CA2616531A1 - Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation - Google Patents
Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation Download PDFInfo
- Publication number
- CA2616531A1 CA2616531A1 CA002616531A CA2616531A CA2616531A1 CA 2616531 A1 CA2616531 A1 CA 2616531A1 CA 002616531 A CA002616531 A CA 002616531A CA 2616531 A CA2616531 A CA 2616531A CA 2616531 A1 CA2616531 A1 CA 2616531A1
- Authority
- CA
- Canada
- Prior art keywords
- sterile
- forming
- emulsifier
- multiphase
- drop
- 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.)
- Granted
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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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- 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
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Ophthalmology & Optometry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to a sterile, drop-forming, multi-phase, emulsifier-free ophthalmic product, in particular a gel product, comprising at least one liquid aqueous phase and at least one liquid hydrophobic phase, the product comprising at least one phosphate salt and having a viscosity in the range from > 200 mPa.s to < 2000 mPa.s.
Claims (26)
1. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation, in particular gel preparation, comprising at least one liquid aqueous phase and at least one liquid hydrophobic phase, characterised in that the preparation comprises at least one phosphate salt and has a viscosity in the range of >= 200 mPa.cndot.s to <= 2000 mPa.cndot.s, determined by the cone/plate-method ("Platte-Kegel-Verfahren") at 20°C.
2. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to claim 1, characterised in that the viscosity is in the range of >= 300 mPa.cndot.s to <= 1800 mPa.cndot.s, preferably in the range of >= 400 mPa.cndot.s to <= 1500 mPa.cndot.s, preferably in the range of >= 500 mPa.cndot.s to <= 1400 mPa.cndot.s, especially preferred in the range of >= 600 mPa.cndot.s to <= 1350 mPa.cndot.s, in particular preferred in the range of >= 650 mPa.cndot.s to <= 1300 mPa.cndot.s.
3. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to claims 1 or 2, characterised in that a water-soluble phosphate salt is selected from the group comprising alkali phosphate salts, alkaline-earth phosphate salts, ammonium phosphate salts, mono- or dihydrogen phosphates thereof and/or mixtures thereof, preferably selected from the group comprising sodium dihydrogen phosphate, sodium monohydrogen phosphate, potassium dihydrogen phosphate, potassium monohydrogen phosphate and/or mixtures thereof.
4. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises Na2HPO4 ×
12 H2O in the range of >= 0.01 wt.-% to <= 5.0 wt.-%, based on the total weight of the composition, preferably in the range of >= 0.05 wt.-% to <= 0.5 wt.-%, preferably in the range of >= 0.08 wt.-% to <= 0.2 wt.-%, especially preferred comprises about 0.1 wt.-% of Na2HPO4 × 12 H2O.
12 H2O in the range of >= 0.01 wt.-% to <= 5.0 wt.-%, based on the total weight of the composition, preferably in the range of >= 0.05 wt.-% to <= 0.5 wt.-%, preferably in the range of >= 0.08 wt.-% to <= 0.2 wt.-%, especially preferred comprises about 0.1 wt.-% of Na2HPO4 × 12 H2O.
5. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises the aqueous phase as continuous phase and the hydrophobic phase as droplets dispersed therein.
6. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises at least one polymeric gel-forming component, preferably a polyacrylic acid and/or a polymeric acrylic acid derivative, preferably a carbomer.
7. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises an ophthalmic acceptable organic oil, preferably a triglyceride, preferably a mid-chain triglyceride.
8. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises at least one ophthalmic active agent, preferably a vitamin A component, preferably vitamin A palmitate, especially preferred in combination with an antioxidant, such as vitamin E.
9. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises sorbitol.
10. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises sodium hydroxide.
11. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises preservatives, preferably selected from the group comprising cetrimide, benzododecinium chloride, benzalkonium chloride, alexidine and/or thiomersal, preferably selected from the group comprising cetrimide and/or alexidine.
12. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises glycerol, preferably in the range of >= 0.01 wt.-% to <= 1.0 wt.-%, based on the total weight of the preparation, preferably in the range of >= 0.1 wt.-% to <= 0.5 wt.-%, preferably in the range of >=
0.2 wt.-% to <= 0.3 wt.-%.
0.2 wt.-% to <= 0.3 wt.-%.
13. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation has an osmolality in the range of >= 100 mosmol/kg to <= 500 mosmol/kg, preferably in the range of >= 200 mosmol/kg to <= 300 mosmol/kg, preferably in the range of >= 220 mosmol/kg to <= 260 mosmol/kg.
14. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation has a pH value in the range of >= 6 to <= 8, preferably in the range of >= 6.8 to <= 7.2.
15. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises substances selected from the group comprising polyacrylic acid, polymeric acrylic acid derivatives, preferably carbomers, triglycerides, preferably mid-chain triglycerides, water-soluble phosphate salts, preferably Na2HPO4 × 12 H2O, a vitamin A component, preferably vitamin A
palmitate, vitamin E, preferably D,L-.alpha.-tocopherol, sorbitol, sodium hydroxide, preservatives, preferably cetrimide, benzododecinium chloride, benzalkonium chloride or alexidine, glycerol and/or water.
palmitate, vitamin E, preferably D,L-.alpha.-tocopherol, sorbitol, sodium hydroxide, preservatives, preferably cetrimide, benzododecinium chloride, benzalkonium chloride or alexidine, glycerol and/or water.
16. Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims, characterised in that the preparation comprises the following substances, based on the total weight of the preparation:
a. 0.2 wt.-% polymeric acrylic acid;
b. 4.0 wt.-% sorbitol;
c. 0.1 wt.-% Na2HPO4 × 12 H2O;
d. 0.0665 wt.-% sodium hydroxide;
e. 1.0 wt.-% mid-chain triglycerides;
f. ad 100 wt.-% water.
a. 0.2 wt.-% polymeric acrylic acid;
b. 4.0 wt.-% sorbitol;
c. 0.1 wt.-% Na2HPO4 × 12 H2O;
d. 0.0665 wt.-% sodium hydroxide;
e. 1.0 wt.-% mid-chain triglycerides;
f. ad 100 wt.-% water.
17. Method of preparing a sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of claims 1 to 16, characterised in that a liquid hydrophobic phase, in particular a mid-chain triglyceride, is homogeneously dispersed into a continuous aqueous phase, in particular a sterile hydrogel previously prepared.
18. Method of preparing a preparation according to claim 17, characterised in that a polyacrylic acid and/or a polymeric acrylic acid derivative, preferably a carbomer is used, which is converted for gel-forming by neutralisation of the carboxyl groups with a suitable base, in particular sodium hydroxide solution.
19. Method of preparing a preparation according to claims 17 or 18, characterised in that at least one water-soluble phosphate salt is added to the aqueous phase.
20. Method of preparing a preparation according to any one of the preceding claims, characterised in that an active agent, preferably vitamin A, is added under aseptic conditions and homogeneously mixed into the sterile preparation.
21. Use of a sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims for the preparation of a cosmetic and/or pharmaceutical preparation for the treatment of diseases or conditions of the eye or the organs or tissues surrounding the eye or being connected therewith, in particular of dry eye.
22. Preparation for the treatment of diseases or conditions of the eye or organs or tissues surrounding the eye or being connected therewith, in particular in the form of a gel preparation, comprising substances in accordance with any one of the preceding claims.
23. Single-dose container comprising a sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims.
24. Single-dose container according to claim 23, characterised in that the ophthalmic preparation is free of preservatives.
25. Multiple-dose container comprising a sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation according to any one of the preceding claims.
26. Multiple-dose container according to claim 25, characterised in that the ophthalmic preparation is free of preservatives.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102005035986A DE102005035986B4 (en) | 2005-07-28 | 2005-07-28 | Sterile drippable multiphase emulsifier-free ophthalmic preparation |
DE102005035986.8 | 2005-07-28 | ||
PCT/EP2006/064557 WO2007012625A1 (en) | 2005-07-28 | 2006-07-24 | Sterile, drop-forming, multi-phase, emulsifier-free ophthalmic product |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2616531A1 true CA2616531A1 (en) | 2007-02-01 |
CA2616531C CA2616531C (en) | 2011-02-08 |
Family
ID=37416192
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2616531A Active CA2616531C (en) | 2005-07-28 | 2006-07-24 | Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation |
Country Status (11)
Country | Link |
---|---|
EP (1) | EP1915128B1 (en) |
JP (1) | JP5349963B2 (en) |
CN (1) | CN101227891A (en) |
AT (1) | ATE423545T1 (en) |
BR (1) | BRPI0616013A2 (en) |
CA (1) | CA2616531C (en) |
DE (2) | DE102005035986B4 (en) |
ES (1) | ES2321875T3 (en) |
MX (1) | MX2008001040A (en) |
RU (1) | RU2414887C2 (en) |
WO (1) | WO2007012625A1 (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9278062B2 (en) | 2009-09-30 | 2016-03-08 | Rohto Pharmaceutical Co., Ltd. | Eye drops |
US11413304B2 (en) * | 2016-04-15 | 2022-08-16 | Dr. Gerhard Mann Chem.-Pharm. Fabrik Gmbh | Storage-stable ophthalmic composition |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE102006049091A1 (en) * | 2006-10-18 | 2008-04-24 | Dr. Gerhard Mann Chem.-Pharm. Fabrik Gmbh | Emulsifier-free ophthalmic preparation containing vegetable oil |
US9308165B2 (en) * | 2013-08-22 | 2016-04-12 | Therapeutic Vision, Inc. | Composition for treating ocular effects of diabetes |
SG11202010742UA (en) * | 2018-05-01 | 2020-11-27 | Chibi Inc | Liquid depot for non-invasive sustained delivery of agents to the eye |
CN111035615B (en) * | 2020-01-15 | 2022-03-11 | 欧普康视科技股份有限公司 | Gel type hard contact lens lubricating liquid |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3440352A1 (en) * | 1984-11-05 | 1986-05-07 | Dr. Thilo & Co GmbH, 8029 Sauerlach | Dry-eye packing |
SE9401108D0 (en) * | 1994-03-31 | 1994-03-31 | Leiras Oy | Ophthalmic composition I |
SE9401109D0 (en) * | 1994-03-31 | 1994-03-31 | Leiras Oy | Opthalmic composition II |
DE19511322C2 (en) * | 1995-03-28 | 1999-09-02 | Mann Gerhard Chem Pharm Fab | Sterile eye gels containing medium chain triglycerides and process for their preparation |
AU5601598A (en) * | 1996-12-10 | 1998-07-03 | Children's Medical Center Corporation | Improved hydrogel composition |
AU4602399A (en) * | 1998-06-30 | 2000-01-24 | Leo Pharmaceutical Products Ltd. A/S (Lovens Kemiske Fabrik Produktionsaktieselskab) | Prolonged release ophthalmic compositions containing a fluoroquinolone |
AR034371A1 (en) * | 2001-06-08 | 2004-02-18 | Novartis Ag | PHARMACEUTICAL COMPOSITIONS |
DE10161149B4 (en) * | 2001-12-12 | 2007-03-08 | Ursapharm Arzneimittel Gmbh & Co. Kg | Use of heparin-containing ophthalmic agent |
US7074827B2 (en) * | 2002-10-24 | 2006-07-11 | Sucampo Ag (Usa) Inc. | Method for treating ocular hypertension and glaucoma |
-
2005
- 2005-07-28 DE DE102005035986A patent/DE102005035986B4/en not_active Expired - Fee Related
-
2006
- 2006-07-24 WO PCT/EP2006/064557 patent/WO2007012625A1/en active Application Filing
- 2006-07-24 CA CA2616531A patent/CA2616531C/en active Active
- 2006-07-24 DE DE502006002962T patent/DE502006002962D1/en active Active
- 2006-07-24 RU RU2008107308/15A patent/RU2414887C2/en active
- 2006-07-24 JP JP2008523342A patent/JP5349963B2/en active Active
- 2006-07-24 EP EP06777917A patent/EP1915128B1/en active Active
- 2006-07-24 AT AT06777917T patent/ATE423545T1/en not_active IP Right Cessation
- 2006-07-24 MX MX2008001040A patent/MX2008001040A/en active IP Right Grant
- 2006-07-24 CN CNA200680027112XA patent/CN101227891A/en active Pending
- 2006-07-24 BR BRPI0616013-1A patent/BRPI0616013A2/en not_active IP Right Cessation
- 2006-07-24 ES ES06777917T patent/ES2321875T3/en active Active
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9278062B2 (en) | 2009-09-30 | 2016-03-08 | Rohto Pharmaceutical Co., Ltd. | Eye drops |
US11413304B2 (en) * | 2016-04-15 | 2022-08-16 | Dr. Gerhard Mann Chem.-Pharm. Fabrik Gmbh | Storage-stable ophthalmic composition |
Also Published As
Publication number | Publication date |
---|---|
DE502006002962D1 (en) | 2009-04-09 |
ES2321875T3 (en) | 2009-06-12 |
EP1915128A1 (en) | 2008-04-30 |
CN101227891A (en) | 2008-07-23 |
RU2414887C2 (en) | 2011-03-27 |
JP2009502866A (en) | 2009-01-29 |
DE102005035986B4 (en) | 2009-10-15 |
CA2616531C (en) | 2011-02-08 |
WO2007012625A8 (en) | 2007-04-19 |
JP5349963B2 (en) | 2013-11-20 |
MX2008001040A (en) | 2008-03-19 |
ATE423545T1 (en) | 2009-03-15 |
WO2007012625A1 (en) | 2007-02-01 |
DE102005035986A1 (en) | 2007-02-08 |
EP1915128B1 (en) | 2009-02-25 |
BRPI0616013A2 (en) | 2011-05-31 |
RU2008107308A (en) | 2009-09-10 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
EEER | Examination request |