WO2000072827A3 - Porous drug matrices and methods of manufacture thereof - Google Patents

Porous drug matrices and methods of manufacture thereof Download PDF

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Publication number
WO2000072827A3
WO2000072827A3 PCT/US2000/014578 US0014578W WO0072827A3 WO 2000072827 A3 WO2000072827 A3 WO 2000072827A3 US 0014578 W US0014578 W US 0014578W WO 0072827 A3 WO0072827 A3 WO 0072827A3
Authority
WO
WIPO (PCT)
Prior art keywords
drug
porous matrix
forming agent
pore forming
volatile
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/US2000/014578
Other languages
French (fr)
Other versions
WO2000072827A9 (en
WO2000072827A2 (en
Inventor
Julie Straub
Howard Bernstein
Donald E Chickering Iii
Sarwat Khatak
Greg Randall
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
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27495210&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2000072827(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US09/433,486 external-priority patent/US6395300B1/en
Priority to EP00939365A priority Critical patent/EP1180020B2/en
Priority to CA002371836A priority patent/CA2371836C/en
Priority to IL14665900A priority patent/IL146659A0/en
Priority to BR0010984-3A priority patent/BR0010984A/en
Priority to HK03101310.8A priority patent/HK1048956B/en
Priority to DE60024811T priority patent/DE60024811T3/en
Priority to NZ516083A priority patent/NZ516083A/en
Application filed by Acusphere Inc filed Critical Acusphere Inc
Priority to DK00939365T priority patent/DK1180020T4/en
Priority to AU54459/00A priority patent/AU768022B2/en
Priority to MXPA01012106A priority patent/MXPA01012106A/en
Priority to AT00939365T priority patent/ATE312601T1/en
Priority to JP2000620939A priority patent/JP4722295B2/en
Publication of WO2000072827A2 publication Critical patent/WO2000072827A2/en
Publication of WO2000072827A3 publication Critical patent/WO2000072827A3/en
Priority to US09/798,824 priority patent/US6610317B2/en
Priority to IL146659A priority patent/IL146659A/en
Priority to NO20015753A priority patent/NO323761B1/en
Anticipated expiration legal-status Critical
Publication of WO2000072827A9 publication Critical patent/WO2000072827A9/en
Priority to US11/213,257 priority patent/USRE40493E1/en
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/1682Processes
    • A61K9/1688Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
    • 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
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient

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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)
  • Epoxy Compounds (AREA)

Abstract

Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solutions, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral admisnistration. Paclitaxel or docetaxel can be provided in a porous matrix form, which allows the drug to be formulated without solubilizing agents and administered as a bolus. rocessed using standard techniques into tablets or capsules for oral administration. Paclitaxel or docetaxel can be provided in a porous matrix form, which allows the drug to be formulated without solubilizing agents and administered as a bolus.
PCT/US2000/014578 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof Ceased WO2000072827A2 (en)

Priority Applications (16)

Application Number Priority Date Filing Date Title
AU54459/00A AU768022B2 (en) 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof
AT00939365T ATE312601T1 (en) 1999-05-27 2000-05-25 POROUS MEDICINAL MATRICES AND THEIR PRODUCTION PROCESS
MXPA01012106A MXPA01012106A (en) 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof.
IL14665900A IL146659A0 (en) 1999-05-27 2000-05-25 Porous drug matrices and method of manufacture thereof
BR0010984-3A BR0010984A (en) 1999-05-27 2000-05-25 Porous drug matrices and processes for their manufacture
HK03101310.8A HK1048956B (en) 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof
DE60024811T DE60024811T3 (en) 1999-05-27 2000-05-25 POROUS DRUG MATERIALS AND THEIR MANUFACTURING METHOD
NZ516083A NZ516083A (en) 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof
CA002371836A CA2371836C (en) 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof
DK00939365T DK1180020T4 (en) 1999-05-27 2000-05-25 Porous drug matrices and processes for their preparation
JP2000620939A JP4722295B2 (en) 1999-05-27 2000-05-25 Porous drug matrix and method for producing the same
EP00939365A EP1180020B2 (en) 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof
US09/798,824 US6610317B2 (en) 1999-05-27 2001-03-02 Porous paclitaxel matrices and methods of manufacture thereof
IL146659A IL146659A (en) 1999-05-27 2001-11-21 Methods for preparing a porous matrix of drug
NO20015753A NO323761B1 (en) 1999-05-27 2001-11-26 Process for the preparation of a porous matrix of drug and pharmaceutical composition comprising it.
US11/213,257 USRE40493E1 (en) 1999-05-27 2005-08-26 Porous paclitaxel matrices and methods of manufacture thereof

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US13632399P 1999-05-27 1999-05-27
US60/136,323 1999-05-27
US15865999P 1999-10-08 1999-10-08
US60/158,659 1999-10-08
US09/433,486 1999-11-04
US09/433,486 US6395300B1 (en) 1999-05-27 1999-11-04 Porous drug matrices and methods of manufacture thereof
US18631000P 2000-03-02 2000-03-02
US60/186,310 2000-03-02

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US09/798,824 Continuation US6610317B2 (en) 1999-05-27 2001-03-02 Porous paclitaxel matrices and methods of manufacture thereof

Publications (3)

Publication Number Publication Date
WO2000072827A2 WO2000072827A2 (en) 2000-12-07
WO2000072827A3 true WO2000072827A3 (en) 2001-01-25
WO2000072827A9 WO2000072827A9 (en) 2002-01-31

Family

ID=27495210

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/014578 Ceased WO2000072827A2 (en) 1999-05-27 2000-05-25 Porous drug matrices and methods of manufacture thereof

Country Status (18)

Country Link
EP (1) EP1180020B2 (en)
JP (1) JP4722295B2 (en)
KR (2) KR100883477B1 (en)
CN (1) CN1240373C (en)
AT (1) ATE312601T1 (en)
AU (1) AU768022B2 (en)
BR (1) BR0010984A (en)
CA (1) CA2371836C (en)
DE (1) DE60024811T3 (en)
DK (1) DK1180020T4 (en)
ES (1) ES2250141T5 (en)
HK (1) HK1048956B (en)
IL (2) IL146659A0 (en)
MX (1) MXPA01012106A (en)
NO (1) NO323761B1 (en)
NZ (1) NZ516083A (en)
TW (1) TWI274589B (en)
WO (1) WO2000072827A2 (en)

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US7306812B2 (en) 2003-05-09 2007-12-11 Cephalon, Inc. Dissolvable backing layer for use with a transmucosal delivery device
US7879358B2 (en) 2002-03-20 2011-02-01 Alkermes, Inc. Pulmonary delivery for levodopa
US8852623B2 (en) 2003-03-31 2014-10-07 Titan Pharmaceuticals, Inc. Implantable polymeric device for sustained release of dopamine agonist

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US7879358B2 (en) 2002-03-20 2011-02-01 Alkermes, Inc. Pulmonary delivery for levodopa
USRE43711E1 (en) 2002-03-20 2012-10-02 Civitas Therapeutics, Inc. Pulmonary delivery for levodopa
US8852623B2 (en) 2003-03-31 2014-10-07 Titan Pharmaceuticals, Inc. Implantable polymeric device for sustained release of dopamine agonist
US9278163B2 (en) 2003-03-31 2016-03-08 Titan Pharmaceuticals, Inc. Implantable polymeric device for sustained release of dopamine agonist
US7276246B2 (en) 2003-05-09 2007-10-02 Cephalon, Inc. Dissolvable backing layer for use with a transmucosal delivery device
US7306812B2 (en) 2003-05-09 2007-12-11 Cephalon, Inc. Dissolvable backing layer for use with a transmucosal delivery device

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DK1180020T4 (en) 2009-10-05
DE60024811T2 (en) 2006-09-14
EP1180020B2 (en) 2009-06-24
IL146659A0 (en) 2002-07-25
ES2250141T3 (en) 2006-04-16
NO323761B1 (en) 2007-07-02
NO20015753L (en) 2002-01-28
NZ516083A (en) 2003-08-29
IL146659A (en) 2010-05-31
KR100752000B1 (en) 2007-08-28
CA2371836C (en) 2006-01-31
JP4722295B2 (en) 2011-07-13
DE60024811T3 (en) 2010-01-07
AU5445900A (en) 2000-12-18
DE60024811D1 (en) 2006-01-19
KR100883477B1 (en) 2009-02-16
BR0010984A (en) 2002-04-30
WO2000072827A9 (en) 2002-01-31
HK1048956A1 (en) 2003-04-25
CN1240373C (en) 2006-02-08
CA2371836A1 (en) 2000-12-07
ATE312601T1 (en) 2005-12-15
EP1180020B1 (en) 2005-12-14
TWI274589B (en) 2007-03-01
KR20020011992A (en) 2002-02-09
CN1365274A (en) 2002-08-21
HK1094775A1 (en) 2007-04-13
EP1180020A2 (en) 2002-02-20
WO2000072827A2 (en) 2000-12-07
AU768022B2 (en) 2003-11-27
ES2250141T5 (en) 2009-11-05
JP2003500438A (en) 2003-01-07
NO20015753D0 (en) 2001-11-26
KR20070069219A (en) 2007-07-02
DK1180020T3 (en) 2006-03-27
HK1048956B (en) 2006-07-28
MXPA01012106A (en) 2003-06-30

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