CA2382577A1 - Injectable buprenorphine microparticle compositions and their use - Google Patents

Injectable buprenorphine microparticle compositions and their use Download PDF

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Publication number
CA2382577A1
CA2382577A1 CA002382577A CA2382577A CA2382577A1 CA 2382577 A1 CA2382577 A1 CA 2382577A1 CA 002382577 A CA002382577 A CA 002382577A CA 2382577 A CA2382577 A CA 2382577A CA 2382577 A1 CA2382577 A1 CA 2382577A1
Authority
CA
Canada
Prior art keywords
partial
opioid antagonist
opioid agonist
opioid
composition
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
CA002382577A
Other languages
French (fr)
Other versions
CA2382577C (en
Inventor
Thomas R. Tice
Jay K. Staas
Teresa M. Ferrell
Peter Markland
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.)
Evonik Corp
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2382577A1 publication Critical patent/CA2382577A1/en
Application granted granted Critical
Publication of CA2382577C publication Critical patent/CA2382577C/en
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • 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
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse

Abstract

An injectable slow-release partial opioid agonist or opioid antagonist formulation is provided comprising a partial opioid agonist or opioid antagonist in a poly(D,L-lactide) excipient with a small amount of residual ethyl acetate. Upon intramuscular injection of the composition, a partial opioid agonist or opioid antagonist is released in a controlled manner over an extended period of time. The composition finds use in the treatment of heroin addicts and alcoholics to reduce consumption of the abused substances.
Of particular interest are the drugs buprenorphine, methadone and naltrexone.
CA002382577A 1999-08-27 2000-08-25 Injectable buprenorphine microparticle compositions and their use Expired - Lifetime CA2382577C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15111299P 1999-08-27 1999-08-27
US60/151,112 1999-08-27
PCT/US2000/023390 WO2001015699A1 (en) 1999-08-27 2000-08-25 Injectable buprenorphine microparticle compositions and their use

Publications (2)

Publication Number Publication Date
CA2382577A1 true CA2382577A1 (en) 2001-03-08
CA2382577C CA2382577C (en) 2008-01-22

Family

ID=22537367

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002382577A Expired - Lifetime CA2382577C (en) 1999-08-27 2000-08-25 Injectable buprenorphine microparticle compositions and their use

Country Status (24)

Country Link
US (2) US6495155B1 (en)
EP (1) EP1212061B1 (en)
JP (1) JP4913298B2 (en)
KR (1) KR100730440B1 (en)
CN (2) CN100387228C (en)
AT (1) ATE280579T1 (en)
AU (1) AU765496C (en)
BR (1) BR0013650A (en)
CA (1) CA2382577C (en)
CY (1) CY1106043T1 (en)
CZ (1) CZ2002728A3 (en)
DE (1) DE60015370T2 (en)
EA (1) EA009080B1 (en)
ES (1) ES2230154T3 (en)
HK (1) HK1046858B (en)
HU (1) HUP0203613A3 (en)
IL (2) IL148343A0 (en)
MX (1) MXPA02002105A (en)
NO (2) NO322650B1 (en)
NZ (1) NZ517997A (en)
PL (1) PL198334B1 (en)
PT (1) PT1212061E (en)
RO (1) RO121631B1 (en)
WO (1) WO2001015699A1 (en)

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US8329216B2 (en) 2001-07-06 2012-12-11 Endo Pharmaceuticals Inc. Oxymorphone controlled release formulations
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US20070141160A1 (en) * 2005-12-15 2007-06-21 Brown Laura J Method of treatment for osteoarthritis by local intra-articular injection of microparticles
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PL2341899T3 (en) 2008-09-24 2015-05-29 Evonik Roehm Gmbh Ph-dependent controlled release pharmaceutical opioid composition with resistance against the influence of ethanol
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TW201811332A (en) 2012-04-17 2018-04-01 美商普渡製藥有限合夥事業 Systems and methods for treating an opioid-induced adverse pharmacodynamic response
CN102836131A (en) * 2012-09-28 2012-12-26 山东大学 Sustained release microsphere preparation for hypodermic injection of buprenorphine and preparation method thereof
US9393211B2 (en) * 2013-03-15 2016-07-19 Oakwood Laboratories LLC High drug load buprenorphine microspheres and method of producing same
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Also Published As

Publication number Publication date
HK1046858B (en) 2005-03-24
ES2230154T3 (en) 2005-05-01
CZ2002728A3 (en) 2002-08-14
EA200200295A1 (en) 2002-08-29
US7473431B2 (en) 2009-01-06
AU765496C (en) 2005-08-25
CY1106043T1 (en) 2011-04-06
DE60015370T2 (en) 2006-03-09
NO20020924L (en) 2002-04-03
US6495155B1 (en) 2002-12-17
BR0013650A (en) 2002-05-07
HUP0203613A3 (en) 2005-01-28
EA009080B1 (en) 2007-10-26
HUP0203613A2 (en) 2003-02-28
CN1788721A (en) 2006-06-21
WO2001015699A1 (en) 2001-03-08
PL198334B1 (en) 2008-06-30
PT1212061E (en) 2005-01-31
EP1212061B1 (en) 2004-10-27
JP2003508439A (en) 2003-03-04
NO322650B1 (en) 2006-11-13
NO20020924D0 (en) 2002-02-26
CA2382577C (en) 2008-01-22
CN1382051A (en) 2002-11-27
RO121631B1 (en) 2008-01-30
KR20020053057A (en) 2002-07-04
IL148343A (en) 2008-03-20
CN1248689C (en) 2006-04-05
IL148343A0 (en) 2002-09-12
AU765496B2 (en) 2003-09-18
CN100387228C (en) 2008-05-14
PL354977A1 (en) 2004-03-22
NZ517997A (en) 2002-11-26
KR100730440B1 (en) 2007-06-19
US20030152638A1 (en) 2003-08-14
HK1046858A1 (en) 2003-01-30
JP4913298B2 (en) 2012-04-11
NO20063239L (en) 2002-04-03
EP1212061A1 (en) 2002-06-12
MXPA02002105A (en) 2003-12-11
AU7075100A (en) 2001-03-26
ATE280579T1 (en) 2004-11-15
DE60015370D1 (en) 2004-12-02

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Effective date: 20200825