Nasal Corticoid-Antibiotic Composition for Sinusitis

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Solution Overview

Problem

Current treatments for sinusitis lack efficacy and often result in high toxicity and excessive antibiotic use.

Innovation Solution

A pharmaceutical composition of unit dose for inhalation with a high corticoid/antibiotic ratio of 0.02 to 20, specifically 0.4 to 2, and quinolone or fusidic acid amounts between 10 to 400 μg, primarily using budesonide, fluticasone furoate, triamcinolone, and ciprofloxacin, formulated as a nasal spray for targeted delivery to the respiratory tract.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If conventional compositions with balanced corticoid/antibiotic ratios are used, then treatment coverage is maintained, but toxicity increases and antibiotic amounts become excessive

Engineering Contradiction:
ImprovetoxicityVSAvoidantibiotic amount
Core Design Contradiction:
Object-affected harmful factorsVSQuantity of substance

Solution Approach 1:

The patent fundamentally changes the parameter relationship between corticoid and antibiotic by establishing a new ratio range (0.02 to 20, preferably 0.4 to 2) and reducing antibiotic amount to less than 1 mg per unit dose. This parameter optimization resolves the contradiction by achieving effective treatment with significantly reduced antibiotic quantities and lowered toxicity compared to conventional balanced ratios.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If higher antibiotic amounts are used to ensure treatment efficacy, then treatment coverage improves, but toxicity and resistance risk increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the corticoid/antibiotic ratio parameter to fall within 0.02 to 20 (preferably 0.4 to 2) while maintaining antibiotic amounts below 1 mg per unit dose. This parameter change enables achieving reliable treatment efficacy through enhanced corticoid activity and synergistic effects, while simultaneously reducing toxicity and minimizing resistance risk associated with high antibiotic dosing.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If conventional antibiotic dosing is used, then infection coverage is achieved, but antibiotic resistance develops and amounts become excessive

Engineering Contradiction:
Improveinfection coverageVSAvoidantibiotic resistance
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The patent reduces the antibiotic amount parameter to less than 1 mg per unit dose and optimizes the corticoid/antibiotic ratio to 0.02 to 20 (preferably 0.4 to 2). This parameter optimization achieves infection coverage through improved pharmacokinetics and synergistic interactions, while minimizing antibiotic resistance development by reducing overall antibiotic exposure and selecting for resistant strains.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9636350B2Pharmaceutical composition for use in nasal administration containing corticoid, and a quinolone or fusidic acid
Publication Date: 2017.05.02 COMBISIN SARL

AI summary

The invention relates to a pharmaceutical composition of unit dose for inhalation by a human subject comprising a topical corticoid and a quinolone or fucidic acid, characterized in that the ratio of the weight of the topical corticoid to the weight of the quinolone or fucidic acid is between 0.02 and 20 and the amount of quinolone or of fucidic acid is less than 1 mg. This composition can be administered by nasal spray and is used for treating the upper and lower respiratory tract, in particular sinusitis and nasal polyps.