Drug – bio-affecting and body treating compositions – Topical body preparation containing solid synthetic organic... – Anti-inflammatory or anti-irritant
Reexamination Certificate
2001-11-30
2003-03-11
Azpuru, Carlos (Department: 1615)
Drug, bio-affecting and body treating compositions
Topical body preparation containing solid synthetic organic...
Anti-inflammatory or anti-irritant
C424S078040
Reexamination Certificate
active
06531120
ABSTRACT:
BACKGROUND OF THE INVENTION
Field of the Invention
The present invention relates to ophthalmic histamine-containing preparations for the treatment of ocular irritation. More precisely, the invention relates to an aqueous formulation of histamine or similar compounds, to be instilled in and around the eye as well as in the conjunctival sac to treat various forms of ocular irritation.
There are a number of patents that address various ophthalmic formulations to ease ocular irritation. For example, U.S. Pat. Nos. 5,895,645; 5,877,154; 5,872,086; and 5,861,148; each recite an ophthalmic solution formulated to ease ocular irritation. However, none of these patents discuss the use of histamine-containing formulations for the reduction of ocular irritation.
SUMMARY OF THE INVENTION
One embodiment of the present invention is an ophthalmic composition for use in reducing ocular irritation, comprising a compound selected from the group consisting of histamine, a histamine receptor analog, serotonin and a serotonin analog, and a pharmaceutically acceptable ophthalmic carrier. In one aspect of this embodiment, the histamine is histamine dihydrochloride or histamine phosphate. Preferably, the histamine is present at a concentration of between about 0.001% and 10% by weight. More preferably, the histamine is present at a concentration of between about 0.05% and 5% by weight. Most preferably, the histamine is present at a concentration of between about 0.1% and 1% by weight. In one aspect of this preferred embodiment, the pharmaceutically acceptable carrier is an aqueous solution, gel or ointment. Preferably, the aqueous solution has a pH of between about 6.8 and 7.6.
Another embodiment of the present invention provides a method for treating ocular irritation in a subject in need thereof, comprising administering to the subject an effective ocular irritation-reducing amount of an ophthalmic composition comprising a compound selected from the group consisting of histamine, a histamine receptor analog, serotonin and a serotonin analog, and a pharmaceutically acceptable ophthalmic carrier. In one aspect of this embodiment, the histamine is histamine dihydrochloride or histamine phosphate. Advantageously, the subject is a human. In one aspect of this embodiment, the ocular irritation is caused by exposure to a pollutant, chemical compound, dust particles, ultraviolet light or a pathogen. The pathogen can be, for example, a virus or bacterium. In one aspect of this embodiment, the virus is a herpes virus. In another aspect of this embodiment, the bacterium is
Neisseria gonorrhea.
The ocular irritation can be caused by, for example, laser in situ keratomileusis (LASIK), radial keratotomy (RK), photo refractive keratectomy (PRK) or cataract surgery, or an allergic reaction. The compositions described herein can be administered by spraying into the eye, application of an ophthalmic gel or eye drops. Preferably, 1-2 drops of the composition is administered per eye, between 4 and 8 times per day.
Another embodiment of the present invention is a composition comprising a compound selected from the group consisting of histamine, a histamine receptor analog, serotonin and a serotonin analog, and a pharmaceutically acceptable ophthalmic carrier for use in reducing ocular irritation in a subject. In one aspect of this embodiment, the histamine is histamine dihydrochloride or histamine phosphate. The ophthalmic carrier is preferably an aqueous solution, gel or ointment. Preferably, the histamine is present at a concentration of between about 0.001% and 10% by weight. More preferably, the histamine is present at a concentration of between about 0.05% and 5% by weight. Most preferably, the histamine is present at a concentration of between about 0.1% and 1% by weight.
Another embodiment of the present invention provides the use of a composition comprising a compound selected from the group consisting of histamine, a histamine receptor analog, serotonin and a serotonin analog, and a pharmaceutically acceptable ophthalmic carrier for reducing ocular irritation in a subject. In one aspect of this embodiment, the histamine is histamine dihydrochloride or histamine phosphate. Preferably, the histamine is present at a concentration of between about 0.001% and 10% by weight. More preferably, the histamine is present at a concentration of between about 0.05% and 5% by weight. Most preferably, the histamine is present at a concentration of between about 0.1% and 1% by weight.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
The present invention relates to the use of ophthalmic pharmaceutical formulations comprising histamine for reducing ocular irritation. Ocular irritation can result from various ophthalmic surgical procedures, contact lens wear, exposure to allergens, ocularly irritating chemical compounds, pollutants, dust particles, ultraviolet light, and various pathogenic agents that cause conjunctivitis, including various infections of the eye such as herpetic infections, other viral infections, and bacterial infections. Surprisingly, ophthalmic administration of histamine-containing formulations is effective to reduce ocular irritation.
The histamine-containing formulations described herein preferably comprise histamine dihydrochloride, however, other forms of histamine, such as histamine phosphate, as well as histamine receptor analogs, serotonin and serotonin analogs are also contemplated for use in the present invention.
The histamine is present in the pharmaceutical formulations in an amount effective to reduce ocular irritation. The concentration of histamine, or a similarly functioning compound, in the formulations described herein is expressed in terms of percent histamine by weight of the total composition. For example, in one embodiment, histamine is present in an amount between about 0.001 and 10 percent by weight. In another embodiment, histamine is present in an amount between about 0.05 and 5 percent by weight. In still another embodiment, histamine is present in an amount of between about 0.1 and 1 percent by weight.
The formulations described herein comprise histamine and a pharmaceutically acceptable carrier. In a preferred embodiment, the carrier is a sterile, aqueous solution that is buffered with compounds such as phosphate buffers, carbonate buffers and the like. The composition is preferably provided as a buffered aqueous solution having a viscosity of from about 1 to 50 centipoise (cps). In another preferred embodiment, the composition is formulated as a viscous liquid having a viscosity of between about 50 and several thousand cps using viscosity-enhancing agents such as, for example propylene glycol, hydroxymethyl cellulose or glycerin.
Other ophthalmic histamine-containing pharmaceutical carriers are also contemplated, including, for example, gels and ointments. The formulations can also comprise ingredients which regulate the osmolarity of the final formulation, as well as the pH of the formulations.
For example, the resulting preparations for ocular use are advantageously hypotonic, and have an osmolarity of between about 140 and 280 mOsm/l, and a pH of between about 6.8 and 7.6. The osmolarity of the solutions can be adjusted by means of well known osmolarity adjusting agents such as sodium chloride, potassium chloride and monosaccharides. Alternatively, the resulting preparations can be isotonic, or in another embodiment, the resulting preparations can be hypertonic. The present formulations may also contain other conventional ingredients used in ophthalmic preparations, such as dextrose, preservatives (e.g. Thimerosal™, i.e., sodium ethylmercurithiosalicylate (Sigma; St. Louis, Mo.), benzalkonium chloride), corticosteroids (e.g. prednisone), analgesics (e.g., ibuprofen), antibiotics (e.g., gentamicin, streptomycin), antioxidants (e.g. ascorbic acid, BHA, BHT), demulcents (e.g., glycerin, propylene glycol), and the like. Descriptions of compounds used in standard ophthalmic formulations may be found in, for example,
Remington's Pharmaceutical Sciences,
latest edition, Ma
Azpuru Carlos
Knobbe Martens Olson & Bear LLP
Maxim Pharmaceuticals, Inc.
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