N-Alkylamide Solid Dispersion via Hot Extrusion
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Solution Overview
Problem
Current formulations of natural or synthetic N-alkylamides have low bioavailability due to poor solubility and dispersion in aqueous phases, leading to ineffective delivery and bioaccessibility, and existing manufacturing processes are complex and difficult to implement.
Innovation Solution
A composition comprising a thermoformed extrudate with natural or synthetic N-alkylamides dispersed in carriers like amino acids, peptides, proteins, saccharides, or lipids, using hot extrusion to create a solid dispersion with enhanced solubility and bioavailability, packaged in various forms for administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If N-alkylamides are formulated in conventional carriers, then the formulation can be manufactured, but the solubility and dispersion in aqueous phases remains poor leading to low bioavailability
Solution Approach 1:
The patent changes the physical state of the N-alkylamide from crystalline to amorphous form, and incorporates it into a solid dispersion matrix with hydrophilic carriers. This parameter change in molecular arrangement and phase state dramatically improves aqueous solubility and bioavailability while maintaining manufacturing feasibility
Solution Approach 2:
The patent creates a composite material system consisting of amorphous N-alkylamide dispersed within a solid matrix of hydrophilic carriers (polymers, surfactants, or lipids). This composite structure combines the therapeutic properties of N-alkylamide with the solubility-enhancing properties of the carrier materials, resolving the contradiction between poor solubility and manufacturing capability
2Reliability
If complex manufacturing processes are used to improve solubility and bioavailability, then the formulation performance improves, but the manufacturing complexity and difficulty increases
Solution Approach 1:
The patent utilizes phase transition during hot melt extrusion, where the N-alkylamide and carrier materials are heated above their melting points to form a homogeneous molten mixture, then cooled to create a solid dispersion. This controlled phase transition simplifies manufacturing by eliminating the need for complex solvent-based processes while ensuring consistent amorphous formation and high bioavailability
Solution Approach 2:
The patent replaces complex multi-step mechanical mixing and drying processes with a single hot melt extrusion step. The extrusion process combines heating, mixing, and forming in one continuous operation, significantly simplifying manufacturing while producing the required amorphous solid dispersion structure for high bioavailability
3Ease of operation
If N-alkylamides are administered in conventional forms, then the administration is straightforward, but the release properties and effective delivery to target sites is insufficient
Solution Approach 1:
The patent changes the physical form of N-alkylamide from crystalline to amorphous within a solid dispersion, which fundamentally alters the release properties. The amorphous form provides faster dissolution and more predictable release kinetics in biological fluids, ensuring effective delivery to target sites while maintaining ease of administration through various dosage forms such as tablets, capsules, or injectables
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 significantly increases the bioavailability and stability of N-alkylamides, maintaining effective solubility and release properties over time, even in intestinal environments, and is easier to manufacture and administer.
Implementation Method 1
using hot extrusion to create a solid dispersion with enhanced solubility and bioavailability
Implementation Method 2
The composition significantly increases the bioavailability and stability of N-alkylamides
Implementation Method 3
A composition comprising a thermoformed extrudate with natural or synthetic N-alkylamides dispersed in carriers like amino acids, peptides, proteins, saccharides, or lipids, using hot extrusion to create a solid dispersion with enhanced solubility and bioavailability
Data Source
Figure 1~2
AI summary
The present invention relates to a composition comprising at least one natural or synthetic N-alkylamide as an active substance, its manufacturing process and its use.