Integrated Tangential Flow Filtration for PEGylated Coagulation Factor Production

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Solution Overview

Problem

Current methods for producing PEGylated coagulation factor conjugates require multiple unit operations, making them complex, difficult to scale, and inefficient, especially in commercial production due to the need for separate systems and manual handling, and challenges in implementing size exclusion chromatography at commercial scales.

Innovation Solution

An integrated tangential flow filtration system is used to integrate activation, removal of the activation agent, and conjugation steps, allowing for efficient and scalable production of PEGylated coagulation factors by utilizing reducing agents like dithiothreitol or tris 2-carboxyethyl phosphine, with subsequent separation via size exclusion or ion exchange chromatography.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If multiple separate unit operations are used for activation, removal of activating agent, and conjugation, then each step can be performed with dedicated equipment, but the overall process becomes complex and difficult to scale

Engineering Contradiction:
Improveprocess reliabilityVSAvoidsystem complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines three separate unit operations (activation, removal of activating agent, and conjugation) into a single integrated tangential flow filtration system. The system uses a single membrane module to perform all three functions sequentially, eliminating the need for multiple separate equipment units and manual transfers between systems.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The tangential flow filtration membrane system is designed to perform multiple functions: it acts as a barrier for activating agent removal, enables conjugation reaction, and facilitates product recovery. This multi-functional approach replaces multiple specialized equipment with a single versatile system.

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Manufacturing precision

If size exclusion chromatography is used for separation, then product purity can be achieved, but implementation at commercial scale becomes challenging

Engineering Contradiction:
Improveproduct purityVSAvoidscalability
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

The patent extracts the separation function from traditional size exclusion chromatography and implements it through tangential flow filtration. The membrane system physically separates the PEGylated product from unconjugated starting material based on size differences, achieving purification without requiring chromatography columns and complex elution protocols.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses hydraulic principles through tangential flow filtration, where pressurized buffer flows tangentially across the membrane surface. This hydrodynamic approach enables continuous processing and easy scale-up by simply increasing flow rates or membrane area, unlike batch chromatography methods.

Inventive Principle:
Principle #29Pneumatics and hydraulics

3Reliability

If manual handling and transfer between systems are required, then process control can be maintained, but productivity decreases and manual labor increases

Engineering Contradiction:
Improveprocess controlVSAvoidproduction efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

By integrating all process steps into a single system, the patent eliminates manual transfer operations between separate equipment. The continuous tangential flow filtration process maintains process control through automated parameter monitoring while significantly reducing manual intervention and increasing throughput.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent implements continuous processing where the biomolecule solution continuously flows through the membrane system, allowing activation, purification, and conjugation to occur without interruption. This continuous operation eliminates downtime associated with manual transfers and batch processing, thereby increasing productivity.

Inventive Principle:
Principle #20Continuity of useful action

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 method simplifies the process, making it reproducible and scalable, reducing manual handling and enabling efficient production of PEGylated coagulation factors with high PEGylation efficiency, suitable for commercial pharmaceutical production.

Implementation Method 1

activating the coagulation factor by contact with an activating agent; wherein the activating agent is a reducing agent

Methodology Applied
Scientific EffectReduction: Reduction

Implementation Method 2

the steps of the method are integrated into an integrated tangential flow filtration system

Methodology Applied
Scientific EffectSize exclusion: Chromatography

Implementation Method 3

conjugating the coagulation factor by reacting the coagulation factor with an activated polymer

Methodology Applied
Scientific EffectChemical bonding: Chemical Bonding

Data Source

PatentEP2536399B1Method for activation and conjugation of biomolecules
Publication Date: 2019.11.20 BAYER HEALTHCARE LLC
  • EP2536399B1 patent drawingFigure 1
  • EP2536399B1 patent drawingFigure 2
  • EP2536399B1 patent drawingFigure 3

AI summary

The present invention is directed to a method for producing a biomolecule conjugate where the method is integrated into a single unit operation.