5-MeO-DMT Hydrobromide Salt Non-Hygroscopic Formulation

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Solution Overview

Problem

5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) is challenging to handle and formulate into effective pharmaceutically useful compositions due to its hygroscopic nature, leading to issues with bioavailability, stability, and manufacturing processes.

Innovation Solution

Development of non-hygroscopic salts such as 5-MeO-DMT hydrobromide, which maintains high solubility and stability, reducing the need for costly moisture control measures and enhancing bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If 5-MeO-DMT is used in its free base form, then it exhibits psychoactive activity, but it is hygroscopic and difficult to handle and formulate

Engineering Contradiction:

ImproveEase of handling and formulationVSAvoidStability and bioavailability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent applies parameter changes by converting 5-MeO-DMT from its free base form to various salt forms (hydrobromide, phosphate, fumarate, oxalate, tartrate, benzenesulfonate, tosylate, glycolate, ketoglutarate, malate, saccharinate). This chemical parameter change transforms the hygroscopic free base into stable, non-hygroscopic salts that are easier to handle and formulate while maintaining psychoactive activity. The salt formation process modifies the physical and chemical properties without altering the core psychoactive mechanism.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If moisture control measures are implemented for hygroscopic 5-MeO-DMT, then stability is maintained, but manufacturing costs increase

Engineering Contradiction:

ImproveStabilityVSAvoidManufacturing cost

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent converts the harmful hygroscopic property of 5-MeO-DMT into a beneficial characteristic by forming salt derivatives. The hygroscopic nature is transformed through chemical modification into stable, non-hygroscopic salt forms. This approach eliminates the need for costly moisture control measures during manufacturing while maintaining or enhancing stability. The salt formation process inherently solves the moisture sensitivity problem rather than requiring additional protective measures.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If 5-MeO-DMT is formulated for pharmaceutical use, then therapeutic effect is achieved, but formulation challenges arise due to hygroscopicity

Engineering Contradiction:

ImproveTherapeutic efficacyVSAvoidFormulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent simplifies formulation complexity by changing the chemical parameter of 5-MeO-DMT from free base to salt forms. The salt derivatives exhibit improved solubility, stability, and flow characteristics, making them more suitable for various pharmaceutical dosage forms. This parameter change eliminates the need for complex formulation strategies to manage hygroscopicity, allowing for straightforward formulation development while ensuring therapeutic efficacy.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS11773063B1Pharmaceutically acceptable salts and compositions thereof

Publication Date: 2023.10.03 BECKLEY PSYTECH LIMITED

AI summary

Pharmaceutically acceptable salts of 5-methoxy-N,N-dimethyltryptamine are described, as well as compositions/formulations and uses thereof as a medicament.