Divalent Cation-Charged Insulin for Oral Delivery
Find Innovative SolutionsGenerate Solutions
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 and bioavailable oral insulin product.
Innovation Solution
Development of a divalent cation-charged insulin composition, specifically with Zinc, Calcium, or Magnesium, that survives stomach acid and is absorbed through the gastrointestinal tract by using a chelating agent like EDTA to remove loosely bound ions and replace them with these divalent cations, enabling oral administration and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If insulin is administered through subcutaneous injection, then it can be effectively absorbed by the body, but it causes injection site complications and does not mimic natural physiological conditions
Solution Approach 1:
The patent uses a chelating agent (EDTA) as an intermediary to remove loosely bound metal ions from insulin, then introduces divalent cations (Zinc, Calcium, or Magnesium) as new intermediaries to stabilize the insulin molecule. This allows oral administration by protecting insulin from degradation while enabling absorption, eliminating injection complications while maintaining effectiveness
Solution Approach 2:
The patent changes the chemical parameters of insulin by replacing loosely bound surface ions with specifically selected divalent cations. This parameter change (ionic composition) transforms insulin from a form suitable only for injection to a form stable enough for oral administration, while maintaining its biological activity and pharmacokinetic properties
2Ease of operation
If insulin is administered orally, then it mimics natural physiological conditions and avoids injection complications, but it is degraded by stomach acid and enzymes
Solution Approach 1:
The patent applies preliminary action by pre-treating insulin with a chelating agent to remove unstable loosely bound ions, then stabilizing it with divalent cations before oral administration. This preliminary stabilization prevents degradation by stomach acid and enzymes, enabling reliable oral delivery while maintaining convenience
Solution Approach 2:
Divalent cations act as protective intermediaries between insulin and the harsh gastric environment. These cations stabilize the insulin molecule structure, preventing denaturation and degradation by stomach acid and proteases, thereby enabling oral administration to succeed
3Reliability
If subcutaneous injection is used, then insulin reaches the bloodstream effectively, but it is stored in muscle and fat tissues instead of the liver
Solution Approach 1:
The patent replaces the mechanical injection system with a chemical stabilization system using divalent cations. This substitution allows insulin to be delivered through the gastrointestinal tract naturally, following the same physiological pathway as endogenous insulin, thereby restoring pharmacokinetic similarity to natural insulin production while maintaining effective delivery
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 divalent cation-charged insulin composition effectively reduces blood glucose levels and is absorbed into the bloodstream, providing long-lasting glucose control, similar to naturally produced insulin, with bioavailability demonstrated in both animal and human trials, and the ability to convert subcutaneously injected insulins like Lispro and Glargine for oral use.
Implementation Method 1
removing any loosely bound surface ions present on a general insulin molecule using a chelating agent
Implementation Method 2
replacing all the loosely bound surface ions with Zinc, Calcium, or Magnesium or some combination thereof
Data Source
AI summary
This invention is directed to a cation-charged insulin composition that is effective in treating diabetes and lowering and stabilizing blood glucose levels when administered orally. The cation-charged insulin is acid and enzyme resistant, such that the cation-charged insulin is capable of surviving the acidic conditions of the stomach. The cation-charged insulin is capable of being absorbed through the gastrointestinal tract and stored in the liver, such that the cation-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 cation-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, magnesium, or calcium.