Ophthalmic Formulation for Presbyopia via Pilocarpine and Alpha-1 Agonists

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Solution Overview

Problem

Current treatments for presbyopia, such as eyeglasses and surgical corrections, are either cumbersome or invasive and do not effectively address the age-related decline in near focusing ability while maintaining accommodative function.

Innovation Solution

An ophthalmic formulation comprising an effective amount of pilocarpine, a parasympathomimetic drug, and one or more α1 adrenergic agonists or antagonists, such as phenylephrine, which can be applied topically to the eye to improve near vision without affecting distance vision, thereby reducing presbyopia symptoms while maintaining accommodative function.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If eyeglasses or corrective lenses are used to treat presbyopia, then near vision is improved, but the device becomes cumbersome and requires removal for distance vision

Engineering Contradiction:
Improvenear vision correctionVSAvoidconvenience of use
Core Design Contradiction:
Manufacturing precisionVSEase of operation

Solution Approach 1:

The patent replaces the mechanical system of eyeglasses and corrective lenses with a chemical/pharmacological system using ophthalmic drops containing pilocarpine and phenylephrine. This substitution eliminates the need for external optical devices by directly acting on the eye's accommodation mechanism through drug receptors, thereby improving convenience while maintaining near vision correction capability

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The treatment enables the eye's own accommodation system to function properly by pharmacologically stimulating the ciliary muscle and adjusting the crystalline lens curvature. Rather than using external devices to compensate for accommodation loss, the medication restores the eye's natural ability to focus on near objects, allowing the biological system to serve itself

Inventive Principle:
Principle #25Self-service

2Manufacturing precision

If surgical correction is performed to treat presbyopia, then near vision is improved, but the procedure becomes invasive and carries risks

Engineering Contradiction:
Improvenear vision correctionVSAvoidsurgical risks
Core Design Contradiction:
Manufacturing precisionVSObject-affected harmful factors

Solution Approach 1:

The patent employs a non-invasive, reversible pharmacological treatment using topical ophthalmic drops instead of permanent surgical intervention. The medication provides temporary but effective near vision correction that can be applied as needed without surgical risks, tissue damage, or permanent alteration of eye structure

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent introduces a chemical intermediary (ophthalmic drops containing pilocarpine and phenylephrine) that mediates between the user and the eye's accommodation system. This intermediary substance temporarily modifies physiological parameters to enable near focusing without requiring direct mechanical or surgical intervention on the eye structures

Inventive Principle:
Principle #24Intermediary (Mediator)

3Manufacturing precision

If corrective lenses are used to compensate for accommodation loss, then near vision is improved, but distance vision or accommodative function is compromised

Engineering Contradiction:
Improvenear vision correctionVSAvoiddistance vision maintenance
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

The patent creates a dynamic treatment approach where the eye's accommodation system remains active and adjustable rather than being statically corrected by fixed-power lenses. The pharmacological treatment temporarily enhances ciliary muscle contraction and lens flexibility, allowing the eye to dynamically adjust focus for near objects while maintaining the ability to return to distance vision by stopping medication use

Inventive Principle:
Principle #15Dynamics

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 formulation enables patients to focus on objects at nearby distances, including normal reading distances, without the need for corrective lenses or surgery, by improving near vision while preserving distance vision and accommodative ability.

Implementation Method 1

an ophthalmic formulation comprises an effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof

Methodology Applied
Scientific EffectParasympathomimetic action:

Implementation Method 2

one or more α1 adrenergic agonists or antagonists. The one or more α1 adrenergic agonists or antagonists may be selected from a group consisting of phenylephrine, phenylpropanolamine, etylefrine, oxymetazoline, xilometazoline, tramazoline

Methodology Applied
Scientific Effectα1 adrenergic agonism or antagonism:

Data Source

PatentUS10507245B2Ophthalmic formulation and method for ameliorating presbyopia
Publication Date: 2019.12.17 VEJARANO RESTREPO LUIS FELIPE

AI summary

An ophthalmic formulation having an effective amount of a parasympathomimetic agent comprising pilocarpine, or a pharmaceutically acceptable salt thereof, and one or more α1 adrenergic agonists or antagonists is disclosed. The ophthalmic formulation may enable treatment of conditions adversely affecting the visual acuity of a patient, including presbyopia. A method of using the disclosed ophthalmic formulation to treat or ameliorate symptoms of presbyopia is also disclosed.