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WO2007064084A1 - Granules contenant du pranlukast et leurs procedes de preparation - Google Patents

Granules contenant du pranlukast et leurs procedes de preparation Download PDF

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Publication number
WO2007064084A1
WO2007064084A1 PCT/KR2006/004402 KR2006004402W WO2007064084A1 WO 2007064084 A1 WO2007064084 A1 WO 2007064084A1 KR 2006004402 W KR2006004402 W KR 2006004402W WO 2007064084 A1 WO2007064084 A1 WO 2007064084A1
Authority
WO
WIPO (PCT)
Prior art keywords
pranlukast
granules
surfactant
water
containing granules
Prior art date
Application number
PCT/KR2006/004402
Other languages
English (en)
Inventor
Young-Joon Park
Sei-Yeon Park
Original Assignee
Yuhan Corporation
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 Yuhan Corporation filed Critical Yuhan Corporation
Publication of WO2007064084A1 publication Critical patent/WO2007064084A1/fr

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
    • A61K9/14—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
    • 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
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • 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
    • 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
    • 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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

Definitions

  • the present invention relates to granules containing pranlukast and a process for preparing the same.
  • pranlukast is a poorly water-soluble drug having very strong adhesiveness.
  • pranlukast when formulated into tablets or capsules, it adheres to a punch, a die, and the like, making continuous production difficult.
  • a therapeutic dosage of 200 mg or more is recommended.
  • the preparation of the solid dispersion involves dissolving pranlukast and (hydroxypropyl)methyl cellulose or (hydroxypropyl)cellulose in an organic solvent (i.e., a mixed solvent of dichloromethane and methanol), and thus, problems such as the probability of environmental contamination and the potential toxicity of residual organic solvent may be caused. Furthermore, since a large amount of the organic solvent is required to completely dissolve pranlukast, drying (e.g., spray-drying) is complicated and requires a long time, which renders commercialization difficult.
  • an organic solvent i.e., a mixed solvent of dichloromethane and methanol
  • FlG. 1 illustrates the results of comparative dissolution tests for tablets made from granules of the present invention and a commercially available formulation. Best Mode for Carrying Out the Invention
  • pranlukst-containing granules comprising a granular core; and a drug coating layer which comprises pranlukast, a water-soluble polymer, and a surfactant, and is formed on the granular core.

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne des granules contenant du pranlukast qui comprennent: un noyau granulaire; et une couche d'enrobage de médicament qui comprend du pranlukast, un polymère soluble dans l'eau et un tensioactif, et qui est formée sur le noyau granulaire. L'invention concerne également le procédé de préparation de ces granules. Lesdites granules, dans lesquelles la surface du pranlukast est modifiée (ou recouverte) par un tensioactif, permettent d'améliorer l'adhésivité et la solubilité du pranlukast et augmenter sa vitesse de dissolution et sa biodisponibilité, et peuvent de ce fait être administrées selon une dose remarquablement réduite par rapport aux formulations classiques. En outre, ces granules peuvent être préparées en l'absence de solvant organique, ce qui permet une production de masse à grande échelle sans problème de toxicité dû à un solvant résiduel.
PCT/KR2006/004402 2005-10-28 2006-10-27 Granules contenant du pranlukast et leurs procedes de preparation WO2007064084A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020050102489A KR100981751B1 (ko) 2005-10-28 2005-10-28 프란루카스트를 함유하는 과립 및 그의 제조방법
KR10-2005-0102489 2005-10-28

Publications (1)

Publication Number Publication Date
WO2007064084A1 true WO2007064084A1 (fr) 2007-06-07

Family

ID=38092395

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2006/004402 WO2007064084A1 (fr) 2005-10-28 2006-10-27 Granules contenant du pranlukast et leurs procedes de preparation

Country Status (2)

Country Link
KR (1) KR100981751B1 (fr)
WO (1) WO2007064084A1 (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20120087723A (ko) * 2011-01-28 2012-08-07 제이더블유중외제약 주식회사 건조 시럽 조성물
KR102363727B1 (ko) * 2015-06-01 2022-02-16 삼아제약 주식회사 생체이용률이 개선된 프란루카스트 함유 고형 제제의 조성물 및 그 제조방법
KR20240164596A (ko) 2023-05-09 2024-11-20 삼아제약 주식회사 복약편의성이 증진된 프란루카스트 함유 약제학적 조성물
KR20250015905A (ko) 2023-07-18 2025-02-03 삼아제약 주식회사 프란루카스트 함유 약제학적 조성물의 제조방법 및 상기 제조방법에 의해 제조된 약제학적 조성물
KR20250052834A (ko) 2023-10-12 2025-04-21 주식회사 다산제약 프란루카스트의 생체이용률이 개선된 약제학적 조성물 및 그 제조방법

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5876760A (en) * 1995-06-12 1999-03-02 Ono Pharmaceutical Co., Ltd. Granules containing pranlukast, process for producing the granules, and method of improving adhesiveness of pranlukast
WO2001089574A1 (fr) * 2000-05-20 2001-11-29 Sang Deuk Lee Systeme de dispersion solide de pranlukast avec dissolution amelioree et technique de preparation de celui-ci
JP2005139085A (ja) * 2003-11-04 2005-06-02 Ono Pharmaceut Co Ltd 顆粒

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20070022712A (ko) * 2004-06-07 2007-02-27 와이어쓰 당 코팅 및 이의 방법
KR101233235B1 (ko) * 2005-08-26 2013-02-15 에스케이케미칼주식회사 초기 용출율이 개선된 프란루카스트 고체분산체의 약제학적조성물 및 그의 제조방법

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5876760A (en) * 1995-06-12 1999-03-02 Ono Pharmaceutical Co., Ltd. Granules containing pranlukast, process for producing the granules, and method of improving adhesiveness of pranlukast
WO2001089574A1 (fr) * 2000-05-20 2001-11-29 Sang Deuk Lee Systeme de dispersion solide de pranlukast avec dissolution amelioree et technique de preparation de celui-ci
JP2005139085A (ja) * 2003-11-04 2005-06-02 Ono Pharmaceut Co Ltd 顆粒

Also Published As

Publication number Publication date
KR100981751B1 (ko) 2010-09-10
KR20070045799A (ko) 2007-05-02

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