KR970704476A - 이중 코팅을 갖는 철-함유 나노입자 및 진단 및 치료에 있어서의 그의 용도(Ironcontaining nanoparticles with double coating and their use in diagnosis and therapy) - Google Patents

이중 코팅을 갖는 철-함유 나노입자 및 진단 및 치료에 있어서의 그의 용도(Ironcontaining nanoparticles with double coating and their use in diagnosis and therapy) Download PDF

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KR970704476A
KR970704476A KR1019970700649A KR19970700649A KR970704476A KR 970704476 A KR970704476 A KR 970704476A KR 1019970700649 A KR1019970700649 A KR 1019970700649A KR 19970700649 A KR19970700649 A KR 19970700649A KR 970704476 A KR970704476 A KR 970704476A
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iron
nanoparticle
mixture
containing core
synthetic polymer
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크레세 마이크
프페페러 테트레프
라바첵크 뤼디거
바그너 수잔네
에버트 볼프강
엘스테 볼커
셈믈러 볼프하르트
타우피츠 마티아스
가이다 요젭
헤르만 안자
유클 모니카
스비더스키 우드
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셈믈러 볼프하르트
인스티튜트 피르 디아그노스티크포르슝 게엠베하 안 데르 프라이엔 유니버시태트 베를린
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Abstract

본 발명은 모듈 구조를 갖는 철-함유 나노입자, 그의 제조방법 및 진단 및 치료 목적에 있어서 그의 용도에 관한 것이다.
본 발명에 따른 나노입자는 철-함유코어, 제1코트(합성중합체) 및 제2코트(표적 중합체), 및 임의로 약제학적 보조제, 약제 및/또는 흡착 매체/증강제로 구성됨을 특징으로 한다.

Description

이중 코팅을 갖는 철-함유 나노입자 및 진단 및 치료에 있어서의 그의 용도(lron-containing nanoparticles with double coating and their use in diagnosis and therapy)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (32)

  1. 철-함유 코어, 제1코트(합성 중합체) 및 제2코트(표적 중합체), 및 임의로 약제학적 보조제, 약제 및/또는 흡착 매체/증강제로 구성됨을 특징으로 하는 나노입자.
  2. 제1항에 있어서, 제1코트 및 철-함유 코어의 기본 구조 유니트의 유체역학적 직경이 용액중에서 100mm 보다 작으며, 철-함유 코어의 직경보다 5배 이상 크지 않음을 특징으로 하는 나노입자.
  3. 제1항 또는 2항에 있어서, 철-함유 코어가 마그네타이트 및/또는 마그헤마이트로 구성되거나, 또는 이들 두 성분중의 적어도 하나를 함유함을 특징으로 하는 나노입자.
  4. 제1항 내지 3항 중의 어느 하나에 있어서, 철-함유 코어중의 철 25중량% 이하가 다른 금속 이온으로 대체됨을 특징으로 하는 나노입자.
  5. 제4항에 있어서, 비-철 금속 이온이 상자성 또는 반자성이거나, 상자성 및 반자성 금속 이온의 혼합물임을 특징으로 하는 나노입자.
  6. 제1항 내지 5항 중의 어느 하나에 있어서, 철-함유 코어가 전자 현미경을 사용하여 측정한 것으로 30nm미만의 직경을 갖고, 최소 50개의 금속 이온을 함유하며, 입자 크기 분포가 적어도 90%의 철-함유 코어가 0.7×평균 내지 1.3×평균 범위에 있도록 되어 있음을 특징으로 하는 나노입자.
  7. 제1항 내지 6항 중의 어느 하나에 있어서, 존재하는 금속 이온의 총 합의 0.01배 내지 1배 양(w/w) 의 합성 중합체를 함유함을 특징으로 하는 나노입자.
  8. 제1항 내지 7항중의 어느 하나에 있어서, 합성 중합체가 모노머 또는 폴리머 물질, 또는 이들 물질 또는 유도체의 혼합물, 또는 기능 그룹을 갖는 유도체의 혼합물, 또는 부가적으로 치환된 유도체의 혼합물이며, 10,000Da 미만의 분자량을 가짐을 특징으로 하는 나노입자.
  9. 제1항 내지 8항 중의 어느 하나에 있어서, 합성 중합체가 덱스트란, 그의 유도체, 또는 덱스트란 및/ 또는 덱스트란 유도체의 혼합물임을 특징으로 하는 나노입자.
  10. 제8항 또는 9항에 있어서, 합성 중합체가 그의 분자내에 하나 또는 다수의 산 그룹, 또는 N,S,P또는 O원자를 함유하는 수개의 기능 그룹을 포함함을 특징으로 하는 나노입자.
  11. 제1항 내지 10항 중의 어느 하나에 있어서, 표적 및 합성 중합체가 동일하거나 상이한 물질 또는 이들 물질의 혼합물임을 특징으로 하는 나노입자.
  12. 제1항 내지 11항 중의 어느 하나에 있어서, 함유된 표적 중합체의 중량이 존재하는 금속 이온 중량의 0.5배 내지 50배 임을 특징으로 하는 나노입자.
  13. 제1항 내지 12항 중의 어느 하나에 있어서, 함유된 금속 이온 총 중량보다 작거나 또는 이와 동일한 양으로 흡착 매체/증강제를 함유함을 특징으로 하는 나노입자.
  14. 제13항에 있어서, 흡착 매체/증강제로서 펩타이드를 함유함을 특징으로 하는 나노입자.
  15. 제1항 내지 14항 중의 어느 하나에 있어서, 모든 성분의 유체역학적 직경이 그의 철-함유 코어의 직경의 10배를 넘지 않으며, 그의 기본 구조 유니트의 직경보다 최대 20%큼을 특징으로 하는 나노입자.
  16. 제1항 내지 15항 중의 어느 하나에 있어서, 어떤 시기에나 배합될 수 있는 기본 구조 유니트, 표적 중합체, 약제 및 흡착매체와 같은 개개 모듈로 구성됨을 특징으로 하는 나노입자.
  17. 제1단계에서 합성 중합체의 존재하에 염기 처리하여 철-함유 코어를 제조하고, 제2단계에서 탈착 방법에 의해 철 대 합성 중합체 비를 변화시키고, 제3단계에서 표적 중합체를 흡착시키고, 임의로 흡착 매체/증강제, 약제학적 보조제 및/또는 약제를 첨가함을 특징으로 하여, 제1항에 따르는 나노입자를 제조하는 방법.
  18. 제17항에 있어서, 철(Ⅱ) 및 철(Ⅲ) 염의 혼합물을 사용하여 철-함유 코어를 제조하고, 여기에서 2가대 3가 철의 비는 1 : 1내지 1:20임을 특징으로 하는 방법.
  19. 제17항 또는 18항에 있어서, 철(Ⅲ) 염 혼합물을 환원제와 함께 사용하여 철 -함유 코어를 제조하고, 철(Ⅱ) 대 철(Ⅲ) 비가 1;1 내지 1:20이 되도록 환원제의 양을 선택함을 특징으로 하는 방법.
  20. 제17항 내지 19항 중의 어느 하나에 있어서, 사용된 철 화합물이 무기 및 유기 염과 그의 착물의 혼합물임을 특징으로 하는 방법.
  21. 제17항 내지 20항 중의 어느 하나에 있어서, 철-함유 결정이 각각 제조된 수산화철(Ⅱ)및 수산화철(Ⅲ)용액을 혼합함으로써 제조됨을 특징으로 하는 방법.
  22. 제17항 내지 21항 중의 어느 하나에 있어서, 사용한 금속 이온의 25% 이하가 비-철 이온임을 특징으로 하는 방법.
  23. 제22항에 있어서, 비-철 금속 이온이 상자성 또는 반자성이거나, 상자성 및 반자성 금속 이온의 혼합물임을 특징으로 하는 방법.
  24. 제17항 내지 23항 중의 어느 하나에 있어서, 물질 또는 물질의 배합물이 상호 침전에 의해 생성된 결정을 분리하는 합성 중합체로서 사용되고, 반응 혼합물중의 합성 중합체의 양이 함유된 금속이온의 중량의 0.5내지 20배를 초과하지만 반응 혼합물의 50%(g/v) 를 초과하지 않음을 특징으로 하는 방법.
  25. 제17항 내지 24항 중의 어느 하나에 있어서, 0.1 내지 10N 염기를 사용하여 신속히 첨가되는 철 화합물을 침전시킴을 특징으로 하는 방법.
  26. 제25항에 있어서, 암모니아 기체 또는 염, 아민 또는 아민 유도체, 또는 휘발성 완충액을 사용하여 철화합물을 침전시킴을 특징으로 하는 방법.
  27. 제17항 내지 26항 중의 어느 하나에 있어서, 기본 구조 유니트가 0℃ 내지 120℃의 온도 범위에서 합성됨을 특징으로 하는 방법.
  28. 제17항 내지 27항 중의 어느 하나에 있어서, 철 대 합성 중합체의 비가 1:0.01 내지 1:1(w/w)임로 고정됨을 특징으로 하는 방법.
  29. 제17항 내지 28항 중의 어느 하나에 있어서, 첨가된 표적 중합체의 양이 표적 중합체에 대한 존재하는 금속 이온의 비가 1:0.5 내지 1:50이 되도록 선택됨을 특징으로 하는 방법.
  30. 제17항 내지 29항 중의 어느 하나에 있어서, 나노입자가 안정한 콜로이드상졸이거나 동결건조되고, 단순한 용매를 사용하여 용액으로 되돌아갈 수 있거나, 또는 기본 구조 유니트, 표적 성분 및 임의의 보조제가 적용 용액을 제조하는 특정 시간에 혼합되는 분리 용액 또는 동결건조물로서 사용될 수 있음을 특징으로 하는 방법.
  31. 제17항 내지 30항 중의 어느 하나에 있어서, 나노입자의 개개 모듈이 어떤 시기에나 배합될 수 있음을 특징으로 하는 방법.
  32. 진단시 조영제로서, 수술과 같은 의약 분야에서 가시화 표지 물질로서 및 활성제용 비히클 또는 치료용 활성제로서의 나노입자의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019970700649A 1994-08-04 1995-07-10 이중 코팅을 갖는 철-함유 나노입자 및 진단 및 치료에 있어서의 그의 용도 KR100278513B1 (ko)

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PCT/DE1995/000924 WO1996004017A1 (de) 1994-08-04 1995-07-10 Eisen enthaltende nanopartikel mit doppeltem coating und anwendung in der diagnostik und therapie

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