KR930702963A - 장질환 치료를 위한 서방성 경구 투약 형태 - Google Patents

장질환 치료를 위한 서방성 경구 투약 형태

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Publication number
KR930702963A
KR930702963A KR1019930702488A KR930702488A KR930702963A KR 930702963 A KR930702963 A KR 930702963A KR 1019930702488 A KR1019930702488 A KR 1019930702488A KR 930702488 A KR930702488 A KR 930702488A KR 930702963 A KR930702963 A KR 930702963A
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South Korea
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dosage form
granules
drug
capsule
coated
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KR1019930702488A
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English (en)
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KR100220322B1 (ko
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로데스 죤
케네쓰 에반스 브라이언
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로데스 죤
케네쓰 에반스 브라이언
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Publication of KR100220322B1 publication Critical patent/KR100220322B1/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
    • A61K9/48—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
    • 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
    • A61K9/4891—Coated capsules; Multilayered drug free capsule shells
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/65—Tetracyclines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/245—Bismuth; Compounds 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/52—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an inorganic compound, e.g. an inorganic ion that is complexed with the active ingredient
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/58—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
    • 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
    • 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
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

본 발명은 장에 약물을 선택적으로 투여하기 위한 소장에서 과립을 방출시키는 장용성 코팅 캡슐에 함유된 약물의 다수의 장용성 코팅 과립을 포함하는 경구 투여가능한 제약학적 투약 형태에 관한 것이다. 과립은 바람직하게는 코팅된 과립이 최소한 회장에 도달할때까지 무상으로 존재한 후 결장에서 약물을 지속적으로 방출시키는 코팅으로 코팅된다. 적당한 코팅물질은 (메타) 아크릴레이트 및 (메타)아크릴산 중합체의 Eudragit범위에서 선택된다. 본 발명은 특히 국소적으로 활성인스테로이드, 비스무트 염 및 복합체와 같은 국소적으로 활성인 약물, 특히 5-아미노 살리산에 적용된다.

Description

장질환 치료를 위한 서방성 경구 투약 형태
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 다양한 pH가 시간경과에 따라 약물방출에 미치는 효과를 도시한 그래프도이다.

Claims (13)

  1. 캠슐에 함유된 약물의 다수의 과립을 포함하는 장에 약물을 선택적으로 투여하기 위한 경구 투여가능한 제약적 투약 형태로, 상기 과립 및 상기 캡슐이 장에서 용해되는 동일 또는 상이한 코팅물질로 코팅되는 것을 특징으로 하는 투약 형태.
  2. 제1항에 있어서, 소장에서 과립을 방출하는 장용성 코팅 캡슐에 함유된 약물의 다수의 과립을 포함하며, 코팅된 과립이 최소한 회장에 도달할 때까지 무상으로 유지되는 코팅으로 상기 과립이 코팅되는 것을 특징으로 하는 투약 형태.
  3. 제2항에 있어서, 상기 코팅이 결장에서 약물을 지속적으로 방출시키는 것을 특징으로 하는 투약 형태.
  4. 제2항에 있어서, 상기 과립 코팅이 pH7이하의 위액 및 장액에는 불용성이지만 결장의 장액에는 녹을수 있는 음이온성 중합체로 이루어짐으로써 방출된 코팅된 과립상의 코팅이, 과립이 최소한 회장에 도달할때까지 무상으로 유지되는 것을 특징으로 하는 투약 형태.
  5. 제4항에 있어서, 상기 코팅이 결장에서 약물을 지속적으로 방출시키는 것을 특징으로 하는 투약 형태.
  6. 제1항에 있어서, 상기 약물이 5-아미노살리실 산 또는 약학적으로 허용되는 염 또는 그것의 에스테르인 것을 특징으로 하는 투약 형태.
  7. 제1항에 있어서, 상기 약물이 국소적으로 활성인 스테로이드 또는 비스무트염 또는 복합체인 것을 특징으로 하는 투약 형태.
  8. 제4항에 있어서, 음이온성 중합체가 부분적으로 메틸 에스테르화된 메타크릴산 중합체인 것을 특징으로 하는 투약 형태.
  9. 제8항에 있어서, 부분적으로 메틸 에스테르화된 메타크릴산 중합체가 약 1:2의 유리산기 대 에스테르기의 비율을 갖는 것을 특징으로 하는 투약 형태.
  10. 제1항에 있어서, 캡슐이 경질 젤라틴 캡슐인 것을 특징으로 하는 투약 형태.
  11. 제1항에 있어서, 캡슐이 음이온성 카르복실계 아크릴계 중합체로 코팅되는 것을 특징으로 하는 투약형태.
  12. 제11항에 있어서, 캡슐 코팅이 부분적으로 메틸 에스테르화된 메타크릴산 중합체인 것을 특징으로 하는 투약 형태.
  13. 제12항에 있어서, 캡슐 코팅이 약 1:1의 유리산기 대 에스테르 기비율을 가지는 부분적으로 메틸 에스테르화된 메타크릴산 중합체인 것을 특징으로 하는 투약 형태.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930702488A 1991-02-22 1992-02-21 장질환 치료를 위한 서방성 경구 투약 제형 KR100220322B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9103795A GB2253346A (en) 1991-02-22 1991-02-22 Delayed release oral dosage forms for treatment of intestinal disorders
GB9103795.2 1991-02-22
PCT/GB1992/000318 WO1992014452A1 (en) 1991-02-22 1992-02-21 Delayed release oral dosage forms for treatment of intestinal disorders

Publications (2)

Publication Number Publication Date
KR930702963A true KR930702963A (ko) 1993-11-29
KR100220322B1 KR100220322B1 (ko) 1999-09-15

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KR1019930702488A KR100220322B1 (ko) 1991-02-22 1992-02-21 장질환 치료를 위한 서방성 경구 투약 제형

Country Status (23)

Country Link
US (1) US5401512A (ko)
EP (1) EP0572486B1 (ko)
JP (1) JP2958116B2 (ko)
KR (1) KR100220322B1 (ko)
AT (1) ATE129893T1 (ko)
AU (1) AU652032B2 (ko)
CA (1) CA2104686C (ko)
CZ (1) CZ281792B6 (ko)
DE (1) DE69205971T2 (ko)
DK (1) DK0572486T3 (ko)
ES (1) ES2079183T3 (ko)
FI (1) FI105255B (ko)
GB (1) GB2253346A (ko)
GE (1) GEP19971086B (ko)
GR (1) GR3018455T3 (ko)
HU (1) HU219449B (ko)
IE (1) IE74225B1 (ko)
IL (1) IL101036A (ko)
IN (1) IN179089B (ko)
NO (1) NO307405B1 (ko)
NZ (1) NZ241687A (ko)
WO (1) WO1992014452A1 (ko)
YU (1) YU17892A (ko)

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IN179089B (ko) 1997-08-23
DE69205971D1 (de) 1995-12-14
DK0572486T3 (da) 1995-12-11
GB2253346A (en) 1992-09-09
HU9302379D0 (en) 1993-11-29
ATE129893T1 (de) 1995-11-15
GB9103795D0 (en) 1991-04-10
CZ281792B6 (cs) 1997-01-15
ES2079183T3 (es) 1996-01-01
NO932979D0 (no) 1993-08-20
EP0572486B1 (en) 1995-11-08
FI933680A0 (fi) 1993-08-20
CA2104686C (en) 2000-05-02
NZ241687A (en) 1993-09-27
JP2958116B2 (ja) 1999-10-06
GR3018455T3 (en) 1996-03-31
HUT65914A (en) 1994-07-28
EP0572486A1 (en) 1993-12-08
IL101036A (en) 1996-05-14
IE920548A1 (en) 1992-08-26
WO1992014452A1 (en) 1992-09-03
AU652032B2 (en) 1994-08-11
AU1279592A (en) 1992-09-15
KR100220322B1 (ko) 1999-09-15
CZ162693A3 (en) 1994-10-19
DE69205971T2 (de) 1996-04-11
CA2104686A1 (en) 1992-08-23
YU17892A (sh) 1994-12-28
IE74225B1 (en) 1997-07-16
JPH06505246A (ja) 1994-06-16
NO307405B1 (no) 2000-04-03
US5401512A (en) 1995-03-28
NO932979L (no) 1993-08-20
IL101036A0 (en) 1992-11-15
FI105255B (fi) 2000-07-14
GEP19971086B (en) 1997-12-02
HU219449B (hu) 2001-04-28

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