Artemether Injection Stability via Low-Temperature Micronization
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Solution Overview
Problem
Current treatments for leukemia lack effective and non-toxic options with minimal side effects, as existing therapies often result in drug tolerance and significant harm to normal cells.
Innovation Solution
Artemether, combined with a water-soluble cyclodextrin derivative in a specific weight ratio, is formulated into an injection or lyophilized powder for injection, using micronization technology at low temperatures to maintain stability and enhance dissolution, thereby inhibiting leukemia cell growth with minimal toxicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If conventional pulverization technique is used to prepare artemether, then the drug can be processed, but local excessive temperatures cause degradation of artemether
Solution Approach 1:
The patent changes the temperature parameter from conventional room temperature pulverization to low temperature (0°C-10°C) pulverization. This parameter change prevents local excessive temperatures that would degrade artemether, while still allowing the drug to be processed into fine particles for injection formulation.
Solution Approach 2:
The patent introduces water-soluble cyclodextrin derivatives as intermediary substances that form inclusion complexes with artemether. This mediator protects artemether from degradation during processing and enhances its water solubility, enabling injection formulation without direct exposure to degrading conditions.
2Reliability
If existing leukemia therapies are used, then treatment can be provided, but drug tolerance develops and significant harm is caused to normal cells
Solution Approach 1:
The patent applies the local quality principle by using cyclodextrin derivatives to create a localized delivery system. The inclusion complex provides targeted protection and release of artemether, concentrating the therapeutic effect on leukemia cells while minimizing exposure and damage to normal cells, thereby reducing overall toxicity.
Solution Approach 2:
The patent creates a composite material system consisting of artemether encapsulated within water-soluble cyclodextrin derivatives. This composite structure combines the antitumor properties of artemether with the protective and solubilizing characteristics of cyclodextrins, enabling effective leukemia treatment with reduced side effects and drug tolerance.
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
Artemether demonstrates significant inhibition of leukemia cell growth in nude mice models, achieving inhibition ratios of 60-80% with minimal toxicity, comparable to cyclophosphamide, indicating its potential as a new anti-tumor drug.
Implementation Method 1
artemether is added into an aqueous solution of a water-soluble cyclodextrin derivative at 50℃-90℃, stirred to dissolve artemether
Implementation Method 2
artemether is pulverized in a low-temperature pulverizer at 0℃-10℃
Implementation Method 3
treated or lyophilized according to a conventional process of an injection to obtain a finished product
Data Source
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AI summary
Disclosed is a use of artemether in the preparation of a drug for treating leukemia. The drug is an artemether injection or lyophilized powder for injection, and is prepared with the artemether and a water soluble cyclodextrin derivative in a weight ratio of 1:30-70.