Psilocin Co-Crystal Formulation for Stability and Dissolution Control

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Solution Overview

Problem

Existing psilocin formulations lack desirable properties for pharmaceutical applications, such as high crystallinity, chemical and physical stability, and suitable processing characteristics, which are essential for effective treatment of psychiatric disorders.

Innovation Solution

Development of co-crystals and salts of psilocin with co-formers like L-lactic acid, decanoic acid, ethyl maltol, oleic acid, palmitic acid, p-coumaric acid, propyl gallate, and stearic acid, which enhance crystallinity, stability, and processing suitability, and modulate dissolution and solubility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional psilocin formulations are used, then the basic pharmacological activity is maintained, but the crystallinity, chemical and physical stability, and processability are insufficient for effective pharmaceutical treatment

Engineering Contradiction:
Improvechemical and physical stabilityVSAvoidprocessability
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent changes the physical and chemical parameters of psilocin by forming co-crystals with specific co-formers (L-lactic acid, decanoic acid, ethyl maltol, oleic acid, palmitic acid, p-coumaric acid, propyl gallate, and stearic acid). This transforms the solid form from amorphous or poorly crystalline to highly crystalline, thereby improving chemical and physical stability while also enhancing processability for pharmaceutical manufacturing.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite crystalline structures by combining psilocin with multiple different co-formers to produce co-crystals. Each co-crystal combination represents a composite material with optimized properties, where the co-former molecules are incorporated into the crystal lattice with psilocin, resulting in enhanced stability and improved manufacturing characteristics.

Inventive Principle:
Principle #40Composite materials

2Reliability

If co-crystals with multiple co-formers are developed, then crystallinity and stability are improved, but the complexity of formulation development increases

Engineering Contradiction:
ImprovecrystallinityVSAvoidformulation development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the co-former options into distinct categories (L-lactic acid, decanoic acid, ethyl maltol, oleic acid, palmitic acid, p-coumaric acid, propyl gallate, and stearic acid), allowing systematic evaluation and selection of the most suitable co-former(s). This segmentation enables managed complexity by organizing the development process into manageable steps rather than treating all possibilities as a single complex problem.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

By systematically varying the chemical structure and properties of co-formers (changing parameters such as molecular size, functional groups, and physical properties), the patent optimizes crystallinity and stability while managing development complexity through structured parameter exploration rather than unstructured trial-and-error.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If dissolution rate and solubility are modulated through co-crystal formation, then pharmaceutical performance is improved, but the control over dissolution characteristics becomes more difficult

Engineering Contradiction:
Improvedissolution rateVSAvoidcontrol over dissolution characteristics
Core Design Contradiction:
ProductivityVSEase of operation

Solution Approach 1:

The patent modulates dissolution rate and solubility by changing the crystal structure parameters through co-crystal formation. Different co-formers produce co-crystals with different lattice energies, packing arrangements, and surface properties, which systematically control dissolution characteristics. This provides predictable control over dissolution behavior rather than unpredictable variation.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The co-formers act as intermediary substances that mediate between psilocin molecules, facilitating the formation of crystal structures with optimized dissolution properties. These co-formers serve as control elements that allow pharmacologists to tune dissolution characteristics by selecting appropriate co-formers, making the control process more manageable and predictable.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 co-crystals and salts provide improved pharmaceutical formulations with enhanced stability, processability, and controlled dissolution rates, suitable for treating psychological and neurological disorders.

Implementation Method 1

a co-crystal comprising psilocin and a co-former provides a crystalline form with favourable properties such as high crystallinity

Methodology Applied
Scientific EffectCrystallisation: Crystallisation

Implementation Method 2

The use of the co-crystal may also provide modulation of the dissolution rate and kinetic solubility

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentUS12559458B2Co-crystals or salts of psilocin and methods of treatment therewith
Publication Date: 2026.02.24 RESET PHARMACEUTICALS INC
  • US12559458B2 patent drawing
  • US12559458B2 patent drawing
  • US12559458B2 patent drawing

AI summary

The invention relates to a co-crystal or salt comprising psilocin and a co-former. The co-crystal or salt is useful in methods of treating or preventing a disease or condition selected from depression, anxiety, death anxiety, demoralization, adjustment disorders, hopelessness, suicidal ideation, desire for hastened death, cocaine-related disorders, opioid-related disorders and stimulant-related disorders in a patient. A kit comprising the co-crystal or salt is also described.