Lipid Matrix Core Particles for Stable Fat-Soluble Drug Loading

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Solution Overview

Problem

Existing technologies face challenges in incorporating therapeutically effective amounts of fat-soluble active ingredients into multi-particulate materials while maintaining potency and shelf-stability, particularly due to the difficulty in processing and layering these ingredients on inert cores.

Innovation Solution

A composition comprising particles with a lipid matrix core containing a fat-soluble active ingredient, which can be coated with additional layers, ensuring the active ingredient is dispersed within the core and protected from degradation, thereby enhancing potency and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If fat-soluble active ingredients are processed into dry form and micronized for layering on inert cores, then they can be incorporated into multi-particulate materials, but potency is greatly reduced and stability issues arise

Engineering Contradiction:
Improveease of layeringVSAvoidpotency and stability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the physical state parameter of the fat-soluble active ingredient from dry micronized powder to liquid or semi-liquid form. This parameter change enables direct incorporation into the core material without requiring micronization processing, thereby maintaining potency and stability while achieving ease of manufacture through simple mixing processes

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite core material consisting of a lipid matrix combined with fat-soluble active ingredients in liquid or semi-liquid form. This composite approach allows the active ingredient to be uniformly distributed and stabilized within the lipid matrix, eliminating the need for micronization while maintaining both manufacturability and product reliability

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If therapeutically effective amounts of fat-soluble active ingredients are incorporated into multi-particulate materials, then product potency is improved, but shelf-stability deteriorates due to degradation

Engineering Contradiction:
Improveamount of active ingredientVSAvoidshelf-stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent changes the physical state parameter of the active ingredient to liquid or semi-liquid form and incorporates it into the core material in this state. This parameter change allows for better integration and protection within the matrix, maintaining stability while achieving therapeutically effective concentrations

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent incorporates stabilizing components into the core formulation beforehand to prevent degradation of the fat-soluble active ingredient. This prior cushioning approach addresses stability issues before they occur during storage, allowing high concentrations of active ingredient to be maintained with improved shelf-stability

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

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 solution allows for the effective incorporation of fat-soluble active ingredients, such as carotenoids and cannabinoids, into oral dosage forms, maintaining potency and preventing degradation, thus addressing issues of stability and product quality.

Implementation Method 1

a core containing a lipid matrix having an active ingredient dispersed therein

Methodology Applied
Scientific EffectDispersion: Dispersion (of waves)

Data Source

PatentEP4054348B1Particles containing a lipid matrix core and active ingredient
Publication Date: 2026.01.28 LONZA SALES AG

AI summary

A composition containing a plurality of particles containing a core having a lipid matrix including an active ingredient dispersed therein is disclosed. The active ingredient can include a fat-soluble active ingredient. The particles can be contained in a capsule. Also provided are methods for producing a pharmaceutical composition containing a plurality of particles containing a core having a lipid matrix including an active ingredient dispersed therein.