Porous Phytosterol Microparticles for Cholesterol Management

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Solution Overview

Problem

Current phytosterol preparations face challenges in achieving high bioavailability and stability for cholesterol-lowering tablets or pills, with existing solutions often resulting in low physiological activity, shelf-life issues, and the need for large dosages due to inefficient delivery mechanisms.

Innovation Solution

A method involving the preparation of porous microparticles by creating a homogeneous melt of phytosterols with partially water-soluble components, such as fatty acids or surfactants, followed by solidification and processing into a fine powder, which is then treated with an aqueous phase to enhance bioavailability and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional phytosterol preparations are used, then cholesterol lowering effect is achieved, but bioavailability is low and large dosages are required

Engineering Contradiction:
Improvephytosterol dosageVSAvoidbioavailability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent employs porous silica gel particles as a carrier material to adsorb phytosterols. The porous structure provides high surface area and pore volume, enabling increased phytosterol loading capacity while maintaining particle integrity. This resolves the contradiction by allowing effective delivery of phytosterols in smaller dosages through enhanced adsorption capacity.

Inventive Principle:
Principle #31Porous materials

Solution Approach 2:

The invention creates a composite material system combining phytosterols with porous silica gel particles. The composite structure leverages the adsorption properties of silica gel and the cholesterol-lowering activity of phytosterols, achieving improved bioavailability and reduced dosage requirements through synergistic material combination.

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If phytosterol concentration is increased to improve efficacy, then cholesterol lowering effect is enhanced, but stability and shelf-life deteriorate

Engineering Contradiction:
Improvephytosterol concentrationVSAvoidshelf-life
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent extracts phytosterols from their native oil environment and transfers them onto porous silica gel particles. This separation removes phytosterols from the triglyceride matrix that causes instability, allowing high concentration formulation while maintaining stability through the inert porous carrier structure.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The porous silica gel acts as an intermediary carrier between the phytosterols and the final formulation environment. It provides a stable platform that prevents direct interaction between phytosterols and degrading factors, enabling high concentration storage with improved shelf-life.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of manufacture

If phytosterols are delivered in conventional forms, then manufacturing is simple, but physiological activity is low

Engineering Contradiction:
Improvemanufacturing simplicityVSAvoidphysiological activity
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent performs preliminary adsorption of phytosterols onto porous silica gel particles before final formulation. This pre-concentration and stabilization step enhances physiological activity by improving bioavailability, while the straightforward adsorption process maintains manufacturing simplicity.

Inventive Principle:
Principle #10Preliminary action

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 method produces microparticles with significantly increased surface area and bioavailability, allowing for effective cholesterol lowering with higher phytosterol concentrations in compact, stable formulations, as demonstrated by clinical studies showing substantial LDL-cholesterol reduction.

Implementation Method 1

A composition according to any one of claims 1-6, wherein the phytosterol component is adsorbed onto the porous support material

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentUS9078464B2Compositions of phytosterols with enhanced bioavailability
Publication Date: 2015.07.14 EDIO HEALTHCARE
  • US9078464B2 patent drawing
  • US9078464B2 patent drawing

AI summary

A method for preparing porous microparticles containing phytosterol, by preparing a homogeneous melt of phytosterol and a partially water soluble component, cooling the melt to obtain an amorphous solid material, processing the material into a fine powder, and bringing the powder into contact with an aqueous phase under stirring conditions. A composition suitable for preparing a porous microparticle containing phytosterol. A porous microparticle containing phytosterol. A pharmaceutical or food product useful for lowering the cholesterol level in blood.