Phytosterol Ester and Diacylglyceride Mixture for Cholesterol Reduction

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Solution Overview

Problem

Phytosterol supplementation can adversely affect the bioavailability of lipophilic vitamins and pharmaceutical active ingredients, such as vitamins A, E, and carotenoids, due to their mechanism of inhibiting cholesterol absorption, which is a concern for individuals requiring these nutrients for health conditions like hypercholesterolemia and cardiovascular diseases.

Innovation Solution

A method involving a mixture of phytosterol esters (PS-E) and diacylglycerides (DAG), dissolved or dispersed in edible oils or fats, is administered to maintain or increase the bioavailability of lipophilic vitamins and drugs, while delivering phytosterols for therapeutic benefits without compromising their absorption.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional phytosterol preparations are administered to reduce cholesterol levels, then cholesterol absorption is inhibited and blood cholesterol levels decrease, but the bioavailability of lipophilic vitamins (A, E) and carotenoids is adversely affected

Engineering Contradiction:
Improvecholesterol levelsVSAvoidbioavailability of lipophilic vitamins and carotenoids
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent introduces an intermediary substance (phytosterol ester mixed with specific lipids such as triglycerides, diglycerides, or monoglycerides) that mediates between the cholesterol-lowering effect and the bioavailability of lipophilic vitamins. This lipid matrix acts as a carrier that prevents the phytosterol ester from interfering with vitamin absorption while maintaining its cholesterol-inhibiting properties.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite material by combining phytosterol esters with specific lipids (triglycerides, diglycerides, or monoglycerides) in defined ratios. This composite formulation maintains the hypocholesterolemic effect while the lipid component ensures proper absorption and bioavailability of both the phytosterol and co-administered lipophilic vitamins and carotenoids.

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If higher amounts of plant sterols and stanols are consumed to enhance cholesterol-lowering effects, then blood cholesterol levels decrease more significantly, but absorption and bioavailability of other lipophilic nutrients are further reduced

Engineering Contradiction:
Improvecholesterol-lowering effectVSAvoidabsorption of lipophilic vitamins and carotenoids
Core Design Contradiction:
Quantity of substanceVSLoss of substance

Solution Approach 1:

The patent changes the physical and chemical parameters of the phytosterol delivery system by esterifying the phytosterols and mixing them with specific lipids. This parameter change (from free phytosterols to phytosterol esters in a lipid matrix) allows for enhanced cholesterol-lowering effects at higher doses without proportionally increasing the loss of other lipophilic nutrients, as the lipid matrix facilitates their co-absorption.

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 PS-E and DAG combination maintains or increases the serum levels of vitamins A, E, and carotenoids, while effectively reducing cholesterol levels, providing a therapeutic advantage over conventional phytosterol preparations by minimizing adverse effects on bioavailability.

Implementation Method 1

The consumption of higher amounts of plant sterols and plant stanols lowers blood cholesterol levels by inhibiting the absorption of dietary and endogenously-produced cholesterol from the small intestine. This inhibition is related to the similarity in physico-chemical properties of plant sterols and stanols to cholesterol.

Methodology Applied
Scientific EffectMicelle formation and competition: Emulsion

Implementation Method 2

A method involving a mixture of phytosterol esters (PS-E) and diacylglycerides (DAG), dissolved or dispersed in edible oils or fats, is administered to maintain or increase the bioavailability of lipophilic vitamins and drugs

Methodology Applied
Scientific EffectLipid carrier-mediated absorption: Solvation

Data Source

PatentUS8772270B2Treatment methods requiring phyto-ingredients
Publication Date: 2014.07.08 ENZYMOTEC
  • US8772270B2 patent drawing
  • US8772270B2 patent drawing
  • US8772270B2 patent drawing

AI summary

The invention provides methods for treatment of conditions which require phytosterol therapy without adversely affecting the bioavailability of lipophilic vitamins or lipophilic drugs. The method includes administering a mixture of phytosterol ester(s) (PS-E) and 1,3-diglyceride(s) (DAG) dissolved in an edible oil or fat. The invention also provides a method of improving weight management and a method of treating metabolic conditions that result in overweight. Dietary nutrients, food supplements and food articles containing the mixture are also provided.