EP0768872A1 - New oral pharmaceutical formulation containing magnesium salt of omeprazole - Google Patents

New oral pharmaceutical formulation containing magnesium salt of omeprazole

Info

Publication number
EP0768872A1
EP0768872A1 EP95926067A EP95926067A EP0768872A1 EP 0768872 A1 EP0768872 A1 EP 0768872A1 EP 95926067 A EP95926067 A EP 95926067A EP 95926067 A EP95926067 A EP 95926067A EP 0768872 A1 EP0768872 A1 EP 0768872A1
Authority
EP
European Patent Office
Prior art keywords
formulation according
omeprazole
formulation
enteric
enteric coating
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.)
Withdrawn
Application number
EP95926067A
Other languages
German (de)
English (en)
French (fr)
Inventor
Siv Inga Bengtsson
Kurt Ingmar Lövgren
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.)
AstraZeneca AB
Original Assignee
Astra AB
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 Astra AB filed Critical Astra AB
Publication of EP0768872A1 publication Critical patent/EP0768872A1/en
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—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
    • 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
    • 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

Definitions

  • the present invention is related to a new pharmaceutical formulation containing a novel physical form of a magnesium salt of omeprazole, to a method for the manufacture of such a formulation, and to the use of such a formulation in medicine.
  • omeprazole From what is said about the stability properties of omeprazole, it is obvious that an oral dosage form of omeprazole must be protected from contact with the acid gastric juice and the active substance must be transferred in intact form to that part of the gastrointestinal tract where pH is near neutral and where rapid absorption of omeprazole can occur.
  • the new pharmaceutical formulation is defined in claims 1-9, a process for the manufacture of the pharmaceutical formulation according to the present invention is defined in claims 10-11, the use of the formulation in medicine is defined in claims 12-18 and a press- through blister package is stated in claim 19.
  • the powder mixture is then formulated into pellets, granules, beads or tablets by pharmaceutical procedures.
  • the pellets, granules, beads or tablets are used as core material for further processing.
  • the enteric coating layer is applied in one or more layers onto the formulated core material by coating procedures in suitable equipments such as pan coating, coating granulator or fluidized bed apparatus using solutions of polymers in water, or by using latex suspensions of said polymers or optionally using polymer solutions in suitable organic solvents.
  • suitable equipments such as pan coating, coating granulator or fluidized bed apparatus using solutions of polymers in water, or by using latex suspensions of said polymers or optionally using polymer solutions in suitable organic solvents.
  • enteric coating layer can optionally contain a pharmaceutically acceptable plasticizer for example cetanol, triacetin, citric acid es- ters such as, those known under the trade name Citroflex® (Pfizer), phthalic acid esters, dibutyl succinate, polyethylene glycol (PEG) or similar plasticizers.
  • a pharmaceutically acceptable plasticizer for example cetanol, triacetin, citric acid es- ters such as, those known under the trade name Citroflex® (Pfizer), phthalic acid esters, dibutyl succinate, polyethylene glycol (PEG) or similar plasticizers.
  • Paraffin powder 0.05 Tablets with the composition described above have been manufactured in a laboratory scale of about 20 000 tablets.
  • Amount omeprazole 40 Ingredient (mg/tabl.) ⁇
  • Magnesium omeprazole, mannitol, hydroxypropyl methylcellulose, microcrystalline cellulose and sodium starch glycolate are dry-mixed, moistened with water and wet mixed. The wet mass is dried and milled and finally mixed with anti-adherent and lubricant substances. T e milled granulate is compressed to tablets with a diameter of 7 mm. The tablets are enteric coated with a methacrylic acid copolymer film.
  • Enteric coated pellet formulation containing magnesium omeprazole being produced as described in WO95/01977.
  • Non-pareil pellets 1.5 kg Hydroxypropyl methylcellulose 0.23 kg

Landscapes

  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (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)
EP95926067A 1994-07-08 1995-07-05 New oral pharmaceutical formulation containing magnesium salt of omeprazole Withdrawn EP0768872A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE9400679 1994-07-08
WOPCT/SE94/00679 1994-07-08
PCT/SE1995/000816 WO1996001622A1 (en) 1994-07-08 1995-07-03 New oral pharmaceutical formulation containing magnesium salt of omeprazole

Publications (1)

Publication Number Publication Date
EP0768872A1 true EP0768872A1 (en) 1997-04-23

Family

ID=20393105

Family Applications (1)

Application Number Title Priority Date Filing Date
EP95926067A Withdrawn EP0768872A1 (en) 1994-07-08 1995-07-05 New oral pharmaceutical formulation containing magnesium salt of omeprazole

Country Status (15)

Country Link
EP (1) EP0768872A1 (cs)
KR (1) KR970704426A (cs)
BR (1) BR9508261A (cs)
CA (1) CA2193681A1 (cs)
CZ (1) CZ379596A3 (cs)
EE (1) EE03378B1 (cs)
FI (1) FI970058A (cs)
HU (1) HUT78132A (cs)
IS (1) IS4398A (cs)
MX (1) MX9700152A (cs)
NO (1) NO970036D0 (cs)
NZ (1) NZ289958A (cs)
PL (1) PL181265B1 (cs)
SK (1) SK166096A3 (cs)
WO (1) WO1996001622A1 (cs)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9500478D0 (sv) * 1995-02-09 1995-02-09 Astra Ab New pharmaceutical formulation and process
US5840737A (en) 1996-01-04 1998-11-24 The Curators Of The University Of Missouri Omeprazole solution and method for using same
US6489346B1 (en) 1996-01-04 2002-12-03 The Curators Of The University Of Missouri Substituted benzimidazole dosage forms and method of using same
US5900258A (en) * 1996-02-01 1999-05-04 Zeolitics Inc. Anti-bacterial compositions
SI9700186B (sl) 1997-07-14 2006-10-31 Lek, Tovarna Farmacevtskih In Kemicnih Izdelkov, D.D. Nova farmacevtska oblika z nadzorovanim sproscanjem zdravilnih ucinkovin
US6096340A (en) 1997-11-14 2000-08-01 Andrx Pharmaceuticals, Inc. Omeprazole formulation
US6174548B1 (en) 1998-08-28 2001-01-16 Andrx Pharmaceuticals, Inc. Omeprazole formulation
SE9704869D0 (sv) * 1997-12-22 1997-12-22 Astra Ab New pharmaceutical formulaton II
SE9704870D0 (sv) * 1997-12-22 1997-12-22 Astra Ab New pharmaceutical formulation I
US6733778B1 (en) 1999-08-27 2004-05-11 Andrx Pharmaceuticals, Inc. Omeprazole formulation
SE9802973D0 (sv) 1998-09-03 1998-09-03 Astra Ab Immediate release tablet
US6316020B1 (en) * 1999-08-26 2001-11-13 Robert R. Whittle Pharmaceutical formulations
EP1133987A1 (en) * 2000-03-09 2001-09-19 Ian Whitcroft Treatment of inflammatory dermatoses with combinations of erythromycin or clarythromycin, metronidazole and a hydrogen pump inhibitor
CA2413923A1 (en) * 2000-03-09 2001-09-13 Andrew Ilchyshyn Treatment of inflammatory dermatoses comprising erythromycin or clarythromycin metronidazole and a gastrointestinal hydrogen pump inhibitor
CA2771725C (en) 2002-10-16 2015-08-18 Takeda Pharmaceutical Company Limited Solid preparation comprising a non-toxic base and a proton pump inhibitor
US8993599B2 (en) 2003-07-18 2015-03-31 Santarus, Inc. Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them
US8906940B2 (en) 2004-05-25 2014-12-09 Santarus, Inc. Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them
EP1755566A2 (en) * 2004-06-15 2007-02-28 Teva Pharmaceutical Industries Ltd Stable pharmaceutical formulations of benzimidazole compounds
CN105106168B (zh) * 2015-08-19 2018-03-06 德州德药制药有限公司 一种埃索美拉唑镁肠胶囊及其制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2189698A (en) * 1986-04-30 1987-11-04 Haessle Ab Coated omeprazole tablets
JPH0768125B2 (ja) * 1988-05-18 1995-07-26 エーザイ株式会社 酸不安定化合物の内服用製剤
SE9302396D0 (sv) * 1993-07-09 1993-07-09 Ab Astra A novel compound form
SE9302395D0 (sv) * 1993-07-09 1993-07-09 Ab Astra New pharmaceutical formulation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9601622A1 *

Also Published As

Publication number Publication date
AU2994795A (en) 1996-02-09
HU9700039D0 (en) 1997-02-28
PL318464A1 (en) 1997-06-09
IS4398A (is) 1996-12-17
BR9508261A (pt) 1997-12-23
CA2193681A1 (en) 1996-01-25
CZ379596A3 (en) 1997-08-13
KR970704426A (ko) 1997-09-06
HUT78132A (hu) 2000-06-28
NZ289958A (en) 1998-09-24
FI970058A0 (fi) 1997-01-07
MX9700152A (es) 1997-04-30
FI970058A (fi) 1997-01-07
NO970036L (no) 1997-01-06
EE03378B1 (et) 2001-04-16
WO1996001622A8 (en) 1999-12-23
PL181265B1 (pl) 2001-06-29
WO1996001622A1 (en) 1996-01-25
SK166096A3 (en) 1997-09-10
EE9700014A (et) 1997-06-16
NO970036D0 (no) 1997-01-06
AU695723B2 (en) 1998-08-20

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