KR920021134A - 저 용해도 약제로 피복된 비이드 조성물 - Google Patents

저 용해도 약제로 피복된 비이드 조성물 Download PDF

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Publication number
KR920021134A
KR920021134A KR1019920008311A KR920008311A KR920021134A KR 920021134 A KR920021134 A KR 920021134A KR 1019920008311 A KR1019920008311 A KR 1019920008311A KR 920008311 A KR920008311 A KR 920008311A KR 920021134 A KR920021134 A KR 920021134A
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South Korea
Prior art keywords
sugar
weight
beads
polyethylene glycol
polyoxyethylene
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KR1019920008311A
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English (en)
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스텟스코 그레그
챵 쿠에이-튜
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원본미기재
스터링 윈드롭 인코포레이티드
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Publication of KR920021134A publication Critical patent/KR920021134A/ko

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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
    • A61K9/14—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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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

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

Abstract

내용 없음.

Description

저 용해도 약제로 피복된 비이드 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

1중량%미만의 수용해도를 갖는 약제 약 1 내지 약 80중량%, 하이드록시프로필 셀룰로즈 및 하이드록시프로필 메틸셀룰로즈로 구성된 군으로 부터 선택된 셀룰로즈 유도체 약 1 내지 약 30중량%, 약 1,000 내지 약 8,000의 분자량을 갖는 폴리에틸렌 글리콜 및 d-α 토코페릴 폴리에틸렌 글리콜 1000 숙시네이트(여기서, 폴리에틸렌 글리콜 성분은 약 1,000의 평균 화학식량을 가짐)로 구성된 군으로부터 선택된 폴리에틸렌 글리콜 또는 그의 유도체 약 1 내지 약 30중량% 및 하기 구조식(I)의 폴리옥시에틸렌-폴리옥시프로필렌-폴리옥시에틸렌 블록 공중합체, 설포부탄디오산 1,4-비스(2-에틸헥실)에스테르 나트륨 염 및 황산 모노도데실 에스테르 나트륨염으로 구성된 군으로부터 선택된 밀랍질(waxy)고형물 약 1 내지 약 30중량%로 필수적으로 이루어진 피복 조성물 약 10 내지 약 300중량%로 피복된 당 또는 당/전분 비이드(bead) :
HO(CH2CH2O)a[CH(CH3)CH2O]b(CH2CH20)aH (I)
상기 식에서, a는 약 79이고, b는 약 28이다.
제1항에 있어서, 1중량%미만의 수용해도를 갖는 약제 약 1 내지 약80중량%, 하이드록시프로필 메틸셀룰로즈 약 1 내지 약 30중량%, 약 1,000 내지 약 8,000의 분자량을 갖는 폴리에틸렌 글리콜 약 1 내지 약 30중량% 및 하기 구조식(I)의 폴리옥시에틸렌-폴리옥시프로필렌-폴리옥시에틸렌 블록 공중합체 약 1 내지 약 30중량% 로 필수적으로 이루어진 피복 조성물 약 10 내지 약 300중량%로 피복된 당 또는 당/전분 비이드 :
HO(CH2CH2O)a[CH(CH3)CH2O]b(CH2CH20)aH (I)
상기 식에서, a는 약 79이고, b는 약 28이다.
제2항에 있어서, 상기 약제가 항안드로젠성 스테로이드인 피복된 당 또는 당/전분 비이드.
제3항에 있어서, 상기 항안드로젠성 스테로이드가 (5α, 17α)-1'-(메틸설포닐)-1' H-프레근-20-이노[3,2-c]피라졸-17-올이고 피복 조성물의 약 40 내지 약 80중량%를 차지하며, 폴리에틸렌 글리콜이 약 3350의 분자량을 가지고 있으며, 하이드로프로필 메틸설룰로주, 폴리에틸렌 글리콜 및 폴리옥시에틸렌-폴리옥시프로필렌-폴리옥시에틸렌 블록 공중합체 각각의 양이 피복 조성물의 약 5 내지 약 15중량%를 차지하는 피복된 당 또는 당/전분 비이드.
제1항에 따른 피복된 당 또는 당/전분 비이드 약 40mg 내지 약 700m으로 충진된 약학적 캡슐.
제4항에 따른 피복된 당 또는 당/전분 비이드 약 40mg 내지 약 700m으로 충진된 약학적 캡슐.
하이드록시프로필 셀룰로즈 또는 하이드록시프로필 메틸셀룰로즈, 폴리에틸렌 글리콜 또는 그의 유도체, 및 밀랍질 고형물을 이들의 혼합중량의 약3내지 약 10배의 물에 가온시키면서 용해하고, 수득된 용액에 약제를 교반하면서 현탁시키고, 수득된 현탁액으로 비이드를 피복한 다음, 수득된 피복 비이드를 건조함을 포함하는, 제1항에 따른 피복된 당 또는 당/전분 비이드의 제조방법.
하이드록시프로필 메틸셀룰로즈, 폴리에틸렌 글리콜 및 폴리옥시에틸렌-폴리옥시프로플렌-폴리옥시에틸렌 블록 공중합체를 이들의 혼합중량의 약 3 내지 약 10배의 물에 가온시키면서 용해하고, 수득된 용액에 약제를 교반하면서 현탁시키고, 수득된 현탁액으로 비이드를 피복한 다음, 수득된 피복 비이드를 건조함을 포함하는, 제2항에 따른 피복된 당 또는 당/전분 비이드의 제조방법.
하이드록시프로필 메틸셀룰로즈, 폴리에틸렌 글리콜 및 폴리옥시에틸렌-폴리옥시프로플렌-폴리옥시에틸렌 블록 공중합체를 이들의 혼합중량의 약 3 내지 약 10배의 물에 가온시키면서 용해하고, 수득된 용액에 약제를 교반하면서 현탁시키고, 수득된 현탁액으로 비이드를 피복한 다음, 수득된 피복 비이드를 건조함을 포함하는, 제3항에 따른 피복된 당 또는 당/전분 비이드의 제조방법.
하이드록시프로필 메틸셀룰로즈, 폴리에틸렌 글리콜 및 폴리옥시에틸렌-폴리옥시프로플렌-폴리옥시에틸렌 블록 공중합체를 이들의 혼합중량의 약 3 내지 약 10배의 물에 가온시키면서 용해하고, 수득된 용액에 약제를 교반하면서 현탁시키고, 수득된 현탁액으로 비이드를 피복한 다음, 수득된 피복 비이드를 건조함을 포함하는, 제4항에 따른 피복된 당 또는 당/전분 비이드의 제조방법.
※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920008311A 1991-05-16 1992-05-16 저 용해도 약제로 피복된 비이드 조성물 KR920021134A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US700968 1991-05-16
US07/700,968 US5223268A (en) 1991-05-16 1991-05-16 Low solubility drug-coated bead compositions

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KR920021134A true KR920021134A (ko) 1992-12-18

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US (2) US5223268A (ko)
EP (1) EP0514967A1 (ko)
JP (1) JPH05132417A (ko)
KR (1) KR920021134A (ko)
AU (1) AU1492092A (ko)
CA (1) CA2067314A1 (ko)
FI (1) FI922234A (ko)
HU (1) HUT62461A (ko)
IE (1) IE921568A1 (ko)
IL (1) IL101884A0 (ko)
MX (1) MX9202247A (ko)
NO (1) NO921924L (ko)
NZ (1) NZ242357A (ko)

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HUT62461A (en) 1993-05-28
US5340589A (en) 1994-08-23
HU9201623D0 (en) 1992-08-28
IE921568A1 (en) 1992-11-18
EP0514967A1 (en) 1992-11-25
CA2067314A1 (en) 1992-11-17
FI922234A0 (fi) 1992-05-15
NO921924L (no) 1992-11-17
JPH05132417A (ja) 1993-05-28
AU1492092A (en) 1992-11-19
IL101884A0 (en) 1992-12-30
NZ242357A (en) 1993-06-25
FI922234A (fi) 1992-11-17
MX9202247A (es) 1992-11-01
US5223268A (en) 1993-06-29
NO921924D0 (no) 1992-05-15

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