Biphasic Excipient Solid Phase Surface Area
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Solution Overview
Problem
Bioactive agents with high octanol-water partition coefficients exhibit poor oral bioavailability and pharmacokinetics due to aggregation in lipid phases in the gastrointestinal tract, leading to limited absorption and significant excretion.
Innovation Solution
Formulating biphasic compositions with a high surface-area-to-volume solid phase and a solvent-rich liquid phase to enhance the dissolution of hydrophobic agents, allowing them to partition into the gastrointestinal epithelium rather than lipid phases, thereby improving bioavailability and pharmacokinetics, and potentially bypassing hepatic-portal circulation by dissolving in the buccal cavity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hydrophobic agents are administered orally, then they can be delivered to the body, but they aggregate in lipid phases in the gastrointestinal tract leading to poor absorption and excretion
Solution Approach 1:
The invention divides the hydrophobic agent into fine particles with a surface-area-to-volume ratio greater than 500 per meter, creating a solid phase that can be dispersed in the liquid phase. This segmentation prevents aggregation in lipid phases and enables the agent to partition into the gastrointestinal epithelium for improved absorption and reduced excretion.
2Ease of manufacture
If hydrophobic agents are dissolved in lipid phases, then they can be formulated for administration, but they partition into lipid phases in the gastrointestinal tract rather than being absorbed
Solution Approach 1:
The invention changes the physical parameters of the hydrophobic agent by creating a solid phase with extremely high surface-area-to-volume ratio (>500 per meter) and formulating it in a biphasic composition with a solvent-rich liquid phase. This parameter change allows the agent to dissolve in the liquid phase during buccal cavity dissolution, bypassing hepatic-portal circulation and enabling direct absorption into the body.
3Reliability
If hydrophobic agents are absorbed into the body, then they can exert therapeutic effects, but they undergo oxidation by cytochrome P450 enzymes in the liver reducing their effectiveness
Solution Approach 1:
The invention uses the buccal cavity as an intermediary route for dissolution and absorption. By formulating the biphasic composition to dissolve in the buccal cavity, the hydrophobic agent can be absorbed directly into the bloodstream, bypassing the hepatic-portal circulation and avoiding first-pass metabolism by cytochrome P450 enzymes, thereby preserving therapeutic effectiveness.
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 biphasic composition method significantly enhances the oral bioavailability and pharmacokinetics of hydrophobic agents by facilitating their absorption into the body, reducing excretion, and potentially bypassing first-pass metabolism through the liver.
Implementation Method 1
The oral administration of such biphasic compositions results in the dissolution of the excipients. When the hydrophobic agents are sufficiently separated in the biphasic composition, then the dissolution of the excipients results in the partitioning of the hydrophobic agents into the gastrointestinal epithelium
Implementation Method 2
the dissolution of the excipients results in the partitioning of the hydrophobic agents into the gastrointestinal epithelium rather than aggregation or partitioning into a lipid phase
Data Source
AI summary
Various aspects of this disclosure relate to excipients comprising a solid phase and a liquid phase, wherein the solid phase has a surface-area-to-volume ratio of at least 500 per meter, which improves the bioavailability and pharmacokinetics of various hydrophobic ingredients. Compositions comprising such excipients can be utilized to disperse a hydrophobic ingredient in a beverage, which improves the bioavailability and pharmacokinetics of the dispersed hydrophobic ingredient.