KR920703008A - 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 - Google Patents

수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도

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KR920703008A
KR920703008A KR1019920701734A KR920701734A KR920703008A KR 920703008 A KR920703008 A KR 920703008A KR 1019920701734 A KR1019920701734 A KR 1019920701734A KR 920701734 A KR920701734 A KR 920701734A KR 920703008 A KR920703008 A KR 920703008A
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independently
alkylene
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스텔라 발렌티노
라제우스키 로저
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더 유니버시티 오브 캔사스
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    • C08L5/00—Compositions of polysaccharides or of their derivatives not provided for in groups C08L1/00 or C08L3/00
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Abstract

내용 없음

Description

수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
[도면의 간단한 설명]
제1도는 비유도체화된 시클로덱스트린, 하이드록시프로필-유도체화된 시클로덱스트린 및 본 발명의 2가지 술포알킬 시클로 덱스트린 유도체의 경우에 쥐에서의 누적된 뇨성 시클로덱스트린 배설을 도식화한 것이다.
제2도 및 제3도는 적혈구 용혈 현상을 조사하여 측정한 것으로서, 대부분 막파괴를 야기시키는 비유도체화된 시클로덱스트린과의 일치환된 알킬술포산 유도체와 비교하여 본 비교하여 본 발명의 더욱 고도로 치환된 알킬 술폰산이 막파괴들 덜 야기시키고, 본 발명의 일치환된 알킬술폰산 유도체는 역시 적혈구 용혈현상을 조사하여 측정한 것으로서, 하이드록시 프로필 시클로덱스트린 유도체와 거의 동일한 정도의 막파괴를 야기시키는 것을 보여주는 데이타를 제공한다.
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (16)

  1. 일반식(2)의 정제된 시콜로덱스트린 유도체.
    상기 식에서, n은 4,5 또는 6이고; R1, R2, R3, R4, R5, R6, R7, R8및 R9는 각각 서로 독립적으로 O-또는 O-(C2-6알킬렌)-SO3 -,그룹이며, R1및 R2중의 적어도 하나는 독립적으로 O-(C2-6알킬렌)-SO3 -그룹이고; S1, S2, S3, S4, S5, S6, S7, S8, 및 S9는 각각 서로 독립적으로 약제학적으로 허용되는 양이온이다.
  2. 제1항에 R1,R2및 R3중의 적어도 하나는 서로 독립적으로 O-(C2-6알킬)-SO3 -그룹인 유도체.
  3. 제1항에 있어서, R1,R2및 R3중의 적어도 하나는 각각 독립적으로 O-(CH2)m-SO3 -그룹이고, 여기에서, m이 2,3,4,5 또는 6인 유도체.
  4. 제1항에 있어서, R1,R2및 R3는 각각 독립적으로 O-(CH2)m-SO3 -그룹이고, 여기에서 m이 2,3,4,5, 또는 6인 유도체.
  5. 제1항에 있어서, R4,R6및 R8중의 적어도 하나는 독립적으로 O-(C2-6-알킬렌)-SO3 -그룹이고; R5,R7및 R9는 모두 O-인 유도체.
  6. 제2항에 있어서, R4,R6및 R8중의 적어도 하나는 독립적으로 O-(C2-6-알킬렌)-SO3 -그룹이고; R5,R7및 R9는 모두 O-인 유도체.
  7. 제2항에 있어서, R4,R6및 R8중은 독립적으로 O-(C2-6-알킬렌)-SO3 -그룹이고; R5,R7및 R9는 모두 O-인 유도체.
  8. 일반식(2)의 시클로덱스트린 유도체와 복합체를 형성한 약제를 함유하며, 5 중량%를 이하의 비유도체화된 시클로덱스트린을 함유함을 특징으로 하는 조성물.
    상기식에서, n은 4,5 또는 6이고; R1, R2, R3, R4, R5, R6, R7, R8및 R9는 각각 서로 독립적으로 O-또는 O-(C2-6알킬렌)-SO3- 그룹이며, R1및 R2중의 적어도 하나는 독립적으로 O-(C2-6알킬렌)-SO3 -그룹이고; S1내지 S9는 각각 서로 독립적으로 약제학적으로 허용되는 양이온이다.
  9. 제8항에 있어서, R1,R2및 R3가 각각 독립적으로 O-(C2-6알킬렌)-SO3 -그룹인 조성물.
  10. 제8항에 있어서, R4,R6및 R8중 적어도 하나는 독립적으로 O-(C2-6-알킬렌)-SO3 -; R5,R7및 R9는 모두 O-인 조성물.
  11. 제9항에 있어서, R4,R6및 R8중 적어도 하나는 독립적으로 O-(C2-6-알킬렌)-SO3 -; R5,R7및 R9는 모두 O-인 조성물.
  12. 제11항에 있어서, R4,R6및 R8이 각각 독립적으로 O-(C2-6-알킬렌)-SO3 -그룹인 조성물.
  13. 제8항에 있어서, 약제가 이들로 제한되지는 않지만 아모바르비탈, 아스피린, 베클로메타손, 벤조카인, 벤조디아제핀, 베타메타손. 베타메타손 클로람부실, 클로람페니콜, 클로르프로마진 클로피브레이트, 조효소 A, 코티손 아세테이트, 시클로바르비탈, 덱사메타손, 덱사메타손 아세테이트, 디아제팜, 디기톡손, 디곡신, 에스트라디올, 5-플루오로우라실, 플루르비프로펜, 그리세오풀빈, 히드로코티손, 히드로코티손 아세테이트, 이부프로펜, 인도메타신, 케토프로펜, 메티실린, 메트로니다졸, 미토마이신, 니트라제팜, 니트로글리세린, 페네실린, 펜토바르비탈, 페노바르비탈, 페노바르비톤, 페니토인, 프레드니솔론, 프레드니솔론 아세테이트, 프로게스테론, 프로스타글라딘 A류, 프로스타글라딘 B류, 프로스타글라딘 E류, 프로스타글라디 F류, 레세르핀, 슬프아세트아미드 나트륨, 테스토스테론, 비타민 A, 비타민 D3, 비타민 E, 비타민 K3 및 와파린으로 이루어진 그룹으로부터 선택된 것중의 하나인 조성물.
  14. 일반식(2)의 시클로덱스트린 유도체와 복합체를, 형성한 약제를 함유하는 포접 복합체 및 약제학적으로 허용되는 담체를 함유하며, 5중량% 이하의 비유도체화된 시콜로덱스트린을 함유함을 특징으로 하는, 약제학적으로 허용되는 조성물.
    상기식에서, n은 4,5 또는 6이고; R1, R2, R3, R4, R5, R6, R7, R8및 R8는 각각 서로 독립적으로 O-또는 O-(C2-6알킬렌)-SO3 -그룹이며, R1및 R2중의 적어도 하나는 독립적으로 O-(C2-6알킬렌)-SO3-그룹이고; S1내지 S9는 각각 서로 독립적으로 약제학적으로 허용되는 양이온이다.
  15. 제14항에 있어서, 담체가 비경구 투여에 적합한 담체인 조성물.
  16. 일반식(2)의 정제된 시클로덱스트린 유도체와 복합체를 형성한 약제를 함유하는 서방성 약제학적 조성물.
    상기식에서, n은 4,5 또는 6이고; R1, R2, R3, R4, R5, R6, R7, R8및 R9는 각각 서로 독립적으로 O-또는 O-(C2-6알킬렌)-SO3 -그룹이며, R1및 R2중의 적어도 하나는 독립적으로 O-(C2-6알킬렌)-SO3-그룹이고; S1내지 S9는 각각 서로 독립적으로 약제학적으로 허용되는 양이온이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920701734A 1990-01-23 1990-01-22 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 KR0166088B1 (ko)

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US469,087 1990-01-23
US07/469,087 US5134127A (en) 1990-01-23 1990-01-23 Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
PCT/US1991/000326 WO1991011172A1 (en) 1990-01-23 1991-01-22 Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof

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KR920703008A true KR920703008A (ko) 1992-12-17
KR0166088B1 KR0166088B1 (ko) 1999-01-15

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US (1) US5134127A (ko)
EP (1) EP0512050B1 (ko)
JP (1) JP2722277B2 (ko)
KR (1) KR0166088B1 (ko)
AT (1) ATE170742T1 (ko)
AU (1) AU646020B2 (ko)
CA (1) CA2074186C (ko)
DE (1) DE69130165T2 (ko)
RU (1) RU2099354C1 (ko)
WO (1) WO1991011172A1 (ko)

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ATE170742T1 (de) 1998-09-15
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US5134127A (en) 1992-07-28
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AU7236491A (en) 1991-08-21
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