MD3769753T2 - Procedeu de preparare a suspensiilor de nanocristale de propionat de fluticazonă Forma A apoase oftalmice sterile - Google Patents
Procedeu de preparare a suspensiilor de nanocristale de propionat de fluticazonă Forma A apoase oftalmice sterileInfo
- Publication number
- MD3769753T2 MD3769753T2 MDE20210297T MDE20210297T MD3769753T2 MD 3769753 T2 MD3769753 T2 MD 3769753T2 MD E20210297 T MDE20210297 T MD E20210297T MD E20210297 T MDE20210297 T MD E20210297T MD 3769753 T2 MD3769753 T2 MD 3769753T2
- Authority
- MD
- Moldova
- Prior art keywords
- fluticasone propionate
- nanocrystals
- aqueous
- nanosuspension
- suspension
- Prior art date
Links
- WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical group C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 title claims abstract description 199
- 239000002159 nanocrystal Substances 0.000 title claims abstract description 144
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- 229960000289 fluticasone propionate Drugs 0.000 claims abstract description 112
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 128
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 72
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- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 50
- 239000008135 aqueous vehicle Substances 0.000 claims description 43
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 claims description 43
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- OVBJJZOQPCKUOR-UHFFFAOYSA-L EDTA disodium salt dihydrate Chemical compound O.O.[Na+].[Na+].[O-]C(=O)C[NH+](CC([O-])=O)CC[NH+](CC([O-])=O)CC([O-])=O OVBJJZOQPCKUOR-UHFFFAOYSA-L 0.000 claims description 27
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- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 claims description 9
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- GNFTZDOKVXKIBK-UHFFFAOYSA-N 3-(2-methoxyethoxy)benzohydrazide Chemical compound COCCOC1=CC=CC(C(=O)NN)=C1 GNFTZDOKVXKIBK-UHFFFAOYSA-N 0.000 claims description 4
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- BBMHARZCALWXSL-UHFFFAOYSA-M sodium dihydrogenphosphate monohydrate Chemical compound O.[Na+].OP(O)([O-])=O BBMHARZCALWXSL-UHFFFAOYSA-M 0.000 claims description 3
- 238000001816 cooling Methods 0.000 claims description 2
- 229940061607 dibasic sodium phosphate Drugs 0.000 claims description 2
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
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Classifications
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- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/569—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
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- 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
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| US201962877599P | 2019-07-23 | 2019-07-23 | |
| US201962942551P | 2019-12-02 | 2019-12-02 |
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| MD3769753T2 true MD3769753T2 (ro) | 2022-04-30 |
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| EP3769753B1 (en) * | 2019-07-23 | 2021-11-17 | Nicox Ophthalmics, Inc. | Process for the preparation of sterile ophthalmic aqueous fluticasone propionate form a nanocrystals suspensions |
| CN115887372A (zh) * | 2022-10-25 | 2023-04-04 | 苏州欧康维视生物科技有限公司 | 丙酸氟替卡松混悬液及其制备方法 |
| CN115554238A (zh) * | 2022-10-25 | 2023-01-03 | 苏州欧康维视生物科技有限公司 | 眼用混悬液及其制备方法 |
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| AU674852B2 (en) * | 1992-05-06 | 1997-01-16 | Alcon Laboratories, Inc. | Use of borate-polyol complexes in ophthalmic compositions |
| JP3450805B2 (ja) * | 2000-08-08 | 2003-09-29 | わかもと製薬株式会社 | 水性医薬組成物 |
| US6900184B2 (en) * | 2003-04-14 | 2005-05-31 | Wyeth Holdings Corporation | Compositions containing pipercillin and tazobactam useful for injection |
| US20060229219A1 (en) * | 2005-04-11 | 2006-10-12 | Advanced Medical Optics, Inc. | Borate-polyol mixtures as a buffering system |
| US8010032B2 (en) * | 2005-05-23 | 2011-08-30 | Xerox Corporation | Fuser member comprising deflocculated material |
| US20110105450A1 (en) * | 2009-06-05 | 2011-05-05 | Aciex Therapeutics, Inc. | Ophthalmic formulations of fluticasone and methods of use |
| TWI489997B (zh) | 2009-06-19 | 2015-07-01 | Alcon Res Ltd | 含有硼酸－多元醇錯合物之水性藥學組成物 |
| WO2013025696A1 (en) | 2011-08-15 | 2013-02-21 | Teva Pharmaceutical Industries Ltd. | Ophthalmic formulations and processes for their preparation |
| ES2727474T3 (es) * | 2012-05-08 | 2019-10-16 | Nicox Ophthalmics Inc | Nanocristales de propionato de fluticasona |
| JP6294893B2 (ja) * | 2012-12-17 | 2018-03-14 | グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ | 炎症性及び／又はアレルギー性の状態を治療するためのレボカバスチンとフルチカゾンフランカルボン酸エステルとの併用 |
| TWI773641B (zh) | 2015-05-08 | 2022-08-11 | 日商活效製藥股份有限公司 | 含有糖皮質類固醇（ｇｌｕｃｏｃｏｒｔｉｃｏｉｄｓ）之奈米微粒子之水性懸浮液劑 |
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