Encapsulated Phytoactive Combination for Bioavailability

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Solution Overview

Problem

Curcumin, chlorogenic acid, and catechin have poor bioavailability due to low solubility, rapid metabolism, and rapid elimination, limiting their therapeutic effects, and existing formulations lack synergistic combinations to enhance their absorption and stability.

Innovation Solution

A combination of phytoactives is developed by encapsulating curcumin, chlorogenic acid, and catechin using modified starch and maltodextrin as encapsulating agents, with solvents like dichloromethane and ethanol, to increase bioavailability and stability, allowing for enhanced delivery through oral routes in the form of powders or granules.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If curcumin, chlorogenic acid and catechin are administered orally, then therapeutic effects are achieved, but bioavailability is poor due to low solubility and rapid metabolism

Engineering Contradiction:
ImprovebioavailabilityVSAvoidrapid metabolism and elimination
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The patent uses piperine as an intermediary substance that inhibits metabolic enzymes and transporters, thereby reducing rapid metabolism and elimination of curcumin, chlorogenic acid and catechin. This mediator approach directly addresses the bioavailability problem by preventing premature degradation of the active ingredients in the gastrointestinal tract.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite formulation combining curcumin, chlorogenic acid, catechin, and piperine in specific ratios within a unified dosage form. This composite approach allows the ingredients to work synergistically, where piperine enhances the bioavailability of all three active ingredients simultaneously, overcoming the individual bioavailability limitations of each component.

Inventive Principle:
Principle #40Composite materials

2Reliability

If curcumin is used at high doses to improve therapeutic effect, then anti-inflammatory and antitumor activities increase, but absorption remains poor and metabolism accelerates

Engineering Contradiction:
Improvetherapeutic effectVSAvoidabsorption and bioavailability
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

Piperine serves as a metabolic inhibitor that blocks the breakdown of curcumin and other active ingredients, allowing higher therapeutic doses to be absorbed effectively. This intermediary mechanism enables the body to retain and utilize higher quantities of the active substances without rapid metabolism eliminating them.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the pharmacokinetic parameters of curcumin, chlorogenic acid and catechin by combining them with piperine, which changes the absorption and metabolism rates. This parameter change allows the active ingredients to remain in the bloodstream longer at higher concentrations, improving therapeutic effectiveness.

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If green coffee beans are roasted to reduce chlorogenic acid, then flavor and color improve, but health benefits related to weight loss and diabetes risk reduction decrease

Engineering Contradiction:
Improveprocessing and flavorVSAvoidchlorogenic acid content
Core Design Contradiction:
Ease of manufactureVSQuantity of substance

Solution Approach 1:

The patent extracts chlorogenic acid from green coffee beans before roasting, preserving the health benefits in the extract while allowing the beans to be roasted for flavor and color development. This extraction approach separates the functional component (chlorogenic acid) from the sensory component (roasted bean characteristics), enabling both quality attributes to be optimized independently.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent performs the extraction of chlorogenic acid as a preliminary step before roasting the coffee beans. This preliminary action preserves the bioactive compounds in their most potent form while the subsequent roasting process develops the desired flavor and color properties, avoiding the loss of health benefits that would occur if chlorogenic acid were present during roasting.

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 encapsulated combination significantly increases bioavailability, stability, and therapeutic effects, improving endurance, reducing cortisol levels, aiding in muscle recovery, and promoting weight and fat loss, with synergistic effects beyond individual active ingredients.

Implementation Method 1

encapsulating curcumin, chlorogenic acid and/or catechin using modified starch and maltodextrin as encapsulating agents

Methodology Applied
Scientific EffectEncapsulation: Physical Containment

Implementation Method 2

enhanced delivery through oral routes in the form of powders or granules

Methodology Applied
Scientific EffectOral absorption: Absorption (physical)

Data Source

PatentUS20220143126A1Synergistic combination of phytoactives
Publication Date: 2022.05.12 JEYAKODI SHANKARANARAYANAN

AI summary

The present invention relates to a combination of phytoactives comprising plant extracts that deliver curcumin, chlorogenic acid and/or catechin. The invention also relates to a process for preparing such combination with enhanced therapeutic and pharmacological effect. The phytoactives combination is used for enhancing endurance and stamina, for significantly reducing cortisol levels thus reducing stress, for elevating hydrolysis of adenosine triphosphate (ATP), for improving blood flow, for quick recovery from sports injury, for better weight and fat loss compared to individual actives, for increasing and strengthening muscles and for increasing maximum oxygen uptake during incremental exercise.