Crystalline Salt Forms of Compound 1 for Solubility and Stability
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Solution Overview
Problem
There is a need for crystalline forms of psychedelics to improve physiochemical properties such as solubility, bioavailability, stability, and melting point for effective treatment of psychiatric disorders.
Innovation Solution
Development of pharmaceutically acceptable salt forms of Compound 1, including monofumarate, sesquifumarate, succinate, L-tartrate, and hydrochloride salts, characterized by specific X-ray powder diffraction patterns and thermal properties, to enhance the crystalline forms of psychedelics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If crystalline forms of psychedelics are developed, then solubility and bioavailability are improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies parameter changes by developing multiple salt forms (monofumarate, sesquifumarate, succinate, L-tartrate, hydrochloride) of Compound 1, each with distinct crystalline structures characterized by specific XRPD patterns. This allows optimization of solubility and bioavailability parameters while providing manufacturing flexibility through multiple viable crystal forms
Solution Approach 2:
The patent creates composite materials by forming salts between Compound 1 and various acids (fumaric acid, succinic acid, L-tartaric acid, hydrochloric acid). These composite salt forms exhibit improved physicochemical properties including enhanced solubility and stability while maintaining the core psychoactive compound structure
2Stability of the object's composition
If crystalline forms of psychedelics are developed, then stability is improved, but manufacturing precision requirements increase
Solution Approach 1:
The patent utilizes parameter changes by establishing specific XRPD peak patterns for each salt form (e.g., monofumarate Form 1 shows peaks at 12.8±0.2, 18.7±0.2, and 23.2±0.2° 2θ). These defined parameter ranges provide clear manufacturing specifications that balance stability requirements with achievable precision levels
Solution Approach 2:
The patent applies local quality by characterizing specific regions of the XRPD pattern for each polymorphic form. For example, Form 1 is identified by its distinctive peak pattern in the 12-24° 2θ range, allowing manufacturers to focus quality control efforts on these critical regions rather than requiring uniform precision across the entire spectrum
3Adaptability or versatility
If multiple salt forms are developed, then physiochemical properties are optimized, but product complexity increases
Solution Approach 1:
The patent systematically varies chemical parameters by creating five distinct salt forms with different counterions (fumarate, succinate, L-tartrate, hydrochloride). Each salt form offers tailored physicochemical properties, allowing selection based on specific formulation needs while maintaining a unified compound core
Solution Approach 2:
The patent segments the product portfolio into distinct polymorphic forms (Form 1 through Form 9 for monofumarate alone) and salt types. This segmentation allows each form to be optimized for specific applications while providing a structured framework that manages overall product complexity through clear classification
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 developed salt forms exhibit improved physiochemical properties, providing enhanced solubility, stability, and bioavailability, making them suitable for pharmaceutical applications in treating psychiatric disorders.
Implementation Method 1
the monofumarate salt of Compound 1 is characterized by an X-ray powder diffraction (XRPD) pattern having peaks at 12.8±0.2, 18.7±0.2, and 23.2±0.2 °2θ
Implementation Method 2
X-ray powder diffraction (XRPD) pattern having peaks at 12.8±0.2, 18.7±0.2, and 23.2±0.2 °2θ
Implementation Method 3
the monofumarate salt of Compound 1 is characterized by a Differential Scanning Calorimetry (DSC) thermogram comprising an endothermic event between 88±° C. to 142±5° C.
Implementation Method 4
the monofumarate salt of Compound 1 is characterized by about a 4.8% weight loss from 36±5° C. to 180±5° C. as determined by thermal gravimetric analysis (TGA)
Data Source
AI summary
The present disclosure provides salt forms of Compound 1,