WO2011002424A3 - Solubility and stability enchancing pharmaceutical formulation comprising ezetimibe and simvastatin - Google Patents

Solubility and stability enchancing pharmaceutical formulation comprising ezetimibe and simvastatin Download PDF

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Publication number
WO2011002424A3
WO2011002424A3 PCT/TR2010/000125 TR2010000125W WO2011002424A3 WO 2011002424 A3 WO2011002424 A3 WO 2011002424A3 TR 2010000125 W TR2010000125 W TR 2010000125W WO 2011002424 A3 WO2011002424 A3 WO 2011002424A3
Authority
WO
WIPO (PCT)
Prior art keywords
ezetimibe
simvastatin
solubility
stability
enchancing
Prior art date
Application number
PCT/TR2010/000125
Other languages
French (fr)
Other versions
WO2011002424A2 (en
Inventor
Bilgic Mahmut
Original Assignee
Bilgic Mahmut
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 Bilgic Mahmut filed Critical Bilgic Mahmut
Publication of WO2011002424A2 publication Critical patent/WO2011002424A2/en
Publication of WO2011002424A3 publication Critical patent/WO2011002424A3/en

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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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Pyrane Compounds (AREA)

Abstract

The present invention relates to pharmaceutical formulations comprising a combination of a therapeutic agent with solubility problem (ezetimibe) and a therapeutic agent with stability problem (simvastatin), and the methods for the preparation thereof, and the use thereof.
PCT/TR2010/000125 2009-07-02 2010-06-25 Solubility and stability enchancing pharmaceutical formulation WO2011002424A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR2009/05147 2009-07-02
TR200905147 2009-07-02

Publications (2)

Publication Number Publication Date
WO2011002424A2 WO2011002424A2 (en) 2011-01-06
WO2011002424A3 true WO2011002424A3 (en) 2011-04-28

Family

ID=42752137

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/TR2010/000125 WO2011002424A2 (en) 2009-07-02 2010-06-25 Solubility and stability enchancing pharmaceutical formulation

Country Status (1)

Country Link
WO (1) WO2011002424A2 (en)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004010993A1 (en) * 2002-07-26 2004-02-05 Merck Sharp & Dohme Limited Composition comprising a cholesterol absorption inhibitor, an hmg-coa reductase inhibitor and a stabilizing agent
WO2006134604A1 (en) * 2005-06-15 2006-12-21 Hetero Drugs Limited Combination composition of cholesterol absorption inhibitor and 3-hydroxy-3-methylglutaryl-coenzyme a (hmg-coa) reductase inhibitor
WO2007003365A1 (en) * 2005-07-06 2007-01-11 Krka Pharmaceutical composition comprising simvastatin and ezetimibe
WO2008101723A2 (en) * 2007-02-23 2008-08-28 Krka Pharmaceutical composition containing a cholesterol absorption inhibitor
WO2010021609A1 (en) * 2008-08-22 2010-02-25 Mahmut Bilgic Solubility and stability enhancing pharmaceutical formulation
WO2010063667A2 (en) * 2008-12-01 2010-06-10 Lek Pharmaceuticals D.D. Pharmaceutical composition comprising ezetimibe and simvastatin

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
US4293496A (en) 1980-02-04 1981-10-06 Merck & Co., Inc. 6(R)-[2-(8-Hydroxy-2,6-dimethylpolyhydronaphthyl-1)-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones
AU548996B2 (en) 1980-02-04 1986-01-09 Merck & Co., Inc. Tetrahydro-2h-pyran-2-one derivatives
US4450171A (en) 1980-08-05 1984-05-22 Merck & Co., Inc. Antihypercholesterolemic compounds
US5631365A (en) 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
EP1868653A2 (en) 2005-04-12 2007-12-26 PSivida Inc. Hmgcoa reductase inhibitor codrugs and uses thereof

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004010993A1 (en) * 2002-07-26 2004-02-05 Merck Sharp & Dohme Limited Composition comprising a cholesterol absorption inhibitor, an hmg-coa reductase inhibitor and a stabilizing agent
US20040126423A1 (en) * 2002-07-26 2004-07-01 Moore William D. Pharmaceutical formulation
WO2006134604A1 (en) * 2005-06-15 2006-12-21 Hetero Drugs Limited Combination composition of cholesterol absorption inhibitor and 3-hydroxy-3-methylglutaryl-coenzyme a (hmg-coa) reductase inhibitor
WO2007003365A1 (en) * 2005-07-06 2007-01-11 Krka Pharmaceutical composition comprising simvastatin and ezetimibe
WO2008101723A2 (en) * 2007-02-23 2008-08-28 Krka Pharmaceutical composition containing a cholesterol absorption inhibitor
WO2010021609A1 (en) * 2008-08-22 2010-02-25 Mahmut Bilgic Solubility and stability enhancing pharmaceutical formulation
WO2010063667A2 (en) * 2008-12-01 2010-06-10 Lek Pharmaceuticals D.D. Pharmaceutical composition comprising ezetimibe and simvastatin

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DAVIDSON M H ET AL: "Ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia", JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY, ELSEVIER, NEW YORK, NY, US, vol. 40, no. 12, 18 December 2002 (2002-12-18), pages 2125 - 2134, XP001155704, ISSN: 0735-1097, DOI: DOI:10.1016/S0735-1097(02)02610-4 *

Also Published As

Publication number Publication date
WO2011002424A2 (en) 2011-01-06

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