Insulin Suspension Formulation for Stability and Dual-Action Profile
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current insulin preparations for diabetes treatment face challenges in providing a stable and effective formulation that balances fast and prolonged action, with existing formulations often experiencing chemical deterioration due to high NaCl and glycerol concentrations, and lacking resistance to physical stress.
Innovation Solution
A pharmaceutical formulation comprising crystalline and dissolved insulin analogues or derivatives, protamine, Zn2+, a buffer, a phenolic compound, and an isotonic agent in specific ratios, prepared through a method involving acidic and alkaline solution mixing to achieve a stable suspension with adjustable pH and composition.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If high NaCl concentration is used to stabilize insulin preparations, then stability is improved, but chemical deterioration increases due to interaction with glycerol and glucose
Solution Approach 1:
The patent removes NaCl from the insulin preparation formulation entirely, replacing it with alternative stabilizing agents. This extraction of the harmful component (NaCl) eliminates the source of chemical deterioration while maintaining stability through other means such as optimized pH control and alternative excipients.
Solution Approach 2:
The patent changes the formulation parameters by reducing or eliminating NaCl concentration and adjusting the concentrations of other components such as glycerol, glucose, and buffer systems. This parameter change resolves the contradiction by finding a new formulation balance that provides stability without the harmful chemical deterioration caused by high NaCl.
2Adaptability or versatility
If protamine insulin crystals are suspended in solution to provide both fast and prolonged action, then therapeutic effectiveness is improved, but resistance to physical stress decreases
Solution Approach 1:
The patent creates a composite formulation containing both dissolved insulin and protamine insulin crystals in a unified suspension system. This composite structure allows the preparation to exhibit both fast-acting (dissolved insulin) and prolonged-acting (crystalline insulin) properties while maintaining physical stability through optimized formulation components and ratios.
Solution Approach 2:
The patent optimizes physical stress resistance by adjusting formulation parameters including pH, ionic strength, and excipient concentrations. These parameter changes enhance the stability of the crystal suspension without compromising the dual-action therapeutic profile, thereby improving reliability under various storage and handling conditions.
3Adaptability or versatility
If crystalline and dissolved insulin are combined in a premixed suspension, then both fast and prolonged action are achieved, but formulation complexity increases
Solution Approach 1:
The patent merges dissolved insulin and crystalline protamine insulin into a single premixed suspension formulation. This combining eliminates the need for separate fast-acting and long-acting injections, simplifying the treatment regimen for patients while maintaining the dual-action profile through a unified, stable formulation system.
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 formulation provides a stable suspension with improved resuspendability and uniform distribution, maintaining insulin activity and reducing chemical deterioration, thus enhancing the quality of life for diabetic patients by offering a balanced action profile.
Implementation Method 1
retarded acting insulin preparations can be suspensions containing insulin in crystalline and/or amorphous form precipitated by addition of zinc salts alone or by addition of protamine
Implementation Method 2
insulin in crystalline and/or amorphous form precipitated by addition of zinc salts alone or by addition of protamine
Data Source
AI summary
The invention provides a pharmaceutical formulation and a method for preparing the formulation.