KR900005960A - 용해속도를 증가시키기에 적합한 형태로 중합체 기질상에 지지된 저-가용성 약제 - Google Patents
용해속도를 증가시키기에 적합한 형태로 중합체 기질상에 지지된 저-가용성 약제 Download PDFInfo
- Publication number
- KR900005960A KR900005960A KR1019890014823A KR890014823A KR900005960A KR 900005960 A KR900005960 A KR 900005960A KR 1019890014823 A KR1019890014823 A KR 1019890014823A KR 890014823 A KR890014823 A KR 890014823A KR 900005960 A KR900005960 A KR 900005960A
- Authority
- KR
- South Korea
- Prior art keywords
- solvent
- contacting
- polymer
- crosslinked
- water
- Prior art date
Links
- 238000004090 dissolution Methods 0.000 title claims 6
- 239000003795 chemical substances by application Substances 0.000 title claims 5
- 239000000758 substrate Substances 0.000 title 1
- 239000002904 solvent Substances 0.000 claims 21
- 238000000034 method Methods 0.000 claims 14
- 239000003814 drug Substances 0.000 claims 8
- 229920000642 polymer Polymers 0.000 claims 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 6
- 239000007788 liquid Substances 0.000 claims 5
- 229920000307 polymer substrate Polymers 0.000 claims 5
- 229940079593 drug Drugs 0.000 claims 4
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims 4
- 239000002245 particle Substances 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 2
- 229920000858 Cyclodextrin Polymers 0.000 claims 2
- 229920002307 Dextran Polymers 0.000 claims 2
- IIUZTXTZRGLYTI-UHFFFAOYSA-N Dihydrogriseofulvin Natural products COC1CC(=O)CC(C)C11C(=O)C(C(OC)=CC(OC)=C2Cl)=C2O1 IIUZTXTZRGLYTI-UHFFFAOYSA-N 0.000 claims 2
- 239000001116 FEMA 4028 Substances 0.000 claims 2
- ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 claims 2
- UXWOXTQWVMFRSE-UHFFFAOYSA-N Griseoviridin Natural products O=C1OC(C)CC=C(C(NCC=CC=CC(O)CC(O)C2)=O)SCC1NC(=O)C1=COC2=N1 UXWOXTQWVMFRSE-UHFFFAOYSA-N 0.000 claims 2
- DDUHZTYCFQRHIY-UHFFFAOYSA-N Negwer: 6874 Natural products COC1=CC(=O)CC(C)C11C(=O)C(C(OC)=CC(OC)=C2Cl)=C2O1 DDUHZTYCFQRHIY-UHFFFAOYSA-N 0.000 claims 2
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 claims 2
- 235000011175 beta-cyclodextrine Nutrition 0.000 claims 2
- 229960004853 betadex Drugs 0.000 claims 2
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 claims 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 2
- DDUHZTYCFQRHIY-RBHXEPJQSA-N griseofulvin Chemical group COC1=CC(=O)C[C@@H](C)[C@@]11C(=O)C(C(OC)=CC(OC)=C2Cl)=C2O1 DDUHZTYCFQRHIY-RBHXEPJQSA-N 0.000 claims 2
- 229960002867 griseofulvin Drugs 0.000 claims 2
- 229960000905 indomethacin Drugs 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-dimethylformamide Substances CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 229920006037 cross link polymer Polymers 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 229930195733 hydrocarbon Natural products 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- 239000010410 layer Substances 0.000 claims 1
- 229960001786 megestrol Drugs 0.000 claims 1
- RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 claims 1
- 238000002156 mixing Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 238000005507 spraying Methods 0.000 claims 1
- 239000002344 surface layer Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 230000008961 swelling Effects 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
- Polyoxymethylene Polymers And Polymers With Carbon-To-Carbon Bonds (AREA)
- Processes Of Treating Macromolecular Substances (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (19)
- 물중에서 팽윤될 수는 있지만 용해되지는 않는 가교결합된 중합체 입자내로 약제를 혼합시키고, 수득된 생성물을, 중합체를 팽윤시킬 수 있는 기체상 또는 액상 용매와 접촉시킨 다음, 진공하에서 건조시킴을 특징으로 하여, 용해속도를 증가시킬 수 있는 형태로 중합체 기질상에 지지된 약제를 제조하는 방법.
- 제1항에 있어서, 용매와의 접촉단계가, 용매가 증기형태로 공급되는 쳄버에서수행되는 방법.
- 제1항에 있어서, 용매와의 접촉단계가, 챔버 자체내에서 생성되는 용매 증기로 포함된 쳄버에서 수행되는 방법.
- 제1항에 있어서, 용매와의 접촉단계가 유동화 베드에서 액상 용매을 사용하여 입자를 분무시킴으로써 수행되는 방법.
- 제1항에 있어서, 용매와의 접촉단계가 유동화 베드에서 용매증기로 포화된 공기 스트림에 의해 수행되는 방법.
- 제1항에 있어서, 용매와의 접촉단계가 생성물을 액상 용매중에 현탁시킴으로써 수행되는 방법.
- 제1항에 있어서, 기체상 용매와의 접촉단계가, 용매가 물이 아닌 경우에는 0.5 내지 48시간동안 수행되며 용매가 물인 경우에는 12 내지 36시간동안 수행되는 방법.
- 제1항에 있어서, 액상 용매와의 접촉단계가, 용매가 물이 아닌 경우에는 1분 내지 96시간동안 수행되며 용매가 물인 경우에는 1 내지 15시간동안 수행되는 방법.
- 제1항에 있어서, 기체상 용매와의 접촉단계가 20 내지 100℃의 온도에서 수행되는 방법.
- 제1항에 있어서, 액상 용매와의 접촉단계가 5 내지 90℃의 온도에서 수행되는 방법.
- 제1항에 있어서, 건조단계가 20 내지 100℃의 온도에서 수행되는 방법.
- 제1항에 있어서, 중합체가 가교결합된 폴리비닐피롤리돈, 가교결합된 나트륨 카복시메틸셀룰로즈, 가교결합된 β-사이클로덱스트린 중합체 또는 가교결합된 덱스트란인 방법.
- 제1항에 있어서, 약제가 그리세오풀빈, 인도메타신, 디아세레인, 메제스트롤 또는 니세르골린인 방법.
- 제1항에 있어서, 용매가 물, 물-알코올 혼합물, 메탄올, 에탄올, 고금 알코올, 아세톤, 염소화된 용매, 포름아미드, DMF 또는 불화 탄화수소인 방법.
- 제1항 내지 14항중 어느 한 항에 따른 방법에 의해 제조되는, 용해속도를 증가시킬 수 있는 형태로 중합체 기질상에 지지된 저-가용성 약제.
- 약제 농도가 중합체 입자의 내부층에서보다 표면층에서 더 높음을 특징으로 하여, 용해 속도를 증가시킬 수 있는 형태로 중합체 기질상에 지지된 저-가용성 약제.
- 약제가 나노미터(nm) 크기의 입자 형태임을 특징으로 하여, 용해속도를 증가시킬 수 있는 형태로 중합체 기질상에 지지된 저-가용성 약제.
- 중합체가 가교결합된 폴리비닐피롤리돈, 가교결합된 나트륨 카복시메틸셀룰로즈, 가교결합된 β-사이클로덱스트린 중합체 또는 가교결합된 덱스트란이며, 약제는 그리세오풀빈, 인도메타신, 디아세레인, 메제스트롤 또는 니세르골린임을 특징으로 하여, 용해 속도를 증가시킬 수 있는 형태로 중합체 기질상에 지지된 저-가용성 약제.
- 서방성 캅셀제 및 정제, 현택제, 및 경피 필름제를 제조하기 위한 제15항 내지 17항중 어느 한 항에 따른 약제의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT22336A/88 | 1988-10-17 | ||
| IT8822336A IT1230566B (it) | 1988-10-17 | 1988-10-17 | Farmaci poco solubili supportati su sostanze polimeriche in forma atta all'aumento della velocita' di dissoluzione |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR900005960A true KR900005960A (ko) | 1990-05-07 |
| KR0148006B1 KR0148006B1 (ko) | 1998-08-17 |
Family
ID=11194858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019890014823A KR0148006B1 (ko) | 1988-10-17 | 1989-10-16 | 용해속도를 증가시키기에 적합한 형태로 중합체 기재로 지지된 저가용성약제 및 이의 제조방법 |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP0364944B1 (ko) |
| JP (1) | JP2869103B2 (ko) |
| KR (1) | KR0148006B1 (ko) |
| AT (1) | ATE91622T1 (ko) |
| CA (1) | CA2000744C (ko) |
| DE (1) | DE68907687T2 (ko) |
| ES (1) | ES2060715T3 (ko) |
| HU (1) | HU203481B (ko) |
| IT (1) | IT1230566B (ko) |
| YU (1) | YU198489A (ko) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1243745B (it) * | 1990-10-17 | 1994-06-21 | Vectorpharma Int | Composizioni terapeutiche transdermali contenenti farmaco e/o agente promotore dell'assorbimento cutaneo supportato su particelle microporose e microsfere polimeriche e loro preparazione. |
| EP0519428B1 (en) * | 1991-06-21 | 2000-09-20 | Takeda Chemical Industries, Ltd. | Cyclodextrin compositions with fumagillol derivates |
| IT1252867B (it) * | 1991-12-31 | 1995-06-28 | Gentili Ist Spa | Composizioni farmaceutiche contenenti progesterone ad elevata biodisponibilita' |
| AU722246B2 (en) * | 1995-06-07 | 2000-07-27 | Johnson & Johnson Consumer Products, Inc. | Stable complexes of crosslinked polyvinylpyrrolidone and iodine and method of making the same |
| NL1003503C2 (nl) * | 1996-07-04 | 1998-01-07 | Negma Steba International Dev | Farmaceutische samenstelling voor orale toediening. |
| US6287693B1 (en) * | 1998-02-25 | 2001-09-11 | John Claude Savoir | Stable shaped particles of crystalline organic compounds |
| ATE356637T1 (de) * | 1998-12-04 | 2007-04-15 | California Inst Of Techn | Supramolekulare komplexe enthaltende arzneimittel |
| IT1318404B1 (it) * | 2000-03-17 | 2003-08-25 | Eurand Int | Processo per la preparazione di formulazioni a rilascio accelerato conimpiego di fluidi compressi. |
| EP1534340B1 (en) | 2002-09-06 | 2011-11-16 | Cerulean Pharma Inc. | Cyclodextrin-based polymers for delivering the therapeutic agents covalently bound thereto |
| WO2004110408A2 (en) | 2003-06-13 | 2004-12-23 | John Claude Savoir | Process for the manufacture of stable shaped particles consisting of estradiol and cholesterol |
| DE102006026578B4 (de) | 2006-06-08 | 2009-01-08 | Lts Lohmann Therapie-Systeme Ag | Wirkstoffpartikelhaltiges Transdermales Therapeutisches System mit erhöhtem Wirkstofffluss und Verfahren zu seiner Herstellung sowie Verwendung |
| JP2010516625A (ja) | 2007-01-24 | 2010-05-20 | インサート セラピューティクス， インコーポレイテッド | 制御された薬物送達のためのテザー基を有するポリマー−薬物コンジュゲート |
| EP2471517A3 (en) | 2007-09-14 | 2012-12-26 | Wockhardt Limited | Rhein or diacerein compositions |
| GB0812742D0 (en) | 2008-07-11 | 2008-08-20 | Critical Pharmaceuticals Ltd | Process |
| TWI473610B (zh) * | 2008-10-28 | 2015-02-21 | Twi Biotechnology Inc | 包含雙醋瑞因（ｄｉａｃｅｒｅｉｎ）之醫藥組合物 |
| IE20100799A1 (en) | 2010-12-22 | 2012-08-01 | Eurand Pharmaceuticals Ltd | Pharmaceutical composites of poorly water soluble drugs and polymers |
| US20140094432A1 (en) | 2012-10-02 | 2014-04-03 | Cerulean Pharma Inc. | Methods and systems for polymer precipitation and generation of particles |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU189534B (en) | 1981-09-09 | 1986-07-28 | Chinoin Rt.,Hu | Process for producing new tablets containing cyclodextrin polymer as desintegrator |
| DE3326167A1 (de) * | 1983-07-20 | 1985-02-21 | Dr. Rentschler Arzneimittel Gmbh & Co, 7958 Laupheim | Feste arzneiformen, die als wirkstoff n-4-(2-(5-chlor-2-methoxybenzamido)-ethyl)-phenylsulfonyl-n'-cyclohexylharnstoff enthalten und verfahren zu ihrer herstellung |
| IE63321B1 (en) * | 1986-02-03 | 1995-04-05 | Elan Corp Plc | Drug delivery system |
-
1988
- 1988-10-17 IT IT8822336A patent/IT1230566B/it active
-
1989
- 1989-10-13 YU YU01984/89A patent/YU198489A/xx unknown
- 1989-10-16 CA CA002000744A patent/CA2000744C/en not_active Expired - Lifetime
- 1989-10-16 KR KR1019890014823A patent/KR0148006B1/ko not_active IP Right Cessation
- 1989-10-16 HU HU895330A patent/HU203481B/hu unknown
- 1989-10-17 JP JP1270148A patent/JP2869103B2/ja not_active Expired - Lifetime
- 1989-10-17 ES ES89119241T patent/ES2060715T3/es not_active Expired - Lifetime
- 1989-10-17 EP EP89119241A patent/EP0364944B1/en not_active Expired - Lifetime
- 1989-10-17 AT AT89119241T patent/ATE91622T1/de not_active IP Right Cessation
- 1989-10-17 DE DE89119241T patent/DE68907687T2/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CA2000744A1 (en) | 1990-04-17 |
| DE68907687D1 (de) | 1993-08-26 |
| YU198489A (en) | 1991-08-31 |
| EP0364944B1 (en) | 1993-07-21 |
| EP0364944A1 (en) | 1990-04-25 |
| JPH02149513A (ja) | 1990-06-08 |
| JP2869103B2 (ja) | 1999-03-10 |
| KR0148006B1 (ko) | 1998-08-17 |
| ES2060715T3 (es) | 1994-12-01 |
| ATE91622T1 (de) | 1993-08-15 |
| HU895330D0 (en) | 1990-01-28 |
| IT1230566B (it) | 1991-10-28 |
| HU203481B (en) | 1991-08-28 |
| DE68907687T2 (de) | 1993-10-28 |
| HUT52398A (en) | 1990-07-28 |
| IT8822336A0 (it) | 1988-10-17 |
| CA2000744C (en) | 1999-12-07 |
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