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WO2004045510A2 - Procedes et compositions pour soulager les yeux secs - Google Patents

Procedes et compositions pour soulager les yeux secs Download PDF

Info

Publication number
WO2004045510A2
WO2004045510A2 PCT/US2003/036121 US0336121W WO2004045510A2 WO 2004045510 A2 WO2004045510 A2 WO 2004045510A2 US 0336121 W US0336121 W US 0336121W WO 2004045510 A2 WO2004045510 A2 WO 2004045510A2
Authority
WO
WIPO (PCT)
Prior art keywords
composition
progestin
gonadal steroid
steroid
dry eyes
Prior art date
Application number
PCT/US2003/036121
Other languages
English (en)
Other versions
WO2004045510A3 (fr
Inventor
Sherwyne Bakar
William Leroy Heinrichs
Jory E. Moon
Original Assignee
Panaseca, 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 Panaseca, Inc. filed Critical Panaseca, Inc.
Priority to AU2003290776A priority Critical patent/AU2003290776A1/en
Publication of WO2004045510A2 publication Critical patent/WO2004045510A2/fr
Publication of WO2004045510A3 publication Critical patent/WO2004045510A3/fr

Links

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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol

Definitions

  • the present invention relates to methods and compositions for alleviating dry eyes.
  • Dry eyes as in lack of tear formation, may arise from a number of physiological, pharmacological, or physical conditions, including, for example, chemical imbalance or decrease of blink rate. Dry eyes are increasingly common among computer users and among the aging population. There are a number of eye drops in the market that are being used to alleviate dry eyes. However, none of them are particularly effective for sustained or long-term therapy. [0003] It would be desirable, therefore, to have a more effective composition and method for alleviating dry eyes.
  • a method of alleviating dry eyes where the method includes providing a composition containing a gonadal steroid, a physiological precursor or a derivative thereof and a pharmaceutically acceptable carrier, and applying the composition to the eyes, for example, into the conjunctival sac of the eyes.
  • the compositions are administered to the eyelid and the active ingredient(s) delivered transdermally.
  • the pharmaceutically acceptable carrier is a conventional eye drops.
  • the conventional eye drops is selected from one consisting of Visine Tears, Advanced Relief Visine, Visine Original, Nisine L.R., Visine A, and Visine A.C.
  • the conventional eye drops is selected from the group consisting of Similasan Eye Drops #1, Similasan Eye Drops #2, and Similasan Eye Drops #3.
  • the conventional eye drops is selected from the group consisting of Alcon's Bion Tears, Opticrom , Bausch and Lomb's Moisture Eyes, azelastine, and Mavala Eye Lite.
  • the gonadal steroid is estrogen.
  • compositions for alleviating dry eyes where the composition contains a gonadal steroid and a pharmaceutically acceptable carrier.
  • the pharmaceutically acceptable carrier is a conventional eye drops.
  • the pharmaceutically acceptable carrier may be, for example, pluronic lecithin gel.
  • the pharmaceutically acceptable carrier may be one or more cosmetics.
  • a method of delivery a composition to a subject to alleviate dry eyes where the method includes applying a composition as above to the eyes.
  • composition in the preparation of a medicament for alleviating dry eyes, where the composition contains a gonadal steroid as above.
  • compositions for alleviating dry eyes where the composition contains a gonadal steroid.
  • compositions as above where the composition further comprises a pharmaceutically acceptable carrier or excipient.
  • the composition of the invention contains a gonadal steroid, a physiological precursor or derivative thereof and a pharmaceutically acceptable carrier.
  • a "pharmaceutically acceptable carrier” refers to a non-toxic solid, semi- solid or liquid filler, diluent, encapsulating material or formulation auxiliary of any conventional type. See, also, Remington's Pharmaceutical Sciences, 18th Edition (Easton,
  • a pharmaceutically acceptable carrier is non-toxic to recipients at the dosages and concentrations employed, and is compatible with other ingredients of the formulation.
  • the carrier for a formulation containing gonadal steroid does not include oxidizing agents and other compounds that are known to be deleterious to such steroid.
  • Suitable carriers include, but are not limited to, water, dextrose, glycerol, physiological saline, phosphate buffered saline, sodium silver chloride complex, dextran, hydroxypropyl methylcellulose, hydrochloric acid, sodium hydroxide, sodium cromolglycate, benzalkonium chloride, disodium edetate, propylene glycol, glycerin, boric acid, potassium chloride, sodium borate, tetrahydrozoline hydrochloride, benzoic acid, chlorobutanol, benzyl alcohol, terpineol, pluronic lethicin gel, and combinations thereof.
  • the carrier can contain additional agents such as wetting agents, pH buffering agents, or adjuvants which enhance the effectiveness of the formulation. Other materials such as anti-oxidants, humectants, and similar agents can be added as necessary.
  • the gonadal steroid, derivative or salt thereof suitable for use herein are those that do not bind to or react with testosterone 5- ⁇ -reductase at a higher affinity than testosterone.
  • Such gonadal steroids include, for example, estrogen or its derivatives, as in the form of ethyl-estradiol, and androgenic progestins, as described in Hammond, G.L, Rabe, T., and Wagner, J.D., Am. J. Obstet. Gynecol. 185(2 Suppl.): S24-31 (Aug. 2001) and in Kuhl, H., Drugs, 51(2): 188-215 (Feb. 1996), the contents of both of which are incorporated herein by reference.
  • the androgenic progestin is a 19-nor-steroid progestin. More preferably, the androgenic progestin is norethindrone or its acetate salt, or levonorgestral. Other 19-nor-progestins, such as norgestrel or norethynodrel may also be used.
  • the dose of the gonadal steroid suitable for use herein is an effective amount.
  • An effective amount of the active agent is administered to a subject, where "effective amount" means a dosage sufficient to produce a desired result.
  • the dosage of the present composition that can be applied can be determined by a person skilled in the art or by the subject using the composition on an as needed basis.
  • EE is in the range of about 4 ⁇ g to about 28 ⁇ g
  • the dose of EE can be in the range of about 2 ⁇ g to about 14 ⁇ g.
  • the dose of EE can be in the range of about 1 ⁇ g to about 7 ⁇ g.
  • the dose of EE can also be in the range of about 0.5 ⁇ g to about 3.5 ⁇ g.
  • the dose of EE can be in the range of about 0.25 ⁇ g to about 1.75 ⁇ g.
  • the dose of the androgenic progestin (“AP”) is generally in the range of about 80 ⁇ g to about 600 ⁇ g. Further, the dose of AP can be in the range of about 40 ⁇ g to about 300 ⁇ g.
  • the does of AP can be in the range of about 20 ⁇ g to about 150 ⁇ g.
  • the dose of AP can be in the range of about 10 ⁇ g to about 75 ⁇ g.
  • the pharmaceutically acceptable carrier herein can be any conventional eye drops including, for example, Visine Tears, Advanced Relief Visine, Visine Original, Visine L. R., Visine-A, and Visine A.C., manufactured by Pfizer, Similasan Eye Drops #1,
  • the composition containing the gonadal steroid, or physiological precursor thereof, for example, dehydroepiandrosterone or androstenedione or their salts, and pharmaceutically acceptable carrier is applied to the eyes in any conventional or acceptable manner.
  • the present composition can be applied as eyes drops using an eye dropper or a container that functions as an eye dropper.
  • the present composition can also be applied to the eyes transdermally, such as in the form of a transdermal patch.
  • the transdermal patch can be translucent or transparent.
  • the transdermal patch can be colored, for example, such as to match a subject's skin color or to confer a different color.
  • the transdermal patch can be shaped and colored in such a way to look like eye shadow, for example.
  • the transdermal patch can be one on which color or other cosmetics can be applied thereto.
  • the present composition can be applied into the conjunctival sac of the eyes.
  • the present composition can be applied to the eyes in the form of an implant in the eyes or as part of a contact lens applied to the eyes.
  • the compositions described herein can also be applied concurrently, before or after additional preparations such as cosmetics.
  • compositions described herein may form a base for cosmetics applied near the eye.
  • the present composition for alleviating dry eyes can be applied on an as needed basis, for example, at least once a month, preferably at least once a week, more preferably, at least once a day; most preferably, at least twice a day or at least three times a day.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne un procédé et une composition associée permettant de soulager les yeux secs. La composition contient un stéroïde gonadique et un excipient pharmaceutiquement acceptable. Dans un autre procédé pour soulager les yeux secs, le stéroïde gonadique se lie à la testostérone 5-α réductase avec une affinité inférieure à celle de la testostérone.
PCT/US2003/036121 2002-11-15 2003-11-14 Procedes et compositions pour soulager les yeux secs WO2004045510A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003290776A AU2003290776A1 (en) 2002-11-15 2003-11-14 Methods and compositions for alleviating dry eyes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42683602P 2002-11-15 2002-11-15
US60/426,836 2002-11-15

Publications (2)

Publication Number Publication Date
WO2004045510A2 true WO2004045510A2 (fr) 2004-06-03
WO2004045510A3 WO2004045510A3 (fr) 2004-08-12

Family

ID=32326435

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/036121 WO2004045510A2 (fr) 2002-11-15 2003-11-14 Procedes et compositions pour soulager les yeux secs

Country Status (2)

Country Link
AU (1) AU2003290776A1 (fr)
WO (1) WO2004045510A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010511730A (ja) * 2006-12-05 2010-04-15 サザン カレッジ オブ オプトメトリー テストステロンおよびプロゲスターゲンを用いたドライアイのための処置

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5041434A (en) * 1991-08-17 1991-08-20 Virginia Lubkin Drugs for topical application of sex steroids in the treatment of dry eye syndrome, and methods of preparation and application

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010511730A (ja) * 2006-12-05 2010-04-15 サザン カレッジ オブ オプトメトリー テストステロンおよびプロゲスターゲンを用いたドライアイのための処置
JP2010511729A (ja) * 2006-12-05 2010-04-15 サザン カレッジ オブ オプトメトリー ドライアイのための処置

Also Published As

Publication number Publication date
AU2003290776A1 (en) 2004-06-15
AU2003290776A8 (en) 2004-06-15
WO2004045510A3 (fr) 2004-08-12

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