Low-dose Brimonidine Combinations for Glaucoma IOP Control

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current glaucoma treatments face limitations in effectively lowering intraocular pressure (IOP) and are often accompanied by significant side effects such as eye redness, conjunctival hyperemia, and systemic effects, which can lead to patient non-compliance due to discomfort and unhealthy appearance.

Innovation Solution

A composition comprising low-dose brimonidine (0.01% to 0.059% w/v) combined with a second glaucoma drug or a histamine antagonist, which reduces IOP, alleviates eye redness, and minimizes side effects like conjunctival hyperemia and systemic delivery, while providing eye whitening and inflammation reduction.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stress or pressure

If higher dose brimonidine (0.15-0.2%) is used to achieve greater IOP reduction, then IOP lowering effect is improved, but local side effects such as conjunctival hyperemia, blepharitis, and allergy increase substantially

Engineering Contradiction:

Improveintraocular pressureVSAvoidlocal side effects

Core Design Contradiction:

Stress or pressureVSObject-affected harmful factors

Solution Approach 1:

The patent changes the concentration parameter of brimonidine from conventional doses (0.15-0.2%) to low doses (0.01%-0.059%), fundamentally altering the dosage regime to achieve a different therapeutic profile that maintains IOP control while minimizing local side effects

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite pharmaceutical formulations by combining low-dose brimonidine with other glaucoma medications, allowing synergistic effects that enable effective IOP reduction at lower brimonidine concentrations, thereby reducing side effects while maintaining therapeutic efficacy

Inventive Principle:

Principle #40Composite materials

2Reliability

If standard dose brimonidine is used to achieve moderate IOP reduction, then therapeutic effect is improved, but patient compliance deteriorates due to side effects and appearance concerns

Engineering Contradiction:

Improvetherapeutic effectVSAvoidpatient compliance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

By changing the dosage parameter to low doses (0.01%-0.059%), the patent reduces the incidence and severity of side effects, directly improving patient compliance while maintaining adequate IOP control through extended dosing intervals or combination therapy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent converts the previously harmful side effects into benefits by using low-dose brimonidine in combination with other agents, where the combination achieves synergistic IOP reduction allowing even lower brimonidine doses, thereby transforming compliance issues into compliance advantages

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Stress or pressure

If brimonidine is used to reduce IOP, then glaucoma treatment effect is improved, but systemic effects such as fatigue, hypotension, and bradycardia increase

Engineering Contradiction:

Improveintraocular pressureVSAvoidsystemic effects

Core Design Contradiction:

Stress or pressureVSObject-generated harmful factors

Solution Approach 1:

The patent changes the concentration parameter to low doses (0.01%-0.059%), which reduces systemic absorption and consequently minimizes systemic side effects like fatigue, hypotension, and bradycardia, while maintaining ocular therapeutic effects

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses composite formulations combining low-dose brimonidine with other glaucoma medications, allowing the alternative agents to contribute to IOP reduction, thereby enabling even lower brimonidine doses and further reducing systemic exposure and associated side effects

Inventive Principle:

Principle #40Composite materials

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The combination of low-dose brimonidine with other glaucoma drugs or histamine antagonists achieves synergistic IOP reduction and alleviates side effects, enhancing patient compliance by reducing systemic and local adverse reactions, and providing improved eye whitening.

Implementation Method 1

Brimonidine, a known alpha-2 (α-2) adrenergic receptor agonist

Methodology Applied

Scientific EffectAlpha-2 adrenergic receptor agonism:

Implementation Method 2

minimizes side effects like conjunctival hyperemia and systemic delivery

Methodology Applied

Scientific EffectReduced systemic delivery:

Data Source

PatentUS20210369706A1Low-dose brimonidine combinations and uses thereof

Publication Date: 2021.12.02 EYE THERAPIES LLC

AI summary

The present invention is directed to compositions containing low-dose brimonidine and a second glaucoma drug. The present invention is further directed to methods of treating glaucoma by administering compositions of the present invention.