Atropine Ophthalmic Composition pH and Viscosity Control

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Solution Overview

Problem

Current atropine ophthalmic solutions effectively inhibit myopia progression but cause significant mydriasis and loss of accommodation, impacting daily activities, and the viscosity of atropine solutions decreases over time, compromising stability.

Innovation Solution

An aqueous composition containing 0.001 - 0.1% atropine or its salt, a water-soluble polymer, and a buffer at pH 6 or lower, with limited or no benzalkonium chloride, and a nonionic tonicity agent to maintain viscosity and stability, reducing mydriatic effects and accommodating loss.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If atropine ophthalmic solution is used to inhibit myopia progression, then the elongation of ocular axial length is prevented, but significant mydriasis and loss of accommodation occur

Engineering Contradiction:
Improvemyopia progression inhibitionVSAvoidmydriasis and accommodation loss
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the pH parameter of the ophthalmic solution to pH 6 or lower, which modifies the pharmacological behavior of atropine. This parameter change reduces the mydriatic action and accommodation loss while preserving the myopia progression inhibition effect. The specific pH optimization allows atropine to maintain its ability to prevent ocular axial length elongation while minimizing harmful side effects on pupil size and lens accommodation.

Inventive Principle:
Principle #35Parameter changes

2Stability of the object's composition

If atropine ophthalmic solution is formulated with conventional excipients, then stability is achieved, but viscosity decreases over time

Engineering Contradiction:
Improveatropine stabilityVSAvoidviscosity maintenance
Core Design Contradiction:
Stability of the object's compositionVSDuration of action of stationary object

Solution Approach 1:

The patent uses a composite formulation combining multiple excipients including hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), and polyethylene glycol (PEG) in specific concentration ranges. This composite material system provides synergistic effects where HPMC contributes to initial viscosity, PVA maintains structural integrity, and PEG prevents polymer degradation. Together, these materials maintain stable viscosity over time while ensuring atropine stability through the controlled pH environment.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP4112055A1Atropine-containing aqueous composition
Publication Date: 2023.01.04 SINGAPORE HEALTH SERVICES PTE LTD
  • EP4112055A1 patent drawingFigure 1
  • EP4112055A1 patent drawingFigure 2
  • EP4112055A1 patent drawingFigure 3

AI summary

Disclosed herein is an aqueous composition comprising 0.001 - 0.1 % (w/v) atropine or a salt thereof, and a phosphate buffer, which is at a pH range of 6 or lower.