Fat-Soluble Active Ingredient Formulation with Protective Colloid

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Solution Overview

Problem

Current formulations of fat-soluble active ingredients face challenges in achieving high bioavailability and stability, particularly due to extrusion loss during tablet formation, which affects shelf life and bioavailability in pharmaceutical applications.

Innovation Solution

A composition of a fat-soluble active ingredient combined with a protective colloid, characterized by a high extinction coefficient when dissolved in water, and a process to minimize extrusion loss, resulting in a formulation with enhanced bioavailability and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If fat-soluble active ingredient is incorporated into tablets, then bioavailability is improved, but extrusion loss occurs during tablet formation reducing stability and shelf life

Engineering Contradiction:
ImprovebioavailabilityVSAvoidextrusion loss
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

A protective colloid is introduced as an intermediary substance between the fat-soluble active ingredient and the tablet matrix. This protective colloid forms a stable dispersion that prevents the active ingredient from being extruded during tablet formation, thereby eliminating extrusion loss while maintaining bioavailability. The protective colloid acts as a mediator that protects the active ingredient from harmful interactions with the tablet formulation components.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Stability of the object's composition

If amount of fat-soluble active ingredient is increased to compensate for extrusion loss, then stability is maintained, but bioavailability efficiency decreases

Engineering Contradiction:
ImprovestabilityVSAvoidamount of active ingredient
Core Design Contradiction:
Stability of the object's compositionVSQuantity of substance

Solution Approach 1:

The protective colloid provides a feedback mechanism by forming a stable dispersion that continuously protects the active ingredient from extrusion. This stable dispersion maintains consistent levels of active ingredient throughout the tablet's shelf life, eliminating the need to overcompensate with higher initial amounts. The feedback loop ensures that the active ingredient remains protected and bioavailable without requiring excessive quantities.

Inventive Principle:
Principle #23Feedback

3Duration of action of stationary object

If protective colloid is used to prevent extrusion loss, then stability and shelf life are improved, but formulation complexity increases

Engineering Contradiction:
Improveshelf lifeVSAvoidformulation complexity
Core Design Contradiction:
Duration of action of stationary objectVSDevice complexity

Solution Approach 1:

The protective colloid changes the physical-chemical parameters of the formulation by creating a stable dispersion system. This dispersion has specific rheological properties that prevent extrusion while maintaining simplicity in the overall formulation approach. The parameter changes in the protective colloid's structure and behavior enable it to provide long-term stability without requiring complex multi-component systems or sophisticated formulation strategies.

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

The formulation achieves high bioavailability with reduced extrusion loss, leading to improved stability and extended shelf life of fat-soluble active ingredients in pharmaceutical tablets, and is suitable for use in dietary supplements, food, feed, and personal care products.

Implementation Method 1

a protective colloid characterized in that said composition when dissolved, dispersed or diluted in/with water has an extinction E1/1

Methodology Applied
Scientific EffectColloidal protection: Colloid

Implementation Method 2

measuring the absorption of the solution, and o calculation of the percentage of the total amount of the fat-soluble active ingredient pressed out

Methodology Applied
Scientific EffectLight absorption: Absorption (EM radiation)

Data Source

PatentEP1940249B1Novel formulations of fat-soluble active ingredients with high bioavailability
Publication Date: 2015.06.03 DSM IP ASSETS BV

AI summary

The present invention relates to formulations of a pharmacological effective fat-soluble active ingredient with a high bioavailability of said fat-soluble active ingredient as well as to their manufacture and use as dietary supplement, food, feed, personal care product and/or pharmaceutical. Such formulations are those which when dissolved, dispersed or diluted in/with water have an extinction E 1/1 at a wavelength in the range of from 200 to 800 nm, preferably in the range of from 250 to 600 nm, more preferably in the range of from 250 to 500 nm, more preferably in the range of from 370 to 485 nm, of = 380, preferably of = 600, most preferably = 900. In preferred embodiments of the formulations of the present invention such formulations show an extrusion loss of fat-soluble active ingredient of = 30% when pressed to tablets.