DK1795186T4 - Flupirtinomfattende lægemiddelformulering med en kontrolleret frisætning af det aktive middel - Google Patents
Flupirtinomfattende lægemiddelformulering med en kontrolleret frisætning af det aktive middel Download PDFInfo
- Publication number
- DK1795186T4 DK1795186T4 DK06022985.3T DK06022985T DK1795186T4 DK 1795186 T4 DK1795186 T4 DK 1795186T4 DK 06022985 T DK06022985 T DK 06022985T DK 1795186 T4 DK1795186 T4 DK 1795186T4
- Authority
- DK
- Denmark
- Prior art keywords
- active ingredient
- flupirtine
- release
- pharmaceutical preparation
- preparation according
- Prior art date
Links
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- WBAZQELGBFQHPE-UHFFFAOYSA-N ethyl n-[2-amino-6-[(4-fluorophenyl)methylamino]pyridin-3-yl]carbamate;hydron;chloride Chemical compound Cl.N1=C(N)C(NC(=O)OCC)=CC=C1NCC1=CC=C(F)C=C1 WBAZQELGBFQHPE-UHFFFAOYSA-N 0.000 description 1
- XPNLOZNCOBKRNJ-UHFFFAOYSA-N ethyl prop-2-enoate;methyl 2-methylprop-2-enoate Chemical compound CCOC(=O)C=C.COC(=O)C(C)=C XPNLOZNCOBKRNJ-UHFFFAOYSA-N 0.000 description 1
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- 235000005985 organic acids Nutrition 0.000 description 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 description 1
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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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (15)
1. Fast farmaceutisk tilberedning omfattende flupirtin eller dets fysiologisk forligelige salte som aktiv ingrediens, hvor i det mindste en del af flupirtinet eller dets fysiologisk forligelige salte er til stede som en aktiv ingrediensformulering med en forsinket frisætning af aktiv ingrediens, kendetegnet ved, at a. den aktive ingrediensformulering med forsinket aktiv ingrediensfrisætning indbefatter aktive ingredienskompaktater, som fortrinsvis er jævnt dækket med en forsinkelseskomponent og indbefatter almindelige farmaceutiske ingredienser om nødvendigt, således at en jævn frisætning af flupirtinet ud af kompaktaterne garanteres, og b. det aktive ingredienskompaktat har en partikelstørrelse på 160 til 800 pm, fortrinsvis 250 til 500 pm, og er fortrinsvis sfæriske eller omtrent sfæriske.
2. Farmaceutisk tilberedning ifølge krav 1, kendetegnet ved, at de aktive ingredienskompaktater har en rumvægt på mindre end 5 ml/g, fortrinsvis mindre end 3 ml/g, og mere foretrukket mindre end 2,5 ml/g og mest foretrukket mellem 0,8 og 2,5 ml/g.
3. Farmaceutisk tilberedning ifølge et af kravene 1 eller 2, kendetegnet ved, at forsinkelseskomponenterne sikrer en diffusionskontrolleret frisætning af den aktive ingrediens.
4. Farmaceutisk tilberedning ifølge et af kravene 1 til 3, kendetegnet ved, at forsinkelseskomponenten indbefatter en forsinkende polymerfilm og eventuelt almindelige farmaceutiske excipienser fortrinsvis frisætningsmidler og pigmenter om nødvendigt, hvor den forsinkende polymerfilm fortrinsvis indbefatter mindst en polymer eller copolymer fremstillet af acrylsyre, acrylsyrederivater, methacryl-syre og/eller methacrylsyrederivater eller en blanding heraf.
5. Farmaceutisk tilberedning ifølge krav 4, kendetegnet ved, at i den aktive ingrediensformulering med forsinket aktiv ingrediensfrisætning er forholdet i vægtandele af forsinkende polymerfilm til flupirtin eller dets fysiologisk forligelige salte mellem 0,001 og 20, fortrinsvis mellem 0,01 og 10 og mest foretrukket mellem 0,05 og 0,1.
6. Farmaceutisk tilberedning ifølge et af kravene 1 til 5, kendetegnet ved, at in vitro frisættes flupirtin eller dets fysiologisk forligelige salte inden for 240 minutter mellem 35 og 75 procent, fortrinsvis inden for 15 minutter mellem 15 og 35 procent, mere foretrukket inden for 240 minutter mellem 55 og 75 procent, og inden for 600 minutter 75 procent.
7. Farmaceutisk tilberedning ifølge et af kravene 1 til 6, kendetegnet ved, at en del af flupirtinet eller dets fysiologisk forligelige salte er til stede som en aktiv ingrediensformulering med umiddelbar frisætning af aktiv ingrediens.
8. Farmaceutisk tilberedning ifølge krav 7, kendetegnet ved, at forholdet mellem flupirtin som en aktiv ingrediensformulering med forsinket aktiv ingrediens-frisætning og flupirtin som en aktiv ingrediensformulering med umiddelbar aktiv ingrediensfrisætning er mellem 1 til 2 og 9 til 1, fortrinsvis 3 til 1.
9. Farmaceutisk tilberedning ifølge et af kravene 1 til 8, kendetegnet ved, at den er til stede i form af tabletter, filmovertrukne tabletter, hårde gelatinekapsler, bløde gelatinekapsler, pellets, granulat, overtrukne tabletter eller mikrokapsler.
10. Farmaceutisk tilberedning ifølge et af kravene 1 til 9, kendetegnet ved, at den yderligere indbefatter mindst en ekstern fasekomponent.
11. Farmaceutisk tilberedning ifølge krav 10, kendetegnet ved, at den eksterne fasekomponent indbefatter natrium-crosscarmellose, mikrokrystallinsk cellulose, højdispergeret siliciumdioxid, magnesiumstearat, cellulose i pulverform, calcium-hydrogenphosphatdihydrat, lactose, mannitol og/eller stivelse eller blandinger heraf.
12. Farmaceutisk tilberedning ifølge et af kravene 1 til 11, kendetegnet ved, at den er delelig.
13. Fremgangsmåde til fremstilling af en farmaceutisk tilberedning ifølge et af kravene 1 til 12, kendetegnet ved, at a. flupirtin eller dets fysiologisk forligelige salte kompakteres til aktive ingre-dienskompaktater med de farmaceutisk almene additiver om nødvendigt, b. aktive ingredienskompaktater med en partikelstørrelse på 160 til 800 pm separeres fra, og c. de separerede aktive ingredienskompaktater dækkes med en forsinkelseskomponent.
14. Fremgangsmåde ifølge krav 13, kendetegnet ved, at ved anvendelse afen forsinkelseskomponent med stærkt klæbende tilbøjeligheder, følger dernæst et overtræk med et frisættelsesmiddel, således at fejl i overtrækket undgås.
15. Fremgangsmåde ifølge krav 13 eller 14, kendetegnet ved, at i de aktive ingredienskompaktater forarbejdes yderligere med tilsætning af eksterne fasekomponenter om nødvendigt til en farmaceutisk tilberedning fortrinsvis til tabletter, filmovertrukne tabletter, hårde gelatinekapsler, bløde gelatinekapsler, pellets, granulat, overtrukne tabletter eller mikrokapsler eller suppositorier på farmaceutisk sædvanlig vis.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005054610A DE102005054610B4 (de) | 2005-11-08 | 2005-11-08 | Flupirtin enthaltende Arzneimittelzubereitung mit kontrollierter Wirkstofffreisetzung |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DK1795186T3 DK1795186T3 (da) | 2014-01-27 |
| DK1795186T4 true DK1795186T4 (da) | 2018-03-05 |
Family
ID=37908079
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK06022985.3T DK1795186T4 (da) | 2005-11-08 | 2006-11-04 | Flupirtinomfattende lægemiddelformulering med en kontrolleret frisætning af det aktive middel |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP1795186B2 (da) |
| CY (1) | CY1115709T1 (da) |
| DE (1) | DE102005054610B4 (da) |
| DK (1) | DK1795186T4 (da) |
| ES (1) | ES2443468T5 (da) |
| PL (1) | PL1795186T5 (da) |
| PT (1) | PT1795186E (da) |
| RU (1) | RU2352338C2 (da) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8222282B2 (en) | 2008-06-09 | 2012-07-17 | Teva Pharmaceuticals Usa, Inc. | Sulfonate salts of 2-amino-3-carbethoxyamino-6-(4-fluoro-benzylamino)-pyridine |
| US8183267B2 (en) | 2008-06-09 | 2012-05-22 | Awd. Pharma Gmbh & Co. Kg | Carboxylic acid salts of 2-amino-3-carbethoxyamino-6-(4-fluoro-benzylamino)-pyridine |
| DE102008051783A1 (de) * | 2008-10-17 | 2010-04-22 | Tiefenbacher Pharmachemikalien Alfred E. Tiefenbacher Gmbh & Co. Kg | Valsartan enthaltende Tablette |
| AR087501A1 (es) | 2011-08-09 | 2014-03-26 | Hydra Biosciences Inc | Compuestos inhibidores del canal ionico del potencial receptor transitorio trpa1 |
| WO2013127539A2 (de) * | 2012-03-02 | 2013-09-06 | Meda Pharma Gmbh & Co. Kg | Pharmazeutische formulierungen |
| US20140163048A1 (en) * | 2012-08-09 | 2014-06-12 | Cubist Pharmaceuticals, Inc. | Compositions with increased stability for inhibiting transient receptor potential ion channel trpa1 |
| US9394308B2 (en) | 2013-01-18 | 2016-07-19 | Merck Sharp & Dohme Corp. | Inhibiting the transient receptor potential A1 ion channel |
| DE102013014417A1 (de) | 2013-08-29 | 2015-03-05 | Klinipharm Gmbh | Schwammkollagen umfassende Zubereitungen mit definiertem in vivo-Freisetzungsprofil vor allem im Colon, deren Herstellung und Verwendung |
| CN109806233B (zh) * | 2017-11-21 | 2022-05-20 | 北京泰德制药股份有限公司 | 一种含有氟吡汀或其药用盐的组合物及其制备方法 |
| RU2680244C1 (ru) * | 2017-12-28 | 2019-02-19 | Общество С Ограниченной Ответственностью "Валента-Интеллект" | Комбинации флупиртина и циклобензаприна для лечения болевых синдромов |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3416609A1 (de) * | 1984-05-05 | 1985-11-07 | Degussa Ag, 6000 Frankfurt | 2-amino-3-ethoxycarbonylamino-6-(p-fluor-benzylamino)- pyridin-gluconat und pharmazeutische zubereitungen, die diese substanz enthalten |
| DE4319649A1 (de) * | 1993-03-18 | 1994-09-22 | Asta Medica Ag | Feste Flupirtin enthaltende orale Darreichungsformen mit kontrollierter Wirkstoffabgabe |
| AUPN605795A0 (en) * | 1995-10-19 | 1995-11-09 | F.H. Faulding & Co. Limited | Analgesic pharmaceutical composition |
| US7985422B2 (en) * | 2002-08-05 | 2011-07-26 | Torrent Pharmaceuticals Limited | Dosage form |
| DE10328260A1 (de) * | 2003-06-23 | 2005-01-27 | Schmidt, K.-G., Dr. med. | Flupirtine-Präparat |
| US20060240043A1 (en) * | 2004-10-08 | 2006-10-26 | Meyerson Laurence R | Methods and compositions for treating migraine pain |
-
2005
- 2005-11-08 DE DE102005054610A patent/DE102005054610B4/de not_active Expired - Fee Related
-
2006
- 2006-11-04 ES ES06022985.3T patent/ES2443468T5/es active Active
- 2006-11-04 DK DK06022985.3T patent/DK1795186T4/da active
- 2006-11-04 EP EP06022985.3A patent/EP1795186B2/de active Active
- 2006-11-04 PT PT60229853T patent/PT1795186E/pt unknown
- 2006-11-04 PL PL06022985T patent/PL1795186T5/pl unknown
- 2006-11-07 RU RU2006139127/15A patent/RU2352338C2/ru not_active IP Right Cessation
-
2014
- 2014-01-23 CY CY20141100058T patent/CY1115709T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2006139127A (ru) | 2008-05-20 |
| EP1795186A2 (de) | 2007-06-13 |
| PT1795186E (pt) | 2014-01-22 |
| PL1795186T5 (pl) | 2018-05-30 |
| CY1115709T1 (el) | 2017-01-25 |
| ES2443468T3 (es) | 2014-02-19 |
| ES2443468T5 (es) | 2018-03-26 |
| EP1795186B2 (de) | 2017-12-06 |
| DK1795186T3 (da) | 2014-01-27 |
| EP1795186B1 (de) | 2013-10-23 |
| DE102005054610B4 (de) | 2010-06-10 |
| EP1795186A3 (de) | 2007-10-24 |
| DE102005054610A1 (de) | 2007-07-12 |
| RU2352338C2 (ru) | 2009-04-20 |
| PL1795186T3 (pl) | 2014-05-30 |
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