Preservative-Free Ophthalmic Emulsion for Glaucoma

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Solution Overview

Problem

Current glaucoma treatments primarily focus on reducing intraocular pressure (IOP) but fail to address decreased blood flow to the optic nerve, which contributes to glaucoma progression, and conventional ophthalmic compositions contain preservatives that can be toxic to ocular tissues.

Innovation Solution

A preservative-free ophthalmic pharmaceutical emulsion containing latanoprostene bunod, a nitric oxide-donating prostaglandin F2α derivative, is developed, which promotes blood velocity in the optic nerve head and treats glaucoma by increasing ocular blood flow, while avoiding toxic preservatives.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If conventional ophthalmic compositions contain preservatives to maintain stability, then the shelf life and stability are improved, but the toxic effects on ocular tissues worsen

Engineering Contradiction:
ImprovestabilityVSAvoidtoxic effects
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent removes preservatives from the ophthalmic composition entirely, extracting the harmful component while maintaining stability through alternative means (proper formulation and packaging)

Inventive Principle:
Principle #2Taking out (Extraction)

2Stress or pressure

If treatments focus on reducing IOP to treat glaucoma, then the IOP control is improved, but the blood flow to optic nerve worsens

Engineering Contradiction:
ImproveIOPVSAvoidblood flow velocity
Core Design Contradiction:
Stress or pressureVSSpeed

Solution Approach 1:

The patent uses latanoprostene bunod which performs multiple functions: it reduces IOP through prostaglandin F2α activity while simultaneously improving optic nerve head blood flow through nitric oxide donation, addressing both parameters with a single agent

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 emulsion effectively reduces IOP and increases blood flow to the optic nerve, potentially slowing glaucoma progression and reducing the risk of retinal ischemia diseases without the toxic effects of preservatives.

Implementation Method 1

Latanoprostene bunod (LBN) is a nitric oxide-donating prostaglandin F2α analog rapidly metabolized into latanoprost acid and butanediol mononitrate in situ after administration to the eye. NO released from butanediol mononitrate relaxes trabecular meshwork and Schlemm's canal, causing increased aqueous humor outflow and reduction of IOP.

Methodology Applied
Scientific EffectNitric oxide donation:

Implementation Method 2

they found that LBN promote the blood velocity of ONH of the patients with glaucoma, which may prevent glaucoma progression. On the other hand, improved ocular blood flow may also reduce risk of RVO or RAO.

Methodology Applied
Scientific EffectVasodilation:

Data Source

PatentUS20230330104A1Preservative-free ophthalmic pharmaceutical emulsion and its application
Publication Date: 2023.10.19 CARAVEL THERAPEUTICS INC
  • US20230330104A1 patent drawing

AI summary

A preservative-free ophthalmic pharmaceutical emulsion includes a nitric oxide-donating prostaglandin F2α derivative or a pharmaceutically acceptable salts or esters thereof as an active ingredient. A method applies promoting blood velocity of optic nerve head (ONH) for treating glaucoma patients and lowering risks for open angle glaucoma and retinal ischemia disease, such as retinal vein occlusion (RVO), including central retinal vein occlusion (CRVO) and branch retinal vein occlusion (BRVO), and retinal artery occlusion (RAO), including central retinal artery occlusion (CRAO) and branch retinal artery occlusion (BRAO).