Teicoplanin A2 A3 Ratio Synergy Antibiotic Activity

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Solution Overview

Problem

Current glycopeptide antibiotics, such as Teicoplanin, have limitations in antibiotic activity due to the lower efficacy of certain components like Teicoplanin A3 compared to Teicoplanin A2, and existing methods do not effectively harness the synergistic potential of these components for enhanced antibiotic activity.

Innovation Solution

A glycopeptide antibiotic composition is developed with a specific ratio of Teicoplanin A2 (TA2) and Teicoplanin A3 (TA3) components, where the TA3 content is adjusted within a certain range to achieve a synergistic effect, improving the overall antibiotic activity by combining TA2 and TA3 in a pharmaceutical composition.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If Teicoplanin A3 component is used to reduce production cost, then manufacturing cost decreases, but antibiotic activity is reduced

Engineering Contradiction:

Improveproduction costVSAvoidantibiotic activity

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the concentration parameter of TA3 in the composition from trace amounts (0-12%) to a specific range (16-73%). This parameter optimization reveals that moderate TA3 content enhances antibiotic activity through synergistic interaction with TA2, resolving the contradiction between production cost and antibiotic efficacy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite glycopeptide composition by combining TA2 and TA3 in specific ratios. This composite approach leverages the synergistic effect between the two components, where TA3 enhances the antibiotic activity of TA2, achieving improved efficacy while maintaining cost-effectiveness

Inventive Principle:

Principle #40Composite materials

2Reliability

If Teicoplanin A2 is used as the main component, then antibiotic activity is maintained, but production cost increases

Engineering Contradiction:

Improveantibiotic activityVSAvoidproduction cost

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent optimizes the concentration parameter of TA2 from near 100% to a range of 27-84%, demonstrating that reduced TA2 content combined with optimized TA3 content maintains or enhances antibiotic activity while reducing production cost

Inventive Principle:

Principle #35Parameter changes

3Reliability

If pure Teicoplanin A2 is used, then antibiotic activity is high, but synergistic potential is not utilized

Engineering Contradiction:

Improveantibiotic activityVSAvoidsynergistic potential

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent merges TA2 and TA3 into a combined composition with optimized ratios. This merging exploits the synergistic potential between the two components, where TA3 enhances the antibiotic activity of TA2, achieving activity levels up to 150 IU higher than commercial compositions containing only TA2

Inventive Principle:

Principle #5Merging (Combining)

Data Source

PatentUS7981859B2Glycopeptide composition with improved antibiotic activity

Publication Date: 2011.07.19 AXELLIA PHARMA APS

AI summary

A glycopeptide composition with improved antibiotic activity is disclosed, along with a method of preparing such a composition and a pharmaceutical composition made therefrom.