Ferric Maltol Polymorphs for Iron Deficiency
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Solution Overview
Problem
Current pharmaceutical formulations for iron deficiency and anemia lack effective polymorphs of ferric maltol, which are essential for improved bioavailability, stability, and solubility, particularly in pathological conditions such as inflammatory gastrointestinal diseases and post-operative blood loss.
Innovation Solution
Development of new polymorphs of ferric maltol, specifically Form I, Form II, Form III, and Form IV, characterized by distinct X-ray diffraction patterns and production processes involving ferric citrate and maltol anions, with the use of seed crystals and specific solvents, to enhance stability and solubility.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional iron formulations are used, then iron supplementation is provided, but bioavailability and solubility are insufficient particularly in pathological conditions
Solution Approach 1:
The patent applies parameter changes by discovering and utilizing different polymorphic forms (Forms I, II, III, IV) of ferric maltol, each with distinct crystal lattice arrangements that result in different thermodynamic properties, stabilities, and solubilities. This allows optimization of both bioavailability and solubility parameters simultaneously through selection of appropriate polymorphic form.
Solution Approach 2:
The patent utilizes phase transitions between different polymorphic forms of ferric maltol. By controlling crystallization conditions and using seed crystals of specific polymorphic forms, the patent enables transition between different solid phases, each offering improved bioavailability and solubility characteristics for treating iron deficiency in various pathological conditions.
2Reliability
If ferric maltol is used for iron supplementation, then treatment of iron deficiency is achieved, but stability and ease of preparation are compromised
Solution Approach 1:
The patent applies preliminary action by preparing and characterizing multiple stable polymorphic forms of ferric maltol in advance, with Forms I, II, III, and IV each offering different stability profiles. This preliminary identification and stabilization of specific polymorphic forms enables easier and more reliable manufacturing processes, as the stable crystal structures reduce degradation and improve handling during production.
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 new polymorphs provide improved bioavailability, stability, and solubility, making them effective for treating iron deficiency and anemia, with specific forms offering advantages in ease of preparation, pharmacokinetics, and chemical stability, suitable for various administration routes.
Implementation Method 1
combining ferric citrate with maltol anions to form a mixture comprising ferric maltol and wherein the process comprises the use of a ferric maltol seed crystal
Implementation Method 2
characterized by a powder X-ray diffraction pattern comprising characteristic crystalline peaks
Data Source
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AI summary
There is provided polymorphs of ferric maltol. Such forms may be useful in the treatment of iron deficiency with or without anaemia, such as iron deficiency anaemia.