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
Engineering 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
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.
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.
2Reliability
If co-crystals with multiple co-formers are developed, then crystallinity and stability are improved, but the complexity of formulation development increases
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.
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.
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
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.
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.
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
Implementation Method 2
The use of the co-crystal may also provide modulation of the dissolution rate and kinetic solubility
Data Source
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.


