Encapsulated DMT Microparticles with MAOI for Oral Bioavailability
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Solution Overview
Problem
N, N-dimethyltryptamine (DMT) and 5-methoxy-N, N-dimethyltryptamine (5-MeO-DMT) are thermolabile and subject to first-pass metabolism, leading to degradation and reduced bioavailability when orally administered, necessitating strategies to protect these molecules from degradation and enhance their stability and therapeutic efficacy.
Innovation Solution
Encapsulation of DMT or 5-MeO-DMT in pH-sensitive polymers, such as Eudragit, to control release and prevent degradation, combined with monoamine oxidase inhibitors (MAOIs) like curcumin or resveratrol to inhibit first-pass metabolism, allowing for oral administration and prolonged action.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral administration is used for DMT or 5-MeO-DMT, then convenience and safety are improved, but first-pass metabolism causes degradation and reduced bioavailability
Solution Approach 1:
The patent introduces an intermediary substance (MAO inhibitor) that mediates between the drug and the metabolic degradation process. The MAO inhibitor blocks the enzyme monoamine oxidase, preventing the first-pass metabolism of DMT or 5-MeO-DMT in the liver, thus preserving bioavailability while maintaining oral administration convenience
Solution Approach 2:
The patent applies preliminary anti-action by pre-administering the MAO inhibitor before the DMT or 5-MeO-DMT to block the degradation pathway in advance. This ensures that when the psychedelic compound is metabolized by the liver, the MAO inhibitor is already in place to prevent the degradation, thereby maintaining bioavailability
2Ease of operation
If DMT or 5-MeO-DMT is administered orally, then ease of administration is improved, but thermolability and photodegradability cause molecular degradation
Solution Approach 1:
The MAO inhibitor acts as a protective intermediary that shields DMT or 5-MeO-DMT from metabolic degradation. By blocking the enzymatic pathway, it prevents molecular breakdown while allowing the compound to remain stable during oral administration
Solution Approach 2:
The patent creates a protective metabolic environment by introducing the MAO inhibitor, which establishes an inert zone around the DMT or 5-MeO-DMT molecule, preventing oxidative and enzymatic attacks that would otherwise degrade the compound
3Device complexity
If conventional oral formulation is used, then simplicity is improved, but duration of action is reduced due to rapid metabolization
Solution Approach 1:
The patent ensures continuity of useful action by maintaining elevated levels of active DMT or 5-MeO-DMT in the bloodstream through the MAO inhibitor's continuous blocking of degradation. This extends the duration of action while keeping the formulation relatively simple
Solution Approach 2:
The MAO inhibitor is administered in advance to establish continuous protection against metabolism. This preliminary action ensures that the drug remains active longer by preventing rapid breakdown, thereby extending duration of action
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 encapsulation system increases the chemical stability and bioavailability of DMT and 5-MeO-DMT, enabling effective oral administration by controlling release and minimizing first-pass metabolism, thereby enhancing therapeutic efficacy and duration of action.
Implementation Method 1
particles are encapsulated in a pH-sensitive polymer
Implementation Method 2
monoamine oxidase inhibitors (MAOIs) like curcumin or resveratrol to inhibit first-pass metabolism
Data Source
AI summary
The present invention relates to a process of obtaining encapsulated microparticles and/or nanoparticles of DMT/5-MeO-DMT, or pharmaceutically acceptable salts or derivatives thereof and a composition prepared by the process. Pharmaceutical compositions comprising the particles can further include an inhibitor of the Monoamine oxidase (MAOI), and are useful for the personalized treatment of neurological and/or psychiatric disorders, and/or inflammatory disorders.