Asarinin Extraction via SFE-CO2 for High-Purity Antitussive Formulations

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Solution Overview

Problem

Current methods for extracting asarinin from Asarum, a traditional Chinese medicine, are complex, involve heating and toxic organic reagents, leading to unstable components and residue issues, making it unsuitable for industrial mass production and lacking a method for direct extraction from volatile oil using SFE-CO2.

Innovation Solution

A method involving optimizing SFE-CO2 conditions to extract high-purity asarinin from Asarum volatile oil by standing the oil at low temperature, performing suction extraction at reduced pressure, and recrystallizing with absolute ethyl alcohol to obtain white acicular crystals with purity greater than 98%, avoiding oxidation and pyrolysis, and eliminating organic solvent residues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If traditional extraction methods (ethanol-thermal extraction, steam distillation, extraction with diethyl ether) are used to obtain asarinin, then asarinin can be extracted from Asarum, but the process becomes complex and requires heating treatment and toxic organic reagents, causing unstable components and residue issues

Engineering Contradiction:
Improvepurity of asarininVSAvoidcomplexity of extraction process
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent extracts asarinin directly from Asarum volatile oil using SFE-CO2 method, separating the target compound from the volatile oil matrix through selective extraction with supercritical carbon dioxide, followed by precipitation to obtain pure asarinin crystals

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the extraction parameters by using supercritical fluid conditions (high pressure and temperature) with CO2, which allows extraction without toxic organic solvents and heating that degrades components, achieving both simplicity and high purity

Inventive Principle:
Principle #35Parameter changes

2Manufacturing precision

If traditional extraction methods are used to obtain asarinin, then asarinin can be extracted from Asarum, but toxic organic reagents (Pb(OAC)2, H2S, ET2O) need to be added, causing residue problems

Engineering Contradiction:
Improvepurity of asarininVSAvoidresidue of organic reagents
Core Design Contradiction:
Manufacturing precisionVSObject-generated harmful factors

Solution Approach 1:

The patent uses supercritical carbon dioxide as the extraction medium, which is non-toxic, non-flammable, and leaves no harmful residues. CO2 is an inert gas that can be easily removed after extraction, eliminating the need for toxic organic reagents and their associated residue problems

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

Solution Approach 2:

The patent employs carbon dioxide, a cheap and environmentally benign substance, as the extraction solvent. CO2 is used in supercritical state for extraction then returns to gaseous state, leaving no persistent residues in the final product

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

3Productivity

If heating treatment is applied in the extraction process, then extraction efficiency can be improved, but unstable components of traditional Chinese medicine are easily degraded

Engineering Contradiction:
Improveextraction efficiencyVSAvoidstability of Asarum components
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent uses supercritical fluid extraction conditions with controlled temperature and pressure parameters. By maintaining temperature below degradation points while achieving supercritical state through pressure, the method achieves high extraction efficiency without degrading unstable components of Asarum

Inventive Principle:
Principle #35Parameter changes

4Manufacturing precision

If the existing extraction method is used, then asarinin can be obtained, but it is not suitable for industrial mass production due to process complexity

Engineering Contradiction:
Improvepurity of asarininVSAvoidsuitability for industrial mass production
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

The patent extracts asarinin directly from Asarum volatile oil using SFE-CO2 method, simplifying the process by eliminating multiple extraction and purification steps required by traditional methods, making it suitable for industrial scale-up

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent replaces complex chemical extraction procedures with supercritical fluid extraction, a physical process that is easier to control and scale. The SFE-CO2 method eliminates the need for multiple chemical treatments and recrystallization steps, streamlining the manufacturing process

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

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 a simple, effective process for producing high-purity asarinin with proven antitussive function, suitable for treating coughs, expanding the selection of antitussive medicines and ensuring product quality through quantifiable analysis.

Implementation Method 1

obtaining asarum volatile oil by optimizing SFE-CO2 conditions

Methodology Applied
Scientific EffectSupercritical fluid extraction: Supercritical Fluid Extraction

Implementation Method 2

standing the asarum volatile oil at a low temperature, carrying out suction extraction at reduced pressure and recrystallization with absolute ethyl alcohol

Methodology Applied
Scientific EffectCrystallization: Crystallisation

Implementation Method 3

carrying out suction extraction at reduced pressure

Methodology Applied
Scientific EffectVacuum evaporation: Vacuum Distillation

Implementation Method 4

recrystallization with absolute ethyl alcohol to obtain white acicular crystals

Methodology Applied
Scientific EffectRecrystallization: Crystallisation

Data Source

PatentUS10501470B2Use of asarinin in preparation of medicines for treating various coughs
Publication Date: 2019.12.10 THE FIRST AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV (GUANGZHOU RESPIRATORY CENT)
  • US10501470B2 patent drawing
  • US10501470B2 patent drawing
  • US10501470B2 patent drawing

AI summary

The invention discloses a use of asarinin in preparation of medicines for treating various coughs. The asarinin is used for preparing medicines for treating various coughs separately or in combination with other medicines. The asarinin can be extracted by an SFE-CO2 method. The asarinin and usable drug carriers or excipients are made into various formulations. And the formulations are granules, tablets, capsules, soft capsules, pills, dripping pills, ointments, syrups, injection, oral liquid, tinctures, sustained-releasing drugs, controlled release drugs or targeting preparations.