Oleandrin Extraction via Subcritical Liquid and Organic Solvent Methods

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Solution Overview

Problem

Current methods for producing oleandrin, a compound with therapeutic properties, face challenges in achieving high yields and optimal compositional profiles, particularly in extracting oleandrin from Nerium oleander, with existing processes like supercritical fluid extraction yielding low oleandrin content and varying therapeutic activity profiles.

Innovation Solution

The implementation of subcritical liquid extraction (SbCLE) and organic solvent extraction methods to produce oleandrin-containing extracts, combining these to create a dual extract composition with enhanced oleandrin content and a broader range of phytochemicals, thereby improving yield and therapeutic efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If supercritical fluid extraction is used to produce oleandrin-containing extract, then extraction efficiency is improved, but oleandrin content and therapeutic activity are reduced

Engineering Contradiction:
Improveextraction efficiencyVSAvoidoleandrin content
Core Design Contradiction:
ProductivityVSQuantity of substance

Solution Approach 1:

The patent changes the extraction parameters by using subcritical liquid extraction conditions (lower temperature and pressure) instead of supercritical fluid extraction. This parameter change allows for higher oleandrin content (0.5-5% w/w) while maintaining extraction efficiency, resolving the contradiction between extraction efficiency and oleandrin content

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite extract containing multiple phytochemicals (oleandrin, oleanolic acid, ursolic acid, betulinic acid, kanerocin, kanerodione) with specific compositional ratios. This composite approach ensures both high extraction efficiency and optimal therapeutic activity profile with oleandrin as the predominant cardiac glycoside

Inventive Principle:
Principle #40Composite materials

2Ease of manufacture

If traditional extraction methods are used, then process simplicity is maintained, but oleandrin yield and compositional profile are suboptimal

Engineering Contradiction:
Improveprocess simplicityVSAvoidoleandrin yield
Core Design Contradiction:
Ease of manufactureVSProductivity

Solution Approach 1:

The patent modifies traditional extraction parameters by controlling temperature (30-50°C) and pressure (73-300 atm) to achieve subcritical liquid extraction conditions. This parameter optimization maintains relative process simplicity while dramatically improving oleandrin yield (0.5-5% w/w) and compositional quality

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses carbon dioxide as an intermediary solvent that can be easily controlled and removed. The CO2 acts as a mediator between the plant material and the extraction process, allowing for simple yet efficient extraction with optimal oleandrin recovery and clean product isolation

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If extraction conditions are optimized for high oleandrin content, then therapeutic efficacy is improved, but extraction complexity increases

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidextraction process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent optimizes extraction parameters (temperature 30-50°C, pressure 73-300 atm, extraction time 1-24 hours) to achieve high oleandrin content (0.5-5% w/w) and consistent therapeutic efficacy. These parameter changes provide reliable therapeutic results while using standard extraction equipment, avoiding excessive complexity

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

This approach results in higher oleandrin yields and a more favorable compositional profile compared to traditional methods, enhancing the therapeutic effectiveness of oleandrin-containing compositions for treating cardiac glycoside-responsive diseases and disorders.

Implementation Method 1

The invention provides a method of producing oleandrin or oleandrin-containing extract from oleandrin-containing biomass by a) subcritical liquid (SbCL) extraction (SbCLE) with carbon dioxide

Methodology Applied
Scientific EffectSubcritical liquid extraction: Supercritical Fluid

Implementation Method 2

b) extraction with organic solvent (OSE), optionally further comprising water

Methodology Applied
Scientific EffectOrganic solvent extraction: Solvation

Data Source

PatentUS12097234B2Extract containing oleandrin and method of production thereof
Publication Date: 2024.09.24 PHOENIX BIOTECHNOLOGY INC
  • US12097234B2 patent drawing
  • US12097234B2 patent drawing
  • US12097234B2 patent drawing

AI summary

A subcritical liquid extraction process for the production of oleandrin or oleandrin-containing extract is provided. The process provides improvements over other methods of preparing oleandrin-containing extract. The extract, pharmaceutical compositions, dosage forms and nutraceutical compositions comprising oleandrin or said extract are provided. Methods of treating diseases, disorders or conditions that are therapeutically responsive to oleandrin are also provided.