Detailed Analysis of the Scope and Claims of United States Patent 8,829,005
Introduction
United States Patent 8,829,005, titled "Ophthalmic formulations of cetirizine and methods of use," is a significant patent in the field of ophthalmic treatments, particularly for allergic conjunctivitis and allergic rhinoconjunctivitis. This patent, issued on September 9, 2014, to Aciex Therapeutics, Inc. (later assigned to Nicox Ophthalmics, Inc.), outlines innovative formulations and methods for using cetirizine in ophthalmic applications.
Inventors and Assignees
The patent was invented by Mark Barry Abelson, Matthew J. Chapin, Paul Gomes, George Minno, and Jackie Nice, and assigned to Aciex Therapeutics, Inc., which later transferred the rights to Nicox Ophthalmics, Inc.[2].
Patent Expiration Date
The patent is set to expire on March 15, 2030, which is 20 years from the date of filing, consistent with standard patent durations[2].
Scope of the Patent
Ophthalmic Formulations of Cetirizine
The patent describes stable ophthalmic formulations of cetirizine, which are effective in treating the signs and symptoms of both acute and late-phase allergic conjunctivitis. These formulations can be used alone or in combination with other active agents, such as fluticasone[1].
Concentration and Form
The cetirizine in these formulations is typically in the form of cetirizine hydrochloride or dihydrochloride, with concentrations ranging from 0.01% to 1.0% (w/v), preferably between 0.05% and 0.5% (w/v)[1].
Vehicle Composition
The formulations are composed of a vehicle that includes:
- 1% Polyethylene Glycol 400, NF
- 0.2% Dibasic Sodium Phosphate, Anhydrous, USP
- 0.25% Hypromellose, USP
- 0.1% Polysorbate 80, NF
- 1.2% to 1.8% Glycerin, USP
- 0.025% Edetate Disodium, USP
- 0.01% Benzalkonium Chloride, NF (pH 7.0)[1].
Tear Substitute
The formulations include a tear substitute, typically hydroxypropylmethyl cellulose (Hypromellose or HPMC), with concentrations ranging from about 0.1% to about 2% w/v. This component helps in maintaining the stability and comfort of the formulation when instilled in the eye[1].
Claims of the Patent
Method of Treatment
The patent includes method of treatment claims that cover the use of cetirizine ophthalmic solution for treating allergic conjunctivitis and/or allergic rhinoconjunctivitis. These methods involve the topical application of the cetirizine formulations directly to the eye[2].
Formulation Claims
The patent claims cover various aspects of the formulation, including the concentration of cetirizine, the vehicle composition, and the use of tear substitutes and preservatives. It also includes claims for combination formulations with other active agents like fluticasone[1].
Mucoadhesive Vehicles
The patent describes mucoadhesive vehicles suitable for use in the formulations, including aqueous polymeric suspensions with polymeric suspending agents such as dextrans, polyethylene glycol, and cross-linked carboxy-containing polymer systems like Noveon AA-1, Carbopol®, and DuraSite®[1].
Patent Landscape
Related Patents
There are several related patents that extend the scope of the original invention. For example, U.S. Patent 9,750,684 and U.S. Patent 9,993,471, also assigned to Nicox Ophthalmics, Inc., further elaborate on the stable topical formulations of cetirizine and their methods of use[2].
Generic Availability
As of the current date, there is no therapeutically equivalent generic version of Zerviate (the brand name for cetirizine ophthalmic solution) available in the United States, indicating that the patent remains exclusive to the assignee[2].
Intellectual Property Protection
The patent analytics for this invention would involve tracking the claims and scope concepts to ensure comprehensive protection of the intellectual property. This includes categorizing patents by claims and overarching scope concepts to identify gaps or opportunities in the patent landscape[3].
Key Takeaways
- Innovative Formulations: The patent introduces stable ophthalmic formulations of cetirizine for treating allergic conjunctivitis and rhinoconjunctivitis.
- Specific Concentrations: The formulations have specific concentrations of cetirizine and other components to ensure efficacy and comfort.
- Tear Substitutes: The use of tear substitutes like Hypromellose enhances the stability and comfort of the formulations.
- Method of Treatment: The patent includes method of treatment claims for topical application of cetirizine formulations.
- Patent Exclusivity: The patent remains exclusive until its expiration date in 2030, with no generic equivalents available.
Frequently Asked Questions (FAQs)
What is the primary use of the cetirizine ophthalmic formulations described in U.S. Patent 8,829,005?
The primary use is for treating the signs and symptoms of allergic conjunctivitis and allergic rhinoconjunctivitis.
What are the typical concentrations of cetirizine in these formulations?
The concentrations range from 0.01% to 1.0% (w/v), with a preferred range of 0.05% to 0.5% (w/v).
What is the role of Hypromellose in the formulations?
Hypromellose serves as a tear substitute, enhancing the stability and comfort of the formulation when instilled in the eye.
Are there any combination formulations described in the patent?
Yes, the patent includes formulations of cetirizine in combination with other active agents, such as fluticasone.
When is the patent set to expire?
The patent is set to expire on March 15, 2030.
Sources:
- Google Patents - Ophthalmic formulations of cetirizine and methods of use[1].
- Drugs.com - Generic Zerviate Availability[2].
- SLWIP - Patent Analytics[3].
