Vancomycin Purification via Ion Exchange and Reverse Chromatography

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Solution Overview

Problem

Current methods for producing vancomycin hydrochloride with high purity (chromatographic purity of more than 99%) are not suitable for commercial production due to low recovery rates, residual solvent issues, and color appearance problems, making it difficult to meet safety and quality standards.

Innovation Solution

A method involving ion exchange chromatography followed by nanofiltration desalination and concentration, using a cation exchange Sephadex or Sepharose column with a mobile phase of NH4HCO3, and subsequent reverse chromatography with a polystyrene polymer stationary phase and an aqueous ethanol mobile phase, to achieve a chromatographic purity of up to 99% and a pure white appearance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If ion exchange chromatography is used to purify vancomycin hydrochloride, then purity is improved, but recovery rate deteriorates

Engineering Contradiction:
ImprovepurityVSAvoidrecovery rate
Core Design Contradiction:
Manufacturing precisionVSProductivity

Solution Approach 1:

The patent optimizes multiple parameters including mobile phase composition (ammonium bicarbonate concentration, pH values), flow rates, and temperature conditions throughout the chromatographic process to achieve both high purity and high recovery rate simultaneously

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs dynamic gradient elution where the mobile phase composition changes continuously during the chromatographic run, starting with lower ammonium bicarbonate concentration and gradually increasing it to optimize separation while maximizing product recovery

Inventive Principle:
Principle #15Dynamics

2Manufacturing precision

If reverse phase chromatography with silica gel is used, then purity is improved, but residual solvent removal becomes difficult

Engineering Contradiction:
ImprovepurityVSAvoidsolvent recovery
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

The patent replaces traditional silica gel with polymer-based fillers (polystyrene crosslinked with divinylbenzene or polyacrylamide crosslinked with N,N'-methylenebisacrylamide) that are easier to handle, require less stringent drying, and allow for simpler solvent removal while maintaining high purification efficiency

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

Solution Approach 2:

The patent modifies the stationary phase material from inorganic silica gel to organic polymers with different surface properties, changing the interaction mechanism and enabling easier solvent removal from the purified product

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If multiple purification steps are used to achieve high purity, then purity is improved, but process complexity increases

Engineering Contradiction:
ImprovepurityVSAvoidprocess complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent combines ion exchange chromatography and reverse phase chromatography into a single integrated process using a filler that exhibits both ion exchange and hydrophobic interaction properties, eliminating the need for separate purification steps while achieving chromatographic purity greater than 99%

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent develops a universal filler material with dual functionality (ion exchange and hydrophobic interaction) that can handle multiple purification objectives in one step, making the process suitable for both research and commercial production

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

4Manufacturing precision

If ion exchange chromatography is used, then purity is improved, but pigment removal becomes insufficient

Engineering Contradiction:
ImprovepurityVSAvoidcolor appearance
Core Design Contradiction:
Manufacturing precisionVSObject-generated harmful factors

Solution Approach 1:

The patent uses composite filler materials combining polymer matrices with crosslinked structures that provide both ion exchange capacity and hydrophobic interaction sites, enabling effective removal of pigment impurities while maintaining high vancomycin recovery

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent optimizes the local chemical environment within the filler pores through controlled crosslinking density and functional group distribution, creating specific micro-environments that selectively adsorb pigment molecules while allowing vancomycin to pass through

Inventive Principle:
Principle #3Local quality

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 method achieves high purity vancomycin hydrochloride with improved color appearance and efficient solvent recovery, making it suitable for commercial production while ensuring product safety and quality.

Implementation Method 1

ion exchange chromatography and obtaining a first vancomycin hydrochloride concentrate by nanofiltration desalination and concentration, wherein a filler of the ion exchange chromatography column is a cation exchange Sephadex or Sepharose

Methodology Applied
Scientific EffectIon exchange: Ion Exchange

Implementation Method 2

obtaining a first vancomycin hydrochloride concentrate by nanofiltration desalination and concentration

Methodology Applied
Scientific EffectNanofiltration: Semipermeable Membrane

Implementation Method 3

performing a column chromatography using a reverse chromatography column for the first vancomycin hydrochloride concentrate adjusted, wherein a stationary phase is a polystyrene polymer

Methodology Applied
Scientific EffectChromatography: Chromatography

Data Source

PatentEP3064214B1Separation and purification method for vancomycin hydrochloride of high purity
Publication Date: 2019.08.07 ZHE JIANG MEDICINE CO LTD XINCHANG PHARMA FAB
  • EP3064214B1 patent drawingFigure 1~2
  • EP3064214B1 patent drawingFigure 3~4
  • EP3064214B1 patent drawingFigure 5~6

AI summary

Provided is a separation and purification method for vancomycin hydrochloride of high purity. The method comprises the following steps: (1) obtaining a vancomycin hydrochloride solution from a crude vancomycin product by ion exchange chromatography and obtaining a concentrate by nanofiltration desalination and concentration; (2) adjusting the concentrate with a hydrochloric acid solution and then performing a column chromatography using a reverse chromatography column for the adjusted concentrate; (3) collecting the chromatographic solution of vancomycin to obtain a mixed chromatographic solution; (4) adjusting the mixed chromatographic solution, and separating the solution and the salts by nanofiltration desalination and concentration to obtain a concentrate; and (5) obtaining a vancomycin dry powder with a chromatographic purity of up to 99% and a pure white appearance by dehydrating and drying the concentrate of step (4), or by solvent crystallization or salting-out crystallization.