U.S. patent application number 09/741245 was filed with the patent office on 2001-07-05 for use of ophthalmic agent.
Invention is credited to Fetz, Andrea, Trimming, Julian.
Application Number | 20010006968 09/741245 |
Document ID | / |
Family ID | 8239699 |
Filed Date | 2001-07-05 |
United States Patent
Application |
20010006968 |
Kind Code |
A1 |
Trimming, Julian ; et
al. |
July 5, 2001 |
Use of ophthalmic agent
Abstract
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.
Inventors: |
Trimming, Julian; (Forch,
CH) ; Fetz, Andrea; (Wetzikon, CH) |
Correspondence
Address: |
THOMAS HOXIE
NOVARTIS CORPORATION
PATENT AND TRADEMARK DEPT
564 MORRIS AVENUE
SUMMIT
NJ
079011027
|
Family ID: |
8239699 |
Appl. No.: |
09/741245 |
Filed: |
December 20, 2000 |
Current U.S.
Class: |
514/254.07 |
Current CPC
Class: |
Y10S 514/912 20130101;
A61K 9/0048 20130101; A61P 27/14 20180101; A61K 31/4535 20130101;
A61P 27/02 20180101 |
Class at
Publication: |
514/254.07 |
International
Class: |
A61K 031/497 |
Foreign Application Data
Date |
Code |
Application Number |
Dec 23, 1999 |
EP |
99125739.5 |
Claims
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. Use of claim 1 wherein the ketotifen salt is ketotifen
fumarate.
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. Use of claim 1 wherein said eye medicament further comprises a
non-ionic tonicity agent, said tonicity agent being preferably
glycerol.
5. Use of claim 1 wherein said eye medicament further comprises a
preservative.
6. Use of claim 1 wherein said eye medicament comprises no
preservative.
7. Use of claim 1 wherein said eye medicament comprises:
2 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 (.about.0.075%), Water for injection ad ad 1.0
ml.
8. Use of claim 1 wherein said eye medicament comprises:
3 Ketotifen fumarate 0.25 mg (0.025%), Glycerol 100% 21.25 mg
(2.125%), Sodium hydroxide 1N about 0.75 mg (.about.0.075%), Water
for injection ad ad 1.0 ml.
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. Method of claim 9, wherein said allergic conjunctivitis is
seasonal allergic conjunctivitis and wherein said ketotifen is
preferably a non-preserved composition.
Description
[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.
[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.
[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.
[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.
[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%.
[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.
[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%.
[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.
[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.
[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.
[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.
[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.
[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.
1 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 (.about.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 (.about.0.075%) Water for injection ad
ad 1.0 ml
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