EDTA Oral Bioavailability via Piperine and Enteric Coating

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Solution Overview

Problem

The existing oral administration of EDTA for treating atherosclerosis and heavy metal accumulation is limited by poor bioavailability and absorption, making intravenous administration time-consuming and expensive, and traditional oral forms less effective.

Innovation Solution

Combining EDTA with piperine and using enteric coating to enhance bioavailability and absorption, potentially with additional therapeutic agents like ACE inhibitors or statins, to create a time-release formulation for improved oral administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration of EDTA is used, then patient convenience and cost are improved, but bioavailability and absorption are insufficient

Engineering Contradiction:
Improvepatient convenienceVSAvoidbioavailability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent combines EDTA with piperine to create a composite formulation. Piperine enhances the bioavailability and absorption of EDTA in the gastrointestinal tract, allowing oral administration to achieve therapeutic blood levels that were previously only attainable through intravenous injection. This composite approach resolves the contradiction by maintaining patient convenience while improving reliability of drug delivery.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

Piperine acts as an intermediary substance that facilitates the absorption of EDTA. It modifies the gastrointestinal environment and transport mechanisms to enable better uptake of EDTA, thereby serving as a mediator between the oral route of administration and the bloodstream, resolving the bioavailability issue while preserving oral convenience.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If intravenous administration of EDTA is used, then bioavailability is improved, but treatment time and cost increase

Engineering Contradiction:
ImprovebioavailabilityVSAvoidtreatment time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent enables patients to self-administer EDTA at home through oral tablets or capsules containing the EDTA-piperine formulation. This eliminates the need for time-consuming intravenous injections administered by medical professionals in clinical settings. Patients can take the medication conveniently at home, significantly reducing treatment time and healthcare facility requirements while maintaining effective bioavailability through the piperine enhancement.

Inventive Principle:
Principle #25Self-service

3Quantity of substance

If higher dosages of EDTA are administered, then therapeutic effectiveness is improved, but side effects increase

Engineering Contradiction:
ImprovedosageVSAvoidside effects
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the delivery parameters of EDTA by combining it with piperine and using enteric coating technology. This changes the absorption profile and bioavailability of EDTA, allowing lower dosages to achieve the same therapeutic effect that previously required higher doses. By improving the efficiency of drug delivery, the formulation reduces the total quantity of EDTA needed, thereby minimizing side effects while maintaining therapeutic effectiveness.

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

This approach allows for more effective and stable therapeutic levels of EDTA in the body, reducing the frequency of administration, enabling higher dosages, and potentially lowering treatment costs by allowing self-administration outside medical facilities, while minimizing side effects.

Implementation Method 1

agents in combination with EDTA that can improve the bioavailability, absorption, and/or half-life of EDTA in the body

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

agents in combination with EDTA that can improve the bioavailability, absorption, and/or half-life of EDTA in the body

Methodology Applied
Scientific EffectAbsorption enhancement: Absorption (physical)

Implementation Method 3

orally available composition including enteric coated EDTA or a pharmaceutically acceptable derivative or pro-drug thereof

Methodology Applied
Scientific EffectProtective coating: Coatings

Implementation Method 4

create a time-release formulation for improved oral administration

Methodology Applied
Scientific EffectControlled release:

Implementation Method 5

Ethylenediamine tetra-acetic acid (EDTA) binds to metals, for example transition state metals

Methodology Applied
Scientific EffectChelation: Chemical Bonding

Data Source

PatentUS8685374B2EDTA containing compositions and uses thereof
Publication Date: 2014.04.01 RAY & TERRY S HEALTH PROD

AI summary

EDTA and EDTA related compositions and methods of using them are described herein. The compositions can have improved bioavailability over EDTA alone. The compositions can be useful in the treatment or prevention of atherosclerosis or for the treatment of heavy metal accumulation.