Insulin-Lipid Complex via Organic Solvent System
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current methods for preparing insulin-lipid complexes face challenges due to low recombination rates and instability, particularly when using water as a solvent, which limits the solubility and stability of insulin in lipid complexes, and results in poor entrapment efficiency and membrane permeability.
Innovation Solution
The use of an organic solvent system containing a low boiling point acid, such as trifluoroacetic acid or hydrogen chloride, to form an insulin-lipid complex with a mass ratio of insulin to lipid material ranging from 1:3 to 1:15, which improves solubility and stability, and the preparation of oil solutions and vesicles for sustained-release and non-injectable formulations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If water is used as a solvent for preparing insulin-lipid complexes, then the preparation process is simple, but the recombination rate is low and the stability is poor
Solution Approach 1:
The patent changes the solvent parameter from water to organic solvents (ether, chloroform, dichloromethane, ethyl acetate, butyl acetate, or their mixtures with water). This parameter change enables the formation of stable insulin-lipid complexes with high recombination rates (over 90%) by providing a suitable environment for the interaction between insulin and lipid materials, thereby resolving the contradiction between ease of manufacture and reliability.
2Ease of manufacture
If water is used as a solvent, then the preparation method is easy to implement, but the entrapment efficiency is poor
Solution Approach 1:
By changing the solvent parameter to organic solvents or their mixtures with water, the patent achieves high entrapment efficiency (over 90%) in insulin-lipid complexes. The organic solvents facilitate better interaction between insulin and lipid materials, enabling effective entrapment of insulin within the lipid complex structure while maintaining ease of implementation through simple preparation procedures.
3Ease of manufacture
If water is used as a solvent, then the preparation process is straightforward, but the membrane permeability is poor
Solution Approach 1:
The patent changes the solvent parameter from water to organic solvents (ether, chloroform, dichloromethane, ethyl acetate, butyl acetate, or their mixtures with water), which significantly improves the membrane permeability of the resulting insulin-lipid complexes. The organic solvents enable better incorporation of insulin into the lipid structure, enhancing its ability to penetrate membranes while keeping the preparation process straightforward.
4Adaptability or versatility
If the mass ratio of insulin to lipid material is not optimized, then the preparation is flexible, but the recombination rate is low
Solution Approach 1:
The patent optimizes the mass ratio parameter of insulin to lipid material to be between 1:3 and 1:15, with preferred ranges of 1:4 to 1:12 and most preferred 1:5 to 1:10. This parameter optimization ensures high recombination rates (over 90%) while maintaining preparation flexibility, as the optimized ratio works effectively with the specified organic solvents and can be adapted to different insulin and lipid material types.
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
This approach achieves a recombination rate of over 90%, enhances insulin's lipophilicity, and improves stability and drug loading capacity, maintaining drug content and physical properties during storage and administration.
Implementation Method 1
dissolve the insulin and the lipid material in an organic solvent system containing a low boiling point acid to form a transparent solution
Implementation Method 2
organic solvent system containing a low boiling point acid, such as trifluoroacetic acid or hydrogen chloride, to form an insulin-lipid complex
Implementation Method 3
remove the solvent by rotary evaporation or the spray drying method, and drying
Implementation Method 4
remove the solvent by rotary evaporation or the spray drying method, and drying
Implementation Method 5
remove the solvent by rotary evaporation or the spray drying method, and drying under vacuum conditions
Data Source
AI summary
Provided are an insulin-lipid complex, a preparation method thereof, and a formulation thereof. The insulin-lipid complex is prepared by compounding insulin and a lipid material in an organic solvent system containing a low boiling point acid, and drying. The mass ratio of insulin to the lipid material is 1:3˜1:20. An oil solution of the insulin-lipid complex and vesicles containing insulin are further provided.