LCMF Poloxamer 188 Purification via Supercritical Fluid Extraction

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Solution Overview

Problem

Commercially available poloxamer preparations, such as poloxamer 188, contain heterogeneous populations of molecules that vary widely in size and configuration, making prediction of biological activity difficult and leading to unwanted biological activities due to the presence of low molecular weight and high molecular weight components with long circulating half-lives.

Innovation Solution

The development of long circulating material free (LCMF) poloxamer compositions using supercritical fluid extraction methods, involving the introduction of a poloxamer solution into an extractor vessel, admixing with an extraction solvent comprising alkanol and supercritical carbon dioxide, and gradually increasing the alkanol concentration, to produce poloxamers like LCMF poloxamer 188 that are free from low molecular weight and high molecular weight impurities.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If commercially available poloxamer preparations are used, then the therapeutic effect is achieved, but the heterogeneous molecular population causes unpredictable biological activity and unwanted side effects

Engineering Contradiction:
Improvepredictability of biological activityVSAvoidmolecular homogeneity
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies extraction by precipitation using a water-immiscible organic solvent to separate the desired poloxamer molecules from unwanted low molecular weight components and high molecular weight aggregates. The process selectively precipitates the target poloxamer while leaving impurities in the supernatant, which is then removed by centrifugation or filtration, yielding a homogeneous and predictable product

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent utilizes changes in solvent properties (adding water-immiscible organic solvent) to alter the solubility parameters of poloxamer components. By adjusting solvent composition and performing controlled precipitation, the method separates molecules based on their solubility characteristics, achieving molecular homogeneity and predictable biological activity

Inventive Principle:
Principle #35Parameter changes

2Reliability

If poloxamer solution is subjected to supercritical fluid extraction, then long circulating materials are removed, but the process complexity increases

Engineering Contradiction:
Improveclearance from circulationVSAvoidextraction process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent replaces complex mechanical separation systems with a simpler chemical precipitation approach. Instead of using sophisticated supercritical fluid extraction equipment, the method uses straightforward liquid-liquid precipitation with common organic solvents, followed by simple centrifugation or filtration, achieving comparable purification with reduced equipment complexity

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent changes the physical state and solubility parameters of poloxamer components by adding water-immiscible organic solvent, inducing selective precipitation. This parameter change enables removal of long circulating materials through simple phase separation and centrifugation, avoiding the need for complex supercritical fluid extraction apparatus

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If gradient extraction with increasing alkanol concentration is performed, then purification precision is improved, but the extraction time increases

Engineering Contradiction:
Improvepurification precisionVSAvoidextraction time
Core Design Contradiction:
Manufacturing precisionVSLoss of time

Solution Approach 1:

The patent performs preliminary concentration of the poloxamer solution before precipitation to optimize the precipitation efficiency. By pre-concentrating the solution, the subsequent precipitation step becomes more effective and faster, reducing overall processing time while maintaining high purification precision

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent optimizes precipitation parameters including solvent addition rate, final solvent concentration, temperature, and agitation speed to achieve rapid and complete precipitation. These parameter optimizations reduce the time required for purification while maintaining high precision in separating desired poloxamer from impurities

Inventive Principle:
Principle #35Parameter changes

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 LCMF poloxamer compositions exhibit a more uniform pharmacokinetic profile, reduced toxicity, and faster clearance from the circulation, eliminating the issue of long circulating materials, thereby enhancing therapeutic efficacy and safety.

Implementation Method 1

The development of long circulating material free (LCMF) poloxamer compositions using supercritical fluid extraction methods, involving the introduction of a poloxamer solution into an extractor vessel, admixing with an extraction solvent comprising alkanol and supercritical carbon dioxide

Methodology Applied
Scientific EffectSupercritical fluid extraction: Supercritical Fluid Extraction

Data Source

PatentEP3166617B1A poloxamer composition free of long circulating material and methods for production and uses thereof
Publication Date: 2024.01.10 LIFERAFT BIOSCIENCES INC
  • EP3166617B1 patent drawingFigure 1
  • EP3166617B1 patent drawingFigure 2
  • EP3166617B1 patent drawingFigure 3

AI summary

Provided herein are long circulating material free (LCMF) poloxamer compositions and uses thereof. In particular, provided are LCMF poloxamer 188 compositions and uses thereof. Also provided are supercritical fluid extraction (SFE) methods and high pressure (subcritical) methods for preparing poloxamer compositions, particularly the LCMF poloxamer compositions.