KR100360827B1 - 난용성 약물을 가용화하기 위한 고분자 조성물 및 그의 제조방법 - Google Patents
난용성 약물을 가용화하기 위한 고분자 조성물 및 그의 제조방법Info
- Publication number
- KR100360827B1 KR100360827B1 KR1019990033500A KR19990033500A KR100360827B1 KR 100360827 B1 KR100360827 B1 KR 100360827B1 KR 1019990033500 A KR1019990033500 A KR 1019990033500A KR 19990033500 A KR19990033500 A KR 19990033500A KR 100360827 B1 KR100360827 B1 KR 100360827B1
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- Prior art keywords
- composition
- block copolymer
- water
- polyethylene glycol
- polymer
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L101/00—Compositions of unspecified macromolecular compounds
- C08L101/12—Compositions of unspecified macromolecular compounds characterised by physical features, e.g. anisotropy, viscosity or electrical conductivity
- C08L101/14—Compositions of unspecified macromolecular compounds characterised by physical features, e.g. anisotropy, viscosity or electrical conductivity the macromolecular compounds being water soluble or water swellable, e.g. aqueous gels
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L71/00—Compositions of polyethers obtained by reactions forming an ether link in the main chain; Compositions of derivatives of such polymers
- C08L71/02—Polyalkylene oxides
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L2203/00—Applications
- C08L2203/02—Applications for biomedical use
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L2205/00—Polymer mixtures characterised by other features
- C08L2205/05—Polymer mixtures characterised by other features containing polymer components which can react with one another
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L67/00—Compositions of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Compositions of derivatives of such polymers
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L67/00—Compositions of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Compositions of derivatives of such polymers
- C08L67/04—Polyesters derived from hydroxycarboxylic acids, e.g. lactones
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Dispersion Chemistry (AREA)
- Organic Chemistry (AREA)
- Polymers & Plastics (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Abstract
Description
약물봉입효율(%) | 용해도(mg/ml) | |
조성물 1 | 100 | 30 |
조성물 2 | 100 | 15 |
조성물 3 | 100 | 60 |
조성물 4 | 100 | 30 |
조성물 5 | 100 | 30 |
조성물 6 | 100 | 30 |
조성물 7 | 100 | 30 |
조성물 8 | 100 | 10 |
조성물 9 | 100 | 10 |
조성물 10 | 100 | 30 |
조성물 11 | 100 | 30 |
조성물 12 | 100 | 30 |
조성물 13 | 100 | 30 |
조성물 14 | 100 | 30 |
조성물 15 | 100 | 30 |
비교조성물 1 | - | 0.001 |
비교조성물 2 | - | 0.008 |
비교조성물 3 | - | 0.010 |
비교조성물 4 | - | 0.002 |
* 약물봉입효율(%)=(용해된 난용성 약물양/가해진 난용성 약물양) X 100 |
Claims (13)
- 친수성 폴리알킬렌글리콜과 소수성 생분해성 고분자의 블록 공중합체 및 폴리에틸렌글리콜 또는 그의 유도체를 함유하는 고분자 조성물로서, 물 또는 체액에 가하였을 때 고분자 미셀을 형성하는 것을 특징으로 하는 조성물.
- 제1항에 있어서,블록 공중합체 5 내지 95 중량% 및 폴리에틸렌글리콜 또는 그의 유도체 5 내지 95 중량%로 이루어진 조성물.
- 제1항에 있어서,상기 블록 공중합체가 친수성 폴리알킬렌글리콜 블록(A)과 소수성 생분해성 고분자 블록(B)으로 구성된 A-B 형의 이중블록 공중합체 또는 A-B-A 형의 삼중블록 공중합체인 조성물.
- 제1항에 있어서,상기 블록 공중합체중 폴리알킬렌글리콜 블록의 함량이 40 내지 80 중량%인 조성물.
- 제1항에 있어서,상기 친수성 폴리알킬렌글리콜이 폴리에틸렌글리콜 또는 모노메톡시 폴리에틸렌글리콜이고 분자량이 1,000 내지 15,000 달톤인 조성물.
- 제1항에 있어서,상기 소수성 생분해성 고분자가 폴리락트산, 락트산과 글리콜산의 공중합체, D,L-락타이드와 글리콜라이드의 공중합체, 폴리카프로락톤, 폴리언하이드라이드, 폴리오르소에스터, 락타이드와 1,4-다이옥산-2-온의 공중합체, 또는 카프로락톤과 1,4-다이옥산-2-온의 공중합체이고 분자량이 1,000 내지 10,000 달톤인 조성물.
- 제1항에 있어서,상기 폴리에틸렌글리콜 또는 그의 유도체가 하기 화학식 1의 구조를 가지며 분자량이 200 내지 10,000 달톤인 것을 특징으로 하는 조성물:화학식 1R-O-CH2CH2-(OCH2CH2)n-O-R여기에서,R은 수소, C1-C4알킬기, 벤질기 또는 아실기이고,n은 3 내지 220의 정수이다.
- 제1항에 있어서,수-난용성 약물을 추가로 포함하는 조성물.
- 제8항에 있어서,수-난용성 약물의 함량이 블록 공중합체를 기준으로 0.1 내지 50 중량%인 조성물.
- 제8항에 있어서,상기 수-난용성 약물이 물에 대한 용해도가 10 ㎎/㎖ 이하인 항암제, 항균제, 스테로이드류, 소염 진통제, 성 호르몬, 면역억제제, 항바이러스제, 마취제, 항구토제 또는 항히스타민제인 조성물.
- 제8항에 있어서,상기 수-난용성 약물이 파클리탁셀, 캄토테신, 독소루비신, 아드리아마이신, 시스플레틴, 5-플루오로우라실, 싸이클로스포린 A, 암포테리신 B, 이트라코나졸, 케토코나졸, 인도메타신, 테스토스테론, 에스트라다이올, 덱사메타손, 프레드니솔론 또는 트리암시노론 아세토나이드인 조성물.
- 제8항에 있어서,에탄올, 아세트산, 락트산, 글리콜산, N-메틸 2-피롤리돈, 벤질알콜, 글리세린, N,N-디메틸 아세트아미드, 프로필렌글리콜, 디에틸아민 또는 이들의 혼합물로부터 선택된 용해보조제를 추가로 포함하는 조성물.
- (a) 친수성 폴리알킬렌글리콜과 소수성 생분해성 고분자의 블록 공중합체, 수-난용성 약물, 및 폴리에틸렌글리콜 또는 그의 유도체를 혼합하는 단계, 및(b) 상기 혼합물을 가열하거나, 상기 혼합물에 용해보조제를 가한 후 가열하거나, 상기 혼합물을 유기용매에 가하여 용해시킨 후 유기용매를 증발시키는 단계를 포함하는, 제8항에 따른 고분자 조성물의 제조 방법.
Priority Applications (13)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1019990033500A KR100360827B1 (ko) | 1999-08-14 | 1999-08-14 | 난용성 약물을 가용화하기 위한 고분자 조성물 및 그의 제조방법 |
DE60031286T DE60031286T2 (de) | 1999-08-14 | 2000-08-10 | Polymere zusammensetzung zur lösung von schwer wasserlöslichen medikamenten und verfahren zu deren herstellung |
EP00952029A EP1226212B1 (en) | 1999-08-14 | 2000-08-10 | Polymeric composition for solubilizing poorly water soluble drugs and process for the preparation thereof |
ES00952029T ES2269168T3 (es) | 1999-08-14 | 2000-08-10 | Composicion polimerica para solubilizar farmacos poco solubles en agua y procedimiento para su preparacion. |
AT00952029T ATE342306T1 (de) | 1999-08-14 | 2000-08-10 | Polymere zusammensetzung zur lösung von schwer wasserlöslichen medikamenten und verfahren zu deren herstellung |
NZ517036A NZ517036A (en) | 1999-08-14 | 2000-08-10 | A composition comprising a block copolymer of a hydrophilic poly(alkylene glycol) block and a hydrophobic biodegradable polymer block dispersed in a poly(ethylene glycol) matrix |
CA002381729A CA2381729C (en) | 1999-08-14 | 2000-08-10 | Polymeric composition for solubilizing poorly water soluble drugs and process for the preparation thereof |
PCT/KR2000/000885 WO2001012718A1 (en) | 1999-08-14 | 2000-08-10 | Polymeric composition for solubilizing poorly water soluble drugs and process for the preparation thereof |
AU64792/00A AU763154B2 (en) | 1999-08-14 | 2000-08-10 | Polymeric composition for solubilizing poorly water soluble drugs and process for the preparation thereof |
US09/807,487 US6616941B1 (en) | 1999-08-14 | 2000-08-10 | Polymeric composition for solubilizing poorly water soluble drugs and process for the preparation thereof |
JP2001517608A JP3363142B1 (ja) | 1999-08-14 | 2000-08-10 | 難水溶性薬物を可溶化するための重合組成物及びその製造方法 |
CNB008117160A CN1164675C (zh) | 1999-08-14 | 2000-08-10 | 用于溶解不良水溶性药物的聚合物组合物及其制备方法 |
MXPA02001527A MXPA02001527A (es) | 1999-08-14 | 2000-08-10 | Composicion polimerica para solubilizar farmacos escasamente solubles en agua y proceso para la preparacion de los mismos. |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1019990033500A KR100360827B1 (ko) | 1999-08-14 | 1999-08-14 | 난용성 약물을 가용화하기 위한 고분자 조성물 및 그의 제조방법 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR20010017804A KR20010017804A (ko) | 2001-03-05 |
KR100360827B1 true KR100360827B1 (ko) | 2002-11-18 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019990033500A KR100360827B1 (ko) | 1999-08-14 | 1999-08-14 | 난용성 약물을 가용화하기 위한 고분자 조성물 및 그의 제조방법 |
Country Status (13)
Country | Link |
---|---|
US (1) | US6616941B1 (ko) |
EP (1) | EP1226212B1 (ko) |
JP (1) | JP3363142B1 (ko) |
KR (1) | KR100360827B1 (ko) |
CN (1) | CN1164675C (ko) |
AT (1) | ATE342306T1 (ko) |
AU (1) | AU763154B2 (ko) |
CA (1) | CA2381729C (ko) |
DE (1) | DE60031286T2 (ko) |
ES (1) | ES2269168T3 (ko) |
MX (1) | MXPA02001527A (ko) |
NZ (1) | NZ517036A (ko) |
WO (1) | WO2001012718A1 (ko) |
Cited By (1)
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AU6479200A (en) | 2001-03-13 |
EP1226212A4 (en) | 2005-01-12 |
JP2003507514A (ja) | 2003-02-25 |
CN1164675C (zh) | 2004-09-01 |
CA2381729C (en) | 2008-07-29 |
DE60031286T2 (de) | 2007-05-24 |
EP1226212A1 (en) | 2002-07-31 |
DE60031286D1 (de) | 2006-11-23 |
MXPA02001527A (es) | 2002-07-02 |
ATE342306T1 (de) | 2006-11-15 |
JP3363142B1 (ja) | 2003-01-08 |
CA2381729A1 (en) | 2001-02-22 |
ES2269168T3 (es) | 2007-04-01 |
CN1370201A (zh) | 2002-09-18 |
NZ517036A (en) | 2003-07-25 |
EP1226212B1 (en) | 2006-10-11 |
AU763154B2 (en) | 2003-07-17 |
KR20010017804A (ko) | 2001-03-05 |
US6616941B1 (en) | 2003-09-09 |
WO2001012718A1 (en) | 2001-02-22 |
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