• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    The present invention is related to the use an ophthalmic composition comprising ketotifen in the preparation of an eye medicament for the treatment allergic conjunctivitis of contact lens wearers.
    公开号:US20010006968A1
    申请号:US09/741,245
    申请日:2000-12-20
    公开日:2001-07-05
    发明作者:Julian Trimming；Andrea Fetz
    申请人:Novartis AG；
    IPC主号:A61K9-0048
    专利说明:
    [0001] This invention is directed to the use of an ophthalmic composition comprising a pharmaceutically active agent, in particular ketotifen as an active agent in connection with contact lens, in particular soft contact lens. [0001]
    [0002] Prior art teaches that patients who use topical ophthalmic medications and wear soft contact lens must remove their lenses before drop instillation to prevent absorption of the medication into the lenses (Christensen et al., CLAO Journal, 1998, 227-231). If said contact lens is not removed and said medicament is administered repeatedly, an accumulation of said absorbed medicament is presumed, which might typically cause ocular irritation, hypersensitivity, keratitis and the like. [0002]
    [0003] It has now surprisingly found, that a composition comprising ketotifen or a pharmaceutically acceptable salt thereof, in particular in a concentration of from 0.01 to 0.05%, is compatible with soft contact lens. Consequently, patients do not have to remove their lens when they are in need of said medication. [0003]
    [0004] An object of the present invention is therefore the use of ketotifen or a pharmaceutically acceptable salt thereof in the preparation of an eye medicament to treat allergic conjunctivitis in a patient wearing soft contact lens. [0004]
    [0005] A pharmaceutically acceptable ketotifen salt is preferably ketotifen fumarate. The concentration of a ketotifen salt is preferably 0.005 to 0.05%, more preferred 0.01 to 0.03%, and highly preferred 0.025%. [0005]
    [0006] An addressed composition further comprises a non-ionic tonicity agent and is preferably glycerol. The non-ionic tonicity agent is preferably present in an amount such that the total tonicity of the composition has an osmolarity in the range of 230 to 260 milliosmoles, more preferred to 235 to 255 milliosmoles. If glycerol is used, the concentration of glycerol is preferably in the range of 1.5 to 2.5%. A preservative may be present, in particular for multi-dose units, but it is routinely not present in single dose units. Such single dose units are in particular preferred in the context with the present invention. [0006]
    [0007] If a preservative is present, a preferred preservative is benzalkonium chloride. Typically the amount of the preservative is 0.005 to 0.02%, more preferred 0.01%. [0007]
    [0008] An acid or base may be used in small amounts, such as 0.05 to 0.1%, for adjusting the pH of such solution. Preferred is for example the use of small amounts of sodium hydroxide 1N, e.g. 0.075%. The pH of an addressed composition is adjusted to weak acidity for optimization of stability and tolerability, and said pH of weak acidity is understood to mean preferably a pH of 4.4 to 5.8, more preferably a pH of 5 to 5.5, and most preferably a pH of 5.3. [0008]
    [0009] A preferred composition of this invention comprises ketotifen fumarate, in a concentration of 0.01 to 0.04%, glycerol in a concentration of 2 to 2.5%, optionally benzalkonium chloride in an amount of 0.005 to 0.02%, sodium hydroxide, and water. An even more preferred composition comprises ketotifen fumarate, in a concentration of 0.025%, glycerol in a concentration of 2.125%, optionally benzalkonium chloride in an amount of 0.01%, sodium hydroxide, and water. [0009]
    [0010] The ophthalmic compositions mentioned above are useful as eye drops, in particular as unpreserved single dose units. Said eye drops do have a high therapeutic value because they can be used for the treatment and the temporary prevention of itching of the eye due to allergic conjunctivitis, and they can be used for the treatment and prevention of signs and symptoms of seasonal allergic conjunctivitis. Their therapeutic utility has now been greatly improved by the findings of the present invention, which clearly indicate that ketotifen is not significantly absorbed in soft contact lens and is therefore compatible with soft contact lens. [0010]
    [0011] Soft contact lenses are typically classified both by their water content and the ionic nature of the polymer. Soft contact lenses contain typically of from 1 to 85% water, preferably of from 5 to 60% water and in particular of from 25-55% water. A particular generic class of soft contact lens material is called “filcon”. Typical examples of a filcon material are nelfilcon, etafilcon, alfafilcon and vifilcon. Accordingly, within the scope of the present invention, the term soft contact lens is preferably referring to a filcon material, more preferably to nelfilcon, etafilcon, alfafilcon and vifilcon material, and most preferably to a nelfilcon material. [0011]
    [0012] Another object of the present invention is a method to treat allergic conjunctivitis in a patient wearing soft contact lens, which method comprises the direct administration of an aqueous eye drop preparation comprising ketotifen or a pharmaceutically active salt thereof, characterized in that said ketotifen is not significantly absorbed in said soft contact lens. [0012]
    [0013] An ophthalmic composition of the present invention may be manufactured by mixing the ingredients, and packaging the resulting mixture, both as known in the art. Sterilization of the composition and the primary package can be effected e.g. by gamma irradiation, by ethyleneoxide treatment, by electron beam, by autoclaving or by steam sterilization. Typical examples are mentioned infra but are not deemed to restrict the scope of the utility of the present invention. [0013] Example 1: Multidose Units: Ketotifen fumarate 0.25 mg (0.025%) Benzalkonium chloride 0.10 mg (0.010%) Glycerol 100% 21.25 mg (2.125%) Sodium hydroxide 1N about 0.75 mg (˜0.075%) Water for injection ad ad 1.0 ml Example 2: Single dose Units: Ketotifen fumarate 0.25 mg (0.025%) Glycerol 100% 21.25 mg (2.125%) Sodium hydroxide 1N about 0.75 mg (˜0.075%) Water for injection ad ad 1.0 ml
    权利要求:
    Claims (10)
    [1" id="US-20010006968-A1-CLM-00001] 1. Use of ketotifen or a pharmaceutically acceptable salt thereof in the preparation of an eye medicament to treat allergic conjunctivitis in a patient wearing soft contact lens.
    [2" id="US-20010006968-A1-CLM-00002] 2. Use of
    claim 1 wherein the ketotifen salt is ketotifen fumarate.
    [3" id="US-20010006968-A1-CLM-00003] 3. Use of
    claim 1 wherein the concentration of the ketotifen salt is 0.005 to 0.05%, more preferred 0.01 to 0.03%, and highly preferred 0.025%.
    [4" id="US-20010006968-A1-CLM-00004] 4. Use of
    claim 1 wherein said eye medicament further comprises a non-ionic tonicity agent, said tonicity agent being preferably glycerol.
    [5" id="US-20010006968-A1-CLM-00005] 5. Use of
    claim 1 wherein said eye medicament further comprises a preservative.
    [6" id="US-20010006968-A1-CLM-00006] 6. Use of
    claim 1 wherein said eye medicament comprises no preservative.
    [7" id="US-20010006968-A1-CLM-00007] 7. Use of
    claim 1 wherein said eye medicament comprises: Ketotifen fumarate 0.25 mg (0.025%), Benzalkonium chloride 0.10 mg (0.010%), Glycerol 100% 21.25 mg (2.125%), Sodium hydroxide 1N about 0.75 mg (˜0.075%), Water for injection ad ad 1.0 ml.
    [8" id="US-20010006968-A1-CLM-00008] 8. Use of
    claim 1 wherein said eye medicament comprises: Ketotifen fumarate 0.25 mg (0.025%), Glycerol 100% 21.25 mg (2.125%), Sodium hydroxide 1N about 0.75 mg (˜0.075%), Water for injection ad ad 1.0 ml.
    [9" id="US-20010006968-A1-CLM-00009] 9. Method to treat allergic conjunctivitis in a patient wearing soft contact lens, which method comprises the direct administration of an aqueous eye drop preparation comprising ketotifen or a pharmaceutically active salt thereof, characterized in that said ketotifen is not significantly absorbed in said soft contact lens.
    [10" id="US-20010006968-A1-CLM-00010] 10. Method of
    claim 9 , wherein said allergic conjunctivitis is seasonal allergic conjunctivitis and wherein said ketotifen is preferably a non-preserved composition.
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    同族专利:
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    EP1244449A1|2002-10-02|
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    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    WO2004069338A1|2003-01-31|2004-08-19|Schering Corporation|Use of combinations of h1 and h3 histamine receptor antagonists for the preparation of a medicament for the treatment of allergic skin and allergic ocular conditions|
    US20060036220A1|2003-01-22|2006-02-16|Kohji Kawahara|Percutaneous absorption preparation for treating ophthalmic disease, use thereof and method for migration of ophthalmic remedy into topical tissue in eye|
    US20060177483A1|2005-02-04|2006-08-10|Byrne Mark E|Contact drug delivery system|
    US20080085922A1|2006-09-29|2008-04-10|Raja Ranganath R|Methods and ophthalmic devices used in the treatment of ocular allergies|
    US20080124378A1|2005-02-04|2008-05-29|Byrne Mark E|Therapeutic contact lenses with anti-fungal delivery|
    US20080138408A1|2006-11-13|2008-06-12|Siddharth Venkatesh|Drug delivery system and method|
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    US20090324691A1|2008-06-30|2009-12-31|Shivkumar Mahadevan|Methods and ophthalmic devices used in the treatment of ocular allergies|
    US20120207701A1|2005-09-07|2012-08-16|Rolf Bergman|Bi-modal hyaluronate|
    US8388995B1|2006-02-03|2013-03-05|Auburn University|Controlled and extended delivery of hyaluronic acid and comfort molecules via a contact lens platform|
    US9238003B2|2005-02-04|2016-01-19|Auburn University|Extended or continuous wear silicone hydrogel contact lenses for the extended release of comfort molecules|
    US20180311225A1|2015-10-29|2018-11-01|Teika Pharmaceutical Co., Ltd.|External preparation|JPS62277323A|1986-02-19|1987-12-02|Sankyo Co Ltd|Production of eye drop containing ketotifen fumarate|
    JPH07324034A|1994-05-30|1995-12-12|Toa Yakuhin Kk|Eye drop containing ketotifen fumarate|
    WO1998056381A1|1997-06-09|1998-12-17|Bridge Pharma, Inc.|Compounds with combined antihistaminic and mast cell stabilizing activities, intended for ophthalmic use|
    WO1999051230A1|1998-04-02|1999-10-14|Novartis Ag|Method for stabilizing pharmaceutical compositions by special use of an antioxidant|EP0938896A1|1998-01-15|1999-09-01|Novartis AG|Autoclavable pharmaceutical compositions containing a chelating agent|
    JP4906247B2|2003-06-26|2012-03-28|ロート製薬株式会社|Eye drops that can be applied while wearing contact lenses|
    JP4683835B2|2003-12-01|2011-05-18|ロート製薬株式会社|Preservative and aqueous composition containing the same|
    US20060089384A1|2004-10-25|2006-04-27|Minno George E|Ophthalmic compositions and methods of using the same|
    AU2005299696B2|2004-10-25|2012-01-12|Bausch & Lomb Incorporated|Ophthalmic compositions and methods of using the same|
    JP5275214B2|2006-03-17|2013-08-28|ジョンソン・アンド・ジョンソン・ビジョン・ケア・インコーポレイテッド|Ophthalmic stable composition comprising an oxidatively unstable component|
    CN101534793A|2006-11-06|2009-09-16|诺瓦提斯公司|Ocular devices and methods of making and using thereof|
    EP2249921B1|2008-02-25|2020-06-17|Eyegate Pharmaceuticals, Inc.|Enhanced delivery of dexamethasone phosphate to ocular tissues through iontophoresis|
    JP2012520880A|2009-03-17|2012-09-10|アーシエックスセラピューティックス，インコーポレイテッド|Ketotifen ophthalmic formulation and method of use|
    GB201419540D0|2014-11-03|2014-12-17|Nanomerics Ltd|Delivery of drugs|
    法律状态:
    2002-04-11| AS| Assignment|Owner name: NOVARTIS AG, SWITZERLAND Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:TRIMMING, JULIAN;FETZ, ANDREA;REEL/FRAME:012829/0919;SIGNING DATES FROM 20001117 TO 20001120 |
    2002-05-10| STCF| Information on status: patent grant|Free format text: PATENTED CASE |
    2003-07-08| AS| Assignment|Owner name: LOCUS DIALOGUE, INC., CANADA Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNOR:INFOSPACE SPEECH SOLUTIONS, COMPANY;REEL/FRAME:014249/0810 Effective date: 20021119 |
    2003-07-21| AS| Assignment|Owner name: LOCUS DIALOGUE, INC., CANADA Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNOR:INFOSPACE SPEECH SOLUTIONS, COMPANY;REEL/FRAME:014300/0759 Effective date: 20021119 |
    2005-10-30| FPAY| Fee payment|Year of fee payment: 4 |
    2009-10-28| FPAY| Fee payment|Year of fee payment: 8 |
    2013-10-30| FPAY| Fee payment|Year of fee payment: 12 |
    2019-12-10| AS| Assignment|Owner name: ALCON INC., SWITZERLAND Free format text: CONFIRMATORY DEED OF ASSIGNMENT EFFECTIVE APRIL 8, 2019;ASSIGNOR:NOVARTIS AG;REEL/FRAME:051454/0788 Effective date: 20191111 |
    优先权:
    申请号 | 申请日 | 专利标题
    EP99125739||1999-12-23||
    EP99125739||1999-12-23||
    EP99125739.5||1999-12-23||
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