Micronized Drug Dispersion in Hydrophilic Polymer Matrix
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Solution Overview
Problem
Developing a sustained release oral dosage form for highly water-soluble drugs with short half-lives and high doses is challenging due to rapid absorption and metabolism, leading to sharp concentration spikes and falls, necessitating multiple daily dosing, which is inconvenient and reduces patient compliance.
Innovation Solution
A pharmaceutical composition comprising a highly water-soluble, short half-life active agent micronized and dispersed in a hydrophilic polymer matrix, allowing for controlled release and achieving a high drug loading of over 50% of the total weight, suitable for once or twice daily administration, maintaining therapeutic levels for extended periods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional sustained release methods are used for highly water-soluble drugs, then the drug release is retarded, but the dosage unit size becomes too large to be easily swallowed
Solution Approach 1:
The patent changes the particle size parameter of the highly water-soluble drug by micronizing it to a fine particle size range (D90 ≤ 10 μm). This parameter change increases the surface area and improves the dispersion of drug particles within the matrix, allowing for more efficient use of space. Consequently, the dosage unit can be reduced in size while still incorporating sufficient drug and matrix materials to achieve the desired sustained release duration of 8-24 hours.
Solution Approach 2:
The patent creates a composite material system consisting of micronized highly water-soluble drug particles dispersed in a hydrophilic polymer matrix. This composite structure allows the fine drug particles to be uniformly distributed throughout the matrix, maximizing drug loading efficiency. The composite nature of the formulation enables both sustained release functionality and reduced dosage unit size, as the fine particles require less matrix material to achieve the same release profile compared to conventional particle sizes.
2Duration of action of moving object
If a large amount of inactive ingredients is used to provide sustained release property, then the sustained release effect is achieved, but the drug content percentage decreases
Solution Approach 1:
By micronizing the highly water-soluble drug to fine particles (D90 ≤ 10 μm), the patent increases the specific surface area of the drug particles. This parameter change allows for better interaction between the drug and the hydrophilic polymer matrix, improving the efficiency of the release control mechanism. As a result, less matrix material is required to achieve the same sustained release effect, thereby increasing the drug content percentage in the final dosage unit.
Solution Approach 2:
The patent utilizes the porous structure that forms during matrix tablet compression and dissolution. The fine micronized drug particles create a more uniform porous network within the hydrophilic polymer matrix, allowing for controlled water penetration and drug release. This porous structure enhances the release control efficiency, enabling sustained release with reduced amounts of inactive ingredients, thus increasing the drug content percentage.
3Quantity of substance
If the drug is highly water-soluble, then the drug dissolves readily, but the drug releases in a burst and is absorbed quickly
Solution Approach 1:
The patent changes the particle size parameter of the highly water-soluble drug by micronizing it to a fine particle size (D90 ≤ 10 μm). This parameter change, combined with dispersion in the hydrophilic polymer matrix, creates a more uniform distribution of drug particles throughout the dosage unit. The fine particles are embedded within the matrix structure, which controls their release by regulating water penetration and drug dissolution. This prevents the burst release phenomenon while maintaining the high water solubility advantage for complete drug dissolution.
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 provides sustained plasma levels of the active agent for 8-24 hours, reducing dosing frequency and improving patient compliance by maintaining therapeutic concentrations for longer periods compared to immediate release formulations.
Implementation Method 1
the drug is usually mixed with a gelling material, which upon contact with water can form a thick layer of gel that slows down the diffusion of the drug
Implementation Method 2
Both diffusion and erosion contribute to drug release
Data Source
AI summary
The present invention provides pharmaceutical compositions for controlled release of pharmaceutically active agents, especially those with a high water solubility, high dose, and/or short half-life. In addition, the present application provides methods for preparing and using such pharmaceutical compositions.