Low-Concentration Atropine Ophthalmic Composition for NITM Treatment

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Solution Overview

Problem

Current treatments and prevention methods for Near-Work Induced Transient Myopia (NITM) are inadequate and lacking effective solutions.

Innovation Solution

A pharmaceutical composition comprising low-concentration atropine (0.001% to 0.2%) with a pH adjusting agent like boric acid or borate, potentially combined with thickening agents and osmotic regulators, formulated as an ophthalmic preparation to treat and prevent NITM.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If atropine is used to treat NITM, then therapeutic effect is achieved, but mydriatic side effects occur

Engineering Contradiction:
Improvetherapeutic effectVSAvoidmydriatic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by using low concentration atropine (0.001%-0.2%) instead of conventional higher concentrations, and by adjusting the pH to 4.5-5.5 using boric acid or borate. This changes the pharmacological parameters to achieve therapeutic effect while reducing mydriatic side effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses a composite formulation combining atropine with boric acid or borate buffer system. This composite approach creates a synergistic effect where the borate system enhances atropine's therapeutic action on NITM while mitigating its mydriatic side effects through pH adjustment and osmotic balance.

Inventive Principle:
Principle #40Composite materials

2Ease of manufacture

If conventional treatments are used for NITM, then treatment is provided, but effectiveness is insufficient

Engineering Contradiction:
Improvetreatment availabilityVSAvoidtreatment effectiveness
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the concentration parameter of atropine to low ranges (0.001%-0.2%) and adjusts pH to 4.5-5.5 using boric acid/borate, which significantly improves treatment effectiveness for NITM compared to conventional formulations while maintaining ease of manufacture.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The boric acid or borate acts as an intermediary substance that enhances the effectiveness of atropine in treating NITM. It mediates between the atropine molecule and the target tissue, improving therapeutic action through pH adjustment and osmotic regulation.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 composition effectively treats and prevents NITM, showing a dose-dependent therapeutic effect, with boric acid or borate enhancing the treatment efficacy and reducing mydriatic side effects, particularly when used within a pH range of 4.5 to 5.5.

Implementation Method 1

the pharmaceutical composition has a pH value of 4.5 to 5.5; the pharmaceutical composition comprises a pH adjusting agent in an amount of 0.05% weight to 5% weight, and the pH adjusting agent is one or more selected from a group consisting of boric acid and borate

Methodology Applied
Scientific EffectpH adjustment:

Implementation Method 2

low-concentration atropine can effectively treat NITM, and the therapeutic effect shows a dose-dependent pharmacodynamic relationship (0.001% to 0.2%)

Methodology Applied
Scientific EffectPharmacological action of atropine:

Implementation Method 3

the best effect is achieved especially when only boric acid is used to adjust pH value and osmotic pressure

Methodology Applied
Scientific EffectOsmosis: Osmosis

Data Source

PatentEP3858353B1Pharmaceutical composition for preventing and treating NITM and pharmaceutical use thereof
Publication Date: 2024.02.07 SHENYANG XINGQI PHARM CO LTD
  • EP3858353B1 patent drawing
  • EP3858353B1 patent drawing
  • EP3858353B1 patent drawing

AI summary

The present invention belongs to the field of medicine and relates to a pharmaceutical composition for preventing and treating NITM and a medical use thereof. Specifically, the pharmaceutical composition is an ophthalmic pharmaceutical composition such as an ophthalmic preparation. Specifically, the present invention relates to a pharmaceutical composition comprising 0.001% to 0.2% of atropine or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients; wherein the pH value of the pharmaceutical composition is of 4.0 to 6.5; the pharmaceutical composition comprises 0.5% to 5% of a pH adjusting agent, and the pH adjusting agent is any one or more selected from sodium dihydrogen phosphate, disodium hydrogen phosphate, citric acid, citrate, boric acid and borates. The pharmaceutical composition of the present invention can effectively treat and/or prevent NITM, and thus has a good application prospect.