Crystalline Tryptamine Salts for Accurate Molecular Weight Dosing
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Solution Overview
Problem
There is a need to obtain and characterize crystalline forms of tryptamines and other psychedelic drug compounds to improve chemical and physical properties, ensuring accurate molecular weight determination for precise dosing and reducing errors in drug development.
Innovation Solution
The development of specific crystalline forms of tryptamine derivatives, characterized by unique X-ray powder diffraction patterns and space groups, such as 5-MeO-PiPT chloride, 4-methylcarbonato-DPT chloride, NiPT fumarate, and others, along with their pharmaceutical compositions and therapeutic uses.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If crystalline forms of tryptamine derivatives are developed, then chemical and physical properties are improved and molecular weight determination becomes accurate, but the complexity of drug development increases
Solution Approach 1:
The patent applies parameter changes by developing specific crystalline forms with defined space groups and unit cell dimensions. The crystalline forms have specific physical parameters (density, melting point, solubility) that differ from amorphous forms, enabling accurate molecular weight determination through standardized measurement protocols while maintaining drug development feasibility.
Solution Approach 2:
The patent utilizes phase transitions by characterizing tryptamine derivatives in their crystalline phase rather than amorphous phase. The crystalline forms exhibit distinct X-ray powder diffraction patterns and can be prepared through controlled crystallization processes, providing stable reference standards for accurate molecular weight determination without significantly complicating the overall drug development workflow.
2Manufacturing precision
If specific crystalline forms are characterized with unique X-ray powder diffraction patterns, then manufacturing precision improves, but the time and resources required for characterization increase
Solution Approach 1:
The patent applies preliminary action by pre-characterizing multiple crystalline forms (Forms 1-7) with their specific X-ray powder diffraction patterns, unit cell dimensions, and space groups before actual drug manufacturing. These pre-characterized forms serve as reference standards that can be quickly identified and used during manufacturing, reducing the time required for crystalline form verification while ensuring manufacturing precision.
Solution Approach 2:
The patent uses copying by creating standardized reference profiles for each crystalline form, including their characteristic X-ray powder diffraction patterns at specific temperatures. These reference copies enable rapid identification and verification of crystalline forms during manufacturing without requiring full re-characterization, thus improving manufacturing precision while minimizing characterization time and resources.
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
These crystalline forms provide improved chemical and physical properties, enabling accurate molecular weight determination and reducing errors in drug concentration calculations, thus enhancing the precision and efficacy of psychedelic drug compounds.
Implementation Method 1
crystalline form 1 of 5-MeO-PiPT chloride is characterized by: a monoclinic, P21 space group at a temperature of about 297(2) K; unit cell dimensions a=9.5054(9) Å, b=7.3960(7) Å, c=13.4481(12) Å, α=90°, β=109.924(3)°, and γ=90°; an X-ray powder diffraction (XRPD) pattern substantially similar to FIG. 25
Implementation Method 2
an X-ray powder diffraction pattern characterized by at least two peaks selected from 7.0, 10.0, and 21.1 °2θ±0.2 °2θ
Data Source
AI summary
This disclosure relates to 5-MeO-PiPT chloride, crystalline 5-MeO-PiPT chloride, 4-methylcarbonato-DPT chloride, crystalline 4-methylcarbonato-DPT chloride, NiPT fumarate, crystalline NiPT fumarate, NiPT chloride, crystalline NiPT chloride, MDPT iodide, crystalline MDPT iodide, 5-HT, crystalline 5-HT, 5-HT chloride butanol solvate, crystalline 5-HT chloride butanol solvate, N-cyclohexyltryptammonium fumarate, crystalline N-cyclohexyltryptammonium fumarate, 5-HO-TET iodide, crystalline 5-HO-TET iodide, TALT iodide, crystalline TALT iodide, 4-(4-chlorobenzoato)-DPT chloride, crystalline 4-(4-chlorobenzoato)-DPT chloride, and specific crystalline forms thereof, including crystalline form 1 of 5-MeO-PiPT chloride, crystalline form 1 of 4-methylcarbonato-DPT chloride, crystalline form 1 of NiPT fumarate, crystalline form 1 of NiPT chloride, crystalline form 1 of MDPT iodide, crystalline form 1 of 5-HT, crystalline form 1 of 5-HT chloride butanol solvate, crystalline form 1 of N-cyclohexyltryptammonium fumarate, crystalline form 1 of 5-HO-TET iodide, crystalline form 1 of TALT iodide, and crystalline form 1 of 4-(4-chlorobenzoato)-DPT chloride, to compositions containing the same, and to methods of treatment using them.