DK1532985T3 - Fremgangsmåde til fremstilling af en sammensætning med langvarig frigivelse - Google Patents

Fremgangsmåde til fremstilling af en sammensætning med langvarig frigivelse Download PDF

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Publication number
DK1532985T3
DK1532985T3 DK03760937.7T DK03760937T DK1532985T3 DK 1532985 T3 DK1532985 T3 DK 1532985T3 DK 03760937 T DK03760937 T DK 03760937T DK 1532985 T3 DK1532985 T3 DK 1532985T3
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DK
Denmark
Prior art keywords
lactic acid
polymer
leuprorelin
acid
acid polymer
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DK03760937.7T
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English (en)
Inventor
Kazumichi Yamamoto
Kazuhiro Saito
Tetsuo Hoshino
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Takeda Pharmaceuticals Co
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Publication of DK1532985T3 publication Critical patent/DK1532985T3/da

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/02—Peptides of undefined number of amino acids; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (14)

1. Fremgangsmåde til fremstilling afen mikrokugle- eller en mikrokapselsammensæt-ning med langvaring frigivelse, som omfatter at blande og at emulgere en vandig opløsning indeholdende leuprorelin og eddikesyre i en molær mængde af 1,65 til 3 gange den af leu-prorelin med en opløsning af en mælkesyre-glycolsyrepolymer i dichlormethan og derefter tørre den fremkomne vand-i-olie-emulsion.
2. Fremgangsmåde ifølge krav 1, hvor den vandige opløsning er tilvejebragt ved anvendelse af et salt af leuprorelin med eddikesyre.
3. Fremgangsmåde ifølge krav 1, hvor andelen af leuprorelin i sammensætningen med langvarig frigivelse er 0,001 til 50 vægt%.
4. Fremgangsmåde ifølge krav 1, hvor molforholdet af mælkesyre til glycolsyre i mæl-kesyre-glycolsyrepolymeren er 100:0 til 50:50.
5. Fremgangsmåde ifølge krav 4, hvor molforholdet af mælkesyre til glycolsyre i mæl-kesyre-glycolsyrepolymeren er 100:0.
6. Fremgangsmåde ifølge krav 1, hvor den gennemsnitlige molekylvægt af mæl kesyre-glycolsyrepolymeren er 5.000 til 50.000.
7. Fremgangsmåde ifølge krav 1, hvor den gennemsnitlige molekylvægt af mælkesyre-glycolsyrepolymeren er 17.000 til 30.000.
8. Fremgangsmåde ifølge krav 1, hvor mælkesyre-glycolsyrepolymeren er en mælkesyrepolymer, der har en gennemsnitlig molekylvægt på 15.000 til 50.000 og indholdet afen polymer, der har en gennemsnitlig molekylvægt på 5.000 eller mindre i mælkesyrepolymeren, er 5 vægt% eller mindre.
9. Fremgangsmåde ifølge krav 1, hvor mælkesyre-glycolsyrepolymeren er en mælkesyrepolymer, der har 20 til 1.000 pmol af terminal carboxylsyregruppe per masseenhed (gram) af polymeren.
10. Fremgangsmåde ifølge krav 1, hvor partikelstørrelsen af vand-i-olie-emulsionen er 0,1 til 300 pm.
11. Fremgangsmåde ifølge krav 1, hvor tørringen af vand-i-olie-emulsionen ertørring-i-vand.
12. Fremgangsmåde ifølge krav 11, hvor en vandig opløsning af et osmotisk trykreguleringsmiddel valgt blandt aminosyrer, glycerin, arabitol, xylitol, adonitol, mannitol, sorbitol og dulcitol anvendes som en ydre vandig fase i nævnte tørring-i-vand.
13. Fremgangsmåde ifølge krav 12, hvor det osmotisk trykreguleringsmiddel er mannitol.
14. Anvendelse af en vandig opløsning indeholdende leuprorelin og eddikesyre i en molær mængde af 1,65 til 3 gange den af leuprorelin med en opløsning af en mælkesyre-glycolsyrepolymer i dichlormethan til fremstilling af en mikrokugle- eller mikrokapselsam-mensætning med langvarig frigivelse indeholdende leuprorelin.
DK03760937.7T 2002-06-25 2003-06-24 Fremgangsmåde til fremstilling af en sammensætning med langvarig frigivelse DK1532985T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002185352 2002-06-25
PCT/JP2003/007950 WO2004000363A1 (ja) 2002-06-25 2003-06-24 徐放性組成物の製造方法

Publications (1)

Publication Number Publication Date
DK1532985T3 true DK1532985T3 (da) 2016-12-05

Family

ID=29996733

Family Applications (1)

Application Number Title Priority Date Filing Date
DK03760937.7T DK1532985T3 (da) 2002-06-25 2003-06-24 Fremgangsmåde til fremstilling af en sammensætning med langvarig frigivelse

Country Status (10)

Country Link
US (1) US8088726B2 (da)
EP (1) EP1532985B1 (da)
KR (2) KR101041767B1 (da)
CN (1) CN1662260B (da)
AU (1) AU2003244157A1 (da)
CA (1) CA2490351C (da)
DK (1) DK1532985T3 (da)
ES (1) ES2605402T3 (da)
PT (1) PT1532985T (da)
WO (1) WO2004000363A1 (da)

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Also Published As

Publication number Publication date
KR20110050744A (ko) 2011-05-16
CA2490351C (en) 2011-11-01
PT1532985T (pt) 2017-01-20
CN1662260B (zh) 2010-04-28
CA2490351A1 (en) 2003-12-31
EP1532985B1 (en) 2016-10-12
CN1662260A (zh) 2005-08-31
ES2605402T3 (es) 2017-03-14
KR20050023334A (ko) 2005-03-09
EP1532985A4 (en) 2008-04-16
AU2003244157A1 (en) 2004-01-06
WO2004000363A1 (ja) 2003-12-31
US20050214330A1 (en) 2005-09-29
KR101041767B1 (ko) 2011-06-17
US8088726B2 (en) 2012-01-03
KR101139112B1 (ko) 2012-04-30
EP1532985A1 (en) 2005-05-25

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