CA2481394A1 - Preparation ophthalmologique en gel formant des gouttes et contenant de la diclofenamide et du timolol - Google Patents
Preparation ophthalmologique en gel formant des gouttes et contenant de la diclofenamide et du timolol Download PDFInfo
- Publication number
- CA2481394A1 CA2481394A1 CA002481394A CA2481394A CA2481394A1 CA 2481394 A1 CA2481394 A1 CA 2481394A1 CA 002481394 A CA002481394 A CA 002481394A CA 2481394 A CA2481394 A CA 2481394A CA 2481394 A1 CA2481394 A1 CA 2481394A1
- Authority
- CA
- Canada
- Prior art keywords
- composition according
- ophthalmic composition
- gel
- diclofenamide
- timolol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 47
- GJQPMPFPNINLKP-UHFFFAOYSA-N diclofenamide Chemical compound NS(=O)(=O)C1=CC(Cl)=C(Cl)C(S(N)(=O)=O)=C1 GJQPMPFPNINLKP-UHFFFAOYSA-N 0.000 title claims abstract description 31
- 229960005081 diclofenamide Drugs 0.000 title claims abstract description 31
- TWBNMYSKRDRHAT-RCWTXCDDSA-N (S)-timolol hemihydrate Chemical compound O.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1 TWBNMYSKRDRHAT-RCWTXCDDSA-N 0.000 title claims abstract description 22
- 229960004605 timolol Drugs 0.000 title claims abstract description 22
- 229940100655 ophthalmic gel Drugs 0.000 title claims description 4
- 239000000203 mixture Substances 0.000 claims abstract description 38
- 206010030348 Open-Angle Glaucoma Diseases 0.000 claims abstract description 7
- 206010030043 Ocular hypertension Diseases 0.000 claims abstract description 4
- 201000006366 primary open angle glaucoma Diseases 0.000 claims abstract description 3
- 229920002125 Sokalan® Polymers 0.000 claims description 13
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 9
- 239000002253 acid Substances 0.000 claims description 8
- 230000004410 intraocular pressure Effects 0.000 claims description 7
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical class OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 5
- 239000004584 polyacrylic acid Substances 0.000 claims description 5
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 4
- 239000000654 additive Substances 0.000 claims description 4
- 239000003755 preservative agent Substances 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- 239000002585 base Substances 0.000 claims description 3
- JBIROUFYLSSYDX-UHFFFAOYSA-M benzododecinium chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 JBIROUFYLSSYDX-UHFFFAOYSA-M 0.000 claims description 3
- 229960004074 benzododecinium chloride Drugs 0.000 claims description 3
- 229920003086 cellulose ether Polymers 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 239000012458 free base Substances 0.000 claims description 3
- 230000004089 microcirculation Effects 0.000 claims description 3
- 239000002245 particle Substances 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 2
- 150000007513 acids Chemical class 0.000 claims description 2
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 2
- 150000004676 glycans Chemical class 0.000 claims description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 claims description 2
- 239000011707 mineral Substances 0.000 claims description 2
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims description 2
- 229920001282 polysaccharide Polymers 0.000 claims description 2
- 239000005017 polysaccharide Substances 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 230000002335 preservative effect Effects 0.000 claims description 2
- 239000000945 filler Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000499 gel Substances 0.000 description 53
- 239000000725 suspension Substances 0.000 description 19
- 239000004480 active ingredient Substances 0.000 description 18
- 230000000694 effects Effects 0.000 description 14
- 208000010412 Glaucoma Diseases 0.000 description 12
- 239000000243 solution Substances 0.000 description 10
- 229910052783 alkali metal Inorganic materials 0.000 description 9
- -1 alkali metal salts Chemical class 0.000 description 9
- 230000002411 adverse Effects 0.000 description 7
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 description 7
- 230000000699 topical effect Effects 0.000 description 5
- 238000010521 absorption reaction Methods 0.000 description 4
- 239000002997 ophthalmic solution Substances 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 230000002035 prolonged effect Effects 0.000 description 3
- 206010015946 Eye irritation Diseases 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 230000004406 elevated intraocular pressure Effects 0.000 description 2
- 231100000013 eye irritation Toxicity 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000011159 matrix material Substances 0.000 description 2
- 210000002850 nasal mucosa Anatomy 0.000 description 2
- 210000001331 nose Anatomy 0.000 description 2
- 230000000704 physical effect Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 230000002195 synergetic effect Effects 0.000 description 2
- 230000009885 systemic effect Effects 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 235000016068 Berberis vulgaris Nutrition 0.000 description 1
- 241000335053 Beta vulgaris Species 0.000 description 1
- 201000004569 Blindness Diseases 0.000 description 1
- 208000028006 Corneal injury Diseases 0.000 description 1
- 101710200331 Cytochrome b-245 chaperone 1 Proteins 0.000 description 1
- 102100037186 Cytochrome b-245 chaperone 1 Human genes 0.000 description 1
- 101710119396 Cytochrome b-245 chaperone 1 homolog Proteins 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 241001505295 Eros Species 0.000 description 1
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- 102000004867 Hydro-Lyases Human genes 0.000 description 1
- 108090001042 Hydro-Lyases Proteins 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 230000003276 anti-hypertensive effect Effects 0.000 description 1
- CYDRXTMLKJDRQH-UHFFFAOYSA-N benzododecinium Chemical class CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 CYDRXTMLKJDRQH-UHFFFAOYSA-N 0.000 description 1
- 239000002876 beta blocker Substances 0.000 description 1
- 229960001631 carbomer Drugs 0.000 description 1
- 230000004087 circulation Effects 0.000 description 1
- 210000000795 conjunctiva Anatomy 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- IAVUPMFITXYVAF-XPUUQOCRSA-N dorzolamide Chemical compound CCN[C@H]1C[C@H](C)S(=O)(=O)C2=C1C=C(S(N)(=O)=O)S2 IAVUPMFITXYVAF-XPUUQOCRSA-N 0.000 description 1
- 229960003933 dorzolamide Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 210000000744 eyelid Anatomy 0.000 description 1
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 description 1
- 239000006260 foam Substances 0.000 description 1
- 239000000017 hydrogel Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000007803 itching Effects 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 229940100654 ophthalmic suspension Drugs 0.000 description 1
- 210000001328 optic nerve Anatomy 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 238000009827 uniform distribution Methods 0.000 description 1
Classifications
-
- 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
- A61K31/18—Sulfonamides
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La présente invention concerne une composition ophthalmologique se présentant sous forme de préparation en gel formant des gouttes et contenant de la diclofenamide se présentant sous sa forme libre et du timolol. L'invention concerne également l'utilisation de telles préparations en gel formant des gouttes pour traiter l'hypertension oculaire et les glaucomes à angle ouvert primaires et secondaires.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2002/005738 WO2003099258A1 (fr) | 2002-05-24 | 2002-05-24 | Preparation ophthalmologique en gel formant des gouttes et contenant de la diclofenamide et du timolol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2481394A1 true CA2481394A1 (fr) | 2003-12-04 |
Family
ID=29558277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002481394A Abandoned CA2481394A1 (fr) | 2002-05-24 | 2002-05-24 | Preparation ophthalmologique en gel formant des gouttes et contenant de la diclofenamide et du timolol |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1507513A1 (fr) |
| AU (1) | AU2002325220A1 (fr) |
| CA (1) | CA2481394A1 (fr) |
| WO (1) | WO2003099258A1 (fr) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10183076B2 (en) | 2005-05-16 | 2019-01-22 | Resdevco Research And Development Co. L | Topical compositions for treatment of irritation of mucous membranes |
| USRE49758E1 (en) | 2012-01-23 | 2023-12-19 | Novaliq Gmbh | Stabilised protein compositions based on semifluorinated alkanes |
| US12128010B2 (en) | 2015-09-30 | 2024-10-29 | Novaliq Gmbh | Semifluorinated compounds and their compositions |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL168603A (en) * | 2005-05-16 | 2011-05-31 | Resdevco Res And Dev Co | Pharmaceutical or cosmetic composition for the prevention and treatment of irritation of mucous cells or skin cells |
| ES2564502T3 (es) | 2010-03-17 | 2016-03-23 | Novaliq Gmbh | Composición farmacéutica para el tratamiento de la presión intraocular aumentada |
| EP2895144B1 (fr) | 2012-09-12 | 2017-01-11 | Novaliq GmbH | Compositions d'alcane semifluoré |
| AU2017329983B2 (en) | 2016-09-23 | 2022-05-05 | Novaliq Gmbh | Ophthalmic compositions comprising ciclosporin |
| JP7814839B2 (ja) | 2017-09-27 | 2026-02-17 | ノバリック ゲーエムベーハー | 眼疾患の治療に使用するためのラタノプロストを含む眼科用組成物 |
| CN111182893A (zh) | 2017-10-04 | 2020-05-19 | 诺瓦利克有限责任公司 | 包含f6h8的眼用组合物 |
| US11576893B2 (en) | 2018-03-02 | 2023-02-14 | Novaliq Gmbh | Pharmaceutical compositions comprising nebivolol |
| AU2019246035B2 (en) * | 2018-03-28 | 2024-07-18 | Novaliq Gmbh | Pharmaceutical composition comprising timolol |
| JP7855312B2 (ja) | 2018-04-27 | 2026-05-08 | ノバリック ゲーエムベーハー | 緑内障の治療のためのタフルプロストを含む眼科用組成物 |
| EP3923907B1 (fr) | 2019-02-13 | 2024-09-25 | Novaliq GmbH | Compositions et procédés pour le traitement de la néovascularisation oculaire |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ192673A (en) * | 1979-02-02 | 1984-07-06 | Merck & Co Inc | Ophthalmic compositions for lowering intraocular pressure |
| EP0033042B1 (fr) * | 1980-01-28 | 1984-08-22 | Merck & Co. Inc. | Inserts ophtalmiques d'inhibiteurs d'anhydrase carbonique pour l'application topique dans le traitement d'hypertension intraoculaire |
| US4678855A (en) * | 1985-10-09 | 1987-07-07 | Merck & Co., Inc. | Substituted benzenesulfonamides |
| US6159458A (en) * | 1997-11-04 | 2000-12-12 | Insite Vision | Sustained release ophthalmic compositions containing water soluble medicaments |
| DK1251826T3 (da) * | 2000-01-20 | 2003-11-17 | Mann Gerhard Chem Pharm Fab | Diclofenamidsuspensionsgel |
-
2002
- 2002-05-24 WO PCT/EP2002/005738 patent/WO2003099258A1/fr not_active Ceased
- 2002-05-24 EP EP02758204A patent/EP1507513A1/fr not_active Withdrawn
- 2002-05-24 CA CA002481394A patent/CA2481394A1/fr not_active Abandoned
- 2002-05-24 AU AU2002325220A patent/AU2002325220A1/en not_active Abandoned
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10183076B2 (en) | 2005-05-16 | 2019-01-22 | Resdevco Research And Development Co. L | Topical compositions for treatment of irritation of mucous membranes |
| USRE49758E1 (en) | 2012-01-23 | 2023-12-19 | Novaliq Gmbh | Stabilised protein compositions based on semifluorinated alkanes |
| US12128010B2 (en) | 2015-09-30 | 2024-10-29 | Novaliq Gmbh | Semifluorinated compounds and their compositions |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1507513A1 (fr) | 2005-02-23 |
| WO2003099258A1 (fr) | 2003-12-04 |
| AU2002325220A1 (en) | 2003-12-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |