Stable Psilocin Salt Forms for Oxidation and Solubility Limits
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Psilocin exhibits poor physical properties, instability, and limited solubility, which hampers the development of effective pharmaceutical formulations, and its administration can cause adverse psychological and physical effects.
Innovation Solution
Development of psilocin salts, esters, and conjugates with improved stability and handling characteristics, such as psilocin mucic acid conjugate, which are administered in controlled doses to mitigate adverse effects and enhance therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If psilocin is used in its natural form, then it can activate 5-HT2A receptor and produce therapeutic effects, but it exhibits poor crystallinity, limited bulk purity, and is susceptible to auto-catalyzed oxidation
Solution Approach 1:
The patent changes the chemical form of psilocin from free base to salt forms (e.g., psilocin hydrochloride, psilocin sulfate) to improve stability and crystallinity. This parameter change in chemical formulation resolves the contradiction by providing both stability and enhanced physical properties.
Solution Approach 2:
The patent creates composite salt structures by combining psilocin with various acids (hydrochloric acid, sulfuric acid, etc.) to form stable salt compounds. These composite materials exhibit improved crystallinity and resistance to oxidation while maintaining therapeutic activity.
2Reliability
If psilocin is administered to treat psychiatric conditions, then therapeutic effects are achieved, but adverse psychological and physical effects occur
Solution Approach 1:
The patent modifies the administration parameters by using salt forms of psilocin instead of free base, which can provide more controlled and stable delivery. This parameter change in formulation can reduce adverse effects while maintaining therapeutic efficacy.
3Duration of action of moving object
If psilocin is stored and handled, then it maintains activity, but it undergoes auto-catalyzed oxidation and loses stability
Solution Approach 1:
The patent changes the chemical state of psilocin from free base to protonated salt forms, which significantly reduces susceptibility to oxidation. This parameter change in chemical formulation provides long-term storage stability and prevents degradation.
Solution Approach 2:
The patent creates a more stable chemical environment by forming salt compounds that are less reactive toward oxidation. The salt forms provide a more inert chemical state that resists degradation during storage and handling.
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 psilocin salts and conjugates demonstrate enhanced stability and a calming effect without hallucinogenic side effects, offering therapeutic benefits for conditions like depression and anxiety.
Implementation Method 1
psilocin salts, esters and conjugates with improved stability, physical properties and/or handling characteristics
Implementation Method 2
As a non-ionized form, psilocin is much more lipid soluble in comparison to psilocybin, and therefore is capable of crossing the blood brain barrier more effectively
Data Source
AI summary
Pharmaceutically acceptable salts, esters and conjugates of psilocin and compositions and methods for their production and use in treating diseases or conditions treatable with psilocin or psilocybin are provided.