Zinc-Charged Insulin Oral Delivery via Ion Cloud Protection

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Solution Overview

Problem

Current methods for administering insulin, such as subcutaneous injections, are invasive, prone to complications, and do not mimic the natural physiological and pharmacokinetic conditions of insulin production, while oral administration is challenging due to insulin degradation in the stomach, lacking an effective, FDA-approved oral insulin product.

Innovation Solution

A zinc-charged insulin composition is developed, where loosely bound surface ions on insulin molecules are removed using a chelating agent and replaced with zinc, creating a 'zinc ion cloud' that protects insulin from stomach acid and enzymes, allowing it to be absorbed through the gastrointestinal tract.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If insulin is administered through subcutaneous injection, then effective absorption by the body is achieved, but injection site complications and pain occur

Engineering Contradiction:
Improveabsorption effectivenessVSAvoidinjection site complications
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses an absorption enhancer as an intermediary substance that facilitates insulin absorption through the intestinal wall without requiring injection. The absorption enhancer temporarily modifies the intestinal membrane permeability, allowing insulin to pass through while minimizing damage and inflammation, thus resolving the contradiction between effective delivery and avoiding injection site complications

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical injection system with a chemical absorption enhancement system. Instead of using physical force (needle injection) to deliver insulin into the tissue, the invention uses chemical agents (absorption enhancers) to facilitate passive diffusion of insulin through the intestinal wall into the bloodstream, eliminating the need for mechanical penetration and associated complications

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Reliability

If insulin is administered through subcutaneous injection, then effective absorption is achieved, but the pharmacokinetic conditions do not reflect natural insulin production

Engineering Contradiction:
Improveabsorption effectivenessVSAvoidpharmacokinetic similarity to natural insulin
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent inverts the traditional administration route by delivering insulin through the oral gastrointestinal tract rather than through subcutaneous injection. This inversion allows insulin to follow the natural physiological pathway it would take if secreted by the pancreas, where it would naturally be absorbed into the portal circulation and delivered to the liver first, thereby restoring pharmacokinetic similarity to natural insulin production

Inventive Principle:
Principle #13The other way round (Inversion)

3Stability of the object's composition

If insulin is administered orally, then natural physiological and pharmacokinetic conditions are reflected, but insulin is destroyed by stomach acid and enzymes

Engineering Contradiction:
Improvepharmacokinetic similarity to natural insulinVSAvoidinsulin degradation
Core Design Contradiction:
Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent applies preliminary protective action by pre-coating insulin molecules with absorption enhancers and protective polymers before oral administration. This preliminary encapsulation protects the insulin from stomach acid and enzymes during gastric passage, preventing degradation before the insulin can reach the absorption site in the intestinal wall

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent converts the harmful acidic environment of the stomach into a beneficial controlled-release mechanism. The absorption enhancers and protective coatings are designed to be stable in acidic conditions, allowing the insulin to survive gastric passage intact, then release the insulin in the intestinal environment where absorption can occur, thus converting the previously harmful stomach environment into a manageable delivery phase

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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 zinc-charged insulin effectively survives stomach conditions, is absorbed into the bloodstream, and provides long-lasting glucose regulation, reducing the frequency of administration and minimizing injection site complications, as demonstrated by significant reductions in blood glucose levels in both mice and human subjects.

Implementation Method 1

replacing all the loosely bound surface ions with Zinc... creating a 'zinc ion cloud' that protects insulin from stomach acid and enzymes

Methodology Applied
Scientific EffectChemical protection:

Implementation Method 2

removing any loosely bound surface ions present on a general insulin molecule using a chelating agent

Methodology Applied
Scientific EffectChelation:

Implementation Method 3

allowing it to be absorbed through the gastrointestinal tract

Methodology Applied
Scientific EffectGastrointestinal absorption: Absorption (physical)

Data Source

PatentUS11478534B1Formulation and method of preparing zinc-charged insulin for oral administration
Publication Date: 2022.10.25 AMERICA GREAT HEALTH
  • US11478534B1 patent drawing
  • US11478534B1 patent drawing
  • US11478534B1 patent drawing

AI summary

This invention is directed to a zinc-charged insulin composition that is effective in treating diabetes and lowering and stabilizing blood glucose levels when administered orally. The zinc-charged insulin is acid and enzyme resistant, such that the zinc-charged insulin is capable of surviving the acidic conditions of the stomach. The zinc-charged insulin is capable of being absorbed through the gastrointestinal tract and stored in the liver, such that the zinc-charged insulin is long lasting and pharmacokinetically similar to the insulin normally generated by the body. The invention is further directed to a method of preparing the zinc-charged insulin composition, including: (1) removing any loosely bound surface ions present on an insulin molecule using a chelating agent; and (2) replacing all the loosely bound surface ions with zinc.