CA2110730A1 - Sustained-release preparation - Google Patents

Sustained-release preparation

Info

Publication number
CA2110730A1
CA2110730A1 CA002110730A CA2110730A CA2110730A1 CA 2110730 A1 CA2110730 A1 CA 2110730A1 CA 002110730 A CA002110730 A CA 002110730A CA 2110730 A CA2110730 A CA 2110730A CA 2110730 A1 CA2110730 A1 CA 2110730A1
Authority
CA
Canada
Prior art keywords
group
formula
sustained
release preparation
amino
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
CA002110730A
Other languages
French (fr)
Other versions
CA2110730C (en
Inventor
Shigeru Kamei
Yasutaka Igari
Yasuaki Ogawa
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.)
Takeda Pharmaceutical Co Ltd
Original Assignee
Shigeru Kamei
Yasutaka Igari
Yasuaki Ogawa
Takeda Chemical Industries, Ltd.
Takeda Pharmaceutical Company Limited
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 Shigeru Kamei, Yasutaka Igari, Yasuaki Ogawa, Takeda Chemical Industries, Ltd., Takeda Pharmaceutical Company Limited filed Critical Shigeru Kamei
Publication of CA2110730A1 publication Critical patent/CA2110730A1/en
Application granted granted Critical
Publication of CA2110730C publication Critical patent/CA2110730C/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
    • A61K9/48—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/23—Luteinising hormone-releasing hormone [LHRH]; 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
    • A61K38/04—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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

A sustained-release preparation which comprises a physiologically active peptide of general formula (SEE FORMULA I) wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula (SEE FORMULA II) wherein R3' is a heterocyclic group; R5 represents a group of the formula -( CH2)n-R5' wherein n is 2 or 3, and R5' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula -(CH2)n-R6' wherein n is 2 or 3, and R6' is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time without an initial burst.
CA002110730A 1992-12-07 1993-12-06 Sustained-release preparation Expired - Lifetime CA2110730C (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
JP32707092 1992-12-07
JP327070/1992 1992-12-07
JP1897893 1993-02-05
JP018978/1993 1993-02-05
JP14513493 1993-06-16
JP145134/1993 1993-06-16

Publications (2)

Publication Number Publication Date
CA2110730A1 true CA2110730A1 (en) 1994-06-08
CA2110730C CA2110730C (en) 2008-09-16

Family

ID=27282444

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002110730A Expired - Lifetime CA2110730C (en) 1992-12-07 1993-12-06 Sustained-release preparation

Country Status (24)

Country Link
US (7) US5480868A (en)
EP (2) EP0601799B1 (en)
JP (1) JP3725906B2 (en)
KR (2) KR100305951B1 (en)
CN (2) CN1099893C (en)
AT (2) ATE295733T1 (en)
AU (1) AU669939B2 (en)
CA (1) CA2110730C (en)
DE (2) DE69333817T2 (en)
DK (2) DK1088555T3 (en)
EE (1) EE03117B1 (en)
ES (2) ES2238247T3 (en)
FI (2) FI935471A (en)
GE (1) GEP19991600B (en)
GR (1) GR3037085T3 (en)
HK (1) HK1037519A1 (en)
LV (1) LV10927B (en)
MX (1) MX9307686A (en)
NO (1) NO310704B1 (en)
NZ (1) NZ250349A (en)
PT (2) PT601799E (en)
SG (1) SG46283A1 (en)
TW (1) TW333456B (en)
WO (1) WO1994013317A1 (en)

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