Moxifloxacin Dexamethasone Ophthalmic Solution Stability

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Solution Overview

Problem

Current solutions for topical administration of moxifloxacin and dexamethasone do not provide stable, preserved, multi-dose solution compositions suitable for both eye and ear applications, with existing compositions either being unstable or not effectively formulated for multi-dose use.

Innovation Solution

Aqueous compositions comprising moxifloxacin hydrochloride, dexamethasone phosphate, edetate disodium, an ionic tonicity adjusting agent, boric acid, a nonionic surfactant, and either benzalkonium chloride or sorbitol, formulated to maintain a pH of 7.5-8.1, ensuring stability and multi-dose capability for topical administration to the eye or ear.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing moxifloxacin and dexamethasone compositions are formulated, then antibiotic and anti-inflammatory therapy is provided, but the compositions are unstable or not suitable for multi-dose use

Engineering Contradiction:
ImprovestabilityVSAvoidmulti-dose capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by optimizing the pH range to 7.5-8.1 and adjusting ionic strength through specific tonicity agents. These parameter modifications enable the formulation to achieve both chemical stability and multi-dose usability, resolving the contradiction between reliability and adaptability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material formulation by combining moxifloxacin hydrochloride with dexamethasone phosphate in a specific aqueous system containing edetate disodium, tonicity agents, and preservatives. This composite approach creates a stable multi-dose solution that neither component achieves alone, simultaneously improving reliability and multi-dose capability.

Inventive Principle:
Principle #40Composite materials

2Ease of operation

If moxifloxacin and dexamethasone are combined in solution form, then topical administration to eye and ear is enabled, but stability is compromised

Engineering Contradiction:
Improvetopical administrabilityVSAvoidsolution stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent resolves the contradiction between ease of operation and stability by precisely controlling the pH parameter within 7.5-8.1 and adjusting ionic strength. These parameter changes enable the solution to remain stable while maintaining suitability for topical administration to both ocular and otic tissues.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces edetate disodium as an intermediary chelating agent that stabilizes the combination of moxifloxacin and dexamethasone in solution. This intermediary substance prevents precipitation and degradation, enabling stable topical formulations for both eye and ear applications.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Object-affected harmful factors

If preservatives are added to enable multi-dose use, then microbial protection is improved, but chemical stability may be affected

Engineering Contradiction:
Improvemicrobial protectionVSAvoidchemical stability
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by optimizing the pH range to 7.5-8.1, which enhances the effectiveness of preservatives like benzalkonium chloride while maintaining chemical stability of the active ingredients. This parameter optimization resolves the contradiction between microbial protection and chemical stability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses a composite preservative system combining benzalkonium chloride with edetate disodium and specific tonicity agents. This composite approach provides effective microbial protection while the synergistic interactions maintain chemical stability, resolving the contradiction between these two requirements.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS8173671B2Topical ophthalmic or otic solution formulations containing moxifloxacin hydrochloride and dexamethasone phosphate
Publication Date: 2012.05.08 NOVARTIS AG

AI summary

Topical ophthalmic and otic solution compositions of moxifloxacin and dexamethasone phosphate are disclosed.