Buffered Psilocybin Formulations for Fast Stable Subcutaneous Delivery
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Solution Overview
Problem
There is a need for new pharmaceutical compositions that provide rapid onset of therapeutic activity and meet regulatory criteria for approved drug products to treat psychiatric disorders, particularly those involving psilocybin derivatives.
Innovation Solution
Pharmaceutical formulations comprising psilocybin derivatives in the form of pH buffered aqueous solutions with pharmaceutically acceptable excipients, including pH modifiers and tonicity agents, are developed for parenteral administration, specifically subcutaneous delivery, to enhance stability and efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If psilocybin derivatives are formulated in conventional pharmaceutical compositions, then therapeutic activity can be achieved, but rapid onset of action and extended shelf-life are not simultaneously obtained
Solution Approach 1:
The patent applies parameter changes by formulating psilocybin derivatives in pH buffered aqueous solutions with specific pH ranges (5.5-6.5 for phosphate buffer, 6.0-7.5 for histidine buffer) and controlled concentrations (2-40 mg/mL). These parameter adjustments optimize both the rapid onset of therapeutic activity and the stability/shelf-life of the formulation, resolving the contradiction between speed of action and compositional stability.
2Speed
If psilocybin derivatives are administered via conventional routes, then therapeutic effect is achieved, but rapid onset and reduced injection site reactions are not accomplished
Solution Approach 1:
The patent uses pH buffered aqueous solutions as an intermediary medium to deliver psilocybin derivatives via subcutaneous injection. The buffered solution acts as a mediator that enables rapid onset of therapeutic activity while minimizing injection site reactions by controlling the chemical environment (pH 5.5-7.5) and formulation characteristics, thus resolving the contradiction between rapid onset and reduced harm.
3Quantity of substance
If high concentration of psilocybin derivative is used, then therapeutic efficacy is improved, but stability and shelf-life are compromised
Solution Approach 1:
The patent resolves the contradiction between high concentration and stability by implementing specific parameter changes: using pH buffered aqueous solutions with controlled pH (5.5-7.5), optimizing concentration ranges (2-40 mg/mL), and incorporating stabilizing excipients. These parameter adjustments allow high therapeutic concentrations while maintaining formulation stability and extended shelf-life.
Data Source
AI summary
The present disclosure provides stable liquid formulations comprising Compound 1, or a pharmaceutically acceptable salt of Compound 1, and one or more pharmaceutically acceptable excipients. The liquid formulation may comprise a pH buffered aqueous solution, and optionally a pH modifier and/or a tonicity agent. Also provided herein are methods of delivering the formulation via parenteral administration (e.g., subcutaneous injection), and methods of using the formulation in the treatment of neuropsychiatric diseases (e.g., treatment resistant depression).