Multiphase Active Preparations for Oxidation-Sensitive Compounds

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Solution Overview

Problem

Oxidation-sensitive active compounds in existing preparations suffer from stability issues during storage due to oxidation reactions, which are typically addressed by jointly adding antioxidants, leading to suboptimal shelf life.

Innovation Solution

Separately add antioxidants to an aqueous phase and then add oxidation-sensitive active compounds, forming separate multiparticulate phases within a coherent phase, ensuring spatial separation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If antioxidants are jointly added with active compounds, then the preparation process is simplified, but the shelf life and stability of oxidation-sensitive active compounds deteriorate

Engineering Contradiction:

Improvepreparation process simplicityVSAvoidshelf life and stability

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The invention divides the preparation into separate phases: an aqueous phase containing antioxidants and a hydrophobic phase containing oxidation-sensitive active compounds. This segmentation prevents direct contact between antioxidants and active compounds, eliminating oxidation while maintaining manufacturing feasibility through phase-separated formulation

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention introduces a hydrophobic phase (oil phase) as an intermediary barrier between the antioxidant-containing aqueous phase and the oxidation-sensitive active compounds. This intermediary layer physically isolates the active compounds from oxidation while allowing the system to remain stable and manufacturable

Inventive Principle:

Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If antioxidants are added to protect active compounds, then oxidation resistance improves, but the active compounds may still undergo oxidation reactions during storage

Engineering Contradiction:

Improveoxidation resistanceVSAvoidcompositional stability during storage

Core Design Contradiction:

Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The invention segments the formulation into distinct aqueous and hydrophobic phases, with antioxidants confined to the aqueous phase and oxidation-sensitive active compounds confined to the hydrophobic phase. This physical segmentation provides both oxidation resistance and compositional stability by preventing harmful interactions while maintaining ingredient integrity

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention applies local quality by creating different chemical environments in different phases: the aqueous phase provides antioxidant protection, while the hydrophobic phase provides oxidation isolation. Each phase has optimized local properties that collectively solve both oxidation resistance and compositional stability

Inventive Principle:

Principle #3Local quality

3Device complexity

If antioxidants and active compounds are premixed, then the formulation process is simplified, but oxidation reactions occur reducing active compound integrity

Engineering Contradiction:

Improveformulation process complexityVSAvoidactive compound integrity

Core Design Contradiction:

Device complexityVSManufacturing precision

Solution Approach 1:

The invention segments the formulation into separate aqueous and hydrophobic phases that do not require intensive mixing. The aqueous phase containing antioxidants and the hydrophobic phase containing active compounds can be combined with minimal mixing, reducing formulation complexity while maintaining active compound integrity through phase separation

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention creates locally optimized phases where antioxidants reside in the aqueous phase and active compounds reside in the hydrophobic phase. This local quality differentiation allows simple formulation processing while ensuring active compound integrity is maintained through physical isolation from oxidation-prone environments

Inventive Principle:

Principle #3Local quality

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 method significantly enhances the shelf life of active compound preparations by stabilizing oxidation-sensitive compounds, particularly retinoids and vitamin D, through spatial separation of antioxidants and active compounds.

Implementation Method 1

two separate phases are embedded multiparticulately into a coherent phase... one of the embedded phases comprises at least one oxidation-sensitive active compound and the second comprises at least one antioxidant

Methodology Applied

Scientific EffectPhase separation: Emulsion

Data Source

PatentUS20260000615A1Multiphase active substance preparations

Publication Date: 2026.01.01 BASF SE

AI summary

The present invention relates to solid, at least three-phase active substance preparations, in which two separate phases are embedded multiparticulately into a coherent, active substance-free and antioxidant-free phase, where one of the embedded phases comprises at least one oxidation-sensitive active substance and the second comprises at least one antioxidant. The invention also relates to a method for producing these active substance preparations, and to the use thereof in food supplements, foods, feeds, body care products, and pharmaceuticals.