Azole Antifungal Stabilization via Basic Substance Neutralization
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Azole-based antifungal agents modified to improve absorption are unstable when formulated and stored, particularly in acidic conditions, leading to reduced efficacy.
Innovation Solution
A pharmaceutical composition comprising an azole-based compound, unstable in acids, combined with a basic substance that stabilizes the compound, maintaining its antifungal activity and absorption when formulated into stable forms like tablets or granules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If the azole-based antifungal agent is modified to improve absorption, then absorption is improved, but stability during formulation and storage deteriorates
Solution Approach 1:
A basic substance is introduced as an intermediary component in the pharmaceutical composition. This basic substance interacts with the acid-unstable azole-based compound to form a stable complex or salt, thereby protecting the active ingredient from acid-induced degradation while maintaining its absorption-enhancing modifications intact
Solution Approach 2:
The pH parameter of the pharmaceutical composition is adjusted by incorporating a basic substance. This pH modification creates a basic or neutral environment that prevents acid-catalyzed decomposition of the azole-based compound, thereby improving stability without affecting the modified structure's absorption properties
2Stability of the object's composition
If the azole-based antifungal agent is formulated with acid stability in mind, then stability improves, but absorption deteriorates
Solution Approach 1:
The pharmaceutical composition is segmented into distinct functional components: the modified azole-based compound responsible for absorption enhancement and the basic substance responsible for stability. This segmentation allows each component to fulfill its specific function without compromising the other
3Ease of manufacture
If the pharmaceutical composition is stored in acidic conditions, then manufacturing simplicity improves, but compound stability deteriorates
Solution Approach 1:
The basic substance is incorporated into the formulation during manufacturing to preemptively neutralize acidic conditions. This preliminary action creates a stable basic environment throughout the formulation process and storage period, preventing acid-induced degradation before it can occur
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 composition remains stable during storage and exhibits excellent antifungal action, ensuring effective systemic administration and improved bioavailability.
Implementation Method 1
an azole-based compound that is unstable in an acid... combined with a basic substance that stabilizes the compound
Data Source
AI summary
It is an object of the present invention to provide a pharmaceutical composition containing a stable azole-based compound, which is useful as an antifungal agent. According to the present invention, the above-mentioned object can be achieved by adding magnesium hydroxide carbonate, triethylamine, arginine, or another such basic substance to an azole-based compound that is unstable in acids. The above-mentioned pharmaceutical composition is stable enough that the compound will not degrade if the temperature, humidity, or other such conditions should change during production or storage. Also, this composition is useful as a therapeutic agent for deep mycoses because systemic administration is possible by applying it to an oral agent or an injection.