WO2002058668A2 - Composition de larmes artificielles adaptee pour etre utilisee avec des lentilles de contact - Google Patents

Composition de larmes artificielles adaptee pour etre utilisee avec des lentilles de contact Download PDF

Info

Publication number
WO2002058668A2
WO2002058668A2 PCT/US2001/048550 US0148550W WO02058668A2 WO 2002058668 A2 WO2002058668 A2 WO 2002058668A2 US 0148550 W US0148550 W US 0148550W WO 02058668 A2 WO02058668 A2 WO 02058668A2
Authority
WO
WIPO (PCT)
Prior art keywords
artificial tear
contact lenses
solution
rewetting drop
antimicrobial agent
Prior art date
Application number
PCT/US2001/048550
Other languages
English (en)
Other versions
WO2002058668A3 (fr
Inventor
Masood Chowhan
Original Assignee
Alcon, Inc
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 Alcon, Inc filed Critical Alcon, Inc
Priority to AU2002245134A priority Critical patent/AU2002245134A1/en
Priority to US10/415,802 priority patent/US20040028645A1/en
Priority to JP2002559002A priority patent/JP2004530644A/ja
Publication of WO2002058668A2 publication Critical patent/WO2002058668A2/fr
Publication of WO2002058668A3 publication Critical patent/WO2002058668A3/fr

Links

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
    • A61K9/0012—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
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

Definitions

  • the present invention is directed to artificial tear compositions that are formulated in a manner such as to also be capable of being utilized as a rewetting drop for contact lenses.
  • the dual function of the solutions of the present invention requires the solution to not only be effective as artificial tears, but also to be compatible with contact lenses, particularly soft contact lenses.
  • Ophthalmic solutions are sometimes used by patients in an inappropriate manner. For example, patients sometimes apply inappropriate artificial tear products to the eyes while wearing their contact lenses, or soak the lenses in a solution that is not designed to be used for this purpose. This inappropriate use of products can be either accidental or intentional. But in either case, the use of products that are not designed for treating contact lenses can result in ocular irritation, due to the uptake of preservatives or other ingredients by the lenses. An artificial tear and rewetting drop product that is specifically designed for application to contact lenses while the lenses are being worn would therefore be highly desirable.
  • rewetting drop refers to a solution that can be applied to a contact lens while it is being worn by a patient in order to lubricate the lens and re-hydrate the lens, thereby making the lens more comfortable.
  • the objective of the present invention is to provide an improved artificial tear/rewetting drop that is particularly useful in connection with soft contact lenses. More specifically, the principal objective of the present invention is to provide a novel solution that is capable of functioning effectively as an artificial tear and rewetting drop without any of the ingredients of the solution being adsorbed to the surfaces of soft contact lenses.
  • the present invention is based on the use of a citric acid/sodium citrate buffering system to prevent complexation or other uptake of antimicrobial agents or other ingredients of the present artificial tear solution by soft contact lenses.
  • the citric acid sodium citrate buffer system is combined with several other ingredients to provide a fairly complex combination of ingredients which are carefully balanced so as to provide an effective tear replacement solution that is also capable of being utilized as a rewetting drop for soft contact lenses.
  • a citric acid/sodium citrate buffer system allows the artificial tear/rewetting drop solutions of the present invention to be applied directly to contact lenses, particularly soft contact lenses.
  • this type of buffer system has been utilized previously in solutions utilized to disinfect contact lenses, it has not been used in an artificial tear product of the type described herein, that is, an artificial tear product that can be applied directly to contact lenses while the lenses are being worn and is also suitable to be used as a rewetting drop for contact lenses.
  • the artificial tear/rewetting drop solutions of the present invention will also contain one or more demulcents to facilitate hydration of the eye and an ophthalmically acceptable antimicrobial preservative.
  • the artificial tear/rewetting drop of the present invention has been developed based on several criteria.
  • a principal criterion was that the product must satisfy the preservative effectiveness standards of the United States Pharmacopoeia and Japanese Pharmacopoeia, as well as similar standards in other countries.
  • the preservative effectiveness test or "PET" standards require products to have sufficient antimicrobial activity such that there is no risk of microbial contamination of the product during the period it is being utilized by patients.
  • the use of antimicrobial agents to preserve the formulation from microbial contamination creates a problem.
  • the use of antimicrobial agents in solutions to be applied to contact lenses creates a risk that patients' eyes will become irritated due to the antimicrobial agent becoming bound to contact lenses, adsorbed to the surfaces of the lenses, absorbed within porous contact lens materials, or otherwise taken up by soft contact lenses.
  • This potential problem which is generally referred to herein as involving an "uptake" of the antimicrobial agent by the contact lens, is particularly significant in the event the product is to be applied to the contact lenses while being worn, rather than simply being utilized to rinse or wash the contact lenses when removed from the eyes.
  • a second major criterion for the solution of the present invention was the need to provide a solution that imitates the effect of natural tear fluid in lubricating and hydrating the cornea, without interfering with the comfort of contact lenses while being worn.
  • the above-stated objectives have been achieved by combining a citric acid/sodium citrate buffer system with demulcents and an ophthalmically acceptable, cationic antimicrobial preservative.
  • the buffer system prevents uptake (i.e., binding, adsorption and/or absorption) of the cationic antimicrobial agent by soft contact lenses, and thereby eliminates the risk of ocular irritation when the artificial tear/rewetting drop is applied directly to the contact lenses.
  • the concentration of the citric acid/sodium citrate buffer system required for the above- described purpose will depend on various factors, such as the particular cationic antimicrobial agent selected and the concentration of antimicrobial agent being utilized.
  • concentration of the buffer system required to eliminate or significantly reduce uptake of the antimicrobial agent by contact lenses is referred to herein as "an effective amount”.
  • concentration of the buffer system will generally be in the range of from about 0.25 weight/volume percent ("w/v %") to about 0.65 w/v %.
  • the demulcents utilized in the present invention include all of those known in the art of artificial tear products.
  • the preferred demulcent agents are hydroxypropyl methylcellulose ("HPMC"), glycols and dextrans.
  • HPMC hydroxypropyl methylcellulose
  • various other agents known to provide a demulcent effect and facilitate hydration of the eye may also be utilized. These agents also provide a cushioning effect, thereby increasing the comfort of the contact lenses on the eyes.
  • the amount of demulcent required to facilitate hydration of the eye and provide a cushioning effect will vary depending on the particular demulcent selected.
  • the concentration required for the foregoing purposes is referred to herein as "an effective amount”.
  • the concentration will generally be in the range of from about 0.01 w/v % to about 5 w/v %.
  • the preferred concentration ranges for particular demulcents are as follows:
  • HEC Hydroxyethyl cellulose
  • HPMC Hydroxypropyl methylcellulose
  • Polyethylene glycol 300 0.2 - 1 w/v %
  • Polyethylene glycol 400 0.2 - 1 w/v %
  • demulcents may be utilized either alone or in combination with one or more other demulcents.
  • HPMC and dextran 70 are particularly preferred.
  • the cationic antimicrobial preservatives utilized in the present invention are selected from the group consisting of polymeric quaternary ammonium compounds and polymeric biguanides.
  • the preferred antimicrobial preservatives are polyquaternium-1 and polyhexamethylene biguanide ("PHMB"). Polyquaternium-1 is most preferred.
  • the cationic antimicrobial agents described above will be utilized in an amount effective to prevent the artificial tear/rewetting drop solutions of the present invention from becoming contaminated by microorganisms. Such an amount is referred to herein as a "preservative effective amount”.
  • the concentration of the antimicrobial agent will be dependent on the particular antimicrobial agent selected and the concentration of the citric acid/sodium citrate buffer system.
  • the general concentration range will be 0.00001 to 0.01 w/v %.
  • the preferred solutions of the present invention will contain polyquaternium-1 in at a concentration of from about 0.0001 to 0.005 w/v %.
  • the artificial tear/rewetting drop formulations of the present invention are aqueous solutions and are formulated to be isotonic, relative to human tear fluid.
  • the solutions will generally have an osmolality in the range of from about 200 to 400 milliosmoles/kilogram water ("mOsm/kg”), preferably from about 280 mOsm/kg to about 320 mOsm/kg.
  • mOsm/kg milliosmoles/kilogram water
  • the solutions are also formulated to have a physiologically compatible pH.
  • Example 1 Formulation of Preferred Embodiment Formulation
  • Citric acid monohydrate 0.021
  • Container II a. boric acid b. mannitol c. sodium chloride d. sodium citrate e. citric acid f. dextran 70 g. disodium edetate h. polyquaternium-1 With continuous stirring, dissolve above chemicals until solution is clear.
  • the artificial tear/rewetting drop formulation described in Example 1 above was tested to determine if it meets PET standards of the United States Pharmacopoeia and Japanese Pharmacopoeia.
  • the formulation was tested in accordance with the procedures described in the United States Pharmacopoeia, 24 th Edition (2000), Section 51, pages 1809-1811.
  • the preservative system of the solution was determined to be effective against gram positive (Staphylococcus aureus) and gram negative (Escherichia coli, Pseudomonas aeruginosa) bacteria, yeast (Candida albicans) and mold (Aspergillus niger).
  • Two samples of the formulation were tested (i.e., Lot Number 1 and Lot Number 2).
  • the test data are shown in Tables 1 and 2 below.

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une solution aqueuse de larmes artificielles/gouttes lubrifiantes. Cette solution peut être utilisée à la fois comme larmes artificielles pour des personnes portant des lentilles de contact et comme gouttes lubrifiantes pour des lentilles de contact. Ladite solution est basée sur l'utilisation d'un système tampon d'acide citrique/de citrate de sodium, afin d'empêcher une liaison ou autre complexation entre des conservateurs antimicrobiens cationiques et des lentilles de contact souples, permettant ainsi d'appliquer la solution directement sur les lentilles de contact lorsque les lentilles sont portées.
PCT/US2001/048550 2000-12-21 2001-12-13 Composition de larmes artificielles adaptee pour etre utilisee avec des lentilles de contact WO2002058668A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU2002245134A AU2002245134A1 (en) 2000-12-21 2001-12-13 Artificial tear composition adapted to be used with contact lenses
US10/415,802 US20040028645A1 (en) 2001-12-13 2001-12-13 Artificial tear composition adapted to be used with contact lenses
JP2002559002A JP2004530644A (ja) 2000-12-21 2001-12-13 コンタクトレンズとの併用に適した人工涙組成物

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25757300P 2000-12-21 2000-12-21
US60/257,573 2000-12-21

Publications (2)

Publication Number Publication Date
WO2002058668A2 true WO2002058668A2 (fr) 2002-08-01
WO2002058668A3 WO2002058668A3 (fr) 2002-12-27

Family

ID=22976835

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/048550 WO2002058668A2 (fr) 2000-12-21 2001-12-13 Composition de larmes artificielles adaptee pour etre utilisee avec des lentilles de contact

Country Status (3)

Country Link
JP (1) JP2004530644A (fr)
AU (1) AU2002245134A1 (fr)
WO (1) WO2002058668A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005115475A1 (fr) * 2004-05-27 2005-12-08 Santen Pharmaceutical Co., Ltd. Épaississant à usage ophthalmique
JP2006089460A (ja) * 2004-05-27 2006-04-06 Santen Pharmaceut Co Ltd 眼科用粘稠化剤
EP3040085A4 (fr) * 2013-08-30 2017-04-19 NOF Corporation Solution ophtalmique

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4462406B2 (ja) * 2003-02-20 2010-05-12 ライオン株式会社 ソフトコンタクトレンズ取り外し液
JP5314349B2 (ja) * 2007-07-25 2013-10-16 ロート製薬株式会社 眼科用組成物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2358896A1 (fr) * 1976-07-23 1978-02-17 Alcon Lab Inc Solution ophtalmique a teneur de chlorure de benzalkonium
WO1994004134A1 (fr) * 1992-08-20 1994-03-03 Leiras Oy Preparation ophtalmologique
WO1996031195A1 (fr) * 1995-04-04 1996-10-10 Otsuka Pharmaceutical Co., Ltd. Emballage contenant une formulation de solution aqueuse de chlorhydrate de procaterol et formulation de solution aqueuse de chlorhydrate de procaterol
WO1998032421A1 (fr) * 1997-01-29 1998-07-30 Bausch & Lomb Incorporated Compositions ophtalmiques comportant de la glycerine et du propylene glycol

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2358896A1 (fr) * 1976-07-23 1978-02-17 Alcon Lab Inc Solution ophtalmique a teneur de chlorure de benzalkonium
WO1994004134A1 (fr) * 1992-08-20 1994-03-03 Leiras Oy Preparation ophtalmologique
WO1996031195A1 (fr) * 1995-04-04 1996-10-10 Otsuka Pharmaceutical Co., Ltd. Emballage contenant une formulation de solution aqueuse de chlorhydrate de procaterol et formulation de solution aqueuse de chlorhydrate de procaterol
WO1998032421A1 (fr) * 1997-01-29 1998-07-30 Bausch & Lomb Incorporated Compositions ophtalmiques comportant de la glycerine et du propylene glycol

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005115475A1 (fr) * 2004-05-27 2005-12-08 Santen Pharmaceutical Co., Ltd. Épaississant à usage ophthalmique
JP2006089460A (ja) * 2004-05-27 2006-04-06 Santen Pharmaceut Co Ltd 眼科用粘稠化剤
EP3040085A4 (fr) * 2013-08-30 2017-04-19 NOF Corporation Solution ophtalmique
AU2014313287B2 (en) * 2013-08-30 2019-05-23 Nof Corporation Ophthalmic solution

Also Published As

Publication number Publication date
WO2002058668A3 (fr) 2002-12-27
AU2002245134A1 (en) 2002-08-06
JP2004530644A (ja) 2004-10-07

Similar Documents

Publication Publication Date Title
ES2374607T3 (es) Composiciones oftálmicas con un tensioactivo anfótero y ácido hialurónico.
US4560491A (en) Soft contact lens wetting solution and in-eye comfort solution containing preservative and method
US4525346A (en) Aqueous antimicrobial ophthalmic solutions
AU721273B2 (en) Method and composition for rewetting contact lenses and relieving eye dryness
EP0180309B2 (fr) Solutions pour la désinfection et la conservation des lentilles de contact et procédés d'utilisation
US6620797B2 (en) Artificial tear composition containing a combination of three demulcents
CA2512320A1 (fr) Lentille de contact et compositions de goutte ophtalmique de rehumidification et leurs utilisations
WO2003086442A2 (fr) Preparations ophtalmiques, pharmaceutiques et de soins de sante contenant des composes, des extraits et des derives naturels d'origine vegetale
US4626292A (en) Soft contact lens wetting and preservation method
US20110230424A1 (en) Ophthalmic solutions, including contact lens care and eye drops comprising carnosine, preferably in combination with dexpanthenol and/or hyaluronic acid
CA2578242A1 (fr) Compositions contenant des tampons a base de n,n,n',n'-tetrakis(hydroxyalkyl)diamine ou de n,n,n',n'-tetrakis(hydroxyalkoxy)diamine
US20040028645A1 (en) Artificial tear composition adapted to be used with contact lenses
EP2591780B1 (fr) Formulations topiques avec un oxyde d'amine tertiaire
WO2002058668A2 (fr) Composition de larmes artificielles adaptee pour etre utilisee avec des lentilles de contact
TW548261B (en) Composition and method for inhibiting uptake of biguanide disinfectants by poly(ethylene)
EP0883408B1 (fr) Compositions a usage ophtalmologique, produits contenant cette composition et processus de desinfection et/ou de nettoyage de lentilles de contact
JP2006000170A (ja) コンタクトレンズ用組成物
RU2755298C1 (ru) Раствор для ухода за контактными линзами
JPS6169023A (ja) 防腐剤を含有するソフトコンタクトレンズ湿潤用及び眼内鎮静用溶液と方法
US4539330A (en) Imidazolidinyl urea and derivatives thereof for use in opthalmic solutions

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AU BR CA JP MX US

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
AK Designated states

Kind code of ref document: A3

Designated state(s): AU BR CA JP MX US

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR

WWE Wipo information: entry into national phase

Ref document number: 10415802

Country of ref document: US

WWE Wipo information: entry into national phase

Ref document number: 2002559002

Country of ref document: JP

122 Ep: pct application non-entry in european phase