KR880007086A - 항암성 안트라사이클린 글리코사이드-함유 즉시-사용형 주사 용액 - Google Patents
항암성 안트라사이클린 글리코사이드-함유 즉시-사용형 주사 용액 Download PDFInfo
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- KR880007086A KR880007086A KR870013744A KR870013744A KR880007086A KR 880007086 A KR880007086 A KR 880007086A KR 870013744 A KR870013744 A KR 870013744A KR 870013744 A KR870013744 A KR 870013744A KR 880007086 A KR880007086 A KR 880007086A
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- solution
- acid
- physiologically acceptable
- doxorubicin
- anthracycline glycoside
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- 229940045799 anthracyclines and related substance Drugs 0.000 title claims 12
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- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 26
- 229960004679 doxorubicin Drugs 0.000 claims description 15
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- 150000002338 glycosides Chemical class 0.000 claims 11
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- 239000002904 solvent Substances 0.000 claims 9
- 239000003381 stabilizer Substances 0.000 claims 9
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 6
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- 238000004090 dissolution Methods 0.000 claims 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- 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
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 멸균수중 55℃에서의 독소루비신. HCI 분해에 대한 Kobs－pH 프로필(실시예 1),
제2도는 5% 댁스트로즈중 55℃에서의 독소루비신. HCI 분해에 대한 Kobs－pH 프로필(실시예 1),
제3도는 0.9%(생리적) 염수중 55℃에서의 독소루비신. HCI 분해에 대한 Kobs－pH 프로필(실시예 1),
Claims (45)
- 생리적으로 허용되는 용매중에 용해된 안트라사이클린 글리코사이드의 생리적으로 허용되는 염을 필수적으로 함유하며, 동결건조물로부터 재조제되지 않은 pH 2.5 내지 4.0의, 발열물질－비함유 보관 안정한 안트라사이클린 글리코사이드 멸균 주사 용액.
- 제1항에 있어서, 밀봉 용기내의 용액.
- 제1항 또는 2항에 있어서, 안트라사이클린 글리코사이드가 독소루비신, 4′－에피－독소루비신, 4′－데속시－독소루비신, 4′－데속시－4′－요도－독소루비신, 다우노루비신 및 4－데메톡시－디우노루비신중에서 선택된 용액.
- 제3항에 있어서, 안트라사이클린 글리코사이드가 독소루비신 또는 4′－에피－독소루비신인 용액.
- 제1항 내지 4항 중 어느 한 항에 있어서, 안트라사이클린 글리코사이드의 생리적으로 허용되는 염이 염산, 브롬화수소산, 황산, 인산, 질산, 아세트산, 숙신산, 타르타르산, 아스코르브산, 시트르산, 글루탐산, 벤조산, 메탄설폰산 및 에탄설폰산 중에서 선택된 생리적으로 허용되는 산과의 염인 용액.
- 제5항에 있어서, 안트라사이클린 글리코사이드의 생리적으로 허용되는 염이 염산과의 염인 용액.
- 제1항에 내지 6항 중 어느 한 항에 있어서, 안트라사이클린 글리코사이드에 대해 생리적으로 허용되는 용매가 물, 생리적 염수, 5% 덱스트로스 수용액, 에탄올, 폴리에틸렌글리콜, 디메틸아세트아미드 및 이의 혼합물중에서 선택된 용액.
- 제7항에 있어서, 생리적으로 허용되는 용매가 물, 생리적 염수 또는 5% 덱스트로즈 수용액인 용액.
- 제1항 내지 8항 중의 어느 한 항에 있어서, 안트라사이클린 글리코사이드의 농도가 0.1mg/ml 내지 100mg/ml인 용액.
- 제9항에 있어서, 안트라사이클린 글리코사이드의 농도가 0.1mg/ml 내지 50mg/ml인 용액.
- 제10항에 있어서, 안트라사이클린 글리코사이드의 농도가 1mg/ml 내지 20mg/ml인 용액.
- 제1항 내지 11항 중 어느 한 항에 있어서, 2.5 내지 3.7인 용액.
- 제12항에 있어서, pH 2.6 내지 3.5인 용액.
- 제1 내지 13항 중 어느 한 항에 있어서, 보조용해 안정화제, 강장 조절제, 저장 및 약제학적으로 허용되는 킬레이트화제중에서 선택된 제형보조제 하나이상을 함유하는 용액.
- 제14항에 있어서, 안정화제 및/또는 강장조절제로서 덱스트로즈, 락토즈, 소르비톨 또는 만니톨을 함유하는 용액.
- 제15항에 있어서, 약 5중량%의 덱스트로즈, 락토즈, 소르비톨 또는 만니톨을 함유하는 용액.
- 제14항에 있어서, 안정화제로서 갈락토즈, 프럭토즈, 퓨코즈, 덱스트란, α－, β－또는 γ－사이클로덱스트린, 글리세롤, 티오글리세롤, 에탄올 또는 이노시톨을 함유하는 용액.
- 제17항에 있어서, 0.25 내지 10% W/V의 안정화제를 함유하는 용액.
- 제1 내지 18항 중 어느 한 항에 있어서, pH 3인 용액.
- 제1 내지 18항 중 어느 한 항에 있어서, pH 3.0 내지 3.5인 용액.
- 생리적으로 허용되는 용매중에 용해된 독소루비신의 생리적으로 허용되는 염을 필수적으로 함유하며, 동결건조물로부터 제조제되지 않은 pH 2.5 내지 4.0의 발열 물질－비함유 보관 안정한 독소루빗?? 멸균 용액.
- 제21항에 있어서, 용기내의 용액.
- 제21항 또는 제22항에 있어서, 독소루비신의 생리적으로 허용되는 염이 염산, 브롬화 수소산, 황산, 인산, 질산, 아세트산, 숙신산, 타르타르산, 아스코르브산, 시트르산, 글루탐산, 벤조산, 메탄설폰산 및 에탄설폰산중에서 선택된 생리적으로 허용되는 산과의 염인 용액.
- 제23항에 있어서, 독소루비신의 생리적으로 허용되는 염이 염산과의 염인 용액.
- 제21항 내지 제24항 중 어느 한 항에 있어서, 독소루비신에 대해 생리적으로 허용되는 용매가 물, 생리적 염수, 5% 덱스트로즈 수용액, 에탄올, 폴리에틸렌글리콜, 디메틸아세트아미드 및 이의 혼합물중에서 선택된 용액.
- 제25항에 있어서, 생리적으로 허용되는 용매가 물, 생리적 염수 또는 5% 덱스트로즈 수용액인 용액.
- 제21항 내지 제26항 중 어느 한 항에 있어서, 독소루비신의 농도가 0.1mg/ml 내지 10mg/ml인 용액.
- 제27항에 있어서, 독소루비신의 농도가 2mg/ml 내지 50mg/ml인 용액.
- 제28항에 있어서, 독소루비신의 농도가 2mg/ml 내지 20mg/ml인 용액.
- 제29항에 있어서, 독소루비신의 농도가 2mg/ml 내지 5mg/ml인 용액.
- 제21항 내지 30항 중 어느 한 항에 있어서, pH 2.5 내지 3.7인 용액.
- 제31항에 있어서, pH 2.6 내지 3.6인 용액.
- 제21항 내지 32항 중 어느 한 항에 있어서, 보조용해제, 안정화제, 강장조절제, 저장제 및 약제학적으로 허용되는 킬레이트화제 중에서 선택된 제형보조제 하나이상을 함유하는 용액.
- 제33항에 있어서, 안정화제 및/또는 강장 조절제로서 덱스트로즈, 락토즈, 소르비톨 또는 만니톨을 함유하는 용액.
- 제34항에 있어서, 약 5중량%의 덱스트로즈, 락토즈, 소르비톨 또는 만니톨을 함유하는 용액.
- 제33항에 있어서, 안정화제로서 갈락토즈, 프럭토즈, 퓨코즈, 덱스트란, α－, β－, γ－사이클로덱스트린, 글리세롤, 티오글리세롤, 에탄올 또는 이노시톨을 함유하는 용액.
- 제36항에 있어서, 0.25 내지 10% W/V의 안정화제를 함유하는 용액.
- 제21항 내지 37항 중 어느 한 항에 있어서, pH 약 3인 용액.
- 제21항 내지 37항 중 어느 한 항에 있어서, pH 약 3.0 내지 3.5인 용액.
- (i) 동결건조물 형태가 아닌 생리적으로 허용되는 염을 생리적으로 허용되는 용매에 용해시키고 ; (ii) 임의로 보조용해제, 안정화제, 강장조절제, 저정제 및 약제학적으로 허용되는 킬레이트화제 중에서 선택된 제형 보조제를 하나이상 가하고 ; (iii) 생리적으로 허용되는 산 또는 완충제를 가하여 pH를 2.5 내지 4.0으로 조절하며, 필요한 경우, 생성된 용액이 발열물질－비함유 멸균상태이도록 하는 방법으로 상기 방법을 수행함을 특징으로 하여, 제1항 내지 39항 중 어느 한 항에 따른 발열물질－비함유 보관 안정한 주사용 멸균용액을 제조하는 방법.
- 제40항에 있어서, 용액을 단계(iii) 후에 멸균여과기를 통과시키는 방법.
- 제40항에 있어서, 사용되는 물질이 발열물질－비함유 완전멸균되는 방법.
- 제40 내지 42항 중 어느 한 항에 있어서, 보조용해제가 폴리비닐피롤리돈인 방법.
- 육종, 암, 임파종, 신경아세포종, 색소세포종, 골수종, 백혈병 및 우리름스(Wilms) 종앙중에서 선택한 종양 치료에 사용하기 위한 제1항 내지 39항 중 어느 한 항에 따른 발열물질－비함유 보관 안정한 멸균 용액.
- 제44항에 있어서, 종양이 몰로니 육종 비루스(Molony Sarcoma Virus), 육종 180복수종(Sarcoma 180 Asutes), 충실성 육종 180(Solid Sarcoma 180), 육안적 이식성 백혈병(gross transplantable leukemia), γ1210백혈병 및 임파구성 p388 백혈병(lymphocytic p388 leukemia) 중에서 선택되는 용액.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8629193 | 1986-12-05 | ||
| GB07/064653 | 1986-12-05 | ||
| GB868629193A GB8629193D0 (en) | 1986-12-05 | 1986-12-05 | Injectable ready-to-use solutions |
| US6465387A | 1987-06-22 | 1987-06-22 | |
| US07/064653 | 1987-06-22 | ||
| US8629193 | 1987-06-22 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR880007086A true KR880007086A (ko) | 1988-08-26 |
| KR960007861B1 KR960007861B1 (ko) | 1996-06-13 |
Family
ID=26291656
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019870013744A KR960007861B1 (ko) | 1986-12-05 | 1987-12-03 | 항종양성 안트라사이클린 글리코사이드-함유 즉시-사용형 주사 용액 및 이의 제조방법 |
| KR1019870013744Q KR0158672B1 (en) | 1986-12-05 | 1987-12-03 | Injectable ready-to-use solutions containing an antitumour anthracycline glycoside |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019870013744Q KR0158672B1 (en) | 1986-12-05 | 1987-12-03 | Injectable ready-to-use solutions containing an antitumour anthracycline glycoside |
Country Status (22)
| Country | Link |
|---|---|
| EP (4) | EP0438183B1 (ko) |
| JP (1) | JP2621255B2 (ko) |
| KR (2) | KR960007861B1 (ko) |
| CN (1) | CN1058391C (ko) |
| AT (2) | ATE240108T1 (ko) |
| AU (1) | AU632036B2 (ko) |
| BE (1) | BE1000540A5 (ko) |
| CH (1) | CH680494A5 (ko) |
| DE (4) | DE3741037A1 (ko) |
| DK (1) | DK175815B1 (ko) |
| ES (3) | ES2039460T3 (ko) |
| FI (1) | FI91710C (ko) |
| FR (1) | FR2607702B1 (ko) |
| GB (1) | GB2200047B (ko) |
| GR (2) | GR871846B (ko) |
| HK (3) | HK39591A (ko) |
| IT (1) | IT1226072B (ko) |
| NL (1) | NL8702914A (ko) |
| NO (1) | NO175802C (ko) |
| PT (1) | PT86285B (ko) |
| SE (1) | SE512881C2 (ko) |
| SG (1) | SG36591G (ko) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8519452D0 (en) * | 1985-08-02 | 1985-09-11 | Erba Farmitalia | Injectable solutions |
| DE10300323A1 (de) * | 2003-01-09 | 2004-10-14 | Baxter Healthcare S.A. | Sicherheitsbehälter mit erhöhter Bruch und Splitterfestigkeit sowie kontaminationsfreier Außenfläche für biologisch aktive Substanzen und Verfahren zu deren Herstellung |
| CA2446837C (en) * | 2001-05-11 | 2012-01-03 | Mitsubishi Pharma Corporation | Stable high-concentration injection containing pyrazolone derivative |
| AU2006213440A1 (en) * | 2005-02-11 | 2006-08-17 | Dabur Pharma Limited | Stabilized anthracycline glycoside pharmaceutical compositions |
| EP1814525A2 (en) * | 2005-05-11 | 2007-08-08 | Sicor Inc. | Stable lyophilized anthracycline glycosides |
| MX2010001263A (es) * | 2007-09-04 | 2010-10-04 | Meiji Seika Kaisha | Inyeccion, solucion de inyeccion y preparacion de equipo de inyeccion. |
| EP2174651A1 (en) * | 2008-10-09 | 2010-04-14 | Charité-Universitätsmedizin Berlin (Charité) | A polymer-free hydrogel |
| CN102614118B (zh) * | 2012-03-15 | 2014-04-30 | 北京协和药厂 | 注射用盐酸表柔比星制剂的制备方法及制剂 |
| CN111617030B (zh) * | 2020-05-22 | 2021-09-07 | 广东药科大学 | 壳寡糖口服液及其在制备减肥药物中的应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4177264A (en) * | 1977-10-17 | 1979-12-04 | Sri International | N-benzyl anthracyclines |
| GB2007645B (en) * | 1977-10-17 | 1982-05-12 | Stanford Res Inst Int | Benzyl anthracyclines and pharmaceutical compositions containing them |
| GB2187311B (en) * | 1984-07-27 | 1988-02-10 | Ae Plc | Automatic vehicle speed control system |
| GB8426672D0 (en) * | 1984-10-22 | 1984-11-28 | Erba Farmitalia | Pharmaceutical compositions |
| GB8519452D0 (en) * | 1985-08-02 | 1985-09-11 | Erba Farmitalia | Injectable solutions |
| JPH0655667A (ja) * | 1992-08-06 | 1994-03-01 | Nippon Zeon Co Ltd | 複合成形体 |
-
1987
- 1987-12-03 FR FR878716814A patent/FR2607702B1/fr not_active Expired - Lifetime
- 1987-12-03 CN CN87108225A patent/CN1058391C/zh not_active Expired - Lifetime
- 1987-12-03 DE DE19873741037 patent/DE3741037A1/de not_active Withdrawn
- 1987-12-03 EP EP91102986A patent/EP0438183B1/en not_active Revoked
- 1987-12-03 DE DE3752368T patent/DE3752368T2/de not_active Revoked
- 1987-12-03 NL NL8702914A patent/NL8702914A/nl not_active Application Discontinuation
- 1987-12-03 AT AT95101919T patent/ATE240108T1/de not_active IP Right Cessation
- 1987-12-03 ES ES198787310632T patent/ES2039460T3/es not_active Expired - Lifetime
- 1987-12-03 DE DE3751589T patent/DE3751589T2/de not_active Revoked
- 1987-12-03 KR KR1019870013744A patent/KR960007861B1/ko not_active IP Right Cessation
- 1987-12-03 DE DE8787310632T patent/DE3777365D1/de not_active Expired - Lifetime
- 1987-12-03 GR GR871846A patent/GR871846B/el unknown
- 1987-12-03 FI FI875340A patent/FI91710C/fi not_active IP Right Cessation
- 1987-12-03 AU AU82059/87A patent/AU632036B2/en not_active Expired
- 1987-12-03 ES ES95101919T patent/ES2198424T3/es not_active Expired - Lifetime
- 1987-12-03 EP EP87310632A patent/EP0273603B1/en not_active Expired - Lifetime
- 1987-12-03 EP EP02025856A patent/EP1283044A3/en not_active Withdrawn
- 1987-12-03 BE BE8701384A patent/BE1000540A5/fr not_active IP Right Cessation
- 1987-12-03 KR KR1019870013744Q patent/KR0158672B1/ko active
- 1987-12-03 PT PT86285A patent/PT86285B/pt unknown
- 1987-12-03 DK DK198706352A patent/DK175815B1/da not_active IP Right Cessation
- 1987-12-03 EP EP95101919A patent/EP0659435B1/en not_active Revoked
- 1987-12-03 CH CH4724/87A patent/CH680494A5/de not_active IP Right Cessation
- 1987-12-03 AT AT91102986T patent/ATE129896T1/de not_active IP Right Cessation
- 1987-12-03 GB GB8728313A patent/GB2200047B/en not_active Expired - Lifetime
- 1987-12-03 SE SE8704849A patent/SE512881C2/sv not_active IP Right Cessation
- 1987-12-03 ES ES91102986T patent/ES2082023T3/es not_active Expired - Lifetime
- 1987-12-03 IT IT8722869A patent/IT1226072B/it active
- 1987-12-03 JP JP62304699A patent/JP2621255B2/ja not_active Expired - Lifetime
- 1987-12-03 NO NO875055A patent/NO175802C/no not_active IP Right Cessation
-
1991
- 1991-05-13 SG SG365/91A patent/SG36591G/en unknown
- 1991-05-23 HK HK395/91A patent/HK39591A/xx not_active IP Right Cessation
-
1992
- 1992-04-08 GR GR920400665T patent/GR3004303T3/el unknown
-
1998
- 1998-11-30 HK HK03101548.2A patent/HK1049440A1/zh unknown
- 1998-11-30 HK HK98112442A patent/HK1011288A1/xx not_active IP Right Cessation
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