Amorphous Solid Dispersion with Low Polymer Content for Faster Disintegration
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Solution Overview
Problem
Conventional solid dispersions containing poorly water-soluble compounds require high polymer content, leading to prolonged disintegration times of the pharmaceutical compositions.
Innovation Solution
A solid dispersion comprising a substance with a molecular weight of 1,000 g/mol to 5,000 g/mol and a polymer ratio less than 1.0, with specific glass transition temperature relationships, ensuring excellent amorphous stability and reduced polymer content.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If the content of polymer is increased to ensure sufficient amorphous stability, then the amorphous stability is improved, but the disintegration time is prolonged
Solution Approach 1:
The invention changes the molecular weight parameter of the substance to be dispersed, specifically selecting compounds with molecular weights of 1,000 g/mol or more and 5,000 g/mol or less. This parameter change allows the substance to achieve sufficient amorphous stability with reduced polymer content, thereby resolving the contradiction between amorphous stability and disintegration time
Solution Approach 2:
The invention applies local quality by selecting specific substances with particular molecular weight characteristics (1,000-5,000 g/mol) to be dispersed in the polymer matrix. This localized selection of substances with appropriate molecular weights enables optimal amorphous stability while maintaining acceptable disintegration properties, without requiring excessive polymer content
2Loss of time
If the content of polymer is reduced, then the disintegration time is shortened, but the amorphous stability may be compromised
Solution Approach 1:
By changing the molecular weight parameter of the dispersed substance to fall within 1,000-5,000 g/mol, the invention enables reduced polymer content (ratio less than 1.0) while maintaining adequate amorphous stability. The specific molecular weight range provides the right balance between stability requirements and disintegration performance
Solution Approach 2:
The invention creates a composite material system consisting of a substance to be dispersed (with specific molecular weight 1,000-5,000 g/mol) and a polymer, where the ratio of polymer to substance is less than 1.0. This composite structure achieves both reduced disintegration time and maintained amorphous stability through the synergistic combination of appropriately selected 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 solution provides a solid dispersion with enhanced amorphous stability and reduced disintegration times, suitable for pharmaceutical compositions.
Implementation Method 1
a glass transition temperature of the substance to be dispersed and a glass transition temperature of the solid dispersion are different by 1°C or more
Data Source
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AI summary
The present invention relates to a solid dispersion comprising (1) a substance to be dispersed that has a molecular weight of 1,000 g/mol or more and 5,000 g/mol or less and is amorphous; and (2) a polymer, wherein a ratio of a total mass of the polymer to a total mass of the substance to be dispersed is less than 1.0, and the solid dispersion meets the following (I) or (II): (I) a glass transition temperature of the substance to be dispersed and a glass transition temperature of the solid dispersion are different by 1°C or more; (II) the glass transition temperature of the solid dispersion is 94.5% or more and 105.5% or less with respect to a value of Tga represented by the following formula (A); [Expression 1] Tga=WcWa×Tgc+WpWa×Tgp in the formula (A), Tgc represents the glass transition temperature of the substance to be dispersed, Tgp represents the glass transition temperature of the polymer, Wa represents the total mass of the solid dispersion, Wc represents the total mass of the substance to be dispersed contained in the solid dispersion, and Wp represents the total mass of the polymer contained in the solid dispersion, respectively.