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CA2616531A1 - Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation - Google Patents

Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation Download PDF

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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
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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
Application number
CA002616531A
Other languages
French (fr)
Other versions
CA2616531C (en
Inventor
Gudrun Claus-Herz
Christoph Kessler
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bausch and Lomb Inc
Original Assignee
Individual
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2616531A1 publication Critical patent/CA2616531A1/en
Application granted granted Critical
Publication of CA2616531C publication Critical patent/CA2616531C/en
Active legal-status Critical Current
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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic 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.
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.-%.
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.
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.
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.
CA2616531A 2005-07-28 2006-07-24 Sterile, drop-forming, multiphase, emulsifier-free ophthalmic preparation Active CA2616531C (en)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Cited By (2)

* Cited by examiner, † Cited by third party
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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