JP5148813B2 - プロトンポンプ阻害剤の液体剤形 - Google Patents
プロトンポンプ阻害剤の液体剤形 Download PDFInfo
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- JP5148813B2 JP5148813B2 JP2004519828A JP2004519828A JP5148813B2 JP 5148813 B2 JP5148813 B2 JP 5148813B2 JP 2004519828 A JP2004519828 A JP 2004519828A JP 2004519828 A JP2004519828 A JP 2004519828A JP 5148813 B2 JP5148813 B2 JP 5148813B2
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- liquid
- microparticles
- viscosity
- ppi
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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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
-
- 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
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Description
本実施例では、ランソプラゾール(登録商標)(aPPI)を含有する微粒子を各種液体懸濁ビヒクル中に懸濁して、均一用量がバルク懸濁液から分配され得るかを調べた。
本実施例では、実施例1と同様にして懸濁液を調製し、各懸濁液の単一サンプルを分析した。各サンプルは、蒸留水(10ml)、LFDT錠(1個)及びサッシェ不活性成分(2g)を用いて調製した。10懸濁液の各々の理論の%を下表3に示す。また、1つの懸濁液からの複数のアリコートの理論の%が再現性であるかを調べるためにサンプル10から2個の追加サンプルを採取した。これらの結果を下表4に示す。
本実施例では、組成物中の活性成分の安定性を評価した。具体的には、組成物中の酸不安定性薬物ランソプラゾールの安定性を調べた。
本実施例では、異なる量の増粘剤(サッシェ不活性成分)を蒸留水に添加し、生じた溶液の粘度を測定した。粘度は標準#3スピンドル及び温度プローブを備えたブルックフィールド粘度計を用いて測定した。各サンプル(150ml)を200ml容量トールビーカーに入れ、粘度を5ppmで回転するスピンドルを用いて測定した。
Claims (4)
- (a)腸溶コーティングを被したプロトンポンプ阻害剤を含む微粒子;及び
(b)6.0未満のpHと、500cP以上且つ8614cP以下の粘度とを有する液体懸濁ビヒクル、
を含むヒト患者に投与するのに好適な組成物であって、前記微粒子が100〜900μmの大きさであり、少なくとも90%のプロトンポンプ阻害剤が組成物の全体にわたって分散している、前記組成物。 - 活性成分がランソプラゾールである請求の範囲第1項に記載の組成物。
- a)腸溶コーティングを被したプロトンポンプ阻害剤を含む微粒子を収容した第1容器;及び
b)液体を収容した第2容器、
を含むキットであって、
前記第1または第2容器が更に酸性賦形剤を含み、
前記第1及び第2容器の内容物を混合して生ずる液体が前記微粒子を懸濁させる500cP以上且つ8614cP以下の粘度を有するよう、前記第1または第2容器が更に増粘剤を含み、
前記微粒子が100〜900μmの大きさである、キット。 - プロトンポンプ阻害剤がランソプラゾールである請求の範囲第3項に記載のキット。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US19023902A | 2002-07-03 | 2002-07-03 | |
US10/190,239 | 2002-07-03 | ||
PCT/US2003/020946 WO2004004690A1 (en) | 2002-07-03 | 2003-07-02 | Liquid dosage forms of proton pump inhibitors |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2012165900A Division JP2013028603A (ja) | 2002-07-03 | 2012-07-26 | プロトンポンプ阻害剤の液体剤形 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2005535661A JP2005535661A (ja) | 2005-11-24 |
JP2005535661A5 JP2005535661A5 (ja) | 2006-08-10 |
JP5148813B2 true JP5148813B2 (ja) | 2013-02-20 |
Family
ID=30114048
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004519828A Expired - Fee Related JP5148813B2 (ja) | 2002-07-03 | 2003-07-02 | プロトンポンプ阻害剤の液体剤形 |
JP2012165900A Pending JP2013028603A (ja) | 2002-07-03 | 2012-07-26 | プロトンポンプ阻害剤の液体剤形 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2012165900A Pending JP2013028603A (ja) | 2002-07-03 | 2012-07-26 | プロトンポンプ阻害剤の液体剤形 |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP1572151A1 (ja) |
JP (2) | JP5148813B2 (ja) |
CA (1) | CA2490142A1 (ja) |
MX (1) | MXPA05000301A (ja) |
WO (1) | WO2004004690A1 (ja) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9901551B2 (en) * | 2009-04-20 | 2018-02-27 | Ambra Bioscience Llc | Chemosensory receptor ligand-based therapies |
EP2630491A4 (en) | 2010-10-19 | 2014-08-27 | Elcelyx Therapeutics Inc | THERAPIES BASED ON CHEMOSOUS RECEPTOR LIGANDS |
WO2013058996A1 (en) * | 2011-10-19 | 2013-04-25 | R.P. Scherer Technologies, Llc | Two phase pharmaceutical delivery system |
GB2535130B (en) * | 2014-09-29 | 2020-09-02 | Veriton Pharma Ltd | A Suspension |
WO2017145146A1 (en) | 2016-02-25 | 2017-08-31 | Dexcel Pharma Technologies Ltd. | Compositions comprising proton pump inhibitors |
GB202116644D0 (en) | 2021-11-18 | 2022-01-05 | Innovate Pharmaceuticals Ltd | Liquid composition |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE9301489D0 (sv) * | 1993-04-30 | 1993-04-30 | Ab Astra | Veterinary composition |
US5708017A (en) * | 1995-04-04 | 1998-01-13 | Merck & Co., Inc. | Stable, ready-to-use pharmaceutical paste composition containing proton pump inhibitors |
EE04576B1 (et) * | 1997-12-08 | 2006-02-15 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Suposiit happes ebapüsivate toimeainete tarbeks, selle valmistamismeetod, toimeaineühik ja selle valmistamismeetod ning preparaat |
DE19925710C2 (de) * | 1999-06-07 | 2002-10-10 | Byk Gulden Lomberg Chem Fab | Neue Zubereitung und Darreichungsform enthaltend einen säurelabilen Protonenpumpenhemmer |
UA80393C2 (uk) * | 2000-12-07 | 2007-09-25 | Алтана Фарма Аг | Фармацевтична композиція, яка містить інгібітор фде 4, диспергований в матриці |
BR0115989A (pt) * | 2000-12-07 | 2004-01-13 | Altana Pharma Ag | Preparação farmacêutica na forma de uma suspensão compreendendo um ingrediente ativo instável a ácido |
-
2003
- 2003-07-02 EP EP03763155A patent/EP1572151A1/en not_active Withdrawn
- 2003-07-02 JP JP2004519828A patent/JP5148813B2/ja not_active Expired - Fee Related
- 2003-07-02 WO PCT/US2003/020946 patent/WO2004004690A1/en active Application Filing
- 2003-07-02 MX MXPA05000301A patent/MXPA05000301A/es active IP Right Grant
- 2003-07-02 CA CA002490142A patent/CA2490142A1/en not_active Abandoned
-
2012
- 2012-07-26 JP JP2012165900A patent/JP2013028603A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
JP2013028603A (ja) | 2013-02-07 |
EP1572151A1 (en) | 2005-09-14 |
MXPA05000301A (es) | 2005-03-31 |
WO2004004690A1 (en) | 2004-01-15 |
CA2490142A1 (en) | 2004-01-15 |
JP2005535661A (ja) | 2005-11-24 |
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