5MeODMT Benzoate Salt Formulation via Cyclodextrin Complexation

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Solution Overview

Problem

5-methoxy-N,N-dimethyltryptamine (5MeODMT) is not well understood and poses challenges in formulating effective pharmaceutically useful compositions due to its handling difficulties and limited exploration of its uses.

Innovation Solution

Development of pharmaceutically acceptable salts, specifically benzoate salts of 5MeODMT, with adjustable dosage forms and delivery methods, including oral, transdermal, inhalable, and rectal forms, to enhance handling and efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If 5MeODMT is formulated for effective delivery, then therapeutic efficacy is improved, but handling difficulties and formulation challenges increase

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidformulation difficulty
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent uses cyclodextrins as intermediary molecules that form inclusion complexes with 5MeODMT. The cyclodextrin cavity encapsulates the tryptamine molecule, creating a stable complex that is easier to handle and formulate while maintaining therapeutic efficacy. This mediator approach resolves the contradiction by making the difficult-to-handle 5MeODMT more manageable through molecular complexation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates composite formulations combining 5MeODMT with excipients including mucoadhesive enhancers and cyclodextrins. These composite materials integrate multiple functional components that collectively improve handling properties, stability, and delivery efficiency while maintaining the active compound's therapeutic effects.

Inventive Principle:
Principle #40Composite materials

2Reliability

If particle size is reduced to enhance bioavailability, then absorption is improved, but manufacturing complexity increases

Engineering Contradiction:
ImprovebioavailabilityVSAvoidmanufacturing complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent systematically varies particle size parameters to optimize bioavailability. By controlling particle size within specific ranges and using different polymorphic forms, the formulation achieves enhanced absorption without requiring overly complex manufacturing processes. The parameter optimization approach balances performance improvement with manufacturing feasibility.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If permeation is increased for effective delivery, then bioavailability is improved, but mucosal irritation increases

Engineering Contradiction:
ImprovebioavailabilityVSAvoidmucosal irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs mucoadhesive enhancers as intermediary substances that facilitate drug permeation through mucosal barriers without directly causing irritation. These mediators enable controlled transport of 5MeODMT across mucosal membranes, improving bioavailability while the mucoadhesive properties provide a protective effect that reduces direct irritation to the mucosa.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the potentially harmful high permeation capability into a beneficial effect by using controlled release mechanisms and mucoadhesive formulations. The high permeation property, which could cause irritation, is harnessed in a controlled manner to improve bioavailability while the formulation design mitigates the harmful irritation effects, effectively converting a potential harm into a benefit.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentEP4279070A2Composition comprising a benzoate salt of 5-methoxy-n,n-dimethyltryptamine
Publication Date: 2023.11.22 BECKLEY PSYTECH LIMITED
  • EP4279070A2 patent drawingFigure 1~3
  • EP4279070A2 patent drawingFigure 4A~4E
  • EP4279070A2 patent drawingFigure 5

AI summary

A composition comprising a pharmaceutically effective amount of a pharmaceutically acceptable benzoate salt of 5-methoxy-N,N-dimethyltryptamine (5MeODMT).