CA2329875A1 - Matrices formed of polymer and hydrophobic compounds for use in drug delivery - Google Patents

Matrices formed of polymer and hydrophobic compounds for use in drug delivery Download PDF

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Publication number
CA2329875A1
CA2329875A1 CA002329875A CA2329875A CA2329875A1 CA 2329875 A1 CA2329875 A1 CA 2329875A1 CA 002329875 A CA002329875 A CA 002329875A CA 2329875 A CA2329875 A CA 2329875A CA 2329875 A1 CA2329875 A1 CA 2329875A1
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CA
Canada
Prior art keywords
drug
hydrophobic
matrix
integrated
drug delivery
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.)
Granted
Application number
CA002329875A
Other languages
French (fr)
Other versions
CA2329875C (en
Inventor
Howard Bernstein
Donald Chickering
Sarwat Khattak
Julie Straub
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.)
Acusphere Inc
Original Assignee
Acusphere, Inc.
Howard Bernstein
Donald Chickering
Sarwat Khattak
Julie Straub
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 Acusphere, Inc., Howard Bernstein, Donald Chickering, Sarwat Khattak, Julie Straub filed Critical Acusphere, Inc.
Publication of CA2329875A1 publication Critical patent/CA2329875A1/en
Application granted granted Critical
Publication of CA2329875C publication Critical patent/CA2329875C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647Polyesters, e.g. poly(lactide-co-glycolide)

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)

Abstract

A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix.
The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
CA002329875A 1998-04-30 1999-03-08 Matrices formed of polymer and hydrophobic compounds for use in drug delivery Expired - Fee Related CA2329875C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US8363698P 1998-04-30 1998-04-30
US60/083,636 1998-04-30
US09/255,179 US6423345B2 (en) 1998-04-30 1999-02-22 Matrices formed of polymer and hydrophobic compounds for use in drug delivery
US09/255,179 1999-02-22
PCT/US1999/005187 WO1999056731A1 (en) 1998-04-30 1999-03-08 Matrices formed of polymer and hydrophobic compounds for use in drug delivery

Publications (2)

Publication Number Publication Date
CA2329875A1 true CA2329875A1 (en) 1999-11-11
CA2329875C CA2329875C (en) 2003-09-16

Family

ID=26769533

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002329875A Expired - Fee Related CA2329875C (en) 1998-04-30 1999-03-08 Matrices formed of polymer and hydrophobic compounds for use in drug delivery

Country Status (19)

Country Link
US (5) US6423345B2 (en)
EP (1) EP1073422B1 (en)
JP (1) JP5153032B2 (en)
KR (1) KR100703051B1 (en)
CN (1) CN1201729C (en)
AT (1) ATE319433T1 (en)
AU (1) AU746696B2 (en)
BR (1) BR9910340A (en)
CA (1) CA2329875C (en)
DE (1) DE69930240T2 (en)
DK (1) DK1073422T3 (en)
ES (1) ES2259472T3 (en)
IL (2) IL139252A0 (en)
MX (1) MXPA00010566A (en)
NO (1) NO324895B1 (en)
NZ (1) NZ508470A (en)
PL (1) PL196159B1 (en)
PT (1) PT1073422E (en)
WO (1) WO1999056731A1 (en)

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KR20010043136A (en) 2001-05-25
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CN1201729C (en) 2005-05-18
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US6689390B2 (en) 2004-02-10
PT1073422E (en) 2006-05-31
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US6423345B2 (en) 2002-07-23
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US20010000470A1 (en) 2001-04-26
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US7052719B2 (en) 2006-05-30

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