10 2018-10-18 東和薬品株式会社 Composition médicinale comprenant de l'escitalopram

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005525993A (ja) * 2001-07-31 2005-09-02 ハー・ルンドベック・アクチエゼルスカベット エスシタロプラムを含む結晶性組成物
JP2011126906A (ja) * 2004-02-20 2011-06-30 Eisai R & D Management Co Ltd ワルファリンカリウム含有医薬組成物とその製造方法
JP2009519969A (ja) * 2005-12-14 2009-05-21 ハー・ルンドベック・アクチエゼルスカベット エスシタロプラムの放出調節製剤およびパルス型放出製剤
JP2011520798A (ja) * 2008-05-07 2011-07-21 へクサル アーゲー シュウ酸エスシタロプラムを含む粒状物
US20160008375A1 (en) * 2013-03-01 2016-01-14 Sanovel Ilac Sanayi Ve Ticaret A.S. Pharmaceutical formulations comprising quetiapine and escitalopram
JP2015178482A (ja) * 2014-03-20 2015-10-08 日医工株式会社 ロスバスタチン含有医薬製剤
JP2015147821A (ja) * 2015-05-29 2015-08-20 大日本住友製薬株式会社 光安定性の向上した組成物
CN106176691A (zh) * 2016-08-31 2016-12-07 齐鲁制药有限公司 一种草酸艾司西酞普兰口溶膜剂及其制备方法

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023529499A (ja) * 2020-06-15 2023-07-10 ホワン イン ファーマシューティカル カンパニー リミテッド 医薬組成物
JP2022001562A (ja) * 2020-06-22 2022-01-06 東和薬品株式会社 エスシタロプラム錠剤
JP7453859B2 (ja) 2020-06-22 2024-03-21 東和薬品株式会社 エスシタロプラム錠剤
JP2023018887A (ja) * 2021-07-28 2023-02-09 共和薬品工業株式会社 エスシタロプラムシュウ酸塩含有錠剤
WO2024165628A1 (fr) 2023-02-07 2024-08-15 Kinast Lasse Forme pharmaceutique orale à libération immédiate d'escitalopram ou de racémate de celui-ci avec une teneur accrue en api

Also Published As

Publication number Publication date
JPWO2018190294A1 (ja) 2019-04-25
JP2019006829A (ja) 2019-01-17
JP6487599B2 (ja) 2019-03-20
JP2018177815A (ja) 2018-11-15
JP6423133B1 (ja) 2018-11-14
JP7051638B2 (ja) 2022-04-11

Similar Documents

Publication Publication Date Title
JP6487599B2 (ja) エスシタロプラム医薬組成物
KR102006000B1 (ko) 몬테루카스트 또는 이의 약학적으로 허용가능한 염 및 레보세티리진 또는 이의 약학적으로 허용가능한 염을 함유하는 캡슐 제제
JP6588915B2 (ja) Ａｚｄ９２９１を含む医薬組成物
US20160271124A1 (en) Formulations containing nalbuphine and uses thereof
EP2800558B1 (fr) Formulation pharmaceutique stable destinée à une administration par voie orale comprenant de la lévocétirizine ou un sel pharmaceutiquement acceptable de celle-ci, et du montélukast ou un sel pharmaceutiquement acceptable de celui-ci
CN107613978B (zh) Mek抑制剂的药物组合物及其制备方法
ES2616115T3 (es) Forma farmacéutica oral de liberación controlada que comprende oxicodona
US9555005B2 (en) Extended-release topiramate capsules
JP2011020960A (ja) オロパタジン固形製剤、およびオロパタジン錠剤の製造方法
CN102026626B (zh) 包含草酸艾司西酞普兰的颗粒
IL293096A (en) Oral pharmaceutical composition comprising carbamate compound and preparation method therefor
ES2533956T3 (es) Desfesoterodina en forma de una sal de ácido tartárico
CN114096530B (zh) 一种复合物的药物组合物及其制备方法
WO2013172297A1 (fr) Préparation contenant un dérivé de 7-carbamoylmorphinane 6,7-insaturé
JP5611502B2 (ja) ジベンゾ［ｂ，ｅ］オキセピン誘導体を含有する固形製剤
WO2020111089A1 (fr) Composition pharmaceutique
KR102481517B1 (ko) 약제학적 제제
JP2020147529A (ja) ダビガトランエテキシラートを含む製剤および安定化方法
WO2015069203A1 (fr) Capsule comprenant du fumarate de rupatadine et du montélukast sodique
JP5563371B2 (ja) クエチアピンフマル酸塩含有経口用錠剤
JP2020189815A (ja) デュロキセチン製剤およびその安定化方法
JP2023152768A (ja) 固形製剤、固形製剤の製造方法、および固形製剤の安定化方法
JP2024088413A (ja) 錠剤、錠剤の製造方法、および錠剤の安定化方法
WO2024251197A1 (fr) Dispersion solide d'inhibiteur d'eed, formulation orale la comprenant, et son procédé de préparation
JP2025165551A (ja) 錠剤、錠剤の製造方法、およびパルボシクリブまたはその薬学的に許容される塩の類縁物質の生成を抑制する方法

Legal Events

Date Code Title Description
ENP Entry into the national phase

Ref document number: 2018540506

Country of ref document: JP

Kind code of ref document: A

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 18784529

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 18784529

Country of ref document: EP

Kind code of ref document: A1