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WO2003028645A2 - Nouvelles compositions de carvedilol - Google Patents

Nouvelles compositions de carvedilol Download PDF

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Publication number
WO2003028645A2
WO2003028645A2 PCT/US2002/031123 US0231123W WO03028645A2 WO 2003028645 A2 WO2003028645 A2 WO 2003028645A2 US 0231123 W US0231123 W US 0231123W WO 03028645 A2 WO03028645 A2 WO 03028645A2
Authority
WO
WIPO (PCT)
Prior art keywords
carvedilol
composition according
spray
pluronic
parts
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.)
Ceased
Application number
PCT/US2002/031123
Other languages
English (en)
Other versions
WO2003028645A3 (fr
Inventor
Vlassios Andronis
Choon K. Oh
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.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 SmithKline Beecham Corp filed Critical SmithKline Beecham Corp
Priority to AU2002341901A priority Critical patent/AU2002341901A1/en
Publication of WO2003028645A2 publication Critical patent/WO2003028645A2/fr
Publication of WO2003028645A3 publication Critical patent/WO2003028645A3/fr
Anticipated expiration legal-status Critical
Ceased 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin

Definitions

  • compositions of carvedilol are provided wherein carvedilol is present in a spray-dried powder.
  • the compositions are prepared using a process that involves wet bead milling and spray-drying.
  • Compositions are prepared by admixture and, thus, they are suitably adapted for oral, parenteral or pulmonary administration.
  • the compositions may be formulated in the form of tablets, capsules, reconstitutable powders or suppositories. Orally administrable formulations are preferred.
  • the chamber mill is then filled with the grinding beads and the agitator is set to run at a speed of from about 1500-2500 rpm.
  • the carvedilol suspensions are circulated through the mill and the milling process is stopped after the average particle size is from about 700-500 nm.
  • excipients are added into the milled carvedilol suspension and the resulting suspension is homogenized.
  • Spray-drying for example using Niro Mobile Minor Spray Dryer, is then carried out.
  • the carvedilol suspensions hereinbefore described are comprised of 30.0% of carvedilol and 6.0% of Pluronic F127.
  • Tablets and capsules for oral administration are usually presented in a unit dose, and contain conventional excipients such as binding agents, fillers and diluents (tableting or compression aids), lubricants, disintegrants, colorants, flavorings, and wetting agents.
  • excipients such as binding agents, fillers and diluents (tableting or compression aids), lubricants, disintegrants, colorants, flavorings, and wetting agents.
  • the tablets may be coated according to techniques well known in the art.
  • 1200 mL YTZ grinding beads 1.0 mm beads for the first in-line chamber, 0.65 mm beads for the second in-line chamber, and 0.4 mm beads for the third in-line chamber.
  • the agitators were run at a speed of 1500 rpm. Approximately 5 mL suspension was collected every 30 or 60 minutes for in-process particle size analysis. The milled carvedilol suspensions were finally collected in stainless steel containers and held at 5 °C until commencing the spray-drying process.
  • the spray drying was carried out with a Niro Mobile Minor 2000 Spray Dryer (two fluid 0.8 mm nozzle, co-current spraying, Nitrogen gas). Prior to spray drying, necessary excipients were added into the milled Carvedilol suspension and the resulting suspension was homogenized for approximately 30 minutes. Later in development, a PVP/cellulose solution was prepared, held at 5 °C overnight and then mixed with the milled carvedilol suspension prior to spray drying. The carvedilol suspension was then spray-dried. The spray-dried powder was collected using glass bottles.

Landscapes

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

Abstract

La présente invention concerne une nouvelle composition à base de carvedilol et des méthodes d'utilisation de ladite composition pour traiter l'hypertension, l'insuffisance cardiaque congestive et l'angor.
PCT/US2002/031123 2001-10-01 2002-10-01 Nouvelles compositions de carvedilol Ceased WO2003028645A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002341901A AU2002341901A1 (en) 2001-10-01 2002-10-01 Novel compositions of carvedilol

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US32636701P 2001-10-01 2001-10-01
US60/326,367 2001-10-01
US33023401P 2001-10-18 2001-10-18
US60/330,234 2001-10-18

Publications (2)

Publication Number Publication Date
WO2003028645A2 true WO2003028645A2 (fr) 2003-04-10
WO2003028645A3 WO2003028645A3 (fr) 2004-03-25

Family

ID=26985374

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/031123 Ceased WO2003028645A2 (fr) 2001-10-01 2002-10-01 Nouvelles compositions de carvedilol

Country Status (2)

Country Link
AU (1) AU2002341901A1 (fr)
WO (1) WO2003028645A2 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1661558A1 (fr) * 2004-11-30 2006-05-31 Basf Aktiengesellschaft Compositions basées sur des particules poloxamères obtenu en forme de micro goutelettes solidifiées, les méthodes de leur production
US7268156B2 (en) 2002-06-27 2007-09-11 Sb Pharmco Puerto Rico Inc. Carvedilol phosphate salts and/or solvates thereof, corresponding compositions and/or methods of treatment
WO2008068731A1 (fr) * 2006-12-06 2008-06-12 Biovail Laboratories International S.R.L. Formulations de carvedilol à libération prolongée
US7649010B2 (en) 2002-06-27 2010-01-19 SmithKline Beechman Cork Limited Carvedilol hydrobromide
US7750036B2 (en) 2003-11-25 2010-07-06 Sb Pharmco Puerto Rico Inc. Carvedilol salts, corresponding compositions, methods of delivery and/or treatment
WO2024231554A1 (fr) * 2023-05-11 2024-11-14 Catalent U.K. Swindon Zydis Limited Augmentation de la perméation pour l'absorption pré-gastrique d'ingrédients pharmaceutiques actifs

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19637082A1 (de) * 1996-09-12 1998-03-19 Boehringer Mannheim Gmbh Schnellzerfallende Pellets
US6395300B1 (en) * 1999-05-27 2002-05-28 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7268156B2 (en) 2002-06-27 2007-09-11 Sb Pharmco Puerto Rico Inc. Carvedilol phosphate salts and/or solvates thereof, corresponding compositions and/or methods of treatment
US7626041B2 (en) 2002-06-27 2009-12-01 Smithkline Beecham (Cork) Ltd Carvedilol phosphate salts and/or solvates thereof, corresponding compositions, and/or methods of treatment
US7649010B2 (en) 2002-06-27 2010-01-19 SmithKline Beechman Cork Limited Carvedilol hydrobromide
US7759384B2 (en) 2002-06-27 2010-07-20 Smithkline Beecham (Cork) Limited Carvedilol phosphate salts and/or solvates thereof, corresponding compositions, and/or methods of treatment
US7893100B2 (en) 2002-06-27 2011-02-22 Sb Pharmco Puerto Rico Inc. Carvedilol phosphate salts and/or solvates thereof, corresponding compositions, and/or methods of treatment
US7902378B2 (en) 2002-06-27 2011-03-08 Smithkline Beecham (Cork) Limited Carvedilol phosphate salts and/or solvates thereof, corresponding compositions, and/or methods of treatment
US7750036B2 (en) 2003-11-25 2010-07-06 Sb Pharmco Puerto Rico Inc. Carvedilol salts, corresponding compositions, methods of delivery and/or treatment
EP1661558A1 (fr) * 2004-11-30 2006-05-31 Basf Aktiengesellschaft Compositions basées sur des particules poloxamères obtenu en forme de micro goutelettes solidifiées, les méthodes de leur production
JP2006151980A (ja) * 2004-11-30 2006-06-15 Basf Ag 微造粒ポリマーの形成方法
WO2008068731A1 (fr) * 2006-12-06 2008-06-12 Biovail Laboratories International S.R.L. Formulations de carvedilol à libération prolongée
WO2024231554A1 (fr) * 2023-05-11 2024-11-14 Catalent U.K. Swindon Zydis Limited Augmentation de la perméation pour l'absorption pré-gastrique d'ingrédients pharmaceutiques actifs

Also Published As

Publication number Publication date
AU2002341901A1 (en) 2003-04-14
WO2003028645A3 (fr) 2004-03-25

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