WO2016114017A1 - オルメサルタンメドキソミルを含有するフィルムコーティング錠剤 - Google Patents

オルメサルタンメドキソミルを含有するフィルムコーティング錠剤 Download PDF

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Publication number
WO2016114017A1
WO2016114017A1 PCT/JP2015/083347 JP2015083347W WO2016114017A1 WO 2016114017 A1 WO2016114017 A1 WO 2016114017A1 JP 2015083347 W JP2015083347 W JP 2015083347W WO 2016114017 A1 WO2016114017 A1 WO 2016114017A1
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WO
WIPO (PCT)
Prior art keywords
tablet
magnesium carbonate
olmesartan medoxomil
diacetyl
film
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/JP2015/083347
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English (en)
French (fr)
Japanese (ja)
Inventor
一博 五丁森
孫市 酒向
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.)
Ohara Pharmaceutical Co Ltd
Original Assignee
Ohara 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 Ohara Pharmaceutical Co Ltd filed Critical Ohara Pharmaceutical Co Ltd
Publication of WO2016114017A1 publication Critical patent/WO2016114017A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone

Definitions

  • Olmesartan medoxomil has the chemical structure shown in FIG.
  • medoxomil shown in FIG. 2 is generated by hydrolysis. This medoxomil releases carbon dioxide and changes to 2,3-butanedione, or “diacetyl”, as shown in FIG. This diacetyl is a causative substance of off-flavors.
  • the total thickness of the coating film is reduced, and the use of magnesium carbonate The amount can be reduced.
  • the layer thickness of the moisture-proof coating film not containing magnesium carbonate can be appropriately selected from the range of the thickness of the film containing magnesium carbonate.
  • plasticizer that can be used in the present invention is not particularly limited and can be appropriately selected by those skilled in the art.
  • plasticizers include propylene glycol, polyethylene glycol, polypropylene glycol, glycerin and sorbitol, glycerin triacetate, diethyl phthalate and triethyl citrate, lauric acid, sucrose, dextrose, sorbitol, triacetin, and acetyl triethyl titrate. , Triethyl titrate, tributyl titrate, acetyl tributyl titrate and the like.
  • Olmesartan medoxomil 40.0 g, D-mannitol 150.0 g, crystalline cellulose 32.0 g, and low-substituted hydroxypropylcellulose 16.0 g were charged into a fluidized bed granulator (manufactured by Paulec: MP-01 type). A solution obtained by dissolving 7.0 g of cellulose in 100.0 g of purified water was sprayed and granulated. The obtained granules were dried and sieved with a JIS 30 mesh sieve. To 122.5 g of the obtained sized product, 1.5 g of calcium stearate was added and mixed in a polyethylene bag.
  • this mixture was compression-molded to a diameter of 8 mm using a rotary tableting machine (manufactured by Kikusui Seisakusho: VELA5 type) to obtain an uncoated tablet having a mass of 120 mg.
  • the uncoated tablet was put into a coating machine (Freund Corporation: HC-FZ-Labo type), and polyvinyl alcohol / acrylic acid / methyl methacrylate copolymer (POVACOAT: registered trademark of Daido Kasei Co., Ltd.) 21 in advance.
  • 0.08 g and 21.0 g of talc were added to 378.0 g of purified water, and the uniformly dispersed liquid was sprayed, coated to a weight of 124 mg per tablet, and dried to obtain coated tablets. Further, the above coated tablets were put into a coating machine (Freund's HC-FZ-Labo type), to which 24.15 g of hypromellose, 1.575 g of titanium oxide, 3.15 g of talc, 1.575 g of polyethylene glycol and carbonic acid carbonate were added. 1.05 g of magnesium was added to 472.5 g of purified water, and the uniformly dispersed liquid was sprayed, coated until the mass of one tablet was about 127 mg, and dried to obtain coated tablets.
  • Olmesartan medoxomil 150.0 g, D-mannitol 531.0 g, crystalline cellulose 120.0 g, low-substituted hydroxypropylcellulose 60.0 g and light anhydrous silicic acid 1.5 g were fluidized bed granulator (manufactured by Paulec Co., Ltd .: MP-01) Type) and a solution obtained by dissolving 26.25 g of hydroxypropylcellulose in 498.75 g of purified water was sprayed and granulated. The obtained granules were dried and sieved with a JIS 30 mesh sieve. 10.5 g of magnesium stearate was added to 829.5 g of the obtained sized product, and mixed in a polyethylene bag.
  • Magnesium (6.3 g) was added to purified water (472.5 g), and the uniformly dispersed liquid was sprayed, coated until the mass of one tablet was about 127 mg, and dried to obtain coated tablets.
  • [Components] [Weight per tablet (mg)] Olmesartan medoxomil 20.0 D-mannitol 70.8 Crystalline cellulose 16.0 Low-substituted hydroxypropyl cellulose 8.0 Hydroxypropyl cellulose 3.5 Light anhydrous silicic acid 0.2 Magnesium stearate 1.5 Polyvinyl alcohol / acrylic acid / methyl methacrylate copolymer 2.0 Talc 2.3 Hypromellose 1.8 Polyethylene glycol 0.15 Titanium oxide 0.15 Magnesium carbonate 0.6
  • Olmesartan medoxomil 150.0 g, D-mannitol 531.0 g, crystalline cellulose 120.0 g, low-substituted hydroxypropylcellulose 60.0 g and light anhydrous silicic acid 1.5 g were fluidized bed granulator (manufactured by Paulec Co., Ltd .: MP-01) Type) and a solution obtained by dissolving 26.25 g of hydroxypropylcellulose in 498.75 g of purified water was sprayed and granulated. The obtained granules were dried and sieved with a JIS 30 mesh sieve. 10.5 g of magnesium stearate was added to 829.5 g of the obtained sized product, and mixed in a polyethylene bag.
  • this mixture was compression-molded to a diameter of 8 mm using a rotary tableting machine (manufactured by Kikusui Seisakusho: VELA5 type) to obtain an uncoated tablet having a mass of 120 mg.
  • the uncoated tablet was put into a coating machine (Freund Corporation: HC-FZ-Labo type), and polyvinyl alcohol / acrylic acid / methyl methacrylate copolymer (POVACOAT: registered trademark of Daido Kasei Co., Ltd.) 21 in advance.
  • 0.08 g and 21.0 g of talc were added to 378.0 g of purified water, and the uniformly dispersed liquid was sprayed, coated to a weight of 124 mg per tablet, and dried to obtain coated tablets. Furthermore, the above coated tablets were put into a coating machine (Freund Corporation: HC-FZ-Labo type), and 25.2 g of hypromellose, 1.575 g of titanium oxide, 3.15 g of talc and 1.575 g of polyethylene glycol were purified in advance. In addition to 472.5 g of water, the uniformly dispersed liquid was sprayed, coated until the mass of one tablet was about 127 mg, and dried to obtain a two-layer coated tablet.
  • the unpleasant odor is suppressed remarkably and the olmesartan medoxomil containing film coating formulation excellent in commercial property can be provided to a medical field.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
PCT/JP2015/083347 2015-01-15 2015-11-27 オルメサルタンメドキソミルを含有するフィルムコーティング錠剤 Ceased WO2016114017A1 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2015-005618 2015-01-15
JP2015005618 2015-01-15

Publications (1)

Publication Number Publication Date
WO2016114017A1 true WO2016114017A1 (ja) 2016-07-21

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PCT/JP2015/083347 Ceased WO2016114017A1 (ja) 2015-01-15 2015-11-27 オルメサルタンメドキソミルを含有するフィルムコーティング錠剤

Country Status (2)

Country Link
JP (2) JP6188091B2 (enExample)
WO (1) WO2016114017A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025137498A1 (en) * 2023-12-20 2025-06-26 Areteia Therapeutics, Inc. Matrix tablets of dexpramipexole and methods of manufacturing and use thereof

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7209555B2 (ja) * 2019-01-18 2023-01-20 日本ジェネリック株式会社 ラメルテオン含有フィルムコーティング錠剤
KR20240031121A (ko) * 2022-08-31 2024-03-07 (주)셀트리온 이중 냄새 차폐 약학 조성물

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002191387A (ja) * 2000-12-26 2002-07-09 Yakult Honsha Co Ltd 乳酸菌培養上清およびその製造方法並びに当該上清を利用する皮膚外用剤
WO2009113420A1 (ja) * 2008-03-13 2009-09-17 第一三共株式会社 オルメサルタンメドキソミルを含む製剤の溶出性の改善

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH092976A (ja) * 1995-06-20 1997-01-07 Lion Corp 被覆組成物
JP2002201418A (ja) * 2000-12-28 2002-07-19 Nonogawa Shoji Kk コーティング剤及びこれを用いたコーティング錠
WO2010018777A1 (ja) * 2008-08-11 2010-02-18 第一三共株式会社 におい抑制方法
JP5744340B2 (ja) * 2013-05-24 2015-07-08 持田製薬株式会社 フィルムコーティング用組成物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002191387A (ja) * 2000-12-26 2002-07-09 Yakult Honsha Co Ltd 乳酸菌培養上清およびその製造方法並びに当該上清を利用する皮膚外用剤
WO2009113420A1 (ja) * 2008-03-13 2009-09-17 第一三共株式会社 オルメサルタンメドキソミルを含む製剤の溶出性の改善

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025137498A1 (en) * 2023-12-20 2025-06-26 Areteia Therapeutics, Inc. Matrix tablets of dexpramipexole and methods of manufacturing and use thereof

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Publication number Publication date
JP2016135755A (ja) 2016-07-28
JP6188091B2 (ja) 2017-08-30
JP2017119714A (ja) 2017-07-06

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