JP4523278B2 - 酸に不安定なベンズイミダゾール化合物を含む腸溶性コーティングを備えた、経口用圧縮薬学的剤形 - Google Patents
酸に不安定なベンズイミダゾール化合物を含む腸溶性コーティングを備えた、経口用圧縮薬学的剤形 Download PDFInfo
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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
- A61K9/2072—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
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- 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
- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- 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
- A61K9/2886—Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
-
- 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
- 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
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Description
(a)i)不活性コアと、
ii)酸性媒質中で不安定なベンズイミダゾール化合物と、非アルカリの水溶性不活性ポリマーと、1または複数の薬学的に許容される不活性賦形剤とから形成される前記不活性i)コア上に堆積させた活性層と、
iii)非アルカリの水溶性不活性ポリマーと1または複数の薬学的に許容される不活性賦形剤とから形成される不活性な非アルカリ性コーティングから構成され、前記不活性コアi)を被覆する前記活性層ii)上に配置された中間層と、
を含む、活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含む複数のユニットと、
(b)1または複数の薬学的に許容される不活性賦形剤であって、そのうちの1または複数が圧縮賦形剤である賦形剤と、
(c)活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含む前記複数のユニットと前記薬学的に許容される不活性賦形剤(b)とをコートする腸溶性コーティングと、
を含む。
R1は水素、メトキシまたはジフルオロメトキシであり、
R2はメチルまたはメトキシであり、
R3はメトキシ、2,2,2−トリフルオロエトキシまたは3−メトキシプロポキシであり、および
R4は水素またはメチルである)。
1,250gの活性成分[オメプラゾールまたはランソプラゾール]および478.73gのHPMCを4,033gの精製(脱イオン)水中に分散させて、活性成分の懸濁液を調製する。
Claims (8)
- (a)i)不活性コアと、
ii)酸性媒質中で不安定なベンズイミダゾール化合物と、非アルカリの水溶性不活性ポリマーと、1または複数の薬学的に許容される不活性賦形剤とから形成される、前記不活性コアi)上に堆積させた活性層と、
iii)非アルカリの水溶性不活性ポリマーと1または複数の薬学的に許容される不活性賦形剤から形成される不活性な非アルカリ性コーティングから構成され、前記不活性コアi)を被覆する前記活性層ii)上に配置される中間層と、
を含む、活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含む複数のユニットと、
(b)1または複数の薬学的に許容される不活性賦形剤であって、そのうちの1または複数が圧縮賦形剤である賦形剤と、
(c)活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含む前記複数のユニットと前記薬学的に許容される不活性賦形剤(b)とをコートする腸溶性コーティングと、
を含む、活性成分として、酸性媒質中で不安定なベンズイミダゾール化合物を含む複数のユニットから構成される、腸溶性コーティングで被覆された、錠剤型の経口用薬学的剤形。 - 前記酸性媒質中で不安定なベンズイミダゾール化合物は、オメプラゾール、ランソプラゾール、ラベプラゾールおよびパントプラゾールまたはそれらの対応する鏡像異性体からなる群から選択される請求項1記載の錠剤型の経口用薬学的剤形。
- 前記活性層ii)中に存在する前記非アルカリの水溶性不活性ポリマーは、ヒドロキシプロピルメチルセルロース(HPMC)およびヒドロキシプロピルセルロース(HPC)の中から選択される請求項1〜3のいずれか1項に記載の錠剤型の経口用薬学的剤形。
- 前記中間層iii)中に存在する前記非アルカリの水溶性不活性ポリマーは、ヒドロキシプロピルメチルセルロース(HPMC)である請求項1〜3のいずれか1項に記載の錠剤型の経口用薬学的剤形。
- 前記圧縮賦形剤は、希釈剤、崩壊剤、潤滑剤およびそれらの混合物により形成される群のなかから選択される請求項1記載の錠剤型の経口用薬学的剤形。
- 前記活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含む前記複数のユニットと前記薬学的に許容される賦形剤(b)とを被覆する前記腸溶性コーティング層(c)は、胃耐性ポリマーと、可塑剤と、または複数の薬学的に許容される不活性賦形剤とを含む請求項1記載の錠剤型の経口用薬学的剤形。
- 酸性媒質中で不安定なベンズイミダゾールと、非アルカリの水溶性不活性ポリマーと、1または複数の薬学的に許容される不活性賦形剤との水溶性懸濁液を不活性コアに塗布し、不活性コアをコートする活性層を得る工程と、
前記活性層上に、非アルカリの水溶性不活性ポリマーと1または複数の薬学的に許容される不活性賦形剤とからなる非アルカリの不活性コーティングを含む中間層を塗布し、活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含むユニットを得る工程と、
活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含む前記複数のユニットを、1または複数の薬学的に許容される不活性賦形剤であって、前記不活性賦形剤のうちの1または複数が圧縮賦形剤である不活性賦形剤と混合し、前記混合物を圧縮し、錠剤を得る工程と、
胃耐性ポリマーと、可塑剤と、1または複数の薬学的に許容される不活性賦形剤とを含む水溶性懸濁液で、前記錠剤を被覆し、外側腸溶性コーティング層を形成する工程と、
を含む、請求項1〜7のいずれか1項に記載の活性成分として酸性媒質中で不安定なベンズイミダゾール化合物を含む複数のユニットからなる、腸溶性コーティングで被覆された錠剤型の経口用薬学的剤形を調製するためのプロセス。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES200102820A ES2198195B1 (es) | 2001-12-18 | 2001-12-18 | Forma de dosificacion farmaceutica oral comprimida, con recubrimiento enterico, que contiene un compuesto de bencimidazol labil en medio acido. |
PCT/ES2002/000536 WO2003051342A1 (es) | 2001-12-18 | 2002-11-18 | Forma de dosificacion farmaceutica oral comprimida, con recubrimiento enterico, que contiene un compuesto de bencimidazol labil en medio acido |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2005523884A JP2005523884A (ja) | 2005-08-11 |
JP4523278B2 true JP4523278B2 (ja) | 2010-08-11 |
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Application Number | Title | Priority Date | Filing Date |
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JP2003552275A Expired - Fee Related JP4523278B2 (ja) | 2001-12-18 | 2002-11-18 | 酸に不安定なベンズイミダゾール化合物を含む腸溶性コーティングを備えた、経口用圧縮薬学的剤形 |
Country Status (19)
Country | Link |
---|---|
US (1) | US7217429B2 (ja) |
EP (1) | EP1464331B9 (ja) |
JP (1) | JP4523278B2 (ja) |
KR (1) | KR100877649B1 (ja) |
AT (1) | ATE410149T1 (ja) |
AU (1) | AU2002350750B2 (ja) |
CA (1) | CA2470609C (ja) |
DE (1) | DE60229295D1 (ja) |
DK (1) | DK1464331T3 (ja) |
ES (2) | ES2198195B1 (ja) |
HR (1) | HRP20040596A2 (ja) |
HU (1) | HUP0402488A3 (ja) |
IL (2) | IL162544A0 (ja) |
MX (1) | MXPA04005902A (ja) |
NO (1) | NO20042630L (ja) |
NZ (1) | NZ533886A (ja) |
PT (1) | PT1464331E (ja) |
WO (1) | WO2003051342A1 (ja) |
ZA (1) | ZA200405078B (ja) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI372066B (en) * | 2003-10-01 | 2012-09-11 | Wyeth Corp | Pantoprazole multiparticulate formulations |
ES2278511B1 (es) * | 2005-07-28 | 2008-06-16 | Laboratorios Almirall S.A. | Comprimidos con perfil de disolucion mejorado. |
WO2007100984A2 (en) * | 2006-02-24 | 2007-09-07 | Allergan, Inc. | Beads containing pyridin-sulfinyl benzoimidazole sulfonyl phenoxy acetate derivatives |
CA2748783A1 (en) * | 2009-01-05 | 2010-07-08 | Mcneil-Ppc, Inc. | Three layer tablet containing cetirizine, pseudoephedrine, and naproxen |
US8377475B2 (en) * | 2009-01-05 | 2013-02-19 | Mcneil-Ppc, Inc. | Tablet containing cetirizine, pseudoephedrine, and naproxen containing a barrier layer |
US8252330B2 (en) * | 2009-01-05 | 2012-08-28 | Mcneil-Ppc, Inc. | Tablet containing coated particles of cetirizine, pseudoephedrine, and/or naproxen |
WO2010117756A2 (en) * | 2009-03-31 | 2010-10-14 | Dr. Reddy's Laboratories Ltd | Substituted benzimidazole pharmaceutical formulations |
EP2345408A3 (en) * | 2010-01-08 | 2012-02-29 | Dr. Reddy's Laboratories Ltd. | Acid labile drug formulations |
NZ607225A (en) * | 2010-07-22 | 2015-02-27 | Lupin Ltd | Multiple unit tablet composition |
US10058542B1 (en) | 2014-09-12 | 2018-08-28 | Thioredoxin Systems Ab | Composition comprising selenazol or thiazolone derivatives and silver and method of treatment therewith |
EP3288556A4 (en) | 2015-04-29 | 2018-09-19 | Dexcel Pharma Technologies Ltd. | Orally disintegrating compositions |
US10736855B2 (en) | 2016-02-25 | 2020-08-11 | Dexcel Pharma Technologies Ltd. | Compositions comprising proton pump inhibitors |
US10076494B2 (en) | 2016-06-16 | 2018-09-18 | Dexcel Pharma Technologies Ltd. | Stable orally disintegrating pharmaceutical compositions |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB2189699A (en) | 1986-04-30 | 1987-11-04 | Haessle Ab | Coated acid-labile medicaments |
GB2189698A (en) * | 1986-04-30 | 1987-11-04 | Haessle Ab | Coated omeprazole tablets |
CZ289804B6 (cs) * | 1994-07-08 | 2002-04-17 | Astrazeneca Ab | Multijednotková tabletovaná dávková forma I |
SE9402431D0 (sv) * | 1994-07-08 | 1994-07-08 | Astra Ab | New tablet formulation |
ES2094694B1 (es) | 1995-02-01 | 1997-12-16 | Esteve Quimica Sa | Nueva formulacion farmaceuticamente estable de un compuesto de bencimidazol y su proceso de obtencion. |
SE9500422D0 (sv) * | 1995-02-06 | 1995-02-06 | Astra Ab | New oral pharmaceutical dosage forms |
DK1308159T3 (da) * | 1995-09-21 | 2005-02-14 | Pharma Pass Ii Llc | Farmaceutisk sammensætning indeholdende en syre-labil omeprazol og fremgangsmåde til fremstilling deraf |
SE9600070D0 (sv) * | 1996-01-08 | 1996-01-08 | Astra Ab | New oral pharmaceutical dosage forms |
SE9700885D0 (sv) * | 1997-03-12 | 1997-03-12 | Astra Ab | New pharmaceutical formulation |
ES2168043B1 (es) * | 1999-09-13 | 2003-04-01 | Esteve Labor Dr | Forma farmaceutica solida oral de liberacion modificada que contiene un compuesto de bencimidazol labil en medio acido. |
JP2002363080A (ja) * | 2001-06-08 | 2002-12-18 | Towa Yakuhin Kk | 安定な内服用抗潰瘍製剤の製造法 |
-
2001
- 2001-12-18 ES ES200102820A patent/ES2198195B1/es not_active Expired - Fee Related
-
2002
- 2002-11-18 MX MXPA04005902A patent/MXPA04005902A/es active IP Right Grant
- 2002-11-18 ES ES02785447T patent/ES2315416T3/es not_active Expired - Lifetime
- 2002-11-18 EP EP02785447A patent/EP1464331B9/en not_active Expired - Lifetime
- 2002-11-18 AT AT02785447T patent/ATE410149T1/de active
- 2002-11-18 HU HU0402488A patent/HUP0402488A3/hu unknown
- 2002-11-18 KR KR1020047009314A patent/KR100877649B1/ko not_active IP Right Cessation
- 2002-11-18 DK DK02785447T patent/DK1464331T3/da active
- 2002-11-18 IL IL16254402A patent/IL162544A0/xx unknown
- 2002-11-18 JP JP2003552275A patent/JP4523278B2/ja not_active Expired - Fee Related
- 2002-11-18 DE DE60229295T patent/DE60229295D1/de not_active Expired - Lifetime
- 2002-11-18 WO PCT/ES2002/000536 patent/WO2003051342A1/es active IP Right Grant
- 2002-11-18 NZ NZ533886A patent/NZ533886A/en not_active IP Right Cessation
- 2002-11-18 CA CA2470609A patent/CA2470609C/en not_active Expired - Fee Related
- 2002-11-18 AU AU2002350750A patent/AU2002350750B2/en not_active Ceased
- 2002-11-18 PT PT02785447T patent/PT1464331E/pt unknown
- 2002-12-12 US US10/317,702 patent/US7217429B2/en not_active Expired - Fee Related
-
2004
- 2004-06-15 IL IL162544A patent/IL162544A/en not_active IP Right Cessation
- 2004-06-23 NO NO20042630A patent/NO20042630L/no not_active Application Discontinuation
- 2004-06-25 ZA ZA200405078A patent/ZA200405078B/en unknown
- 2004-06-30 HR HR20040596A patent/HRP20040596A2/hr not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
NZ533886A (en) | 2005-12-23 |
ZA200405078B (en) | 2005-06-27 |
IL162544A (en) | 2010-04-29 |
PT1464331E (pt) | 2008-11-19 |
US7217429B2 (en) | 2007-05-15 |
HUP0402488A2 (hu) | 2005-05-30 |
KR20040079906A (ko) | 2004-09-16 |
DE60229295D1 (de) | 2008-11-20 |
ES2198195B1 (es) | 2004-10-01 |
KR100877649B1 (ko) | 2009-01-12 |
US20030118650A1 (en) | 2003-06-26 |
ES2315416T3 (es) | 2009-04-01 |
EP1464331B1 (en) | 2008-10-08 |
AU2002350750A1 (en) | 2003-06-30 |
AU2002350750B2 (en) | 2008-10-16 |
CA2470609A1 (en) | 2003-06-26 |
JP2005523884A (ja) | 2005-08-11 |
EP1464331A1 (en) | 2004-10-06 |
WO2003051342A1 (es) | 2003-06-26 |
MXPA04005902A (es) | 2004-09-13 |
IL162544A0 (en) | 2005-11-20 |
ATE410149T1 (de) | 2008-10-15 |
NO20042630L (no) | 2004-08-13 |
HRP20040596A2 (en) | 2004-10-31 |
HUP0402488A3 (en) | 2009-09-28 |
DK1464331T3 (da) | 2009-01-05 |
ES2198195A1 (es) | 2004-01-16 |
CA2470609C (en) | 2010-09-28 |
EP1464331B9 (en) | 2009-10-14 |
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