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1. WO2000040259 - PROLONGED RELEASE MICROSPHERE ENCAPSULATING LUTEINIZING HORMONE-RELEASING HORMONE ANALOGUES AND METHOD FOR PREPARING THE SAME

Publication Number WO/2000/040259
Publication Date 13.07.2000
International Application No. PCT/KR1999/000071
International Filing Date 11.02.1999
Chapter 2 Demand Filed 17.01.2000
IPC
A61K 9/16 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders
16Agglomerates; Granulates; Microbeadlets
CPC
A61K 38/22
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
A61K 9/1617
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
16Agglomerates; Granulates; Microbeadlets ; ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
1605Excipients; Inactive ingredients
1617Organic compounds, e.g. phospholipids, fats
A61K 9/1647
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
16Agglomerates; Granulates; Microbeadlets ; ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
1605Excipients; Inactive ingredients
1629Organic macromolecular compounds
1641obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
1647Polyesters, e.g. poly(lactide-co-glycolide)
A61K 9/1682
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
16Agglomerates; Granulates; Microbeadlets ; ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
1682Processes
A61P 13/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
08of the prostate
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
Applicants
  • DONG KOOK PHARMACEUTICAL CO., LTD. [KR/KR]; 997-8, Taechi-dong Kangnam-ku Seoul, KR (AllExceptUS)
  • BAEK, Myoung, Ki [KR/KR]; KR (UsOnly)
  • PARK, Jin, Kyu [KR/KR]; KR (UsOnly)
  • PARK, Mork, Soon [KR/KR]; KR (UsOnly)
  • PARK, Tae, Kwan [KR/KR]; KR (UsOnly)
  • CHOI, Seung, Ho [KR/KR]; KR (UsOnly)
Inventors
  • BAEK, Myoung, Ki; KR
  • PARK, Jin, Kyu; KR
  • PARK, Mork, Soon; KR
  • PARK, Tae, Kwan; KR
  • CHOI, Seung, Ho; KR
Agents
  • HWANG, E-Nam ; Yegun Building 3rd floor 823-42, Yoksam-dong Kangnam-ku Seoul 135-080, KR
Priority Data
1998/6214230.12.1998KR
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROLONGED RELEASE MICROSPHERE ENCAPSULATING LUTEINIZING HORMONE-RELEASING HORMONE ANALOGUES AND METHOD FOR PREPARING THE SAME
(FR) MICROSPHERE A LIBERATION PROLONGEE UTILISEE POUR ENCAPSULER DES ANALOGUES DE LA LUTEOLIBERINE, ET SON PROCEDE DE PRODUCTION
Abstract
(EN)
There is disclosed a prolonged release microsphere which can constantly release medicinal drugs, such as luteinizing hormone-releasing hormone analogues and encapsulate them at high content rates. It is prepared by dissolving a copolymer of lactide and gycolide in methylene chloride, dissolving a luteinizing hormone-releasing hormone analogue and a release-controlling material in a subsidiary solvent, combining the above two solutions with each other to produce an emulsion phase, dispersing the emulsion phase in a solution of polyvinyl alcohol in distilled water to give a single emulsion system, removing the combined solvent of the emulsion phase to generate a polymeric microsphere; freeze-drying the polymeric microsphere. The microsphere prepared has a much finer inner structure, by virtue of which the microsphere is secured in a constant release rate. The single emulsion system which simplifies the preparation, allows for the maintenance of a drug content of 10 % or more. The charged groups of the release-controlling materials associated with the polymers minimize the excess release of the oppositely charged drugs at an initial stage, playing an important role in keeping the release rate constant.
(FR)
L'invention concerne une microsphère à libération prolongée, qui peut libérer constamment des substances médicinales, telles que des analogues de la lutéolibérine et qui peut en encapsuler des quantités importantes. On produit ladite microsphère en dissolvant un copolymère de lactide et de glycolide dans du chlorure de méthylène, en dissolvant un analogue de lutéolibérine et une matière de retenue dans un solvant auxiliaire, en combinant les deux solutions sus-mentionnées, de sorte qu'une phase d'émulsion soit produite, en dispersant la phase d'émulsion dans une solution de poly(alcool de vinyle) dans de l'eau distillée, afin de produire un seul système d'émulsion, en enlevant le solvant combiné de la phase d'émulsion, de manière à générer une microsphère polymère; en lyophylisant la microsphère polymère. La microsphère de l'invention présente une structure interne beaucoup plus fine et est donc sûre en ce sa vitesse de libération est constante. Le système d'émulsion unique qui simplifie la préparation, permet le maintien d'une teneur en médicament de 10 % ou plus. Les groupes chargés des matières de retenue associées aux polymères minimisent la libération excessive de médicaments à charge opposée dans une étape initiale, ce qui est important dans le maintien d'une vitesse de libération constante.
Also published as
EP1999905340
ININ/PCT/2001/00555/MUM
TR2001/01913
US09869599
Latest bibliographic data on file with the International Bureau