Low Molecular Weight Leech Extract for Thrombosis Safety
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Solution Overview
Problem
Conventional extracts of leeches and earthworms for treating thrombotic diseases pose safety concerns due to immunogenicity and the risk of eliminating anticoagulant and antithrombotic active ingredients during purification, leading to reduced drug efficacy and potential allergic reactions.
Innovation Solution
An extract with a molecular weight of less than 5,800 daltons, comprising 15% to 38% amino acids, 40% to 60% saccharides, and 0.3% to 1% hypoxanthine, obtained through ultrafiltration and ion-exchange chromatography, which can be directly infused or injected without dermal tests, specifically designed for emergency treatment of thromboembolic cardiovascular and cerebrovascular diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional extracts of leeches and earthworms are used for treating thrombotic diseases, then anticoagulant and antithrombotic effects are achieved, but immunogenicity and allergic reactions occur due to high molecular weight polypeptides
Solution Approach 1:
The patent applies segmentation by dividing the conventional extract into different molecular weight fractions through ultrafiltration. The extract is separated into high molecular weight (HMW) and low molecular weight (LMW) fractions, with the LMW fraction (<5800 daltons) being the therapeutic agent. This segmentation removes immunogenic polypeptides while retaining anticoagulant activity.
Solution Approach 2:
The patent extracts and isolates the beneficial low molecular weight components from the conventional leech and earthworm extract while removing harmful high molecular weight polypeptides. The LMW fraction is obtained through ultrafiltration and ion-exchange chromatography, extracting only the therapeutic molecules that meet specific molecular weight criteria.
2Object-affected harmful factors
If purification processes are applied to remove harmful materials, then safety is improved, but anticoagulant and antithrombotic active ingredients may be eliminated reducing drug efficacy
Solution Approach 1:
The patent applies parameter changes by establishing specific molecular weight parameters as the basis for purification. Ultrafiltration membranes with specific pore sizes (5000-6000 daltons) are used to separate molecules based on their molecular weight. This parameter-based approach ensures that only molecules within the therapeutic range (<5800 daltons) are retained, preserving efficacy while removing harmful components.
Solution Approach 2:
The patent employs feedback mechanisms through quality control testing that measures both safety parameters (immunogenicity, microparticle content) and efficacy parameters (anticoagulant activity). The purification process is monitored and adjusted based on feedback from these tests to ensure the LMW fraction maintains therapeutic effectiveness while being safe for clinical use.
3Object-affected harmful factors
If dermal tests and extensive purification are performed, then safety is ensured, but treatment time is extended and patient suffering increases
Solution Approach 1:
The patent applies preliminary action by pre-purifying the extract during manufacturing to remove immunogenic components before clinical use. The LMW fraction is prepared in advance with controlled molecular weight specifications, eliminating the need for dermal testing and extensive purification during patient treatment. This preliminary preparation significantly reduces treatment time and patient suffering.
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 extract maintains or improves therapeutic effects while significantly enhancing safety by minimizing immune reactions and insoluble microparticles, allowing for effective prevention of blood coagulation and thrombosis without dermal testing, thus shortening treatment time and reducing patient suffering.
Implementation Method 1
filtration with ultrafiltration membrane or ultrafiltration column which can stay materials with molecular weight of no more than 6,000 daltons
Implementation Method 2
ion-exchange chromatography
Data Source
AI summary
An extract for preventing or treating thrombotic diseases, particularly, an extract of at least one of leeches and earthworms having a molecular weight of no more than 5,800 daltons is provided, wherein the extract includes 15% to 38% amino acid, 40% to 60% saccharide and 0.3% to 1% hypoxanthine. Processes for preparation, pharmaceutical compositions and uses thereof are also provided. Compared to conventional arts, the extract has safety greatly improved and drug actions maintained and even improved.