Solid Dosage Form Composition for Stability and Water Suspensibility
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Solution Overview
Problem
Existing pediatric anti-influenza preparations face challenges with poor stability, suspensibility in water, and fluidity, leading to issues like drug accumulation at the bottom of containers and hindered production.
Innovation Solution
A solid dosage form containing a polycyclic pyridone compound stabilized by alkali metal chlorides, organic acids, polyhydric alcohol esters, and fatty acid esters, along with sugar alcohols, sugars, water-soluble polymers, and inorganic substances, enhancing stability and suspensibility.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If conventional pediatric anti-influenza preparations are used, then the drug can be administered to children, but the preparation shows poor stability and suspensibility in water, causing drug accumulation at the bottom of containers
Solution Approach 1:
The patent uses a composite formulation containing the polycyclic pyridone compound combined with multiple excipients including sugar alcohols (maltitol, mannitol), sugars, water-soluble polymers, and inorganic substances. This composite material approach allows the preparation to maintain both stability and suspensibility by combining materials with complementary properties.
Solution Approach 2:
The patent optimizes the concentration ratios of various components in the formulation. Specifically, it controls the content of sugar alcohols and sugars at 5-50 mass%, water-soluble polymers at 1-20 mass%, and inorganic substances at 1-10 mass% relative to the active ingredient. These parameter changes enable the preparation to achieve both stability and good suspensibility.
2Reliability
If the drug concentration in the preparation is lowered for pediatric use, then the preparation is safer for children, but the amount of related substances increases during temporal stability tests
Solution Approach 1:
The patent carefully controls the concentration of the polycyclic pyridone compound within specific ranges (0.1-10 mass%) while adjusting the concentrations of stabilizing excipients. This parameter optimization ensures that even at low drug concentrations suitable for pediatric use, the amount of related substances generated during stability tests remains minimal.
Solution Approach 2:
The patent introduces sugar alcohols, sugars, and water-soluble polymers as intermediary substances that stabilize the polycyclic pyridone compound. These intermediaries prevent degradation reactions, thereby reducing the formation of related substances while maintaining low drug concentrations safe for children.
3Ease of manufacture
If the fluidity of dry syrup or fine granule is improved for production, then manufacturing becomes easier, but the suspensibility in water may be compromised
Solution Approach 1:
The patent applies different functional excipients to different aspects of the formulation: inorganic substances (light anhydrous silicic acid, talc) are added specifically to improve fluidity for manufacturing, while sugar alcohols, sugars, and water-soluble polymers are used to ensure suspensibility in water. This local quality approach allows each component to optimize a specific property without compromising others.
Solution Approach 2:
The formulation combines materials with different functional properties: inorganic substances provide fluidity and prevent caking, while hydrophilic polymers and sugar alcohols provide suspensibility. This composite material strategy enables the preparation to meet both manufacturing and usage requirements simultaneously.
Data Source
AI summary
The present invention provides a solid dosage form having good stability, suspensibility in water and fluidity by preparing a solid dosage form containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a stabilizer, a sugar alcohol and/or a sugar, a water-soluble polymer and an inorganic substance.