Amorphous Psilocybin Solid Dispersion for Fast Onset Stability

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Solution Overview

Problem

Current psilocybin formulations have a slow onset and long duration of action, and the amorphous form is unstable, leading to challenges in therapeutic applications for conditions like anxiety, headache, and eating disorders.

Innovation Solution

Development of stable compositions of amorphous psilocybin and deuterated psilocybin that modulate serotonin 5-HT2 receptors, preventing crystallization and allowing for faster therapeutic onset and shorter duration, with formulations like lyophilized fast-dissolving tablets and once-daily dosing.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If amorphous psilocybin is used to improve solubility and therapeutic onset, then therapeutic onset speed is improved, but stability deteriorates due to crystallization tendency

Engineering Contradiction:

Improvetherapeutic onset speedVSAvoidamorphous form stability

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent introduces a polymer matrix as an intermediary carrier that stabilizes amorphous psilocybin by preventing crystallization. The polymer acts as a mediating substance that maintains the amorphous state during storage and administration, enabling the drug to retain improved solubility and faster onset characteristics without undergoing unwanted crystallization.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite material system combining psilocybin with specific polymers to form a stable amorphous solid dispersion. This composite structure leverages the favorable pharmacokinetic properties of amorphous psilocybin while the polymer component provides structural stability, resolving the contradiction between rapid onset and compositional stability.

Inventive Principle:

Principle #40Composite materials

2Stability of the object's composition

If crystalline psilocybin is used to improve stability, then shelf life is improved, but therapeutic onset speed deteriorates

Engineering Contradiction:

Improveshelf lifeVSAvoidtherapeutic onset speed

Core Design Contradiction:

Stability of the object's compositionVSSpeed

Solution Approach 1:

The patent changes the physical state parameter of psilocybin from crystalline to amorphous through formulation in a polymer matrix. This parameter change enables the drug to achieve both improved solubility/faster onset and acceptable stability, as the amorphous form in the solid dispersion maintains molecular-level disorder that prevents rapid crystallization while enhancing dissolution characteristics.

Inventive Principle:

Principle #35Parameter changes

3Duration of action of moving object

If extended release formulation is used to prolong duration of action, then duration of therapeutic effect is improved, but onset speed deteriorates

Engineering Contradiction:

Improveduration of therapeutic effectVSAvoidonset speed

Core Design Contradiction:

Duration of action of moving objectVSSpeed

Solution Approach 1:

The patent segments the drug delivery system into multiple functional components: the polymer matrix provides controlled release to extend duration, while the amorphous psilocybin dispersed in the matrix ensures rapid initial dissolution and onset. This segmentation allows simultaneous optimization of both onset speed and duration of action through the combined effects of different formulation elements.

Inventive Principle:

Principle #1Segmentation

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

These compositions provide improved pharmaceutical performance with quicker therapeutic effects, reducing psychedelic side effects and improving neural plasticity and cognitive functions, suitable for treating various psychiatric and neurological disorders.

Implementation Method 1

stable formulations of amorphous psilocybin and/or deuterated psilocybin which prevent/reduce amorphous to crystalline transitions

Methodology Applied

Scientific EffectCrystallization prevention:

Implementation Method 2

a solid dispersion comprising a therapeutically effective amount of a compound of Formula (I) in amorphous form dispersed in a polymer

Methodology Applied

Scientific EffectPhysical stabilization:

Data Source

PatentUS20250360148A1Solid dispersions of psilocybin

Publication Date: 2025.11.27 CYBIN IRL LTD

AI summary

The present disclosure relates to stable pharmaceutical compositions of amorphous psilocybin and deuterated psilocybin, and to the use of such pharmaceutical compositions in the treatment of diseases associated with a serotonin 5-HT2 receptor. The pharmaceutical compositions are formulated with solid dispersions of psilocybin or deuterated psilocybin in amorphous form dispersed in a polymer.