WO2007120134A1 - Compositions de libération modifiées de lercanidipine - Google Patents

Compositions de libération modifiées de lercanidipine Download PDF

Info

Publication number
WO2007120134A1
WO2007120134A1 PCT/US2006/014398 US2006014398W WO2007120134A1 WO 2007120134 A1 WO2007120134 A1 WO 2007120134A1 US 2006014398 W US2006014398 W US 2006014398W WO 2007120134 A1 WO2007120134 A1 WO 2007120134A1
Authority
WO
WIPO (PCT)
Prior art keywords
lercanidipine
dosage form
modified release
pharmaceutical composition
release
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/US2006/014398
Other languages
English (en)
Inventor
Wattanaporn Abramowitz
Ram P. Kapil
Todd A. Riccobene
Mahendra G. Dedhiya
Yan Yang
Anil Chhettry
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.)
Forest Laboratories LLC
Original Assignee
Forest Laboratories LLC
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 Forest Laboratories LLC filed Critical Forest Laboratories LLC
Priority to PCT/US2006/014398 priority Critical patent/WO2007120134A1/fr
Publication of WO2007120134A1 publication Critical patent/WO2007120134A1/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
    • A61K9/48—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
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • 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
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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

Definitions

  • the amount of surfactant may be adjusted, so as to moderate the solubility, permeability and bioavailability of lercanidipine.
  • the ratio of surfactant to lercanidipine on a mass basis is from about 0.001 : 1 to about 0.2:1, more preferably from about 0.005:1 to 0.1:1 and most preferably from about 0.01:1 to about 0.075:1.
  • the acrylic polymer of the present invention is an acrylic resin lacquer used in the form of an aqueous dispersion.
  • Acrylic polymers embodied by the present invention include those commercially available under several generic and brand names. One skilled in art will recognize these polymers available from Rohm Pharma (Piscataway, NJ) under the Tradename Eudragit R ® .
  • the acrylic coating comprises a mixture of two acrylic resin lacquers, copolymer of Acrylic acid and methacrylic acid ester, commercially available from Rohm Pharma under the Tradenames, e.g., Eudragit ® RL 30 D (permeable to highly permeable) and Eudragit ® RS 30 D (poorly permeable).
  • Plasticizers may be incorporated into the outer layer in any amount sufficient to impart the modified release composition of the present invention with the desired physical properties.
  • the plasticizer is present in amounts between about 10 and about 35% and most preferably between about 15 and about 25% of the polymer weight.
  • the precise amount of plasticizer may depend upon several factors including the type of polymer and the coating conditions and in many instances may require routine experimentation to determine.
  • the lercanidipine immediate release core of the present example was prepared by loading approximately 8.18 kg sugar spheres, USP Pauler Crop, Cranbury NJ having a size of approximately 20-25 mesh into a GPCG5 fluidized bed coater. The sugar spheres were preheated for about 5 minutes between 34 and 44 0 C.

Landscapes

  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (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)
  • Medicinal Preparation (AREA)

Abstract

Cette invention a permis de découvrir qu'une composition de libération modifiée contenant l'agent de faible perméabilité et de solubilité médiocre, lercanidipine, peut être préparée, laquelle fournit des concentrations thérapeutiquement efficaces de lercanidipine dans le plasma pendant une période d'environ 20 à 25 heures. La composition de libération modifiée de la présente invention assure une libération modifiée de lercanidipine indépendante du pH et, par conséquent, assure une libération de lercanidipine même lors de l'exposition aux environnements d'utilisation de faible pH, tels que le fluide gastrique.
PCT/US2006/014398 2006-04-17 2006-04-17 Compositions de libération modifiées de lercanidipine Ceased WO2007120134A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/US2006/014398 WO2007120134A1 (fr) 2006-04-17 2006-04-17 Compositions de libération modifiées de lercanidipine

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2006/014398 WO2007120134A1 (fr) 2006-04-17 2006-04-17 Compositions de libération modifiées de lercanidipine

Publications (1)

Publication Number Publication Date
WO2007120134A1 true WO2007120134A1 (fr) 2007-10-25

Family

ID=38609796

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/014398 Ceased WO2007120134A1 (fr) 2006-04-17 2006-04-17 Compositions de libération modifiées de lercanidipine

Country Status (1)

Country Link
WO (1) WO2007120134A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050096296A1 (en) * 2003-11-03 2005-05-05 David Fikstad Pharmaceutical compositions with synchronized solubilizer release
US20060018933A1 (en) * 2002-08-05 2006-01-26 Navin Vaya Novel drug delivery system

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060018933A1 (en) * 2002-08-05 2006-01-26 Navin Vaya Novel drug delivery system
US20050096296A1 (en) * 2003-11-03 2005-05-05 David Fikstad Pharmaceutical compositions with synchronized solubilizer release

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