CA2424656A1 - Composition and method for stable injectable liquids - Google Patents

Composition and method for stable injectable liquids Download PDF

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Publication number
CA2424656A1
CA2424656A1 CA002424656A CA2424656A CA2424656A1 CA 2424656 A1 CA2424656 A1 CA 2424656A1 CA 002424656 A CA002424656 A CA 002424656A CA 2424656 A CA2424656 A CA 2424656A CA 2424656 A1 CA2424656 A1 CA 2424656A1
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CA
Canada
Prior art keywords
composition according
component
glass
microparticles
sugar
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
CA002424656A
Other languages
French (fr)
Other versions
CA2424656C (en
Inventor
Bruce Joseph Roser
Arcadio Garcia De Castro
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.)
NOVA BIO-PHARMA TECHNOLOGIES Ltd
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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
Priority to CA2689856A priority Critical patent/CA2689856C/en
Publication of CA2424656A1 publication Critical patent/CA2424656A1/en
Application granted granted Critical
Publication of CA2424656C publication Critical patent/CA2424656C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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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
    • A61K9/10—Dispersions; Emulsions
    • 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
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dispersion Chemistry (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

A composition for delivering a stable, bioactive compound to a subject comprising a first component and a second component, the first component comprises microparticles of sugar glass or a phosphate glass containing the bioactive agent. The sugar glass or phosphate glass optionally includes a glass formation facilitator compound, and the second component comprises at least one biocompatible liquid perfluorocarbon in which the first component is insoluble and dispersed. The liquid perfluorocarbon optionally includes a surfactant.

Claims (3)

1. A composition for delivering a stable, bioactive compound to a subject comprising a first component and a second component, said first component comprising microparticles of sugar glass, metal carboxylate glass or a phosphate glass containing said bioactive agent, wherein said sugar glass, metal carboxylate glass or phosphate glass optionally includes a glass formation facilitator compound, and said second component consisting of at least one biocompatible liquid perfluorocarbon in which said first component is insoluble and dispersed, wherein said liquid perfluorocarbon optionally includes a surfactant.
2. The composition according to claim 1, wherein said sugar glass is formed from a sugar selected from the group consisting of trehalose, sucrose, raffinose, stachyose, glucopyranosyl sorbitol, glucopyranosyl mannitol, palatinit, lactitol, a monosaccharide alcohol or sugar molecules modified by the addition of hydrophobic side chains selected from the group consisting of sucrose octaacetate or trehalose octaacetate.
3. The composition according to claim 1, wherein said phosphate glass or carboxylate glass is produced from mixtures of divalent metal phosphates or metal carboxylates.
5. The composition according to claim 1, wherein said optional glass formation facilitator is selected from the group consisting of a peptide, a protein, dextran, polyvinylpyrollidone, borate ion, calcium lactate, sodium polyphosphate, and silicate or acetate salts.
6. The composition according to claim 1, wherein said sugar glass microparticles are from about 0.1 to about 100 micrometers in diameter.
7. The composition according to claim 6, wherein said diameter range is from 1 to 10 micrometers.
8. The composition according to claim 1, wherein said microparticles have a water content of no more than 4% and preferably less than 2% and ideally less than 1 %.

9. The composition according to claim 1, wherein said first component is monodispersed in said second component.
10. The composition according to claim 1, wherein the concentration of said first component in said second component is from about 1 % to about 40% by weight.
11. The composition according to claim 10, wherein said concentration range is 10% to 15%.
12. The composition according to claim 1, wherein said surfactant concentration in said second component ranges from about 0.01 % to about 10%.
13. The composition according to claim 12, wherein said concentration is about 1 %.
14. The composition according to claim l, further comprising first component microparticles to which is added an inorganic salt in an amount effective to produce in said microparticles a density matching that of said second component liquid phase.
15. The composition according to claim 1, further comprising the incorporation into said microparticles of an excipient that confers upon said microparticles a weak residual electrostatic charge such that said microparticles repel one another.
16. The composition according to claim 15, wherein said excipient is an amino acid.
17. The composition according to claim 1 wherein said perfluorocarbon is selected from a group consisting of perfluorohexane, perfluorodecalin and perfluorophenanthrene.
18. The composition according to claim 1, wherein said bioactive compound is a vaccine, a drug, an enzyme or a diagnostic reagent.
19. A method for delivering a bioactive substance to a subject patient, comprising the steps of:
(a) producing first component microparticles according to claim 1;
(b) suspending said microparticles in said second component perfluorocarbon according to claim 1; and (c) administering said admixture to said patient.
CA2424656A 2000-10-13 2000-10-13 Composition and method for stable injectable liquids Expired - Lifetime CA2424656C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2689856A CA2689856C (en) 2000-10-13 2000-10-13 Composition and method for stable injectable liquids

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2000/028244 WO2002032402A1 (en) 2000-10-13 2000-10-13 Composition and method for stable injectable liquids

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2689856A Division CA2689856C (en) 2000-10-13 2000-10-13 Composition and method for stable injectable liquids

Publications (2)

Publication Number Publication Date
CA2424656A1 true CA2424656A1 (en) 2002-04-25
CA2424656C CA2424656C (en) 2010-03-23

Family

ID=21741883

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2424656A Expired - Lifetime CA2424656C (en) 2000-10-13 2000-10-13 Composition and method for stable injectable liquids
CA2689856A Expired - Lifetime CA2689856C (en) 2000-10-13 2000-10-13 Composition and method for stable injectable liquids

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2689856A Expired - Lifetime CA2689856C (en) 2000-10-13 2000-10-13 Composition and method for stable injectable liquids

Country Status (12)

Country Link
EP (1) EP1328255A1 (en)
JP (1) JP2004513093A (en)
KR (1) KR20030096224A (en)
CN (1) CN100339066C (en)
AU (2) AU1198601A (en)
CA (2) CA2424656C (en)
ES (1) ES2337252T3 (en)
MX (1) MXPA03003236A (en)
NO (1) NO20031706D0 (en)
PL (1) PL360052A1 (en)
PT (1) PT1452171E (en)
WO (1) WO2002032402A1 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050267222A1 (en) * 2002-10-22 2005-12-01 Dainippon Pharmaceutical Co. Ltd. Stabilized composition
JP2007001865A (en) * 2003-09-16 2007-01-11 Ltt Bio-Pharma Co Ltd Fine particle enclosing fat-soluble medicine, method for producing the same and preparation containing the same
KR20070009639A (en) 2004-04-13 2007-01-18 캠브리지 바이오스테빌리티 리미티드 Liquids containing suspended glass particles
GB0408199D0 (en) * 2004-04-13 2004-05-19 Cambridge Biostability Ltd Liquids containing suspended sugar glass particles
GB2430880A (en) * 2005-10-04 2007-04-11 Cambridge Biostability Ltd Pharmaceutical compositions stabilized in glassy particles
GB0523638D0 (en) * 2005-11-21 2005-12-28 Cambridge Biostability Ltd Pharmaceutical device for the administration of substances to patients
US8946200B2 (en) 2006-11-02 2015-02-03 Southwest Research Institute Pharmaceutically active nanosuspensions
KR101340129B1 (en) * 2008-01-18 2013-12-10 아사히 가세이 파마 가부시키가이샤 Stable pharmaceutical composition
US8404850B2 (en) 2008-03-13 2013-03-26 Southwest Research Institute Bis-quaternary pyridinium-aldoxime salts and treatment of exposure to cholinesterase inhibitors
US8722706B2 (en) 2008-08-15 2014-05-13 Southwest Research Institute Two phase bioactive formulations of bis-quaternary pyridinium oxime sulfonate salts
US8309134B2 (en) 2008-10-03 2012-11-13 Southwest Research Institute Modified calcium phosphate nanoparticle formation
WO2010146536A1 (en) 2009-06-18 2010-12-23 Koninklijke Philips Electronics N.V. Suspension of particles with drug
WO2011007327A2 (en) 2009-07-16 2011-01-20 Koninklijke Philips Electronics N.V. Suspension for therapeutic use and device for delivering said suspension
ES2362525B8 (en) 2009-10-08 2013-01-03 Azurebio, S.L. Medication formulation in the form of penetrating percutaneous needles.
US9028873B2 (en) 2010-02-08 2015-05-12 Southwest Research Institute Nanoparticles for drug delivery to the central nervous system
TWI654098B (en) 2014-03-24 2019-03-21 日商精工愛普生股份有限公司 Belt printing device and tape printing system
RU2016141948A (en) * 2014-03-27 2018-04-27 Новартис Аг SPRAY DRIED DISPERSIONS OF SOLID-IN-OIL-IN-WATER OF ACTIVE PHARMACEUTICAL INGREDIENTS FOR INHALATION

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GR78151B (en) * 1982-04-05 1984-09-26 Alcon Lab Inc
US5518731A (en) * 1990-09-27 1996-05-21 Allergan, Inc. Nonaqueous fluorinated drug delivery vehicle suspensions
WO1993018748A1 (en) * 1992-03-19 1993-09-30 Allergan, Inc. Compositions comprising a drug delivery vehicle suspended in a nonaqueous fluorinated liquid
GB9705588D0 (en) * 1997-03-18 1997-05-07 Anglia Research Foundation Stable particle in liquid formulations
US6190701B1 (en) * 1999-03-17 2001-02-20 Peter M. Ronai Composition and method for stable injectable liquids

Also Published As

Publication number Publication date
CN100339066C (en) 2007-09-26
CA2689856A1 (en) 2002-04-25
NO20031706L (en) 2003-04-11
NO20031706D0 (en) 2003-04-11
WO2002032402A1 (en) 2002-04-25
CA2689856C (en) 2013-09-24
AU2001211986B2 (en) 2007-04-26
KR20030096224A (en) 2003-12-24
CN1527699A (en) 2004-09-08
PL360052A1 (en) 2004-09-06
PT1452171E (en) 2010-03-08
MXPA03003236A (en) 2004-12-03
AU1198601A (en) 2002-04-29
CA2424656C (en) 2010-03-23
JP2004513093A (en) 2004-04-30
ES2337252T3 (en) 2010-04-22
EP1328255A1 (en) 2003-07-23

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