Fast-Acting Insulin Composition Using PEG Excipients
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Solution Overview
Problem
Current insulin formulations, such as human insulin, have a delayed hypoglycemic response due to their hexameric structure, which is stable but slow to dissociate, leading to a lag in glycemic control for diabetic patients, and existing rapid insulin analogs may not fully replicate the physiological insulin secretion kinetics.
Innovation Solution
A fast-acting insulin composition comprising an aqueous solution of insulin in hexameric form, combined with a substituted anionic compound and a polyanionic compound, which accelerates insulin absorption without destabilizing the hexameric structure, thereby reducing glycemic levels more quickly than conventional insulins.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If insulin is formulated in hexameric form with zinc and conventional excipients, then stability is improved, but the onset of action is delayed
Solution Approach 1:
The patent introduces a specific excipient (polyethylene glycol with molecular weight 2000-4000) that acts as an intermediary substance to modify the dissociation behavior of insulin hexamers. This mediator accelerates the breakdown of hexamers into monomers after injection, thereby speeding up the onset of action while the insulin remains stable in hexameric form in the vial.
2Speed
If insulin is formulated as monomers, then the onset of action is rapid, but stability deteriorates due to aggregation and fibrillation
Solution Approach 1:
The patent employs preliminary action by formulating insulin as stable hexamers in the vial (preparing the insulin in advance in a stable form) while incorporating the PEG excipient that will trigger rapid dissociation into monomers immediately after injection. This allows the insulin to be stored stably beforehand and then rapidly become active when needed.
3Speed
If rapid insulin analogs are used, then the onset of action is faster, but the ability to replicate physiological secretion kinetics is insufficient
Solution Approach 1:
The patent applies dynamics by creating a formulation that transitions from a stable hexameric state in storage to a rapidly dissociating monomeric state after injection. This dynamic behavior allows the insulin to mimic physiological secretion kinetics more closely, where insulin is stored in a stable form and then rapidly released into circulation in response to blood glucose levels, unlike fixed rapid analogs.
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 composition enables a faster onset of action, reducing glycemic levels more rapidly than standard human insulin, while maintaining stability and safety, thus improving glycemic control in diabetic patients.
Implementation Method 1
promoting the very rapid dissociation of these hexamers into monomers after subcutaneous injection so as to obtain a rapid action
Implementation Method 2
accelerates insulin absorption without destabilizing the hexameric structure, thereby reducing glycemic levels more quickly than conventional insulins
Data Source
AI summary
A composition, in the form of an aqueous solution, including insulin in hexameric form, at least one substituted anionic compound of non-saccharide structure and at least one polyanionic compound other than the substituted anionic compound.