Lipoic Acid Pellets Coated for Stability

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Solution Overview

Problem

Lipoic acid's chemical-physical characteristics, such as insolubility in water and reactivity, pose challenges in formulating stable pharmaceutical compositions, leading to degradation and interactions with other components, resulting in unstable and ineffective formulations.

Innovation Solution

The use of lipoic acid pellets coated with a polymeric insulating layer and a gastric pH-resistant layer, combined with a lipophilic medium like fish oil or cod liver oil, which contains Omega 3 fatty acids, prevents interactions and ensures stability and high purity of the active ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If lipoic acid is used in powder form without pre-treatment, then the formulation process is simple, but the composition stability deteriorates due to polymerisation and interactions with other components

Engineering Contradiction:
Improveformulation process simplicityVSAvoidcomposition stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The lipoic acid is segmented into individual pellets, each encapsulated in a protective coating system. This segmentation isolates the reactive lipoic acid from direct contact with other components, preventing polymerisation and interactions while maintaining formulation simplicity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

An intermediary coating layer is introduced between the lipoic acid and other composition components. This coating acts as a barrier that prevents direct interactions and chemical reactions, thereby stabilizing the composition without complicating the manufacturing process.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If lipoic acid is combined with multiple active ingredients, then the therapeutic effect is enhanced, but the stability deteriorates due to interactions and degradation between components

Engineering Contradiction:
Improvecombination with multiple active ingredientsVSAvoidcomposition stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

Each active ingredient is encapsulated in separate pellets with individual protective coatings. This segmentation allows multiple ingredients to coexist in the same formulation without direct interactions, maintaining both therapeutic versatility and composition stability.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

Different pellets have different coating properties tailored to their specific active ingredients. This local quality approach allows each ingredient to be protected according to its specific stability requirements, enabling stable combinations of multiple ingredients with diverse chemical characteristics.

Inventive Principle:
Principle #3Local quality

3Ease of manufacture

If lipoic acid is used as is without coating, then the manufacturing process is simple, but the manufacturing precision deteriorates due to difficulty in handling and formulation

Engineering Contradiction:
Improvemanufacturing process simplicityVSAvoidformulation precision
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The physical and chemical parameters of lipoic acid are changed by enclosing it in pellets with controlled coating properties. This transformation improves handling characteristics and formulation precision while maintaining ease of manufacture through a standardized coating process.

Inventive Principle:
Principle #35Parameter changes

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

This approach results in stable, easy-to-formulate compositions that maintain the integrity of lipoic acid and other active ingredients, reducing degradation and allowing for high-purity formulations, even with reactive components like gamma-linolenic acid, enhancing the stability and effectiveness of the final product.

Implementation Method 1

particles consisting of an inert nucleus, coated with lipoic acid, in turn further coated by a first layer of insulating polymeric material and a second polymeric layer resistant to the gastric pH

Methodology Applied
Scientific EffectPhysical containment: Physical Containment

Data Source

PatentEP2217220B1Lipoic acid pellet composition
Publication Date: 2011.04.20 LAB CHIM INTERNAZ

AI summary

The present invention concerns a new composition based on pellets of lipoic acid in a lipophilic medium, if necessary combined with other active ingredients.