SEC Molecular Weight Distribution Analysis for Glatiramoids

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Solution Overview

Problem

Current methods for determining the molecular weight distribution (MWD) of glatiramoids like glatiramer acetate are either relative and unreliable due to the use of inappropriate standards or impractical due to the sensitivity of multi-angle light scattering detectors, making it challenging to achieve accurate and reproducible results for pharmaceutical quality control.

Innovation Solution

A method using conventional size exclusion chromatography (SEC) calibrated with broad molecular weight standards that are similar in structure and properties to the glatiramer acetate, employing a combination of multi-angle light scattering and refractive index or ultraviolet detectors to determine absolute molecular weight distribution, allowing for accurate calibration and analysis of MWD.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If multi-angle light scattering detectors are used to determine absolute molecular weight distribution, then measurement accuracy is improved, but device complexity and sensitivity to aggregation increase

Engineering Contradiction:
Improvemolecular weight distribution accuracyVSAvoiddetector system complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent uses SEC (size exclusion chromatography) as an intermediary technique to separate polypeptide species by size before detection. This preprocessing step reduces the complexity of direct absolute MWD measurement by providing fractionated samples that can be analyzed with simpler detectors, while still achieving accurate molecular weight distribution data through the combination of SEC separation with light scattering or refractive index detection.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs calibration curves generated from standards with known molecular weights to create a reference model. This copying approach allows the system to determine unknown MWD by comparing against the calibrated response, reducing the need for complex absolute measurements while maintaining measurement accuracy through the established calibration relationship.

Inventive Principle:
Principle #26Copying

2Ease of operation

If conventional SEC with inappropriate standards is used, then ease of operation is improved, but measurement reliability deteriorates

Engineering Contradiction:
Improvemethod simplicityVSAvoidmolecular weight distribution reliability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent changes the critical parameter of standard selection from inappropriate monodisperse standards to appropriate broad MWD standards that match the polypeptide sample characteristics. This parameter change transforms the SEC calibration to accurately reflect the hydrodynamic volume-molecular weight relationship for complex polypeptide mixtures, thereby improving measurement reliability while maintaining the simplicity of conventional SEC operation.

Inventive Principle:
Principle #35Parameter changes

3Measurement precision

If broad MWD standards similar to glatiramer acetate are used for calibration, then measurement precision is improved, but standard preparation complexity increases

Engineering Contradiction:
ImproveMWD determination accuracyVSAvoidstandard preparation complexity
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent uses commercially available broad MWD standards (such as dextran or other polysaccharides) that are readily accessible and do not require complex preparation. These standards, while not identical to glatiramer acetate, provide sufficient calibration accuracy when used with appropriate SEC conditions, avoiding the need for laborious preparation of custom polypeptide standards while maintaining measurement precision.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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

This approach provides a robust and practical method for determining the absolute molecular weight distribution of glatiramer acetate, enhancing the reliability and reproducibility of the analysis, which is crucial for pharmaceutical quality control and batch release.

Implementation Method 1

Size exclusion chromatography (SEC) is a chromatographic technique that separates molecules in solution by their molecular size, or more precisely, by their hydrodynamic volume. The SEC stationary phase is a porous material with a characteristic pore size distribution, and depending on molecular size, a larger or lesser fraction of the pores is accessible to the macromolecules.

Methodology Applied
Scientific EffectSize exclusion chromatography: Chromatography

Implementation Method 2

The SEC stationary phase is a porous material with a characteristic pore size distribution

Methodology Applied
Scientific EffectPorosity: Porosity

Implementation Method 3

a molecular weight sensitive detector, e.g. a Right-Angle Light Scattering (RALS), a Low-Angle Light Scattering (LALS), RALS/LALS hybrids or a Multi-Angle Light Scattering (MALS)

Methodology Applied
Scientific EffectLight scattering: Scattering

Implementation Method 4

either based on refractive index (RI)

Methodology Applied
Scientific EffectRefractive index detection: Refraction

Implementation Method 5

or ultraviolet absorption (UV)

Methodology Applied
Scientific EffectUltraviolet absorption: Absorption (EM radiation)

Data Source

PatentEP3147667B1Analysis of the molecular weight distribution of complex polypeptide mixtures
Publication Date: 2019.06.12 CHEMI SPA
  • EP3147667B1 patent drawingFigure 1
  • EP3147667B1 patent drawingFigure 2
  • EP3147667B1 patent drawingFigure 3

AI summary

The present invention relates to simple size exclusion chromatography (SEC) analytical methods useful for the assessment of accurate molecular weight distributions (MWDs) of certain polypeptide mixtures known as glatiramoids. The use of a SEC method based on one or more broad MWD standards furnishes the absolute (not relative) molecular weight distribution profile of complex polypeptide mixtures like, for instance, the glatiramer acetate (GA) polymer.