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KR890701093A - 아라키돈산 대사물질 관련 리포좀 제조방법 및 그 제제 - Google Patents

아라키돈산 대사물질 관련 리포좀 제조방법 및 그 제제

Info

Publication number
KR890701093A
KR890701093A KR1019890700041A KR890700041A KR890701093A KR 890701093 A KR890701093 A KR 890701093A KR 1019890700041 A KR1019890700041 A KR 1019890700041A KR 890700041 A KR890700041 A KR 890700041A KR 890701093 A KR890701093 A KR 890701093A
Authority
KR
South Korea
Prior art keywords
liposome
prostaglandin
composition
solution
liposome composition
Prior art date
Application number
KR1019890700041A
Other languages
English (en)
Other versions
KR970005171B1 (ko
Inventor
로버트 피 린크
미첼 엠 톰쇼우
로버트 엘 수디스
로버트 제어 림샥
Original Assignee
알렌부룸
디 리포조옴 캄파니, 인코포레이티드
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Application filed by 알렌부룸, 디 리포조옴 캄파니, 인코포레이티드 filed Critical 알렌부룸
Publication of KR890701093A publication Critical patent/KR890701093A/ko
Application granted granted Critical
Publication of KR970005171B1 publication Critical patent/KR970005171B1/ko

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Classifications

    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/5575—Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A61K9/1277—Preparation processes; Proliposomes
    • A61K9/1278—Post-loading, e.g. by ion or pH gradient
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S436/00—Chemistry: analytical and immunological testing
    • Y10S436/829—Liposomes, e.g. encapsulation
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T428/00—Stock material or miscellaneous articles
    • Y10T428/29—Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
    • Y10T428/2982—Particulate matter [e.g., sphere, flake, etc.]
    • Y10T428/2984—Microcapsule with fluid core [includes liposome]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

내용 없음

Description

아라키돈산 대사물질 관련 리포좀 제조방법 및 그 제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (49)

  1. 아라키돈산 대사물질, 지질 및 건조용 보호제를 함유하며 분배향상용 완충액을 함유해서 되는 리포좀 조성물.
  2. 제 1 항에 있어서, 아라키돈산 대사물질이 프로스태그랜딘인 리포좀 조성물.
  3. 제 2 항에 있어서, 프로스태그랜딘에 프로스태그랜딘 E1을 포함하는 리포좀 조성물.
  4. 제 1 항에 있어서, 리포좀에 막투과 농도 기울기가 있는 리포좀 조성물.
  5. 제 4 항에 있어서, 막투과 농도기울기가 이온 기울기인 리포좀 조성물.
  6. 제 5 항에 있어서, 이온 기울기가 pH 기울기인 리포좀 조성물.
  7. 제 1 항에 있어서, 분배향상 완충액이 건조용 보호제 용액과 시트르산 용액을 포함해서 되는 리포좀 조성물.
  8. 제 7 항에 있어서, 건조용 보호제 용액이 당류용액인 리포좀 조성물.
  9. 제 8 항에 있어서, 당류용액의 pH가 약 3.0 - 약11.0인 리포좀 조성물.
  10. 제 9 항에 있어서, 당류용액의 pH가 약 7.0인 리포좀 조성물.
  11. 제 8 항에 있어서, 시트르산 용액의 pH가 약 2.5 - 약 4.5인 리포좀 조성물.
  12. 제 8 항에 있어서, 시트르산 용액의 pH가 약 3.0인 리포좀 조성물.
  13. 제 8 항에 있어서, 용액중의 당류가 텍스트로오스, 수크로오스 또는 말토오스인 당류용액.
  14. 제13항에 있어서, 당류가 말토오스인 당류용액.
  15. 제 8 항에 있어서, 당류를 약 5% - 약 20%함유하는 당류용액.
  16. 제15항에 있어서, 당류를 약 10% - 약 12%함유하는 당류용액.
  17. 제 1 항에 있어서, 지질에 인지질을 포함하는 리포좀 조성물.
  18. 제17항에 있어서, 인지질에 포스파티딜콜린을 포함하는 리포좀 조성물.
  19. 제18항에 있어서, 포스파티딜콜린에 난 포스파티딜로콜린을 포함하는 리포좀 조성물.
  20. 제 1 항에 있어서, 리포좀의 직경이 약 10nm - 약 500nm인 리포좀 조성물.
  21. 제20항에 있어서, 리포좀의 평균직경이 150 - 200nm인 리포좀 조성물.
  22. 제20항에 있어서, 조성물을 동결건조시켜서 되는 리포좀 조성물.
  23. 제 2 항에 있어서, 리포좀내의 프로스태그랜딘의 함입율이 약 50% - 약 100%인 리포좀 조성물.
  24. 프로스테그랜딘 E1, 난 포스파티딜콜린 및 10% 말토오스를 함유하고 분배향상 완충액을 함유해서되는 리포좀 조성물.
  25. 조성물을 환자에게 정맥에 주사하는 제24항의 리포좀 조성물의 투여방법.
  26. 제24항의 리포좀 조성물과 약제학적으로 허용되는 담체나 부형제로된 약제학적 조성물.
  27. 제24항에 있어서, 지질 대 프로스태그랜딘의 약 300 : 1 - 약 800 : 1인 리포좀 조성물.
  28. 제27항에 있어서, 지질 대 프로스태그랜딘의 중량비가 약 300 : 1 - 약 800 : 1인 리포좀 조성물.
  29. 지질, 프로스태그랜딘 및 건조용 보호제 약 10% 로된 동결 건조된 리포좀 - 프로스태그랜딘 조성물.
  30. 제29항에 있어서, 건조용 보호제에 당류를 포함하는 동결건조된 조성물.
  31. 제30항에 있어서, 당류에 덱스트로오스, 수크로오스 또는 말토오스를 포함하는 동결건조된 조성물.
  32. 막투과 pH 기울기에 의해 프로스태그랜딘과 리포좀을 결합시키는 단계를 포함해서 되는 리포좀 - 프로스태그랜딘 조성물 제조방법.
  33. 제32항에 있어서, 막투과 pH 기울기를 : (a) 비교적 염기성인 수용액중에서 리포좀을 제조하고 ; (b) 위 (a)단계의 현탁액의 프로스태그랜딘을 가한다음 ; (c) 리포좀의 외부매체를 산성화하는 단계에 따라 발생시키는 제조방법.
  34. 제35항에 있어서, (a)단계의 리포좀의 크기를 축소시켜서 되는 제조방법.
  35. 제34항에 있어서, 굴곡형 통로를 가진 필터를 통해 리포좀을 여과함으로써 그 크기를 축소시키는 제조방법.
  36. 제34항에 있어서, 곧은 총로형 막필터를 통해 리포좀을 여과함으로써 그 크기를 축소시키는 제조방법.
  37. 제34항에 있어서, 균질화에 의해 리포좀의 크기를 축소시키는 제조방법.
  38. 제33항에 있어서, 리포좀을 동결건조시키는 제조방법.
  39. 제33항에 있어서, 지질 대 프로스태그랜딘의 중량비가 약 300 : 1 - 1000 : 1인 제조방법.
  40. 제39항에 있어서, 지질 대 프로스태그랜딘의 중량비가 약 300 : 1 - 800 : 1인 제조방법.
  41. 프로스태그랜딘을 함유한 건조용 보호재의 수용액과 건조된 지질필름을 혼합하는 단계로 되는 지질, 프로스태그랜딘 E1및 건조용 보호제로된 리포좀 - 프로스태그랜딘 제조방법.
  42. 제41항에 있어서, 리포좀을 동결건조시켜서 되는 제조방법.
  43. (a) 지질의 에탄올성 용액과 건조용 보호제의 비교적 염기성인 용액을 혼합하여 리포좀을 만들고 ; (b) 이 리포좀의 크기를 축소시키고 ; (c) 이 리포좀과 프로스태그랜딘 E1의 에탄올성 용액을 혼합하고 ; (d) (c)단계의 리포좀을 동결건조시키며 ; (e) 비교적 산성인 시트르산용액으로 이 리포좀을 재생시키는 단계로 되는 지질, 프로스태그랜딘 E1건조용 보호제 및 분배향상 완충액으로된 리포좀 - 프로스태그랜딘 조성물 제조방법.
  44. 제43항에 있어서, 지질이 난 포스파티딜콜린인 제조방법.
  45. 제43항에 있어서, 건조용 보호제가 당류인 제조방법.
  46. 제45항에 있어서, 당류가 덱스트로오스, 수크로오스 또는 말토오스인 제조방법.
  47. 제46항에 있어서, 당류가 말토오스인 제조방법.
  48. 제43항에 있어서, (a)단계의 리포좀의 크기를 균질화에 의해 축소시켜서 되는 제조방법.
  49. 제43항의 방법으로 제조한 리포좀을 함유하는 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890700041A 1987-05-22 1988-05-18 아라키돈산 대사물질 관련 리포좀 제조방법 및 그 제제 KR970005171B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5330587A 1987-05-22 1987-05-22
US053,305 1987-05-22
PCT/US1988/001714 WO1988009170A1 (en) 1987-05-22 1988-05-18 Prostaglandin-lipid formulations

Publications (2)

Publication Number Publication Date
KR890701093A true KR890701093A (ko) 1989-12-19
KR970005171B1 KR970005171B1 (ko) 1997-04-14

Family

ID=21983292

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019890700041A KR970005171B1 (ko) 1987-05-22 1988-05-18 아라키돈산 대사물질 관련 리포좀 제조방법 및 그 제제

Country Status (13)

Country Link
US (1) US5082664A (ko)
EP (1) EP0292403B1 (ko)
KR (1) KR970005171B1 (ko)
AT (1) ATE109982T1 (ko)
AU (1) AU617678B2 (ko)
CA (1) CA1323838C (ko)
DE (1) DE3851090T2 (ko)
ES (1) ES2058317T3 (ko)
FI (1) FI95199C (ko)
HK (1) HK1007496A1 (ko)
PT (1) PT87545B (ko)
WO (1) WO1988009170A1 (ko)
ZA (1) ZA883653B (ko)

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US5082664A (en) 1992-01-21
ZA883653B (en) 1989-03-29
FI895554A0 (fi) 1989-11-21
DE3851090T2 (de) 1995-01-12
PT87545A (pt) 1989-05-31
ES2058317T3 (es) 1994-11-01
EP0292403A3 (en) 1988-12-21
FI95199B (fi) 1995-09-29
AU617678B2 (en) 1991-12-05
CA1323838C (en) 1993-11-02
WO1988009170A1 (en) 1988-12-01
EP0292403A2 (en) 1988-11-23
DE3851090D1 (de) 1994-09-22
AU1954588A (en) 1988-12-21
FI95199C (fi) 1996-01-10

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