WO2021060304A1 - 不快な味がマスクされた顆粒剤及びその製造方法 - Google Patents

不快な味がマスクされた顆粒剤及びその製造方法 Download PDF

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Publication number
WO2021060304A1
WO2021060304A1 PCT/JP2020/035883 JP2020035883W WO2021060304A1 WO 2021060304 A1 WO2021060304 A1 WO 2021060304A1 JP 2020035883 W JP2020035883 W JP 2020035883W WO 2021060304 A1 WO2021060304 A1 WO 2021060304A1
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WIPO (PCT)
Prior art keywords
active ingredient
particles
unpleasant taste
core particles
ethyl cellulose
Prior art date
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Ceased
Application number
PCT/JP2020/035883
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English (en)
French (fr)
Japanese (ja)
Inventor
野村　達雄
亨 安澤
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.)
Nobelpharma Co Ltd
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Nobelpharma 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 Nobelpharma Co Ltd filed Critical Nobelpharma Co Ltd
Priority to CN202080059661.5A priority Critical patent/CN114340601A/zh
Priority to CA3153004A priority patent/CA3153004A1/en
Priority to JP2021503619A priority patent/JP6905781B1/ja
Priority to EP20867214.7A priority patent/EP4035733A4/en
Priority to US17/642,107 priority patent/US20230016901A1/en
Priority to AU2020352037A priority patent/AU2020352037A1/en
Publication of WO2021060304A1 publication Critical patent/WO2021060304A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/30—Zinc; Compounds 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5089—Processes

Definitions

  • the present invention relates to a granule in which the unpleasant taste of the active ingredient is masked and the quick-release property of the active ingredient is maintained, and a method for producing the same.
  • the present invention relates to granules containing zinc acetate as an active ingredient having an unpleasant taste and a method for producing the same.
  • the therapeutic agents containing zinc acetate that have been used so far are capsules and film-coated tablets, the problem of the unpleasant taste of the active ingredient when taken has not become apparent.
  • zinc acetate preparations are used for patients of a wide range of ages from children to the elderly, granule-form preparations that are easier to take and whose dose can be easily adjusted are desired.
  • Patent Document 1 in the production of a quick-release granular preparation masking an unpleasant taste, ethyl cellulose and hydroxypropyl cellulose are dissolved in hydrous ethanol for a nucleus containing a pharmacologically active substance, and this is dissolved for elementary granules.
  • a method of coating 60 to 100% is disclosed.
  • Patent Document 2 discloses a method using an aqueous ethyl cellulose suspension as a coating method that does not use an organic solvent.
  • Patent Document 2 discloses a method in which a nucleus containing a pharmacologically active substance is coated with an aqueous suspension of ethyl cellulose and then heat-treated under a constant humidity.
  • Patent Document 3 as a technique for masking an unpleasant taste and for rapid release, a core containing a pharmacologically active substance is first coated with a water-soluble polymer as an intermediate layer, and then a certain amount is provided.
  • a method of coating a 20-40% aqueous suspension of ethyl cellulose containing a plasticizer of the above is disclosed.
  • the present invention has been made in view of the above circumstances, and an object of the present invention is to provide a granule in which the unpleasant taste of the active ingredient is masked and the quick-release property of the active ingredient is maintained, and a method for producing the same.
  • the present inventors have diligently studied the heat treatment in the coating process with a conventional release system, and surprisingly, this heating process is put into a sealed state contrary to the common general technical knowledge. By doing so, the problem was solved and the present invention was reached. That is, by heat-treating the core particles sprayed with the water-dispersed ethyl cellulose suspension in a closed state, the active ingredient having an unpleasant taste is not released in the mouth after taking the drug, but the active ingredient in the stomach after swallowing. Succeeded in obtaining a granule having a coating having an amount or thickness capable of immediately releasing the substance, and reached the present invention.
  • the term core particle is used to mean the particle which becomes the center of each particle which constitutes a granule.
  • immediate release is used to mean that the active ingredient is released early in the stomach after swallowing.
  • the present invention comprises (1) a step of obtaining core particles containing an active ingredient having an unpleasant taste, (2) a step of coating the surface of the core particles obtained in step (1) with ethyl cellulose, and (3).
  • a method for producing granules which comprises a step of heat-treating the particles obtained in the step (2) in a sealed state, in which the unpleasant taste of the active ingredient is masked and the quick-release property of the active ingredient is maintained. ..
  • the present invention is a granule obtained by the production method described in the present specification, in which the unpleasant taste of the active ingredient is masked and the quick-release property of the active ingredient is maintained.
  • the present invention is effective in masking the unpleasant taste of the active ingredient by coating the core particles containing the active ingredient having an unpleasant taste with a film containing 2 to 12% by weight of ethyl cellulose with respect to the core particles. It is a granule in which the quick-release property of the ingredient is maintained.
  • core particles containing an active ingredient having an unpleasant taste are coated with a film containing 2 to 12% by weight of ethyl cellulose with respect to the core particles, and the second method of dissolution test (paddle) of the Japanese Pharmacopoeia. It is a granule having an elution 5-minute value of 80% or less and an elution 15-minute value of 85% or more according to the method, test solution: water, test solution amount: 900 mL, 50 rpm).
  • Examples of the active ingredient having an unpleasant taste that can be used in the present invention include various substances having an unpleasant flavor such as bitterness and astringency, but it is difficult to maintain immediate release while masking the conventional taste. It is particularly effective to use it for a highly water-soluble substance, for example, zinc acetate.
  • Zinc acetate may be anhydrous or hydrated, more preferably dihydrate.
  • the step (1) can be a step of spraying a solution or suspension of the active ingredient onto the core particles of the core particles to coat the particles with the active ingredient.
  • the core particle of the core particle is not particularly limited as long as it is a particle whose main component is a substance having disintegration in the body, such as saccharide and / or crystalline cellulose.
  • particles containing sucrose and corn starch as main constituents, particles composed of lactose and crystalline cellulose, spherical particles composed of D-mannitol, granulated sugar and the like can be used.
  • the shape of the core particles of the core particles is not particularly limited, but preferably substantially spherical particles can be used. The closer the particle shape is to a sphere, the more uniform the coating of the active ingredient and the like, and the more stable the quality.
  • step (1) can be a step of coating a binder in addition to the active ingredient.
  • the binder may be contained in a solution or suspension of the active ingredient and sprayed together with the active ingredient, prepared as a solution separate from the solution or suspension of the active ingredient, and sprayed simultaneously with or individually of the active ingredient. You may. By coating the binder together with the active ingredient, the bond between the active ingredient and the core particles can be strengthened.
  • the binder may be any one generally used in the pharmaceutical field, and examples thereof include hydroxypropyl cellulose, polyvinyl alcohol, hydroxypropyl methyl cellulose, methyl cellulose, gum arabic, gelatin, starch and the like, and hydroxypropyl cellulose is preferable.
  • the blending amount of the binder may be appropriately set as long as the amount of the core particles and the active ingredient can be sufficiently bonded.
  • step (1) can be a step of coating a disintegrant in addition to the active ingredient.
  • the disintegrant may be contained in a solution or suspension of the active ingredient and sprayed together with the active ingredient, prepared as a solution separate from the solution or suspension of the active ingredient, and sprayed simultaneously with or individually of the active ingredient. You may.
  • the disintegrant may be any one generally used in the pharmaceutical field, and examples thereof include partially pregelatinized starch, carboxymethyl cellulose, croscarmellose sodium, crospovidone and the like, and partially pregelatinized starch is preferable.
  • the amount of disintegrant can be appropriately adjusted so as to achieve the desired dissolution rate.
  • either one of the binder and the disintegrant may be coated on the particles together with the active ingredient, or these may be simultaneously coated on the particles together with the active ingredient.
  • the binder and the disintegrant may be mixed with the solution or suspension of the active ingredient and sprayed together with the active ingredient, and the binder and the disintegrant may be bonded separately from the solution or suspension of the active ingredient. Solutions of agents and disintegrants may be prepared and sprayed simultaneously with or individually of the active ingredient.
  • an active ingredient having an unpleasant taste is granulated together with a formulation aid such as an excipient, pulverized, and sieved so as to have a constant particle size. It can be a process.
  • excipients examples include sugars such as lactose, sucrose and mannitol, starches such as corn starch and potato starch, and binders such as hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, polyvinyl alcohol and polyvinyl alcohol.
  • sugars such as lactose, sucrose and mannitol
  • starches such as corn starch and potato starch
  • binders such as hydroxypropyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, polyvinyl alcohol and polyvinyl alcohol.
  • step (2) can be a step of spray-coating the aqueous dispersion ethyl cellulose suspension.
  • the coating amount of ethyl cellulose is 2 to 12% by weight, preferably 5 to 9% by weight, and more preferably 5 to 7% by weight with respect to the core particles.
  • step (2) can be a step of coating a plasticizer together with ethyl cellulose.
  • a plasticizer By coating ethyl cellulose with a plasticizer, particles can be formed more completely.
  • the plasticizer may be any one generally used in the pharmaceutical field, and examples thereof include triethyl citrate, polyethylene glycol, propylene glycol, and triacetin.
  • the amount of plasticizer can be appropriately selected and used. For example, when coating a granule having a particle size of 200 to 1000 ⁇ m, an amount of about 5 to 20% by weight may be used with respect to ethyl cellulose.
  • the heat treatment in the step (3) heats the particles in a sealed state so as to prevent the moisture contained in the particles from being released to the outside of the system due to overheating to some extent.
  • Heating the particles in a closed state means heating the particles under closed conditions, even if the water contained in the particles can be prevented from being released to the outside of the system to some extent. Just do it.
  • it means putting the particles obtained in the step (2) into a closed container and heating them.
  • the heating in the step (3) is preferably performed under a so-called airtight condition in which liquid does not enter and exit, and more preferably performed in a so-called closed state under a condition in which water vapor, air and other gases do not enter and exit. ..
  • the heating may be performed under conditions sufficient for forming a film with ethyl cellulose coated on the particle surface, for example, the temperature may be 70 to 100 ° C., and the treatment time may be 15 to 180 minutes.
  • a fluidizing agent in the heating step in the step (3), can be added to the particles obtained in the step 2 in advance. By adding the fluidizing agent, it is possible to prevent the particles from adhering to each other and agglomerating in the heating step.
  • the fluidizing agent may be any one generally used in the pharmaceutical field, and examples thereof include light anhydrous silicic acid.
  • the amount of the fluidizing agent added may be an amount sufficient to disperse the particles, and specifically, it may be used in an amount of about 0.5 to 1% by weight based on the particles.
  • the term "the unpleasant taste of the active ingredient was masked and the rapid release of the active ingredient was maintained" is used in the initial stage of administration of the granule (the time during which the granule is present in the mouth). It means that the active ingredient does not elute, and that a sufficient amount of the active ingredient elutes after a certain period of time (early time point after swallowing). For example, when the test was carried out by the second dissolution test method (paddle method, test solution: water, test solution volume: 900 mL, 50 rpm) of the Japanese Pharmacy, the dissolution 5-minute value of the active ingredient was 80% or less, and dissolution.
  • the production method according to the present invention comprises step (1): spraying a solution or suspension containing an active ingredient and a binder onto substantially spherical particles containing saccharides and / or crystalline cellulose as a main component. Then, a step of spraying a solution or suspension of a disintegrant, step (2): a step of spraying an aqueous dispersion ethyl cellulose suspension containing a plasticizer, a step (3): adding a fluidizing agent and sealing.
  • the step of heating in a state of 70 to 100 ° C. for 15 to 180 minutes can be carried out in sequence.
  • One aspect of the granules of the present invention is a granule obtained by a method including the above-mentioned steps (1), (2), and (3).
  • one aspect of the granule of the present invention is that the core particles containing the active ingredient having an unpleasant taste are coated with a film containing 2 to 12% by weight of ethyl cellulose with respect to the core particles, which is unpleasant for the active ingredient. It is a granule in which the taste is masked and the quick-release of the active ingredient is maintained.
  • Such granules can be produced, for example, by the method described above.
  • One aspect of the granules of the present invention is to coat core particles containing an active ingredient having an unpleasant taste with a film containing 2 to 12% by weight of ethyl cellulose with respect to the core particles, and elute from the Japanese Pharmacopoeia.
  • Granules having an elution 5-minute value of 80% or less and an elution 15-minute value of 85% or more according to the second test method (paddle method, test solution: water, test solution amount: 900 mL, 50 rpm).
  • Such granules can be produced, for example, by the method described above.
  • Examples of the active ingredient having an unpleasant taste that can be used in the granules of the present invention include the above-mentioned active ingredients, for example, zinc acetate.
  • Zinc acetate may be anhydrous or hydrated, more preferably dihydrate.
  • the particle size of the granules of the present invention can be appropriately selected and is not particularly limited, but can be, for example, about 200 to 700 ⁇ m. By using a particle size of this degree, it is possible to obtain a preparation that is easy to take even for children and the elderly.
  • Example 1 450 g of a 20% ethyl cellulose suspension containing about 2% triethyl citrate was sprayed onto 1500 g of the obtained API particles, and sieved using an 18-mesh sieve to obtain ethyl cellulose-coated particles. To the obtained ethyl cellulose-coated particles, 0.7% of light anhydrous silicic acid was added, mixed, placed in a closed container, and heated at 80 ° C. for 2 hours (hereinafter, referred to as “sealed condition heated granules”). ..
  • the elution 15-minute value was almost 100% for both the closed-condition heated granules and the release-condition heated granules, and no difference was observed between the two. From this result, it was confirmed that both the sealed condition heated granules and the release condition heated granules had sufficient quick-release properties of the active ingredient.
  • the elution of the sealed condition heated granules was significantly suppressed as compared with the release condition heated granules. This result indicates that the elution of the active ingredient in the early stage after administration is significantly suppressed and the unpleasant taste is effectively masked by performing the heat treatment under the closed condition.
  • the production method of the present invention that is, a production method including performing the heat treatment in the coating step under closed conditions, the unpleasant taste of the active ingredient is masked and the quick release of the active ingredient can be achieved. It was confirmed that the maintained granules could be produced.
  • Example 2 Coating amount of ethyl cellulose
  • the amount of the 20% ethyl cellulose suspension containing about 2% of triethyl citrate sprayed on the drug substance-coated elementary particles is adjusted so that the coating amount (the amount of ethyl cellulose coated on the drug substance-coated elementary particles) is 5, 6 and 7% by weight. Except for the adjustment, the same operation as in Example 1 was carried out to prepare sealed condition heated granules, and the elution amount of the active ingredient was confirmed by the same test method as in Example 1. The results are shown in FIG. 2 (relationship between the amount of ethyl cellulose coated and the elution rate of the active ingredient).
  • the elution 15-minute value showed a value of 85% or more for all coating amounts of granules. From this result, it was confirmed that the quick-release property of the active ingredient was maintained in all the granules. In addition, the 5-minute elution value was less than 70% for all the coating amounts of the granules, which was a good value. From this result, it was confirmed that the unpleasant taste was masked in all the granules.
  • Example 2 The same operation as in Example 1 was carried out except that the amount of the plasticizer to be blended in the ethyl cellulose suspension was adjusted to be 7, 9 and 11% by weight based on ethyl cellulose, and the sealed condition heated granules were prepared. The preparation was carried out, and the elution amount of the active ingredient was confirmed by the same test method as in Example 1. The results are shown in FIG. 3 (relationship between the amount of plasticizer added and the elution rate of the active ingredient).

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
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  • Diabetes (AREA)
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  • Obesity (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
PCT/JP2020/035883 2019-09-25 2020-09-24 不快な味がマスクされた顆粒剤及びその製造方法 Ceased WO2021060304A1 (ja)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN202080059661.5A CN114340601A (zh) 2019-09-25 2020-09-24 掩盖了令人不快的味道的颗粒剂及其制造方法
CA3153004A CA3153004A1 (en) 2019-09-25 2020-09-24 Granule having masked unpleasant taste and method for producing same
JP2021503619A JP6905781B1 (ja) 2019-09-25 2020-09-24 不快な味がマスクされた顆粒剤及びその製造方法
EP20867214.7A EP4035733A4 (en) 2019-09-25 2020-09-24 Granule having masked unpleasant taste and method for producing same
US17/642,107 US20230016901A1 (en) 2019-09-25 2020-09-24 Granule in which unpleasant taste is masked and method for producing granule
AU2020352037A AU2020352037A1 (en) 2019-09-25 2020-09-24 Granule having masked unpleasant taste and method for producing same

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2019-173744 2019-09-25
JP2019173744 2019-09-25

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WO2021060304A1 true WO2021060304A1 (ja) 2021-04-01

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US (1) US20230016901A1 (https=)
EP (1) EP4035733A4 (https=)
JP (3) JP6905781B1 (https=)
CN (1) CN114340601A (https=)
AU (1) AU2020352037A1 (https=)
CA (1) CA3153004A1 (https=)
TW (1) TWI865615B (https=)
WO (1) WO2021060304A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024005767A1 (en) * 2022-07-01 2024-01-04 Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi A taste masked solid composition of zinc active

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020352037A1 (en) * 2019-09-25 2022-04-21 Nobelpharma Co., Ltd. Granule having masked unpleasant taste and method for producing same

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09194347A (ja) 1996-01-18 1997-07-29 Asahi Chem Ind Co Ltd フィルムコーティング粒剤の製造方法
JP2000053563A (ja) 1998-08-07 2000-02-22 Bayer Yakuhin Ltd 苦味がマスクされた速放性細粒剤
JP2007031292A (ja) * 2005-07-22 2007-02-08 Hamari Chemicals Ltd 亜鉛化合物含有組成物およびその製造方法
WO2008013197A1 (fr) * 2006-07-26 2008-01-31 Asahi Kasei Chemicals Corporation Granulé brut sphérique et son procédé de fabrication
JP2008081448A (ja) 2006-09-28 2008-04-10 Kowa Pharmaceutical Co Ltd 酒石酸ゾルピデムの苦味マスキング速放性粒子
WO2011043370A1 (ja) * 2009-10-09 2011-04-14 旭化成ケミカルズ株式会社 コーティングフィルム、及びそれを用いた顆粒、錠剤

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2542122B2 (ja) * 1990-04-18 1996-10-09 旭化成工業株式会社 球状核、球形顆粒およびその製造方法
KR101168189B1 (ko) * 2003-10-29 2012-07-25 시오노기세이야쿠가부시키가이샤 불쾌미를 개선한 피복 제제의 제조 방법
CN102048734B (zh) * 2005-05-26 2013-11-20 大日本住友制药株式会社 药物组合物
AU2010325746B2 (en) * 2009-12-02 2016-02-25 Adare Pharmaceuticals S.R.L. Fexofenadine microcapsules and compositions containing them
CN102018658B (zh) * 2010-07-16 2014-03-12 钟术光 一种控释制剂及其制备方法
JP5823401B2 (ja) * 2010-09-13 2015-11-25 大鵬薬品工業株式会社 不快な味が遮蔽された薬物含有膜被覆粒子
AU2020352037A1 (en) * 2019-09-25 2022-04-21 Nobelpharma Co., Ltd. Granule having masked unpleasant taste and method for producing same

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09194347A (ja) 1996-01-18 1997-07-29 Asahi Chem Ind Co Ltd フィルムコーティング粒剤の製造方法
JP2000053563A (ja) 1998-08-07 2000-02-22 Bayer Yakuhin Ltd 苦味がマスクされた速放性細粒剤
JP2007031292A (ja) * 2005-07-22 2007-02-08 Hamari Chemicals Ltd 亜鉛化合物含有組成物およびその製造方法
WO2008013197A1 (fr) * 2006-07-26 2008-01-31 Asahi Kasei Chemicals Corporation Granulé brut sphérique et son procédé de fabrication
JP2008081448A (ja) 2006-09-28 2008-04-10 Kowa Pharmaceutical Co Ltd 酒石酸ゾルピデムの苦味マスキング速放性粒子
WO2011043370A1 (ja) * 2009-10-09 2011-04-14 旭化成ケミカルズ株式会社 コーティングフィルム、及びそれを用いた顆粒、錠剤

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"Handbook of Pharmaceutical Excipients", 28 February 2007, YAKUJI NIPPO, LIMITED, JP , ISBN: 978-4-8408-0968-9, article "Zinc acetate", pages: 340 - 341, XP009533810 *
See also references of EP4035733A4

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024005767A1 (en) * 2022-07-01 2024-01-04 Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi A taste masked solid composition of zinc active

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EP4035733A1 (en) 2022-08-03
CN114340601A (zh) 2022-04-12
TWI865615B (zh) 2024-12-11
JPWO2021060304A1 (ja) 2021-10-07
CA3153004A1 (en) 2021-04-01
JP6905781B1 (ja) 2021-07-21
TW202128143A (zh) 2021-08-01
JP2025107467A (ja) 2025-07-17
US20230016901A1 (en) 2023-01-19
EP4035733A4 (en) 2024-01-10
AU2020352037A1 (en) 2022-04-21
JP2021138775A (ja) 2021-09-16
JP7715378B2 (ja) 2025-07-30

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