Sustained-Release Nutraceutical Powders for Higher Bioavailability
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Solution Overview
Problem
Existing nutraceutical delivery technologies are costly, inefficient, and result in low bioavailability due to high active compound load limitations, large dosage forms, and rapid metabolism of highly water-soluble compounds, making them uneconomical and inconvenient for consumers.
Innovation Solution
Formulations combining lipophilic or hydrophilic nutraceuticals with surfactants, oils, and sustained release polymers, converted into water dispersible powders, allowing for both immediate and sustained release properties, enhancing bioavailability and residence time.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If microemulsions and self-emulsifying formulations are used to improve bioavailability, then solubility and uptake of lipophilic nutraceuticals are enhanced, but the active compound load is limited to 5%-10% resulting in large capsules or multiple smaller capsules which are not economical and inconvenient for consumers
Solution Approach 1:
The patent uses composite materials by combining nutraceuticals with cyclodextrins to form inclusion complexes. This composite approach allows high active compound load (20%-80%) while maintaining improved bioavailability, resolving the contradiction between reliability and quantity of substance.
Solution Approach 2:
The patent changes the physical state and solubility parameters of the nutraceutical by complexing with cyclodextrins. This parameter change enables the formulation to achieve both high active compound load and improved bioavailability, eliminating the need for large capsules or multiple smaller capsules.
2Reliability
If cyclodextrin complexation is used to enhance solubility and bioavailability, then absorption is improved, but the process involves large amounts of aqueous or organic solvents or kneading equipment and requires drying and milling resulting in high processing costs and reduced active compound load to 10%-25%
Solution Approach 1:
The patent extracts and eliminates the need for large amounts of aqueous or organic solvents and complex kneading equipment by using a simplified one-step mixing process. This extraction of unnecessary components reduces processing cost while maintaining the ability to achieve high active compound load (20%-80%) and improved bioavailability.
3Reliability
If solid dispersions are used to improve solubility and bioavailability of nutraceuticals, then absorption is enhanced, but the process uses dissolving the active compound in a solvent and incorporation into the matrix followed by drying or wet granulation and milling making it uneconomical due to multiple steps, use of organic solvents, and necessary equipment
Solution Approach 1:
The patent segments the complex solid dispersion process into a single simple mixing step. This segmentation eliminates multiple steps including dissolving, incorporating, drying, wet granulation, and milling, thereby reducing device complexity and processing cost while maintaining improved bioavailability and high active compound load.
4Ease of manufacture
If melt granulation is used to granulate the active compound with polymers, then formulation is improved, but the process involves prolonged heating at the melting point of wax making it not suitable for many nutraceuticals that are heat sensitive
Solution Approach 1:
The patent replaces the heat-intensive melt granulation process with a cold or ambient temperature mixing process using cyclodextrin complexes. This substitution eliminates the need for prolonged heating at high temperatures, making the process suitable for heat-sensitive nutraceuticals while maintaining formulation capability.
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 formulations achieve higher bioavailability and sustained release of nutraceuticals, reducing dosage frequency and size, and maintaining therapeutic levels for extended periods, thus improving therapeutic efficacy and consumer compliance.
Implementation Method 1
The composition comprises a mixture of the active compound with surfactants, oil, and sustained release polymers
Implementation Method 2
The composition is converted into a water dispersible powder that can be formulated with other ingredients
Data Source
AI summary
The present disclosure describes economical processes to improve the bioavailability of nutraceuticals by formulations that induce micronization and sustained release. The inventive process can be used to increase the solubility and bioavailability of lipophilic and moderately water-soluble nutraceuticals by combining excipients that increase the solubility and induce sustained release of the active compounds. The inventive process also can be used to increase the residence time of highly water-soluble nutraceuticals that are metabolized and eliminated quickly from the body, consequently increasing the therapeutic potential. The disclosed formulations advantageously are freely flowing powders that can be used to formulate with other ingredients into tablets, capsules, or the like; or used as bulk powders.