DK2965749T3 - Nanopartikelsuspensioner indeholdende carboxyvinylpolymer - Google Patents
Nanopartikelsuspensioner indeholdende carboxyvinylpolymer Download PDFInfo
- Publication number
- DK2965749T3 DK2965749T3 DK15179323.9T DK15179323T DK2965749T3 DK 2965749 T3 DK2965749 T3 DK 2965749T3 DK 15179323 T DK15179323 T DK 15179323T DK 2965749 T3 DK2965749 T3 DK 2965749T3
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- nepafenac
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- 229920002125 Sokalan® Polymers 0.000 title claims abstract description 47
- 239000000725 suspension Substances 0.000 title abstract description 21
- 239000002105 nanoparticle Substances 0.000 title description 4
- 239000000203 mixture Substances 0.000 claims abstract description 96
- QEFAQIPZVLVERP-UHFFFAOYSA-N nepafenac Chemical compound NC(=O)CC1=CC=CC(C(=O)C=2C=CC=CC=2)=C1N QEFAQIPZVLVERP-UHFFFAOYSA-N 0.000 claims abstract description 42
- 229960001002 nepafenac Drugs 0.000 claims abstract description 40
- 229920000926 Galactomannan Polymers 0.000 claims abstract description 24
- 150000001875 compounds Chemical class 0.000 claims abstract description 18
- OMDQUFIYNPYJFM-XKDAHURESA-N (2r,3r,4s,5r,6s)-2-(hydroxymethyl)-6-[[(2r,3s,4r,5s,6r)-4,5,6-trihydroxy-3-[(2s,3s,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]methoxy]oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O[C@H]2[C@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)[C@H](O)[C@H](O)[C@H](O)O1 OMDQUFIYNPYJFM-XKDAHURESA-N 0.000 claims abstract description 17
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims abstract description 13
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- 239000011780 sodium chloride Substances 0.000 claims description 6
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical group [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims description 5
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 5
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- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical group [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 4
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Classifications
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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Claims (15)
1. Topisk indgivelig vandig opthalmisk suspensionssammensætning omfattende: en carboxyvinylpolymer i en koncentration på 0,1 til 0,5 vægt/volumen%; en galactomannan i en koncentration på 0,1 til 0,4 vægt/volumen%; borat i en koncentration på 0,4 til 2,0 vægt/volumen%; og en svagt opløselig partikelformet forbindelse, hvilken forbindelse har en opløselighed i vand ved 25°C på 0,001 til 0,1 vægt/volumen%.
2. Sammensætning ifølge krav 1, som yderligere omfatter et pH-justerende middel i en mængde, som er tilstrækkelig til at forårsage, at sammensætningen haren pH på 5,0 til 7,2.
3. Sammensætning ifølge krav 1, som yderligere omfatter et tonicitets-justerende middel i en mængde, som er tilstrækkelig til at forårsage, at sammensætningen haren osmolalitet på 250 til 350 mOsm/kg.
4. Sammensætning ifølge krav 1, hvor den svagt opløselige partikelformede forbindelse er nepafenac i en koncentration på 0,1 til 1,0 vægt/volumen%.
5. Sammensætning ifølge krav 1, hvor den nævnte carboxyvinylpolymer er carbomer i en koncentration på 0,4 vægt/volumen%.
6. Sammensætning ifølge krav 1, som yderligere omfatter et formalingsmiddel i en koncentration på 0,005 til 0,1 vægt/volumen%, hvor formalingsmidlet er valgt blandt tyloxapol, polysorbat 80 og natriumcarboxymethylcellulose, fortrinsvis hvor formalingsmidlet er natriumcarboxymethylcellulose.
7. Sammensætning ifølge krav 1, som yderligere omfatter et metalchloridsalt-tonicitet-justeringsmiddel, fortrinsvis natriumchlorid i en koncentration på 0,4 vægt/volumen%.
8. Sammensætning ifølge krav 1, som yderligere omfatter en ikke-ionisk hydroxyl-forbindelse som et tonicitet-justeringsmiddel.
9. Sammensætning ifølge krav 1, som yderligere omfatter såvel et konserveringsmiddel som en chelatdanner.
10. Sammensætning ifølge krav 9, hvor konserveringsmidlet er benzalkoniumchlorid i en koncentration på 0,005 vægt/volumen% og chelatdanneren er edetatdinatrium i en koncentration på 0,01 vægt/volumen%.
11. Sammensætning ifølge krav 1, hvor carboxyvinylpolymeren er carbomer, galacto-mannanet er guar, boratet er borsyre og den svagt opløselige partikelformede forbindelse er nepafenac i en koncentration på 0,1 til 1,0 vægt/volumen%.
12. Sammensætning ifølge krav 11, omfattende 0,4 vægt/volumen% carbomer, 0,2 vægt/volumen% guar, 0,5 vægt/volumen% borsyre og 0,3 vægt/volumen% nepafenac.
13. Sammensætning ifølge krav 12, hvor det nævnte nepafenac har en gennemsnitlig partikelstørrelse på 400 nm.
14. Sammensætning ifølge krav 1 til anvendelse ved en fremgangsmåde til behandling af ophthalmiske lidelser hos en patient, omfattende topisk indgivelse til patienten af sammensætningen.
15. Fremgangsmåde til opretholdelse af viskositeten for en topisk ophthalmisk sammensætning omfattende 0,1 til 0,5 vægt/volumen% carbomer, når sammensætningen påføres topisk på øjet, hvilken fremgangsmåde omfatter: tilføjelse af galactomannan i tilstrækkelig mængde til tilvejebringelse af en koncentration på 0,1 vægt/volumen% til 0,4 vægt/volumen% galactomannan i sammensætningen, og borat i en tilstrækkelig mængde til tilvejebringelse af en koncentration på 0,4 vægt/volumen% til 0,6 vægt/volumen% i sammensætningen.
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| EP13152584.2A EP2586426B1 (en) | 2009-12-03 | 2010-12-01 | Carboxyvinyl polymer-containing nanoparticle suspensions |
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| DK13152584.2T DK2586426T3 (da) | 2009-12-03 | 2010-12-01 | Carboxyvinylpolymer-holdige nanopartikelsuspensioner |
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Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8435631B2 (en) * | 2010-04-15 | 2013-05-07 | Ppg Industries Ohio, Inc. | Microporous material |
| PT2596072E (pt) * | 2010-07-20 | 2014-09-02 | C Ip S A | Suspensão de um composto de boro |
| TW201336527A (zh) * | 2012-02-10 | 2013-09-16 | Alcon Res Ltd | 具增強的穩定性之水性藥學組成物 |
| MX2015002208A (es) * | 2012-08-31 | 2015-05-08 | Bausch & Lomb | Composiciones oftalmicas con acidos grasos omega-3. |
| WO2014207769A1 (en) | 2013-06-27 | 2014-12-31 | Mylan Laboratories Ltd | Process for the preparation of nepafenac |
| US20150191647A1 (en) * | 2014-01-07 | 2015-07-09 | Trican Well Service Ltd. | Stability of viscous fluids in low salinity environments |
| EP3470059B1 (en) | 2015-01-26 | 2020-04-01 | Bausch & Lomb Incorporated | Ophthalmic suspension composition |
| WO2016205574A1 (en) * | 2015-06-18 | 2016-12-22 | Common Pharma, Inc | Antimicrobial formulations |
| US11730699B2 (en) | 2018-02-21 | 2023-08-22 | Alcon Inc. | Lipid-based ophthalmic emulsion |
| TWI884130B (zh) * | 2018-02-21 | 2025-05-21 | 瑞士商愛爾康公司 | 基於脂質的眼用乳劑 |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3864183A (en) * | 1972-11-21 | 1975-02-04 | Tokyo Hat | Method for producing pen core from filament tows |
| US4313949A (en) | 1979-09-26 | 1982-02-02 | A. H. Robins Company, Inc. | Method of producing an inhibitory effect on blood platelet aggregation |
| IL80298A (en) | 1986-10-14 | 1993-01-31 | Res & Dev Co Ltd | Eye drops |
| US5192535A (en) | 1988-02-08 | 1993-03-09 | Insite Vision Incorporated | Ophthalmic suspensions |
| US5188826A (en) * | 1988-02-08 | 1993-02-23 | Insite Vision Incorporated | Topical ophthalmic suspensions |
| US5461081A (en) * | 1989-09-28 | 1995-10-24 | Alcon Laboratories, Inc. | Topical ophthalmic pharmaceutical vehicles |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| US5429824A (en) | 1992-12-15 | 1995-07-04 | Eastman Kodak Company | Use of tyloxapole as a nanoparticle stabilizer and dispersant |
| US5475034A (en) * | 1994-06-06 | 1995-12-12 | Alcon Laboratories, Inc. | Topically administrable compositions containing 3-benzoylphenylacetic acid derivatives for treatment of ophthalmic inflammatory disorders |
| FR2761959B1 (fr) * | 1997-04-15 | 1999-05-21 | Oreal | Ensemble de conditionnement et d'application d'un produit fluide |
| DE69839355T2 (de) | 1997-07-29 | 2009-06-04 | Alcon Laboratories, Inc., Fort Worth | Ophthalmische Zusammensetzungen enthaltend Galaktomannanpolymere und Borat |
| IT1306123B1 (it) | 1999-04-02 | 2001-05-30 | Technopharma Sa | Soluzione oftalmica viscosizzata con azione detergente sulle lenti acontatto. |
| ITMI991453A1 (it) | 1999-07-01 | 2001-01-01 | Farmila Farma Milano | Composizioni oftalmiche in forma di gel acquosi |
| CN1402629A (zh) | 1999-12-23 | 2003-03-12 | 辉瑞产品公司 | 提供提高的药物浓度的药物组合物 |
| PE20020146A1 (es) | 2000-07-13 | 2002-03-31 | Upjohn Co | Formulacion oftalmica que comprende un inhibidor de ciclooxigenasa-2 (cox-2) |
| PE20020578A1 (es) | 2000-10-10 | 2002-08-14 | Upjohn Co | Una composicion de antibiotico topico para el tratamiento de infecciones oculares |
| TNSN03137A1 (en) | 2001-06-22 | 2005-12-23 | Pfizer Prod Inc | PHARMACEUTICAL COMPOSITIONS COMPRISING LOW SOLUBILITY AND / OR ACID SENSITIVE DRUGS AND NEUTRALIZED ACID POLYMERS. |
| EP1448209A2 (en) | 2001-10-23 | 2004-08-25 | Ranbaxy Laboratories, Ltd. | A process for the preparation of pharmaceutical compositions for topical delivery of cyclooxygenase-2 enzyme inhibitors |
| US7045121B2 (en) | 2001-12-14 | 2006-05-16 | Allergan, Inc. | Ophthalmic compositions for lubricating eyes and methods for making and using same |
| MXPA04008171A (es) * | 2002-02-22 | 2004-11-26 | Pharmacia Corp | Formulacion oftalmica con sistema de goma. |
| TWI336257B (en) * | 2003-06-13 | 2011-01-21 | Alcon Inc | Ophthalmic compositions containing a synergistic combination of three polymers |
| US7947295B2 (en) | 2003-06-13 | 2011-05-24 | Alcon, Inc. | Ophthalmic compositions containing a synergistic combination of two polymers |
| EP1654002B2 (en) | 2003-08-07 | 2014-01-29 | Allergan, Inc. | Compositions for delivery of therapeutics into the eyes |
| FR2865648B1 (fr) | 2004-02-03 | 2006-06-30 | Philippe Perovitch | Procede de diffusion de molecules insolubles en milieu aqueux et composition mettant en oeuvre ce procede |
| TWI358290B (en) | 2004-12-02 | 2012-02-21 | Alcon Inc | Topical nepafenac formulations |
| WO2006062875A1 (en) | 2004-12-08 | 2006-06-15 | Merck & Co., Inc. | Ophthalmic nanoparticulate formulation of a cyclooxygenase-2 selective inhibitor |
| TWI393567B (zh) | 2005-03-31 | 2013-04-21 | Bausch & Lomb | 治療乾眼之組合物及相關之製造方法及使用方法 |
| JP4257860B2 (ja) * | 2005-04-19 | 2009-04-22 | 中得工業株式会社 | 化粧材の塗布具 |
| BRPI0609227A2 (pt) * | 2005-05-10 | 2010-03-09 | Alcon Inc | composições de suspensão de nepafenac e outros fármacos oftálmicos, bem como uso das referidas composições no tratamento tópico de distúrbios oftálmicos |
| DK1906916T3 (da) * | 2005-05-10 | 2009-01-19 | Alcon Inc | Oftalmisk suspension, der omfatter et oftalmisk lægemiddel, en poloxamin og et tonicitetsregulerende glycolbaseret middel, anvendelse af sammensætningen til fremstilling af et medikament til behandling af oftalmiske lidelser |
| AU2006254825A1 (en) | 2005-06-08 | 2006-12-14 | Targegen, Inc. | Methods and compositions for the treatment of ocular disorders |
| JP5112669B2 (ja) * | 2005-09-30 | 2013-01-09 | 富山化学工業株式会社 | 難溶性薬物のナノ微粒子を含有する水性懸濁液剤 |
| WO2007058935A2 (en) | 2005-11-14 | 2007-05-24 | Bausch & Lomb Incorporated | Ophthalmic composition for dry eye therapy |
| US20080039398A1 (en) | 2006-01-25 | 2008-02-14 | Ousler George W Iii | Formulations and methods for treating dry eye |
| US20070297981A1 (en) | 2006-01-25 | 2007-12-27 | Ousler George W Iii | Formulations and methods for treating dry eye |
| US20070254841A1 (en) | 2006-01-25 | 2007-11-01 | Ophthalmic Research Associates, Inc. | Formulations and methods for treating dry eye |
| US20070299124A1 (en) | 2006-01-25 | 2007-12-27 | Ousler George W Iii | Formulations and methods for treating dry eye |
| WO2008002485A2 (en) | 2006-06-23 | 2008-01-03 | Alza Corporation | Increased amorphous stability of poorly water soluble drugs by nanosizing |
| US20080260837A1 (en) | 2007-04-20 | 2008-10-23 | Qpharma, L.L.C. | Physically stable aqueous suspensions of active pharmaceuticals |
| WO2008153746A1 (en) | 2007-05-24 | 2008-12-18 | Aciex Therapeutics, Inc. | Formulations and methods for treating dry eye |
| BRPI0910717A2 (pt) * | 2008-04-26 | 2015-09-29 | Alcon Res Ltd | sistema polimérico de lágrima artificial |
| JP4395189B1 (ja) * | 2008-08-29 | 2010-01-06 | 株式会社ソリトン | 塗布具 |
| EP2393837A1 (en) * | 2009-02-05 | 2011-12-14 | Alcon Research, Ltd. | Process for purifying guar |
| JP5716960B2 (ja) * | 2011-05-23 | 2015-05-13 | オーベクス株式会社 | 塗布体用素材の製造方法及び塗布体用素材並びに塗布体及び塗布具 |
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