Amorphous Folate Salt Composition for Dual-Solvent Solubility

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Solution Overview

Problem

Existing folate salts exhibit limited solubility in both aqueous and apolar solvents, hindering the development of versatile pharmaceutical compositions for conditions positively influenced by folate administration.

Innovation Solution

Development of amorphous folate salts comprising tetrahydrofolic acid anions and organic cations such as arginine, choline, and their oxidized derivatives, which demonstrate high solubility in both water and apolar solvents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If conventional folate salts are used, then they provide basic folate delivery, but they exhibit limited solubility in both aqueous and apolar solvents

Engineering Contradiction:

Improvesolubility in both aqueous and apolar solventsVSAvoidstability of folate salts

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent creates composite folate salts by combining tetrahydrofolic acid with specific organic cations (arginine, choline, or their derivatives) to produce a material that exhibits properties of both water solubility and apolar solvent solubility, resolving the contradiction between adaptability to different solvent systems and stability

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent changes the chemical parameters of the folate salt by selecting specific organic cations with particular structural characteristics (basic amino groups) that enable the compound to achieve high solubility in both polar and non-polar environments while maintaining stability

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If folate salts with improved water solubility are developed, then they enhance bioavailability, but they show very limited solubility in apolar solvents

Engineering Contradiction:

Improvesolubility in apolar solventsVSAvoidversatility in pharmaceutical compositions

Core Design Contradiction:

Adaptability or versatilityVSEase of manufacture

Solution Approach 1:

The patent develops folate salts that serve multiple functions simultaneously - they are soluble in both aqueous and apolar solvents, can be used in diverse pharmaceutical compositions, and maintain stability, making them universally applicable across different formulation requirements

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS12622913B2Folate salts for medical use

Publication Date: 2026.05.12 APROFOL

AI summary

The invention relates to amorphous folate salt. The salt consists of a folate anion and an organic cation. The folate anion is selected from the group consisting of 5-formyl-(6S)-tetrahydrofolic acid, 10-formyl-(6R)-tetrahydrofolic acid, 5-methyl-(6S)-tetrahydrofolic acid, (6S)-tetrahydrofolic acid, 5,10-Methylene-(6R)-tetrahydrofolic acid, and its oxidized derivatives JK12A and Mefox, and the cation is an organic compound selected from the group arginine, choline, acetylcholine, 1,1-dimethyl-biguanidin phenylethylbiguanidin, betaine-methylester and dimethylaminoethanol. The cation is an organic compound with a complementary pharmacological activity.