ATE207344T1 - Verfahren zur herstellung einer feststoffdespersion eines im wasser schwerlöslichen arzneimittel - Google Patents
Verfahren zur herstellung einer feststoffdespersion eines im wasser schwerlöslichen arzneimittelInfo
- Publication number
- ATE207344T1 ATE207344T1 AT96917457T AT96917457T ATE207344T1 AT E207344 T1 ATE207344 T1 AT E207344T1 AT 96917457 T AT96917457 T AT 96917457T AT 96917457 T AT96917457 T AT 96917457T AT E207344 T1 ATE207344 T1 AT E207344T1
- Authority
- AT
- Austria
- Prior art keywords
- pct
- poorly soluble
- producing
- water
- solid dispersion
- Prior art date
Links
- 239000007962 solid dispersion Substances 0.000 title abstract 3
- 238000004519 manufacturing process Methods 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title 1
- 239000006185 dispersion Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- WOXKDUGGOYFFRN-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 WOXKDUGGOYFFRN-IIBYNOLFSA-N 0.000 abstract 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
- 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
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Colloid Chemistry (AREA)
- Glass Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9511220.7A GB9511220D0 (en) | 1995-06-02 | 1995-06-02 | Solid dispersions |
| PCT/EP1996/002299 WO1996038131A1 (en) | 1995-06-02 | 1996-05-30 | Method of producing a solid dispersion of a poorly water soluble drug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE207344T1 true ATE207344T1 (de) | 2001-11-15 |
Family
ID=10775439
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT96917457T ATE207344T1 (de) | 1995-06-02 | 1996-05-30 | Verfahren zur herstellung einer feststoffdespersion eines im wasser schwerlöslichen arzneimittel |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US5985326A (de) |
| EP (1) | EP0828479B1 (de) |
| AT (1) | ATE207344T1 (de) |
| AU (1) | AU6002696A (de) |
| DE (1) | DE69616313T2 (de) |
| ES (1) | ES2167566T3 (de) |
| GB (1) | GB9511220D0 (de) |
| WO (1) | WO1996038131A1 (de) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6143746A (en) * | 1994-01-21 | 2000-11-07 | Icos Corporation | Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use |
| DE69833254T2 (de) | 1997-06-23 | 2006-11-02 | Cellegy Pharmaceuticals, Inc., Brisbane | Microdosistherapie von gefässbedingten erscheinungen durch no-donoren |
| US6350786B1 (en) † | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
| SA99191255B1 (ar) | 1998-11-30 | 2006-11-25 | جي دي سيرل اند كو | مركبات سيليكوكسيب celecoxib |
| HUP0001632A3 (en) * | 1999-04-30 | 2001-12-28 | Lilly Icos Llc Wilmington | Pharmaceutical compositions comprising selective phosphodiestherase inhibitors |
| US6451807B1 (en) | 1999-04-30 | 2002-09-17 | Lilly Icos, Llc. | Methods of treating sexual dysfunction in an individual suffering from a retinal disease, class 1 congestive heart failure, or myocardial infarction using a PDE5 inhibitor |
| UA71629C2 (en) * | 1999-08-03 | 2004-12-15 | Lilli Icos Llc | Composition containing free drug particulate form of ?-carboline (variants), method for its manufacture (variants), and method for treating sexual dysfunction |
| US6821975B1 (en) | 1999-08-03 | 2004-11-23 | Lilly Icos Llc | Beta-carboline drug products |
| UA72922C2 (uk) * | 1999-08-03 | 2005-05-16 | Ліллі Айкос Ллк | ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ З <font face="Symbol">b</font>-КАРБОЛІНОМ (ВАРІАНТИ) ТА СПОСІБ ЛІКУВАННЯ СЕКСУАЛЬНОЇ ДИСФУНКЦІЇ |
| AR028253A1 (es) * | 2000-03-16 | 2003-04-30 | Pfizer Prod Inc | Inhibidores de la glucogeno fosforilasa |
| HUP0300725A3 (en) * | 2000-08-11 | 2005-11-28 | Pfizer | Treatment of the insulin resistance syndrome with selective cgmp pde5 inhibitors |
| US7037528B2 (en) | 2000-12-22 | 2006-05-02 | Baxter International Inc. | Microprecipitation method for preparing submicron suspensions |
| US6977085B2 (en) | 2000-12-22 | 2005-12-20 | Baxter International Inc. | Method for preparing submicron suspensions with polymorph control |
| US9700866B2 (en) | 2000-12-22 | 2017-07-11 | Baxter International Inc. | Surfactant systems for delivery of organic compounds |
| US6884436B2 (en) | 2000-12-22 | 2005-04-26 | Baxter International Inc. | Method for preparing submicron particle suspensions |
| US6951656B2 (en) | 2000-12-22 | 2005-10-04 | Baxter International Inc. | Microprecipitation method for preparing submicron suspensions |
| US8067032B2 (en) | 2000-12-22 | 2011-11-29 | Baxter International Inc. | Method for preparing submicron particles of antineoplastic agents |
| US20050048126A1 (en) | 2000-12-22 | 2005-03-03 | Barrett Rabinow | Formulation to render an antimicrobial drug potent against organisms normally considered to be resistant to the drug |
| US7193084B2 (en) | 2000-12-22 | 2007-03-20 | Baxter International Inc. | Polymorphic form of itraconazole |
| CN1558755A (zh) | 2001-09-26 | 2004-12-29 | ���ع��ʹ�˾ | 通过分散和除去溶剂或液相制备亚微米大小的纳米颗粒 |
| US20060003012A9 (en) | 2001-09-26 | 2006-01-05 | Sean Brynjelsen | Preparation of submicron solid particle suspensions by sonication of multiphase systems |
| US7112340B2 (en) | 2001-10-19 | 2006-09-26 | Baxter International Inc. | Compositions of and method for preparing stable particles in a frozen aqueous matrix |
| MXPA04007428A (es) * | 2002-02-01 | 2004-10-11 | Pfizer Prod Inc | Formas de dosificacion de liberacion inmediata que contienen dispersiones de farmaco solido. |
| WO2004113424A1 (ja) * | 2003-06-20 | 2004-12-29 | Meiji Seika Kaisha, Ltd. | 難水溶性物質と水溶性高分子との共沈物の製造方法 |
| WO2005068464A2 (en) * | 2003-12-15 | 2005-07-28 | Cadila Healthcare Limited | Process for preparing tadalafil and its intermediates |
| CA2582092A1 (en) * | 2004-11-02 | 2006-05-11 | Teva Pharmaceutical Industries Ltd. | Tadalafil crystal forms and processes for preparing them |
| US9040558B2 (en) * | 2004-12-31 | 2015-05-26 | Dr. Reddy's Laboratories Ltd. | Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors |
| US8604055B2 (en) | 2004-12-31 | 2013-12-10 | Dr. Reddy's Laboratories Ltd. | Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors |
| WO2006091975A1 (en) * | 2005-02-25 | 2006-08-31 | Teva Pharmaceutical Industries Ltd. | Process of synthesizing tadalafil |
| US7417044B2 (en) * | 2005-02-25 | 2008-08-26 | Teva Pharmaceutical Industries Ltd. | Tadalafil having a large particle size and a process for preparation thereof |
| MX2007010431A (es) * | 2005-02-25 | 2007-10-11 | Teva Pharma | Proceso para purificar tadalafil. |
| MX2008016569A (es) * | 2006-07-07 | 2009-01-30 | Teva Pharma | Composiciones solidas que contienen tadalafil y al menos un portador. |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| KR20100012867A (ko) * | 2007-04-25 | 2010-02-08 | 테바 파마슈티컬 인더스트리즈 리미티드 | 타다라필을 포함하는 고체 제형 |
| EP2155166A2 (de) * | 2007-05-11 | 2010-02-24 | F. Hoffmann-Roche AG | Pharmazeutische zusammensetzung für schwer lösliche heilmittel |
| US8722736B2 (en) | 2007-05-22 | 2014-05-13 | Baxter International Inc. | Multi-dose concentrate esmolol with benzyl alcohol |
| US8426467B2 (en) | 2007-05-22 | 2013-04-23 | Baxter International Inc. | Colored esmolol concentrate |
| DE102007028869A1 (de) | 2007-06-22 | 2008-12-24 | Ratiopharm Gmbh | Verfahren zur Herstellung eines Arzneimittels enthaltend Tadalafil |
| MX2010000617A (es) | 2007-07-17 | 2010-05-17 | Plexxikon Inc | Compuestos y metodos para modulacion de cinasa, e indicaciones de estos. |
| EA031116B1 (ru) | 2009-04-03 | 2018-11-30 | Ф. Хоффманн-Ля Рош Аг | КРИСТАЛЛИЧЕСКИЕ ПОЛИМОРФНЫЕ ФОРМЫ {3-[5-(4-ХЛОРФЕНИЛ)-1H-ПИРРОЛО[2,3-b]ПИРИДИН-3-КАРБОНИЛ]-2,4-ДИФТОРФЕНИЛ}АМИДА ПРОПАН-1-СУЛЬФОНОВОЙ КИСЛОТЫ |
| EP2238979A1 (de) | 2009-04-06 | 2010-10-13 | LEK Pharmaceuticals d.d. | Auf einem festen Träger adsorbierter pharmazeutischer Wirkstoff |
| DE102009033396A1 (de) | 2009-07-16 | 2011-01-20 | Ratiopharm Gmbh | Wässrige Lösung und gelatinierte Zusammensetzung umfassend einen Phosphodiesterase-5-Inhibitor sowie diesbezügliche Verfahren und Verwendung |
| DE102009035211A1 (de) | 2009-07-29 | 2011-02-17 | Ratiopharm Gmbh | Copräzipitate umfassend einen Phosphodiesterase-5-Inhibitor (PDE-5-Inhibitor) und einen pharmazeutisch verträglichen Trägerstoff, ihre Herstellung und Verwendung |
| UA105813C2 (uk) | 2009-11-06 | 2014-06-25 | Плексікон, Інк. | Сполуки-інгібітори кіназ та фармацевтична композиція (варіанти) |
| WO2012085927A2 (en) * | 2010-12-02 | 2012-06-28 | Mylan Laboratories, Limited | Tadalafil compositions |
| WO2012095151A1 (en) | 2010-12-23 | 2012-07-19 | Zaklady Farmaceutyczne Polpharma Sa | Solid pharmaceutical dosage forms comprising tadalafil and methods of preparation thereof |
| PL2672967T3 (pl) | 2011-02-07 | 2019-04-30 | Plexxikon Inc | Związki i sposoby modulacji kinaz i wskazania ku temu |
| WO2012107092A1 (en) | 2011-02-10 | 2012-08-16 | Synthon Bv | Pharmaceutical composition comprising tadalafil and a cyclodextrin |
| WO2012107541A1 (en) | 2011-02-10 | 2012-08-16 | Synthon Bv | Pharmaceutical composition comprising tadalafil and a cyclodextrin |
| WO2012107090A1 (en) | 2011-02-10 | 2012-08-16 | Synthon Bv | Granulated composition comprising tadalafil and a disintegrant |
| CN103391769A (zh) | 2011-02-17 | 2013-11-13 | 霍夫曼-拉罗奇有限公司 | 通过热熔挤出使活性药物成分从过冷液体状态受控结晶的方法 |
| TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
| EP2535049A1 (de) | 2011-06-17 | 2012-12-19 | Proyecto de Biomedicina Cima, S.L. | Tadalafil zur Behandlung von Demenz |
| WO2013024358A2 (en) | 2011-08-18 | 2013-02-21 | Dr. Reddy's Laboratories Ltd. | Substituted heterocyclic amine compounds as cholestryl ester-transfer protein (cetp) inhibitors |
| MX352074B (es) | 2011-09-27 | 2017-11-08 | Dr Reddys Laboratories Ltd | Derivados de 5-bencilaminometil-6-aminopirazolo [3,4-b] piridina como inhibidores de proteina de transferencia de ester de colesterilo (cetp) utiles para el tratamiento de aterosclerosis. |
| US20140128431A1 (en) | 2012-04-03 | 2014-05-08 | Hoffmann-Laroche Inc. | Pharmaceutical composition with improved bioavailability, safety and tolerability |
| EP2649989B1 (de) | 2012-04-13 | 2017-10-18 | King Saud University | Verfahren zur Herstellung einer Feststoffdispersion, damit hergestellte Feststoffdispersion und Verwendung dafür |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| WO2014003677A1 (en) * | 2012-06-28 | 2014-01-03 | Xspray Microparticles Ab | Pharmaceutical compositions comprising solid dispersion particles containing tadalafil |
| WO2014003678A1 (en) * | 2012-06-28 | 2014-01-03 | Xspray Microparticles Ab | Pharmaceutical compositions comprising ambrisentan and solid dispersion particles containing tadalafil |
| CA2891502A1 (en) | 2012-11-19 | 2014-05-22 | Dr. Reddy's Laboratories Ltd. | Pharmaceutical compositions of cetp inhibitors |
| UA116004C2 (uk) * | 2013-01-22 | 2018-01-25 | Ф. Хоффманн-Ля Рош Аг | Фармацевтична композиція з покращеною біодоступністю |
| CA2953917C (en) | 2013-07-01 | 2021-10-19 | The Research Foundation For The State University Of New York | Ship inhibition to combat obesity |
| WO2015119919A1 (en) * | 2014-02-05 | 2015-08-13 | Merck Sharp & Dohme Corp. | Pharmaceutical composition of selective hcv ns3/4a inhibitors |
| EP3157529B1 (de) | 2014-06-17 | 2021-08-04 | The Research Foundation for The State University of New York | Ship-hemmung zum induzieren der aktivierung von natürlichen killerzellen |
| WO2016012539A1 (en) * | 2014-07-23 | 2016-01-28 | Krka, D.D., Novo Mesto | A process for the preparation of cgmp-phosphodiesterase inhibitor and oral pharmaceutical formulation comprising tadalafil co-precipitates |
| TWI586379B (zh) | 2015-06-29 | 2017-06-11 | 永信藥品工業股份有限公司 | 一種製作難溶藥物固體劑型的方法 |
| CN105384740A (zh) * | 2015-12-18 | 2016-03-09 | 海南通用康力制药有限公司 | 一种制备他达拉非的中间体高纯度晶体及制备方法 |
| CN107663210A (zh) * | 2016-07-28 | 2018-02-06 | 常州爱诺新睿医药技术有限公司 | 一种新的制备无水他达拉非晶型i的方法 |
| WO2018108128A1 (zh) * | 2016-12-15 | 2018-06-21 | 华领医药技术（上海）有限公司 | 葡萄糖激酶激活剂的口服制剂及其制备方法 |
| LT3510997T (lt) | 2018-01-10 | 2021-01-11 | Gap S.A. | Minkšta želatinos kapsulė, apimanti tadalafilio suspensiją |
| DK3804716T3 (da) * | 2018-05-31 | 2025-03-03 | Hua Medicine Shanghai Ltd | Farmaceutisk kombination, sammensætning og kombinationspræparat omfattende glucokinase-aktivator og sglt-2-inhibitor og fremgangsmåder til fremstilling og anvendelser deraf |
| EP4531815A1 (de) | 2022-05-27 | 2025-04-09 | Rontis Hellas S.A. | Verbesserte pharmazeutische zusammensetzung mit tadalafil und nanomühlungsverfahren zur herstellung davon |
| CN118177150B (zh) * | 2024-04-15 | 2024-12-03 | 中国医学科学院医学实验动物研究所 | 遗传多样性高血压小鼠模型的建立与基因转录调控分析 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0297866A3 (de) * | 1987-07-01 | 1989-12-13 | The Boots Company PLC | Arzneimittel |
| US5194263A (en) * | 1989-01-20 | 1993-03-16 | Allied Colloids Limited | Particulate materials, their production and use |
| ES2121925T3 (es) * | 1992-01-21 | 1998-12-16 | Glaxo Wellcome Spa | Derivados de 1,5-benzodiacepina y su uso en medicina. |
| GB9401090D0 (en) * | 1994-01-21 | 1994-03-16 | Glaxo Lab Sa | Chemical compounds |
| US5665331A (en) * | 1995-01-10 | 1997-09-09 | Nanosystems L.L.C. | Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers |
-
1995
- 1995-06-02 GB GBGB9511220.7A patent/GB9511220D0/en active Pending
-
1996
- 1996-05-30 ES ES96917457T patent/ES2167566T3/es not_active Expired - Lifetime
- 1996-05-30 DE DE69616313T patent/DE69616313T2/de not_active Expired - Lifetime
- 1996-05-30 US US08/952,938 patent/US5985326A/en not_active Expired - Lifetime
- 1996-05-30 EP EP96917457A patent/EP0828479B1/de not_active Expired - Lifetime
- 1996-05-30 AT AT96917457T patent/ATE207344T1/de not_active IP Right Cessation
- 1996-05-30 WO PCT/EP1996/002299 patent/WO1996038131A1/en not_active Ceased
- 1996-05-30 AU AU60026/96A patent/AU6002696A/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP0828479A1 (de) | 1998-03-18 |
| US5985326A (en) | 1999-11-16 |
| GB9511220D0 (en) | 1995-07-26 |
| AU6002696A (en) | 1996-12-18 |
| DE69616313T2 (de) | 2002-04-18 |
| ES2167566T3 (es) | 2002-05-16 |
| EP0828479B1 (de) | 2001-10-24 |
| DE69616313D1 (de) | 2001-11-29 |
| WO1996038131A1 (en) | 1996-12-05 |
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