Ophthalmic Composition Combining Anti-Inflammatory and Tear-Stimulating Agents
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Solution Overview
Problem
Current treatments for dry eye syndrome, such as Restasis and Xiidra, have limited modes of action and require frequent application due to inefficient uptake of active pharmaceutical ingredients into ocular surface tissues, leading to discomfort and side effects like blurry vision.
Innovation Solution
A composition comprising an alpha 2 adrenergic agonist, a corticosteroid, a lymphocyte function-associated antigen antagonist, a non-steroidal anti-inflammatory drug, and a sodium channel blocker, formulated as an ophthalmic solution or emulsion to provide a synergistic effect and reduce side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If single active pharmaceutical ingredients are used (e.g., Restasis, Xiidra), then the treatment can be simplified, but the mode of action is limited and frequent application is required
Solution Approach 1:
The patent combines multiple active pharmaceutical ingredients (alpha 2 adrenergic agonist, corticosteroid, LFA-1 antagonist, ENaC inhibitor, NSAID, and/or antibiotic) into a single ophthalmic composition. This merging approach provides multiple modes of action simultaneously - stimulating tear production, reducing inflammation, inhibiting leukocyte migration, and preventing bacterial infection - thereby resolving the contradiction between treatment simplicity and therapeutic versatility.
Solution Approach 2:
The multi-component formulation is designed to address multiple pathophysiological mechanisms of dry eye disease through a single application. The composition simultaneously targets aqueous tear deficiency, evaporative loss, ocular surface inflammation, and infectious risk, making the treatment universally effective across different dry eye subtypes and reducing the need for multiple separate medications.
2Reliability
If frequent application is used to maintain effectiveness, then therapeutic coverage is improved, but patient comfort deteriorates and side effects increase
Solution Approach 1:
By merging multiple mechanisms of action into one formulation, the patent achieves reliable therapeutic coverage without requiring frequent applications. The synergistic combination of tear production stimulants, anti-inflammatories, and other agents maintains continuous effectiveness while reducing application frequency, thereby minimizing side effects and improving patient comfort.
3Productivity
If active pharmaceutical ingredients are applied topically, then direct treatment is achieved, but uptake into ocular surface tissues is inefficient
Solution Approach 1:
The patent employs an ophthalmic composition formulation that acts as an intermediary delivery system. The formulation enhances the uptake and penetration of multiple active pharmaceutical ingredients into ocular surface tissues through optimized vehicle properties, allowing efficient delivery without requiring high concentrations of individual substances.
Data Source
AI summary
The present invention provides a composition comprising two or more of the following pharmaceutically active compounds: (i) an alpha 2 adrenergic agonist; (ii) a corticosteroid; (iii) a lymphocyte function-associated antigen antagonist; (iv) a non-steroidal anti-inflammatory drug (NSAID); (v) a sodium channel blocker; and (vi) an antibiotic, provided at least one of the pharmaceutically active compound is selected from the group consisting of (i) alpha 2 adrenergic agonist and (ii) corticosteroid. The present invention also provides a method for using such composition to treat an eye disorder such as a dry eye syndrome; ocular graft-versus-host-disease; ocular rosacea; allergic conjunctivitis; autoimmune ocular surface disease; thygeson's superficial punctuate keratopathy; herpes zoster keratitis; Stevens-Johnson syndrome; keratitis; conjunctivitis; blepharitis; blepharochalasis; conjunctivochalasis; blepharoconjunctivitis; blepharokeratoconjunctivitis; post-operative inflammation or pain from ocular surgery; scleritis; episcleritis; anterior uveitis; iritis; cyclitis; ocular surface vascular disorder; ulcerative keratitis; photokeratitis; dacryocystitis; eyelid disorder; congenital alacrima; xerophthalmia; dacryoadenitis; vernal keratoconjunctivitis; pinguecula; and/or ocular surface disorder induced by chemical burns, thermal burns, or physical insult to the ocular surface.