Ophthalmic formulations including selective alpha 1 antagonists
AssigneeOcularis Pharma, LLC
InventorGerald Horn
Life of this patent
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Abstract
Ophthalmic formulations are provided. The ophthalmic formulations include one or more active agents that act to optimize pupil light reflex while minimizing, or effectively eliminating, any undesired eye redness in response to application thereof. The active agents include, for example, alpha 1 antagonists, such as alpha 1a selective antagonists.
Claims25
An ophthalmic formulation in an emulsified form for topical administration, the ophthalmic formulation comprising:
- a sterile aqueous carrier including an ophthalmic artificial tear solution, and
- a therapeutically effective amount of an alpha 1 antagonist that selectively effects an iris alpha adrenergic receptor over a vascular alpha adrenergic receptor for optimizing a pupil diameter in a reduced light while minimizing eye redness,
- wherein the alpha 1 antagonist is selected from the group consisting of sulfonamides including tamsulosin;
- uracils including A-131701, fiduloxasin, Ro-70-004, urapidil and 5-methyl urapidil;
- piperidines including 4-oxospiro benzopyran-2,4-piperidine;
- arylpiperazines including RWJ-38063, RWJ-68141, RWJ-68157, RWJ-69736, Ro-70-004, REC 15/2739, SB216469, urapidil and 5-methyl urapidil;
- dihydropyridines including SNAP 5089 and niguldipine;
- aminobenzodioxanes including WB 4101;
- dihydroindoles including RS 17053;
- n-alkylated saccharins;
- and derivatives thereof.
A method of modulating pupil dilation, the method comprising:
- administering to an eye of an individual an ophthalmic formulation in an emulsified form comprising a sterile aqueous carrier including an ophthalmic artificial tear solution, and a therapeutically effective amount of an alpha 1 antagonist that selectively effects an iris alpha adrenergic receptor over a vascular alpha adrenergic receptor;
- and allowing the ophthalmic formulation to remain in contact with the eye for a period of time in a reduced light where a dilator muscle of the eye receives greater stimulation in absence of the ophthalmic formulation and eye redness is minimized, wherein the alpha 1 antagonist is selected from the group consisting of sulfonamides including tamsulosin;
- uracils including A-131701, fiduloxasin, Ro-70-004, urapidil and 5-methyl urapidil;
- piperidines including 4-oxospiro benzopyran-2,4-piperidine;
- arylpiperazines including RWJ-38063, RWJ-68141, RWJ-68157, RWJ-69736, Ro-70-004, REC 15/2739, SB216469, urapidil and 5-methyl urapidil;
- dihydropyridines including SNAP 5089 and niguldipine;
- aminobenzodioxanes including WB 4101;
- dihydroindoles including RS 17053;
- n-alkylated saccharins;
- and derivatives thereof.
A method of administering an ophthalmic formulation comprising a sterile aqueous carrier including an ophthalmic artificial tear solution to an eye of an individual comprising administering a therapeutically effective amount of an alpha 1 antagonist within the ophthalmic formulation that selectively effects an iris alpha adrenergic receptor over a vascular alpha adrenergic receptor wherein the ophthalmic formulation optimizes a pupil diameter while effectively minimizing eye redness, wherein the alpha 1 antagonist is selected from the group consisting of sulfonamides including tamsulosin;
- uracils including A-131701, fiduloxasin, Ro-70-004, urapidil and 5-methyl urapidil;
- piperidines including 4-oxospiro benzopyran-2,4-piperidine;
- arylpiperazines including RWJ-38063, RWJ-68141, RWJ-68157, RWJ-69736, Ro-70-004, REC 15/2739, SB216469, urapidil and 5-methyl urapidil;
- dihydropyridines including SNAP 5089 and niguldipine;
- aminobenzodioxanes including WB 4101;
- dihydroindoles including RS 17053;
- n-alkylated saccharins;
- and derivatives thereof.
Dependencies are inferred from the claim text.