HRP20110025T1 - FARMACEUTSKA FORMULACIJA NITROOKSIDERIVATA NSAID-a - Google Patents
FARMACEUTSKA FORMULACIJA NITROOKSIDERIVATA NSAID-a Download PDFInfo
- Publication number
- HRP20110025T1 HRP20110025T1 HR20110025T HRP20110025T HRP20110025T1 HR P20110025 T1 HRP20110025 T1 HR P20110025T1 HR 20110025 T HR20110025 T HR 20110025T HR P20110025 T HRP20110025 T HR P20110025T HR P20110025 T1 HRP20110025 T1 HR P20110025T1
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- Croatia
- Prior art keywords
- image
- formula
- pharmaceutical formulation
- compound
- formulation according
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract 17
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 title claims abstract 10
- 150000001875 compounds Chemical class 0.000 claims abstract 16
- 239000004094 surface-active agent Substances 0.000 claims abstract 11
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims abstract 9
- 229910004679 ONO2 Inorganic materials 0.000 claims abstract 8
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims abstract 6
- 125000003031 C5-C7 cycloalkylene group Chemical group 0.000 claims abstract 2
- 239000002253 acid Substances 0.000 claims abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims abstract 2
- 125000003262 carboxylic acid ester group Chemical class [H]C([H])([*:2])OC(=O)C([H])([H])[*:1] 0.000 claims abstract 2
- 125000005843 halogen group Chemical group 0.000 claims abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 125000006850 spacer group Chemical group 0.000 claims abstract 2
- 125000001424 substituent group Chemical group 0.000 claims abstract 2
- ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-aminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 claims 10
- 229960004050 aminobenzoic acid Drugs 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical group C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 3
- 239000007787 solid Substances 0.000 claims 3
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims 2
- 229920001992 poloxamer 407 Polymers 0.000 claims 2
- 229940044476 poloxamer 407 Drugs 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 238000004140 cleaning Methods 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- -1 fatty acid alcohols Chemical class 0.000 claims 1
- 239000002736 nonionic surfactant Substances 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 229960000502 poloxamer Drugs 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000002840 nitric oxide donor Substances 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- 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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Farmaceutska formulacija naznačena time da sadrži: a) jedan ili više NO-otpuštajućih NSAID-a formule (I); b) jedan ili više surfaktanata pri čemu je omjer surfaktant: NO- otpuštajući NSAID je od 0.1:1 do 10:1; c) spoj za čišćenje karbonila odabran od slobodnih oblika kiseline, soli, derivata estera karboksilne kiseline spoja prema formuli (II) H2N-(CH2)m-(C6H4)-COOH (II) pri čemu m = 0-10 pri čemu je količina spoja prema formuli (II) od oko 0.01% do oko 5% težinski od ukupne težine pripravka; pri čemu u formuli (I) M je odabran iz skupine koja se sastoji od X je razmaknica, npr. spoj koji tvori most između skupine koja donira dušikov oksid i NSAID-a, te je odabrana od i) ravnog ili razgranatog C1-C20 alkilena, poželjno C1-C10, koji je proizvoljno supstituiran sa jednim ili više supstituenata odabranih iz skupine koja se sastoji od: atoma halogena, hidroksi, -ONO2 ili T, pri čemu T je -OC(O)(C1-C10 alkil)-ONO2 ili -O(C1-C10 alkil)-ONO2;ii) C5-C7 cikloalkilenska skupina proizvoljno supstituirana sa linearnom ili razgranatom C1-C10 alkilnom skupinom, poželjno CH3;iii) pri čemu n je cijeli broj od 0 do 20, poželjno n je cijeli broj od 0 do 5; in1 je cijeli broj od 1 do 20, poželjno n1 je cijeli broj od 1 do 5; pod uvjetom da -ONO2 skupina prema formuli (I) je vezana na -(CH2)n1; iiv) pri čemu X2 je -O- ili -S-;n3 je cijeli broj od 1 do 6, poželjno od 1 do 4, i R2 je H ili CH3.Patent sadrži još 14 patentnih zahtjeva.
Claims (15)
1. Farmaceutska formulacija naznačena time da sadrži:
a) jedan ili više NO-otpuštajućih NSAID-a formule (I);
[image]
b) jedan ili više surfaktanata pri čemu je omjer surfaktant: NO- otpuštajući NSAID je od 0.1:1 do 10:1;
c) spoj za čišćenje karbonila odabran od slobodnih oblika kiseline, soli, derivata estera karboksilne kiseline spoja prema formuli (II)
H2N-(CH2)m-(C6H4)-COOH (II)
pri čemu m = 0-10 pri čemu je količina spoja prema formuli (II) od oko 0.01% do oko 5% težinski od ukupne težine pripravka;
pri čemu u formuli (I)
M je odabran iz skupine koja se sastoji od
[image]
[image]
[image]
[image]
[image]
X je razmaknica, npr. spoj koji tvori most između skupine koja donira dušikov oksid i NSAID-a, te je odabrana od
i) ravnog ili razgranatog C1-C20 alkilena, poželjno C1-C10, koji je proizvoljno supstituiran sa jednim ili više supstituenata odabranih iz skupine koja se sastoji od: atoma halogena, hidroksi, -ONO2 ili T, pri čemu T je -OC(O)(C1-C10 alkil)-ONO2 ili -O(C1-C10 alkil)-ONO2;
ii) C5-C7 cikloalkilenska skupina proizvoljno supstituirana sa linearnom ili razgranatom C1-C10 alkilnom skupinom, poželjno CH3;
iii)
[image]
pri čemu n je cijeli broj od 0 do 20, poželjno n je cijeli broj od 0 do 5; i
n1 je cijeli broj od 1 do 20, poželjno n1 je cijeli broj od 1 do 5; pod uvjetom da -ONO2 skupina prema formuli (I) je vezana na -(CH2)n1; i
iv)
[image]
[image]
pri čemu X2 je -O- ili -S-;
n3 je cijeli broj od 1 do 6, poželjno od 1 do 4,
i R2 je H ili CH3.
2. Farmaceutska formulacija prema zahtjevu 1 naznačena time da količina spoja formule (II) je od oko 0.01% do oko 2% težinski od ukupne težine pripravka.
3. Farmaceutska formulacija prema zahtjevu 1 ili 2 naznačena time da količina spoja formule (II) je od oko 0.01% do oko 1% težinski od ukupne težine pripravka.
4. Farmaceutska formulacija prema bilo kojem od zahtjeva 1 do 3, naznačena time da je omjer surfaktant: NO-otpuštajući NSAID je od 0.3:1 do 3:1.
5. Farmaceutska formulacija, prema bilo kojem od zahtjeva 1 do 4, naznačena time da surfaktant je ne-ionski surfaktant.
6. Farmaceutska formulacija, prema zahtjevu 5, naznačena time da surfaktant je poloksamer.
7. Farmaceutska formulacija prema bilo kojem od zahtjeva 1 do 6, naznačena time da spoj formule (II) je p-aminobenzojeva kiselina.
8. Farmaceutska formulacija prema bilo kojem od zahtjeva 1 do 7 naznačena time da također sadrži ulje ili polu-krutu mast i/ili alkohol kratkog lanca.
9. Farmaceutska formulacija prema zahtjevu 8 naznačena time da polu-kruta mast je odabrana od mono-, di- i triglicerida i alkohola masne kiseline.
10. Farmaceutska formulacija prema zahtjevu 8 naznačena time da alkohol kratkog lanca je linearni ili razgranati mono-, di- ili tri-alkohol koji ima 1-6 atoma ugljika.
11. Farmaceutska formulacija prema bilo kojem od zahtjeva 1 do 10 naznačena time da NO-otpuštajući NSAID prema formuli (I) je odabran iz skupine koja se sastoji od:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
12. Farmaceutska formulacija prema bilo kojem od zahtjeva 1, 3, 4, 5 i 7 naznačena time da NO-otpuštajući NSAID prema formuli (I) je spoj formule (Ia)
[image]
13. Farmaceutska formulacija prema zahtjevu 12 naznačena time da
b) surfaktant je poloksamer 407 i omjer surfaktant: spoj (Ia) je 0.6;
c) spoj formule (II) je p-aminobenzojeva kiselina i količina p-aminobenzojeve kiseline je oko 0.1% težinski od ukupne težine pripravka.
14. Farmaceutska formulacija prema zahtjevu 12 naznačena time da
b) surfaktant je poloksamer 407 i omjer surfaktant: spoj (Ia) je 0.6;
c) spoj formule (II) je p-aminobenzojeva kiselina i količina p-aminobenzojeve kiseline je oko 0.5% težinski od ukupne težine pripravka.
15. Farmaceutska formulacija prema bilo kojem od zahtjeva 12 do 14 naznačena time da također sadrži ulje ili polu-krutu mast i/ili alkohol kratkog lanca
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05106854 | 2005-07-26 | ||
| PCT/EP2006/063672 WO2007012539A2 (en) | 2005-07-26 | 2006-06-29 | Pharmaceutical formulation of nitrooxyderivatives of nsaids |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20110025T1 true HRP20110025T1 (hr) | 2011-03-31 |
Family
ID=37670077
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110025T HRP20110025T1 (hr) | 2005-07-26 | 2011-01-13 | FARMACEUTSKA FORMULACIJA NITROOKSIDERIVATA NSAID-a |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8691869B2 (hr) |
| EP (1) | EP1906938B1 (hr) |
| JP (1) | JP5238499B2 (hr) |
| KR (1) | KR101342910B1 (hr) |
| CN (1) | CN101227896B (hr) |
| AR (1) | AR055094A1 (hr) |
| AT (1) | ATE485033T1 (hr) |
| AU (1) | AU2006274098B2 (hr) |
| CA (1) | CA2616508C (hr) |
| CY (1) | CY1112023T1 (hr) |
| DE (1) | DE602006017701D1 (hr) |
| DK (1) | DK1906938T3 (hr) |
| ES (1) | ES2354278T3 (hr) |
| HK (1) | HK1120414A1 (hr) |
| HR (1) | HRP20110025T1 (hr) |
| IL (1) | IL188253A0 (hr) |
| MX (1) | MX2008001213A (hr) |
| NO (1) | NO20080983L (hr) |
| NZ (1) | NZ564589A (hr) |
| PL (1) | PL1906938T3 (hr) |
| PT (1) | PT1906938E (hr) |
| RU (1) | RU2406482C2 (hr) |
| SI (1) | SI1906938T1 (hr) |
| WO (1) | WO2007012539A2 (hr) |
| ZA (1) | ZA200801009B (hr) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011209757A (ja) * | 2011-07-06 | 2011-10-20 | Rohto Pharmaceutical Co Ltd | コンタクトレンズケア方法及び組成物 |
| US9688607B2 (en) * | 2011-08-15 | 2017-06-27 | Research Foundation Of The City University Of New York | No- and H2S-releasing compounds |
| US20130225529A1 (en) * | 2012-02-27 | 2013-08-29 | Basil Rigas | Phospho-ester derivatives and uses thereof |
| RU2657803C1 (ru) * | 2017-03-21 | 2018-06-15 | федеральное государственное бюджетное образовательное учреждение высшего образования "Алтайский государственный университет" | Средство, обладающее противовоспалительным и анальгезирующим действием |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1925697A (en) * | 1996-03-12 | 1997-10-01 | Novartis Ag | Filled gelatin capsules having a reduced degree of cross-linking |
| TWI243672B (en) * | 1999-06-01 | 2005-11-21 | Astrazeneca Ab | New use of compounds as antibacterial agents |
| SE0000774D0 (sv) * | 2000-03-08 | 2000-03-08 | Astrazeneca Ab | New formulation |
| SE0000773D0 (sv) * | 2000-03-08 | 2000-03-08 | Astrazeneca Ab | New formulation |
| ES2524000T3 (es) * | 2002-06-05 | 2014-12-03 | Teva Czech Industries S.R.O. | Reducción de la reticulación de la gelatina |
| JP2005538993A (ja) * | 2002-07-31 | 2005-12-22 | ファルマシア・コーポレーション | 薄膜を形成しにくいゼラチンカプセル |
-
2006
- 2006-06-29 SI SI200630878T patent/SI1906938T1/sl unknown
- 2006-06-29 EP EP06777502A patent/EP1906938B1/en active Active
- 2006-06-29 ES ES06777502T patent/ES2354278T3/es active Active
- 2006-06-29 WO PCT/EP2006/063672 patent/WO2007012539A2/en active Application Filing
- 2006-06-29 PL PL06777502T patent/PL1906938T3/pl unknown
- 2006-06-29 CN CN2006800272160A patent/CN101227896B/zh not_active Expired - Fee Related
- 2006-06-29 CA CA2616508A patent/CA2616508C/en active Active
- 2006-06-29 AU AU2006274098A patent/AU2006274098B2/en not_active Ceased
- 2006-06-29 NZ NZ564589A patent/NZ564589A/en not_active IP Right Cessation
- 2006-06-29 AT AT06777502T patent/ATE485033T1/de active
- 2006-06-29 DE DE602006017701T patent/DE602006017701D1/de active Active
- 2006-06-29 DK DK06777502.3T patent/DK1906938T3/da active
- 2006-06-29 RU RU2008104505/15A patent/RU2406482C2/ru active
- 2006-06-29 MX MX2008001213A patent/MX2008001213A/es active IP Right Grant
- 2006-06-29 JP JP2008523286A patent/JP5238499B2/ja active Active
- 2006-06-29 US US11/997,094 patent/US8691869B2/en active Active
- 2006-06-29 PT PT06777502T patent/PT1906938E/pt unknown
- 2006-07-25 AR ARP060103209A patent/AR055094A1/es unknown
-
2007
- 2007-12-19 IL IL188253A patent/IL188253A0/en not_active IP Right Cessation
-
2008
- 2008-01-04 KR KR1020087000268A patent/KR101342910B1/ko not_active IP Right Cessation
- 2008-01-30 ZA ZA200801009A patent/ZA200801009B/xx unknown
- 2008-02-25 NO NO20080983A patent/NO20080983L/no unknown
- 2008-11-06 HK HK08112198.7A patent/HK1120414A1/xx not_active IP Right Cessation
-
2011
- 2011-01-07 CY CY20111100026T patent/CY1112023T1/el unknown
- 2011-01-13 HR HR20110025T patent/HRP20110025T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN101227896A (zh) | 2008-07-23 |
| DE602006017701D1 (de) | 2010-12-02 |
| EP1906938B1 (en) | 2010-10-20 |
| JP2009502850A (ja) | 2009-01-29 |
| AU2006274098B2 (en) | 2012-02-09 |
| HK1120414A1 (en) | 2009-04-03 |
| RU2406482C2 (ru) | 2010-12-20 |
| IL188253A0 (en) | 2008-04-13 |
| CN101227896B (zh) | 2013-02-06 |
| NZ564589A (en) | 2010-01-29 |
| PT1906938E (pt) | 2011-01-17 |
| WO2007012539A3 (en) | 2007-04-19 |
| EP1906938A2 (en) | 2008-04-09 |
| MX2008001213A (es) | 2008-03-24 |
| US8691869B2 (en) | 2014-04-08 |
| ES2354278T3 (es) | 2011-03-11 |
| WO2007012539A2 (en) | 2007-02-01 |
| DK1906938T3 (da) | 2011-02-07 |
| ATE485033T1 (de) | 2010-11-15 |
| NO20080983L (no) | 2008-02-25 |
| AR055094A1 (es) | 2007-08-08 |
| AU2006274098A1 (en) | 2007-02-01 |
| JP5238499B2 (ja) | 2013-07-17 |
| KR101342910B1 (ko) | 2013-12-19 |
| PL1906938T3 (pl) | 2011-05-31 |
| RU2008104505A (ru) | 2009-09-10 |
| CA2616508A1 (en) | 2007-02-01 |
| CA2616508C (en) | 2015-02-24 |
| KR20080028412A (ko) | 2008-03-31 |
| US20090203759A1 (en) | 2009-08-13 |
| SI1906938T1 (sl) | 2011-02-28 |
| CY1112023T1 (el) | 2015-11-04 |
| ZA200801009B (en) | 2008-11-26 |
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