Indole Compound Compositions for Controlled Transdermal and Nasal Dosing

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Existing psilocybin and psilocybin analogue dosing methods are unpredictable, subject to first-pass metabolism, and require intensive monitoring due to variable plasma concentrations and individual responses, making it difficult to establish optimal dosing for neurological disorders, and microdosing lacks effective delivery systems for safe and flexible administration.

Innovation Solution

Development of novel indole compounds and pharmaceutical compositions for transdermal and nasal delivery systems that bypass gastrointestinal metabolism, providing controlled release and improved pharmacokinetic profiles, allowing for safer and more flexible dosing regimens for neurological disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral dosing of psilocybin is used, then the compound can be administered easily, but first-pass metabolism reduces bioavailability and creates unpredictable plasma concentrations

Engineering Contradiction:
Improveease of administrationVSAvoidpredictability of plasma concentration
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent uses transdermal patches as an intermediary delivery system between the psilocybin compound and the bloodstream. The patch contains psilocybin embedded in a polymer matrix that controls release through the skin, bypassing first-pass metabolism and providing predictable plasma concentrations without requiring oral ingestion

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If oral dosing of psilocybin is used, then administration is simple, but intensive monitoring is required due to variable individual responses

Engineering Contradiction:
Improveease of administrationVSAvoidmonitoring requirements
Core Design Contradiction:
Ease of operationVSDevice complexity

Solution Approach 1:

The transdermal patch serves as a controlled intermediary that regulates psilocybin delivery through the skin into systemic circulation. The polymer matrix controls release kinetics, providing stable plasma concentrations that reduce inter-individual variability and minimize the need for intensive clinical monitoring

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the delivery parameter from oral ingestion to transdermal penetration. This parameter change results in controlled release kinetics and predictable pharmacokinetics, reducing the variability that currently requires intensive monitoring

Inventive Principle:
Principle #35Parameter changes

3Object-affected harmful factors

If microdosing of psilocybin analogues is used, then therapeutic effects may be achieved with reduced side effects, but effective delivery systems are lacking

Engineering Contradiction:
Improveadverse effectsVSAvoiddelivery system availability
Core Design Contradiction:
Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

The transdermal patch acts as a sophisticated intermediary delivery system that enables precise microdosing of psilocybin analogues. The polymer matrix controls release at low doses, and the transdermal route bypasses first-pass metabolism, providing reliable bioavailability for microdose regimens that previously lacked effective delivery mechanisms

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the delivery parameter to transdermal microdosing, enabling precise control of low doses. This parameter change provides the missing delivery system capability for microdosing psilocybin analogues, achieving therapeutic effects with reduced adverse effects

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12396982B2Compositions of matter and pharmaceutical compositions
Publication Date: 2025.08.26 ATAI THERAPEUTICS INC
  • US12396982B2 patent drawing
  • US12396982B2 patent drawing
  • US12396982B2 patent drawing

AI summary

Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.