NO304010B1 - FremgangsmÕte for fremstilling av en pelletformulering for bruk i behandlingen av inflammatoriske tarmsykdommer - Google Patents
FremgangsmÕte for fremstilling av en pelletformulering for bruk i behandlingen av inflammatoriske tarmsykdommer Download PDFInfo
- Publication number
- NO304010B1 NO304010B1 NO922004A NO922004A NO304010B1 NO 304010 B1 NO304010 B1 NO 304010B1 NO 922004 A NO922004 A NO 922004A NO 922004 A NO922004 A NO 922004A NO 304010 B1 NO304010 B1 NO 304010B1
- Authority
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- Norway
- Prior art keywords
- budesonide
- water
- epimer
- polymer
- insoluble
- Prior art date
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Classifications
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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
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
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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
- A61K9/48—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
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Ultra Sonic Daignosis Equipment (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE8903914A SE8903914D0 (sv) | 1989-11-22 | 1989-11-22 | Oral composition for the treatment of inflammatory bowel diseases |
PCT/SE1990/000738 WO1991007172A1 (en) | 1989-11-22 | 1990-11-15 | Oral composition for the treatment of inflammatory bowel diseases |
Publications (3)
Publication Number | Publication Date |
---|---|
NO922004D0 NO922004D0 (no) | 1992-05-21 |
NO922004L NO922004L (no) | 1992-05-21 |
NO304010B1 true NO304010B1 (no) | 1998-10-12 |
Family
ID=20377544
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
NO922004A NO304010B1 (no) | 1989-11-22 | 1992-05-21 | FremgangsmÕte for fremstilling av en pelletformulering for bruk i behandlingen av inflammatoriske tarmsykdommer |
Country Status (36)
Country | Link |
---|---|
US (1) | US6423340B1 (sr) |
EP (1) | EP0502092B1 (sr) |
JP (1) | JP3145111B2 (sr) |
KR (1) | KR0179042B1 (sr) |
AT (1) | ATE125445T1 (sr) |
AU (1) | AU643021B2 (sr) |
CA (1) | CA2071518C (sr) |
DE (1) | DE69021214T2 (sr) |
DK (1) | DK0502092T3 (sr) |
EG (1) | EG19642A (sr) |
ES (1) | ES2074698T3 (sr) |
FI (2) | FI104949B (sr) |
GR (1) | GR3017691T3 (sr) |
HK (1) | HK51897A (sr) |
HR (1) | HRP920632B1 (sr) |
HU (2) | HU216836B (sr) |
IE (1) | IE74854B1 (sr) |
IL (1) | IL96415A (sr) |
IS (1) | IS1858B (sr) |
LT (1) | LT3696B (sr) |
LV (1) | LV10183B (sr) |
MY (1) | MY104535A (sr) |
NO (1) | NO304010B1 (sr) |
NZ (1) | NZ235807A (sr) |
PL (1) | PL166506B1 (sr) |
PT (1) | PT95946A (sr) |
RU (1) | RU2134104C1 (sr) |
SA (1) | SA90110123B1 (sr) |
SE (1) | SE8903914D0 (sr) |
SG (1) | SG54210A1 (sr) |
SI (1) | SI9012150A (sr) |
TW (1) | TW250435B (sr) |
UA (1) | UA37196C2 (sr) |
WO (1) | WO1991007172A1 (sr) |
YU (1) | YU48583B (sr) |
ZA (1) | ZA908777B (sr) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5316772A (en) * | 1990-12-19 | 1994-05-31 | Solvay & Cie, S.A. (Societe Anonyme) | Bilayered oral pharmaceutical composition with pH dependent release |
BR9307746A (pt) * | 1993-01-08 | 1995-11-14 | Astra Ab | Derivados de esteróides especificos para otratamento de cólon e ileo |
US5914132A (en) * | 1993-02-26 | 1999-06-22 | The Procter & Gamble Company | Pharmaceutical dosage form with multiple enteric polymer coatings for colonic delivery |
DE4332394A1 (de) * | 1993-09-23 | 1995-03-30 | Falk Pharma Gmbh | Budesonid-Pellets mit kontrolliertem Freigabeprofil und Verfahren zu ihrer Herstellung |
US5686106A (en) * | 1995-05-17 | 1997-11-11 | The Procter & Gamble Company | Pharmaceutical dosage form for colonic delivery |
CA2271560C (en) * | 1996-11-15 | 2003-09-23 | Mayo Foundation For Medical Education And Research | Pharmaceutical dosage form for colonic delivery |
SE9604751D0 (sv) | 1996-12-20 | 1996-12-20 | Astra Ab | New therapy |
DE19732903A1 (de) | 1997-07-30 | 1999-02-04 | Falk Pharma Gmbh | Pellet-Formulierung zur Behandlung des Intestinaltraktes |
US6239120B1 (en) | 1998-03-17 | 2001-05-29 | Pharmalink Ab | Method and means for treating glomerulonephritis |
GB9824604D0 (en) | 1998-11-11 | 1999-01-06 | Hewlett Healthcare Limited | Treatment of allergic conditions |
SE9902673D0 (sv) * | 1999-07-12 | 1999-07-12 | Astra Ab | New composition |
DK1392321T3 (da) * | 2001-03-15 | 2010-11-29 | Soligenix Inc | Fremgangsmåde til behandling af inflammatoriske sygdomme i mave-tarm-kanalen ved anvendelse af topisk aktive corticosteroider |
DE10250543A1 (de) * | 2002-10-29 | 2004-05-19 | Röhm GmbH & Co. KG | Mehrschichtige Arzneiform |
US7879833B2 (en) | 2002-12-12 | 2011-02-01 | Nycomed Gmbh | Combination medicament |
US20060188563A1 (en) * | 2003-03-27 | 2006-08-24 | Hisamitsu Pharmaceutical Co., Inc. | Medicinal oral preparations for colon delivery, medicinal oral preparations for treating colon cancer and medicinal oral preparations for treating colitis |
ATE476185T1 (de) * | 2003-09-15 | 2010-08-15 | Nycomed Gmbh | Verwendung von ciclesonid zur behandlung von entzündlichen darmerkrankungen |
EP1670482B2 (en) | 2003-09-16 | 2022-06-29 | Covis Pharma B.V. | Use of ciclesonide for the treatment of respiratory diseases |
CA2570916C (en) | 2004-06-16 | 2013-06-11 | Tap Pharmaceutical Products, Inc. | Pulsed release dosage form of a ppi |
WO2007056539A2 (en) * | 2005-11-08 | 2007-05-18 | Medarex, Inc. | Prophylaxis and treatment of enterocolitis associated with anti-ctla-4 antibody therapy |
JPWO2008117814A1 (ja) * | 2007-03-26 | 2010-07-15 | 帝國製薬株式会社 | 大腸送達用経口製剤 |
GB0808537D0 (en) * | 2008-05-12 | 2008-06-18 | Archimedes Dev Ltd | Compositions |
EP2334178A4 (en) * | 2008-10-03 | 2012-04-11 | Falk Pharma Gmbh | COMPOSITIONS AND METHODS OF TREATING THERAPEUTIC DISEASES WITH GRANULATED MESALAMINE |
US8945615B2 (en) * | 2009-02-17 | 2015-02-03 | Mylan Pharmaceuticals Inc. | Controlled release budesonide minitablets |
US8945616B2 (en) * | 2009-02-17 | 2015-02-03 | Mylan Pharmaceuticals Inc. | Controlled release budesonide minitablets |
AU2012211968A1 (en) * | 2011-02-04 | 2013-08-29 | Optimer Pharmaceuticals, Inc. | Treatment of bacterial infections |
MD480Z5 (ro) * | 2011-07-07 | 2012-09-30 | Эльвира АНДОН | Metodă de tratament al colitei ulceroase nespecifice acute |
JOP20200144A1 (ar) | 2012-04-30 | 2017-06-16 | Tillotts Pharma Ag | تركيبة عقار ذو إطلاق متأخر |
EP3062776A1 (en) | 2013-10-29 | 2016-09-07 | Tillotts Pharma AG | A delayed release drug formulation |
US9707182B2 (en) * | 2015-09-11 | 2017-07-18 | Sun Pharmaceutical Industries Ltd. | Oral pharmaceutical dosage forms of budesonide |
CN105663091A (zh) * | 2016-01-28 | 2016-06-15 | 上海信谊百路达药业有限公司 | 一种布地奈德肠溶缓释胶囊及其制备方法 |
CN108601744B (zh) * | 2016-02-09 | 2022-01-04 | 阿尔比里奥公司 | 口服考来烯胺制剂及其用途 |
RU2750937C2 (ru) * | 2016-02-09 | 2021-07-06 | Альбирео Аб | Пероральный состав холестирамина и его применение |
EP3613414A1 (de) | 2018-08-24 | 2020-02-26 | Dr. Falk Pharma Gmbh | Pellets mit mehrschichtiger struktur zur verzögerten freisetzung des wirkstoffs im distalen kolon |
US11896719B2 (en) | 2022-01-24 | 2024-02-13 | Calliditas Therapeutics Ab | Pharmaceutical compositions |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3996356A (en) | 1969-07-02 | 1976-12-07 | Hoffmann-La Roche Inc. | Composition containing 5-sulfanilamido-3,4-dimethylisoxazole and a trimethoxybenzyl pyrimidine |
SE378109B (sr) | 1972-05-19 | 1975-08-18 | Bofors Ab | |
SE7813246L (sv) | 1978-12-22 | 1980-06-23 | Haessle Ab | Fast farmaceutisk beredning innehallande kroppar med flera ytskikt |
FR2471186A1 (fr) | 1979-12-10 | 1981-06-19 | Roussel Uclaf | Nouveaux comprimes a delitescence colique, ainsi que leur procede de preparation |
SE8003805L (sv) | 1980-05-21 | 1981-11-22 | Haessle Ab | En farmaceutisk beredning med forbettrade utlosningsegenskap |
SE8008524L (sv) | 1980-12-04 | 1982-06-05 | Draco Ab | 4-pregnen-derivat, ett forfarande for deras framstellning, beredning och metod for behandling av inflammatoriska tillstand |
ZA825384B (en) | 1981-07-31 | 1983-05-25 | Tillott J B Ltd | Orally administrable pharmaceutical compositions |
SE8306370D0 (sv) | 1983-11-18 | 1983-11-18 | Draco Ab | Novel androstane-17beta-carboxylic acid esters, a process and intermediates for their preparation, compositions and method for the treatment of inflammatory conditions |
US4708867A (en) | 1983-12-19 | 1987-11-24 | Key Pharmaceuticals, Inc. | Minipellets |
US4606940A (en) | 1984-12-21 | 1986-08-19 | The Ohio State University Research Foundation | Small particle formation and encapsulation |
DE3536267A1 (de) | 1985-10-11 | 1987-04-16 | Bayer Ag | Azofarbstoffe sowie fluessigkristallines material enthaltend azofarbstoffe |
SE8506015D0 (sv) | 1985-12-19 | 1985-12-19 | Draco Ab | Novel 16,17-acetalsubstituted pregnane 21-oic acid derivatives |
GB8630913D0 (en) * | 1986-12-24 | 1987-02-04 | Glaxo Group Ltd | Pharmaceutical compositions |
US4966770A (en) | 1989-07-26 | 1990-10-30 | Himedics, Inc. | Prednisone microencapsulated granules |
DE10307386A1 (de) | 2003-02-21 | 2004-09-09 | Dieter Wildfang Gmbh | Verfahren zum außenseitigen Beschichten eines sanitären Auslaufteiles sowie sanitäres Auslaufteil |
-
1989
- 1989-11-22 SE SE8903914A patent/SE8903914D0/xx unknown
-
1990
- 1990-10-24 NZ NZ235807A patent/NZ235807A/xx unknown
- 1990-11-01 ZA ZA908777A patent/ZA908777B/xx unknown
- 1990-11-07 SA SA90110123A patent/SA90110123B1/ar unknown
- 1990-11-07 TW TW079109396A patent/TW250435B/zh active
- 1990-11-13 SI SI9012150A patent/SI9012150A/sl unknown
- 1990-11-13 YU YU215090A patent/YU48583B/sh unknown
- 1990-11-15 DK DK91900414.3T patent/DK0502092T3/da active
- 1990-11-15 CA CA002071518A patent/CA2071518C/en not_active Expired - Lifetime
- 1990-11-15 HU HU9201700A patent/HU216836B/hu unknown
- 1990-11-15 RU SU5052239A patent/RU2134104C1/ru active
- 1990-11-15 HU HU9201700A patent/HUT60630A/hu unknown
- 1990-11-15 AT AT91900414T patent/ATE125445T1/de not_active IP Right Cessation
- 1990-11-15 KR KR1019920701202A patent/KR0179042B1/ko not_active IP Right Cessation
- 1990-11-15 EP EP91900414A patent/EP0502092B1/en not_active Revoked
- 1990-11-15 JP JP50070991A patent/JP3145111B2/ja not_active Expired - Lifetime
- 1990-11-15 WO PCT/SE1990/000738 patent/WO1991007172A1/en not_active Application Discontinuation
- 1990-11-15 SG SG1996004385A patent/SG54210A1/en unknown
- 1990-11-15 AU AU77864/91A patent/AU643021B2/en not_active Expired
- 1990-11-15 US US09/159,301 patent/US6423340B1/en not_active Expired - Fee Related
- 1990-11-15 DE DE69021214T patent/DE69021214T2/de not_active Revoked
- 1990-11-15 ES ES91900414T patent/ES2074698T3/es not_active Expired - Lifetime
- 1990-11-15 UA UA94051483A patent/UA37196C2/uk unknown
- 1990-11-20 IL IL9641590A patent/IL96415A/en active IP Right Review Request
- 1990-11-20 PL PL90287844A patent/PL166506B1/pl unknown
- 1990-11-20 IE IE417090A patent/IE74854B1/en not_active IP Right Cessation
- 1990-11-20 EG EG69190A patent/EG19642A/xx active
- 1990-11-21 IS IS3644A patent/IS1858B/is unknown
- 1990-11-21 MY MYPI90002053A patent/MY104535A/en unknown
- 1990-11-21 PT PT95946A patent/PT95946A/pt not_active Application Discontinuation
-
1992
- 1992-05-21 NO NO922004A patent/NO304010B1/no not_active IP Right Cessation
- 1992-05-21 FI FI922325A patent/FI104949B/fi active
- 1992-09-30 HR HRP-2150/90A patent/HRP920632B1/xx not_active IP Right Cessation
-
1993
- 1993-08-10 LV LVP-93-1026A patent/LV10183B/en unknown
- 1993-12-31 LT LTIP1751A patent/LT3696B/lt not_active IP Right Cessation
-
1995
- 1995-10-11 GR GR950402797T patent/GR3017691T3/el unknown
-
1997
- 1997-04-24 HK HK51897A patent/HK51897A/xx not_active IP Right Cessation
-
1999
- 1999-09-06 FI FI991893A patent/FI19991893A/fi unknown
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MK1K | Patent expired |