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)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Colloid Chemistry (AREA)
- Medicinal Preparation (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 |
| CA2294480C (en) | 1997-06-23 | 2008-05-20 | Queen's University At Kingston | Microdose therapy of female sexual dysfunction by no, co, and their donors |
| 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 |
| NO20002097L (no) * | 1999-04-30 | 2001-10-26 | Lilly Icos Llc | Fremstillingsgjenstander |
| 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 |
| NZ516616A (en) * | 1999-08-03 | 2003-07-25 | Lilly Icos Llc | Beta-carboline pharmaceutical compositions |
| US6821975B1 (en) | 1999-08-03 | 2004-11-23 | Lilly Icos Llc | Beta-carboline drug products |
| 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 |
| UY26615A1 (es) * | 2000-03-16 | 2001-10-25 | Pfizer Prod Inc | Inhibidor de la glucogeno fosforilasa. |
| AU2001276607A1 (en) * | 2000-08-11 | 2002-02-25 | Pfizer Inc. | Treatment of the insulin resistance syndrome with selective CGMP PDE5 inhibitors |
| US6884436B2 (en) | 2000-12-22 | 2005-04-26 | Baxter International Inc. | Method for preparing submicron particle suspensions |
| US7193084B2 (en) | 2000-12-22 | 2007-03-20 | Baxter International Inc. | Polymorphic form of itraconazole |
| 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 |
| US9700866B2 (en) | 2000-12-22 | 2017-07-11 | Baxter International Inc. | Surfactant systems for delivery of organic compounds |
| US8067032B2 (en) | 2000-12-22 | 2011-11-29 | Baxter International Inc. | Method for preparing submicron particles of antineoplastic agents |
| US6977085B2 (en) | 2000-12-22 | 2005-12-20 | Baxter International Inc. | Method for preparing submicron suspensions with polymorph control |
| US6607784B2 (en) | 2000-12-22 | 2003-08-19 | Baxter International Inc. | Microprecipitation method for preparing submicron suspensions |
| US6951656B2 (en) | 2000-12-22 | 2005-10-04 | Baxter International Inc. | Microprecipitation method for preparing submicron suspensions |
| AU2002337692B2 (en) | 2001-09-26 | 2007-09-13 | Baxter International Inc. | Preparation of submicron sized nanoparticles via dispersion and solvent or liquid phase removal |
| 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 |
| CN1688291A (zh) * | 2002-02-01 | 2005-10-26 | 辉瑞产品公司 | 含有固体药物分散体的即刻释放剂型 |
| JPWO2004113451A1 (ja) * | 2003-06-20 | 2006-08-17 | 明治製菓株式会社 | 難溶性物質と水溶性高分子との共沈物およびその製造方法 |
| WO2005068464A2 (en) * | 2003-12-15 | 2005-07-28 | Cadila Healthcare Limited | Process for preparing tadalafil and its intermediates |
| WO2006050458A2 (en) * | 2004-11-02 | 2006-05-11 | Teva Pharmaceutical Industries, Ltd. | Tadalafil crystal forms and processes for preparing them |
| DK1848430T3 (da) | 2004-12-31 | 2017-11-06 | Dr Reddys Laboratories Ltd | Nye benzylamin-derivativer som cetp-inhibitors |
| US8604055B2 (en) | 2004-12-31 | 2013-12-10 | Dr. Reddy's Laboratories Ltd. | Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors |
| WO2006091974A1 (en) * | 2005-02-25 | 2006-08-31 | Teva Pharmaceutical Industries Ltd. | Tadalafil having a large particle size and a process for preparation thereof |
| WO2006091980A1 (en) * | 2005-02-25 | 2006-08-31 | Teva Pharmaceutical Industries Ltd. | Process of purifying tadalafil |
| KR20070102719A (ko) * | 2005-02-25 | 2007-10-19 | 테바 파마슈티컬 인더스트리즈 리미티드 | 타달라필의 합성 방법 |
| RU2009103660A (ru) * | 2006-07-07 | 2010-08-20 | Тева Фармасьютикал Индастриес Лтд. (Il) | Твердые фармацевтические композиции, включающие тадалафил и по меньшей мере один носитель |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| WO2008134557A2 (en) * | 2007-04-25 | 2008-11-06 | Teva Pharmaceutical Industries Ltd. | Solid dosage forms |
| WO2008138755A2 (en) * | 2007-05-11 | 2008-11-20 | F. Hoffmann-La Roche Ag | Pharmaceutical compositions for poorly soluble drugs |
| US8426467B2 (en) | 2007-05-22 | 2013-04-23 | Baxter International Inc. | Colored esmolol concentrate |
| US8722736B2 (en) | 2007-05-22 | 2014-05-13 | Baxter International Inc. | Multi-dose concentrate esmolol with benzyl alcohol |
| DE102007028869A1 (de) | 2007-06-22 | 2008-12-24 | Ratiopharm Gmbh | Verfahren zur Herstellung eines Arzneimittels enthaltend Tadalafil |
| US20100190777A1 (en) | 2007-07-17 | 2010-07-29 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| HUE027598T2 (en) * | 2009-04-03 | 2016-10-28 | Hoffmann La Roche | Propane-1-sulfonic acid {3- [5- (4-chlorophenyl) -1H-pyrrolo [2,3-B] pyridine-3-carbonyl] -2,4-difluorophenyl} amide compositions and their uses |
| 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 |
| ES2633317T3 (es) | 2009-11-06 | 2017-09-20 | Plexxikon, Inc. | Compuestos y métodos para la modulación de quinasas, e indicaciones para ello |
| 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 |
| MA34948B1 (fr) | 2011-02-07 | 2014-03-01 | Plexxikon Inc | Composes et procedes de modulation de kinase, et leurs indications |
| 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 |
| WO2012107092A1 (en) | 2011-02-10 | 2012-08-16 | Synthon Bv | Pharmaceutical composition comprising tadalafil and a cyclodextrin |
| EP2675434A1 (de) | 2011-02-17 | 2013-12-25 | F.Hoffmann-La Roche Ag | Verfahren zur kontrollierten kristallisierung eines wirkstoffes aus einem unterkühlten flüssigkeitszustand durch schmelzextrusion |
| 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 |
| CA2845284C (en) | 2011-08-18 | 2018-03-06 | Dr. Reddy's Laboratories Ltd. | Substituted heterocyclic amine compounds as cholesteryl ester-transfer protein (cetp) inhibitors |
| JP6140168B2 (ja) | 2011-09-27 | 2017-05-31 | ドクター レディズ ラボラトリーズ リミテッド | アテローム性動脈硬化症の処置のために有用なコレステリルエステル転送タンパク質（ｃｅｔｐ）インヒビターとしての５−ベンジルアミノメチル−６−アミノピラゾロ［３，４−ｂ］ピリジン誘導体 |
| 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 |
| SG11201504499VA (en) * | 2013-01-22 | 2015-08-28 | Hoffmann La Roche | Pharmaceutical composition with improved bioavailability |
| CA2953917C (en) | 2013-07-01 | 2021-10-19 | The Research Foundation For The State University Of New York | Ship inhibition to combat obesity |
| EP3102210A4 (de) * | 2014-02-05 | 2017-10-11 | Merck Sharp & Dohme Corp. | Pharmazeutische zusammensetzungen für selektive hcv-ns3/4a-inhibitoren |
| AU2015277194B2 (en) | 2014-06-17 | 2020-10-22 | The Research Foundation For The State University Of New York | Ship inhibition to induce activation of natural killer cells |
| EA035390B1 (ru) * | 2014-07-23 | 2020-06-05 | КРКА, д.д., НОВО МЕСТО | Совместный осадок тадалафила с фармацевтически приемлемыми эксципиентами, содержащая его фармацевтическая композиция и способ их получения |
| 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 |
| CN109646404B (zh) * | 2016-12-15 | 2022-10-04 | 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 |
| LT3804714T (lt) * | 2018-05-31 | 2025-03-10 | Hua Medicine (Shanghai) Ltd. | Farmacinis derinys ir kompozicija, ir derinio preparatas, kurio sudėtyje yra gliukokinazės aktyvatorius ir biguanido hipoglikeminis vaistas, taip pat jų gamybos būdas ir panaudojimas |
| 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 |
| DK0558104T3 (da) * | 1992-01-21 | 1999-04-26 | Glaxo Wellcome Spa | 1,5-Benzodiazepinderivater og deres anvendelse i lægemidler |
| 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 US US08/952,938 patent/US5985326A/en not_active Expired - Lifetime
- 1996-05-30 AT AT96917457T patent/ATE207344T1/de not_active IP Right Cessation
- 1996-05-30 DE DE69616313T patent/DE69616313T2/de not_active Expired - Lifetime
- 1996-05-30 EP EP96917457A patent/EP0828479B1/de not_active Expired - Lifetime
- 1996-05-30 AU AU60026/96A patent/AU6002696A/en not_active Abandoned
- 1996-05-30 ES ES96917457T patent/ES2167566T3/es not_active Expired - Lifetime
- 1996-05-30 WO PCT/EP1996/002299 patent/WO1996038131A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| DE69616313T2 (de) | 2002-04-18 |
| WO1996038131A1 (en) | 1996-12-05 |
| US5985326A (en) | 1999-11-16 |
| ES2167566T3 (es) | 2002-05-16 |
| EP0828479A1 (de) | 1998-03-18 |
| EP0828479B1 (de) | 2001-10-24 |
| DE69616313D1 (de) | 2001-11-29 |
| AU6002696A (en) | 1996-12-18 |
| GB9511220D0 (en) | 1995-07-26 |
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