Acylated Insulin–GLP-1 Composition for Less Frequent Diabetes Injections
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Solution Overview
Problem
Current insulin and GLP-1 compounds require frequent injections due to short duration of action and lack of effective combination formulations with improved stability and efficacy.
Innovation Solution
A novel pharmaceutical composition comprising acylated insulin and a long-acting GLP-1 compound, formulated with specific additives, achieving enhanced potency, stability, and prolonged action, allowing for less frequent injections.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If natural insulin or conventional insulin derivatives are used, then good drug efficacy is achieved, but the duration of action is short requiring frequent injections
Solution Approach 1:
The patent uses acylated insulin which combines insulin with fatty acid chains (C20-C24) to create a composite molecular structure. This composite material approach extends the duration of action from several hours to more than 24 hours, enabling once-daily or less frequent injections while maintaining therapeutic efficacy.
Solution Approach 2:
The patent modifies the physical and chemical parameters of insulin by acylation at specific positions (B29 or B30) with long-chain fatty acids. This parameter change in molecular structure fundamentally alters the pharmacokinetic profile, extending half-life and duration of action without sacrificing glucose-lowering effectiveness.
2Duration of action of moving object
If PEGylated insulin is used to extend action time, then duration of action is improved, but physical and chemical stability deteriorates
Solution Approach 1:
The patent changes the acylation approach from PEG chains to natural fatty acid chains (C20-C24). This parameter change in the chemical structure improves both duration of action and stability, as the fatty acid-modified insulin maintains better physical and chemical stability compared to PEGylated versions while achieving extended release.
3Reliability
If combination preparation of insulin and GLP-1 is developed, then drug efficacy is improved, but physical and chemical stability deteriorates
Solution Approach 1:
The patent merges acylated insulin with long-acting GLP-1 compounds into a single pharmaceutical composition. This combination product delivers dual mechanisms of action (insulin secretion stimulation and glucose-dependent insulinotropic effect) while maintaining stability through careful formulation design, overcoming the limitation of separate administrations.
Solution Approach 2:
The patent creates a composite pharmaceutical formulation containing both acylated insulin and GLP-1 compound. This composite material approach allows synergistic drug effects while managing physical and chemical stability through optimized excipient selection and formulation parameters.
4Ease of operation
If injection frequency is reduced for patient convenience, then ease of operation is improved, but duration of action must be extended which complicates formulation
Solution Approach 1:
The patent achieves simplified once-daily or less frequent dosing by fundamentally changing the molecular parameters of insulin through acylation. This parameter modification naturally extends duration of action without requiring complex delivery devices or formulations, making the solution both simple and effective.
Data Source
AI summary
Disclosed in the present invention is an acylated insulin preparation, a pharmaceutical composition of an acylated insulin and a long-acting GLP-1 compound, and a medical use of the preparation and the pharmaceutical composition.