Pharmaceutical Composition Stabilization with Fumaric Acid
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Solution Overview
Problem
Current pharmaceutical compositions face challenges in stabilizing nonpeptidic pharmaceutically active ingredients, leading to decomposition issues that affect their efficacy and shelf life, especially under varying temperature and humidity conditions.
Innovation Solution
Incorporating fumaric acid as a stabilizing agent in a pharmaceutical composition containing nonpeptidic pharmaceutically active ingredients and excipients, which maintains the pH above 4.5, thereby preventing decomposition and enhancing stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If nonpeptidic pharmaceutically active ingredients are used in pharmaceutical compositions, then therapeutic efficacy is achieved, but decomposition occurs under varying temperature and humidity conditions
Solution Approach 1:
The patent introduces basic excipients (such as magnesium carbonate, calcium carbonate, or aluminum hydroxide) as intermediary substances that buffer the pH environment. These excipients act as mediators between the pharmaceutically active ingredient and the decomposing environment, maintaining pH within a stable range (above 4.5) to prevent decomposition while preserving therapeutic efficacy.
Solution Approach 2:
The patent applies parameter changes by controlling and maintaining the pH parameter above 4.5 through the use of basic excipients. This parameter control prevents the degradation reactions that occur at lower pH levels, thereby stabilizing the composition without affecting the active ingredient's therapeutic properties.
2Reliability
If basic excipients are added to stabilize the pharmaceutically active ingredient, then decomposition is prevented, but pH control becomes critical
Solution Approach 1:
The basic excipients used in the patent possess self-buffering capabilities that automatically maintain pH above 4.5 without requiring external pH adjustment mechanisms. The excipients self-regulate the pH environment through their inherent basic properties, eliminating the need for complex pH monitoring and adjustment systems.
3Stability of the object's composition
If pH is maintained above 4.5 to prevent decomposition, then stability is improved, but formulation options are constrained
Solution Approach 1:
The patent employs basic excipients that serve multiple functions simultaneously: they buffer pH above 4.5 to prevent decomposition, act as fillers or diluents, and provide structural support in the formulation. This multi-functionality maintains stability while preserving formulation flexibility, as the same excipients fulfill multiple roles without requiring additional components.
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 addition of fumaric acid significantly reduces the formation of decomposed products, resulting in a more stable pharmaceutical composition that retains its potency and quality regardless of storage conditions, ensuring superior preservation stability.
Implementation Method 1
Incorporating fumaric acid as a stabilizing agent in a pharmaceutical composition containing nonpeptidic pharmaceutically active ingredients and excipients, which maintains the pH above 4.5, thereby preventing decomposition and enhancing stability.
Data Source
AI summary
The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. According to the present invention, a pharmaceutical composition can be stabilized by containing a nonpeptidic pharmaceutically active ingredient having a primary or secondary amino group, an excipient and an acidic compound. In addition, a solid preparation containing a pharmaceutically active ingredient, titanium oxide, a plasticizer and a chain organic acid can enhance the stability of the pharmaceutically active ingredient during light irradiation.