Dephosphorylated Alkaloid Transmucosal Composition
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Solution Overview
Problem
Current methods for delivering psychoactive alkaloids, such as psilocybin and psilocin, face challenges including first-pass metabolism, gastric irritation, and difficulty in achieving desired bioactivity levels, especially in non-ingestive routes like parenteral administration, where dephosphorylation does not occur effectively.
Innovation Solution
A non-ingestive oral transmucosal composition comprising a dephosphorylated psychoactive alkaloid extract, a mucoadhesive polymer, and a carrier, with a process involving acidified solvent extraction and pH adjustment to ensure a higher proportion of dephosphorylated alkaloids, facilitating rapid absorption and bypassing gastrointestinal metabolism.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral administration of phosphorylated psychoactive alkaloids is used, then patient compliance is ensured and administration is convenient, but first-pass metabolism reduces bioavailability and gastric irritation occurs
Solution Approach 1:
The patent changes the chemical form of the psychoactive alkaloid from phosphorylated to dephosphorylated form, and switches the administration route from oral ingestion to oral transmucosal delivery. This parameter change allows the composition to bypass first-pass metabolism while maintaining ease of administration, thereby resolving the contradiction between administration convenience and bioavailability
Solution Approach 2:
The patent introduces a mucoadhesive polymer as an intermediary carrier that enables the dephosphorylated psychoactive alkaloid to adhere to and pass through the oral mucosa. This intermediary mechanism facilitates non-ingestive delivery, avoiding gastric irritation and first-pass metabolism while maintaining patient compliance
2Reliability
If parenteral administration is used to bypass first-pass metabolism, then bioavailability improves, but dephosphorylation does not occur effectively and psychoactive effects are reduced
Solution Approach 1:
The patent changes the administration route from parenteral to oral transmucosal, and changes the chemical form from phosphorylated to dephosphorylated alkaloid. This dual parameter change enables the composition to achieve both high bioavailability (by bypassing first-pass metabolism) and effective psychoactive effects (through direct delivery of dephosphorylated form to systemic circulation via mucosal absorption)
3Speed
If dephosphorylated psychoactive alkaloid extract is used in oral transmucosal composition, then rapid absorption and bypassing gastrointestinal metabolism are achieved, but manufacturing complexity increases
Solution Approach 1:
The patent applies preliminary action by performing dephosphorylation during the extraction process itself. The alkaloid extract is treated with alkaline conditions to convert phosphorylated alkaloids to dephosphorylated forms before final formulation. This preliminary conversion simplifies the overall manufacturing process while ensuring the final product contains the desired dephosphorylated form for rapid absorption
Solution Approach 2:
The patent uses parameter changes in the extraction process, specifically adjusting pH to alkaline conditions (pH 9-11) to promote dephosphorylation. This parameter adjustment during manufacturing enables the production of dephosphorylated alkaloid extract, which then provides rapid absorption and bypassing of gastrointestinal metabolism in the final application
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 composition achieves rapid delivery and higher bioavailability of psychoactive alkaloids, ensuring effective psychoactive effects with lower dosage requirements and minimizing gastric irritation, suitable for various patient groups including children and geriatrics.
Implementation Method 1
extracting a psychoactive alkaloid from a dried powdered psychoactive alkaloid source using an acidified solvent with a pH lower than 3.5
Implementation Method 2
Dephosphorylated forms of these psychoactive alkaloids are the bioactive forms that are converted through phosphatase action or chemical hydrolysis
Implementation Method 3
Delivery of APIs via these routes of administration allows bypassing the first pass metabolism. Furthermore, onset of action of the API is faster than oral ingestion
Data Source
AI summary
A transmucosal psychoactive alkaloid composition including a psychoactive alkaloid extract or synthetic psychoactive alkaloid. The alkaloids in the extract are predominantly dephosphorylated rather than phosphorylated. The transmucosal psychoactive alkaloid composition also includes a mucoadhesive polymer, a carrier, and optional further excipients. The non-ingestive composition may be taken orally through the mucosa. A process for obtaining an oral transmucosal psychoactive alkaloid composition includes dephosphorylating the alkaloid during extraction, purifying the extracted alkaloid and standardizing to a specific concentration by adding measured quantities of excipients.