Penicillin G Stabilization Using Malic and Caffeic Acid Buffers

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Solution Overview

Problem

Penicillin G solutions are unstable at varying temperatures and pH levels, leading to rapid degradation and the formation of undesirable side effects, limiting their storage duration and effectiveness as an antibiotic.

Innovation Solution

A composition comprising malic acid, caffeic acid, flavan-3-ols, anthocyanins, and optionally other phenolic compounds, which stabilizes alkali salts of penicillin G, allowing for extended storage and use as a dietary supplement and therapeutic agent, including for cancer treatment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If alkali salts of penicillin G are used to improve water solubility, then solubility is improved, but stability at varying pH and temperature deteriorates

Engineering Contradiction:
Improvewater solubilityVSAvoidstability at varying pH and temperature
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent introduces a buffer system comprising malic acid, caffeic acid, flavan-3-ols, and anthocyanins as intermediary substances that mediate between the penicillin G and the varying pH/temperature conditions. These buffer components maintain a stable pH environment (particularly around pH 3-4) and provide thermal stability, allowing penicillin G to remain stable in aqueous solution without requiring extreme storage conditions.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If penicillin G is stored at room temperature for extended periods, then convenience is improved, but degradation increases

Engineering Contradiction:
Improvestorage convenienceVSAvoidantibacterial efficacy
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent changes the chemical parameters of the solution by adding specific buffer components (malic acid, caffeic acid, flavan-3-ols, anthocyanins) that alter the pH stability and thermal resistance parameters. This allows the penicillin G solution to maintain its antibacterial efficacy at room temperature for extended periods (up to several weeks) without significant degradation, transforming the storage conditions from requiring refrigeration to allowing ambient storage.

Inventive Principle:
Principle #35Parameter changes

3Duration of action of stationary object

If penicillin G solution is stabilized with conventional methods, then storage time is extended, but degradation products causing allergies may still form

Engineering Contradiction:
Improvestorage durationVSAvoiddegradation products causing allergies
Core Design Contradiction:
Duration of action of stationary objectVSObject-generated harmful factors

Solution Approach 1:

The patent converts the potentially harmful degradation process into a beneficial outcome by using the buffer components to control and direct the stability mechanism. The malic acid, caffeic acid, flavan-3-ols, and anthocyanins work synergistically to maintain pH stability and prevent the formation of harmful degradation products like penicilloic acid and penicillenic acid, while still allowing extended storage. The buffer system essentially transforms the unstable degradation pathway into a stable preservation mechanism.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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 maintains the stability and antibacterial efficacy of penicillin G, preventing degradation and side effects, while also providing prophylactic and therapeutic benefits for cancer treatment.

Implementation Method 1

the stability of the alkali salts of penicillin G in water and alcohol is strongly dependent on pH and temperature

Methodology Applied
Scientific EffectpH buffering:

Implementation Method 2

A composition which comprises malic acid (A), caffeic acid (B), at least one compound from the group of flavan-3-ols (C) and at least one compound from the group of anthocyanins (D)

Methodology Applied
Scientific EffectAntioxidant activity: Oxidation

Data Source

PatentEP2135512B1Compound based on malic acid, caffeic acid, a flavan-3-ol and an anthocyane and its use in food and medicine
Publication Date: 2010.06.16 MUIN ALI DR
  • EP2135512B1 patent drawing
  • EP2135512B1 patent drawing

AI summary

Composition comprises malic acid, caffeic acid, at least one compound comprising flavan-3-ol and at least one compound comprising anthocyanin. An independent claim is included for an aqueous solution comprising the composition. ACTIVITY : Cytostatic; Anabolic; Antibacterial; Nootropic; Dermatological; Vulnerary. MECHANISM OF ACTION : None given.