KR920700682A - 글리코실화된 t-PA의 안정화방법 - Google Patents

글리코실화된 t-PA의 안정화방법

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KR920700682A
KR920700682A KR1019910700926A KR910700926A KR920700682A KR 920700682 A KR920700682 A KR 920700682A KR 1019910700926 A KR1019910700926 A KR 1019910700926A KR 910700926 A KR910700926 A KR 910700926A KR 920700682 A KR920700682 A KR 920700682A
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울리히 코너트
라이너 루돌프
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포우크베트·베버
뵈링거 만하임 게엠베하
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Abstract

내용 없음

Description

글리코실화된 t-PA 의 안정화방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (21)

  1. a) 아스코르빈산, b)DETA, c) 일반식 R1R2N-R-X의 아미노 화합물, 식중 X는 SO3H, H,NH2또는 OH,R은 C1-9-알킬렌 C3-6, 시클로알킬렌 또는 벤질리덴, R1및 R2는 서로 무관하게 H또는 C1-3알킬, d)구아니디노부티르산, e) 디메틸바이구아나이드, f) 7-아미노헵탄산, 8-아미노옥탄산,p-아미노메틸벤조산, δ-아미노발레린산, γ-아미노부티르산, g) 글루코스아민, 플럭토스, h)피리미딘 뉴클레오시드 및 피리미딘 뉴졸에오타이드, i)하이드록실, 케토 및/ 또는 또다른 카복실 그룹중 하나이상으로 치환된 카복실산, 으로 구성된 그룹으로부터 선택된 최소한 하나의 화합물과 시트레이트를 함유하는 것을 특징으로 하는 활성이 최소한 1.4MU/ml이고 pH가 4.5-9인 t-PA활성을 지닌 글리코실화된 단백질의 의약 조성물.
  2. 제1항에 있어서, 아미노 화합물이 타우린, 4-아미노부탄올-1, 5-아미노펜탄올-1,6-아미노헥산올-1,1,9-디아미노노난, 1,8-디아미노옥탄, 1,7-디아미노헵탄, 1,6-디아미노헥산, 1,5-디아미노펜탄, 1,4-디아미노부탄 또는 1,3-디아미노프로판인것을 특징으로 하는 의약 제조물.
  3. 제1항에 있어서, 하나이상의 하이드록실, 케토 및/또는 또다른 카복실 그룹으로 치환된 카복실산이 사과산, 락트산, 퓨마르산 또는 2-옥소 글루타르산인 것을 특징으로 하는 의약 제조물.
  4. 제1항에 있어서, 부가적으로 하나 이상의 아미노산을 더 함유하는 것을 특징으로 하는 의약 제조물.
  5. 전기종 항중 어느 한 항에 있어서, 시트레이트의 농도가 5-100mmole/l, 바람직하게는 mmole/l, 인것을 특징으로 하는 의약 제조물.
  6. 전기종항중 어느 한 항에 있어서, 부가적으로 염화물이온을 더 포함하는 것을 특징으로 하는 의약 제조물.
  7. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트, pH6, 0.1-1mole,바람직하게는 0.5-0.3mole의 아스코르빈산을 함유하는 것을 특징으로 하는 의약 제조물.
  8. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트, pH6, 0-200mole,바람직하게는 10-100mole의 EDTA를 함유하는 것을 특징으로 하는 의약 제조물.
  9. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트, pH6, 0.1-0.5mole,바람직하게는 0.1-0.3mole의 타우린을 함유하는 것을 특징으로 하는 의약 제조물.
  10. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트/HC1, pH6, 10-100mole의 4-아미노부탄올, 1,5-아미노펜탄올-1,6-아미노헥산올-1,1,3-디아미노프로판, 1,4-디아미노부탄, 1,5-디아미노펜탄, 1,6-디아미노헥산, 1,7-디아미노헵탄, 1,8-디아미노옥탄 또는 1,9-디아미노노난을 함유하는 것을 특징으로 하는 의약 제조물.
  11. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트/HC1, pH6, 10-200mole,바람직하게는 50-mmole의 구아니디노부티르산을 함유하는 것을 특징으로 하는 의약 제조물.
  12. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트/HC1, pH6, 50-400mole,바람직하게는 100-300mmole의 디메틸바이구아나이드를 함유하는 것을 특징으로 하는 의약 제조물.
  13. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트/HC1, pH6, 0.5-20mmole,바람직하게는 1-10mmole의 7-아미노헵탄산, 8-아미노옥탄산, δ-아미노발레린산, γ-아미노부티르산 또는 P-아미노메틸 벤조산을 함유하는 것을 특징으로 하는 의약 제조물.
  14. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트/HC1, pH6, 1-500mmole,바람직하게는 10-300mmole의 글루코스아민 또는 플릭토스를 함유하는 것을 특징으로 하는 의약 제조물.
  15. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트/HC1, pH6, 1-300mmole,바람직하게는 10-00mmole의 티미딘, 시토신 또는 유리딘을 함유하는 것을 특징으로 하는 의약 제조물.
  16. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트, pH6, 1-1000mmole,바람직하게는 10-500mmole의 사과산, 락트산, 퓨마르산 또는 2-옥소글루타르산을 함유하는 것을 특징으로 하는 의약 제조물.
  17. 제1항에 있어서, 1l당 50mmole의 나트륨 시트레이트, pH6 및 제1항의 a)-i)그룹에서부터 선택된 물질들을 합한 것을 함유하는 것을 특징으로 하는 의약 제조물.
  18. 전기한 항중 어느 한 항의 조성물과 일반적으로 사용되는 의약용 부가제, 부형제 및/또는 담체 물질로 이루어진것을 특징으로 하는. 활성물질로서 t-PA 활성을 지닌 글리코실화된 단백질을 기본으로하는 의약 제조물.
  19. t-PA활성을 지닌 글리코실화된 단백질을 제1항의 a)-i)의 최소한 한 물질과 함께 투약하기에 적당한의약 형태로 전환시키는 것을 특징으로하는 제1-8중 어느 한 항의 의약 조성물을 제조하는 방법.
  20. 제19항에 있어서, 의약의 투약형태가 주사액이나 동격건조물인 것을 특징으로 하는 방법.
  21. 제1항부터 제18항중 어느 한 항의 의약 제조물을 만드는데 사용하는 t-PA 활성을 지닌 글리코실화된 단백질의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
KR1019910700926A 1989-12-20 1990-12-19 글리코실화된 t-PA의 안정화방법 KR920700682A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DEP39421422 1989-12-20
DE3942142A DE3942142A1 (de) 1989-12-20 1989-12-20 Stabilisierung von glykosyliertem t-pa
PCT/EP1990/002252 WO1991008767A1 (de) 1989-12-20 1990-12-19 STABILISIERUNG VON GLYKOSYLIERTEM t-PA

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US (1) US5409699A (ko)
EP (1) EP0458930B1 (ko)
JP (1) JPH0660107B2 (ko)
KR (1) KR920700682A (ko)
AU (1) AU625234B2 (ko)
CA (1) CA2046876A1 (ko)
DE (2) DE3942142A1 (ko)
HU (2) HUT60132A (ko)
WO (1) WO1991008767A1 (ko)

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US5130143A (en) * 1988-11-04 1992-07-14 The Research Foundation Of State University Of New York Use of a low affinity-heparin fraction in conjunction with t-pa for thrombolytic therapy
US4980165A (en) * 1989-01-27 1990-12-25 Genetics Institute, Inc. Pharmaceutical formulations of plasminogen activator proteins

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JPH04506974A (ja) 1992-12-03
EP0458930A1 (de) 1991-12-04
AU625234B2 (en) 1992-07-02
JPH0660107B2 (ja) 1994-08-10
WO1991008767A1 (de) 1991-06-27
AU6914891A (en) 1991-07-18
HU208629B (en) 1993-12-28
HUT60132A (en) 1992-08-28
HU912739D0 (en) 1992-01-28
DE3942142A1 (de) 1991-06-27
CA2046876A1 (en) 1992-06-20
DE59003161D1 (de) 1993-11-25
EP0458930B1 (de) 1993-10-20
US5409699A (en) 1995-04-25

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