PVA Resin Solid Dispersion for Drug Release and Coloration
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Solution Overview
Problem
Existing bases for solid dispersion, particularly those using PVA-based resins, are insufficient in terms of drug release rate and tend to cause coloration issues, limiting their bioavailability and effectiveness.
Innovation Solution
A PVA-based resin with a carboxylic acid metal salt content of 0.8% by weight or less, combined with a saponification degree of 80-95% and an average degree of polymerization of 200-2,500, is used as a base for solid dispersion, which is melt-kneaded with a drug to enhance drug release and reduce coloration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a PVA-based resin with high carboxylic acid metal salt content is used as a base for solid dispersion, then the resin provides good stability and processability, but the drug release rate is insufficient and coloration occurs
Solution Approach 1:
The patent applies parameter changes by precisely controlling the carboxylic acid metal salt content to 0.8% by weight or less, saponification degree to 80-95% by mole, and average degree of polymerization to 200-2,500. This optimization of chemical parameters resolves the contradiction by achieving both stability (through controlled salt content) and high drug release rate (through optimized saponification degree and polymerization level).
Solution Approach 2:
The patent extracts and removes the harmful component (carboxylic acid metal salt) from the PVA-based resin to a minimal level (0.8% by weight or less). By taking out the excess salt content that causes coloration and reduces drug release rate, the invention achieves both stability (retaining necessary salt for processability) and high productivity (improved drug release rate).
2Strength
If a PVA-based resin with high carboxylic acid metal salt content is used as a base for solid dispersion, then the resin maintains structural integrity, but coloration issues occur
Solution Approach 1:
The patent changes the chemical parameter of carboxylic acid metal salt content to 0.8% by weight or less, which eliminates coloration while preserving structural integrity. The controlled salt content maintains necessary intermolecular interactions for structural stability without causing the harmful coloration effect.
Solution Approach 2:
The patent extracts and removes the carboxylic acid metal salt component to a minimal level (0.8% by weight or less), thereby eliminating the coloration harmful factor while retaining sufficient structural integrity through the remaining salt content and optimized polymer properties.
3Ease of manufacture
If conventional PVA-based resins are used for solid dispersion, then manufacturing is simplified, but bioavailability is limited
Solution Approach 1:
The patent applies parameter changes by optimizing the saponification degree (80-95% by mole) and average degree of polymerization (200-2,500) of the PVA-based resin. These parameter optimizations improve drug release rate and bioavailability while maintaining the simplicity of the manufacturing process, as the resin can still be processed using conventional methods.
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
This approach results in a solid dispersion with improved drug release rates and increased bioavailability, while minimizing coloration, thus enhancing the absorption of active ingredients by the body.
Implementation Method 1
solid dispersion having an excellent drug release rate can be obtained by using, as a base for solid dispersion, a PVA-based resin containing only a slight amount of a carboxylic acid metal salt
Implementation Method 2
a method for producing solid dispersion, comprising melt-kneading a mixture of the base for solid dispersion as defined above and a drug, and then cooling the mixture
Implementation Method 3
melt-kneading a mixture of the base for solid dispersion as defined above and a drug, and then cooling the mixture
Data Source
AI summary
[Problem] To provide a base for solid dispersion which is excellent in drug release rate and has less coloration. [Means for Solution] A base for solid dispersion, comprising a polyvinyl alcohol-based resin with a carboxylic acid metal salt content of 0.8% by weight or less.