Bempedoic Acid Sodium Salt Crystals for Non-Sticky Powder Flow
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Solution Overview
Problem
Existing forms of Bempedoic acid, including its base form and previously disclosed solid form, exhibit issues such as stickiness and poor flow properties, which hinder their use in pharmaceutical formulations, and there is a lack of information on suitable salts that could improve solubility and bioavailability.
Innovation Solution
Development of crystalline forms of sodium salt of Bempedoic acid, characterized by specific XRPD patterns, which are prepared through controlled processes involving dissolution in alcohol, addition of sodium bases, and manipulation of temperature and humidity to achieve non-sticky and highly crystalline forms.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Bempedoic acid is prepared as a solid form, then it can be used in pharmaceutical formulations, but it exhibits stickiness and poor flow properties
Solution Approach 1:
The patent changes the chemical form of Bempedoic acid from the free acid to the sodium salt form. This parameter change fundamentally alters the physical properties, transforming the sticky solid with poor flow properties into a free-flowing crystalline solid with excellent handling characteristics suitable for pharmaceutical formulations.
Solution Approach 2:
The patent creates a composite material by forming a salt between Bempedoic acid and sodium hydroxide. This composite sodium salt form combines the therapeutic activity of Bempedoic acid with the beneficial handling properties of the sodium salt, achieving both pharmaceutical suitability and good flow properties.
2Reliability
If Bempedoic acid is prepared as a solid form, then it can be used in pharmaceutical formulations, but it exhibits stickiness
Solution Approach 1:
The patent changes the chemical form of Bempedoic acid from the free acid to the sodium salt form. This parameter change fundamentally alters the physical properties, transforming the sticky solid with poor flow properties into a free-flowing crystalline solid with excellent handling characteristics suitable for pharmaceutical formulations.
3Quantity of substance
If salts of Bempedoic acid are developed, then solubility and bioavailability are improved, but information on suitable salts is lacking
Solution Approach 1:
The patent systematically evaluates different base materials to form salts with Bempedoic acid, allowing the compound itself to guide the selection of suitable counterions. The sodium salt emerged as the optimal form through this self-directed exploration, demonstrating improved solubility and bioavailability while providing valuable information for future formulation work.
4Reliability
If crystalline forms of sodium salt are developed, then crystallinity and solubility are improved, but specific crystalline forms with good flow properties were not previously available
Solution Approach 1:
The patent utilizes phase transition techniques during the salt formation process to generate distinct crystalline forms of the sodium salt. By controlling the crystallization conditions, the patent achieves a specific crystalline phase that exhibits both high crystallinity for stability and good flow properties for manufacturability.
Solution Approach 2:
The patent changes the chemical form of Bempedoic acid from the free acid to the sodium salt form. This parameter change fundamentally alters the physical properties, transforming the sticky solid with poor flow properties into a free-flowing crystalline solid with excellent handling characteristics suitable for pharmaceutical formulations.
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 crystalline forms of sodium salt of Bempedoic acid demonstrate improved solubility, crystallinity, and stability, enabling effective purification and formulation into pharmaceutical preparations with enhanced properties.
Implementation Method 1
dissolution in alcohol, addition of sodium bases
Implementation Method 2
crystalline forms of sodium salt of Bempedoic acid, manipulation of temperature and humidity to achieve non-sticky and highly crystalline forms
Data Source
AI summary
The presented invention relates to crystalline Forms (I) or (II) or (III) or (IV) of sodium salt of Bempedoic acid, processes for preparation thereof and a composition comprising it.