Ibuprofen Solid Solution Composition for Micelle-Based Absorption
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Solution Overview
Problem
Existing solid solution compositions for ibuprofen do not effectively inhibit pro-inflammatory responses and require hydrophilic solvents, limiting their delivery and absorption in the body.
Innovation Solution
A solid solution composition comprising ibuprofen, a mixture of saturated C10-C18 triglycerides, glyceryl monolinoleate, and a stabilizing agent, which forms micelles and is absorbed by the intestine, enhancing absorption by macrophages and dendritic cells without the need for hydrophilic solvents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If hydrophilic solvents are used in solid solution compositions, then the compositions can be formulated, but the delivery and absorption in the body is limited
Solution Approach 1:
The patent changes the fundamental parameter of the solvent system from hydrophilic to entirely hydrophobic components. The composition uses hydrophobic lipids (solid and liquid fats/oils) and hydrophobic co-solvents instead of hydrophilic solvents, fundamentally altering the formulation approach to enable effective delivery and absorption of the therapeutic compound in the body.
Solution Approach 2:
The patent creates a composite formulation system combining multiple hydrophobic components: solid lipids, liquid lipids, and hydrophobic co-solvents. This composite approach allows the composition to maintain structural integrity while enabling effective biological delivery, resolving the contradiction between manufacturability and delivery effectiveness.
2Stability of the object's composition
If lipid component and drug form organized matrices upon cooling, then solid solution composition is formed, but without hydrophilic solvent the formulation is limited
Solution Approach 1:
The patent changes the solvent polarity parameter from hydrophilic to hydrophobic, enabling solid solution formation through hydrophobic interactions while maintaining formulation flexibility. The composition can be adapted by selecting different hydrophobic lipids and co-solvents based on specific therapeutic needs.
Solution Approach 2:
The patent introduces hydrophobic co-solvents as intermediary substances that facilitate the formation of organized lipid-drug matrices. These co-solvents act as mediators between the solid lipid component and the therapeutic compound, enabling versatile formulation while maintaining stable solid solution structures.
3Stability of the object's composition
If only hydrophobic interactions are present, then solid solution composition is formed, but there is no organized alignment resulting in classic solid form
Solution Approach 1:
The patent creates a composite system combining solid lipids, liquid lipids, and hydrophobic co-solvents that work together to provide both stability and organized structure. The combination of different lipid phases and co-solvents creates a structured matrix that maintains solid solution stability while achieving organized alignment through the synergistic interaction of multiple hydrophobic components.
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 effectively inhibits pro-inflammatory responses and improves absorption of ibuprofen, providing improved treatment for inflammation and pain by forming micelles and being absorbed by immune cells.
Implementation Method 1
the resulting melted composition readily forms micelles which may be absorbed by the intestine, assembled into chylomicrons, and ultimately may be absorbed by macrophages or taken up by dendritic cells
Data Source
Figure 1A~1B
Figure 1C
AI summary
A pharmaceutical composition for treatment of inflammation or pain or chronic inflammation is liquid at normal human body temperature, namely 37°C, solid at room temperature, namely 20°C, and comprises: a) 25% to 31 % by weight of a non-steroidal anti-inflammatory drug (NSAID); b) 34% to 40% by weight of a lipid which is solid at room temperature, namely 20°C; c) 22% to 28% by weight of a lipid which is a liquid at room temperature, namely 20°C; and d) 7% to 13% by weight of a stabilizing agent comprising liquid glycol polymer.