KR950032370A - 생분해성 하이드로겔 고분자 - Google Patents

생분해성 하이드로겔 고분자 Download PDF

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KR950032370A
KR950032370A KR1019940010696A KR19940010696A KR950032370A KR 950032370 A KR950032370 A KR 950032370A KR 1019940010696 A KR1019940010696 A KR 1019940010696A KR 19940010696 A KR19940010696 A KR 19940010696A KR 950032370 A KR950032370 A KR 950032370A
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polymer
peo
integer
biodegradable
polyethylene oxide
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KR1019940010696A
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KR0141431B1 (ko
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김호현
송수석
이일웅
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김상응
주식회사 삼양사
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Priority to KR1019940010696A priority Critical patent/KR0141431B1/ko
Priority to US08/268,915 priority patent/US5514380A/en
Priority to JP6168187A priority patent/JPH07309938A/ja
Publication of KR950032370A publication Critical patent/KR950032370A/ko
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    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G63/00Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
    • C08G63/66Polyesters containing oxygen in the form of ether groups
    • C08G63/664Polyesters containing oxygen in the form of ether groups derived from hydroxy carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A61K9/204Polyesters, e.g. poly(lactide-co-glycolide)
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G63/00Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
    • C08G63/02Polyesters derived from hydroxycarboxylic acids or from polycarboxylic acids and polyhydroxy compounds
    • C08G63/06Polyesters derived from hydroxycarboxylic acids or from polycarboxylic acids and polyhydroxy compounds derived from hydroxycarboxylic acids
    • C08G63/08Lactones or lactides
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G81/00Macromolecular compounds obtained by interreacting polymers in the absence of monomers, e.g. block polymers
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G2230/00Compositions for preparing biodegradable polymers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Polyesters Or Polycarbonates (AREA)
  • Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)
  • Polyethers (AREA)
  • Medicinal Preparation (AREA)

Abstract

폴리에틸렌옥사이드(PEO), 폴리락타이드(PLA), 폴리글라이 콜라이드(PGA), 폴리락타이드글리콜라이드(PLGA)등을 포함한 다중블럭 공중합체의 고분자로서, 친수성 고분자 블럭의 분자쇄내에 에스테르 결합이나 아미드 결합등을 포함하여, 체내에 사용시 단순 가수분해 또는 가수분해효소에 의해 작은 분자로 분해되어 신장을 통하여 체외로 배출되거나 체내의 대사과정에 의해 소멸될 수 있는 인체에 무해한 열가소성 생분해성 하이드로겔 합성에 관한 것이다.

Description

생분해성 하이드로겔 고분자
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기식(Ⅰ)a 내지 (Ⅰ)f로 표시되는 친수성 비분해성 고분자(A) 와 소수성생체분해성 고분자(B)를 결합시켜 합성한 생분해성 하이드로겔 고분자
    식(Ⅰ)a
    식(Ⅰ)b
    식(Ⅰ)c
    식(Ⅰ)d
    식(Ⅰ)e
    식(Ⅰ)f
    상기식에서 A(-)는 폴리에틸렌옥사이드(PEO)또는 폴리에틸렌옥사이드/폴리프로필렌옥사이드 공중합체와 같은 친수성 비분해성 고분자이고, B(…)는 폴리락타이드(PLA), 폴리글라이콜라이드(PGA), PLA/PGA공중합체, 폴리카프로락톤(PCL), 폴리오르소에스터, 폴리안하이드라이드와 같은 소수성 생체 분해성 고분자이며, X는 아미드 결합, 에스테르 결합, 카보네이트 결합과 같은 생체내에서 분해되는 화학결합이고, Y는 아미드 결합, 에스테르 결합, 카보네이트 결합과 같은 A와 B, 또는 B들을 공유결합에 의해 연결하는 화학결합이며, n은 0에서 10의 정수이며, q는 3에서 4의 정수이다.
  2. 제1항에 있어서, 2이상의 다양한 수의 소수성 고분자 사슬을 갖는 것을 특징으로 하는 생체 분해성 하이드로겔 고분자.
  3. 제1항에 있어서, 폴리에틸렌옥사이드(PEO), 폴리락타이드(PLA), 폴리글라이콜라이드(PGA) 및 폴리카프로락톤(PCL)등을 포함한 다중블럭 공중합체로 하기 구조식(Ⅰ) 또는 (Ⅰ´)을 갖는 생체 분해성 하이드로겔 고분자
    〔H-O(CH2)z-(OCHR1COOCHR2CO)m-Y-A-Y´-〔(COCHR1OC(=0)CHR2O)m-O(CH2)-H〕…(Ⅰ)
    〔H-O(CH2)z-(O(CH2)5CO)m-Y-A-Y´-〔(CO(CH2)5O)m-O(CH2)z-H〕…(Ⅰ´)
    상기식에서 A는 친수성과 소수성 고분자로 이루어진 다중블럭으로서, 〔(CH2CH2O)n-X-(OCH2CH2)nr이고, X는 -O(COCH2O)X-, -O〔COCH(CH3)O〕X-이며, Y는 -CHyNHCO-, Y´는 -CONHCHy-이고, R1및 R2는 수소원자이거나 메틸기이고, x는 1에서 10의 정수이고, z는 1에서 5의 정수이고, y는 0,1 또는 2이며, 이때 ℓ은 각각 3,2,1의 값을 가지며, m은 1에서 100의 정수이고, n은 20에서 500의 정수이고, k는 0에서 10의 정수이며, r은 0에서 10의 정수이다.
  4. 제3항에 있어서, 폴리에틸렌옥사이드(PEO)의 중량비가 5% 내지 95%의 범위를 갖는 것을 특징으로 하는 생체 분해성 하이드로겔 고분자
  5. 친수성 비분해성 고분자(A)로는 분자량 600 내지 30,000사이의 폴리에틸렌옥사이드(PEO) 또는 폴리에틸렌옥사이드/폴리프로필렌옥사이드 공중합체를 사용하고, 소수성 생체 분해성 고분자(B)블럭은 폴리락타이드(PLA), 폴리글라이콜라이드(PGA), 폴리카프로락톤(PCL) 또는 이들의 공중합체를 사용하여 친수성 고분자 블럭은 PEO 모노머를 음이온 중합기켜 합성하고, 연결부위(Y)에서 소수성 고분자 블럭과 결합시킨후, 친수성 고분자 블럭을 연속적으로 음이온 중합방법에 의해 합성시킴을 특징으로 하는 생체 분해성 하이드로겔 고분자의 제조방법.
  6. 제5항에 있어서, 친수성 비분해성 고분자(A)의 합성은 친수성 폴리에틸렌 글리콜 고분자를 이용하여 폴리에틸렌 글리콜 양말단기에 생분해가 가능한 락타이드, 글리콜라이드 및 카프로락톤등을 중합하고서 다시 에틸렌옥사이드모노머로 중합시킴을 특징으로 하는 생체 분해성 하이드로겔 고분자의 제조방법.
  7. 제5항 또는 제6항에 있어서, 폴리에틸렌옥사이(PEO)의 분자량은 2,000 내지 10,000임을 특징으로 하는 생체 분해성 하이드로겔 고분자의 제조방법.
  8. 제5항 내지 제6항에 있어서, 연결부위(Y)에서의 결합은 다중블럭 PEO를 제조한 후 여기에 트리스(히드록시알킬) 아미노메탄 또는 디히드록시알킬 아미노메탄을 결합시킴을 특징으로 하는 생체 분해성 하이드로겔 고분자의 제조방법.
  9. 제8항에 있어서, 알킬로는 탄소수가 1 내지 5인 지방족 화합물을 사용함을 특징으로 하는 생체 분해성 하이드로겔 고분자의 제조방법.
  10. 제8항에 있어서, 다중블럭 PEO제조 후 P-니트로페닐클로로포메이트(NPC)로 다중블럭 PEO 말단의 히드록실그룹을 보호시켜 결합시킴을 특징으로 하는 생체 분해서 하이드로겔 고분자의 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940010696A 1994-05-17 1994-05-17 생분해성 하이드로겔 고분자 KR0141431B1 (ko)

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Application Number Priority Date Filing Date Title
KR1019940010696A KR0141431B1 (ko) 1994-05-17 1994-05-17 생분해성 하이드로겔 고분자
US08/268,915 US5514380A (en) 1994-05-17 1994-06-30 Biodegradable hydrogel copolymer as drug delivery matrix
JP6168187A JPH07309938A (ja) 1994-05-17 1994-07-20 薬物送達マトリックス用の熱可塑性および生分解性ヒドロゲルマルチブロックコポリマー

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KR1019940010696A KR0141431B1 (ko) 1994-05-17 1994-05-17 생분해성 하이드로겔 고분자

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KR0141431B1 KR0141431B1 (ko) 1998-07-01

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