Pharmaceutical Liquid Composition Stabilized by Water-Soluble Additives
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Solution Overview
Problem
Existing liquid compositions containing N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or its salts suffer from insufficient stability, particularly when prepared with water, which affects their efficacy as anti-inflammatory and anti-pancreatitis agents.
Innovation Solution
Incorporating a water-soluble additive, such as a surfactant, cyclodextrin, or antioxidant, into the liquid composition enhances the stability of N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or its salts, maintaining a residual rate of 90% or more after storage at 40°C for 2 weeks and minimizing decomposition products.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a liquid composition containing water is prepared using commonly used methods, then the composition can be easily manufactured, but the stability of N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or a salt thereof is insufficient
Solution Approach 1:
A water-soluble additive is introduced as an intermediary substance to mediate between the active ingredient and water, improving the stability of N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide in the liquid composition without complicating the manufacturing process
Solution Approach 2:
The composition parameters are optimized by controlling the pH value within 3-9 and the concentration of the water-soluble additive at 0.01-10% by mass, which improves the stability of the active ingredient while maintaining ease of manufacture through straightforward parameter specification
2Duration of action of moving object
If the liquid composition is stored at high temperature (40°C), then the therapeutic effect can be maintained, but the compound decomposes and the residual rate decreases
Solution Approach 1:
A water-soluble additive is incorporated into the composition in advance to cushion against thermal decomposition, enabling the compound to maintain stability even when stored at elevated temperatures of 40°C, thus preserving both duration of action and compositional stability
3Reliability
If no water-soluble additive is added, then the composition is simpler, but the compound decomposes and precipitation occurs
Solution Approach 1:
A water-soluble additive serves as a simple intermediary component that prevents decomposition and precipitation of the active ingredient, achieving improved reliability without significantly increasing composition complexity
Solution Approach 2:
By optimizing the pH value to 3-9 and the additive concentration to 0.01-10% by mass, the composition achieves enhanced stability with minimal complexity, as these parameter ranges cover most conventional pharmaceutical formulations
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 achieves improved chemical and physical stability, ensuring the compound remains effective for a longer duration without precipitation, thereby enhancing its practical use and therapeutic efficacy.
Implementation Method 1
Incorporating a water-soluble additive, such as a surfactant, cyclodextrin, or antioxidant, into the liquid composition enhances the stability of N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or its salts
Implementation Method 2
a water-soluble additive, such as a surfactant, cyclodextrin, or antioxidant
Implementation Method 3
the water-soluble additive is at least one selected from the group consisting of a surfactant, cyclodextrin or a cyclodextrin derivative, and an antioxidant
Data Source
AI summary
The present invention provides a composition which effectively enhances the stability of N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or a salt thereof in a liquid composition. More specifically, the present invention provides a liquid composition comprising N-(2-ethylsulfonylamino-5-trifluoromethyl-3-pyridyl)cyclohexanecarboxamide or a salt thereof, a water-soluble additive and water.