Dissolved Oxide Anion Formulations for Hydrophobic Molecule Absorption
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Solution Overview
Problem
Hydrophobic bioactive molecules exhibit poor bioavailability and pharmacokinetics, necessitating improved formulations to enhance their absorption and distribution in organisms.
Innovation Solution
Formulations comprising anions dissolved in water-miscible liquids that convert into hydrophobic molecules at neutral pH, maximizing surface area and facilitating rapid partitioning and absorption through epithelial tissues to avoid first-pass metabolism.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hydrophobic bioactive molecules are administered in conventional formulations, then the molecules can be delivered to the organism, but bioavailability and pharmacokinetics are poor due to limited absorption
Solution Approach 1:
The patent changes the chemical state of the bioactive molecule from neutral to anionic form for dissolution in water-miscible liquids, then utilizes pH-dependent conversion back to neutral hydrophobic form at the site of action. This parameter change enables both good solubility during administration and effective absorption at the target site, resolving the contradiction between bioavailability and absorption rate.
Solution Approach 2:
The patent introduces water-miscible liquids as intermediary carriers that temporarily hold the anionic form of the bioactive molecule. These liquids serve as a bridge between the hydrophilic administration route and the hydrophobic absorption mechanism, enabling improved bioavailability without sacrificing absorption efficiency.
2Reliability
If hydrophobic molecules are used to improve bioavailability, then absorption can be enhanced, but first-pass metabolism occurs reducing effective delivery
Solution Approach 1:
The patent performs preliminary dissolution of the bioactive molecule in water-miscible liquids in its anionic form before administration. This preliminary step allows the molecule to be properly solubilized and transported to the site of action without undergoing first-pass metabolism, as the conversion to hydrophobic form occurs at the target site rather than in the digestive tract.
3Quantity of substance
If anions are dissolved in water-miscible liquids, then solubility is improved, but the molecules must convert to hydrophobic form for absorption creating a complex mechanism
Solution Approach 1:
The patent employs pH-dependent self-conversion of the anionic form to neutral hydrophobic form at the site of action. The molecule utilizes the local pH environment to automatically convert from the soluble anionic form to the absorbable neutral form without requiring external intervention or complex conversion mechanisms, thus maintaining simplicity while achieving both solubility and absorption.
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
Improves bioavailability and pharmacokinetics by enabling rapid absorption of hydrophobic molecules into blood or skin tissues, bypassing first-pass metabolism.
Implementation Method 1
The administration of anions that are dissolved in a water-miscible liquid to an organism results in the pH-dependent conversion of the anions into hydrophobic molecules
Implementation Method 2
The molecules then rapidly partition out of the water-miscible liquid and adhere to the epithelium where they absorb into the blood
Implementation Method 3
The anions carry net negative charges that repel each other to maximize their surface area
Data Source
AI summary
Various aspects of this patent document relate to compositions that comprise an anion that is the conjugate base of a hydrophobic molecule that has a pKa, for example, of at least 7 and no greater than 12. These compositions display improved properties when formulated to interact with an organism because the anions carry negative charges that allows them to both dissolve in water-miscible liquids and maximize their surface area. Interaction with an organism results in at least partial conversion of the anion into the hydrophobic molecule after which the hydrophobic molecule partitions out of a water-miscible liquid and into the organism.