Psilocin Salt Crystals for Solubility and Dose Stability
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Solution Overview
Problem
Psilocin has limited stability and solubility in aqueous solutions, leading to variable effects and slow onset of therapeutic action, making it difficult to administer accurate doses, especially for intravenous use, and limiting its application in microdosing.
Innovation Solution
Development of crystalline forms of psilocin salts or cocrystals with coformers such as acetic acid, benzenesulfonic acid, and butyric acid, which exhibit improved solubility and stability, allowing for stable formulations suitable for intravenous administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If psilocin is administered orally, then it can be delivered to patients, but the onset of therapeutic effects is slow (up to 40 minutes) and there is variable absorption leading to inaccurate dosing
Solution Approach 1:
The patent changes the physical-chemical parameters of psilocin by converting it from free base form to salt forms (hydrochloride, sulfate, phosphate, nitrate, perchlorate, bromide, iodide, picrate, perrhenate, periodate, periodate, and trifluoroacetate salts). This parameter change enables formulation in aqueous solutions suitable for parenteral administration, achieving faster onset and more precise dosing control.
2Speed
If psilocin is formulated for intravenous administration, then faster onset of action and standardized plasma concentrations can be achieved, but the solubility in aqueous media is relatively low
Solution Approach 1:
The patent applies parameter changes by converting psilocin into various salt forms with different solubility characteristics. The hydrochloride, sulfate, phosphate, and other salt forms exhibit improved aqueous solubility compared to the free base, enabling effective intravenous formulation while maintaining the desired fast onset of action.
3Ease of operation
If psilocin is stored in aqueous solutions, then it can be prepared for administration, but the stability is limited and rapid degradation occurs on exposure to light
Solution Approach 1:
The patent changes the chemical form of psilocin from free base to various stable salt forms. These salt forms exhibit improved stability in aqueous solutions and reduced sensitivity to light exposure, while still allowing for practical formulation preparation and administration.
4Quantity of substance
If microdosing is implemented, then lower quantities of psilocin can be administered for maintenance doses, but the low solubility limits the ability to accurately administer low doses
Solution Approach 1:
The patent applies parameter changes by using psilocin salt forms with improved aqueous solubility. This enables the preparation of low-concentration solutions suitable for microdosing, allowing accurate administration of small maintenance doses that would be difficult to achieve with the less soluble free base form.
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 crystalline forms provide enhanced solubility, stability, and reduced interindividual variability, enabling faster onset of action and more precise dose administration, suitable for intravenous, subcutaneous, and oral delivery.
Implementation Method 1
crystalline forms of psilocin salts or cocrystals with coformers such as acetic acid, benzenesulfonic acid, and butyric acid
Implementation Method 2
cocrystal of psilocin (4-hydroxy-N,N-dimethyltryptamine) and a coformer
Implementation Method 3
crystalline forms having improved physical properties such as aqueous solubility and stability
Data Source
AI summary
The present invention relates to crystalline forms of psilocin (4-hydroxy-N,N-dimethyltryptamine) salts or cocrystals, as well as compositions, methods of preparation and methods of their use. The present invention also relates to said crystalline forms having improved physical properties such as aqueous solubility and stability, wherein the crystalline forms and compositions thereof are suitable for oral, subcutaneous, intravenous, or intramuscular administration.